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公开(公告)号:US5919765A
公开(公告)日:1999-07-06
申请号:US483470
申请日:1995-06-07
IPC分类号: A61K38/00 , A61P7/02 , C07C279/24 , C07C281/06 , C07C309/30 , C07C335/38 , C07K5/06 , C07K5/068 , C07K5/072 , C07K5/08 , A61K38/05 , C07K7/00 , C07K38/06
CPC分类号: C07K5/06095 , C07K5/06034 , C07K5/06086 , C07K5/06191 , A61K38/00
摘要: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
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公开(公告)号:US5721214A
公开(公告)日:1998-02-24
申请号:US485433
申请日:1995-06-07
CPC分类号: C07K5/06086 , C07K5/06095 , A61K38/00
摘要: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
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公开(公告)号:US20100234350A1
公开(公告)日:2010-09-16
申请号:US12559389
申请日:2009-09-14
申请人: Robert M. Scarborough , Wolin Huang , Charles K. Marlowe , Kim A. Kane-McGuire , Hans-Michael Jantzen , David M. Sedlock
发明人: Robert M. Scarborough , Wolin Huang , Charles K. Marlowe , Kim A. Kane-McGuire , Hans-Michael Jantzen , David M. Sedlock
IPC分类号: A61K31/55 , C07D209/44 , A61K31/4035 , C07D401/04 , A61K31/4439 , C07D239/02 , A61K31/505 , C07D277/20 , A61K31/426 , C07D243/24 , A61K31/5513 , C07D223/14 , C07D239/72 , A61K31/517 , C07D215/00 , A61K31/47 , C07D413/14 , A61K31/5377 , C07D471/02 , A61K31/437 , C07D513/02 , C07D285/18 , A61K31/542 , C07D237/26 , A61K31/502 , C07D333/34 , A61K31/381 , A61P9/00 , A61P9/10 , A61P7/02
CPC分类号: C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
摘要翻译: 式(I)至(VIII)的新型化合物,其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物,磺酰基硫脲衍生物,磺酰基胍衍生物,磺酰氰基胍衍生物,硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。 这些衍生物可用于各种药物组合物中,并且对于预防和/或治疗心血管疾病,特别是与血栓形成有关的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法,包括施用治疗有效量的式(I)至(VIII)化合物或其药学上可接受的盐的步骤。
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公开(公告)号:US20080194597A1
公开(公告)日:2008-08-14
申请号:US11841711
申请日:2007-08-20
IPC分类号: A61K31/517 , C07D333/34 , A61K31/381 , A61P9/00 , C07D403/12
CPC分类号: C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
摘要翻译: 式(I)至(VIII)的新型化合物,其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物,磺酰基硫脲衍生物,磺酰基胍衍生物,磺酰氰基胍衍生物,硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。 这些衍生物可用于各种药物组合物中,并且对于预防和/或治疗心血管疾病,特别是与血栓形成有关的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法,包括施用治疗有效量的式(I)至(VIII)化合物或其药学上可接受的盐的步骤。
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公开(公告)号:US07056926B2
公开(公告)日:2006-06-06
申请号:US10941053
申请日:2004-09-13
IPC分类号: C07D409/12 , A61K31/517 , A61P7/02
CPC分类号: C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US6069130A
公开(公告)日:2000-05-30
申请号:US486010
申请日:1995-06-07
IPC分类号: C07D277/24 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/428 , A61K38/00 , A61P7/02 , A61P9/00 , C07C311/64 , C07D263/14 , C07D263/56 , C07D277/68 , C07K5/06 , C07K5/065 , C07K5/072 , C07K5/078 , C07K5/08 , A61K37/00 , C07K5/00
CPC分类号: C07K5/06 , C07K5/06078 , C07K5/06095 , C07K5/06139 , A61K38/00
摘要: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要翻译: 公开了与哺乳动物因子Xa具有活性的新型化合物,其盐和与其相关的组合物。 该化合物在体外或体内可用于预防或治疗凝血障碍。
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公开(公告)号:US5877278A
公开(公告)日:1999-03-02
申请号:US487282
申请日:1995-06-07
申请人: Ronald N. Zuckermann , Dane A. Goff , Simon Ng , Kerry Spear , Barbara O. Scott , Aaron C. Sigmund , Richard A. Goldsmith , Charles K. Marlowe , Yazhong Pei , Lutz Richter , Reyna Simon
发明人: Ronald N. Zuckermann , Dane A. Goff , Simon Ng , Kerry Spear , Barbara O. Scott , Aaron C. Sigmund , Richard A. Goldsmith , Charles K. Marlowe , Yazhong Pei , Lutz Richter , Reyna Simon
IPC分类号: C07D243/14 , A61K38/00 , C07B61/00 , C07D217/24 , C07D221/12 , C07D487/04 , C07K1/04 , C07K7/06 , C07K7/08 , C07K14/00 , C08G69/10
CPC分类号: C40B40/04 , C07K1/04 , C07K1/047 , C07K14/001 , C07K7/06 , C07K7/08 , C08G69/10 , C40B50/14 , A61K38/00 , B01J2219/00497 , B01J2219/00596 , B01J2219/0072 , C07B2200/11 , C40B40/10
摘要: A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two "sub-monomers" directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by --NH.sub.2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound .alpha.-haloacetamide) with a sufficient amount of a second sub-monomer comprising an --NH.sub.2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
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公开(公告)号:US08524721B2
公开(公告)日:2013-09-03
申请号:US13270193
申请日:2011-10-10
申请人: Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles K. Marlowe , Kim A. Kane-Maguire
发明人: Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles K. Marlowe , Kim A. Kane-Maguire
IPC分类号: C07D521/00 , C07D409/12 , C07D209/48 , A61K31/4035 , A61P7/02
CPC分类号: C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
摘要翻译: 式(I)和(VIII)的新型化合物,其更具体地包括作为有效血小板ADP受体抑制剂的磺酰脲衍生物,磺酰基硫脲衍生物,磺酰基胍衍生物,磺酰基氰胍基衍生物,硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。 这些衍生物可用于各种药物组合物中,并且对于预防和/或治疗心血管疾病,特别是与血栓形成有关的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法,包括施用治疗有效量的式(I)至(VIII)化合物或其药学上可接受的盐的步骤。
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公开(公告)号:US07622474B2
公开(公告)日:2009-11-24
申请号:US11841711
申请日:2007-08-20
IPC分类号: C07D521/00 , C07D409/12 , C07D209/48 , A61K31/4035 , A61P7/02
CPC分类号: C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US07358257B2
公开(公告)日:2008-04-15
申请号:US11293026
申请日:2005-12-01
IPC分类号: C07D409/12 , A61K31/517 , A61P7/02
CPC分类号: C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
摘要翻译: 式(I)至(VIII)的新型化合物,其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物,磺酰基硫脲衍生物,磺酰基胍衍生物,磺酰氰基胍衍生物,硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。 这些衍生物可用于各种药物组合物中,并且对于预防和/或治疗心血管疾病,特别是与血栓形成有关的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法,包括施用治疗有效量的式(I)至(VIII)化合物或其药学上可接受的盐的步骤。
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