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公开(公告)号:US20070191376A1
公开(公告)日:2007-08-16
申请号:US11644849
申请日:2006-12-22
申请人: Dong Zou , Wei-Sheng Huang , R. Thomas , Jan Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William Shakespeare , Rajeswari Sundaramoorthi , Chester Metcalf, , David Dalgarno , Tomi Sawyer
发明人: Dong Zou , Wei-Sheng Huang , R. Thomas , Jan Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William Shakespeare , Rajeswari Sundaramoorthi , Chester Metcalf, , David Dalgarno , Tomi Sawyer
IPC分类号: A61K31/53 , A61K31/519 , A61K31/496 , A61K31/503 , A61K31/498 , A61K31/4745 , C07D487/04
CPC分类号: C07D471/04 , C07D473/34 , C07D487/04
摘要: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译: 本发明涉及以下通式的化合物:其中可变基团如本文所定义,及其制备和用途。
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公开(公告)号:US20050065171A1
公开(公告)日:2005-03-24
申请号:US10876116
申请日:2004-06-24
申请人: William Shakespeare , Chester Metcalf , Tomi Sawyer , Yihan Wang , Rajeswari Sundaramoorthi , David Dalgarno , Regine Bohacek , Manfred Weigele
发明人: William Shakespeare , Chester Metcalf , Tomi Sawyer , Yihan Wang , Rajeswari Sundaramoorthi , David Dalgarno , Regine Bohacek , Manfred Weigele
IPC分类号: A61K20060101 , A61K31/522 , A61K31/675 , A61P35/00 , A61P35/02 , C07D473/12 , C07F9/6561 , C12Q1/68
CPC分类号: C07F9/65616
摘要: This invention relates to compounds of the general formula: in which Y, RA, RC and R6 are as defined herein, and to their preparation and use.
摘要翻译: 本发明涉及以下通式的化合物:其中Y,R A,R C和R 6如本文所定义,以及其制备和用途。
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公开(公告)号:US20050096298A1
公开(公告)日:2005-05-05
申请号:US10994962
申请日:2004-11-22
申请人: Chester Metcalf , Manfred Weigele , Tomi Sawyer , Regine Bohacek , William Shakespeare , Rajeswari Sundaramoorthi , Yihan Wang , David Dalgarno
发明人: Chester Metcalf , Manfred Weigele , Tomi Sawyer , Regine Bohacek , William Shakespeare , Rajeswari Sundaramoorthi , Yihan Wang , David Dalgarno
IPC分类号: A61K47/48 , C07D471/04 , C07D487/04 , C07F9/40 , C07F9/58 , C07F9/6558 , C07F9/6561 , A61K31/675
CPC分类号: C07D471/04 , A61K47/54 , A61K47/548 , C07D487/04 , C07F9/4012 , C07F9/405 , C07F9/58 , C07F9/65583 , C07F9/6561 , C07F9/65616
摘要: Novel purines and uses of these compounds for the treatment of bone related disorders and cancer is disclosed.
摘要翻译: 公开了这些化合物用于治疗骨相关疾病和癌症的新型嘌呤和用途。
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4.Sulfonamide substituted aspartic acid interleukin-1.beta. converting enzyme inhibitors 失效
标题翻译: 磺酰胺取代的天冬氨酸白细胞介素-1β转换酶抑制剂公开(公告)号:US6083981A
公开(公告)日:2000-07-04
申请号:US284425
申请日:1999-04-09
申请人: Hamish John Allen , Kenneth Dale Brady , William Glen Harter , Elizabeth Ann Lunney , Mark Stephen Plummer , Tomi Sawyer , Aurash Shahripour , Nigel Walker
发明人: Hamish John Allen , Kenneth Dale Brady , William Glen Harter , Elizabeth Ann Lunney , Mark Stephen Plummer , Tomi Sawyer , Aurash Shahripour , Nigel Walker
IPC分类号: A61K31/192 , A61K31/341 , A61P1/00 , A61P7/08 , A61P19/02 , A61P25/28 , A61P31/04 , C07C311/19 , C07C311/29 , C07C311/46 , C07C323/67 , C07D307/12 , C07D307/40
CPC分类号: C07D307/12 , C07C311/19 , C07C311/29 , C07C311/46 , C07C323/67 , C07C2101/14 , C07C2102/10
摘要: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula I, II, or III. ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock reperfusion injury, Alzheimer's disease, and shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.
摘要翻译: PCT No.PCT / US97 / 18406 Sec。 371日期1999年4月9日第 102(e)1999年4月9日PCT 1997年10月9日PCT公布。 公开号WO98 / 16504 日期:1998年04月23日本发明涉及具有式I,II或III的白细胞介素-1β转换酶抑制剂的化合物。 本发明还涉及治疗中风,炎性疾病,败血性休克再灌注损伤,阿尔茨海默氏病和志贺氏菌病的方法,以及含有作为白细胞介素-1β转换酶抑制剂的化合物的药学上可接受的组合物。
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公开(公告)号:US5786335A
公开(公告)日:1998-07-28
申请号:US744698
申请日:1996-10-31
申请人: Wayne Livingston Cody , Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Tomi Sawyer , Drago Robert Sliskovic
发明人: Wayne Livingston Cody , Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Tomi Sawyer , Drago Robert Sliskovic
CPC分类号: C07K7/06 , C07K5/06026 , C07K5/081 , C07K5/1008 , C07K5/1013 , A61K38/00
摘要: Sulfhydryl containing peptides having the formula X--A.sub.1 --A.sub.2 --A.sub.3 --A.sub.4 --A.sub.5 --Y inhibit the formation of Lp(a) and thus are useful for treating vascular diseases such as coronary heart disease, myocardial infarction, ischemic stroke, cervical atherosclerosis, cerebral infarction, and restenosis.
摘要翻译: 具有式X-A1-A2-A3-A4-A5-Y的含巯基的肽抑制Lp(a)的形成,因此可用于治疗血管疾病如冠心病,心肌梗塞,缺血性中风,颈动脉粥样硬化, 脑梗死和再狭窄。
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公开(公告)号:US10793615B2
公开(公告)日:2020-10-06
申请号:US15759911
申请日:2016-10-21
申请人: Merck Sharp & Dohme Corp. , Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
发明人: Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
IPC分类号: A61K38/00 , A61K38/28 , A61P3/04 , A61P7/12 , A61P3/10 , C07K14/435 , C07K14/605
摘要: Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
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公开(公告)号:US5808062A
公开(公告)日:1998-09-15
申请号:US319768
申请日:1994-10-12
申请人: John Michael Domagala , Edmund Lee Ellsworth , Elizabeth Lunney , Daniel Fred Ortwine , Kimberly Suzanne Para , Josyula Venkata Nagendra Vara Prasad , Tomi Sawyer , Bradley Dean Tait
发明人: John Michael Domagala , Edmund Lee Ellsworth , Elizabeth Lunney , Daniel Fred Ortwine , Kimberly Suzanne Para , Josyula Venkata Nagendra Vara Prasad , Tomi Sawyer , Bradley Dean Tait
IPC分类号: A61K31/365 , A61P31/12 , A61P31/18 , C07D309/38 , C07D335/02 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D413/12 , C07F7/18 , C07D309/30 , C07D417/00 , C07D401/04
CPC分类号: C07D403/06 , C07D309/38 , C07D335/02 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D413/12 , C07F7/1856
摘要: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.
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8.Substituted tetra- and pentapeptide inhibitors of protein: farnesyl transferase 失效
标题翻译: 取代的蛋白质的四肽和五肽抑制剂:法呢基转移酶公开(公告)号:US5763577A
公开(公告)日:1998-06-09
申请号:US667348
申请日:1996-06-21
申请人: Gary Louis Bolton , Alfred Campbell , Richard Gowan , John Cooke Hodges , Donald Hupe , Daniele Leonard , Tomi Sawyer , Judith Sebolt-Leopold , Francis J. Tinney
发明人: Gary Louis Bolton , Alfred Campbell , Richard Gowan , John Cooke Hodges , Donald Hupe , Daniele Leonard , Tomi Sawyer , Judith Sebolt-Leopold , Francis J. Tinney
摘要: Inhibitors of protein:farnesyl transferase enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in controlling tissue proliferative diseases, including cancer and restenosis.
摘要翻译: 本发明描述了蛋白质抑制剂:法呢基转移酶,以及其制备方法及其药物组合物,其可用于控制组织增生性疾病,包括癌症和再狭窄。
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公开(公告)号:US20190338008A1
公开(公告)日:2019-11-07
申请号:US15759911
申请日:2016-10-21
申请人: Anandan PALANI , Ravi NARGUND , Paul E. CARRINGTON , Tomi SAWYER , Qiaolin DENG , Antonello PESSI , Elisabetta BIANCHI , Fe-derica ORYIETO , Merck Sharp & Dohme Corp.
发明人: Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
IPC分类号: C07K14/605 , A61P3/04 , A61K38/28
摘要: Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
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10.Compounds, compositions and methods for inhibiting the binding of proteins containing an SH2 domain to cognate phosphorylated proteins 失效
标题翻译: 用于抑制含有SH2结构域的蛋白质结合以协调磷酸化蛋白质的化合物,组合物和方法公开(公告)号:US5922697A
公开(公告)日:1999-07-13
申请号:US51038
申请日:1998-03-31
申请人: Elizabeth A. Lunney , Kimberly S. Para , Mark S. Plummer , Josyula V. N. V. Prasad , Alan R. Saltiel , Tomi Sawyer , Aurash Shahripour , Juswinder Singh , Charles J. Stankovic
发明人: Elizabeth A. Lunney , Kimberly S. Para , Mark S. Plummer , Josyula V. N. V. Prasad , Alan R. Saltiel , Tomi Sawyer , Aurash Shahripour , Juswinder Singh , Charles J. Stankovic
摘要: The present invention provides compounds that inhibit the binding of proteins containing an SH2 domain to cognate phosphorylated proteins. The invention also provides pharmaceutical compositions containing the compounds and methods of inhibiting the binding of proteins containing an SH2 domain to cognate phosphorylated proteins.
摘要翻译: PCT No.PCT / US96 / 15998 Sec。 371日期1998年3月31日 102(e)1998年3月31日PCT PCT 1996年10月2日PCT公布。 公开号WO97 / 12903 日期1997年04月10日本发明提供了抑制含有SH2结构域的蛋白质与同源磷酸化蛋白质结合的化合物。 本发明还提供含有化合物的药物组合物和抑制含有SH2结构域的蛋白质与相关磷酸化蛋白质结合的方法。
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