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1. 发明申请

WO2011017296A1 4, 5, 6-TRISUBSTITUTED PYRIMIDINE DERIVATIVES AS FACTOR IXA INHIBITORS 审中-公开
标题翻译：作为因子IXA抑制剂的4,5,6-取代的吡嗪衍生物
公开(公告)号：WO2011017296A1
公开(公告)日：2011-02-10
申请号：PCT/US2010/044208
申请日：2010-08-03
申请人： SCHERING CORPORATION , CHELLIAH, Mariappan, V. , CHACKALAMANNIL, Samuel , GREENLEE, William, J. , EAGEN, Keith, A. , GUO, Zhuyan , CLASBY, Martin, C. , XIA, Yan , JAYNE, Charles, L. , DWYER, Michael , KEERTIKAR, Kartik, M. , CHAN, Tin-Yau , WANG, Li
发明人： CHELLIAH, Mariappan, V. , CHACKALAMANNIL, Samuel , GREENLEE, William, J. , EAGEN, Keith, A. , GUO, Zhuyan , CLASBY, Martin, C. , XIA, Yan , JAYNE, Charles, L. , DWYER, Michael , KEERTIKAR, Kartik, M. , CHAN, Tin-Yau , WANG, Li
IPC分类号： C07D239/34 , C07D239/47 , C07D239/52 , A61K31/505 , A61K31/506 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号： C07D239/34 , C07D239/47 , C07D239/52 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to novel heterocyclic compounds of Formulae (I): (Chemical formula should be inserted here as it appears on abstract in paper form) Formula (I) 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）的新型杂环化合物：（化学式应在此插入，如本文摘要中所示）本文公开的式（I），或其药学上可接受的盐，溶剂合物，酯，前药或其立体异构体。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。

2. 发明申请

WO2009143039A2 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：WO2009143039A2
公开(公告)日：2009-11-26
申请号：PCT/US2009/044291
申请日：2009-05-18
申请人： SCHERING CORPORATION , 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 , C07D487/04 , C07D401/04 , C07D403/04 , C07D413/04 , C07D413/14 , C07D403/14 , C07D401/14 , A61P7/02 , A61K31/416 , A61K31/415 , A61K31/4155 , A61K31/4152
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: Formula I; [Chemical Formulas should be inserted here as they appears on abstract in.pdf form.] Formula II; Formula 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：式I; [化学式应该插入这里，因为它们以.pdf形式的抽象出现]。本文公开的式III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。

3. 发明申请

WO2010065717A1 MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS 审中-公开
标题翻译：吗啉酮化合物作为因子IXA抑制剂
公开(公告)号：WO2010065717A1
公开(公告)日：2010-06-10
申请号：PCT/US2009/066548
申请日：2009-12-03
申请人： MOCHIDA PHARMACEUTICAL CO., LTD. , SCHERING CORPORATION , 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
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
IPC分类号： C07D265/30 , C07D265/32 , C07D267/10 , C07D279/06 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/04 , A61K31/4725 , A61K31/54 , A61K31/553 , A61K31/5355 , A61P7/00
CPC分类号： C07D401/12 , C07D265/30 , C07D265/32 , C07D267/10 , C07D279/06 , C07D413/12 , C07D413/14 , C07D417/04
摘要： The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译：本发明提供本文所述的式（I）化合物或其药学上可接受的盐或溶剂合物。本发明还提供包含一种或多种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形成，栓塞，高凝状态或纤维化改变的方法。

4. 发明申请

WO2011025565A1 MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS 审中-公开
标题翻译：吗啉酮化合物作为因子IXA抑制剂
公开(公告)号：WO2011025565A1
公开(公告)日：2011-03-03
申请号：PCT/US2010/036853
申请日：2010-06-01
申请人： MOCHIDA PHARMACEUTICAL CO., LTD. , SCHERING CORPORATION , 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.
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 , C07D413/04 , C07D413/12 , C07D413/14 , A61K31/5377 , A61P7/02
CPC分类号： C07D413/12 , C07D265/32 , C07D413/04 , 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.
摘要翻译：本发明提供具有式（I）化合物或其药学上可接受的盐或溶剂合物，包含一种或多种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形成，栓塞，高凝状态或纤维化改变的方法。

5. 发明申请

WO2007084450A2 CANNIBINOID RECEPTOR MODULATORS 审中-公开
标题翻译：栀子苷受体调节剂
公开(公告)号：WO2007084450A2
公开(公告)日：2007-07-26
申请号：PCT/US2007/001024
申请日：2007-01-16
申请人： SCHERING CORPORATION , 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.
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：具有通式（I）的一般结构的化合物：化学式应该插入到纸上，如抽象中所示。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，例如肥胖，代谢紊乱，成瘾，中枢神经系统疾病，心血管疾病，呼吸障碍和胃肠道疾病。

6. 发明申请

WO2005046688A2 METHODS OF USE OF THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：使用凝血酶受体拮抗剂的方法
公开(公告)号：WO2005046688A2
公开(公告)日：2005-05-26
申请号：PCT/US2004/037519
申请日：2004-11-09
申请人： SCHERING CORPORATION , 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： A61K31/4525
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：治疗疾病的方法包括给予需要这种治疗的哺乳动物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，盐其溶剂化物或共晶形式，其中所述取代基如说明书中所定义，其中所述治疗性病症为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，急性肾病肝，肾，肺或肠道的纤维化病症，阿尔茨海默氏病，糖尿病，糖尿病性神经病，类风湿性关节炎，神经退行性疾病，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，银屑病，辐射纤维化，内皮功能障碍，伤口或脊髓损伤，或其症状或结果。还公开了与其他治疗有效药剂的联合疗法。

7. 发明申请

WO2005118576A1 CONSTRAINED HIMBACINE ANALOGS AS THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：受约束的肝素模拟物作为血红蛋白受体拮抗剂
公开(公告)号：WO2005118576A1
公开(公告)日：2005-12-15
申请号：PCT/US2005/018372
申请日：2005-05-25
申请人： SCHERING CORPORATION , CHELLIAH, Mariappan, V. , CHACKALAMANNIL, Samuel , XIA, Yan , CLASBY, Martin, C. , GREENLEE, William, J. , WANG, Yuguang , VELTRI, Enrico, P. , WU, Wenxue , GRAZIANO, Michael, P. , KOSOGLOU, Teddy , CHINTALA, Madhu
发明人： CHELLIAH, Mariappan, V. , CHACKALAMANNIL, Samuel , XIA, Yan , CLASBY, Martin, C. , GREENLEE, William, J. , WANG, Yuguang , VELTRI, Enrico, P. , WU, Wenxue , GRAZIANO, Michael, P. , KOSOGLOU, Teddy , CHINTALA, Madhu
IPC分类号： C07D405/08
CPC分类号： C07D493/04 , C07D405/06
摘要： A compound represented by the structural formula (Chemical formula should be inserted here as it appears on abstract in paper form) and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is -O- or -NR6- when the double-dashed line represents a single bond; X is H, -OH or -NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.
摘要翻译：公开了由结构式表示的化合物（化学式在此插入，以纸张形式摘录）及其药学上可接受的盐和溶剂，其中：R10和R34之间的环碳上的单点划线附表示单键或双键; X与Y所连接的碳之间的双点划线表示单键或不存在键; 当双点划线表示单键时，X是-O-或-NR6-; 当双点划线表示不存在的键时，X是H，-OH或-NHR 20; 和其他参数如本文所定义。还公开了含有所述化合物及其作为凝血酶受体拮抗剂和大麻素受体的结合物的药物组合物和组合。

8. 发明申请

WO2008002596A2 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：WO2008002596A2
公开(公告)日：2008-01-03
申请号：PCT/US2007/014886
申请日：2007-06-25
申请人： SCHERING CORPORATION , CLASBY, Martin, C. , CHACKALAMANNIL, Samuel , STAMFORD, Andrew
发明人： CLASBY, Martin, C. , CHACKALAMANNIL, Samuel , STAMFORD, Andrew
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个独立地选自H，烷基，卤素，-CF 3，-OCF 3，烷氧基，-OH和-CN; n为0,1或2; 且R和R 1为H或烷基; 还公开了该化合物在治疗CNS疾病如帕金森病中的用途，单独或与其它用于治疗CNS疾病的药物组合，其包含它们的药物组合物和包含组合组分的试剂盒的使用。

9. 发明申请

WO2006068954A2 PYRAZOLO[1,5-A]PYRIMIDINE ADENOSINE A2a RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡唑并[1,5-A]嘧啶腺苷A2a受体拮抗剂
公开(公告)号：WO2006068954A2
公开(公告)日：2006-06-29
申请号：PCT/US2005/045658
申请日：2005-12-19
申请人： SCHERING CORPORATION , CLASBY, Martin, C. , CHACKALAMANNIL, Samuel , NEUSTADT, Bernard, R. , GAO, Xiaobang
发明人： CLASBY, Martin, C. , CHACKALAMANNIL, Samuel , NEUSTADT, Bernard, R. , GAO, Xiaobang
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亚基; 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，羟烷基，氨烷基，环烷基，杂环烷基，被烷基取代的杂环烷基，任选被取代的芳烷基或任选被取代的杂芳烷基; 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。还公开了所述化合物单独或与其他治疗帕金森氏病的药剂组合用于治疗帕金森病的用途，包含它们的药物组合物和包含所述组合的组分的药盒。

10. 发明申请

WO2003033501A1 HIMBACINE ANALOGUES AS THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译： HIMBACINE ANALOGUES as THROMBIN RECEPTOR ANTAGONISTS
公开(公告)号：WO2003033501A1
公开(公告)日：2003-04-24
申请号：PCT/US2002/032936
申请日：2002-10-16
申请人： SCHERING CORPORATION
发明人： CHACKALAMANNIL, Samuel , CHELLIAH, Mariappan, V. , CLASBY, Martin, C. , XIA, Yan
IPC分类号： C07D491/04
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Heterocyclic-substituted tricyclics of the 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 alkyl or optionally substituted alkenyl; R 22 is -COR 23 or a carboxy, sulfinyl, sulfonyl, sulfonamide or amino acid derivative; R 23 is haloalkyl; alkenyl; haloalkenyl; alkynyl; optionally substituted cycloalkyl; cycloalkyl-alkyl; aryl; arylalkyl; heteroaryl; heterocycloalkyl; or -COOH and/or -SO 3 H substituted alkyl; R 1 , R 2 , R 3 , R 9 , R 10 and R 11 are as defined in the specification; are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds.
摘要翻译：式（I）的杂环取代三环或其药学上可接受的盐，其中：n1和n2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 23是卤代烷基; 烯基; 卤代链; 炔基; 任选取代的环烷基; 环烷基 - 烷基; 芳基; 芳; 杂; 杂环; 或-COOH和/或-SO 3 H取代的烷基; R 1，R 2，R 3，R 9，R 10和R 11如说明书中所定义; 以及含有它们的药物组合物以及通过施用所述化合物治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭和癌症相关的疾病的方法。

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