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2- 2-ANTI INFLAMMATORY 2-OXOTHIAZOLES AND 2-OXOOXAZOLES
专利权人:
아벡신 에이에스
发明人:
코코토스 조지,요한슨 베리트,마그리오티 빅토리아,차코스 마이클
申请号:
KR1020187028820
公开号:
KR1020180114228A
申请日:
2010.10.01
申请国别(地区):
KR
年份:
2018
代理人:
摘要:
The present invention relates to compounds of formula (I), or salts, esters, solvates, N-oxides or prodrugs thereof, for the treatment of chronic inflammatory diseases: Formula I In this formula, X is O or S; R 1 and R 2 are each independently H, OH, SH, nitro, NH 2, NHC 1-6 alkyl, N (C 1-6 alkyl) 2, halo, halo-C 1-6 alkyl, CN, C 1- 6 alkyl, OC 1-6 alkyl, C 1-6 alkyl, COOH, C 1-6 alkyl, COOC 1-6 alkyl, C 2-6 alkenyl, C 3-10 cycloalkyl, C 6-10 aryl, C 1- 6 alkyl, C 6-10 aryl, heterocyclyl, heteroaryl, CONH 2, CONHC 1-6 alkyl, CON (C 1-6 alkyl) 2, OCOC 1-6 alkyl, or an acidic group such as a carboxyl group, a phosphate group , A phosphinate group, a sulfate group, a sulfonate group or a group including a tetrazolyl group; R 1 and R 2 together may form a six-membered aromatic ring optionally substituted by up to four R 5 groups; R 3 is H, halo (preferably fluoro) or CHal 3 (preferably CF 3 ); Each R 5 is as defined for R 1 ; V 1 is a covalent bond, a C 1-20 alkyl group, a C 2-20 -unsaturated alkenyl group or a C 2-20 -multi -unsaturated alkenyl group, wherein the alkyl or alkenyl group is O, NH, N (C 1-6 alkyl), S, SO and SO 2 ; M 1 is absent or is a C 5-10 cyclic group or a C 5-15 aromatic group; R 4 is H, halo, OH, CN, nitro, NH 2, NHC 1-6 alkyl, N (C 1-6 alkyl) 2, halo-C 1-6 alkyl, C 1-20 alkyl group, C 2-20 - a monounsaturated alkenyl group or a C 2-20 -multi -unsaturated alkenyl group, wherein said C 1-20 alkyl group or C 2-20 alkenyl group is optionally replaced by O, NH, N (C 1-6 alkyl), S, SO and SO <; 2 >;; only All V 1 M 1 R 4 Group provides four or more skeletal atoms from the C (R <; 3 >;) group.본 발명은 만성 염증 질환을 치료하기 위한 하기 화학식 I의 화합물, 또는 이의 염, 에스터, 용매화물, N-산화물 또는 전구약물에 관한 것이다:화학식 I상기 식에서,X는 O 또는 S이고; R1 및 R2는 각각 독립적으로 H, OH, SH, 니트로, NH2, NHC1-6 알킬, N(C1-6 알킬)2, 할로, 할로C1-6 알킬, CN, C1-6 알킬, OC1-6 알킬, C1-6 알킬COOH, C1-6 알킬COOC1-6 알킬, C2-6 알케닐, C3-10 사이클로알킬, C6-10 아릴, C1-6 알킬C6-10 아릴, 헤테로사이클릴, 헤테로아릴, CONH2, CONHC1-6 알킬, CON(C1-6 알킬)2, OCOC1-6
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