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1. 发明授权

US07906653B2 Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation 失效
标题翻译：茚基乙酸衍生物及其作为药剂，中间体和制备方法的用途
公开(公告)号：US07906653B2
公开(公告)日：2011-03-15
申请号：US12759328
申请日：2010-04-13
申请人： Louis-David Cantin , Soongyu Choi , Roger B. Clark , Martin F. Hentemann , Xin Ma , Joachim Rudolph , Sidney X. Liang , Christiana Akuche , Rico C. Lavoie , Libing Chen , Dyuti Majumdar , Philip L. Wickens
发明人： Louis-David Cantin , Soongyu Choi , Roger B. Clark , Martin F. Hentemann , Xin Ma , Joachim Rudolph , Sidney X. Liang , Christiana Akuche , Rico C. Lavoie , Libing Chen , Dyuti Majumdar , Philip L. Wickens
IPC分类号： C07D277/20
CPC分类号： C07D213/30 , C07C59/72 , C07C59/90 , C07C69/734 , C07C211/48 , C07C217/24 , C07C255/54 , C07C327/48 , C07C333/04 , C07C2602/08 , C07D209/08 , C07D213/63 , C07D213/83 , C07D213/84 , C07D215/20 , C07D231/12 , C07D239/26 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/52 , C07D249/06 , C07D249/08 , C07D261/20 , C07D263/32 , C07D263/56 , C07D277/24 , C07D277/34 , C07D277/56 , C07D277/64 , C07D277/66 , C07D285/08 , C07D307/42 , C07D307/79 , C07D333/16 , C07D405/04 , C07D417/04 , C07D513/04
摘要： This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.
摘要翻译：本发明涉及可用于治疗疾病如糖尿病，肥胖症，高脂血症和动脉粥样硬化疾病的新型茚满乙酸衍生物。本发明还涉及可用于制备茚满乙酸衍生物的中间体和制备方法。

2. 发明申请

US20080009531A1 5-Anilino-4-Heteroarylpyrazole Derivatives Useful for the Treatment of Diabetes 审中-公开
标题翻译：可用于治疗糖尿病的5-苯胺基-4-杂芳基吡唑衍生物
公开(公告)号：US20080009531A1
公开(公告)日：2008-01-10
申请号：US11596959
申请日：2005-05-20
申请人： Louis Cantin , Xin Ma , Christiana Akuche , Sidney Liang
发明人： Louis Cantin , Xin Ma , Christiana Akuche , Sidney Liang
IPC分类号： A61K31/4155 , A61K31/4164 , A61K31/422 , A61K31/427 , A61P3/04 , A61P3/10 , A61P9/00 , C07D231/38 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D493/00 , C07D495/00
CPC分类号： C07D417/04 , A61K31/416 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D513/04
摘要： The present invention relates to 5-anilino-4-heteroarylpyrazole compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.
摘要翻译：本发明涉及5-苯胺基-4-杂芳基吡唑化合物，药物组合物和治疗糖尿病及相关疾病的方法。

3. 发明申请

US20100204472A1 Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation 失效
标题翻译：茚基乙酸衍生物及其作为药剂，中间体和制备方法的用途
公开(公告)号：US20100204472A1
公开(公告)日：2010-08-12
申请号：US12759328
申请日：2010-04-13
申请人： Louis-David Cantin , Soongyu Choi , Roger B. Clark , Martin F. Hentemann , Xin Ma , Joachim Rudolph , Sidney X. Liang , Christiana Akuche , Rico C. Lavoie , Libing Chen , Dyuti Majumdar , Philip L. Wickens
发明人： Louis-David Cantin , Soongyu Choi , Roger B. Clark , Martin F. Hentemann , Xin Ma , Joachim Rudolph , Sidney X. Liang , Christiana Akuche , Rico C. Lavoie , Libing Chen , Dyuti Majumdar , Philip L. Wickens
IPC分类号： C07D239/34 , C07D401/04 , C07D405/10 , C07D213/85 , C07D213/72 , C07D213/55 , C07D513/04 , C07D277/30 , C07D239/42
CPC分类号： C07D213/30 , C07C59/72 , C07C59/90 , C07C69/734 , C07C211/48 , C07C217/24 , C07C255/54 , C07C327/48 , C07C333/04 , C07C2602/08 , C07D209/08 , C07D213/63 , C07D213/83 , C07D213/84 , C07D215/20 , C07D231/12 , C07D239/26 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/52 , C07D249/06 , C07D249/08 , C07D261/20 , C07D263/32 , C07D263/56 , C07D277/24 , C07D277/34 , C07D277/56 , C07D277/64 , C07D277/66 , C07D285/08 , C07D307/42 , C07D307/79 , C07D333/16 , C07D405/04 , C07D417/04 , C07D513/04
摘要： This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.
摘要翻译：本发明涉及可用于治疗疾病如糖尿病，肥胖症，高脂血症和动脉粥样硬化疾病的新型茚满乙酸衍生物。本发明还涉及可用于制备茚满乙酸衍生物的中间体及其制备方法。

4. 发明申请

US20070265298A1 Preparation and Use of Biphenyl-4-Yl-Carbonylamino Acid Derivatives for the Treatment of Obesity 失效
标题翻译：联苯-4-基羰基氨基酸衍生物用于治疗肥胖症的制备与应用
公开(公告)号：US20070265298A1
公开(公告)日：2007-11-15
申请号：US11665317
申请日：2005-10-14
申请人： Roger Smith , Stephen O'Connor , Philip Coish , Derek Lowe , Roger Clark , Jeffrey Stebbins , Ann-Marie Campbell , Christiana Akuche , Tatiana Shelekhin
发明人： Roger Smith , Stephen O'Connor , Philip Coish , Derek Lowe , Roger Clark , Jeffrey Stebbins , Ann-Marie Campbell , Christiana Akuche , Tatiana Shelekhin
IPC分类号： A61K31/435 , A61K31/421 , A61K31/44 , C07D277/00 , C07D471/02 , A61P7/12 , A61K31/426
CPC分类号： C07D235/30 , C07D263/58 , C07D277/82 , C07D513/04
摘要： This invention relates to certain biphenyl-4-yl carbonylamino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
摘要翻译：本发明涉及某些联苯-4-基羰基氨基酸化合物，组合物和治疗或预防肥胖症及相关疾病的方法。

5. 发明授权

US07759376B2 Preparation and use of biphenyl-4-yl-carbonylamino acid derivatives for the treatment of obesity 失效
标题翻译：联苯-4-基 - 羰基氨基酸衍生物的制备和用途，用于治疗肥胖症
公开(公告)号：US07759376B2
公开(公告)日：2010-07-20
申请号：US11665317
申请日：2005-10-14
申请人： Roger Smith , Stephen J. O'Connor , Philip Coish , Derek Lowe , Roger B. Clark , Jeffrey Stebbins , Ann-Marie Campbell , Christiana Akuche , Tatiana Shelekhin
发明人： Roger Smith , Stephen J. O'Connor , Philip Coish , Derek Lowe , Roger B. Clark , Jeffrey Stebbins , Ann-Marie Campbell , Christiana Akuche , Tatiana Shelekhin
IPC分类号： A61K31/425 , C07D277/82
CPC分类号： C07D235/30 , C07D263/58 , C07D277/82 , C07D513/04
摘要： This invention relates to certain biphenyl-4-yl carbonylamino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
摘要翻译：本发明涉及某些联苯-4-基羰基氨基酸化合物，组合物和治疗或预防肥胖症及相关疾病的方法。

6. 发明授权

US07714004B2 Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation 失效
公开(公告)号：US07714004B2
公开(公告)日：2010-05-11
申请号：US10537630
申请日：2003-12-19
申请人： Louis-David Cantin , Soongyu Choi , Roger B. Clark , Martin F. Hentemann , Xin Ma , Joachim Rudolph , Sidney X. Liang , Christiana Akuche , Rico C. Lavoie , Libing Chen , Dyuti Majumdar , Philip L. Wickens
发明人： Louis-David Cantin , Soongyu Choi , Roger B. Clark , Martin F. Hentemann , Xin Ma , Joachim Rudolph , Sidney X. Liang , Christiana Akuche , Rico C. Lavoie , Libing Chen , Dyuti Majumdar , Philip L. Wickens
IPC分类号： A61K31/426 , C07D277/20
CPC分类号： C07D213/30 , C07C59/72 , C07C59/90 , C07C69/734 , C07C211/48 , C07C217/24 , C07C255/54 , C07C327/48 , C07C333/04 , C07C2602/08 , C07D209/08 , C07D213/63 , C07D213/83 , C07D213/84 , C07D215/20 , C07D231/12 , C07D239/26 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/52 , C07D249/06 , C07D249/08 , C07D261/20 , C07D263/32 , C07D263/56 , C07D277/24 , C07D277/34 , C07D277/56 , C07D277/64 , C07D277/66 , C07D285/08 , C07D307/42 , C07D307/79 , C07D333/16 , C07D405/04 , C07D417/04 , C07D513/04
摘要： This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.

7. 发明授权

US06660734B1 Oxazinones having antibacterial activity 失效
标题翻译：具有抗菌活性的恶嗪酮
公开(公告)号：US06660734B1
公开(公告)日：2003-12-09
申请号：US10055831
申请日：2002-01-22
申请人： Saul Wolfe , Christiana Akuche , Stephen Ro
发明人： Saul Wolfe , Christiana Akuche , Stephen Ro
IPC分类号： A61K31535
CPC分类号： A61K31/535 , C07D265/02 , Y02P20/55
摘要： The invention relates to novel oxazinones designed to bind to the penicillin receptor, methods of synthesizing the compounds, and the use of the compounds as antibacterial agents. The compounds have the general formula (I) Preferably the compounds have a carboxyethyl or a substituted carboxymethyl substituent at the 2-position and a hydroxyl group at the 5-position and have a molecular shape suitable for binding to and reacting with the active site of a pencillin-recognizing enzyme. The compounds are synthesized by condensing a carboxyl-protected N-hydroxy amino acid with a 3-hydroxyprotected-4-bromobutanoic acid to form a a doubly protected N-hydroxy N-acylamino acid, which is cyclized with an organic base to yield a: doubly protected 1,2-oxazin-3-one. The protecting groups are then removed to provide an antibacterial agent.
摘要翻译：本发明涉及设计用于结合青霉素受体的新型恶嗪酮，合成化合物的方法以及该化合物作为抗菌剂的用途。化合物具有通式（I）。优选地，化合物在2-位具有羧乙基或取代的羧甲基取代基，在5-位上具有羟基，并具有适于与活性位点结合并与其反应的分子形状一种青霉素识别酶。通过将羧基保护的N-羟基氨基酸与3-羟基保护的-4-溴丁酸缩合形成双重保护的N-羟基N-酰基氨基酸合成化合物，其与有机碱环化，得到：双保护的1,2-恶嗪-3-酮。然后除去保护基团以提供抗菌剂。

8. 发明申请

US20110118302A1 PREPARATION AND USE OF BIPHENYL-4-YL-CARBONYLAMINO ACID DERIVATIVES FOR THE TREATMENT OF OBESITY 审中-公开
标题翻译：联苯胺-4-甲酰氨基酸衍生物用于治疗肥胖症的制备和使用
公开(公告)号：US20110118302A1
公开(公告)日：2011-05-19
申请号：US12836035
申请日：2010-07-14
申请人： Roger Smith , Stephen J. O'Connor , Philip Coish , Derek Lowe , Roger B. Clark , Jeffrey Stebbins , Ann-Marie Campbell , Christiana Akuche , Tatiana Shelekhin
发明人： Roger Smith , Stephen J. O'Connor , Philip Coish , Derek Lowe , Roger B. Clark , Jeffrey Stebbins , Ann-Marie Campbell , Christiana Akuche , Tatiana Shelekhin
IPC分类号： A61K31/437 , A61K31/428 , A61P3/04 , A61P3/10 , A61P3/00 , A61P3/08 , A61P9/10 , A61P9/00 , A61P9/12
CPC分类号： C07D235/30 , C07D263/58 , C07D277/82 , C07D513/04
摘要： This invention relates to certain biphenyl-4-yl carbonylamino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
摘要翻译：本发明涉及某些联苯-4-基羰基氨基酸化合物，组合物和治疗或预防肥胖症及相关疾病的方法。

9. 发明申请

US20060084680A1 Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation 失效
公开(公告)号：US20060084680A1
公开(公告)日：2006-04-20
申请号：US10537630
申请日：2003-12-19
申请人： Louis-David Cantin , Soongyu Choi , Roger Clark , Martin Hentemann , Xin Ma , Joachim Rudolph , Sidney Liang , Christiana Akuche , Rico Lavoie , Libing Chen , Dyuti Majumdar , Philip Wickens
发明人： Louis-David Cantin , Soongyu Choi , Roger Clark , Martin Hentemann , Xin Ma , Joachim Rudolph , Sidney Liang , Christiana Akuche , Rico Lavoie , Libing Chen , Dyuti Majumdar , Philip Wickens
IPC分类号： A61K31/445 , A61K31/195 , A61K31/192
CPC分类号： C07D213/30 , C07C59/72 , C07C59/90 , C07C69/734 , C07C211/48 , C07C217/24 , C07C255/54 , C07C327/48 , C07C333/04 , C07C2602/08 , C07D209/08 , C07D213/63 , C07D213/83 , C07D213/84 , C07D215/20 , C07D231/12 , C07D239/26 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/52 , C07D249/06 , C07D249/08 , C07D261/20 , C07D263/32 , C07D263/56 , C07D277/24 , C07D277/34 , C07D277/56 , C07D277/64 , C07D277/66 , C07D285/08 , C07D307/42 , C07D307/79 , C07D333/16 , C07D405/04 , C07D417/04 , C07D513/04
摘要： This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.

10. 发明授权

US06399600B1 Oxazinones having antibacterial activity 失效
标题翻译：具有抗菌活性的恶嗪酮
公开(公告)号：US06399600B1
公开(公告)日：2002-06-04
申请号：US09102285
申请日：1998-06-22
申请人： Saul Wolfe , Christiana Akuche , Stephen Ro
发明人： Saul Wolfe , Christiana Akuche , Stephen Ro
IPC分类号： C07D27304
CPC分类号： A61K31/535 , C07D265/02 , Y02P20/55
摘要： The invention relates to novel oxazinones designed to bind to the penicillin receptor, methods of synthesizing the compounds, and the use of the compounds as antibacterial agents. The compounds have the general formula (I) Preferably the compounds have a carboxyethyl or a substituted carboxymethyl substituent at the 2-position and a hydroxyl group at the 5-position and have a molecular shape suitable for binding to and reacting with the active site of a pencillin-recognizing enzyme. The compounds are synthesized by condensing a carboxyl-protected N-hydroxy amino acid with a 3-hydroxyprotected-4-bromobutanoic acid to form a a doubly protected N-hydroxy N-acylamino acid, which is cyclized with an organic base to yield a doubly protected 1,2-oxazin-3-one. The protecting groups are then removed to provide an antibacterial agent.
摘要翻译：本发明涉及设计用于结合青霉素受体的新型恶嗪酮，合成化合物的方法以及该化合物作为抗菌剂的用途。化合物具有通式（I）。优选地，化合物在2-位具有羧乙基或取代的羧甲基取代基，在5-位上具有羟基，并具有适于与活性位点结合并与其反应的分子形状一种青霉素识别酶。通过将羧基保护的N-羟基氨基酸与3-羟基保护的-4-溴丁酸缩合以形成双重保护的N-羟基N-酰基氨基酸合成化合物，其与有机碱环化以产生双重保护 1,2-恶嗪-3-酮。然后除去保护基团以提供抗菌剂。

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