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1. 发明专利

JP2010132710A Tricyclic thrombin receptor antagonist 审中-公开
标题翻译： TRICYCLIC THROMBIN RECEPTOR ANTAGONIST
公开(公告)号：JP2010132710A
公开(公告)日：2010-06-17
申请号：JP2010049903
申请日：2010-03-05
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： CHACKALAMANNIL SAMUEL , CLASBY MARTIN C , GREENLEE WILLIAM J , WANG YUGUANG , YAN SHAA , VELTRI ENRICO P , CHELLIAH MARIAPPAN , WU WENXUE
IPC分类号： C07D405/06 , A61K31/4365 , A61K31/443 , A61K31/4709 , A61K31/506 , A61K31/616 , A61K45/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P13/12 , A61P29/00 , A61P35/00 , A61P43/00 , C07D405/14 , C07D417/14
CPC分类号： C07D405/06 , C07D405/14 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide a thrombin receptor antagonist compound. SOLUTION: The invention relates to substituted tricyclic thrombin receptor antagonists and pharmaceutical compositions containing them. Further, the invention relates to their use in treatment of diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, cardiac failure, brain ischemia, cerebral stroke, inflammatory disorder, neurodegenerative disease and cancer. Combination of the new compounds with other cardiovascular agents is also provided. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供凝血酶受体拮抗剂化合物。解决方案：本发明涉及取代的三环类凝血酶受体拮抗剂和含有它们的药物组合物。此外，本发明涉及其用于治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭，脑缺血，脑中风，炎症性疾病，神经变性疾病和癌症相关的疾病的治疗。还提供了新化合物与其它心血管药物的组合。版权所有（C）2010，JPO＆INPIT

2. 发明专利

JP2009029820A Himbacine analogue as thrombin receptor antagonist 审中-公开
标题翻译： HIMBACINE ANALOGUE as THROMBIN RECEPTOR ANTAGONIST
公开(公告)号：JP2009029820A
公开(公告)日：2009-02-12
申请号：JP2008238716
申请日：2008-09-17
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , YAN SHAA
IPC分类号： C07D491/048 , A61K31/4436 , A61K31/444 , A61K31/4741 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D491/04 , C07D493/04 , C07D495/04
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： PROBLEM TO BE SOLVED: To provide a thrombin receptor antagonist. SOLUTION: The compound is a heterocyclic-substituted tricyclic compound of formula (I) or a pharmaceutically acceptable salts thereof. Wherein: n 1 and n 2 are independently 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is an alkyl or an optionally substituted alkenyl; R 22 is -COR 23 or a carboxy, a sulfinyl, a sulfonyl, a sulfonamide or an amino acid derivative; R 23 is a haloalkyl, an alkenyl, a haloalkenyl, an alkynyl, an optionally substituted cycloalkyl, a cycloalkyl-alkyl, an aryl, an arylalkyl, a heteroaryl, a heterocycloalkyl, or -COOH and/or -SO 3 H-substituted alkyl; and, R 1 , R 2 , R 3 , R 9 , R 10 and R 11 are as defined in the specification. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供凝血酶受体拮抗剂。解决方案：化合物是式（I）的杂环取代的三环化合物或其药学上可接受的盐。其中n 1 和n 2 独立地为0-2; Het是任选取代的单，双或三环杂芳族基团; B是烷基或任选取代的烯基; R 22是-COR 23，或羧基，亚磺酰基，磺酰基，磺酰胺或氨基酸衍生物; R 30是卤代烷基，烯基，卤代烯基，炔基，任选取代的环烷基，环烷基 - 烷基，芳基，芳基烷基，杂芳基，杂环烷基或-COOH和/或 -SO 3 S取代的烷基; 和R 1 ，R 2 ，R 3 ，R 9 ，R SP SP >和R 11 如说明书中所定义。版权所有（C）2009，JPO＆INPIT

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

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。

5. 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。

6. 发明申请

WO2006068954A3 PYRAZOLO[1,5-A]PYRIMIDINE ADENOSINE A2a RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯并[1,5-A]吡嗪酮腺苷A2a受体拮抗剂
公开(公告)号：WO2006068954A3
公开(公告)日：2006-12-07
申请号：PCT/US2005045658
申请日：2005-12-19
申请人： SCHERING CORP , CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , NEUSTADT BERNARD R , GAO XIAOBANG
发明人： CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , NEUSTADT BERNARD R , GAO XIAOBANG
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , A61P25/16 , A61P25/18
CPC分类号： C07D487/04
摘要： Compounds having the structural formula (I) are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is -C(O)- or -S(O) 2 -; R 1 is alkyl or cycloalkyl; R 2 is hydrogen, halo or -CN; R 3 is hydrogen or alkyl; R 4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R 3 and R 4 , form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R 7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds 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：公开了具有结构式（I）的化合物，其中A是亚烷基或任选取代的亚芳基，亚环烷基或杂芳基二基; X是-C（O） - 或-S（O）2 - 。 R 1是烷基或环烷基; R 2是氢，卤素或-CN; R 3是氢或烷基; R 4是氢，烷基，烷氧基，羟基烷基，氨基烷基 - ，环烷基，杂环烷基，被烷基，任选取代的芳基烷基或任选取代的杂芳基烷基取代的杂环烷基; 或R 3和R 4，形成任选取代的5-7元环，所述环任选地包含另外的杂原子环成员; R 7是烷基，任选取代的苯基，任选取代的杂芳基，环烷基，卤素，吗啉基，任选取代的哌嗪基或任选取代的氮杂环烷基。还公开了化合物在治疗帕金森病中的用途，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组分的试剂盒的用途。

7. 发明申请

WO2008002596A3 ADENOSINE A2A RECEPTOR ANTAGONISTS 审中-公开
标题翻译：腺苷A2A受体拮抗剂
公开(公告)号：WO2008002596A3
公开(公告)日：2008-07-03
申请号：PCT/US2007014886
申请日：2007-06-25
申请人： SCHERING CORP , CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , STAMFORD ANDREW
发明人： CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , STAMFORD ANDREW
IPC分类号： C07D487/04 , A61K31/522 , A61P25/16
CPC分类号： C07D487/04
摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein: X 1 and X 2 are 1-3 substituents independently selected from the group consisting of H, alkyl, halo, -CF 3 , -OCF 3 , alkoxy, -OH and -CN; n is 0, 1 or 2; and R and R 1 are H or alkyl; also disclosed is the use of the compounds in the treatment of CNS diseases such as Parkinson's disease, alone or in combination with other agents for treating CNS diseases, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
摘要翻译：具有结构式（I）的化合物或其药学上可接受的盐，其中：X 1和X 2是1-3个取代基，独立地选自H，烷基，卤素，-CF 3，-OCF 3，烷氧基，-OH和-CN; n是0,1或2; 并且R和R 1是H或烷基; 还公开了这些化合物单独或与其它治疗CNS疾病的药物一起用于治疗CNS疾病如帕金森氏病的用途，包含它们的药物组合物和包含所述组合的组分的试剂盒。

8. 发明专利

NZ569814A Cannibinoid receptor modulators 未知
公开(公告)号：NZ569814A
公开(公告)日：2011-10-28
申请号：NZ56981407
申请日：2007-01-16
申请人： SCHERING CORP
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： C07D403/06 , C07C233/05 , C07C233/59 , C07D209/44 , C07D209/46 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10 , G21K1/00
摘要： A compound having the general structure of formula (I) and a pharmaceutically acceptable salt, solvate, or ester thereof is disclosed, wherein the variables are as defined in the specification. These compounds have an activity as cannabinoid receptor modulators, particularly, antagonists or inverse agonists of the CB1 receptor, and are 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.

9. 发明专利

CA2771601A1 MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS 未知
公开(公告)号：CA2771601A1
公开(公告)日：2011-03-03
申请号：CA2771601
申请日：2010-06-01
申请人： MOCHIDA PHARM CO LTD , SCHERING CORP
发明人： NISHIDA HIDEMITSU , SAITOH FUMIHIKO , HIRABAYASHI TOMOKAZU , CHACKALAMANNIL SAMUEL , CHAN TIN-YAU , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , DWYER MICHAEL P , GREENLEE WILLIAM J , XIA YAN , NEELAMKAVIL SANTHOSH , SHAH UNMESH G
IPC分类号： C07D265/32 , A61K31/5377 , A61P7/02 , C07D413/04 , C07D413/12 , C07D413/14
摘要： The present invention provides compounds having the formula (I) or a pharmaceutically acceptable salt or a solvate thereof, pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

10. 发明专利

DE60317493D1 未知
公开(公告)号：DE60317493D1
公开(公告)日：2011-01-13
申请号：DE60317493
申请日：2003-04-14
申请人： SCHERING CORP
发明人： CHACKALAMANNIL SAMUEL , CLASBY MARTIN C , GREENLEE WILLIAM J , WANG YUGUANG , XIA YAN , VELTRI ENRICO P , CHELLIAH MARIAPPAN , WU WENXUE
IPC分类号： C07D405/06 , A61K31/44 , A61K31/443 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P13/12 , A61P29/00 , A61P35/00 , A61P43/00 , C07D405/14 , C07D417/14

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