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公开(公告)号:US20060089357A1
公开(公告)日:2006-04-27
申请号:US11296782
申请日:2005-12-07
申请人: Michael Graupe , James Palmer , John Patterson , Stephen Pickett , David Aldous , Sukanthini Thurairatnam , Andreas Timm , Frank Halley , Justine Lai , John Link , Jiayao Li
发明人: Michael Graupe , James Palmer , John Patterson , Stephen Pickett , David Aldous , Sukanthini Thurairatnam , Andreas Timm , Frank Halley , Justine Lai , John Link , Jiayao Li
IPC分类号: A61K31/537 , C07D265/30
CPC分类号: C07D213/40 , A61K31/4245 , A61K31/5375 , A61K31/5377 , C07C317/44 , C07C323/60 , C07D205/08 , C07D207/24 , C07D213/75 , C07D223/12 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/26 , C07D277/64 , C07D285/08 , C07D295/185 , C07D413/04 , C07D413/12
摘要: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
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公开(公告)号:US20070049594A1
公开(公告)日:2007-03-01
申请号:US11295890
申请日:2005-12-07
申请人: Michael Graupe , John Patterson , David Aldous , Sukanthini Thurairatnam , Andreas Timm , John Link , Jiayao Li , Stephen Pickett , Frank Halley , Justine Lai
发明人: Michael Graupe , John Patterson , David Aldous , Sukanthini Thurairatnam , Andreas Timm , John Link , Jiayao Li , Stephen Pickett , Frank Halley , Justine Lai
IPC分类号: A61K31/501 , A61K31/50 , A61K31/4965 , A61K31/497 , C07D417/02 , C07D413/02
CPC分类号: C07D207/273 , A61K31/5375 , A61K31/5377 , C07C317/44 , C07C323/60 , C07D205/08 , C07D207/24 , C07D213/40 , C07D223/10 , C07D223/12 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/26 , C07D277/64 , C07D285/08 , C07D295/185 , C07D413/04 , C07D413/12 , Y02A50/411
摘要: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译: 本发明涉及新的选择性组织蛋白酶S抑制剂,其药学上可接受的盐和N-氧化物,它们作为治疗剂的用途及其制备方法。
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公开(公告)号:US07064123B1
公开(公告)日:2006-06-20
申请号:US10035783
申请日:2001-12-24
申请人: Michael Graupe , John W. Patterson , Stephen D. Pickett , John O. Link , Jiayao Li , David Aldous , Sukanthini Thurairatnam , Andreas P. Timm , Frank Halley , Justine Lai Yeun Quai
发明人: Michael Graupe , John W. Patterson , Stephen D. Pickett , John O. Link , Jiayao Li , David Aldous , Sukanthini Thurairatnam , Andreas P. Timm , Frank Halley , Justine Lai Yeun Quai
IPC分类号: A61K31/535 , C07D295/00 , A61P29/00
CPC分类号: C07D207/273 , A61K31/5375 , A61K31/5377 , C07C317/44 , C07C323/60 , C07D205/08 , C07D207/24 , C07D213/40 , C07D223/10 , C07D223/12 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/26 , C07D277/64 , C07D285/08 , C07D295/185 , C07D413/04 , C07D413/12 , Y02A50/411
摘要: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译: 本发明涉及新的选择性组织蛋白酶S抑制剂,其药学上可接受的盐和N-氧化物,它们作为治疗剂的用途及其制备方法。
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公开(公告)号:US07030116B2
公开(公告)日:2006-04-18
申请号:US10183128
申请日:2002-06-26
申请人: Michael Graupe , James T. Palmer , John W. Patterson , David J. Aldous , Sukanthini Thurairatnam , Andreas P. Timm , John Link , Jiayao Li
发明人: Michael Graupe , James T. Palmer , John W. Patterson , David J. Aldous , Sukanthini Thurairatnam , Andreas P. Timm , John Link , Jiayao Li
IPC分类号: A61K31/535
CPC分类号: C07D213/40 , A61K31/4245 , A61K31/5375 , A61K31/5377 , C07C317/44 , C07C323/60 , C07D205/08 , C07D207/24 , C07D213/75 , C07D223/12 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/26 , C07D277/64 , C07D285/08 , C07D295/185 , C07D413/04 , C07D413/12
摘要: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译: 本发明涉及新型组织蛋白酶S抑制剂,其药学上可接受的盐和N-氧化物,它们作为治疗剂的用途及其制备方法。
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公开(公告)号:US20070135386A1
公开(公告)日:2007-06-14
申请号:US11625369
申请日:2007-01-22
IPC分类号: A61K31/675 , A61K31/4965 , A61K31/50 , A61K31/4415 , A61K31/381 , A61K31/4035
CPC分类号: C07D295/215 , A61K38/00 , C07C317/48 , C07C317/50 , C07D205/085 , C07D207/24 , C07D207/48 , C07D223/12 , C07D307/32 , C07K5/0606 , C07K5/06078 , Y02A50/411 , Y02A50/423
摘要: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译: 本发明涉及新型组织蛋白酶S抑制剂,其药学上可接受的盐和N-氧化物,它们作为治疗剂的用途及其制备方法。
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公开(公告)号:US20060189657A1
公开(公告)日:2006-08-24
申请号:US11409601
申请日:2006-04-24
IPC分类号: A61K31/445 , A61K31/4015
CPC分类号: C07D263/56 , A61K38/00 , C07D263/32 , C07D267/10 , C07D271/06 , C07D271/10 , C07D271/107 , C07D295/195 , C07D295/215 , C07D413/04 , C07D413/12 , C07K5/06191
摘要: Novel inhibitors of cathepsin S, K, B, and L, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译: 组织蛋白酶S,K,B和L的新型抑制剂,其药学上可接受的盐和N-氧化物,它们作为治疗剂的用途及其制备方法。
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公开(公告)号:US20070203138A1
公开(公告)日:2007-08-30
申请号:US11740414
申请日:2007-04-26
申请人: Jiayo Li , David Aldous , Sukanthini Thurairatnam
发明人: Jiayo Li , David Aldous , Sukanthini Thurairatnam
IPC分类号: A61K31/5377 , A61K31/4439 , A61K31/4245
CPC分类号: C07D271/10 , A61K31/4245 , A61K31/4439 , A61K31/5377 , C07D271/06 , C07D401/04 , C07D409/04 , Y02A50/411
摘要: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译: 本发明涉及新的选择性组织蛋白酶S抑制剂,其药学上可接受的盐和N-氧化物,它们作为治疗剂的用途及其制备方法。
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公开(公告)号:US07196099B2
公开(公告)日:2007-03-27
申请号:US10787367
申请日:2004-02-26
IPC分类号: A61K31/4468 , A61K31/45 , C07D401/12
CPC分类号: C07D295/215 , A61K38/00 , C07C317/48 , C07C317/50 , C07D205/085 , C07D207/24 , C07D207/48 , C07D223/12 , C07D307/32 , C07K5/0606 , C07K5/06078 , Y02A50/411 , Y02A50/423
摘要: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译: 本发明涉及新型组织蛋白酶S抑制剂,其药学上可接受的盐和N-氧化物,它们作为治疗剂的用途及其制备方法。
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公开(公告)号:US20050267044A1
公开(公告)日:2005-12-01
申请号:US11166829
申请日:2005-06-24
申请人: Jiayo Li , David Aldous , Sukanthini Thurairatnam
发明人: Jiayo Li , David Aldous , Sukanthini Thurairatnam
IPC分类号: A61K38/00 , A61P1/02 , A61P13/12 , A61P19/02 , A61P21/04 , A61P35/00 , A61P43/00 , C07D271/06 , C07D271/10 , C07D401/04 , C07D409/04 , C07K5/078 , A61K31/5377 , C07D413/14
CPC分类号: C07D271/10 , A61K31/4245 , A61K31/4439 , A61K31/5377 , C07D271/06 , C07D401/04 , C07D409/04 , Y02A50/411
摘要: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译: 本发明涉及新的选择性组织蛋白酶S抑制剂,其药学上可接受的盐和N-氧化物,它们作为治疗剂的用途及其制备方法。
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公开(公告)号:US20050009831A1
公开(公告)日:2005-01-13
申请号:US10803566
申请日:2004-03-18
申请人: Andrew Ratcliffe , Roger Aitchison Walsh , Tahir Majid , Sukanthini Thurairatnam , Shelley Amendola , David Aldous , John Souness , Conception Nemecek , Sylvie Wentzler , Corinne Venot
发明人: Andrew Ratcliffe , Roger Aitchison Walsh , Tahir Majid , Sukanthini Thurairatnam , Shelley Amendola , David Aldous , John Souness , Conception Nemecek , Sylvie Wentzler , Corinne Venot
IPC分类号: A61K31/495 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61K31/551 , A61K45/00 , A61P35/00 , A61P43/00 , C07D487/04
CPC分类号: A61K31/495 , C07D487/04 , Y02A50/411
摘要: The present invention concerns compounds of general formula (I): in which: R1 represents hydrogen, R4, —C(═Y)—NHR4, —SO2NHR4, —C(=Z1)—R4, —SO2—R4 or —C(=Z1)—OR4; R2 represents hydrogen, cyano, halogen or —C≡C—R5; R3 represents hydrogen, acyl, alkoxycarbonyl, alkyl, aroyl, aryl, aryloxycarbonyl, carboxy, cycloalkenyl, cycloalkyl, heteroaroyl, heteroaryl, heterocycloalkyl or —C(═O)—NY1Y2; R4 represents optionally substituted alkyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl or heteroaryl R5 represents hydrogen or alkyl; R6 represents alkyl, acyl, alkoxycarbonyl, alkylsulfonyl, aryl, arylsulfonyl, aroyl, cycloalkyl, cycloalkenyl, heteroaryl, heteroarylsulfonyl, heteroaroyl and heterocycloalkyl; R7 represents optionally substituted alkyl, cycloalkyl or cycloalkylalkyl, R8 represents hydrogen, alkyl, alkenyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl; R9 represents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; R10 represents hydrogen or lower alkyl; R11 represents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; or alkyl optionally substituted by —NY1Y2; R12 represents aryl or heteroaryl; or alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl or heterocycloalkylalkyl each optionally substituted Y represents O, S or NCN; Y1 and Y2 (Y3 and Y4) are independently in particular hydrogen, alkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl or heterocycloalkyl; or the group —NY1Y2 may form 5-7 membered ring or the group —NY3Y4 (—NY5Y6) may form a cyclic amine; Z (Z1) represents O or S; Z2 represents O or S(O)p; n is zero or an integer 1 or 2; m is 1 or 2; p is 1 or 2; and their corresponding N-oxides, their prodrugs; their pharmaceutically acceptable salts and solvates (e.g. hydrates), also together with one or more pharmaceutically acceptable carriers or excipients, such novel indolizines derivatives with inhibitory effects towards kinase proteins and especially for use for preventing or treating diseases that may be modulated by the inhibition of such kinase proteins and particularly solid tumours.
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