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1. 发明申请

US20110065671A1 BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS 审中-公开
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：US20110065671A1
公开(公告)日：2011-03-17
申请号：US12993363
申请日：2009-05-18
申请人： Joel M. Harris , Santhosh Francis , Bernard R. Neustadt , Craig D. Boyle , Hong Liu , Jinsong Hao , Andrew Starnford , Samuel Chackalamannil , William J. Greenlee
发明人： Joel M. Harris , Santhosh Francis , Bernard R. Neustadt , Craig D. Boyle , Hong Liu , Jinsong Hao , Andrew Starnford , Samuel Chackalamannil , William J. Greenlee
IPC分类号： A61K31/675 , C07D239/90 , A61K31/517 , C07D401/12 , A61K31/496 , C07F9/40 , C07D471/04 , A61K31/519 , C07D413/10 , A61K31/5377 , A61P3/00 , A61P9/00
CPC分类号： C07D239/90 , C07D401/06 , C07D401/12 , C07D403/04 , C07D413/04 , C07D417/12 , C07D471/04
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bi-cyclic 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 GPR1 19 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，心血管疾病或病症相关的方法到患者的GPR1 19的活动。

2. 发明授权

US07078408B2 [1,2,4]-Triazole bicyclic adenosine A2a receptor antagonists 有权
标题翻译： [1,2,4] - 三唑双环腺苷A2a受体拮抗剂
公开(公告)号：US07078408B2
公开(公告)日：2006-07-18
申请号：US10973642
申请日：2004-10-26
申请人： Bernard R. Neustadt , Hong Liu
发明人： Bernard R. Neustadt , Hong Liu
IPC分类号： C07D487/04 , A61K31/519 , A61P25/24 , A61P25/16
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds having the structural formula Iwherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1–C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted-aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations
摘要翻译：具有结构式I的化合物，其中：n为0,1,2或3; A是C（R 1）或N; R 1和R 2是H，（C 1 -C 6 -C 6） - 烷基，卤素，CN或 -CF 3 N 3; X是-C（O） - ， - O - ， - SO 2 - 或任选取代的亚甲基，亚氨基，亚芳基或杂芳基二基; Y是-O-，-SO 0-2 - 或任选取代的亚芳基，杂芳基二基或含氮杂环烷基，或具有一定条件的键; R是任选取代的 - 芳基或杂芳基; R 2是任选取代的 - 芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 2 -Y是稠合的哌啶基，取代的哌嗪基或取代的哌啶基; 其用于治疗帕金森病，单独或与其他治疗帕金森病的药物组合，包含它们的药物组合物和包含组合的组分的试剂盒

3. 发明授权

US06875772B2 [1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists 有权
标题翻译： Ä1,2,4'-三唑双环腺苷A2a受体拮抗剂
公开(公告)号：US06875772B2
公开(公告)日：2005-04-05
申请号：US10304939
申请日：2002-11-26
申请人： Bernard R. Neustadt , Hong Liu
发明人： Bernard R. Neustadt , Hong Liu
IPC分类号： A61K31/519 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1-C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
摘要翻译：具有结构式I的化合物，其中n为0,1,2或3; A为C（R 1）或N; R 1和R 1a为H，（C 1 -C 6） - 烷基，卤代，CN或-CF 3; X是-C（O） - ， - O - ， - SO 2 2-或任选取代的亚甲基，亚氨基，亚芳基或杂芳基二; Y是-O-，-SOO- 取代的亚芳基，杂芳基二基或含氮杂环烷基，或具有某些条件的键; R是任选取代的 - 芳基或杂芳基; R 2是任选取代的芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 2 -Y是稠合的哌啶基，取代的哌嗪基或取代的哌啶基;它们用于治疗帕金森病，单独或与其它用于治疗帕金森病的药物组合，其包含它们的药物组合物和包含组合。

4. 发明授权

US07368449B2 2-alkynyl- and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists 有权
标题翻译： 2-炔基 - 和2-烯基 - 吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c] - 嘧啶腺苷A2a受体拮抗剂
公开(公告)号：US07368449B2
公开(公告)日：2008-05-06
申请号：US11135261
申请日：2005-05-23
申请人： Bernard R. Neustadt , Jinsong Hao , Hong Liu , Craig D. Boyle , Samuel Chackalamannil , Unmesh G. Shah , Andrew Stamford
发明人： Bernard R. Neustadt , Jinsong Hao , Hong Liu , Craig D. Boyle , Samuel Chackalamannil , Unmesh G. Shah , Andrew Stamford
IPC分类号： A61K31/497
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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R 1，R 2，R 3，R 3， 4和R 5是H，烷基或烷氧基烷基; R 6是H，烷基，羟基烷基或-CH 2 F; R 7，R 8和R 9是H，烷基，烷氧基，烷硫基，烷氧基烷基，卤素或-CF 3， SUB>; 和Z是任选取代的芳基，杂芳基或杂芳基 - 烷基。还公开了式I化合物在治疗中枢神经系统疾病，特别是帕金森病中单独使用或与用于治疗帕金森病的其它药物组合的用途，以及包含它们的药物组合物的用途。

5. 发明授权

US08410122B2 Bicyclic heterocycle derivatives and methods of use thereof 有权
标题翻译：双环杂环衍生物及其使用方法
公开(公告)号：US08410122B2
公开(公告)日：2013-04-02
申请号：US13141344
申请日：2009-12-21
申请人： Joel M. Harris , Bernard R. Neustadt , Andrew Stamford , Hong Liu
发明人： Joel M. Harris , Bernard R. Neustadt , Andrew Stamford , Hong Liu
IPC分类号： A61K31/505 , A01N43/54
CPC分类号： C07D401/12 , C07D401/14
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 a GPCR 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，糖尿病，代谢紊乱，心血管疾病或与GPCR活性相关的病症的方法病人。

6. 发明申请

US20110263624A1 BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF 有权
标题翻译：双相异构体衍生物及其使用方法
公开(公告)号：US20110263624A1
公开(公告)日：2011-10-27
申请号：US13141344
申请日：2009-12-21
申请人： Joel M. Harris , Bernard R. Neustadt , Andrew Stamford , Hong Liu
发明人： Joel M. Harris , Bernard R. Neustadt , Andrew Stamford , Hong Liu
IPC分类号： A61K31/506 , A61P3/00 , A61P3/10 , A61P3/04 , C07D401/12 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14
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 a GPCR 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，糖尿病，代谢紊乱，心血管疾病或与GPCR活性有关的障碍的方法病人。

7. 发明申请

US20110152256A1 1,2,4-TRIAZOLO[4,3-c]PYRIMIDIN-3-ONE AND PYRAZOLO[4,3-e]-1,2,4-TRIAZOLO[4,3-c]PYRIMIDIN-3-ONE COMPOUNDS FOR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS 有权
标题翻译： 1,2,4-三唑[4,3-c]嘧啶-3-酮和吡唑并[4,3-e] -1,2,4-三唑[4,3-c]吡啶-3-酮化合物用作腺苷A2a受体拮抗剂
公开(公告)号：US20110152256A1
公开(公告)日：2011-06-23
申请号：US12920924
申请日：2009-03-03
申请人： Joel M. Harris , Bernard R. Neustadt , Hong Liu , Jinsong Hao , Andrew W. Stamford
发明人： Joel M. Harris , Bernard R. Neustadt , Hong Liu , Jinsong Hao , Andrew W. Stamford
IPC分类号： A61K31/5377 , C07D487/14 , A61K31/519 , C07D413/14 , A61K31/497 , C07D487/04 , A61P25/16 , A61P25/28
CPC分类号： C07D487/14 , C07D487/04
摘要： Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
摘要翻译：其中R1和R2与它们所键合的碳原子一起形成式（II）的另外的杂芳环以及其药学上可接受的盐，溶剂合物，酯和前药的式I化合物是腺苷A 2a受体拮抗剂和因此，可用于治疗中枢神经系统疾病，特别是帕金森病。

8. 发明申请

US20110105513A1 AMINO-QUINOXALINE AND AMINO-QUINOLINE COMPOUNDS FOR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS 有权
标题翻译：氨基喹啉和氨基喹啉化合物用作腺苷A2a受体拮抗剂
公开(公告)号：US20110105513A1
公开(公告)日：2011-05-05
申请号：US12920928
申请日：2009-03-03
申请人： Joel M. Harris , Bernard R. Neustadt , Hong Liu , Jinsong Hao , Andrew W. Stamford
发明人： Joel M. Harris , Bernard R. Neustadt , Hong Liu , Jinsong Hao , Andrew W. Stamford
IPC分类号： A61K31/498 , C07D241/44 , C07D417/12 , C07D405/12 , C07D401/12 , C07D413/04 , C07D215/38 , A61K31/47 , A61P25/00 , A61P25/24 , A61P25/28 , A61P25/16 , A61P25/18
CPC分类号： C07D241/44 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/04 , C07D417/04 , C07D417/12
摘要： Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(═NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof. Care adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
摘要翻译：式（I）的化合物，其中W表示CH或N; 和Q表示-CN，-C（= NOOH）NH 2，-CONHR1或本文所述的各种杂环基; 以及其药学上可接受的盐，溶剂合物，酯和前药。护理腺苷A2a受体拮抗剂，因此可用于治疗中枢神经系统疾病，特别是帕金森病。

9. 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。

10. 发明申请

US20130096141A1 BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：双相异构体衍生物及其使用方法
公开(公告)号：US20130096141A1
公开(公告)日：2013-04-18
申请号：US13805054
申请日：2011-06-14
申请人： Bernard R. Neustadt , Hong Liu
发明人： Bernard R. Neustadt , Hong Liu
IPC分类号： C07D519/00
CPC分类号： C07D519/00 , C07D471/22 , C07D487/04 , C07D495/04 , A61K45/06
摘要： Compounds of structural formula I: are GPR119 agonists and are useful for the treatment, control or prevention of disorders responsive to agonism of GPR119, such as metabolic-related disorders such as type I diabetes, type II diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia or syndrome X. The compounds are also reported as being useful for controlling weight gain, controlling food intake, and inducing satiety in mammals.
摘要翻译：结构式I的化合物是GPR119激动剂，可用于治疗，控制或预防对GPR119的激动作用反应的病症，例如代谢相关疾病如I型糖尿病，II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，高血糖症，高脂血症，高甘油三酯血症，高胆固醇血症，血脂异常或综合征X.该化合物也被报告用于控制体重增加，控制食物摄入和诱导哺乳动物的饱腹感。

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