M. Bock

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Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.

B. E. Evans, D. Veber, K. Rittle, 1988, Journal of medicinal chemistry.

Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.

B. E. Evans, D. Veber, K. Rittle, 1988, Journal of medicinal chemistry.

Role of Mechanistic Transport Studies in Lead Optimization

M. Bock, Jiunn H. Lin, J. Hochman, 2006 .

Design of potent, orally effective, nonpeptidal antagonists of the peptide hormone cholecystokinin.

B. E. Evans, D. Veber, K. Rittle, 1986, Proceedings of the National Academy of Sciences of the United States of America.

Synthesis and resolution of 3-amino-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-ones

B. E. Evans, D. Veber, K. Rittle, 1987 .

Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3).

M. Bock, R. M. Dipardo, S. Kuduk, 2009, Bioorganic & medicinal chemistry letters.

In vitro studies on L-771,688 (SNAP 6383), a new potent and selective alpha1A-adrenoceptor antagonist.

M. Bock, R. Chang, B. Lagu, 2000, European journal of pharmacology.

Chapter 20. Toward the development of α1a adrenergic receptor antagonists

M. Bock, M. Patane, 2000 .

4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.

M. Bock, R. Chang, M. Patane, 1998, Journal of medicinal chemistry.

Chapter 12. Bradykinin-1 receptor antagonists

M. Bock, J. Hess, D. Pettibone, 2003 .

Progress in the development of oxytocin antagonists for use in preterm labor.

B. E. Evans, M. Bock, D. Reiss, 1995, Advances in experimental medicine and biology.

4-Oxospiro[benzopyran-2,4′-piperidines] as selective α1a-adrenergic receptor antagonists

M. Bock, R. Chang, T. Broten, 1999 .

A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.

M. Bock, R. M. Dipardo, D. Reiss, 2008, Bioorganic & medicinal chemistry letters.

An expedient synthesis of 3-amino-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-one

B. E. Evans, D. Veber, K. Rittle, 1987 .

Benzodiazepine gastrin and brain cholecystokinin receptor ligands: L-365,260.

B. E. Evans, K. Rittle, M. Bock, 1989, Journal of medicinal chemistry.

A Second Generation of Non‐Peptide Cholecystokinin Receptor Antagonists and Their Possible Therapeutic Potential

J. Kemp, M. Bock, R. M. Dipardo, 1994, Annals of the New York Academy of Sciences.

Selective non-peptide ligands for an accommodating peptide receptor. Imidazobenzodiazepines as potent cholecystokinin type B receptor antagonists.

J. Kemp, D. Veber, M. Bock, 1994, Bioorganic & medicinal chemistry.

Benzolactams as non-peptide cholecystokinin receptor ligands

D. Veber, M. Bock, R. M. Dipardo, 1993 .

Design of cholecystokinin peptidomimetics

B. E. Evans, D. Veber, K. Rittle, 1992 .

Bradykinin antagonists: new opportunities.

M. Bock, J. Longmore, 2000, Current opinion in chemical biology.

A key intermediate for the synthesis of maytansine and related antitumor agents

E. Corey, M. Bock, D. Floyd, 1978 .

Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors.

M. Bock, C. Gabel, M. Holloway, 2022, ACS medicinal chemistry letters.

Radioligand binding studies reveal marked species differences in the vasopressin V1 receptor of rat, rhesus and human tissues.

D. Veber, M. Bock, R. Freidinger, 1992, Life sciences.

Development and pharmacological assessment of novel peptide and nonpeptide oxytocin antagonists

B. E. Evans, D. Veber, M. Bock, 1993, Regulatory Peptides.

Discovery of Potent, Selective and State-Dependent NaV1.7 Inhibitors with Robust Oral Efficacy in Pain Models: Structure-Activity Relationship and Optimization of Chroman and Indane Aryl Sulfonamides.

Sneha S. Joshi, P. Gupta, M. Bock, 2020, Journal of medicinal chemistry.

Stereocontrolled route to a key intermediate for the synthesis of maytansine

E. Corey, M. Bock, 1975 .

Pharmacological characterization and radioligand binding properties of a high-affinity, nonpeptide, bradykinin B1 receptor antagonist.

M. Bock, R. Freidinger, R. Chang, 2004, European journal of pharmacology.

L‐368,899, a potent orally active oxytocin antagonist for potential use in preterm labor

B. E. Evans, M. Kaufman, D. Veber, 1993 .

1-(((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido) bicyclo(2.2.1)heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl) piperazine (L-368,899): An Orally Bioavailable, Non-Peptide Oxytocin Antagonist with Potential Utility for Managing Preterm Labor.

B. E. Evans, M. Bock, R. Freidinger, 1994 .

1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor.

B. E. Evans, M. Bock, P. Anderson, 1994, Journal of medicinal chemistry.

5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.

M. Bock, S. Kuduk, T. Prueksaritanont, 2006, Bioorganic & medicinal chemistry letters.

Discovery of a potent, non-peptide bradykinin B1 receptor antagonist.

M. Bock, R. M. Dipardo, R. Freidinger, 2003, Journal of the American Chemical Society.

Second-generation benzodiazepine CCK-B antagonists. Development of subnanomolar analogs with selectivity and water solubility.

J. Kemp, D. Veber, M. Bock, 1994, Journal of medicinal chemistry.

Inhibition of acute nociceptive responses in rat spinal cord by a bradykinin B1 receptor antagonist.

M. Bock, R. M. Dipardo, R. Chang, 2005, European journal of pharmacology.

From Ergolines to Indoles: Improved Inhibitors of the Human H3 Receptor for the Treatment of Narcolepsy

M. Bock, Y. Auberson, Charles R. Yang, 2015, ChemMedChem.

Tetrabutylammonium salt induced denitration of nitropyridines: synthesis of fluoro-, hydroxy-, and methoxypyridines.

M. Bock, R. M. Dipardo, S. Kuduk, 2005, Organic letters.

Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.

M. Bock, R. Freidinger, J. Vacca, 1997, Journal of medicinal chemistry.

Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.

B. E. Evans, M A Jacobson, M. Bock, 1999, Bioorganic & medicinal chemistry letters.

Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series.

M. Bock, R. Freidinger, S. Kuduk, 2005, Bioorganic & medicinal chemistry letters.

Binding modes of dihydroquinoxalinones in a homology model of bradykinin receptor 1.

M. Bock, R. Freidinger, R. Chang, 2005, Biochemical and biophysical research communications.

Benzodiazepines as potent and selective bradykinin B1 antagonists.

Tsing-Bau Chen, M. Bock, R. M. Dipardo, 2003, Journal of medicinal chemistry.

Development of a novel class of cyclic hexapeptide oxytocin antagonists based on a natural product.

M. Bock, W. L. Whitter, G. F. Lundell, 1992, Journal of medicinal chemistry.

Theoretical estimation of pKa values of pyrazinylguanidine derivatives

M. Bock, H. Schlegel, GrahamJ Smith, 1981 .

Protection of primary hydroxyl groups as methylthiomethyl ethers

E. Corey, M. Bock, 1975 .

Cholecystokinin antagonists. Synthesis of asperlicin analogues with improved potency and water solubility.

B. E. Evans, D. Veber, K. Rittle, 1986, Journal of medicinal chemistry.

Expedient synthesis of 5-unsubstituted 3,4-dihydropyrimidin-2(1H)-ones

M. Bock, C. Coburn, T. Steele, 1998 .

Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.

B. E. Evans, D. Veber, K. Rittle, 1988, Journal of medicinal chemistry.

3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.

M. Bock, B. Lagu, M. Ramachandra, 2014, Journal of medicinal chemistry.

Expedient Synthesis of 5-Unsubstituted 3,4-Dihydropyrimidin-2(1H)-ones.

M. Bock, C. Coburn, T. Steele, 1999 .

Renin inhibitors containing hydrophilic groups. Tetrapeptides with enhanced aqueous solubility and nanomolar potency.

B. E. Evans, K. Rittle, M. Bock, 1988, Journal of medicinal chemistry.

Total synthesis of nonpeptidal cholecystokinin antagonists from Aspergillus alliaceus

M. Bock, R. M. Dipardo, R. Freidinger, 1987 .

Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists.

Steven V. Fox, James C Barrow, Cuyue Tang, 2010, Bioorganic & medicinal chemistry letters.

Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists.

Steven V. Fox, S. Doran, G. McGaughey, 2010, ACS medicinal chemistry letters.

Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.

B. E. Evans, D. Veber, K. Rittle, 1987, Journal of medicinal chemistry.

Synthesis of quinazolino[3,2-d]-1,4-benzodiazepin-6,9(5h,7H)-diones

M. Bock, R. M. Dipardo, R. Freidinger, 1985 .

Synthesis of 2,3-diaminodihydropyrroles via thioimidate cyclopropane rearrangement

M. Bock, S. Kuduk, Ronald K. Chang, 2003 .

Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.

M. Bock, R. M. Dipardo, D. Reiss, 2008, Bioorganic & medicinal chemistry letters.

Total synthesis of (.+-.)-N-methylmaysenine

E. Corey, M. Bock, D. Floyd, 1978 .

Cyclic hexapeptide oxytocin antagonists. Potency-, selectivity-, and solubility-enhancing modifications.

M. Bock, R. M. Dipardo, R. Freidinger, 1990, Journal of medicinal chemistry.

A simple and highly effective route to α,β-unsaturated aldehydes

E. Corey, M. Bock, D. Enders, 1976 .

Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.

M. Bock, R. Freidinger, R. Chang, 2006, Journal of medicinal chemistry.

A new amine resolution method and its application to 3-aminobenzodiazepines

B. E. Evans, D. Veber, K. Rittle, 1987 .

Ergoline‐Derived Inverse Agonists of the Human H3 Receptor for the Treatment of Narcolepsy

M. Fendt, M. Bock, Y. Auberson, 2014, ChemMedChem.

Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

M. Bock, R. M. Dipardo, R. Freidinger, 2008, Bioorganic & medicinal chemistry letters.

A New Amine Resolution Method and Its Application to 3‐Aminobenzodiazepines.

B. E. Evans, D. Veber, K. Rittle, 1987 .

Characterization of the binding of [3H]L-365,260: a new potent and selective brain cholecystokinin (CCK-B) and gastrin receptor antagonist radioligand.

M. Bock, R. Freidinger, R. Chang, 1989, Molecular pharmacology.

Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.

M. Bock, Sunil K. Panigrahi, M. Ramachandra, 2022, Journal of medicinal chemistry.

(2S,3S,4R)‐4‐Amino‐3‐hydroxy‐2‐methylpentanoic Acid. Enantioselective Synthesis of an Amino Acid Constituent of Bleomycin.

M. Bock, R. M. Dipardo, 1984 .

Stereochemistry of 1,4-conjugate elimination reactions

M. Bock, R. K. Hill, 1978 .

Synthesis of cephalotaxine analogs

M. Bock, R. K. Hill, S. Sawada, 1987 .

Differentially protected .alpha.-aminoglycine

M. Bock, R. M. Dipardo, R. Freidinger, 1986 .

Nanomolar-affinity, non-peptide oxytocin receptor antagonists.

B. E. Evans, K. Rittle, M. Bock, 1993, Journal of medicinal chemistry.

In vitro pharmacological profile of a novel structural class of oxytocin antagonists.

D. Veber, M. Bock, R. Freidinger, 1991, The Journal of pharmacology and experimental therapeutics.

2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.

M. Bock, R. Freidinger, R. Chang, 2008, Journal of medicinal chemistry.

Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.

M. Bock, R. Freidinger, R. Chang, 2007, Bioorganic & medicinal chemistry letters.

Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.

M. Bock, R. M. Dipardo, D. Reiss, 2007, Journal of medicinal chemistry.

Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.

M. Bock, R. Freidinger, R. Chang, 2004, Bioorganic & Medicinal Chemistry Letters.

2,3-diaminopyridine bradykinin B1 receptor antagonists.

M. Bock, R. Freidinger, R. Chang, 2004, Journal of medicinal chemistry.

Generation and Characterization of a Human Bradykinin Receptor B1 Transgenic Rat as a Pharmacodynamic Model

M. Bock, R. M. Dipardo, R. Chang, 2004, Journal of Pharmacology and Experimental Therapeutics.

Indazole derivatives as novel bradykinin B1 receptor antagonists.

M. Bock, D. Reiss, S. Kuduk, 2010, Bioorganic & medicinal chemistry letters.

CYP2C75-Involved Autoinduction of Metabolism in Rhesus Monkeys of Methyl 3-Chloro-3′-fluoro-4′-{(1R)-1-[({1-[(trifluoroacetyl)amino]cyclopropyl}carbonyl)amino]ethyl}-1,1′-biphenyl-2-carboxylate (MK-0686), a Bradykinin B1 Receptor Antagonist

B. Ma, M. Bock, S. Kuduk, 2008, Journal of Pharmacology and Experimental Therapeutics.

CYP2C75-Involved Autoinduction of Metabolism in Rhesus Monkeys of Methyl 3-Chloro-3 (cid:1) -fluoro-4 (cid:1) -{(1 R -biphenyl-2-carboxylate (MK-0686), a Bradykinin B 1 Receptor Antagonist

B. Ma, M. Bock, S. Kuduk, 2008 .

CYP2C75-Involved Autoinduction of Metabolism in Rhesus Monkeys of MK-0686, a Bradykinin B1 Receptor Antagonist

B. Ma, M. Bock, S. Kuduk, 2008 .

Rhesus Monkeys of MK-0686, a Bradykinin B 1 Receptor Antagonist

B. Ma, M. Bock, S. Kuduk, 2008 .

Bradykinin B1 antagonists: biphenyl SAR studies in the cyclopropanecarboxamide series.

M. Bock, R. M. Dipardo, D. Reiss, 2007, Bioorganic & medicinal chemistry letters.

2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.

Dong-Mei Feng, Cuyue Tang, Christina Ng, 2005, Bioorganic & medicinal chemistry letters.

Generation and characterization of a humanized bradykinin B1 receptor mouse

M. Bock, R. Chang, T. Vogt, 2006, Biological chemistry.

Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.

Steven V. Fox, S. Doran, W. Shipe, 2008, Journal of medicinal chemistry.

Synthesis and biological activity of 3-amino-5-(3,5-diamino-6-chloropyrazin-2-yl)-1,2,4-oxadiazole: an amiloride prodrug.

M. Bock, E. Cragoe, E. H. Blaine, 1986, Journal of Medicinal Chemistry.

Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.

Steven V. Fox, S. Doran, W. Shipe, 2008, Journal of medicinal chemistry.

Development of 1,4-benzodiazepine cholecystokinin type B antagonists.

B. E. Evans, K. Rittle, M. Bock, 1993, Journal of medicinal chemistry.

Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted 1,4-benzodiazepin-2-amines.

B. E. Evans, K. Rittle, M. Bock, 1988, Journal of medicinal chemistry.

Curtius rearrangement in the 5-phenyl-1,4-benzodiazepine series. Unprecedented participation by an imine nitrogen

M. Bock, R. M. Dipardo, R. Freidinger, 1990 .

Curtius Rearrangement in the 5-Phenyl-1,4-benzodiazepine Series. Unprecedented Participation by an Imine Nitrogen.

M. Bock, R. M. Dipardo, R. Freidinger, 1990 .

Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.

B. E. Evans, D. Veber, K. Rittle, 1990, Journal of medicinal chemistry.

Synthesis and Resolution of 3-Amino-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-ones.

B. E. Evans, D. Veber, K. Rittle, 1988 .

Reversal of diastereoselection in the addition of Grignard reagents to chiral 2-pyridyl tert-butyl (Ellman) sulfinimines

M. Bock, R. M. Dipardo, S. Kuduk, 2004 .

Reversal of Diastereoselection in the Addition of Grignard Reagents to Chiral 2-Pyridyl tert-Butyl (Ellman) Sulfinimines.

M. Bock, R. M. Dipardo, S. Kuduk, 2004 .

Bioactivation of 2,3-diaminopyridine-containing bradykinin B1 receptor antagonists: irreversible binding to liver microsomal proteins and formation of glutathione conjugates.

M. Bock, T. Baillie, S. Kuduk, 2005, Chemical research in toxicology.

Bradykinin agonist activity of a novel, potent oxytocin antagonist.

D. Veber, M. Bock, R. Freidinger, 1991, European Journal of Pharmacology.

Novel oxytocin antagonists

B. E. Evans, D. Veber, M. Bock, 1993 .

Potent and selective cyclic hexapeptide oxytocin antagonists

D. Veber, M. Bock, R. M. Dipardo, 1991 .

Potent and Selective Oxytocin Antagonists Obtained by Chemical Modification of a Streptomyces Silvensis Derived Cyclic Hexapeptide and by Total Synthesis

D. Veber, M. Bock, R. M. Dipardo, 1990 .

Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide.

D. Veber, M. Bock, R. M. Dipardo, 1990, Journal of medicinal chemistry.

Antagonism of oxytocin in rats and pregnant rhesus monkeys by the novel cyclic hexapeptides, L-366,682 and L-366,948.

M. Bock, D. Reiss, M. Kaufman, 1991, The Journal of pharmacology and experimental therapeutics.

Prostaglandin isosteres. 2. Chain-modified thiazolidinone prostaglandin analogues as renal vasodilators.

M. Bock, R. M. Dipardo, J. Springer, 1983, Journal of medicinal chemistry.

Orally active, non-peptide oxytocin antagonists

B. E. Evans, D. Veber, M. Bock, 1994 .

The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders

M. Bock, Y. Auberson, Charles R. Yang, 2019, ChemMedChem.

Identification of the critical residues of bradykinin receptor B1 for interaction with the kinins guided by site-directed mutagenesis and molecular modeling.

M. Bock, R. Chang, J. Hess, 2006, Biochemistry.

Bradykinin B1 receptor antagonists as novel analgesics: a retrospective of selected medicinal chemistry developments.

M. Bock, S. Kuduk, 2008, Current topics in medicinal chemistry.