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1. 发明授权

US5476847A Derivatives of phosphinic acid useful as endothelin converting enzyme inhibitors 失效
标题翻译：次膦酸的衍生物可用作内皮素转化酶抑制剂
公开(公告)号：US5476847A
公开(公告)日：1995-12-19
申请号：US267630
申请日：1994-06-29
申请人： Brian A. McKittrick , Michael F. Czarniecki , Samuel Chackalamannil , Shin Chung , Shawn DeFrees , Andrew W. Stamford
发明人： Brian A. McKittrick , Michael F. Czarniecki , Samuel Chackalamannil , Shin Chung , Shawn DeFrees , Andrew W. Stamford
IPC分类号： A61K31/66 , A61P1/00 , A61P3/08 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07F9/30 , C07F9/572 , C07F9/6558 , A61K31/405 , C07D209/14 , C07F9/36
CPC分类号： C07F9/65583 , C07F9/303 , C07F9/5728
摘要： Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R.sub.1 and R.sub.2 form a cycloalkyl ring of 3-8 members and R.sub.3 and R.sub.4 are as defined; or R.sub.3 and R.sub.4 form a cycloalkyl ring of 3-7 members and R.sub.1 and R.sub.2 are as defined; or R.sub.1 and R.sub.2 together, and R.sub.3 and R.sub.4 together, each form a cycloalkyl ring;R.sub.5 is --OR.sub.9 or --NHR.sub.9, wherein R.sub.9 is hydrogen or alkyl;n is 0 or 1;A.sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A.sub.1 and R.sub.5 together form a radical of an .alpha.-aminoacyl derivative; andR.sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or --A.sub.2 --R.sub.7, wherein A.sub.2 is a divalent .alpha.-aminoacyl radical, and R.sub.7 is a substituent on the .alpha.-amino atom selected from H, R.sub.8 OCO--, R.sub.8 SO.sub.2 -- and R.sub.8 NHCO--, wherein R.sub.8 is aryl, arylmethyl or (C.sub.1 -C.sub.8)alkyl;are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R.sup.3 and R.sup.4 form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.
摘要翻译：结构式为“IMAGE”的次膦酸衍生物或其药学上可接受的盐，其中R为H，烷基或烷酰氧基亚甲基; R 1，R 2，R 3和R 4是H，烷基，烯基，链烯基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，羟基烷基，羧基烷基，硫代烷基，烷氧基硫代烷基，氨基烷基，烷基氨基烷基，环烷基取代的烷基或杂环烷基。或R 1和R 2形成3-8成员的环烷基环，并且R 3和R 4如所定义; 或R 3和R 4形成3-7成员的环烷基环，并且R 1和R 2如所定义; 或R 1和R 2一起，并且R 3和R 4一起形成环烷基环; R5是-OR9或-NHR9，其中R9是氢或烷基; n为0或1; A1是对氨基苯甲酰基或对氨基苯磺酰基，或者A1和R5一起形成α-氨基酰基衍生物的基团; R6为苯基甲氧基羰基，芳基羰基，杂芳基羰基或-A2-R7，其中A2为二价α-氨基酰基，R7为选自H，R8OCO-，R8SO2-和R8NHCO-的α-氨基原子上的取代基，其中R8 是芳基，芳甲基或（C1-C8）烷基; 被公开用作内皮素转化酶抑制剂; 还公开了一种其中R3和R4形成环烷基环的新化合物，以及包含所述新化合物的药物组合物。

2. 发明授权

US08822480B2 Bicyclic heterocycle derivatives and use thereof as GPR119 modulators 有权
标题翻译：双环杂环衍生物及其作为GPR119调节剂的用途
公开(公告)号：US08822480B2
公开(公告)日：2014-09-02
申请号：US13003681
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
IPC分类号： C07D519/00 , A61K31/519 , A61P13/12 , A61P3/04
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
摘要翻译：本发明涉及式（I）的双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与在患者中G蛋白偶联受体（GPCR）如GPR119的活性。

3. 发明授权

US08318751B2 Pyrimidinone derivatives and methods of use thereof 失效
标题翻译：嘧啶酮衍生物及其使用方法
公开(公告)号：US08318751B2
公开(公告)日：2012-11-27
申请号：US12595906
申请日：2008-04-17
申请人： Craig D. Boyle , Samuel Chackalamannil , Claire M. Lankin , Unmesh G. Shah , Bernard R. Neustadt , Hong Liu , Andrew W. Stamford
发明人： Craig D. Boyle , Samuel Chackalamannil , Claire M. Lankin , Unmesh G. Shah , Bernard R. Neustadt , Hong Liu , Andrew W. Stamford
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00
CPC分类号： C07D401/04
摘要： The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
摘要翻译：本发明涉及嘧啶酮衍生物，包含嘧啶酮衍生物的组合物，以及使用嘧啶酮衍生物治疗或预防与患者中GPR119活性相关的肥胖，糖尿病，代谢疾病，心血管疾病或病症的方法。

4. 发明申请

US20110166165A1 BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS 有权
标题翻译：双相异构体衍生物及其作为GPR119调节剂的用途
公开(公告)号：US20110166165A1
公开(公告)日：2011-07-07
申请号：US13003681
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
IPC分类号： A61K31/519 , C07D487/04 , A61P3/04 , A61P3/10 , A61P3/00
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
摘要翻译：本发明涉及式（I）的双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与在患者中G蛋白偶联受体（GPCR）如GPR119的活性。

5. 发明申请

US20100113487A1 PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF 失效
标题翻译：吡咯烷酮衍生物及其使用方法
公开(公告)号：US20100113487A1
公开(公告)日：2010-05-06
申请号：US12595906
申请日：2008-04-17
申请人： Craig D Boyle , Samuel Chackalamannil , Claire M. Lankin , Unmesh G. Shah , Bernard R. Neustadt , Hong Liu , Andrew W. Stamford
发明人： Craig D Boyle , Samuel Chackalamannil , Claire M. Lankin , Unmesh G. Shah , Bernard R. Neustadt , Hong Liu , Andrew W. Stamford
IPC分类号： A61K31/519 , C07D471/04 , A61K38/28 , A61K38/22 , A61P3/10
CPC分类号： C07D401/04
摘要： The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
摘要翻译：本发明涉及嘧啶酮衍生物，包含嘧啶酮衍生物的组合物，以及使用嘧啶酮衍生物治疗或预防与患者中GPR119活性相关的肥胖，糖尿病，代谢疾病，心血管疾病或病症的方法。

6. 发明授权

US07531544B2 Xanthine phosphodiesterase V inhibitors 失效
公开(公告)号：US07531544B2
公开(公告)日：2009-05-12
申请号：US11852638
申请日：2007-09-10
申请人： Samuel Chackalamannil , Yuguang Wang , Craig D. Boyle , Andrew W. Stamford
发明人： Samuel Chackalamannil , Yuguang Wang , Craig D. Boyle , Andrew W. Stamford
IPC分类号： A61K31/522 , A61P9/12 , A61P15/10 , C07D473/04 , C07D473/06 , C07D473/08
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08
摘要： A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:

7. 发明授权

US06821978B2 Xanthine phosphodiesterase V inhibitors 失效
标题翻译：黄嘌呤磷酸二酯酶V抑制剂
公开(公告)号：US06821978B2
公开(公告)日：2004-11-23
申请号：US09940760
申请日：2001-08-28
申请人： Samuel Chackalamannil , Yuguang Wang , Craig D. Boyle , Andrew W. Stamford
发明人： Samuel Chackalamannil , Yuguang Wang , Craig D. Boyle , Andrew W. Stamford
IPC分类号： A61K31505
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08
摘要： A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:
摘要翻译：具有式（I）的黄嘌呤磷酸二酯酶V抑制剂，具有本文定义的变量，其特别用于治疗男性（勃起）和女性性功能障碍等生理障碍：例如，本发明的代表性化合物是：

8. 发明申请

US20100190687A1 PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：吡咯烷酮衍生物及其使用方法
公开(公告)号：US20100190687A1
公开(公告)日：2010-07-29
申请号：US12596341
申请日：2008-04-17
申请人： Craig D. Boyle , Santhosh Francis Neelamkavil , Samuel Chackalamannil , Bernard R. Neustadt , Jinsong Hao , Unmesh G. Shah , Joel M. Harris , Hong Liu , Andrew W. Stamford
发明人： Craig D. Boyle , Santhosh Francis Neelamkavil , Samuel Chackalamannil , Bernard R. Neustadt , Jinsong Hao , Unmesh G. Shah , Joel M. Harris , Hong Liu , Andrew W. Stamford
IPC分类号： A61K38/28 , C07D487/04 , A61K31/519 , A61K31/55 , A61K38/22 , A61P3/10 , A61P3/04
CPC分类号： C07D401/04 , C07D487/04
摘要： The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of G protein-coupled receptor 119 (“GPR119”) in a patient.
摘要翻译：本发明涉及嘧啶酮衍生物，包含嘧啶酮衍生物的组合物，以及使用嘧啶酮衍生物治疗或预防与G蛋白偶联受体119的活性相关的肥胖症，糖尿病，代谢紊乱，心血管疾病或病症的方法（“GPR119”）。

9. 发明授权

US09868738B2 Diazine-fused amidines as BACE inhibitors, compositions, and their use 有权
公开(公告)号：US09868738B2
公开(公告)日：2018-01-16
申请号：US15512081
申请日：2015-09-14
申请人： Merck Sharp & Dohme Corp. , Kun Liu , Shuwen He , Jared N. Cumming , Andrew W. Stamford
发明人： Kun Liu , Shuwen He , Jared N. Cumming , Andrew W. Stamford
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K45/06 , A61P25/00
摘要： In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I) or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R1B, R2, RA, ring A, RA, m, L1, RL, ring C, RC, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

10. 发明授权

US09181236B2 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use 有权
标题翻译： 2-螺取代的亚氨基噻嗪及其单和二氧化物作为抑制剂，组合物及其用途
公开(公告)号：US09181236B2
公开(公告)日：2015-11-10
申请号：US14240215
申请日：2012-08-21
申请人： Wen-Lian Wu , Duane A. Burnett , Andrew W. Stamford , Jared N. Cumming , Theodros Asberom , Chad Bennett , Thavalakulamgara K. Sasiskumar , Jack D. Scott
发明人： Wen-Lian Wu , Duane A. Burnett , Andrew W. Stamford , Jared N. Cumming , Theodros Asberom , Chad Bennett , Thavalakulamgara K. Sasiskumar , Jack D. Scott
IPC分类号： C07D417/14 , C07D417/12 , C07D513/04 , C07D513/10 , A61K45/06 , C07D417/04 , C07D417/10 , C07D279/34 , C07D519/00
CPC分类号： C07D417/14 , A61K45/06 , C07D279/34 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04 , C07D513/10 , C07D519/00
摘要： In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of the variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些亚氨基噻嗪二氧化物化合物，包括式（I）化合物及其互变异构体和立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中式如本文所定义。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括阿尔茨海默氏病。

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