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1. 发明申请

WO2009055331A3 BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS MODULATORS OF THE ACTIVITY OF GPR119 审中-公开
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：WO2009055331A3
公开(公告)日：2009-07-30
申请号：PCT/US2008080462
申请日：2008-10-20
申请人： SCHERING CORP , XIA YAN , BOYLE CRAIG D , GREENLEE WILLIAM J , CHACKALAMANNIL SAMUEL , JAYNE CHARLES LEE , STAMFORD ANDREW W , DAI XING , HARRIS JOEL M , NEUSTADT BERNARD R , NEELAMKAVIL SANTHOSH FRANCIS , SHAH UNMESH G , LANKIN CLAIRE M , LIU HONG
发明人： XIA YAN , BOYLE CRAIG D , GREENLEE WILLIAM J , CHACKALAMANNIL SAMUEL , JAYNE CHARLES LEE , STAMFORD ANDREW W , DAI XING , HARRIS JOEL M , NEUSTADT BERNARD R , NEELAMKAVIL SANTHOSH FRANCIS , SHAH UNMESH G , LANKIN CLAIRE M , LIU HONG
IPC分类号： C07D401/14 , A61K31/439 , A61K31/506 , A61K31/537 , A61P3/00 , C07D451/06 , C07D471/08 , C07D487/08 , C07D491/08 , C07D495/08 , 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。

2. 发明申请

WO2007084319A3 DIARYL PIPERIDINES AS CB1 MODULATORS 审中-公开
标题翻译： DIARYL PIPERIDINES作为CB1调节器
公开(公告)号：WO2007084319A3
公开(公告)日：2007-09-20
申请号：PCT/US2007000705
申请日：2007-01-11
申请人： SCHERING CORP , SCOTT JACK D , WEINSTEIN JAY , MILLER MICHAEL W , STAMFORD ANDREW W , GILBERT ERIC J , XIA YAN , GREENLEE WILLIAM J , LI WEI
发明人： SCOTT JACK D , WEINSTEIN JAY , MILLER MICHAEL W , STAMFORD ANDREW W , GILBERT ERIC J , XIA YAN , GREENLEE WILLIAM J , LI WEI
IPC分类号： C07D211/18 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06
CPC分类号： C07D211/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/32 , C07D211/58 , C07D211/60 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D471/10
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome (e.g., obesity, waist circumference, lipid profile, and insulin sensitivity), neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：具有式（I）的通式结构的化合物或其药学上可接受的盐，溶剂化物或酯可用于治疗疾病，病症或病症如代谢综合征（例如，肥胖，腰围，脂质分布和胰岛素敏感性），神经炎症性疾病，认知障碍，精神病，成瘾行为，胃肠道疾病和心血管疾病。

3. 发明申请

WO2005046688A3 METHODS OF USE OF THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：使用硫蛋白受体拮抗剂的方法
公开(公告)号：WO2005046688A3
公开(公告)日：2005-09-29
申请号：PCT/US2004037519
申请日：2004-11-09
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CLASBY MARTIN C , GREENLEE WILLIAM J , WANG YUGUANG , XIA YAN , VELTRI ENRICO P , CHELLIAH MARIAPPAN V , WU WENXUE , GRAZIANO MICHAEL P , KOSOGLOU TEDDY , CHINTALA MADHU
发明人： CHACKALAMANNIL SAMUEL , CLASBY MARTIN C , GREENLEE WILLIAM J , WANG YUGUANG , XIA YAN , VELTRI ENRICO P , CHELLIAH MARIAPPAN V , WU WENXUE , GRAZIANO MICHAEL P , KOSOGLOU TEDDY , CHINTALA MADHU
IPC分类号： A61K31/343 , A61K31/4525 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D521/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P25/28 , A61P29/00 , A61P35/00
CPC分类号： A61K31/4525 , A61K31/343 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14
摘要： A method of treating a therapeutic condition comprising administering to a mammal in need of such treatment an effective amount of at least one compound of the formulas (I) and (II) or a pharmaceutically acceptable isomer, salt, solvate or co-crystal form thereof, wherein the substituents are as defined in the specification, wherein said therapeutic condition is a cardiovascular or circulatory disease or condition, an inflammatory disease or condition, a respiratory tract or disease or condition, cancer, acute renal failure, astrogliosis, a fibrotic disorder of the liver, kidney, lung or intestinal tract, Alzheimer's disease, diabetes, diabetic neuropathy, rheumatoid arthritis, neurodegenerative disease, neurotoxic disease, systemic lupus erythematosus, multiple sclerosis, osteoporosis, glaucoma, macular degeneration, psoriasis, radiation fibrosis, endothelial dysfunction, a wound or a spinal cord injury, or a symptom or result thereof. Combination therapy with other therapeutically effective agents is also disclosed.
摘要翻译：治疗治疗条件的方法包括向需要这种治疗的哺乳动物施用有效量的至少一种式（I）和（II）化合物或其药学上可接受的异构体，盐，溶剂合物或共晶体形式其中所述取代基如说明书中所定义，其中所述治疗条件是心血管或循环系统疾病或病症，炎性疾病或病症，呼吸道或疾病或病症，癌症，急性肾功能衰竭，星形胶质细胞增生症，纤维化疾病肝，肾，肺或肠道，阿尔茨海默病，糖尿病，糖尿病性神经病，类风湿性关节炎，神经变性疾病，神经毒性疾病，系统性红斑狼疮，多发性硬化症，骨质疏松症，青光眼，黄斑变性，牛皮癣，放射纤维化，内皮功能障碍伤口或脊髓损伤，或其症状或结果。还公开了与其它治疗有效药物的联合治疗。

4. 发明申请

WO2009143039A3 HETEROCYCLIC COMPOUNDS AS FACTOR IXA INHIBITORS 审中-公开
标题翻译：异构化合物作为因子IXA抑制剂
公开(公告)号：WO2009143039A3
公开(公告)日：2010-07-08
申请号：PCT/US2009044291
申请日：2009-05-18
申请人： SCHERING CORP , CLASBY MARTIN C , GREENLEE WILLIAM J , CHACKALAMANNIL SAMUEL , XIA YAN , GAO XIAOBANG , CHELLIAH MARIAPPAN V , EAGEN KEITH A , VACCARO HENRY , CHAN TIN-YAU , MCKITTRICK BRIAN , WANG LI YUAN , PU HAIYAN
发明人： CLASBY MARTIN C , GREENLEE WILLIAM J , CHACKALAMANNIL SAMUEL , XIA YAN , GAO XIAOBANG , CHELLIAH MARIAPPAN V , EAGEN KEITH A , VACCARO HENRY , CHAN TIN-YAU , MCKITTRICK BRIAN , WANG LI YUAN , PU HAIYAN
IPC分类号： C07D231/18 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61P7/02 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D487/04
CPC分类号： C07D487/04 , C07D231/18 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14
摘要： The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
摘要翻译：本发明涉及式I-III的新型杂环化合物; 如本文所公开的或其药学上可接受的盐，溶剂化物，酯，前药或立体异构体。还公开了包含所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓栓塞性疾病的方法。

5. 发明申请

WO2007084450A3 CANNIBINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNIBINOID接收器调制器
公开(公告)号：WO2007084450A3
公开(公告)日：2007-11-08
申请号：PCT/US2007001024
申请日：2007-01-16
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , EAGEN KEITH A , SCOTT JACK D , WANG YUGUANG , XIA YAN , GREENLEE WILLIAM J
发明人： CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , EAGEN KEITH A , SCOTT JACK D , WANG YUGUANG , XIA YAN , GREENLEE WILLIAM J
IPC分类号： C07D209/44 , C07C233/05 , C07C233/59 , C07D209/46 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10
CPC分类号： C07D209/46 , C07C233/31 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/90 , C07D209/44 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10
摘要： A compound having the general structure of Formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.
摘要翻译：具有式（I）通式结构的化合物：化学式应插入此处，如出现在摘要中的纸张形式。或其药学上可接受的盐，溶剂化物或酯可用于治疗诸如肥胖症，代谢紊乱，成瘾，中枢神经系统疾病，心血管疾病，呼吸系统疾病和胃肠疾病的疾病，病症或病症。

6. 发明申请

WO2005035504A3 5-H -BENZO [D] NAPHTH [2, 1-B] AZEPINE DERIVATIVE AS SELECTIVE D1/D5 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF OBESITY AND CNS DISORDERS 审中-公开
标题翻译： 5-H-BENZO [D] NAPHTH [2,1-B] AZEPINE衍生物作为选择性D1 / D5受体拮抗剂治疗肥胖和CNS疾病
公开(公告)号：WO2005035504A3
公开(公告)日：2005-06-30
申请号：PCT/US2004015760
申请日：2004-05-20
申请人： SCHERING CORP , BURNETT DUANE A , GREENLEE WILLIAM J , MCKITTRICK BRIAN , SU JING , ZHU ZHAONING , SASIKUMAR THAVALAKULAMGARA K , MAZZOLA ROBERT , QIANG LI , YE YUANZAN
发明人： BURNETT DUANE A , GREENLEE WILLIAM J , MCKITTRICK BRIAN , SU JING , ZHU ZHAONING , SASIKUMAR THAVALAKULAMGARA K , MAZZOLA ROBERT , QIANG LI , YE YUANZAN
IPC分类号： C07D223/14 , C07D401/12 , C07D403/10 , C07D407/12
CPC分类号： C07D223/14
摘要： The present invention provides compounds of formula (I), which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
摘要翻译：本发明提供式（I）化合物，其为D1 / D5受体的新型拮抗剂以及制备这些化合物的方法。在另一个实施方案中，本发明提供了包含这种D1 / D5受体拮抗剂的药物组合物以及使用它们治疗CNS障碍，肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

7. 发明申请

WO2010147969A3 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：WO2010147969A3
公开(公告)日：2011-06-09
申请号：PCT/US2010038649
申请日：2010-06-15
申请人： SCHERING CORP , ZHU ZHAONING , HUANG XIANHAI , PALANI ANANDAN , GREENLEE WILLIAM J , ASLANIAN ROBERT G
发明人： ZHU ZHAONING , HUANG XIANHAI , PALANI ANANDAN , GREENLEE WILLIAM J , ASLANIAN ROBERT G
IPC分类号： C07D471/04 , A61K31/551 , A61K31/553 , A61K31/554 , A61P25/28 , C07D498/04 , C07D513/04
CPC分类号： C07D498/04 , C07D471/04 , C07D513/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula (I): Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula (I).
摘要翻译：本发明提供了作为γ分泌酶调节剂的新型化合物。化合物具有式（I）：还公开了使用式（I）的化合物调节γ-分泌酶活性的方法和治疗阿尔茨海默氏病的方法。

8. 发明申请

WO2005111031A3 NEUROPEPTIDE RECEPTOR MODULATORS 审中-公开
标题翻译：神经肽受体调节剂
公开(公告)号：WO2005111031A3
公开(公告)日：2005-12-22
申请号：PCT/US2005014518
申请日：2005-04-28
申请人： SCHERING CORP , ZHU ZHAONING , SUN ZHONG-YUE , YE YUANZAN , MULLINS DEBORRA E , MCKITTRICK BRIAN , STAMFORD ANDREW , GREENLEE WILLIAM J
发明人： ZHU ZHAONING , SUN ZHONG-YUE , YE YUANZAN , MULLINS DEBORRA E , MCKITTRICK BRIAN , STAMFORD ANDREW , GREENLEE WILLIAM J
IPC分类号： A61K31/428 , A61K31/541 , C07D417/00 , C07D417/12 , C07D487/04 , C07D513/04
CPC分类号： C07D487/04 , C07D417/12 , C07D513/04
摘要： The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. The compounds are represented by the structural Formula 1, Chemical formula should be inderted here as it appears on the abstract in paper form. a prodrug thereof, or any pharmaceutically acceptable salt, solvate, isomer or racemic mixture of the compound or said prodrug wherein R1 is heteroaryl, N-arylaminocarbonyl, N-heteroarylaminocarbonyl, benzimidazolyl or benzothiazolyl; R15 is present or not and if present is H, aryl, alkyl, arylalky or heteroarylalkyl; A is aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene or heterocycloalkyl wherein said aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene and heterocycloalkyl moieties may be substituted or unsubstituted; and B, L, X and R18 are defined herein.
摘要翻译：本发明公开了作为NPY Y1的新受体拮抗剂的化合物以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含这种NPY Y1受体拮抗剂的药物组合物以及使用它们治疗肥胖症，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。这些化合物由结构式1表示，化学式在此以摘要形式出现在本文中应该没有改变。其中R 1为杂芳基，N-芳基氨基羰基，N-杂芳基氨基羰基，苯并咪唑基或苯并噻唑基的化合物或所述前药的任何药学上可接受的盐，溶剂化物，异构体或外消旋混合物; R15存在或不存在并且如果存在则为H，芳基，烷基，芳基烷基或杂芳基烷基; A是芳基，杂芳基，环烷基，环亚烷基，亚杂环烷基或杂环烷基，其中所述芳基，杂芳基，环烷基，亚环烷基，亚杂环烷基和杂环烷基部分可以被取代或未被取代; 并且B，L，X和R 18如本文所定义。

9. 发明申请

WO2009005646A3 SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS 审中-公开
标题翻译：取代的PIPERAZINES作为CB1拮抗剂
公开(公告)号：WO2009005646A3
公开(公告)日：2009-03-19
申请号：PCT/US2008007868
申请日：2008-06-25
申请人： SCHERING CORP , GILBERT ERIC J , MILLER MICHAEL W , SCOTT JACK D , DEMONG DUANE EUGENE , STAMFORD ANDREW , GREENLEE WILLIAM J , CELLY CHANDER SHEKHER
发明人： GILBERT ERIC J , MILLER MICHAEL W , SCOTT JACK D , DEMONG DUANE EUGENE , STAMFORD ANDREW , GREENLEE WILLIAM J , CELLY CHANDER SHEKHER
IPC分类号： C07D241/04 , A61K31/496 , A61K31/506 , A61P3/00 , A61P9/10 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D241/04 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14
摘要： Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或酯可用于治疗由CB1受体介导的疾病或病症，例如代谢综合征和肥胖症，神经炎症性疾病，认知障碍和精神病，成瘾（例如戒烟），胃肠道疾病和心血管疾病。

10. 发明申请

WO2009005671A2 SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS 审中-公开
标题翻译：取代的哌嗪作为CB1拮抗剂
公开(公告)号：WO2009005671A2
公开(公告)日：2009-01-08
申请号：PCT/US2008007917
申请日：2008-06-25
申请人： SCHERING CORP , GILBERT ERIC J , GREENLEE WILLIAM J , LI SARAH WEI , MILLER MICHAEL W , SCOTT JACK D , STAMFORD ANDREW , CELLY CHANDER SHEKHER
发明人： GILBERT ERIC J , GREENLEE WILLIAM J , LI SARAH WEI , MILLER MICHAEL W , SCOTT JACK D , STAMFORD ANDREW , CELLY CHANDER SHEKHER
IPC分类号： C07D241/04 , A61K31/495 , A61P3/00 , C07D401/06
CPC分类号： C07D401/06 , C07D241/04
摘要： Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或酯可用于治疗由CB 1受体介导的疾病或病症，所述疾病或病症例如代谢综合征和肥胖症，神经炎性病症，认知障碍和精神病，成瘾（例如吸烟戒烟），胃肠疾病和心血管疾病。

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