Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56Lck inhibitors

被引：34

作者：

Ping, C

Norris, D

Das, J

Spergel, SH

Wityak, J

Leith, L

Zhao, RL

Chen, BC

Pitt, S

Pang, SH

Ding, RS

Zhang, R

De Fex, HF

Doweyko, AM

McIntyre, KW

Shuster, DJ

Behnia, K

Schieven, GL

Barrish, JC

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Discovery Chem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Immunol Inflammat & Pulm Drug Discovery, Princeton, NJ 08543 USA

[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Macromol Sci, Princeton, NJ 08543 USA

[4] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Metab & Pharmacokinet, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 24期

关键词：

Lck inhibitor; pan-Src-family inhibitor;

D O I：

10.1016/j.bmcl.2004.09.093

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of substituted 2-(aminoheteroaryl)-thiazole-5-carboxamide analogs have been synthesized as novel, potent inhibitors of the Src-family kinase p56(Lck). Among them, compound 2 displayed superior in vitro potency and excellent in vivo efficacy. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：6061 / 6066

页数：6

共 25 条

[21] The Discovery of Polo-Like Kinase 4 Inhibitors: Identification of (1R,2S)-2-(3((E)-4-(((cis)-2,6-Dimethylmorpholino)methyl)styryl)-1H-indazol-6-yl)-5′-methoxyspiro[cyclopropane-1,3′-indolin]-2′-one (CFI-400945) as a Potent, Orally Active Antitumor Agent
Sampson, Peter B.
Liu, Yong
Forrest, Bryan
Cumming, Graham
Li, Sze-Wan
Patel, Narendra Kumar
Edwards, Louise
Laufer, Radoslaw
Feher, Miklos
Ban, Fuqiang
Awrey, Donald E.
Mao, Guodong
Plotnikova, Olga
Hodgson, Richard
Beletskaya, Irina
Mason, Jacqueline M.
Luo, Xunyi
Nadeem, Vincent
Wei, Xin
Kiarash, Reza
Madeira, Brian
Huang, Ping
Mak, Tak W.
Pan, Guohua
Pauls, Henry W.
JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (01) : 147 - 169
[22] Novel inhibitor of p38 map kinase as an anti-TNF-&alpha drug:: Discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatic agent.
Miwatashi, S
Arikawa, Y
Kotani, E
Miyamoto, M
Naruo, K
Kimura, H
Tanaka, T
Asahi, S
Ohkawa, S
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 229 : U130 - U130
[23] Novel inhibitor of p38 MAP kinase as an anti-TNF-α drug:: Discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent
Miwatashi, S
Arikawa, Y
Kotani, E
Miyamoto, M
Naruo, K
Kimura, H
Tanaka, T
Asahi, S
Ohkawa, S
JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (19) : 5966 - 5979
[24] Discovery of 2-(6-{[(1R,2R)-2-hydroxycyclohexyl] amino}-4,5-dimethylpyridazin-3-yl)-5-(trifluoromethyl)phenol (ASP0965): A potent, orally active and brain-penetrable NLRP3 inflammasome inhibitor with a novel scaffold for the treatment of α-synucleinopathy
Inagaki, Yusuke
Kamikubo, Takashi
Kuriwaki, Ikumi
Watanabe, Junko
Yamaki, Susumu
Iida, Maiko
Tomita, Kyoko
Kakefuda, Kenichi
Kurokawa, Jun
Kiso, Tetsuo
Saba, Kengo
Koike, Takanori
BIOORGANIC & MEDICINAL CHEMISTRY, 2025, 118
[25] MEDI 76-Discovery of N-{(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-[(dimethylamino)carbonyl]cyclohexyl}-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride (DT-831j): A novel, potent and orally active direct inhibitor of factor Xa
Nagata, Tsutomu
Yoshino, Toshiharu
Haginoya, Noriyasu
Yoshikawa, Kenji
Nagamochi, Masatoshi
Kobayashi, Shozo
Komoriya, Satoshi
Yokomizo, Aki
Muto, Ryo
Yamaguchi, Mitsuhiro
Osanai, Ken
Suzuki, Makoto
Kanno, Hideyuki
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2007, 234

← 1 2 3 →