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    • 12. 发明专利
      AT502922T  未知
    • AT502922T
    • 2011-04-15
    • AT08163972
    • 2004-09-10
    • GLAXO GROUP LTD
    • GAINES SIMON , HOLMES IAN PETER , MARTIN STEPHEN LEWIS , WATSON STEPHEN PAUL
    • C07D209/48 , A61K31/4035 , A61K31/505 , A61K31/506 , A61P29/00 , C07D239/54 , C07D403/10 , C07D405/10
    • Compounds of Formula (I): Wherein: A represents bond, C 1-6 alkyl or CH=CH-C 1-4 alkyl; B represents bond, O, S, SO, SO 2 , CO, CR 7 R 8 , CO 2 R 14 , CONR 14 R 15 , N(COR 14 )(COR 15 ), N(SO 2 R 14 )(COR 15 ) or NR 14 R 15 ; D represents bond, or C 1-6 alkyl; 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, SO 2 , CO, CNR 5 , CNOR 5 , CNNR 5 R 6 , NR 11 or CR 7 R 8 ; Y represents CR 5 OR 11 , CR 5 SR 11 , NOR 5 , CR 5 NR 6 R 11 , SO, SO 2 , CO, CNR 5 , CNOR 5 or CS; R 1 and R 1' each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 2 represents CO 2 R 12 , CH 2 OR 12 or CONR 12 R 13 , CONR 12 OR 13 , NR 12 COR 13 , SR 12 , PO(OH) 2 , PONHR 12 or SONHR 12 ; R 3 represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH 2 , O, S, SO, SO 2 , NR 5 , OCR 5 R 6 , CR 9 R 10 O or Z, R 4 and Q together form an optionally substituted fused tricyclic group; R 5 and R 6 each independently represent H, C 1-6 alkyl or C 1-4 alkylaryl; R 7 and R 8 each independently represent H, halo, C 1-6 alkyl or C 1-4 alkylaryl; R 9 and R 10 each independently represents H, C 1-6 alkyl optionally substituted by halo, cyano, OR 11 or NR 6 R 11 , C 1-4 alkylaryl optionally substituted by halo, cyano, OR11 or NR 6 R 11 , OR 11 or, together with the N to which they are attached, R 9 and R 10 form a heterocyclic group: R 11 represents H, C 1-6 alkyl, C 1-4 alkylaryl or COR 5 ; R 12 and R 13 each independently represent H, C 1-3 alkyl, C 1-3 alkylaryl or C 1-3 alkylheteroaryl or, together with the functionality to which they are attached, R 12 and R 13 form a heterocyclic group: R 14 and R 15 each independently represent H, C 1-6 alkyl, C 1-4 alkylaryl or C 1-4 alkylheteroaryl or together with the functionality to which they are attached R 14 and R 15 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 14. 发明专利
      DK1663970T3  未知
    • DK1663970T3
    • 2009-01-12
    • DK04765231
    • 2004-09-10
    • GLAXO GROUP LTD
    • GAINES SIMON , HOLMES IAN PETER , MARTIN STEPHEN LEWIS , WATSON STEPHEN PAUL
    • C07D209/48 , A61K31/4035 , A61K31/505 , A61K31/506 , A61P29/00 , C07D239/54 , C07D403/10 , C07D405/10
    • Compounds of Formula (I): Wherein: A represents bond, C 1-6 alkyl or CH=CH-C 1-4 alkyl; B represents bond, O, S, SO, SO 2 , CO, CR 7 R 8 , CO 2 R 14 , CONR 14 R 15 , N(COR 14 )(COR 15 ), N(SO 2 R 14 )(COR 15 ) or NR 14 R 15 ; D represents bond, or C 1-6 alkyl; 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, SO 2 , CO, CNR 5 , CNOR 5 , CNNR 5 R 6 , NR 11 or CR 7 R 8 ; Y represents CR 5 OR 11 , CR 5 SR 11 , NOR 5 , CR 5 NR 6 R 11 , SO, SO 2 , CO, CNR 5 , CNOR 5 or CS; R 1 and R 1' each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 2 represents CO 2 R 12 , CH 2 OR 12 or CONR 12 R 13 , CONR 12 OR 13 , NR 12 COR 13 , SR 12 , PO(OH) 2 , PONHR 12 or SONHR 12 ; R 3 represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH 2 , O, S, SO, SO 2 , NR 5 , OCR 5 R 6 , CR 9 R 10 O or Z, R 4 and Q together form an optionally substituted fused tricyclic group; R 5 and R 6 each independently represent H, C 1-6 alkyl or C 1-4 alkylaryl; R 7 and R 8 each independently represent H, halo, C 1-6 alkyl or C 1-4 alkylaryl; R 9 and R 10 each independently represents H, C 1-6 alkyl optionally substituted by halo, cyano, OR 11 or NR 6 R 11 , C 1-4 alkylaryl optionally substituted by halo, cyano, OR11 or NR 6 R 11 , OR 11 or, together with the N to which they are attached, R 9 and R 10 form a heterocyclic group: R 11 represents H, C 1-6 alkyl, C 1-4 alkylaryl or COR 5 ; R 12 and R 13 each independently represent H, C 1-3 alkyl, C 1-3 alkylaryl or C 1-3 alkylheteroaryl or, together with the functionality to which they are attached, R 12 and R 13 form a heterocyclic group: R 14 and R 15 each independently represent H, C 1-6 alkyl, C 1-4 alkylaryl or C 1-4 alkylheteroaryl or together with the functionality to which they are attached R 14 and R 15 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 16. 发明专利
      MA28039A1 INHIBITEURS DE METALLOPROTEINASES MATRICIELLES 未知
    • INHIBITEURS DE METALLOPROTEINASES MATRICIELLES
    • MA28039A1
    • 2006-07-03
    • MA28873
    • 2006-03-14
    • GLAXO GROUP LTD
    • GAINES SIMON , HOLMES IAN PETER , MARTIN STEPHEN LEWIS , WATSON STEPHEN PAUL
    • A61K31/4035 , A61K31/505 , A61K31/506 , A61P29/00 , C07D209/48 , C07D239/54 , C07D403/10 , C07D405/10
    • L'invention concerne des composés représentés par la formule (I), dans laquelle A représente une liaison, C1-6 alkyle ou CH=CH-C1-4 alkyle; B représente une liaison, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) ou NR14R15; D représente une liaison ou C1-6 alkyle; E représente aryle substitué, eu hétéroaryle substitué ou non substitué; Q représente un noyau aryle ou hétéroaryle à 5 ou 6 chaînons éventuellement substitué; X représente O, S, SO, SO2. CO, CNR5, CNOR5, CNNR5R6, NR11 OU CR7R8; Y représente CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 ou CS; R1 and R1' représentent chacun indépendamment H, C1-6 alkyle ou C1-4 alkylaryle; R2 représente CO2R12, CH2OR12 ou CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 ou SONHR12; R3 représente H, C1-6 alkyle ou C1-4 alkylaryle; R4 représente aryle ou hétéroaryle éventuellement substitué; Z représente une liaison, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9Rl0O ou Z, R4 et Q formant ensemble un groupe tricyclique fusionné éventuellement substitué; R5 et R6 représentent chacun indépendamment H, C1-6 alkyle ou C1-4 alkylaryle; R7 et R8 représentent chacun indépendamment H, halc, C1-6 alkyle ou C1-4 alkylaryle; R9 et R10 représentent chacun indépendamment H, C1-6 alkyle éventuellement substitué par halo, cyano, OR11 ou NR6R11, C14 alkylaryle éventuellement substitué par halo, cyano, OR11 ou NR6R11, ou R9 et R10 forment un groupe hétérocyclique avec l'atome N auquel ils sont liés ; R11 représente H, C1-6 alkyle, C1-4 alkylaryle ou COR5; R12 et R13 représentent indépendamment H, C1-3 alkyle, C1-3 alkylaryle ou C1-3 alkylhétéroaryle, ou R12 et R13 forment un groupe hétérocyclique avec la fonctionnalité à laquelle ils sont liés ; R14 et R15 représentent chacun indépendamment H, C1-6 alkyle, C1-4 alkylaryle ou C1-4 alkylhétéroaryle, ou forment avec la fonctionnalité à laquelle ils sont liés un groupe hétérocyclique ou un groupe hétérocyclique fusionné. L'invention concerne aussi des dérivés physiologiquement fonctionnels de ces composés, des procédés de préparation de ceux-ci, des formulations pharmaceutiques les contenant et leur utilisation comme inhibiteurs des enzymes métalloprotéinases matricielles (MMP).
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 17. 发明专利
      CA2538315A1 MATRIX METALLOPROTEINASE INHIBITORS 未知
    • MATRIX METALLOPROTEINASE INHIBITORS
    • CA2538315A1
    • 2005-03-24
    • CA2538315
    • 2004-09-10
    • GLAXO GROUP LTD
    • GAINES SIMON , MARTIN STEPHEN LEWIS , HOLMES IAN PETER , WATSON STEPHEN PAUL
    • C07D209/48 , A61K31/4035 , A61K31/505 , A61K31/506 , A61P29/00 , C07D239/54 , C07D403/10 , C07D405/10
    • Compounds of Formula (I): Wherein: A represents bond, C1-6alkyl or CH=CH-C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2 R14, 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, NR12COR1 3, 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 eac h 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 ea ch 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 ar e attached, R12 and R13 form a heterocyclic group: R14 and R15 each independently represent H, C1-6 alkyl, C1-4 alkylaryl or C1-4 alkylheteroary l or together with the functionality to which they are attached R14 and R15 fo rm 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 20. 发明专利
      HRP20080668T3 MATRIX METALLOPROTEINASE INHIBITORS 未知
    • MATRIX METALLOPROTEINASE INHIBITORS
    • HRP20080668T3
    • 2009-02-28
    • HRP20080668
    • 2008-12-19
    • GLAXO GROUP LTD
    • GAINES SIMON , HOLMES IAN PETER , MARTIN STEPHEN LEWIS , WATSON STEPHEN PAUL
    • C07D209/48 , A61K31/4035 , A61K31/505 , A61K31/506 , A61P29/00 , C07D239/54 , C07D403/10 , C07D405/10
    • Compounds of Formula (I): Wherein: A represents bond, C 1-6 alkyl or CH=CH-C 1-4 alkyl; B represents bond, O, S, SO, SO 2 , CO, CR 7 R 8 , CO 2 R 14 , CONR 14 R 15 , N(COR 14 )(COR 15 ), N(SO 2 R 14 )(COR 15 ) or NR 14 R 15 ; D represents bond, or C 1-6 alkyl; 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, SO 2 , CO, CNR 5 , CNOR 5 , CNNR 5 R 6 , NR 11 or CR 7 R 8 ; Y represents CR 5 OR 11 , CR 5 SR 11 , NOR 5 , CR 5 NR 6 R 11 , SO, SO 2 , CO, CNR 5 , CNOR 5 or CS; R 1 and R 1' each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 2 represents CO 2 R 12 , CH 2 OR 12 or CONR 12 R 13 , CONR 12 OR 13 , NR 12 COR 13 , SR 12 , PO(OH) 2 , PONHR 12 or SONHR 12 ; R 3 represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH 2 , O, S, SO, SO 2 , NR 5 , OCR 5 R 6 , CR 9 R 10 O or Z, R 4 and Q together form an optionally substituted fused tricyclic group; R 5 and R 6 each independently represent H, C 1-6 alkyl or C 1-4 alkylaryl; R 7 and R 8 each independently represent H, halo, C 1-6 alkyl or C 1-4 alkylaryl; R 9 and R 10 each independently represents H, C 1-6 alkyl optionally substituted by halo, cyano, OR 11 or NR 6 R 11 , C 1-4 alkylaryl optionally substituted by halo, cyano, OR11 or NR 6 R 11 , OR 11 or, together with the N to which they are attached, R 9 and R 10 form a heterocyclic group: R 11 represents H, C 1-6 alkyl, C 1-4 alkylaryl or COR 5 ; R 12 and R 13 each independently represent H, C 1-3 alkyl, C 1-3 alkylaryl or C 1-3 alkylheteroaryl or, together with the functionality to which they are attached, R 12 and R 13 form a heterocyclic group: R 14 and R 15 each independently represent H, C 1-6 alkyl, C 1-4 alkylaryl or C 1-4 alkylheteroaryl or together with the functionality to which they are attached R 14 and R 15 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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