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公开(公告)号：US6011158A
公开(公告)日：2000-01-04
申请号：US659983
申请日：1996-06-07
申请人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck , Marguerita S. L. Lim-Wilby , Ruth F. Nutt , Matthew M. Abelman
发明人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck , Marguerita S. L. Lim-Wilby , Ruth F. Nutt , Matthew M. Abelman
IPC分类号： A61K38/00 , C07D211/56 , C07D211/76 , C07D213/75 , C07D239/46 , C07D239/54 , C07D239/545 , C07D401/12 , C07K5/06 , C07K5/078 , C07D211/72
CPC分类号： C07D211/56 , C07D211/76 , C07D213/75 , C07D239/47 , C07D239/545 , C07D401/12 , C07K5/06139 , C07K5/06191 , A61K38/00
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
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公开(公告)号：US6008351A
公开(公告)日：1999-12-28
申请号：US573775
申请日：1995-12-18
申请人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck , Marguerita S. L. Lim-Wilby , Ruth F. Nutt , Matthew M. Abelman
发明人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck , Marguerita S. L. Lim-Wilby , Ruth F. Nutt , Matthew M. Abelman
IPC分类号： A61K31/44 , A61K31/495 , A61K31/505 , A61K38/00 , A61P7/02 , A61P43/00 , C07C257/18 , C07C279/24 , C07C279/34 , C07C281/06 , C07C311/54 , C07C327/48 , C07D211/56 , C07D211/76 , C07D213/75 , C07D213/76 , C07D239/46 , C07D239/47 , C07D239/52 , C07D239/54 , C07D239/545 , C07D401/12 , C07F7/18 , C07K5/06 , C07K5/078 , C07D239/02
CPC分类号： C07K5/06191 , C07D211/56 , C07D211/76 , C07D213/75 , C07D239/47 , C07D239/545 , C07D401/12 , C07K5/06139 , A61K38/00
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译： 本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。
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公开(公告)号：US5658930A
公开(公告)日：1997-08-19
申请号：US481660
申请日：1995-06-07
申请人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck
发明人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck
IPC分类号： A61K38/00 , C07D211/56 , C07D211/76 , C07D213/75 , C07D239/46 , C07D239/54 , C07D239/545 , C07D401/12 , C07K5/06 , C07K5/078 , A61K31/445 , A61K31/505 , C07D213/64 , C07D233/32 , C07D233/40
CPC分类号： C07D211/56 , C07D211/76 , C07D213/75 , C07D239/47 , C07D239/545 , C07D401/12 , C07K5/06139 , C07K5/06191 , A61K38/00
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译： 本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。
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公开(公告)号：US5656645A
公开(公告)日：1997-08-12
申请号：US484506
申请日：1995-06-07
申请人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck
发明人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck
IPC分类号： A61K38/00 , C07D211/56 , C07D211/76 , C07D213/75 , C07D239/46 , C07D239/54 , C07D239/545 , C07D401/12 , C07K5/06 , C07K5/078 , A61K31/44 , A61K31/505 , C07D213/64 , C07D233/32 , C07D233/40
CPC分类号： C07D211/56 , C07D211/76 , C07D213/75 , C07D239/47 , C07D239/545 , C07D401/12 , C07K5/06139 , C07K5/06191 , A61K38/00
摘要： The present invention discloses heterocyclic aromatic peptide aldehydes which have an oxopyrimidine or oxopyridine group and an argininal tail which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译： 本发明公开了具有氧代嘧啶或氧代吡啶基和精氨酸尾的杂环芳族胺醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及使用它们作为疾病状态的治疗剂的方法 以异常血栓形成为特征的哺乳动物。
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5.发明授权
公开(公告)号：US6034215A
公开(公告)日：2000-03-07
申请号：US950270
申请日：1997-10-14
申请人： Joseph Edward Semple , Robert John Ardecky , Ruth Foelsche Nutt , William Charles Ripka , David C. Rowley , Marguerita S. L. Lim-Wilby , Terence Kevin Brunck
发明人： Joseph Edward Semple , Robert John Ardecky , Ruth Foelsche Nutt , William Charles Ripka , David C. Rowley , Marguerita S. L. Lim-Wilby , Terence Kevin Brunck
IPC分类号： A61K38/55 , A61K38/00 , A61K38/05 , A61P7/02 , C07K20060101 , C07K5/06 , C07K5/078 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/093 , C07K5/097 , A61K38/06
CPC分类号： C07K5/06139 , A61K38/05 , C07K5/06191
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译： 本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。
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6.发明授权
公开(公告)号：US5703208A
公开(公告)日：1997-12-30
申请号：US484720
申请日：1995-06-07
申请人： Joseph Edward Semple , Robert John Ardecky , Ruth Foelsche Nutt , William Charles Ripka , David C. Rowley , Marguerita S. L. Lim-Wilby , Terence Kevin Brunck
发明人： Joseph Edward Semple , Robert John Ardecky , Ruth Foelsche Nutt , William Charles Ripka , David C. Rowley , Marguerita S. L. Lim-Wilby , Terence Kevin Brunck
IPC分类号： A61K38/55 , A61K38/00 , A61K38/05 , A61P7/02 , C07K20060101 , C07K5/06 , C07K5/078 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/093 , C07K5/097 , A61K38/06 , C07D225/02 , C07F9/06
CPC分类号： C07K5/06139 , A61K38/05 , C07K5/06191
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译： 本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。
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公开(公告)号：US06342504B1
公开(公告)日：2002-01-29
申请号：US09194855
申请日：1999-12-21
申请人： Terence Kevin Brunck , Susan Y. Tamura , Joseph Edward Semple , Robert John Ardecky , Yu Ge , William Charles Ripka
发明人： Terence Kevin Brunck , Susan Y. Tamura , Joseph Edward Semple , Robert John Ardecky , Yu Ge , William Charles Ripka
IPC分类号： A61K31505
CPC分类号： C07K5/06191 , A61K38/00 , C07D211/56 , C07D211/76 , C07D213/75 , C07D239/47 , C07D239/545 , C07D401/12 , C07K5/06139
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译： 本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。
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8.发明授权Benzodiazepinones as modulators of metabotropic glutamate receptor functions and neurological uses thereof 有权苯二氮卓酮作为代谢型谷氨酸受体功能的调节剂及其神经用途公开(公告)号：US09193710B2
公开(公告)日：2015-11-24
申请号：US14342339
申请日：2012-08-29
IPC分类号： C07D403/04 , C07D409/14 , C07D243/14 , A61K31/551 , A61K45/06 , C07D243/12 , C07D417/04
CPC分类号： C07D403/04 , A61K31/551 , A61K45/06 , C07D243/12 , C07D243/14 , C07D409/14 , C07D417/04
摘要： The present invention relates to novel benzodiazepinone compounds of Formulae (I) wherein R1, R2, R4, R6, R7, R8, R9, and R10 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, methods of use of such compounds and compositions, and methods for preparing the compounds and compositions. The compounds are Group II metabotropic glutamate antagonists or allosteric modulators and are useful for the treatment of a variety of CNS disorders.
摘要翻译： 本发明涉及式（I）的新的苯并二氮杂酮化合物，其中R 1，R 2，R 4，R 6，R 7，R 8，R 9和R 10如本文所定义。 本发明还涉及含有这些化合物的药物组合物，这种化合物和组合物的使用方法，以及制备化合物和组合物的方法。 化合物是II族代谢型谷氨酸拮抗剂或变构调节剂，可用于治疗各种CNS疾病。
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9.发明申请NOVEL BENZODIAZEPINONES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR FUNCTIONS AND NEUROLOGICAL USES THEREOF 有权新戊酰胆碱作为代谢谷氨酸受体功能的调节剂及其神经用途公开(公告)号：US20150025064A1
公开(公告)日：2015-01-22
申请号：US14342339
申请日：2012-08-29
IPC分类号： C07D403/04 , A61K45/06 , C07D417/04 , A61K31/551 , C07D243/12
CPC分类号： C07D403/04 , A61K31/551 , A61K45/06 , C07D243/12 , C07D243/14 , C07D409/14 , C07D417/04
摘要： The present invention relates to novel benzodiazepinone compounds of Formulae (I) wherein R1, R2, R4, R6, R7, R8, R9, and R10 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, methods of use of such compounds and compositions, and methods for preparing the compounds and compositions. The compounds are Group II metabotropic glutamate antagonists or allosteric modulators and are useful for the treatment of a variety of CNS disorders.
摘要翻译： 本发明涉及式（I）的新的苯并二氮杂酮化合物，其中R 1，R 2，R 4，R 6，R 7，R 8，R 9和R 10如本文所定义。 本发明还涉及含有这些化合物的药物组合物，这种化合物和组合物的使用方法，以及制备化合物和组合物的方法。 化合物是II族代谢型谷氨酸拮抗剂或变构调节剂，可用于治疗各种CNS疾病。
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10.发明授权Methionine sulfone and S-substituted cysteine sulfone derivatives as enzyme inhibitors 失效甲硫氨酸砜和S-取代的半胱氨酸砜衍生物作为酶抑制剂
公开(公告)号：US5658939A
公开(公告)日：1997-08-19
申请号：US423584
申请日：1995-04-18
IPC分类号： A61K38/00 , A61P7/02 , C07K5/06 , C07K5/062 , C07K5/072 , C07K5/078 , A61K31/40 , A61K31/41 , C07D403/12 , C07D403/14
CPC分类号： C07K5/0606 , A61K38/00
摘要： This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
摘要翻译： 本发明涉及抑制凝血酶或因子Xa的化合物。 该化合物含有醛官能团和甲硫氨酸砜或S-取代的半胱氨酸砜残基。 化合物及其药物组合物可用于预防怀疑具有以异常血栓形成为特征的病症的哺乳动物的血栓形成。
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