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公开(公告)号：US08314148B2
公开(公告)日：2012-11-20
申请号：US13469427
申请日：2012-05-11
IPC分类号： A01N41/06 , C07C303/00 , C07D211/70
CPC分类号： C07C311/19 , C07B2200/09 , C07C311/29 , C07C311/42 , C07C311/46 , C07C311/47 , C07D213/42 , C07D295/13
摘要： The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译： 本发明提供式（I）化合物：所述化合物是MMP-9和/或MMP-12和/或MMP-13的抑制剂，因此可用于治疗以异常为特征的病症或疾病 MMP-9，和/或MMP-12和/或MMP-13的活性。 因此，式（I）化合物可用于治疗由MMP-9和/或MMP-12和/或MMP-13介导的疾病或疾病。 最后，本发明还提供药物组合物。
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公开(公告)号：US20120225882A1
公开(公告)日：2012-09-06
申请号：US13469427
申请日：2012-05-11
IPC分类号： C07C311/37 , A61P11/00 , A61P19/02 , A61P9/10 , A61P35/00 , A61P1/16 , A61P13/12 , A61P29/00 , A61P9/04 , A61P25/00 , A61K31/4453 , A61K31/5375 , A61K31/495 , A61K31/4462 , A61P35/04 , A61P11/06
CPC分类号： C07C311/19 , C07B2200/09 , C07C311/29 , C07C311/42 , C07C311/46 , C07C311/47 , C07D213/42 , C07D295/13
摘要： The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译： 本发明提供式（I）化合物：所述化合物是MMP-9和/或MMP-12和/或MMP-13的抑制剂，因此可用于治疗以异常为特征的病症或疾病 MMP-9和/或MMP-12和/或MMP-13的活性。 因此，式（I）化合物可用于治疗由MMP-9和/或MMP-12和/或MMP-13介导的疾病或疾病。 最后，本发明还提供药物组合物。
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公开(公告)号：US06353017B1
公开(公告)日：2002-03-05
申请号：US09643639
申请日：2000-08-22
申请人： Eva Altmann , Claudia Betschart , Keigo Gohda , Miyuki Horiuchi , Rene Lattmann , Martin Missbach , Junichi Sakaki , Michihiro Takai , Naoki Teno , Scott Douglas Cowen , Paul David Greenspan , Leslie Wighton McQuire , Ruben Alberto Tommasi , John Henry van Duzer
发明人： Eva Altmann , Claudia Betschart , Keigo Gohda , Miyuki Horiuchi , Rene Lattmann , Martin Missbach , Junichi Sakaki , Michihiro Takai , Naoki Teno , Scott Douglas Cowen , Paul David Greenspan , Leslie Wighton McQuire , Ruben Alberto Tommasi , John Henry van Duzer
IPC分类号： A61K3140
CPC分类号： C07C255/29 , C07C255/44 , C07C271/22 , C07C317/44 , C07C323/52 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D207/327 , C07D209/18 , C07D209/42 , C07D211/06 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/48 , C07D231/14 , C07D233/54 , C07D233/64 , C07D241/44 , C07D249/06 , C07D261/18 , C07D275/02 , C07D295/088 , C07D295/15 , C07D295/155 , C07D307/24 , C07D307/54 , C07D307/68 , C07D307/85 , C07D317/68 , C07D333/24 , C07D333/38 , C07D333/40 , C07D333/70 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/06043 , C07K5/06078
摘要： N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula I, or physiologically-acceptable and -cleavable esters or a salts thereof wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.
摘要翻译： 定义的N-末端取代的二肽腈可用作半胱氨酸组织蛋白酶的抑制剂，例如， 组织蛋白酶B，K，L和S，可用于治疗半胱氨酸组织蛋白酶依赖性疾病和病症，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松症，肿瘤（特别是肿瘤侵袭和肿瘤转移），冠状动脉疾病，动脉粥样硬化（包括 动脉粥样硬化斑块破裂和不稳定）。 特定的二肽腈是式I化合物或生理上可接受的和可切割的酯或其盐，其中符号如上所定义。特别地，已经发现通过适当选择基团R，R 2，R 3，R 4，R 5， X1，Y和L，化合物作为各种半胱氨酸组织蛋白酶类型的抑制剂的相对选择性，例如 组织蛋白酶B，K，L和S可以被改变，例如， 以获得选择性抑制特定组织蛋白酶类型或组织蛋白酶类型组合的抑制剂。
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公开(公告)号：US20090318511A1
公开(公告)日：2009-12-24
申请号：US12295170
申请日：2007-03-27
IPC分类号： A61K31/44 , C07C311/15 , C07D213/56 , A61K31/18 , A61P35/00
CPC分类号： C07C311/19 , C07B2200/09 , C07C311/29 , C07C311/42 , C07C311/46 , C07C311/47 , C07D213/42 , C07D295/13
摘要： The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译： 本发明提供式（I）化合物：所述化合物是MMP-9和/或MMP-12和/或MMP-13的抑制剂，因此可用于治疗以异常为特征的病症或疾病 MMP-9和/或MMP-12和/或MMP-13的活性。 因此，式（I）化合物可用于治疗由MMP-9和/或MMP-12和/或MMP-13介导的疾病或疾病。 最后，本发明还提供药物组合物。
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公开(公告)号：US08841291B2
公开(公告)日：2014-09-23
申请号：US14042652
申请日：2013-09-30
CPC分类号： C07C311/29 , A61K31/18 , C07C311/19 , C07C311/42 , C07C311/46 , C07C323/60 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/48 , C07D211/60 , C07D211/92 , C07D211/96 , C07D213/42 , C07D213/74 , C07D213/89 , C07D215/36 , C07D223/06 , C07D277/06 , C07D277/80 , C07D279/12 , C07D295/13 , C07D309/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D453/06 , C07D471/08 , C07D487/08
摘要： The present invention provides a compound of formula (I): said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
摘要翻译： 本发明提供式（I）化合物：所述化合物是MMP-12和/或MMP-13的抑制剂，因此可用于治疗特征为MMP-12异常活性和/ 或MMP-13。 因此，式（I）化合物可用于治疗由MMP-12和/或MMP-13介导的病症或疾病。 最后，本发明还提供了包含式（I）化合物的药物组合物。
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公开(公告)号：US20140031399A1
公开(公告)日：2014-01-30
申请号：US14042652
申请日：2013-09-30
IPC分类号： C07C311/29 , C07D213/42 , C07C311/19
CPC分类号： C07C311/29 , A61K31/18 , C07C311/19 , C07C311/42 , C07C311/46 , C07C323/60 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/48 , C07D211/60 , C07D211/92 , C07D211/96 , C07D213/42 , C07D213/74 , C07D213/89 , C07D215/36 , C07D223/06 , C07D277/06 , C07D277/80 , C07D279/12 , C07D295/13 , C07D309/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D453/06 , C07D471/08 , C07D487/08
摘要： The present invention provides a compound of formula (I): said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
摘要翻译： 本发明提供式（I）化合物：所述化合物是MMP-12和/或MMP-13的抑制剂，因此可用于治疗特征为MMP-12异常活性和/ 或MMP-13。 因此，式（I）化合物可用于治疗由MMP-12和/或MMP-13介导的病症或疾病。 最后，本发明还提供包含式（I）化合物的药物组合物。
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公开(公告)号：US08362063B2
公开(公告)日：2013-01-29
申请号：US13481983
申请日：2012-05-29
申请人： Ruben Alberto Tommasi , Michael Shultz , Leslie Wighton McQuire , Pascal Rigollier , Olivier Rogel , Claus Ehrhardt
发明人： Ruben Alberto Tommasi , Michael Shultz , Leslie Wighton McQuire , Pascal Rigollier , Olivier Rogel , Claus Ehrhardt
IPC分类号： A61K31/416 , C07D231/54
CPC分类号： C07D333/22 , A61K31/18 , A61K31/381 , A61K31/402 , A61K31/416 , A61K31/437 , A61K31/4402 , A61K31/4409 , A61K31/451 , A61K31/495 , A61K31/5375 , A61K31/55 , A61K45/06 , C07C311/16 , C07C311/29 , C07C311/39 , C07C311/46 , C07C317/24 , C07C323/67 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/20 , C07D207/30 , C07D207/333 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/80 , C07D209/82 , C07D211/06 , C07D211/14 , C07D211/24 , C07D213/40 , C07D213/50 , C07D213/61 , C07D221/16 , C07D223/04 , C07D231/56 , C07D235/06 , C07D235/08 , C07D241/04 , C07D265/30 , C07D295/112 , C07D295/116 , C07D295/192 , C07D333/18 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/04 , C07D471/04 , C07D487/04
摘要： The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
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公开(公告)号：US06812237B2
公开(公告)日：2004-11-02
申请号：US10275583
申请日：2002-11-07
申请人： Scott Douglas Cowen , Paul David Greenspan , Leslie Wighton McQuire , Ruben Alberto Tommasi , John Henry Van Duzer
发明人： Scott Douglas Cowen , Paul David Greenspan , Leslie Wighton McQuire , Ruben Alberto Tommasi , John Henry Van Duzer
IPC分类号： A61K31445
CPC分类号： C07D209/48 , A61K31/277 , C07C255/26 , C07C255/42 , C07C2601/14 , C07D209/08 , C07D209/20 , C07D209/46 , C07D213/56 , C07D213/79 , C07D233/64 , C07D257/04 , C07D263/58 , C07D277/20 , C07D277/56 , C07D277/62 , C07D307/68 , C07D307/88 , C07D333/36 , C07D333/38 , C07D409/12 , C07D471/04
摘要： Compounds of the formula (I), wherein R1 is aryl or biaryl; R2 is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; Y is O, S, SO, SO2, CO or NR6; R3 is hydrogen or lower alkyl; or R2 and R3 combined are C2-C7-alkylene or C2-C7-alkylene interrupted by Y; R4 is hydrogen or lower alkyl; R5 is hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; R6 is hydrogen, lower alkyl or aryl-lower alkyl; and pharmaceutically acceptable salts thereof, which are useful as cysteine cathepsin inhibitors
摘要翻译： 式（I）的化合物，其中R 1是芳基或联芳基; R2是芳基 - 低级烷基，联芳基 - 低级烷基，苯并稠合环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，芳氧基 - 低级烷基或其中C 2 -C 7 - 烷基被 Y; Y是O，S，SO，SO 2，CO或NR 6; R3是氢或低级烷基; 或R 2和R 3组合为C 2 -C 7亚烷基或被Y中断的C 2 -C 7亚烷基; R4是氢或低级烷基; R 5是氢，任选取代的低级烷基，芳基 - 低级烷基，联芳基 - 低级烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，芳氧基 - 低级烷基或其中C 2 -C 7 - 烷基是 被Y中断 R6是氢，低级烷基或芳基 - 低级烷基; 和其药学上可接受的盐，其可用作半胱氨酸组织蛋白酶抑制剂
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公开(公告)号：US08222424B2
公开(公告)日：2012-07-17
申请号：US12933988
申请日：2009-03-23
申请人： Claus Ehrhardt , Leslie Wighton McQuire , Pascal Rigollier , Olivier Rogel , Michael Shultz , Ruben Alberto Tommasi
发明人： Claus Ehrhardt , Leslie Wighton McQuire , Pascal Rigollier , Olivier Rogel , Michael Shultz , Ruben Alberto Tommasi
IPC分类号： C07D231/54 , A61K31/416
CPC分类号： C07D333/22 , A61K31/18 , A61K31/381 , A61K31/402 , A61K31/416 , A61K31/437 , A61K31/4402 , A61K31/4409 , A61K31/451 , A61K31/495 , A61K31/5375 , A61K31/55 , A61K45/06 , C07C311/16 , C07C311/29 , C07C311/39 , C07C311/46 , C07C317/24 , C07C323/67 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D207/20 , C07D207/30 , C07D207/333 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/80 , C07D209/82 , C07D211/06 , C07D211/14 , C07D211/24 , C07D213/40 , C07D213/50 , C07D213/61 , C07D221/16 , C07D223/04 , C07D231/56 , C07D235/06 , C07D235/08 , C07D241/04 , C07D265/30 , C07D295/112 , C07D295/116 , C07D295/192 , C07D333/18 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/04 , C07D471/04 , C07D487/04
摘要： The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译： 本发明提供式（I）化合物：所述化合物是MMP-2和/或MMP-8和/或MMP-9和/或MMP-12和/或MMP-13的抑制剂，因此 可以用于治疗以MMP-2，/或MMP-8和/或MMP-9，和/或MMP-12和/或MMP-13异常活性为特征的疾病或疾病。 因此，式（I）化合物可用于治疗由MMP-2和/或MMP-8和/或MMP-9和/或MMP-12和/或MMP- 13。 最后，本发明还提供药物组合物。
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10.发明申请公开(公告)号：US20110112076A1
公开(公告)日：2011-05-12
申请号：US13003406
申请日：2009-07-13
IPC分类号： C07C259/06 , C07D211/60 , C07D309/06 , C07D277/06 , C07D211/78 , C07D213/56 , C07D223/06 , C07D401/12 , C07D207/48 , C07D215/36 , C07D295/145 , C07D209/52 , C07D279/12 , C07D221/22 , C07D413/12 , C07D405/12 , C07D413/14 , C07D277/80 , A61K31/165 , A61K31/445 , A61K31/351 , A61K31/426 , A61K31/44 , A61K31/55 , A61K31/4709 , A61K31/40 , A61K31/47 , A61K31/5375 , A61K31/403 , A61K31/54 , A61K31/439 , A61K31/536 , A61K31/4433 , A61K31/5377 , A61K31/428 , A61P11/06 , A61P11/02 , A61P11/08 , A61P19/02 , A61P9/10 , A61P35/00 , A61P35/04 , A61P1/02 , A61P9/04 , A61P9/00 , A61P43/00
CPC分类号： C07C311/29 , A61K31/18 , C07C311/19 , C07C311/42 , C07C311/46 , C07C323/60 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/48 , C07D211/60 , C07D211/92 , C07D211/96 , C07D213/42 , C07D213/74 , C07D213/89 , C07D215/36 , C07D223/06 , C07D277/06 , C07D277/80 , C07D279/12 , C07D295/13 , C07D309/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D453/06 , C07D471/08 , C07D487/08
摘要： The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
摘要翻译： 本发明提供式（I）化合物，所述化合物是MMP-12和/或MMP-13的抑制剂，因此可用于治疗以MMP-12异常活性为特征的疾病或疾病和/或 MMP-13。 因此，式（I）化合物可用于治疗由MMP-12和/或MMP-13介导的病症或疾病。 最后，本发明还提供包含式（I）化合物的药物组合物。
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