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1. CN1278247 - Alpha-hydroxy, amino and -fluoro derivatives of beta-sulphenyl hydroxamic acids matrix metalloproteinases inhibitors

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Office
China
Application Number 98810691.4
Application Date 18.11.1998
Publication Number 1278247
Publication Date 27.12.2000
Grant Number 1168709
Grant Date 29.09.2004
Publication Kind C
IPC
C07C 317/46
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
44having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
46the carbon skeleton being further substituted by singly-bound oxygen atoms
C07C 317/44
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
317Sulfones; Sulfoxides
44having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
CPC
A61P 1/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 13/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
A61P 13/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
10of the bladder
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
Applicants Pharmacia & Upjhn Co.
厄普约翰药物公司
Inventors Martha A. Warpehoski
马萨·A·沃普霍斯金
Mark Allen Mitchell
马克·艾伦·米切尔
Donald E. Harper
唐纳德·E·哈珀
琳达·路易斯·马乔拉
Agents cang jianmeng
北京银龙知识产权代理有限公司
Priority Data 60/072,655 21.11.1997 US
Title
(EN) Alpha-hydroxy, amino and -fluoro derivatives of beta-sulphenyl hydroxamic acids matrix metalloproteinases inhibitors
(ZH) 作为基质金属蛋白酶抑制剂的β－磺酰基异羟肟酸的α－羟基、－氨基和卤代衍生物
Abstract
(EN) The present invention provides a compound of formula (I), or pharmaceutical acceptable salts thereof wherein R1 is C4-12 alkyl, C4-12 alkenyl, C4-12 alkynyl, -(CH2)h-C3-8 cycloalkyl, substituted and unsubstituted -(CH2)h-aryl, substituted and unsubstituted-(CH2)h-het, R2 is substituted and unsubstituted C1-12 alkyl, substituted and unsubstituted C2-12 alkenyl, substituted and unsubstituted C2-12 alkynyl, substituted and unsubstituted-(CH2)h-C3-8 cycloakyl, substituted and unsubstituted -(CH2)h-C3-8 cycloalkenyl, substituted and unsubstituted -(CH2)h-aryl, substituted and unsubstituted -(CH2)h-heterocyclic ring, substituted and unsubstituted -(CH2)i-X-R4 (X is -O-, -S(=O)j-, -NR7-, -S(=O)2NR8-, or -C(=O)-), and -(CH2)iCHR5R6. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation.
(ZH)

本发明提供通式I化合物或其可药用盐，其中R1是C4-12烷基，C4-12链烯基，C4-12炔基，-(CH2)h-C3-8环烷基，取代的和未取代的-(CH2)h-芳基，取代的和未取代的-(CH2)h-het；R2是取代的和未取代的C1-12烷基，取代的和未取代的C2-12链烯基，取代的和未取代的C2-12炔基，取代的和未取代的-(CH2)h-C3-8环烷基，取代的和未取代的-(CH2)h-C3-8环链烯基，取代的和未取代的-(CH2)h-芳基，取代的和未取代的-(CH2)h-杂环，取代的和未取代-(CH2)i-X-R4(X是-O-，-S(＝O)j-，-NR7-，-S(＝O)2NR8-，或-C(＝O))以及-(CH2)hCHR5R6。该化合物是涉及组织降解的基质金属蛋白酶的抑制剂。
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