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1. (CN101218207) Cathepsin cysteine protease inhibitors

Office : China
Application Number: 200680024616.6 Application Date: 05.07.2006
Publication Number: 101218207 Publication Date: 09.07.2008
Publication Kind : A
Prior PCT appl.: Application Number:PCTCA2006001104 ; Publication Number:2007003056 Click to see the data
IPC:
C07D 231/12
A61K 31/415
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
12
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
CPC:
C07D 231/12
Applicants: Merck Frosst Canada Ltd.
默克弗罗斯特加拿大有限公司
Inventors: Black Cameron
C·布莱克
Crane Sheldon
S·克兰
Oballa Renata
R·奥巴拉
Robichaud Joel
J·罗比肖
Agents: duanxiao ling lilian tao
中国专利代理(香港)有限公司
中国专利代理(香港)有限公司
Priority Data: 60/696,970 06.07.2005 US
Title: (EN) Cathepsin cysteine protease inhibitors
(ZH) 组织蛋白酶半胱氨酸蛋白酶抑制剂
Abstract: front page image
(EN) This invention relates to a novel class of compounds, represented by the formula below, wherein the meanings of R<1> , R<2> and R<3> are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsms K, L, S and B These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis, osteoarthritis and rheumatoid arthritis.
(ZH)

本发明涉及一类新的化合物,由右式表示,其中R1、R2、和R3的含义由本文表示,其为半胱氨酸蛋白酶抑制剂,包括但不限于组织蛋白酶K、L、S和B。这些化合物适用于治疗其中显示了骨吸收抑制的疾病,例如骨质疏松、骨关节炎和类风湿性关节炎。


Also published as:
EP1902031JP2009500300US20090093444CN103172568CA2614070AU2006265735
IN259/DELNP/2008WO/2007/003056