专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2005026120A1 MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：WO2005026120A1
公开(公告)日：2005-03-24
申请号：PCT/EP2004/010319
申请日：2004-09-10
申请人： GLAXO GROUP LIMITED , GAINES, Simon , HOLMES, Ian, Peter , MARTIN, Stephen, Lewis , WATSON, Stephen, Paul
发明人： GAINES, Simon , HOLMES, Ian, Peter , MARTIN, Stephen, Lewis , WATSON, Stephen, Paul
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10
摘要： Compounds of Formula (I): Wherein: A represents bond, C1-6alkyl or CH=CH-C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1' each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl; R7 and R8 each independently represent H, halo, C1-6 alkyl or C1-4 alkylaryl; R9 and R10 each independently represents H, C1-6 alkyl optionally substituted by halo, cyano, OR11 or NR6R11 , C1-4 alkylaryl optionally substituted by halo, cyano, OR11 or NR6R11, OR11 or, together with the N to which they are attached, R9 and R10 form a heterocyclic group: R11 represents H, C1-6 alkyl, C1-4 alkylaryl or COR5; R12 and R13 each independently represent H, C1-3 alkyl, C1-3 alkylaryl or C1-3 alkylheteroaryl or, together with the functionality to which they are attached, R12 and R13 form a heterocyclic group: R14 and R15 each independently represent H, C1-6 alkyl, C1-4 alkylaryl or C1-4 alkylheteroaryl or together with the functionality to which they are attached R14 and R15 form a heterocyclic or fused heterocyclic group: and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metallproteinase enzymes (MMPs) are described.
摘要翻译：式（I）化合物：其中：A表示键，C 1-6烷基或CH = CH-C 1-4烷基; B代表键，O，S，SO，SO2，CO，CR7R8，CO2R14，CONR14R15，N（COR14）（COR15），N（SO2R14）（COR15）或NR14R15; D表示键或C 1-6烷基; E表示取代的芳基或取代或未取代的杂芳基; Q表示任选取代的5或6元芳基或杂芳基环; X表示O，S，SO，SO 2，CO，CNR 5，CNOR 5，CNNR 5 R 6，NR 11或CR 7 R 8; Y代表CR5OR11，CR5SR11，NOR5，CR5NR6R11，SO，SO2，CO，CNR5，CNOR5或CS; R 1和R 1'各自独立地表示H，C 1-6烷基或C 1-4烷基芳基; R2代表CO 2 R 12，CH 2 OR 12或CONR 12 R 13，CONR 12 OR 13，NR 12 COR 13，SR 12，PO（OH）2，PONHR 12或SONHR 12; R3表示H，C1-6烷基或C1-4烷基芳基; R 4表示任选取代的芳基或杂芳基; Z表示键，CH2，O，S，SO，SO2，NR5，OCR5R6，CR9R10O或Z，R4和Q一起形成任选取代的稠合三环基团; R5和R6各自独立地表示H，C1-6烷基或C1-4烷基芳基; R 7和R 8各自独立地表示H，卤素，C 1-6烷基或C 1-4烷基芳基; R 9和R 10各自独立地表示H，任选被卤素，氰基，OR 11或NR 6 R 11取代的C 1-6烷基，任选被卤素，氰基，OR 11或NR 6 R 11，OR 11取代的C 1-4烷基芳基或与它们相连的N R 9和R 10形成杂环基：R 11表示H，C 1-6烷基，C 1-4烷基芳基或COR 5; R 12和R 13各自独立地表示H，C 1-3烷基，C 1-3烷基芳基或C 1-3烷基杂芳基，或者与它们所连接的官能团一起，R 12和R 13形成杂环基：R 14和R 15各自独立地表示H， C 1-6烷基，C 1-4烷基芳基或C 1-4烷基杂芳基或与它们所连接的官能团一起R14和R15形成杂环或稠合杂环基团及其生理功能衍生物，其制备方法，含有它们的药物制剂并且其用作基质金属蛋白酶（MMP）的抑制剂。

IPRDB

热门服务

关于我们

友情链接

联系方式