S. Sakamoto

发表

Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor.

K. Mori, T. Kadokura, Yuji Koga, 2011, Journal of medicinal chemistry.

Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: enzyme inhibition and effects on plasma lipid levels.

H. Moritani, T. Ugawa, S. Tsukamoto, 2003, Bioorganic & medicinal chemistry.

Synthesis and Pharmacological Evaluation of 5-(4-Biphenyl)-3-methyl-4-phenyl-1,2,4-triazole Derivatives as a Novel Class of Selective Antagonists for the Human Vasopressin V1A Receptor

J. Tsukada, S. Tsukamoto, S. Sakamoto, 2002 .

Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.

J. Tsukada, S. Tsukamoto, S. Sakamoto, 2002, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of benzyloxyphenyl derivatives as a novel class of NCX inhibitors: effects on heart failure.

Hiroyoshi Yamada, S. Sakamoto, A. Kakefuda, 2005, Bioorganic & medicinal chemistry.

Discovery of N-(3-{4-[(3-fluorobenzyl)oxy]phenoxy}propyl)-2-pyridin-4-ylacetamide as a potent and selective reverse NCX inhibitor.

Hiroyoshi Yamada, S. Sakamoto, A. Kakefuda, 2005, Chemical & pharmaceutical bulletin.

Discovery of an N-(2-aminopyridin-4-ylmethyl)nicotinamide derivative: a potent and orally bioavailable NCX inhibitor.

Hiroyoshi Yamada, S. Sakamoto, A. Kakefuda, 2005, Bioorganic & medicinal chemistry.

Discovery of 4,5-diphenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human V(1A) receptor.

S. Tsukamoto, S. Sakamoto, A. Kakefuda, 2002, Bioorganic & medicinal chemistry.

Synthesis and structure-activity relationships of phenoxypyridine derivatives as novel inhibitors of the sodium-calcium exchanger.

Hiroyoshi Yamada, S. Sakamoto, A. Kakefuda, 2004, Bioorganic & medicinal chemistry.

New thiazole derivatives as potent and selective 5-hydroxytriptamine 3 (5-HT3) receptor agonists for the treatment of constipation.

T. Mase, S. Akuzawa, M. Ohta, 2003, Bioorganic & medicinal chemistry.

Potent and selective TF/FVIIa inhibitors containing a neutral P1 ligand.

M. Okada, T. Niimi, M. Ohta, 2006, Bioorganic & medicinal chemistry.

Effects of 2-[N-(4-Chlorophenyl)-N-methylamino]-4H-pyrido[3.2-e]-1,3-thiazin-4-one (YM928), an Orally Active α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Receptor Antagonist, in Models of Generalized Epileptic Seizure in Mice and Rats

H. Yamashita, Tokio Yamaguchi, M. Okada, 2004, Journal of Pharmacology and Experimental Therapeutics.

Effect of YM928, a novel AMPA receptor antagonist, on seizures in EL mice and kainate-induced seizures in rats

H. Yamashita, Tokio Yamaguchi, M. Okada, 2004, Naunyn-Schmiedeberg's Archives of Pharmacology.

Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.

S. Tsukamoto, K. Sugasawa, S. Sakamoto, 2008, Bioorganic & medicinal chemistry.

Convergent enantioselective synthesis of vinigrol, an architecturally novel diterpenoid with potent platelet aggregation inhibitory and antihypertensive properties. 1. Application of anionic sigmatropy to construction of the octalin substructure.

L. Paquette, I. Kim, S. Sakamoto, 2003, The Journal of organic chemistry.

YM90K: pharmacological characterization as a selective and potent alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor antagonist.

S. Usuda, M. Okada, S. Sakamoto, 1996, The Journal of pharmacology and experimental therapeutics.

Synthesis and biological activity of novel 1,4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity.

Y. Matsumoto, T. Kawasaki, S. Tsukamoto, 2004, Bioorganic & medicinal chemistry.

YM872: a selective, potent and highly water-soluble alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist.

A. Kohara, Tokio Yamaguchi, M. Okada, 2006, CNS drug reviews.

Synthesis, gene silencing activity, thermal stability, and serum stability of siRNA containing four (S)-5′-C-aminopropyl-2′-O-methylnucleosides (A, adenosine; U, uridine; G, guanosine; and C, cytidine)

S. Sakamoto, Ryohei Kajino, Y. Ueno, 2022, RSC advances.

Suppression of fully kindled seizure and retardation of kindling acquisition by YM928 in the rat kindling model of epilepsy.

H. Yamashita, Tokio Yamaguchi, M. Okada, 2004, European journal of pharmacology.

Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands.

M. Okada, T. Niimi, M. Ohta, 2007, Bioorganic & medicinal chemistry.

Synthesis and biological activity of novel 1,2-disubstituted benzene derivatives as factor Xa inhibitors.

N. Katayama, Y. Matsumoto, Y. Iwatsuki, 2005, Bioorganic & medicinal chemistry.

Syntheses of 23-deoxy-23-N-ethyl-23-(2-fluoro-, 2,2-difluoro-, and 2,2,2-trifluoroethyl)amino derivatives of mycaminosyl tylonolide and 4'-deoxymycaminosyl tylonolide.

A. Tanaka, M. Hamada, H. Umezawa, 1984, The Journal of antibiotics.

Design, synthesis and biological activity of YM-60828 derivatives: potent and orally-bioavailable factor Xa inhibitors based on naphthoanilide and naphthalensulfonanilide templates.

H. Kurihara, N. Katayama, Y. Matsumoto, 2002, Bioorganic & medicinal chemistry.

8-(1H-imidazol-1-yl)-7-nitro-4(5H)-imidazo[1,2-alpha]quinoxalinone and related compounds: synthesis and structure-activity relationships for the AMPA-type non-NMDA receptor.

M. Okada, S. Sakamoto, M. Shimizu‐Sasamata, 1997, Journal of medicinal chemistry.

Synthesis of (14R)- and (14S)-14-De(hydroxymethyl)-14-hydroxymycaminosyl Tylonolides

H. Umezawa, S. Sakamoto, S. Umezawa, 1987 .

Syntheses of 23-C-substituted derivatives of mycaminosyl tylonolide.

M. Hamada, H. Umezawa, S. Sakamoto, 1986, The Journal of antibiotics.

N-Substituted derivatives of 23-amino-4',23-dideoxymycaminosyl tylonolide. Synthesis and antibacterial activity.

A. Tanaka, M. Hamada, H. Umezawa, 1985, The Journal of antibiotics.

Development of a Practical and Scalable Synthesis of a Potent Selective Dual Antagonist for 5-HT2B and 5-HT7 Receptors

S. Yoshida, S. Sakamoto, Takenori Kimura, 2012 .

Syntheses and biological evaluation of novel quinuclidine derivatives as squalene synthase inhibitors.

H. Moritani, T. Ugawa, S. Tsukamoto, 2003, Bioorganic & medicinal chemistry.

Acid-mediated Cyclization of 3-Benzoyl-2-cyanobutyronitrile to 2-Amino-4-methyl-5-phenylfuran-3-carbonitrile

S. Tsukamoto, S. Sakamoto, K. Kawaguchi, 2004 .

Synthesis and pharmacological evaluation of N-acyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel specific bradycardic agents.

Toshihiro Watanabe, N. Masuda, S. Tsukamoto, 2004, Bioorganic & medicinal chemistry.

Orally active factor Xa inhibitor: synthesis and biological activity of masked amidines as prodrugs of novel 1,4-diazepane derivatives.

Y. Matsumoto, Y. Iwatsuki, T. Kawasaki, 2004, Bioorganic & medicinal chemistry.

Studies on novel bone resorption inhibitors. I. Synthesis and pharmacological activities of aminomethylenebisphosphonate derivatives.

M. Takeuchi, Y. Isomura, S. Sakamoto, 1993, Chemical & pharmaceutical bulletin.

One‐Pot Preparation of Unsymmetrical Biaryls via Suzuki Cross‐Coupling Reaction of Aryl Halide using Phase‐Transfer Catalyst in a Biphasic Solvent System

M. Okada, M. Ohta, S. Tsukamoto, 2007 .

Synthesis and pharmacological evaluation of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel specific bradycardic agents.

Toshihiro Watanabe, N. Masuda, S. Tsukamoto, 2004, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.

S. Tsukamoto, S. Sakamoto, H. Kubota, 2008, Bioorganic & medicinal chemistry.

Synthesis and biological evaluation of 3-biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as novel glycine transporter 1 inhibitors.

A. Kohara, S. Tsukamoto, S. Sakamoto, 2011, Journal of medicinal chemistry.

Synthesis and Pharmacological Evaluation of 3-[(4-Oxo-4H-pyrido[3,2-e][1,3]thiazin-2-yl)(phenyl)amino]propanenitrile Derivatives as Orally Active AMPA Receptor Antagonists.

H. Yamashita, M. Hirano, T. Yasunaga, 2019, Chemical & pharmaceutical bulletin.

Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists.

C. Kitada, S. Tsukamoto, H. Koshio, 2008, Bioorganic & medicinal chemistry.

AN EFFICIENT SYNTHESIS OF (±)-6,7-DIMETHOXY-1-OXO-2-(3-PIPERIDYL)-1,2,3,4-TETRAHYDROISOQUINOLINE

Toshihiro Watanabe, S. Tsukamoto, S. Sakamoto, 2001 .

A new synthetic route to YM087, an arginine vasopressin antagonist

T. Mase, S. Sakamoto, A. Tanaka, 2004 .

Atropisomeric 4-phenyl-4H-1,2,4-triazoles as selective glycine transporter 1 inhibitors.

Shuichi Sakamoto, Junji Miyata, Takashi Sugane, 2013, Journal of medicinal chemistry.

6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: structure-activity relationships for the AMPA-type non-NMDA receptor.

T. Furuya, K. Hidaka, M. Okada, 1994, Journal of medicinal chemistry.

Synthesis of 3"-epi-dihydrostreptomycin active against resistant bacteria.

H. Umezawa, S. Sakamoto, S. Umezawa, 1976, The Journal of antibiotics.

Synthesis and structure-activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V2 receptor agonists.

S. Tsukamoto, H. Koshio, S. Sakamoto, 2009, Bioorganic & medicinal chemistry.

Design, synthesis and biological activity of YM-60828 derivatives. Part 2: potent and orally-bioavailable factor Xa inhibitors based on benzothiadiazine-4-one template.

H. Kurihara, N. Katayama, Y. Matsumoto, 2003, Bioorganic & medicinal chemistry.

Novel AMPA receptor antagonists: synthesis and structure-activity relationships of 1-hydroxy-7-(1H-imidazol-1-yl)-6-nitro-2,3(1H,4H)- quinoxalinedione and related compounds.

M. Okada, S. Sakamoto, M. Shimizu‐Sasamata, 1996, Journal of medicinal chemistry.

Novel AMPA Receptor Antagonists: Synthesis and Structure-Activity Relationships of 1-Hydroxy-7-(1H-imidazol-1-yl)-6-nitro-2,3(1H,4H) quinoxalinedione and Related Compounds.

M. Okada, S. Sakamoto, M. Shimizu‐Sasamata, 1997 .

Novel α-Amino-3-hydroxy-5-methylisoxazole-4-propionate Receptor Antagonists: Synthesis and Structure−Activity Relationships of 6-(1H-Imidazol-1-yl)- 7-nitro-2,3(1H,4H)-pyrido[2,3-b]pyrazinedione and Related Compounds

M. Okada, H. Kubota, S. Sakamoto, 1996 .

Syntheses of 23-Dialkylamino-23-deoxydemycinosyltylosins and Conformational Study of Mycaminosyl Tylonolide by Nuclear Overhauser Difference Spectroscopy

A. Tanaka, T. Miyake, S. Sakamoto, 1984 .

Novel α-Amino-3-hydroxy-5-methylisoxazole-4-propionate Receptor Antagonists: Synthesis and Structure-Activity Relationships of 6-(1H- Imidazol-1-yl)-7-nitro-2,3(1H,4H)-pyrido(2,3-b)pyrazinedione and Related Compounds.

M. Okada, H. Kubota, S. Sakamoto, 1996 .

In‐vitro Characterization of YM872, a Selective, Potent and Highly Water‐soluble α‐Amino‐3‐hydroxy‐5‐methylisoxazole‐4‐propionate Receptor Antagonist

R. Tsutsumi, A. Kohara, Tokio Yamaguchi, 1998, The Journal of pharmacy and pharmacology.

YM872, a novel selective alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist, reduces brain damage after permanent focal cerebral ischemia in cats.

T. Toya, Masayasu Takahashi, S. Yatsugi, 1998, The Journal of pharmacology and experimental therapeutics.

(+/-)-2-(3-Piperidyl)-1,2,3,4-tetrahydroisoquinolines as a new class of specific bradycardic agents.

Toshihiro Watanabe, N. Masuda, S. Tsukamoto, 2003, Bioorganic & medicinal chemistry letters.

Synthesis and anti-inflammatory activity of 2,6-di-tert-butylphenols with a heterocyclic group at the 4-position. III.

H. Homma, Y. Isomura, K. Kubo, 1984, Chemical & pharmaceutical bulletin.

SYNTHESIS AND ANTIINFLAMMATORY ACTIVITY OF 2,6-DI-TERT-BUTYLPHENOLS WITH A HETEROCYCLIC GROUP AT THE 4-POSITION. III

H. Homma, Y. Isomura, K. Kubo, 1984 .

Neuroprotective Effect of YM90K, a Novel AMPA/Kainate Receptor Antagonist, in Focal Cerebral Ischemia in Cats

D. Uematsu, S. Sakamoto, M. Takahashi, 1996, Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism.

Studies on novel bone resorption inhibitors. II. Synthesis and pharmacological activities of fused aza-heteroarylbisphosphonate derivatives.

M. Takeuchi, Y. Isomura, H. Kurihara, 1998, Chemical & pharmaceutical bulletin.

Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.

S. Usuda, T. Mase, M. Matsumoto, 1996, Journal of medicinal chemistry.

Functional Characterization of YM928, a Novel Noncompetitive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist

H. Yamashita, N. Matsumoto, R. Tsutsumi, 2003, Journal of Pharmacology and Experimental Therapeutics.

Functional Characterization of YM928, a Novel Noncompetitive AMPA Receptor Antagonist

N. Matsumoto, R. Tsutsumi, M. Okada, 2003 .

Synthesis and structure-activity relationships of 6-{4-[(3-fluorobenzyl)oxy]phenoxy}nicotinamide derivatives as a novel class of NCX inhibitors: a QSAR study.

S. Sakamoto, A. Kakefuda, Ippei Sato, 2005, Bioorganic & medicinal chemistry.

Synthesis, structure-activity relationships, and anticonvulsant activities of 2-amino-4H-pyrido[3,2-e][1,3]thiazin-4-one derivatives as orally active AMPA receptor antagonists.

H. Yamashita, T. Yasunaga, S. Sakamoto, 2015, Bioorganic & medicinal chemistry.

The AMPA-receptor antagonist YM90K reduces AMPA receptor-mediated excitotoxicity in rat hippocampal cultures.

R. Tsutsumi, M. Okada, S. Sakamoto, 1998, Japanese journal of pharmacology.

8-(1H-imidazol-1-yl)-7-nitro-4(5H)-imidazo[1,2-alpha]quinoxalinone and related compounds: synthesis and structure-activity relationships for the AMPA-type non-NMDA receptor.

M. Okada, S. Sakamoto, M. Shimizu‐Sasamata, 1997, Journal of medicinal chemistry.