Výsledky vyhledávání - "Eiji, Kawaminami"

Design, Synthesis, and Structure–Activity Relationships Study of N-Pyrimidyl/Pyridyl-2-thiazolamine Analogues as Novel Positive Allosteric Modulators of M3 Muscarinic Acetylcholine Receptor

Autor: Hideyoshi Fuji, Eiji Kawaminami, Katsutoshi Ino, Taisuke Takahashi, Kenichiro Ishizu, Michinori Akaiwa, Hisashi Mihara, Risa Okimoto, Kenji Negoro, Hiroaki Tanaka

Publikováno v: Chemical and Pharmaceutical Bulletin. 69:360-373

The M3 muscarinic acetylcholine receptor (mAChR) plays an essential pharmacological role in mediating a broad range of actions of acetylcholine (ACh) released throughout the periphery and central nerve system (CNS). Nevertheless, its agonistic functi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::28c0b3aab3d69e27ded3b916ab532e73
https://doi.org/10.1248/cpb.c20-00877

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Effect of ASP6432, a Novel Type 1 Lysophosphatidic Acid Receptor Antagonist, on Urethral Function and Prostate Cell Proliferation

Autor: Shuichi Sato, Noriyuki Masuda, Kenichiro Ishizu, Naomi Hosogai, Kazuyuki Sakamoto, Masahiro Takeda, Koji Ueshima, Yukiko Noguchi, Eiji Kawaminami, Hisashi Yamakuni, Akiyoshi Ohtake

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 366:390-396

Current pharmacotherapies for lower urinary tract symptoms associated with benign prostate hyperplasia (LUTS/BPH) are in need of improvement. Lysophosphatidic acid (LPA) is a phospholipid with various biologic functions. However, its exact role in th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::105d42db2c18cca71276ebd6c385f610
https://doi.org/10.1124/jpet.118.247908

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Novel Malonamide Derivatives as .ALPHA.v.BETA.3 Antagonists. Syntheses and Evaluation of 3-(3-Indolin-1-yl-3-Oxopropanoyl)aminopropanoic Acids on Vitronectin Interaction with .ALPHA.v.BETA.3

Autor: Ken-Ichi Suzuki, Souichirou Kawazoe, Shin-ichi Tsukamoto, Shinya Nagashima, Eiji Kawaminami, Seijiro Akamatsu, Yuzo Matsumoto, Tetsuro Ogami, Minoru Okada

Publikováno v: Chemical and Pharmaceutical Bulletin. 49:1420-1432

In attempt to find novel integrin alphavbeta3 antagonists, we selected SC65811 and its guanidine analogue (1) as lead compounds. Modification of the glycine part of SC65811 led to a new series of malonamide derivatives that exhibited alphavbeta3 inhi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a303a44db30d3cde1457a20efecf759b
https://doi.org/10.1248/cpb.49.1420

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Studies on Aromatase Inhibitors IV. Synthesis and Biological Evaluation of N,N-Disubstituted-5-aminopyrimidine Derivatives

Autor: Yosiaki Shimada, Masafumi Kudou, Minoru Okada, Yasuo Isomura, Toru Yoden, Eiji Kawaminami

Publikováno v: Chemical and Pharmaceutical Bulletin. 45:1293-1299

In order to study the potency of the 5-aminopyrimidine skeleton as an aromatase inhibitor, we synthesized various N,N-disubstituted-5-aminopyrimidine derivatives and evaluated their aromatase-inhibitory activity (in vitro) and their inhibitory activi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38101a61fc9dcf24842ef55ad9d248fc
https://doi.org/10.1248/cpb.45.1293

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Studies on Aromatase Inhibitors. II. Synthesis and Biological Evaluation of 1-Amino-1H-1,2,4-triazole Derivatives

Autor: Yasuo Isomura, Yoshiaki Shimada, Toru Yoden, Minoru Okada, Eiji Kawaminami, Masafumi Kudoh

Publikováno v: Chemical and Pharmaceutical Bulletin. 45:333-337

1-N,N-Disubstituted amino-1-H-1,2,4-triazole derivatives were prepared and evaluated for aromatase-inhibitory activity (in vitro) and for the inhibitory activity on pregnant mare serum gonadotropin (PMSG)-induced estrogen synthesis (in vivo). 1-N-par

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbe09af60fb580a7069b6e86eab9ae56
https://doi.org/10.1248/cpb.45.333

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Studies on Aromatase Inhibitors. I. Synthesis and Biological Evaluation of 4-Amino-4H-1,2,4-triazole Derivatives

Autor: Masafumi Kudoh, Takashi Fujikura, Yasuo Isomura, Minoru Okada, Yoshiaki Shimada, Eiji Kawaminami, Hisataka Shikama, Toru Yoden

Publikováno v: Chemical and Pharmaceutical Bulletin. 44:1871-1879

Various 4-N-substituted amino-4H-1, 2, 4-triazole derivatives were synthesized and evaluated for aromatase-inhibitory activity (in vitro) and for pregnant mare serum gonadotropin (PMSG)-induced estrogen synthesis-inhibitory activity (in vivo). The 4-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea56f06ea1b25880de31c78c8302b362
https://doi.org/10.1248/cpb.44.1871

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ChemInform Abstract: Preparation of Novel Tricyclic Ring Systems Containing the Pyridazinone Ring

Autor: Mitsuru Furukawa, Yoshinari Okamoto, Tadashi Okawara, Eiji Kawaminami, Fumi Uchimura, Tetsuo Yamasaki

Publikováno v: ChemInform. 23

Novel tricyclic ring systems, irmdazo[3,4-d]pyridazino[4,5-b][1,4]thiazines 3, imidazo[2,1-b]pyridazino[4,5-e][1,3,4]thiadiazines 15 and 18 were prepared by the reaction of 5-amino-4-chloropyridazin-3(2H)-ones 1 and 5(4)-(1-methylhydrazino)-4(5)-chlo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b3254b525322b3afda84cd1b71e9aeda
https://doi.org/10.1002/chin.199250210

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ChemInform Abstract: Novel Heterocyclization of Hydrazinopyridazinones with Dimethyl Acetylenedicarboxylate with Dehydrogenation and Rearrangement

Autor: Tetsuo Yamasaki, Tadashi Okawara, Mitsuru Furukawa, T. Yamada, Eiji Kawaminami

Publikováno v: ChemInform. 22

5-Hydrazinopyridazin-3(2H)-ones 1 reacted with dimethyl acetylenedicarboxylate 2 to give 4,6-dihydropyridazino[4,5-c] pyridazin-5-(1H)-ones 3 by cyclization with dehydrogenation. On the other hand, the reaction of 4-bromo-5-hydrazino- and 5-bromo-4-h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::93e67efa1a7122ae64ac941cd0798d45
https://doi.org/10.1002/chin.199133196

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