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1. 发明申请

US20110263570A1 PYRIMIDINE DERIVATIVES AS GPCR MODULATORS FOR USE IN THE TREATMENT OF OBESITY AND DIABETES 有权
标题翻译：作为用于治疗糖尿病的GPCR调节剂的吡嗪衍生物
公开(公告)号：US20110263570A1
公开(公告)日：2011-10-27
申请号：US13141227
申请日：2009-12-21
申请人： Bernard R. Neustadt , Andrew Stamford , Jinsong Hao , Charles Lee Jayne , Yan Xia
发明人： Bernard R. Neustadt , Andrew Stamford , Jinsong Hao , Charles Lee Jayne , Yan Xia
IPC分类号： A61K31/55 , A61K31/506 , C07D401/12 , A61P3/00 , C07D498/08 , A61K31/5386 , A61P3/10 , A61P3/04 , C07D401/14 , C07D451/02
CPC分类号： C07D401/14 , C07D401/12 , C07D471/08 , C07D498/08
摘要： The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
摘要翻译：本发明涉及式（I）的嘧啶衍生物，包含嘧啶衍生物的组合物，以及使用嘧啶衍生物治疗或预防肥胖症，糖尿病，糖尿病并发症，代谢障碍，心血管疾病或与 G蛋白偶联受体（GPCR）在患者体内的活性。

2. 发明授权

US08722882B2 Pyrimidine derivatives as GPCR modulators for use in the treatment of obesity and diabetes 有权
标题翻译：嘧啶衍生物作为用于治疗肥胖和糖尿病的GPCR调节剂
公开(公告)号：US08722882B2
公开(公告)日：2014-05-13
申请号：US13141227
申请日：2009-12-21
申请人： Bernard R. Neustadt , Andrew Stamford , Jinsong Hao , Charles Lee Jayne , Yan Xia
发明人： Bernard R. Neustadt , Andrew Stamford , Jinsong Hao , Charles Lee Jayne , Yan Xia
IPC分类号： C07D401/12 , C07D401/14 , C07D471/08 , A61K31/506 , A61P3/04 , A61P3/10
CPC分类号： C07D401/14 , C07D401/12 , C07D471/08 , C07D498/08
摘要： The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
摘要翻译：本发明涉及式（I）的嘧啶衍生物，包含嘧啶衍生物的组合物，以及使用嘧啶衍生物治疗或预防肥胖症，糖尿病，糖尿病并发症，代谢障碍，心血管疾病或与 G蛋白偶联受体（GPCR）在患者体内的活性。

3. 发明申请

US20120040975A1 BRIDGED BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：桥联双环杂环衍生物及其使用方法
公开(公告)号：US20120040975A1
公开(公告)日：2012-02-16
申请号：US13260950
申请日：2010-04-01
申请人： Santhosh Francis Neelamkavil , Bernard R. Neustadt , Andrew Stamford , Yan Xia , Joel M. Harris , Craig D. Boyle , Samuel Chackalamannil , Dipshikha Biswas , Hong Liu , Jinsong Hao , Claire M. Lankin , Unmesh Shah
发明人： Santhosh Francis Neelamkavil , Bernard R. Neustadt , Andrew Stamford , Yan Xia , Joel M. Harris , Craig D. Boyle , Samuel Chackalamannil , Dipshikha Biswas , Hong Liu , Jinsong Hao , Claire M. Lankin , Unmesh Shah
IPC分类号： A61K31/537 , C07D401/12 , C07D491/08 , A61P3/00 , A61K31/506 , C07D487/08 , A61P3/10 , A61P3/04 , C07D451/06 , C07D498/08
CPC分类号： C07D498/08 , C07D401/12 , C07D451/02 , C07D471/08 , C07D487/08 , C07D491/08 , C07D491/113 , C07D495/08
摘要： The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
摘要翻译：本发明涉及桥连双环杂环衍生物，包含桥连双环杂环衍生物的组合物和使用桥连双环杂环衍生物用于治疗或预防肥胖，糖尿病，代谢障碍，心血管疾病或与一名患者的GPCR。

4. 发明申请

US20110118286A1 BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS GPCR MODULATORS 审中-公开
标题翻译：双相异构体衍生物及其作为GPCR调节剂的用途
公开(公告)号：US20110118286A1
公开(公告)日：2011-05-19
申请号：US13054347
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Joel M. Harris , Andre Stamford , Jinsong Hao , Bernard R. Neustadt , Samuel Chackalamannil , Yan Xia , Wiliam J. Greenlee
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Joel M. Harris , Andre Stamford , Jinsong Hao , Bernard R. Neustadt , Samuel Chackalamannil , Yan Xia , Wiliam J. Greenlee
IPC分类号： A61K31/519 , C07D487/04 , A61P3/00
CPC分类号： C07D487/04 , C07D473/30 , C07D473/34
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 diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) 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，糖尿病并发症，代谢障碍，心血管疾病或与患者G蛋白偶联受体（GPCR）的活性相关的紊乱。

5. 发明授权

US06897216B2 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US06897216B2
公开(公告)日：2005-05-24
申请号：US10448854
申请日：2003-05-30
申请人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
发明人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
IPC分类号： A61K31/505 , A61K31/519 , A61P25/08 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00 , C07D487/14
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基，环烯基或杂芳基; X是亚烷基或-C（O）CH 2 - 。 Y是-N（R 2）CH 2 CH 2，N（R 3） - ， - OCH 2， N 2 - （CH 2） - ， - O - ， - S - ， - CH 2 S- ， - （CH 2）2 -NH-或任选取代的m和n为2-3，Q为氮或任选取代的碳; 和Z是任选取代的苯基，苯基烷基或杂芳基，二苯基甲基，R 6 -C（O） - ，R 6 -SO 2 - ， - R 0 -OC（O） - ，R 7 -N（R 8）-C（O） - ，R 7 -N（R 8）-C（S） - ，苯基-CH（OH） - 或苯基-C（-NOR 2） - ; 或当Q为CH时，苯基氨基或吡啶基氨基; 或Z和Y一起是取代的哌啶基或取代的苯基; 和R 2，R 3，R 6，R 7和R 8和/或在说明书中定义的它们在治疗帕金森病中的用途，单独使用或与治疗帕金森病的其它药物组合，以及包含它们的药物组合物; 还公开了制备可用于制备式I化合物的中间体的方法。

6. 再颁专利

USRE44205E1 Adenosine A2a receptor antagonists 有权
公开(公告)号：USRE44205E1
公开(公告)日：2013-05-07
申请号：US13441140
申请日：2012-04-06
申请人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
发明人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
IPC分类号： C07D471/04 , C07D471/22 , C07D487/04
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.

7. 发明授权

US06630475B2 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US06630475B2
公开(公告)日：2003-10-07
申请号：US09865071
申请日：2001-05-24
申请人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
发明人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
IPC分类号： C07D40314
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基，环烯基或杂芳基; X是亚烷基或-C（O）CH 2 - ; Y是-N（R 2）CH 2 CH 2 N（R） 3） - ，-OCH 2 CH 2 N（R 2） - ， - O - ， - S - ， - CH 2 S - ， - （CH 2）2 -NH-或任选地被取代的n和n是2-3，并且Q是氮或任选取代的碳; 和Z是任选取代的苯基，苯基烷基或杂芳基，二苯基甲基，R 6 -C（O） - ，R 6 -SO 2 - ，R 6 -OC（O） - ，R 7 -N C（O） - ，R 7 -N（R 8）-C（S） - ，苯基-CH（OH） - 或苯基-C（= NOR 2） ; 或当Q为CH时，为苯基氨基或吡啶基氨基; 或Z和Y一起是取代的哌啶基或取代的苯基; 和R 2，R 3，R 6，R 7和R 8如说明书中所定义，其用于治疗帕金森病，单独使用或与其它药剂组合用于治疗帕金森病，以及包含它们的药物组合物; 还公开了制备可用于制备式I化合物的中间体的方法。

8. 发明授权

US08907095B2 Bicyclic heterocycle derivatives and their use as modulators of the activity of GPR119 有权
标题翻译：双环杂环衍生物及其作为GPR119活性调节剂的用途
公开(公告)号：US08907095B2
公开(公告)日：2014-12-09
申请号：US12739531
申请日：2008-10-20
申请人： Yan Xia , Craig D. Boyle , William J. Greenlee , Samuel Chackalamannil , Charles Lee Jayne
发明人： Yan Xia , Craig D. Boyle , William J. Greenlee , Samuel Chackalamannil , Charles Lee Jayne
IPC分类号： C07D221/02 , A61K31/439 , C07D451/14 , C07D491/08 , C07D495/08 , C07D471/08 , C07D451/06 , C07D487/08 , C07D401/14 , C07D498/08
CPC分类号： C07D451/06 , A61K31/439 , C07D401/14 , C07D451/14 , C07D471/08 , C07D487/08 , C07D491/08 , C07D495/08 , C07D498/08
摘要： The present invention relates to Bicyclic Heterocycle Derivatives, 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 GPR119 in a patient.
摘要翻译：本发明涉及双环杂环衍生物，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症，糖尿病，代谢紊乱，心血管疾病或与GPR119活性相关的病症的方法患者。

9. 发明申请

US20110212938A1 BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS MODULATORS OF THE ACTIVITY OF GPR119 有权
标题翻译：双相异构体衍生物及其作为GPR119活性调节剂的用途
公开(公告)号：US20110212938A1
公开(公告)日：2011-09-01
申请号：US12739531
申请日：2008-10-20
申请人： Yan Xia , Craig D. Boyle , William J. Greenlee , Samuel Chackalamannil , Charles Lee Jayne
发明人： Yan Xia , Craig D. Boyle , William J. Greenlee , Samuel Chackalamannil , Charles Lee Jayne
IPC分类号： A61K31/506 , C07D471/08 , C07D401/14 , C07D491/08 , C07D471/12 , C07D498/08 , A61K31/537 , C07D487/08 , C07D495/08 , A61P3/04 , A61P3/10
CPC分类号： C07D451/06 , A61K31/439 , C07D401/14 , C07D451/14 , C07D471/08 , C07D487/08 , C07D491/08 , C07D495/08 , C07D498/08
摘要： The present invention relates to Bicyclic Heterocycle Derivatives, 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 GPR119 in a patient.
摘要翻译：本发明涉及双环杂环衍生物，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症，糖尿病，代谢紊乱，心血管疾病或与GPR119活性相关的病症的方法患者。

10. 发明申请

US20100152138A1 CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT 有权
标题翻译：具有苯甲酸替代物的循环胺BACE-1抑制剂
公开(公告)号：US20100152138A1
公开(公告)日：2010-06-17
申请号：US12641952
申请日：2009-12-18
申请人： Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X.H. Le , Jeffrey F. Lowrie , Kurt W. Saionz , Suresh D. Babu
发明人： Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X.H. Le , Jeffrey F. Lowrie , Kurt W. Saionz , Suresh D. Babu
IPC分类号： A61K31/4015 , C07D207/12 , C07D217/24 , C07D413/12 , C07D243/08 , A61K31/47 , A61K31/675 , A61K31/397 , A61K31/5377 , A61K31/551 , A61P25/28
CPC分类号： C07D243/08 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D209/52 , C07D211/26 , C07D211/46 , C07D217/18 , C07D233/32 , C07D241/04 , C07D241/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/06 , C07D409/12 , C07D413/06
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中R1是R是-C（O）-N（R27）（R28），或其余的变量如说明书中所定义。还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。还公开了治疗认知或神经变性疾病的药物组合物和方法，其包含式I化合物与除式I以外的分泌抑制剂抑制剂，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非 - 甾族抗炎药，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂或抗淀粉样蛋白抗体。

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