Fluorine in pharmaceutical industry: fluorine-containing drugs introduced to the market in the last decade (2001-2011).

Introduced to the Market in the Last Decade (2001−2011) Jiang Wang,† María Sańchez-Rosello,́‡,§ Jose ́ Luis Aceña, Carlos del Pozo,‡ Alexander E. Sorochinsky, Santos Fustero,*,‡,§ Vadim A. Soloshonok,* and Hong Liu*,† †Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China ‡Department of Organic Chemistry, Faculty of Pharmacy, University of Valencia, Av. Vicente Andreś Estelleś, 46100 Burjassot, Valencia, Spain Laboratorio de Molećulas Orgańicas, Centro de Investigacioń Príncipe Felipe, C/ Eduardo Primo Yuf́era 3, 46012 Valencia, Spain Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizab́al 3, 20018 San Sebastian, Spain IKERBASQUE, Basque Foundation for Science, Alameda Urquijo, 36-5 Plaza Bizkaia, 48011 Bilbao, Spain Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Murmanska Street 1, 02660 Kyiv-94, Ukraine

[1]  Alicja Wzorek,et al.  Optical purifications via self-disproportionation of enantiomers by achiral chromatography: case study of a series of α-CF3-containing secondary alcohols. , 2013, Chirality.

[2]  I. Ojima Exploration of fluorine chemistry at the multidisciplinary interface of chemistry and biology. , 2013, The Journal of organic chemistry.

[3]  K. Turcheniuk,et al.  Recent advances in the synthesis of fluorinated aminophosphonates and aminophosphonic acids , 2013 .

[4]  Steven V Ley,et al.  The synthesis of Bcr-Abl inhibiting anticancer pharmaceutical agents imatinib, nilotinib and dasatinib. , 2013, Organic & biomolecular chemistry.

[5]  H. Agarwal,et al.  Emtricitabine prodrugs with improved anti-HIV activity and cellular uptake. , 2013, Molecular pharmaceutics.

[6]  V. Soloshonok,et al.  Unconventional preparation of racemic crystals of isopropyl 3,3,3-trifluoro-2-hydroxypropanoate and their unusual crystallographic structure: the ultimate preference for homochiral intermolecular interactions. , 2013, Chemical communications.

[7]  Qiang Huang,et al.  The Manufacture of a Homochiral 4-Silyloxycyclopentenone Intermediate for the Synthesis of Prostaglandin Analogues , 2012 .

[8]  Vadim A. Soloshonok,et al.  Self-Disproportionation of Enantiomers of Chiral, Non-Racemic Fluoroorganic Compounds: Role of Fluorine as Enabling Element , 2012 .

[9]  Jian-qi Li,et al.  A New Route to Roflumilast via Copper-Catalyzed Hydroxylation , 2012 .

[10]  P. Brousset,et al.  Anaplastic lymphoma kinase as a therapeutic target , 2012, Expert opinion on therapeutic targets.

[11]  F. Liu,et al.  Efficient synthesis of prasugrel, a novel P2Y12 receptor inhibitor , 2012 .

[12]  N. Girard Crizotinib in ALK-positive lung cancer. , 2012, The Lancet. Oncology.

[13]  N. Tewari,et al.  A Novel Method for the Large Scale Synthesis of Cinacalcet Hydrochloride Using Iron Catalyzed C–C Coupling , 2012 .

[14]  Zheng Wang,et al.  Aromatic spiroketal bisphosphine ligands: palladium-catalyzed asymmetric allylic amination of racemic Morita-Baylis-Hillman adducts. , 2012, Angewandte Chemie.

[15]  P. Dubey,et al.  A novel asymmetric synthesis of cinacalcet hydrochloride , 2012, Beilstein journal of organic chemistry.

[16]  H. Manning,et al.  Rapid, Microwave-Assisted Organic Synthesis of Selective (V600E)BRAF Inhibitors for Preclinical Cancer Research. , 2012, Tetrahedron letters.

[17]  Claire Henchcliffe,et al.  Biomarkers in Parkinson's disease: an update. , 2012, Current opinion in neurology.

[18]  A. McDonagh,et al.  Synthesis of unsymmetrical biaryl ureas from N-carbamoylimidazoles: kinetics and application , 2012 .

[19]  Haichun Liu,et al.  Design, synthesis and biological evaluation of β-carboline derivatives as novel inhibitors targeting B-Raf kinase. , 2012, Bioorganic & medicinal chemistry letters.

[20]  Z. Tothova,et al.  Anaplastic lymphoma kinase-directed therapy in inflammatory myofibroblastic tumors , 2012, Current opinion in oncology.

[21]  M. Muñoz,et al.  NK-1 receptor antagonists as antitumor drugs: a survey of the literature from 2000 to 2011 , 2012, Expert opinion on therapeutic patents.

[22]  K. Nishio,et al.  Antitumor Action of the MET Tyrosine Kinase Inhibitor Crizotinib (PF-02341066) in Gastric Cancer Positive for MET Amplification , 2012, Molecular Cancer Therapeutics.

[23]  L. Citrome Oral paliperidone extended-release: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability , 2012, Expert opinion on drug metabolism & toxicology.

[24]  L. Mologni Inhibitors of the anaplastic lymphoma kinase , 2012, Expert opinion on investigational drugs.

[25]  J. E. Thomson,et al.  Asymmetric synthesis of (−)-(R)-sitagliptin , 2012 .

[26]  T. Jamison,et al.  Rapid continuous synthesis of 5'-deoxyribonucleosides in flow via Brønsted acid catalyzed glycosylation. , 2012, Organic letters.

[27]  Luyong Zhang,et al.  Synthesis and biological evaluation of ticagrelor derivatives as novel antiplatelet agents. , 2012, Bioorganic & medicinal chemistry letters.

[28]  V. Soloshonok,et al.  Recent Advances in the Asymmetric Synthesis of α‐(Trifluoromethyl)‐Containing α‐Amino Acids , 2012 .

[29]  Domenico Spina,et al.  Selective PDE inhibitors as novel treatments for respiratory diseases. , 2012, Current opinion in pharmacology.

[30]  C. Roussel,et al.  Self-disproportionation of enantiomers via achiral chromatography: a warning and an extra dimension in optical purifications. , 2012, Chemical Society reviews.

[31]  J. Cossy,et al.  Synthesis of Amines from Alcohols in a Nonepimerizing One‐Pot Sequence – Synthesis of Bioactive Compounds: Cinacalcet and Dexoxadrol , 2012 .

[32]  A. Rossi,et al.  The emerging role of ALK inhibitors in the treatment of advanced non-small cell lung cancer , 2012, Expert opinion on therapeutic targets.

[33]  P. Patsalos,et al.  Pharmacotherapy of the third-generation AEDs: lacosamide, retigabine and eslicarbazepine acetate , 2012, Expert opinion on pharmacotherapy.

[34]  R. Rizzo,et al.  A water-based mechanism of specificity and resistance for lapatinib with ErbB family kinases. , 2012, Biochemistry.

[35]  H. Agarwal,et al.  Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors. , 2012, Journal of medicinal chemistry.

[36]  M. Jukič,et al.  Concise and highly efficient approach to three key pyrimidine precursors for rosuvastatin synthesis , 2012 .

[37]  E. Spina,et al.  Interactions between antiepileptics and second-generation antipsychotics , 2012, Expert opinion on drug metabolism & toxicology.

[38]  J. Herrstedt,et al.  Fosaprepitant for the prevention of chemotherapy-induced nausea and vomiting , 2012, Expert review of anticancer therapy.

[39]  Dattatray S. Metil,et al.  Process Improvements of Prasugrel Hydrochloride: An Adenosine Diphosphate Receptor Antagonist , 2012 .

[40]  S. Buchwald,et al.  Completely N1-selective palladium-catalyzed arylation of unsymmetric imidazoles: application to the synthesis of nilotinib. , 2012, Journal of the American Chemical Society.

[41]  S. Rennard,et al.  PDE4: A Novel Target in the Treatment of Chronic Obstructive Pulmonary Disease , 2012, Clinical pharmacology and therapeutics.

[42]  S. Benbadis,et al.  The use of newer antiepileptic drugs in patients with renal failure , 2012, Expert review of neurotherapeutics.

[43]  Stephen P. Thomas,et al.  Enantioenriched synthesis of Escitalopram using lithiation-borylation methodology , 2011 .

[44]  G. Carter,et al.  Natural products and Pharma 2011: strategic changes spur new opportunities. , 2011, Natural product reports.

[45]  A. D’Incecco,et al.  Gefitinib for non-small-cell lung cancer treatment , 2011, Expert opinion on drug safety.

[46]  V. Matoušek,et al.  Synthesis of α-CF3-substituted carbonyl compounds with relative and absolute stereocontrol using electrophilic CF3-transfer reagents. , 2011, Organic letters.

[47]  I. Okamoto,et al.  MET Tyrosine Kinase Inhibitor Crizotinib (PF-02341066) Shows Differential Antitumor Effects in Non-small Cell Lung Cancer According to MET Alterations , 2011, Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer.

[48]  J. Davies First-line therapy for CML: nilotinib comes of age. , 2011, The Lancet. Oncology.

[49]  Y. Bodke,et al.  Diastereoselective Reduction of the Enone Intermediate of Travoprost , 2011 .

[50]  J. Christensen,et al.  Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). , 2011, Journal of medicinal chemistry.

[51]  D. Blackmond,et al.  Innate C-H trifluoromethylation of heterocycles , 2011, Proceedings of the National Academy of Sciences.

[52]  A. Waterson,et al.  Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. , 2011, Bioorganic & medicinal chemistry letters.

[53]  H. Xiang,et al.  A review on steroidal 5α-reductase inhibitors for treatment of benign prostatic hyperplasia. , 2011, Current medicinal chemistry.

[54]  M. Chmielewski,et al.  A formal synthesis of ezetimibe via cycloaddition/rearrangement cascade reaction. , 2011, The Journal of organic chemistry.

[55]  G. Griffiths,et al.  A first synthesis of 18F‐radiolabeled lapatinib: a potential tracer for positron emission tomographic imaging of ErbB1/ErbB2 tyrosine kinase activity , 2011 .

[56]  A. Kamatani,et al.  Fit-for-Purpose Development of the Enabling Route to Crizotinib (PF-02341066) , 2011 .

[57]  E. Donnenfeld Difluprednate for the prevention of ocular inflammation postsurgery: an update , 2011, Clinical ophthalmology.

[58]  F. Qing,et al.  Recent Advances in the Synthesis of Fluorinated Amino Acids , 2011 .

[59]  T. Ritter,et al.  Catalysis for fluorination and trifluoromethylation , 2011, Nature.

[60]  P. Sharma,et al.  Advances in synthetic approach to and antifungal activity of triazoles , 2011, Beilstein journal of organic chemistry.

[61]  E. Deeks Ticagrelor , 2011, Drugs.

[62]  E. Faught Ezogabine: A New Angle on Potassium Gates , 2011, Epilepsy currents.

[63]  S. Buchwald,et al.  Synthesis of unsymmetrical diarylureas via Pd-catalyzed C-N cross-coupling reactions. , 2011, Organic letters.

[64]  P. Dubey,et al.  Synthesis of (±) Travoprost and its Analogs , 2011 .

[65]  C. Foster,et al.  Difluprednate for inflammatory eye disorders. , 2011, Drugs of today.

[66]  K. Huber,et al.  Fresh from the pipeline. Ticagrelor. , 2011, Nature reviews. Drug discovery.

[67]  V. Grushin,et al.  Aromatic trifluoromethylation with metal complexes. , 2011, Chemical reviews.

[68]  F. Musumeci,et al.  Selective Chemical Oxidation of Risperidone: A Straightforward and Cost-Effective Synthesis of Paliperidone , 2011 .

[69]  Donna J. Nelson,et al.  Self-Disproportionation of Enantiomers via Sublimation; New and Truly Green Dimension in Optical Purification , 2011 .

[70]  Jianlin Han,et al.  Biomimetic Transamination – a Metal-Free Alternative to the Reductive Amination. Application for Generalized Preparation of Fluorine-Containing Amines and Amino Acids , 2011 .

[71]  Zdenko Časar,et al.  Application of Chemoselective Pancreatin Powder-Catalyzed Deacetylation Reaction in the Synthesis of Key Statin Side Chain Intermediate (4R,6S)-4-(tert-Butyldimethylsilyloxy)-6-(hydroxymethyl)tetrahydropyran-2-one , 2011 .

[72]  S. Kelleher,et al.  An investigation into the one-pot Heck olefination-hydrogenation reaction. , 2011, The Journal of organic chemistry.

[73]  Aman A Desai,et al.  Sitagliptin manufacture: a compelling tale of green chemistry, process intensification, and industrial asymmetric catalysis. , 2011, Angewandte Chemie.

[74]  Suhas P. Deshmukh,et al.  Industrial Application of the Forster Reaction: Novel One-Pot Synthesis of Cinacalcet Hydrochloride, a Calcimimetic Agent , 2011 .

[75]  M. Cattaneo The platelet P2Y₁₂ receptor for adenosine diphosphate: congenital and drug-induced defects. , 2011, Blood.

[76]  Jun‐An Ma,et al.  Asymmetric construction of stereogenic carbon centers featuring a trifluoromethyl group from prochiral trifluoromethylated substrates. , 2011, Chemical reviews.

[77]  Laith Q Al-Mawsawi,et al.  Allosteric Inhibitor Development Targeting HIV‐1 Integrase , 2011, ChemMedChem.

[78]  P. Schwerdtfeger,et al.  Theoretical investigations into the enantiomeric and racemic forms of α-(trifluoromethyl)lactic acid. , 2011, Physical chemistry chemical physics : PCCP.

[79]  Yong-Li Zhong,et al.  Development of a Second-Generation, Highly Efficient Manufacturing Route for the HIV Integrase Inhibitor Raltegravir Potassium , 2011 .

[80]  S. Melotto,et al.  Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate. , 2011, Journal of medicinal chemistry.

[81]  A. Palyzová,et al.  Diastereoselective reduction of 1-(4-fluorophenyl)-3(R)-[3-oxo-3-(4-fluorophenyl)-propyl]-4(S)-(4-hydroxyphenyl)azetidin-2-one to Ezetimibe by the whole cell catalyst Rhodococcus fascians MO22 , 2010 .

[82]  T. Beckers,et al.  Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity. , 2010, Journal of medicinal chemistry.

[83]  Pradeep Kumar,et al.  An organocatalytic route to the synthesis of lactone moiety of compactin and mevinolin , 2010 .

[84]  D. O'Hagan Fluorine in health care: Organofluorine containing blockbuster drugs , 2010 .

[85]  Nikolaus Stiefl,et al.  Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. , 2010, Bioorganic & medicinal chemistry.

[86]  Kam Y. J. Zhang,et al.  Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma , 2010, Nature.

[87]  A. Córdova,et al.  Asymmetric Synthesis of Maraviroc (UK-427,857) , 2010 .

[88]  Zdenko Časar,et al.  Lactone pathway to statins utilizing the Wittig reaction. The synthesis of rosuvastatin. , 2010, The Journal of organic chemistry.

[89]  J. Javitch,et al.  Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile) analogues at monoamine transporters. , 2010, Journal of medicinal chemistry.

[90]  Christopher Hulme,et al.  The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. , 2010, Bioorganic & medicinal chemistry.

[91]  Lyn Powell,et al.  Development of a Catalytic Cuprate 1,6-Conjugate Dienone Addition Process for the Manufacture of Fulvestrant EAS, a Key Intermediate in the Synthesis of Fulvestrant , 2010 .

[92]  P. Janicak,et al.  Iloperidone for schizophrenia , 2010, Expert opinion on pharmacotherapy.

[93]  Paul N. Devine,et al.  Biocatalytic Asymmetric Synthesis of Chiral Amines from Ketones Applied to Sitagliptin Manufacture , 2010, Science.

[94]  R. Bandichhor,et al.  Synthesis of All Enantiomerically Pure Diastereomers of Aprepitant , 2010 .

[95]  D. Heimbrook,et al.  RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. , 2010, Cancer research.

[96]  Anthony E. Klon,et al.  SU11248 (sunitinib) directly inhibits the activity of mammalian 5'-AMP-activated protein kinase (AMPK) , 2010, Cancer biology & therapy.

[97]  V. Soloshonok,et al.  Rational application of self-disproportionation of enantiomers via sublimation—a novel methodological dimension for enantiomeric purifications , 2010 .

[98]  Whitney H. Mudd,et al.  An efficient synthesis of rufinamide, an antiepileptic drug , 2010 .

[99]  S. Buchwald,et al.  The Palladium-Catalyzed Trifluoromethylation of Aryl Chlorides , 2010, Science.

[100]  A. Börner,et al.  Highly stereoselective hydrogenations--as key-steps in the total synthesis of statins. , 2010, Chirality.

[101]  Katherine C. Wu,et al.  Review: Update on Newer Antihypertensive Medicines and Interventions , 2010, Journal of cardiovascular pharmacology and therapeutics.

[102]  S. Yamazaki,et al.  Gender specific drug metabolism of PF-02341066 in rats--role of sulfoconjugation. , 2010, Current drug metabolism.

[103]  Vadim A. Soloshonok,et al.  Self-disproportionation of enantiomers of α-trifluoromethyl lactic acid amides via sublimation , 2010 .

[104]  Xiaoke Wang,et al.  The Asymmetric Synthesis of Sitagliptin, a Selective Dipeptidyl Peptidase IV Inhibitor for the Treatment of type 2 diabetes , 2010 .

[105]  Martin A. Suhm,et al.  Chirality-dependent sublimation of α-(trifluoromethyl)-lactic acid: Relative vapor pressures of racemic, eutectic, and enantiomerically pure forms, and vibrational spectroscopy of isolated (S,S) and (S,R) dimers , 2010 .

[106]  T. Schacker New tools to track HIV , 2010, Nature Medicine.

[107]  Etsuko Tokunaga,et al.  Self-disproportionation of enantiomers of heterocyclic compounds having a tertiary trifluoromethyl alcohol center on chromatography with a non-chiral system , 2010 .

[108]  Vadim A. Soloshonok,et al.  Self-disproportionation of enantiomers of isopropyl 3,3,3-(trifluoro)lactate via sublimation: Sublimation rates vs. enantiomeric composition , 2010 .

[109]  T. Morris,et al.  Besifloxacin: a novel anti-infective for the treatment of bacterial conjunctivitis , 2010, Clinical ophthalmology.

[110]  Lyn Powell,et al.  Fulvestrant: From the Laboratory to Commercial-Scale Manufacture , 2010 .

[111]  A. Nobili,et al.  New atypical antipsychotics for schizophrenia: iloperidone , 2010, Drug design, development and therapy.

[112]  Saurabh Aggarwal,et al.  An overview on 5α-reductase inhibitors , 2010, Steroids.

[113]  Vadim A. Soloshonok,et al.  Self disproportionation of enantiomers of 3,3,3-trifluorolactic acid amides via sublimation , 2010 .

[114]  V. Soloshonok,et al.  Asymmetric synthesis of fluorine-containing amines, amino alcohols, α- and β-amino acids mediated by chiral sulfinyl group , 2010 .

[115]  P. Dobesh Clopidogrel versus Prasugrel: Times Are Changing, but Not for Everyone , 2009, Pharmacotherapy.

[116]  O. Taboureau,et al.  Mutational Mapping and Modeling of the Binding Site for (S)-Citalopram in the Human Serotonin Transporter* , 2009, The Journal of Biological Chemistry.

[117]  Jinzhong Zhang,et al.  Besifloxacin, a new ophthalmic fluoroquinolone for the treatment of bacterial conjunctivitis , 2009, Expert opinion on pharmacotherapy.

[118]  G. Keating,et al.  Prasugrel , 2009, Drugs.

[119]  V. Soloshonok,et al.  Practical synthesis of fluorine-containing α- and β-amino acids: recipes from Kiev, Ukraine. , 2009, Future medicinal chemistry.

[120]  P. Dubey,et al.  An Improved and Scalable Process for the Synthesis of Ezetimibe: An Antihypercholesterolemia Drug , 2009 .

[121]  N. Shibata,et al.  Catalytic enantioselective trifluoromethylation of azomethine imines with trimethyl(trifluoromethyl)silane. , 2009, Angewandte Chemie.

[122]  M. Rowley,et al.  N-(4-Fluorobenzyl)-3-hydroxy-9,9-dimethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrazino[1,2-a]pyrimidine-2-carboxamides a novel class of potent HIV-1 integrase inhibitors. , 2009, Bioorganic & medicinal chemistry letters.

[123]  Mark E. Scott,et al.  Enantioselective alpha-trifluoromethylation of aldehydes via photoredox organocatalysis. , 2009, Journal of the American Chemical Society.

[124]  Zhe-Sheng Chen,et al.  Nilotinib (AMN107, Tasigna) reverses multidrug resistance by inhibiting the activity of the ABCB1/Pgp and ABCG2/BCRP/MXR transporters. , 2009, Biochemical pharmacology.

[125]  L. Scott,et al.  Lubiprostone , 2009, Drugs.

[126]  R. Beaudegnies,et al.  Herbicidal 4-hydroxyphenylpyruvate dioxygenase inhibitors--a review of the triketone chemistry story from a Syngenta perspective. , 2009, Bioorganic & medicinal chemistry.

[127]  Feng Xu,et al.  Highly efficient asymmetric synthesis of sitagliptin. , 2009, Journal of the American Chemical Society.

[128]  T. Morris,et al.  Besifloxacin, a Novel Fluoroquinolone, Has Broad-Spectrum In Vitro Activity against Aerobic and Anaerobic Bacteria , 2009, Antimicrobial Agents and Chemotherapy.

[129]  A. Wickenden,et al.  Kv7 channels as targets for the treatment of pain. , 2009, Current pharmaceutical design.

[130]  H. Senn,et al.  The fluorine-iminium ion gauche effect: proof of principle and application to asymmetric organocatalysis. , 2009, Angewandte Chemie.

[131]  R. DeVita,et al.  Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. , 2009, Journal of medicinal chemistry.

[132]  I. Ojima Fluorine in medicinal chemistry and chemical biology , 2009 .

[133]  N. Normanno,et al.  Vandetanib (ZD6474), a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and epidermal growth factor receptor (EGFR) tyrosine kinases: current status and future directions. , 2009, The oncologist.

[134]  R. Salgia,et al.  The MET axis as a therapeutic target. , 2009, Update on cancer therapeutics.

[135]  Zdenko Časar,et al.  The First Convenient Entryto δ-Formyl-δ-valerolactone Precursor for the Synthesisof Statins via Lactonized Side Chain , 2009 .

[136]  S. Rusconi Tipranavir: a novel protease inhibitor for HIV therapy , 2009, Expert review of clinical pharmacology.

[137]  G. Leclercq,et al.  Effect of fluorination on the pharmacological profile of 11beta isomers of fulvestrant in breast carcinoma cells. , 2009, Journal of medicinal chemistry.

[138]  V. Serebruany,et al.  Prasugrel development – Claims and achievements , 2008, Thrombosis and Haemostasis.

[139]  J. Ahman,et al.  Process Research and Scale-up of a Commercialisable Route to Maraviroc (UK-427,857), a CCR-5 Receptor Antagonist , 2008 .

[140]  J. Ahman,et al.  Development of a Bulk Enabling Route to Maraviroc (UK-427,857), a CCR-5 Receptor Antagonist , 2008 .

[141]  M. Millan,et al.  Cellular and behavioural profile of the novel, selective neurokinin1 receptor antagonist, vestipitant: A comparison to other agents , 2008, European Neuropsychopharmacology.

[142]  J. Llovet,et al.  Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling , 2008, Molecular Cancer Therapeutics.

[143]  D. Hazuda,et al.  Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. , 2008, Journal of medicinal chemistry.

[144]  H. M. Wright,et al.  Nebivolol: a highly selective beta1-adrenergic receptor blocker that causes vasodilation by increasing nitric oxide. , 2008, Cardiovascular therapeutics.

[145]  David A. Price,et al.  Overcoming hERG affinity in the discovery of maraviroc; a CCR5 antagonist for the treatment of HIV. , 2008, Current topics in medicinal chemistry.

[146]  V. Kouloulias,et al.  Efficacy of the Oral Fluorouracil Pro-drug Capecitabine in Cancer Treatment: a Review , 2008, Molecules.

[147]  Zdenko Časar Straightforward and EfficientSynthesis of (4R,6S)-4-(tert-Butyldimethyl­siloxy)-6-(hydroxymethyl)tetrahydropyran-2-one , 2008 .

[148]  M. Meegan,et al.  Recent developments in the design of anti-depressive therapies: targeting the serotonin transporter. , 2008, Current medicinal chemistry.

[149]  W. Hagmann,et al.  The many roles for fluorine in medicinal chemistry. , 2008, Journal of medicinal chemistry.

[150]  K. Houk,et al.  A polar radical pair pathway to assemble the pyrimidinone core of the HIV integrase inhibitor raltegravir potassium. , 2008, Angewandte Chemie.

[151]  M. Yadav,et al.  Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents. , 2008, Bioorganic & medicinal chemistry.

[152]  Jacob Andersen,et al.  From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: synthesis and structure-activity relationship studies. , 2008, Journal of medicinal chemistry.

[153]  Gloria Hernández-Torres,et al.  Sulfoxide‐Directed Stereocontrolled Access to 2H‐Chromans: Total Synthesis of the (S,R,R,R)‐Enantiomer of the Antihypertensive Drug Nebivolol , 2008 .

[154]  Gopinathenpillai Bijukumar,et al.  Efficient Synthesis of Cinacalcet Hydrochloride , 2008 .

[155]  A. Cleton,et al.  Absorption, Metabolism, and Excretion of Paliperidone, a New Monoaminergic Antagonist, in Humans , 2008, Drug Metabolism and Disposition.

[156]  Kam Y. J. Zhang,et al.  Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity , 2008, Proceedings of the National Academy of Sciences.

[157]  A. Polyzos Activity of SU11248, a multitargeted inhibitor of vascular endothelial growth factor receptor and platelet-derived growth factor receptor, in patients with metastatic renal cell carcinoma and various other solid tumors , 2008, The Journal of Steroid Biochemistry and Molecular Biology.

[158]  A. Hänsicke,et al.  Stereochemical comparison of nebivolol with other β‐blockers , 2008 .

[159]  A. Börner,et al.  Highly Enantioselective Hydrogenation of Ethyl 5,5‐Dimethoxy‐3‐oxopentanoate and its Application for the Synthesis of a Statin Precursor , 2008 .

[160]  A. Börner,et al.  A New Approach to the Total Synthesis of Rosuvastatin , 2008 .

[161]  F. Kratz,et al.  Prodrug Strategies in Anticancer Chemotherapy , 2008, ChemMedChem.

[162]  S. Purser,et al.  Fluorine in medicinal chemistry. , 2008, Chemical Society reviews.

[163]  David O'Hagan,et al.  Understanding organofluorine chemistry. An introduction to the C-F bond. , 2008, Chemical Society reviews.

[164]  S. Schaus,et al.  Asymmetric allylboration of acyl imines catalyzed by chiral diols. , 2007, Journal of the American Chemical Society.

[165]  R. Bandichhor,et al.  A convergent approach to the synthesis of aprepitant: a potent human NK-1 receptor antagonist ☆ , 2007 .

[166]  P. Leeson,et al.  From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis. , 2007, Bioorganic & medicinal chemistry letters.

[167]  F. Diederich,et al.  Fluorine in Pharmaceuticals: Looking Beyond Intuition , 2007, Science.

[168]  R. DeVita,et al.  The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine. , 2007, Bioorganic & medicinal chemistry letters.

[169]  Manabu Yasumoto,et al.  Phenomenon of optical self-purification of chiral non-racemic compounds. , 2007, Journal of the American Chemical Society.

[170]  Michael Rowley,et al.  Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones. , 2007, Journal of medicinal chemistry.

[171]  G. Demetri,et al.  Molecular basis for sunitinib efficacy and future clinical development , 2007, Nature Reviews Drug Discovery.

[172]  Y. Anjaneyulu,et al.  Efficient Synthesis of (1R)‐[3,5‐Bis(trifluoromethyl)phenyl] Ethanol, a Key Intermediate for Aprepitant, an NK‐1 Receptor Antagonist , 2007 .

[173]  T. Lóránd,et al.  Recent advances in antifungal agents. , 2007, Mini reviews in medicinal chemistry.

[174]  K. Satyanarayana,et al.  A Scaleable Synthesis of Dutasteride: A Selective 5α-Reductase Inhibitor† , 2007 .

[175]  Manfred Kansy,et al.  Predicting and Tuning Physicochemical Properties in Lead Optimization: Amine Basicities , 2007, ChemMedChem.

[176]  V. Chandregowda,et al.  Convergent Approach for Commercial Synthesis of Gefitinib and Erlotinib , 2007 .

[177]  W. Shakespeare,et al.  An Efficient Synthesis of Nilotinib (AMN107) , 2007 .

[178]  Ángel García,et al.  A New and Efficient Synthesis of the HMG‐CoA Reductase Inhibitor Pitavastatin , 2007 .

[179]  F. Farowski,et al.  Posaconazole: a next-generation triazole antifungal. , 2007, Future microbiology.

[180]  V. T. Mathad,et al.  An Alternative Approach to Achieve Enantiopure (3S)-4-Benzyl-3- (4-fluorophenyl)morpholin-2-one: A Key Intermediate of Aprepitant, an NK1 Receptor Antagonist† , 2007 .

[181]  D. Hazuda,et al.  Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors. , 2007, Journal of medicinal chemistry.

[182]  S. Frein,et al.  Process for preparing Ezetimibe intermediate by enantioselective CBS catalyzed ketone reduction with BH3–DEA prepared in situ , 2007 .

[183]  Matthew Meyerson,et al.  Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. , 2007, Cancer cell.

[184]  V. T. Mathad,et al.  Substrate Modification Approach to Achieve Efficient Resolution: Didesmethylcitalopram: A Key Intermediate for Escitalopram# , 2007 .

[185]  U. Koch,et al.  From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety. , 2007, Bioorganic & medicinal chemistry letters.

[186]  M. Berger,et al.  Lapatinib plus capecitabine for HER2-positive advanced breast cancer. , 2006, The New England journal of medicine.

[187]  Xinzhi Chen,et al.  A mild synthesis of α,α′-[iminobismethylene]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] , 2006 .

[188]  H. Kantarjian,et al.  Activity of AMN107, a novel aminopyrimidine tyrosine kinase inhibitor, against human FIP1L1-PDGFR-alpha-expressing cells. , 2006, Leukemia research.

[189]  Ian Collins,et al.  New approaches to molecular cancer therapeutics , 2006, Nature chemical biology.

[190]  A. Börner,et al.  Synthesis of the Chiral Side Chain of Statins – Lactone versus Lactol Pathway , 2006 .

[191]  S. Wilhelm,et al.  Discovery and development of sorafenib: a multikinase inhibitor for treating cancer , 2006, Nature Reviews Drug Discovery.

[192]  G. Borgia,et al.  Treating chronic hepatitis B: today and tomorrow. , 2006, Current medicinal chemistry.

[193]  Yan Zhu,et al.  Nanostructural evolution of Zn by dry roller vibration milling at room temperature , 2006 .

[194]  J. Kendrew,et al.  Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics. , 2006, Bioorganic & medicinal chemistry letters.

[195]  Wang Junmoin,et al.  Synthesis and anticonvulsant activity of 1-substituted benzyl-N-substituted-1,2,3-trazoole-4-formamodes , 2006 .

[196]  David A. Price,et al.  Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc. , 2006, Bioorganic & medicinal chemistry letters.

[197]  K. Lackey,et al.  Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series. , 2006, Bioorganic & medicinal chemistry letters.

[198]  D. Bonnet-Delpon,et al.  Recent advances (1995–2005) in fluorinated pharmaceuticals based on natural products ☆ , 2006 .

[199]  P. Comoglio,et al.  The Met pathway: master switch and drug target in cancer progression , 2006, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[200]  K. Kirk,et al.  Fluorine in medicinal chemistry: Recent therapeutic applications of fluorinated small molecules , 2006 .

[201]  G. Sledge,et al.  Synthesis of [11C]Iressa as a new potential PET cancer imaging agent for epidermal growth factor receptor tyrosine kinase. , 2006, Bioorganic & medicinal chemistry letters.

[202]  N. Singewald,et al.  The role of substance P in stress and anxiety responses , 2006, Amino Acids.

[203]  S. Johnston,et al.  Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer. , 2006, Drugs of today.

[204]  J. Mestan,et al.  AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL , 2006, British Journal of Cancer.

[205]  Anandan Palani,et al.  Discovery and development of small-molecule chemokine coreceptor CCR5 antagonists. , 2006, Journal of medicinal chemistry.

[206]  A. Gryff-Keller,et al.  1H NMR, 13C NMR, and computational DFT studies of the structure of 2-acylcyclohexane-1,3-diones and their alkali metal salts in solution. , 2006, The Journal of organic chemistry.

[207]  V. Soloshonok,et al.  Self-disproportionation of enantiomers of (R)-ethyl 3-(3,5-dinitrobenzamido)-4,4,4-trifluorobutanoate on achiral silica gel stationary phase , 2006 .

[208]  G. Ruecroft,et al.  Immobilization of cholesterol esterase for use in multiple batch biotransformations to prepare (-)- FTC (emtricitabine) , 2006 .

[209]  D. O'Hagan,et al.  Fluorine in medicinal chemistry: A review of anti-cancer agents , 2006 .

[210]  N. Nagano Pharmacological and clinical properties of calcimimetics: calcium receptor activators that afford an innovative approach to controlling hyperparathyroidism. , 2006, Pharmacology & therapeutics.

[211]  K. Lackey Lessons from the drug discovery of lapatinib, a dual ErbB1/2 tyrosine kinase inhibitor. , 2006, Current topics in medicinal chemistry.

[212]  S. Frye Discovery and clinical development of dutasteride, a potent dual 5alpha-reductase inhibitor. , 2006, Current topics in medicinal chemistry.

[213]  Gayatry Mohapatra,et al.  Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752 , 2006, Proceedings of the National Academy of Sciences of the United States of America.

[214]  B. Shroot,et al.  The position not the presence of the halogen in corticosteroids influences potency and side effects. , 2006, Journal of drugs in dermatology : JDD.

[215]  V. Soloshonok,et al.  Remarkable amplification of the self-disproportionation of enantiomers on achiral-phase chromatography columns. , 2006, Angewandte Chemie.

[216]  David A. Price,et al.  Maraviroc (UK-427,857), a Potent, Orally Bioavailable, and Selective Small-Molecule Inhibitor of Chemokine Receptor CCR5 with Broad-Spectrum Anti-Human Immunodeficiency Virus Type 1 Activity , 2005, Antimicrobial Agents and Chemotherapy.

[217]  A. Olsson,et al.  Rosuvastatin is cost-effective compared with atorvastatin in reaching cholesterol goals. , 2005, International journal of cardiology.

[218]  G. Sledge,et al.  Synthesis of [18F]SU11248, a new potential PET tracer for imaging cancer tyrosine kinase. , 2005, Bioorganic & medicinal chemistry letters.

[219]  Makiko Yamamoto,et al.  Formulation of an ophthalmic lipid emulsion containing an anti-inflammatory steroidal drug, difluprednate. , 2005, International journal of pharmaceutics.

[220]  Edward J. J. Grabowski,et al.  First Generation Process for the Preparation of the DPP-IV Inhibitor Sitagliptin , 2005 .

[221]  J. Jakubowski,et al.  Stereoselective inhibition of human platelet aggregation by R-138727, the active metabolite of CS-747 (Prasugrel, LY640315), a novel P2Y12 receptor inhibitor , 2005, Thrombosis and Haemostasis.

[222]  David A. Price,et al.  Initial synthesis of UK-427,857 (Maraviroc) , 2005 .

[223]  J. Christensen,et al.  c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention. , 2005, Cancer letters.

[224]  E. A. Kovaleva,et al.  Competitive Formation of β-Amino Acids, Propenoic, and Ylidenemalonic Acids by the Rodionov Reaction from Malonic Acid, Aldehydes, and Ammonium Acetate in Alcoholic Medium , 2005 .

[225]  N. Culhane,et al.  Rosuvastatin for the Treatment of Hypercholesterolemia , 2005, Pharmacotherapy.

[226]  A. Ryan,et al.  ZD6474 – a novel inhibitor of VEGFR and EGFR tyrosine kinase activity , 2005, British Journal of Cancer.

[227]  Simon Gayton,et al.  A Practical Synthesis of Piperidine-/Tropane-Substituted 1,2,4-Triazoles , 2005 .

[228]  S. McLean Do substance P and the NK1 receptor have a role in depression and anxiety? , 2005, Current pharmaceutical design.

[229]  J. Molina,et al.  Emtricitabine: a novel nucleoside reverse transcriptase inhibitor. , 2005, Drugs of today.

[230]  J. Christensen,et al.  A Selective Small Molecule c-MET Inhibitor, PHA665752, Cooperates with Rapamycin , 2005, Clinical Cancer Research.

[231]  R. Carletti,et al.  Down‐regulation of amygdala preprotachykinin A mRNA but not 3H‐SP receptor binding sites in subjects affected by mood disorders and schizophrenia , 2005, The European journal of neuroscience.

[232]  J. Armstrong,et al.  Synthesis of [1,2,4]Triazolo[4,3-α]piperazines via Highly Reactive Chloromethyloxadiazoles , 2005 .

[233]  Donna Neuberg,et al.  Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. , 2005, Cancer cell.

[234]  L. Mitscher Bacterial topoisomerase inhibitors: quinolone and pyridone antibacterial agents. , 2005, Chemical reviews.

[235]  G. Scapin,et al.  (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. , 2005, Journal of medicinal chemistry.

[236]  B. Lipworth Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease , 2005, The Lancet.

[237]  Michael Müller,et al.  Chemoenzymatic synthesis of building blocks for statin side chains. , 2005, Angewandte Chemie.

[238]  M. Huffman,et al.  Syntheses of morpholine-2,3-diones and 2-hydroxymorpholin-3-ones: intermediates in the synthesis of aprepitant , 2004 .

[239]  V. Soloshonok,et al.  Synthesis of fluorine-containing compounds under operationally convenient conditions , 2004 .

[240]  D. Auclair,et al.  BAY 43-9006 Exhibits Broad Spectrum Oral Antitumor Activity and Targets the RAF/MEK/ERK Pathway and Receptor Tyrosine Kinases Involved in Tumor Progression and Angiogenesis , 2004, Cancer Research.

[241]  G. Gribble Natural Organohalogens: A New Frontier for Medicinal Agents?. , 2004 .

[242]  Krystal J Alligood,et al.  A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib) , 2004, Cancer Research.

[243]  Judy W. M. Cheng Rosuvastatin in the management of hyperlipidemia. , 2004, Clinical therapeutics.

[244]  Daniel A. Haber,et al.  Gefitinib-Sensitizing EGFR Mutations in Lung Cancer Activate Anti-Apoptotic Pathways , 2004, Science.

[245]  R. Herbrecht Voriconazole: therapeutic review of a new azole antifungal , 2004, Expert review of anti-infective therapy.

[246]  P. Connett,et al.  Fluorine in medicine , 2004 .

[247]  H. Burris,et al.  Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. , 2004, The oncologist.

[248]  K. Bogeso,et al.  Escitalopram versus citalopram: the surprising role of the R-enantiomer , 2004, Psychopharmacology.

[249]  Martin Stahl,et al.  Fluorine in Medicinal Chemistry , 2004, Chembiochem : a European journal of chemical biology.

[250]  M. Nelson,et al.  Emtricitabine (FTC) for the treatment of HIV infection , 2004, International journal of clinical practice.

[251]  P. Ramachandran,et al.  Relationship between the structure and enantioselectivity in the asymmetric reduction of 2′,6′-disubstituted acetophenones with DIP-ChlorideTM. An ab initio study , 2004 .

[252]  D. Cai,et al.  Dimethyltitanocene: From Millimole to Kilomole , 2004 .

[253]  C. Roehrborn,et al.  α1-Adrenergic Receptors and Their Inhibitors in Lower Urinary Tract Symptoms and Benign Prostatic Hyperplasia , 2004 .

[254]  C. Zhan,et al.  Hydration of the Fluoride Anion: Structures and Absolute Hydration Free Energy from First-Principles Electronic Structure Calculations , 2004 .

[255]  R. Pazdur,et al.  United States Food and Drug Administration Drug Approval Summary , 2004, Clinical Cancer Research.

[256]  H. Hara,et al.  Synthesis of the highly potent prostanoid FP receptor agonist, AFP-168: a novel 15-deoxy-15,15-difluoroprostaglandin F2α derivative , 2004 .

[257]  J. Naismith,et al.  Crystal structure and mechanism of a bacterial fluorinating enzyme , 2004, Nature.

[258]  V. Gotor,et al.  Enzymatic resolution of a quaternary stereogenic centre as the key step in the synthesis of (S)-(+)-citalopram , 2004 .

[259]  G. Tortora,et al.  Antitumor Activity of ZD6474, a Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor, in Human Cancer Cells with Acquired Resistance to Antiepidermal Growth Factor Receptor Therapy , 2004, Clinical Cancer Research.

[260]  P. Cahn Emtricitabine: a new nucleoside analogue for once-daily antiretroviral therapy , 2004, Expert opinion on investigational drugs.

[261]  M. Kageyama,et al.  New fluoroprostaglandin F(2alpha) derivatives with prostanoid FP-receptor agonistic activity as potent ocular-hypotensive agents. , 2003, Biological and Pharmaceutical Bulletin.

[262]  M. Kavana,et al.  Interaction of (4-hydroxyphenyl)pyruvate dioxygenase with the specific inhibitor 2-[2-nitro-4-(trifluoromethyl)benzoyl]-1,3-cyclohexanedione. , 2003, Biochemistry.

[263]  A. Kshirsagar,et al.  Cinacalcet HCl: a calcimimetic agent for the management of primary and secondary hyperparathyroidism , 2003, Expert opinion on investigational drugs.

[264]  J. Humphrey Medicinal chemistry of selective neurokinin-1 antagonists. , 2003, Current topics in medicinal chemistry.

[265]  R. Vaidyanathan,et al.  Early amidation approach to 3-[(4-amido)pyrrol-2-yl]-2-indolinones. , 2003, The Journal of organic chemistry.

[266]  N. Gow,et al.  Antifungal agents: mechanisms of action. , 2003, Trends in microbiology.

[267]  P. Johnston,et al.  5-Fluorouracil: mechanisms of action and clinical strategies , 2003, Nature Reviews Cancer.

[268]  Hui Chen,et al.  Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. , 2003, Journal of medicinal chemistry.

[269]  V. Jordan,et al.  Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents. , 2003, Journal of medicinal chemistry.

[270]  Jing Li,et al.  Efficient synthesis of NK(1) receptor antagonist aprepitant using a crystallization-induced diastereoselective transformation. , 2003, Journal of the American Chemical Society.

[271]  D. Su,et al.  Process for preparing Ezetimibe intermediate by an acid enhanced chemo- and enantioselective CBS catalyzed ketone reduction , 2003 .

[272]  Arun K. Ghosh,et al.  Chelation-controlled reduction: stereoselective formation of syn-1,3-diols and synthesis of compactin and mevinolin lactone. , 2002, The Journal of organic chemistry.

[273]  B. Trost,et al.  Utilization of molybdenum- and palladium-catayzed dynamic kinetic asymmetric transformations for the preparation of tertiary and quaternary stereogenic centers: a concise synthesis of tipranavir. , 2002, Journal of the American Chemical Society.

[274]  V. Hruby,et al.  A Convenient, Room-Temperature–Organic Base Protocol for Preparing Chiral 3-(Enoyl)-1,3-oxazolidin-2-ones , 2002 .

[275]  C. Eap,et al.  Enantiomers’ potential in psychopharmacology—a critical analysis with special emphasis on the antidepressant escitalopram , 2002, European Neuropsychopharmacology.

[276]  B. Riedl,et al.  A Scaleable Synthesis of BAY 43-9006: A Potent Raf Kinase Inhibitor for the Treatment of Cancer , 2002 .

[277]  Hong Ma,et al.  Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways , 2002, Oncogene.

[278]  Pradeep Kumar,et al.  A Concise Synthesis of (+)-Compactin Lactone by Asymmetric Dihydroxylation and Regioselective Cyclic Sulfite Opening Reactions , 2002 .

[279]  P. Reider,et al.  Practical asymmetric synthesis of aprepitant, a potent human NK-1 receptor antagonist, via a stereoselective Lewis acid-catalyzed trans acetalization reaction. , 2002, The Journal of organic chemistry.

[280]  R. Martino,et al.  Clinical studies of three oral prodrugs of 5-fluorouracil (capecitabine, UFT, S-1): a review. , 2002, The oncologist.

[281]  M. Kris,et al.  ZD1839, a selective oral epidermal growth factor receptor-tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumors: results of a phase I trial. , 2002, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[282]  M. Hepperle,et al.  Mono N-arylation of piperazine(III): metal-catalyzed N-arylation and its application to the novel preparations of the antifungal posaconazole and its advanced intermediate , 2002 .

[283]  L. Trusolino,et al.  Invasive growth: from development to metastasis. , 2002, The Journal of clinical investigation.

[284]  J. Hamilton,et al.  Biochemistry: Biosynthesis of an organofluorine molecule , 2002, Nature.

[285]  K. Rossen,et al.  Crystallization-induced diastereoselection: asymmetric synthesis of substance P inhibitors. , 2002, Chemistry.

[286]  S. Wedge,et al.  Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors. , 2002, Journal of medicinal chemistry.

[287]  G. Ruecroft,et al.  Synthesis of the Potent Antiglaucoma Agent, Travoprost , 2002 .

[288]  K. Uneyama,et al.  Diastereoselectivity controlled by electrostatic repulsion between the negative charge on a trifluoromethyl group and that on aromatic rings. , 2001, Chemical communications.

[289]  Y. Fujikawa,et al.  Synthesis and biological evaluations of quinoline-based HMG-CoA reductase inhibitors. , 2001, Bioorganic & medicinal chemistry.

[290]  P. Netland,et al.  Travoprost compared with latanoprost and timolol in patients with open-angle glaucoma or ocular hypertension. , 2001, American journal of ophthalmology.

[291]  K. Gibson,et al.  Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer. , 2001, Bioorganic & medicinal chemistry letters.

[292]  C. Moyes,et al.  3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists. , 2001, Journal of medicinal chemistry.

[293]  P. Ramachandran,et al.  Asymmetric allylboration for the synthesis of β-hydroxy-δ-lactone unit of statin drug analogs , 2001 .

[294]  A. Hoveyda,et al.  Enantioselective Synthesis of Unsaturated Cyclic Tertiary Ethers By Mo-Catalyzed Olefin Metathesis , 2001 .

[295]  M. Rowley,et al.  Current and novel approaches to the drug treatment of schizophrenia. , 2001, Journal of medicinal chemistry.

[296]  Cameron J. Cowden,et al.  A new synthesis of 1,2,4-triazolin-5-ones: application to the convergent synthesis of an NK1 antagonist , 2000 .

[297]  S. Chandrasekhar,et al.  Enantioselective Total Synthesis of the Antihypertensive Agent (S,R,R,R)-Nebivolol , 2000 .

[298]  H. Ishitsuka,et al.  The design and synthesis of a new tumor-selective fluoropyrimidine carbamate, capecitabine. , 2000, Bioorganic & medicinal chemistry.

[299]  A. Wakeling,et al.  Similarities and distinctions in the mode of action of different classes of antioestrogens. , 2000, Endocrine-related cancer.

[300]  J. Kendrew,et al.  Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors. , 1999, Journal of medicinal chemistry.

[301]  H. Ishitsuka,et al.  [Discovery and development of novel anticancer drug capecitabine]. , 1999, Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan.

[302]  D. O'Hagan,et al.  Fluorine-containing natural products , 1999 .

[303]  Y. Yanagawa,et al.  First systematic chiral syntheses of two pairs of enantiomers with 3,5-dihydroxyheptenoic acid chain, associated with a potent synthetic statin NK-104. , 1999, Bioorganic & medicinal chemistry letters.

[304]  M. Hepperle,et al.  Sequential mono-N-arylation of piperazine nitrogens. Part 1: A simplified method and its application to the preparation of a key N,N′-biaryl piperazine antifungal intermediate , 1999 .

[305]  A. Pike,et al.  Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles. , 1999, Journal of medicinal chemistry.

[306]  Xing Chen,et al.  A Novel One-Step Diastereo- and Enantioselective Formation of trans-Azetidinones and Its Application to the Total Synthesis of Cholesterol Absorption Inhibitors. , 1999, The Journal of organic chemistry.

[307]  A. Bailey,et al.  Antagonists of the platelet P2T receptor: a novel approach to antithrombotic therapy. , 1999, Journal of medicinal chemistry.

[308]  J. Metzger,et al.  Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist. , 1998, Journal of medicinal chemistry.

[309]  J. Gage,et al.  A Convergent, Scalable Synthesis of HIV Protease Inhibitor PNU-140690. , 1998, The Journal of organic chemistry.

[310]  K D Watenpaugh,et al.  Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class. , 1998, Journal of medicinal chemistry.

[311]  A. Hoveyda,et al.  Zr-Catalyzed Kinetic Resolution of Allylic Ethers and Mo-Catalyzed Chromene Formation in Synthesis. Enantioselective Total Synthesis of the Antihypertensive Agent (S,R,R,R)-Nebivolol , 1998 .

[312]  E. Lock,et al.  From toxicological problem to therapeutic use: The discovery of the mode of action of 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione (NTBC), its toxicology and development as a drug , 1998, Journal of Inherited Metabolic Disease.

[313]  W. Gerwick,et al.  Biosynthesis of the marine cyanobacterial metabolite barbamide. 1. Origin of the trichloromethyl group , 1998 .

[314]  T. C. White,et al.  Clinical, Cellular, and Molecular Factors That Contribute to Antifungal Drug Resistance , 1998, Clinical Microbiology Reviews.

[315]  J. P. Harrity,et al.  Chromenes through Metal-Catalyzed Reactions of Styrenyl Ethers. Mechanism and Utility in Synthesis , 1998 .

[316]  J. Clader,et al.  Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption. , 1998, Journal of medicinal chemistry.

[317]  Y. Koltin,et al.  The search for new triazole antifungal agents. , 1997, Current opinion in chemical biology.

[318]  J. Blagg,et al.  Pharmacological options in the treatment of benign prostatic hyperplasia. , 1997, Journal of medicinal chemistry.

[319]  Joel Morris,et al.  Asymmetric Syntheses and Absolute Stereochemistry of 5,6-Dihydro-α-pyrones, A New Class of Potent HIV Protease Inhibitors , 1997 .

[320]  J. P. Harrity,et al.  RU-CATALYZED REARRANGEMENT OF STYRENYL ETHERS. ENANTIOSELECTIVE SYNTHESIS OF CHROMENES THROUGH ZR- AND RU-CATALYZED PROCESSES , 1997 .

[321]  K. Hirai,et al.  Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. , 1997, Bioorganic & medicinal chemistry.

[322]  D. McTavish,et al.  Tamsulosin , 1996, Drugs.

[323]  W. Howe,et al.  Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors. , 1996, Journal of medicinal chemistry.

[324]  V. Soloshonok,et al.  Transition metal-catalyzed diastereoselective aldol reactions of prochiral ketones with methyl isocyanoacetate , 1996 .

[325]  V. Soloshonok,et al.  Asymmetric aldol reactions of trifluoromethyl ketones with a chiral Ni(II) complex of glycine: Stereocontrolling effect of the trifluoromethyl group , 1996 .

[326]  R. Burrier,et al.  2-Azetidinone cholesterol absorption inhibitors: structure-activity relationships on the heterocyclic nucleus. , 1996, Journal of medicinal chemistry.

[327]  A. Bell,et al.  Novel antifungal 2-aryl-1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives with high activity against Aspergillus fumigatus , 1996 .

[328]  W. Haiyan,et al.  Concise asymmetric routes to 2,2,4-trisubstituted tetrahydrofurans via chiral titanium imide enolates: Key intermediates towards synthesis of highly active azole antifungals SCH 51048 and SCH 56592 , 1996 .

[329]  C. Halldin,et al.  Synthesis of unlabelled, 3H‐ and 125I‐labelled β‐CIT and its ϖ‐fluoroalkyl analogues β‐CIT‐FE and β‐CIT‐FP, including synthesis of precursors , 1996 .

[330]  V. Soloshonok,et al.  HIGHLY DIASTEREOSELECTIVE ASYMMETRIC ALDOL REACTIONS OF CHIRAL NI(II)-COMPLEX OF GLYCINE WITH ALKYL TRIFLUOROMETHYL KETONES , 1996 .

[331]  A. Hoveyda,et al.  Zirconium-Catalyzed Kinetic Resolution of Cyclic Allylic Ethers. An Enantioselective Route to Unsaturated Medium Ring Systems , 1996 .

[332]  K. Ellsworth,et al.  4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency. , 1995, Journal of medicinal chemistry.

[333]  G. Tsujimoto,et al.  KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues. , 1995, Molecular pharmacology.

[334]  S. Frye,et al.  Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent. , 1995, Journal of medicinal chemistry.

[335]  H. Hartman,et al.  3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). , 1995, Journal of medicinal chemistry.

[336]  A. Tasaka,et al.  Optically Active Antifungal Azoles. IV. Synthesis and Antifungal Activity of (2R, 3R)-3-Azolyl-2-(substituted phenyl)-1-(1H-1, 2, 4-triazol-1-yl)-2-butanols , 1995 .

[337]  W. Haiyan,et al.  Highly stereoselective access to novel 2,2,4-substituted tetrahydrofurans by halocyclization: Practical chemoenzymatic synthesis of Sch 51048, a broad-spectrum orally active antifungal agent , 1995 .

[338]  T. Konoike,et al.  Practical Synthesis of Chiral Synthons for the Preparation of HMG-CoA Reductase Inhibitors , 1994 .

[339]  D. Loebenberg,et al.  Enantioselective synthesis of the optical isomers of broad-spectrum orally active antifungal azoles, Sch 42538 and Sch 45012 , 1994 .

[340]  V. Soloshonok,et al.  Catalytic asymmetric synthesis of β-fluoroalkyl-β-amino acids via biomimetic [1,3]-proton shift reaction , 1994 .

[341]  V. Soloshonok,et al.  Gold(I)-catalyzed asymmetric aldol reactions of fluorinated benzaldehydes with an α-isocyanoacetamide , 1994 .

[342]  V. Soloshonok Biocatalytic resolution of -fluoroalkyl--amino acids , 1994 .

[343]  M. Ashton,et al.  Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues. , 1994, Journal of medicinal chemistry.

[344]  R. Baldessarini,et al.  N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters. , 1994, Journal of medicinal chemistry.

[345]  V. Soloshonok,et al.  Gold(I)-catalyzed asymmetric aldol reaction of methyl isocyanoacetate with fluorinated benzaldehydes , 1994 .

[346]  K. Ishikawa,et al.  Highly diastereoselective aldol reaction of fluoroalkyl aryl ketones with methyl isocyanoacetate catalyzed by silver(I)/triethylamine , 1994 .

[347]  T. Hiyama,et al.  A novel synthetic method of HMG-CoA reductase inhibitor NK-104 via a hydroboration-cross coupling sequence , 1993 .

[348]  Takahashi Kyoko,et al.  A new synthesis of HMG-CoA reductase inhibitor NK-104 through hydrosilylation-cross coupling reaction , 1993 .

[349]  D. Kelly,et al.  Molecular genetic analysis of azole antifungal mode of action. , 1993, Biochemical Society transactions.

[350]  A. Tasaka,et al.  Optically active antifungal azoles. I. Synthesis and antifungal activity of (2R,3R)-2-(2,4-difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl)-2-b utanol and its stereoisomers. , 1993, Chemical & pharmaceutical bulletin.

[351]  Davidr . Evans,et al.  Substrate-directable chemical reactions , 1993 .

[352]  P. Collins,et al.  Synthesis of therapeutically useful prostaglandin and prostacyclin analogs , 1993 .

[353]  N. Bodor,et al.  A theoretical study of prednisolone, 6α-fluoroprednisolone, 9α-fluoroprednisolone, 6α,9α-difluoroprednisolone and related compounds , 1993 .

[354]  S. Takano,et al.  Enantioconvergent synthesis of a promising HMG CoA reductase inhibitor NK-104 from both enantiomers of epichlorohydrin , 1993 .

[355]  L. Bito,et al.  Phenyl-substituted prostaglandins: potent and selective antiglaucoma agents. , 1993, Journal of medicinal chemistry.

[356]  R. Schinazi,et al.  Asymmetric synthesis and biological evaluation of beta-L-(2R,5S)- and alpha-L-(2R,5R)-1,3-oxathiolane-pyrimidine and -purine nucleosides as potential anti-HIV agents. , 1993, Journal of medicinal chemistry.

[357]  R F Schinazi,et al.  Selective inhibition of human immunodeficiency viruses by racemates and enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine , 1992, Antimicrobial Agents and Chemotherapy.

[358]  S. Lindstedt,et al.  Treatment of hereditary tyrosinaemia type I by inhibition of 4-hydroxyphenylpyruvate dioxygenase , 1992, The Lancet.

[359]  R. Schinazi,et al.  Enzyme-mediated enantioselective preparation of pure enantiomers of the antiviral agent 2',3'-dideoxy-5-fluoro-3'-thiacytidine (FTC) and related compounds , 1992 .

[360]  M. Butters Large scale synthesis of 4‐ethylpyrimidine , 1992 .

[361]  R. Schinazi,et al.  Inhibition of the replication of hepatitis B virus in vitro by 2',3'-dideoxy-3'-thiacytidine and related analogues. , 1991, Proceedings of the National Academy of Sciences of the United States of America.

[362]  P B Hoffer,et al.  [123I]-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane: high-affinity SPECT radiotracer of monoamine reuptake sites in brain. , 1991, Journal of medicinal chemistry.

[363]  J. B. Jones,et al.  Enzymes in organic synthesis. 48. Pig liver esterase and porcine pancreatic lipase catalyzed hydrolyses of 3,4-(isopropylidenedioxy)-2,5-tetrahydrofuranyl diesters , 1991 .

[364]  A. Wakeling,et al.  A potent specific pure antiestrogen with clinical potential. , 1991, Cancer research.

[365]  D. Karanewsky,et al.  Practical synthesis of an enantiomerically pure synthon for the preparation of mevinic acid analogs , 1991 .

[366]  T. Hanamoto,et al.  Enantioselective synthesis of .beta.-hydroxy .delta.-lactones: a new approach to the synthetic congeners of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors , 1991 .

[367]  Davidr . Evans,et al.  New procedure for the direct generation of titanium enolates. Diastereoselective bond constructions with representative electrophiles , 1990 .

[368]  M Kasahara,et al.  Triazole antifungals. II. Synthesis and antifungal activities of 3-acyl-4-methyloxazolidine derivatives. , 1990, Chemical & pharmaceutical bulletin.

[369]  Yuko Kobayashi,et al.  An Improved Synthetic Method of (S)-2-Alkoxypropanals from Ethyl (S)-Lactate , 1989 .

[370]  M. Fujita,et al.  New and effective routes to fluoro analogs of aliphatic and aromatic amino acids , 1989 .

[371]  I. Ojima,et al.  Remarkable effects of a pentafluorophenyl group on the stereoselective reactions of a chiral iron acyl complex , 1988 .

[372]  S. Hagen,et al.  Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids. , 1988, Journal of medicinal chemistry.

[373]  C. Heathcock,et al.  Improved procedure for preparation of optically active 3-hydroxyglutarate monoesters and 3-hydroxy-5-oxoalkanoic acids , 1988 .

[374]  M. Okabe,et al.  HOMOGENEOUS CATALYSIS OF MIXED-METAL SYSTEMS. HIGHLY REGIOSELECTIVE HYDROFORMYLATION-AMIDOCARBONYLATION OF A FLUORO OLEFIN CATALYZED BY Co-Rh MIXED-METAL SYSTEMS. OBSERVATION OF CoRh(CO)//7 CATALYSIS. , 1988 .

[375]  M. Okabe,et al.  Hydroformylation of fluoro olefins, RfCH:CH2, catalyzed by group VIII transition-metal catalysts. Crucial factors for extremely high regioselectivity , 1987 .

[376]  C. Hadley,et al.  Total synthesis and biological evaluation of structural analogues of compactin and dihydromevinolin. , 1987, Journal of medicinal chemistry.

[377]  E. Walton,et al.  Azasteroids: structure-activity relationships for inhibition of 5 alpha-reductase and of androgen receptor binding. , 1986, Journal of medicinal chemistry.

[378]  K. Christe Chemical synthesis of elemental fluorine , 1986 .

[379]  B. Trost,et al.  On the use of the O-methylmandelate ester for establishment of absolute configuration of secondary alcohols , 1986 .

[380]  J M Liesch,et al.  Biosynthesis of fluorothreonine and fluoroacetic acid by the thienamycin producer, Streptomyces cattleya. , 1986, The Journal of antibiotics.

[381]  C. Heathcock,et al.  Synthetic and biological studies of compactin and related compounds. 4. Total synthesis of (+)-compactin , 1985 .

[382]  D. B. Ellis,et al.  Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles. , 1985, Journal of medicinal chemistry.

[383]  M. Taschner,et al.  Synthetic and biological studies of compactin and related compounds. II: Synthesis of the lactone moiety of compactin , 1984 .

[384]  C. Heathcock,et al.  A convenient assay for the optical purity of monomethyl 3-hydroxypentanedioate , 1984 .

[385]  I. Ojima,et al.  Regioselective hydroesterification and hydrocarboxylation of 3,3,3-trifluoropropene and pentafluorostyrene catalyzed by phosphine-palladium complex , 1983 .

[386]  A. Gilman,et al.  Aluminum: a requirement for activation of the regulatory component of adenylate cyclase by fluoride. , 1982, Proceedings of the National Academy of Sciences of the United States of America.

[387]  J. Scaiano Laser flash photolysis studies of the reactions of some 1,4-biradicals , 1982 .

[388]  I. Ojima,et al.  Remarkable dependency of regioselectivity on the catalyst metal species in the hydroformylation of trifluoropropene and pentafluorostyrene , 1982 .

[389]  Davidr . Evans,et al.  Asymmetric alkylation reactions of chiral imide enolates. A practical approach to the enantioselective synthesis of .alpha.-substituted carboxylic acid derivatives , 1982 .

[390]  H. Koga,et al.  Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids. , 1980, Journal of medicinal chemistry.

[391]  J. Scaiano,et al.  Hydrogen abstraction by biradicals. Reactions with tri-n-butylstannane and octanethiol , 1980 .

[392]  F. Fukuoka,et al.  Synthetic nucleosides and nucleotides. XI. Facile synthesis and antitumor activities of various 5-fluoropyrimidine nucleosides. , 1978, Chemical & pharmaceutical bulletin.

[393]  U. Niedballa,et al.  Synthesis of nucleosides. 9. General synthesis of N-glycosides. I. Synthesis of pyrimidine nucleosides , 1974 .

[394]  A. Walpole,et al.  Potent luteolytic agents related to prostaglandin F2α , 1974, Nature.

[395]  A. Ercoli,et al.  Antiinflammatory activities of 17,21-methyl ortho esters, 17-mono- and 17,21-diesters of 6 ,9 -difluorocorticosteroids. , 1972, Journal of medicinal chemistry.

[396]  P. Wagner Type II photoelimination and photocyclization of ketones , 1971 .

[397]  G. Y. Lesher,et al.  1,8-NAPHTHYRIDINE DERIVATIVES. A NEW CLASS OF CHEMOTHERAPEUTIC AGENTS. , 1962, Journal of medicinal and pharmaceutical chemistry.

[398]  C. Heidelberger,et al.  Fluorinated Pyrimidines, A New Class of Tumour-Inhibitory Compounds , 1957, Nature.

[399]  E. F. Sabo,et al.  9α-FLUORO DERIVATIVES OF CORTISONE AND HYDROCORTISONE , 1954 .

[400]  E. F. Sabo,et al.  SYNTHESIS OF 17α-HYDROXYCORTICOSTERONE AND ITS 9α-HALO DERIVATIVES FROM 11-EPI-17α-HYDROXYCORTICOSTERONE , 1953 .

[401]  O. Ruff,et al.  Über ein neues Chlorfluorid‐CIF3 , 1930 .

[402]  An Cásar , 1806, Bekenntnisse einer schönen Seele.

[403]  A. Wagstaff,et al.  Nebivolol , 2012, Drugs.

[404]  C. Perry,et al.  Emtricitabine , 2012, Drugs.

[405]  C. Perry,et al.  Tipranavir , 2012, Drugs.

[406]  M. Metra,et al.  Nebivolol , 2012, Drugs.

[407]  L. Scott,et al.  Emtricitabine , 2012, Drugs.

[408]  P. McKiernan Nitisinone in the Treatment of Hereditary Tyrosinaemia Type 1 , 2012, Drugs.

[409]  B. Swahn,et al.  Recent Progress in the Discovery of Kv7 Modulators , 2011 .

[410]  C. Marcocci,et al.  Update on the use of cinacalcet in the management of primary hyperparathyroidism , 2011, Journal of Endocrinological Investigation.

[411]  S. Miknyoczki,et al.  Discovery of small molecule c-Met inhibitors: Evolution and profiles of clinical candidates. , 2010, Anti-cancer agents in medicinal chemistry.

[412]  Liu Wen-mei Fluorine and Health , 2009 .

[413]  C. White,et al.  Role of Prasugrel, a Novel P2Y12 Receptor Antagonist, in the Management of Acute Coronary Syndromes , 2009, American journal of cardiovascular drugs : drugs, devices, and other interventions.

[414]  Michelle A. Schmidt,et al.  To Market, To Market — 2007 , 2008 .

[415]  M. Martinelli,et al.  Practical synthesis of the calcimimetic agent, cinacalcet , 2008 .

[416]  Yoshihisa Inoue,et al.  Chirality-sensing supramolecular systems. , 2008, Chemical reviews.

[417]  A. Yu,et al.  Synthesis of (S,R,R,R)-α,α′-Iminobis(methylene)bis(6-fluoro-3H,4H-dihydro-2H-1-benzopyran-2-methanol) , 2007 .

[418]  M. Saag Emtricitabine, a new antiretroviral agent with activity against HIV and hepatitis B virus. , 2006, Clinical infectious diseases : an official publication of the Infectious Diseases Society of America.

[419]  Shane W. Krska,et al.  Understanding the Origin of Unusual Stepwise Hydrogenation Kinetics in the Synthesis of the 3-(4-Fluorophenyl)morpholine Moiety of NK1 Receptor Antagonist Aprepitant , 2006 .

[420]  D. Loebenberg,et al.  Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5]. , 2006, Bioorganic & medicinal chemistry letters.

[421]  S. Keam,et al.  Escitalopram , 2012, Drugs.

[422]  K. Bogeso,et al.  The pharmacological effect of citalopram resides in the (S)-(+)-enantiomer , 2005, Journal of Neural Transmission / General Section JNT.

[423]  B. Gaede,et al.  Viral Clearance Issues Associated with the Use of an Animal-Derived Enzyme in the Synthesis of Emtricitabine , 2005 .

[424]  C. Walko,et al.  Capecitabine: a review. , 2005, Clinical therapeutics.

[425]  Christopher Bryson The Fluoride Deception , 2004 .

[426]  Y. Itoh,et al.  Fluorinated carbonyl and olefinic compounds: basic character and asymmetric catalytic reactions. , 2004, Chemical reviews.

[427]  T. Hiyama,et al.  Modern synthetic methods for fluorine-substituted target molecules. , 2004, Angewandte Chemie.

[428]  J. Clader The discovery of ezetimibe: a view from outside the receptor. , 2004, Journal of medicinal chemistry.

[429]  Juthamas Sukbuntherng,et al.  In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. , 2003, Clinical cancer research : an official journal of the American Association for Cancer Research.

[430]  K. Goa,et al.  Capecitabine: a review of its pharmacology and therapeutic efficacy in the management of advanced breast cancer. , 2003, Drugs.

[431]  A. Pettman,et al.  Process Development of Voriconazole: A Novel Broad-Spectrum Triazole Antifungal Agent , 2001 .

[432]  E. Manavathu,et al.  Voriconazole: A second-generation triazole. , 2001, Drugs of today.

[433]  K. Goa,et al.  Capecitabine: a review of its use in the treatment of advanced or metastatic colorectal cancer. , 2001, Drugs.

[434]  J. Castaǹer,et al.  ANTIVIRAL FOR AIDS HIV-1 PROTEASE INHIBITOR , 1998 .

[435]  V. Soloshonok,et al.  Gold(I)-catalyzed asymmetric aldol reactions of isocyanoacetic acid derivatives with fluoroaryl aldehydes , 1996 .

[436]  B. Syuto,et al.  Possible involvement of a small G-protein sensitive to exoenzyme C3 of Clostridium botulinum in the regulation of myofilament Ca2+ sensitivity in beta-escin skinned smooth muscle of guinea pig ileum. , 1995, Japanese journal of pharmacology.

[437]  B. Smart,et al.  Organofluorine chemistry : principles and commercial applications , 1994 .

[438]  T. Hiyama,et al.  A novel enantioselective synthesis of HMG Co-A reductase inhibitor NK-104 and a related compound , 1992 .

[439]  M. Lopp,et al.  Synthesis of a novel four-carbon chiron - (R)-1-t-butyldimethylsilyl-3,4-epoxy-but-1-yne , 1991 .

[440]  W. Bartmann,et al.  Synthesis and biological activity of new HMG-CoA reductase inhibitors. 1. Lactones of pyridine- and pyrimidine-substituted 3,5-dihydroxy-6-heptenoic (-heptanoic) acids. , 1990, Journal of medicinal chemistry.

[441]  B. Trost,et al.  Tin mediated palladium catalyzed regiocontrolled alkylations of vinyl epoxides , 1988 .

[442]  I. Ojima,et al.  New and direct route to 5-trifluoromethyl-5,6-dihydrouracils by means of palladium complex catalyzed “ureidocarbonylation” of 2-bromo-3,3,3-trifluoropropene , 1982 .

[443]  R. Newton,et al.  Total synthesis of prostaglandin-F2α through homoconjugate addition of an organocuprate reagent to a tricyclo[3.2.0.02,7]heptanone , 1978 .