公开(公告)号：EP1660443B1

公开(公告)日：2009-03-04

申请号：EP04779938.2

申请日：2004-08-04

申请人： Schering Corporation ,  Pharmacopeia Drug Discovery, Inc.

发明人： CUMMING, Jared, N. ,  ISERLOH, Ulrich ,  STAMFORD, Andrew ,  STRICKLAND, Corey ,  VOIGT, Johannes, H. ,  WU, Yusheng ,  HUANG, Ying ,  XIA, Yan ,  CHACKALAMANNIL, Samuel ,  GUO, Tao ,  HOBBS, Douglas, W. ,  LE, Thuy, X., H. ,  LOWRIE, Jeffrey, F. ,  SAIONZ, Kurt, W. ,  BABU, Suresh, D.

IPC分类号： C07D201/00

CPC分类号： C07D243/08 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/26 ,  C07D209/52 ,  C07D211/26 ,  C07D211/46 ,  C07D217/18 ,  C07D233/32 ,  C07D241/04 ,  C07D241/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06

摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R is-C(O)-N(R27 )(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer’s disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, and N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

公开(公告)号：EP1660443A2

公开(公告)日：2006-05-31

申请号：EP04779938.2

申请日：2004-08-04

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： CUMMING, Jared, N. ,  ISERLOH, Ulrich ,  STAMFORD, Andrew ,  STRICKLAND, Corey ,  VOIGT, Johannes, H. ,  WU, Yusheng ,  HUANG, Ying ,  XIA, Yan ,  CHACKALAMANNIL, Samuel ,  GUO, Tao ,  HOBBS, Douglas, W. ,  LE, Thuy, X., H. ,  LOWRIE, Jeffrey, F. ,  SAIONZ, Kurt, W. ,  BABU, Suresh, D.

IPC分类号： C07D201/00

CPC分类号： C07D243/08 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/26 ,  C07D209/52 ,  C07D211/26 ,  C07D211/46 ,  C07D217/18 ,  C07D233/32 ,  C07D241/04 ,  C07D241/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06

摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R is-C(O)-N(R27 )(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer’s disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, and N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

摘要翻译： 公开了下式化合物或其药学上可接受的盐或溶剂化物，其中R为-C（O）-N（R 27）（R 28）或其余变量如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经退行性疾病例如阿尔茨海默氏病的方法。 还公开了治疗认知或神经退行性疾病的药物组合物和方法，其包含式I化合物与不同于式I的那些β-分泌酶抑制剂，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂， 类固醇抗炎剂和N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂或抗淀粉样蛋白抗体。

公开(公告)号：EP2473491A1

公开(公告)日：2012-07-11

申请号：EP10722268.9

申请日：2010-06-01

申请人： Mochida Pharmaceutical Co., Ltd. ,  Schering Corporation

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）的化合物或其药学上可接受的盐或溶剂化物，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，高凝血或纤维化改变的方法。

公开(公告)号：EP2217596A2

公开(公告)日：2010-08-18

申请号：EP08832779.6

申请日：2008-08-20

申请人： Schering Corporation

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： C07D451/06 ,  C07D471/08 ,  C07D498/08 ,  C07D487/08 ,  C07D491/08 ,  A61K31/46 ,  A61K31/439 ,  A61K31/506 ,  A61K31/537 ,  A61P3/00 ,  C07D401/14 ,  C07D495/08

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.

公开(公告)号：EP2032560A1

公开(公告)日：2009-03-11

申请号：EP07796505.1

申请日：2007-06-27

申请人： Schering Corporation

发明人： CHELLIAH, Mariappan, V. ,  CHACKALAMANNIL, Samuel ,  XIA, Yan

IPC分类号： C07D405/06 ,  A61K31/443 ,  A61P7/02 ,  A61P35/00

CPC分类号： C07D405/06

摘要： Substituted bicyclic and tricyclic modified himbacine derivative of the formula (I) : or a pharmaceutically acceptable salt or solvate of said compound wherein (DU) represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined 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 agents is also claimed.

公开(公告)号：EP1802609A2

公开(公告)日：2007-07-04

申请号：EP05802841.6

申请日：2005-10-05

申请人： SCHERING CORPORATION

发明人： CHACKALAMANNIL, Samuel ,  CHELLIAH, Mariappan, V. ,  XIA, Yan ,  EAGEN, Keith, A.

IPC分类号： C07D405/06 ,  C07D409/14 ,  C07D491/10 ,  C07D413/14 ,  C07D405/14 ,  A61K31/443 ,  A61P7/00

CPC分类号： C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/10

摘要： Heterocyclic-substituted tricyclics of the formula (I) 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 A, B, G, M, X, J, n, Het, R3, R10, R11, R32 and R33 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： 式（I）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合物，其中----代表任选的双键，虚线任选为键或无键，产生 如化合价要求所允许的，并且其中A，B，G，M，X，J，n，Het，R 3，R 10，R 11，R 32和R 33在本文中定义并且其余取代基如定义 在说明书中公开了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。

公开(公告)号：EP2373634A1

公开(公告)日：2011-10-12

申请号：EP09768572.1

申请日：2009-12-03

申请人： Mochida Pharmaceutical Co., Ltd. ,  Schering Corporation

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： 本发明提供如本文所述的式（I）化合物或其药学上可接受的盐或溶剂合物。 本发明还提供了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。

公开(公告)号：EP1436298B1

公开(公告)日：2011-09-21

申请号：EP02801732.5

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 ,  A61K31/445 ,  A61K31/34 ,  A61P29/00 ,  A61P19/02 ,  A61P9/00

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: n1 and n2 are independently 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is alkyl or optionally substituted alkenyl; R22 is -COR23 or a carboxy, sulfinyl, sulfonyl, sulfonamide or amino acid derivative; R23 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, R2, R3, R9, R10 and R11¿ 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.

公开(公告)号：EP2007755A2

公开(公告)日：2008-12-31

申请号：EP07775221.0

申请日：2007-04-11

申请人： Schering Corporation

发明人： XIA, Yan ,  CHELLIAH, Mariappan, V. ,  CHACKALAMANNIL, Samuel

IPC分类号： C07D405/06 ,  A61K31/443 ,  A61P7/02

CPC分类号： C07D405/06 ,  C07D498/04

摘要： Fused-ring, heterocyclic-substituted tricyclics of the Formula (I) or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein Formula (II) represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, 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： 式（I）的稠合环，杂环取代的三环或所述化合物，其异构体或外消旋混合物的药学上可接受的盐或溶剂合物，其中式（II）表示任选的双键，并且其中An，En，Mn，Gn， 本文定义了Jn，R3，n7，R8，R9，R10，R11，R32，R33，X，Y，B和Het，其余的取代基如说明书中所定义，以及含有它们的药物组合物和 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，心律不齐，心力衰竭和癌症相关的疾病的方法。 本发明还要求与其他心血管药物组合治疗。

公开(公告)号：EP1863778A2

公开(公告)日：2007-12-12

申请号：EP06739957.6

申请日：2006-03-29

申请人： Schering Corporation

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。