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1. 发明专利

CA2745121A1 MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS 未知
公开(公告)号：CA2745121A1
公开(公告)日：2010-06-10
申请号：CA2745121
申请日：2009-12-03
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
IPC分类号： C07D265/30 , A61K31/4725 , A61K31/5355 , A61K31/54 , A61K31/553 , A61P7/00 , C07D265/32 , C07D267/10 , C07D279/06 , C07D401/12 , 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.

2. 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.

3. 发明公开

EP2934536A4 FACTOR IXa INHIBITORS 有权转让
公开(公告)号：EP2934536A4
公开(公告)日：2016-09-21
申请号：EP13863880
申请日：2013-12-16
申请人： MERCK SHARP & DOHME , MOCHIDA PHARM CO LTD
发明人： HIRABAYASHI TOMOKAZU , KATSUNO MIKA , SMITH CAMERON JAMES , SHERER EDWARD , CAMPEAU LOUIS-CHARLES , BALKOVEC JAMES , GREENLEE WILLIAM JOHN , LI DERUN , GUO LIANGQIN , CHAN TIN YAN , CHEN YI-HENG , CHEN YILI , CHACKALAMANNIL SAMUEL , TAN JOHN QIANG
IPC分类号： C07D413/12 , A61K31/5377
CPC分类号： C07D513/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D471/04 , C07D498/04
摘要： The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

4. 发明公开

EP2770998A4 FACTOR IXA INHIBITORS 有权转让
公开(公告)号：EP2770998A4
公开(公告)日：2015-03-18
申请号：EP12843432
申请日：2012-10-24
申请人： MERCK SHARP & DOHME , MOCHIDA PHARM CO LTD , ALBANY MOLECULAR RES INC
发明人： CHACKALAMANNIL SAMUEL , OHKOUCHI MUNETAKA , VOSS MATTHEW , SONE HIROKI
IPC分类号： A61K31/4412 , A61K31/4375 , A61K31/4439 , A61K31/4725 , A61K31/5377 , A61P7/02 , C07D401/12 , C07D413/12 , C07D413/14 , C07D471/04
CPC分类号： C07D401/12 , A61K31/4375 , A61K31/4439 , A61K31/4725 , A61K31/5377 , A61K45/06 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt 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.

5. 发明公开

EP2934538A4 FACTOR IXA INHIBITORS 有权转让
标题翻译： FAKTOR-IXA-缝边
公开(公告)号：EP2934538A4
公开(公告)日：2016-06-08
申请号：EP13873301
申请日：2013-12-16
申请人： MERCK SHARP & DOHME , MOCHIDA PHARM CO LTD
发明人： SMITH CAMERON JAMES , TAN JOHN QIANG , ZHANG TING , BALKOVEC JAMES , GREENLEE WILLIAM JOHN , GUO LIANGQIN , XU JIAYI , CHEN YI-HENG , CHEN YILI , CHACKALAMANNIL SAMUEL , HIRABAYASHI TOMOKAZU , NAGASUE HIROSHI , OGAWA KOUKI
IPC分类号： C07D413/12 , A61K31/5377 , A61P7/02
CPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.
摘要翻译：本发明提供式（I）化合物，其中R 1为H或C 1-6烷基，R 2为H或C 1-6烷基或CH 2 OH，R 3为H或C 1-6烷基，R 4为H或C 1-6 烷基，条件是当R 1，R 2和R 3为H时，R 4为C 1-6烷基，当R 1，R 2和R 4为H时，R 3为C 1-6烷基，当R 1，R 3和R 4为H ，R2是C1-6烷基或-CH2OH，当R2，R3和R4是H时，R1是C1-6烷基; A是1）具有1-3个独立地选自N，S和O的杂原子的9-10元双环杂环，其中9-10元双环杂环是未取代的或被R 5取代且未被取代或被R 6取代且未取代或被NH 2取代，或2）未被取代或被未取代或被R 6取代的R 5取代的未取代或被-CH 2 NH 2取代的6-9元单环或双环碳环系统; 且B为1）具有1或2个独立地选自N，S或O的杂原子的5或6元单环杂环，其未取代或在碳或氮原子上被取代或未取代或在碳或氮上取代的R7取代具有R 8的未取代或取代的碳原子或氮原子上的取代基，或2）具有1,2或3个氮原子的8或9元稠合双环杂环，其未被取代或在碳原子或氮原子上被取代， R7，并且在碳或氮原子上未被取代或取代为R8; 和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的方法。

6. 发明公开

EP2934537A4 FACTOR IXA INHIBITORS 有权转让
标题翻译：因子IXA-缝边
公开(公告)号：EP2934537A4
公开(公告)日：2016-05-25
申请号：EP13866418
申请日：2013-12-16
申请人： MERCK SHARP & DOHME , MOCHIDA PHARM CO LTD
发明人： SMITH CAMERON JAMES , TAN JOHN QIANG , ZHANG TING , BALKOVEC JAMES , GREENLEE WILLIAM JOHN , GUO LIANGQIN , CHEN YI-HENG , CHEN YILI , CHACKALAMANNIL SAMUEL , HIRABAYASHI TOMOKAZU , KATSUNO MIKA
IPC分类号： A61K31/5377 , C07D413/12 , C07D413/14 , C07D513/04
CPC分类号： C07D413/14 , C07D413/12 , C07D513/04
摘要： The present invention provides a compound of Formula (I) wherein R1, R2, R3 and R4 are independently H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl, and when R2, R3, and R4 are H, R is C1-6 alkyl; and 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：本发明提供式（I）化合物，其中R 1，R 2，R 3和R 4独立地为H或C 1-6烷基，条件是当R 1，R 2和R 3为H时，R 4为C 1-6烷基，中，R 2和R 4为H，R 3为C 1-6烷基，当R 1，R 3和R 4为H时，R 2为C 1-6烷基，当R 2，R 3和R 4为H时，R为C 1-6烷基 ; 以及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。

7. 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。

8. 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。

9. 发明申请

WO2006105217A3 SPIROCYCLIC THROMBIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2006105217A3
公开(公告)日：2006-11-23
申请号：PCT/US2006011499
申请日：2006-03-29
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , XIA YAN
发明人： CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , XIA YAN
IPC分类号： C07D263/52 , A61K31/4184 , A61P7/02 , A61P9/00
CPC分类号： C07D263/52 , C07D413/08
摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein An, En, Mn, Un, Gn, Jn, Kn, R9, R10, R11, R32, R33, B and Het are herein defined and the remaining substituents 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. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译：下式的杂环取代的三环或所述化合物，异构体或外消旋混合物的药学上可接受的盐或溶剂化物，其中代表任选的双键，虚线任选为键或无键，产生双键或单键，如化合价要求所允许的，并且其中An，En，Mn，Un，Gn，Jn，Kn，R9，R10，R11，R32，R33，B和Het在本文中定义且其余取代基如说明书中所定义，公开了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，心力衰竭和癌症有关的疾病的方法。本发明还要求与其他心血管药物组合治疗。

10. 发明申请

WO2009124103A3 COMBINATION THERAPIES COMPRISING PAR1 ANTAGONISTS WITH PAR4 ANTAGONISTS 审中-公开
标题翻译：包含PAR1拮抗剂与PAR4拮抗剂的组合治疗
公开(公告)号：WO2009124103A3
公开(公告)日：2010-01-14
申请号：PCT/US2009039070
申请日：2009-04-01
申请人： SCHERING CORP , XIA YAN , CHACKALAMANNIL SAMUEL
发明人： XIA YAN , CHACKALAMANNIL SAMUEL
IPC分类号： A61K31/416 , A61K31/443 , A61K31/5377 , A61K45/06 , A61P7/02 , A61P9/00 , A61P25/28 , A61P35/00
CPC分类号： A61K31/443 , A61K31/416 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to a pharmaceutical composition comprising an effective amount of at least one PAR1 antagonist, at least one PAR4 antagonist, optionally, an effective amount of at least one cardiovascular agent, and, optionally, a pharmaceutically acceptable carrier. The present invention also provides for the use of theses pharmaceutical compositions to treat various diseases associated with thrombosis.
摘要翻译：本发明涉及包含有效量的至少一种PAR1拮抗剂，至少一种PAR4拮抗剂，任选的有效量的至少一种心血管药物和任选的药学上可接受的载体的药物组合物。本发明还提供了这些药物组合物用于治疗与血栓形成相关的各种疾病的用途。

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