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

Applicant: 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

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

CPC classification number: C07D451/06 ,  A61K31/439 ,  C07D401/14 ,  C07D451/14 ,  C07D471/08 ,  C07D487/08 ,  C07D491/08 ,  C07D495/08 ,  C07D498/08

Abstract: 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.

Abstract translation: 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。

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

Applicant: SCHERING CORP ,  CLASBY MARTIN C ,  CHACKALAMANNIL SAMUEL ,  STAMFORD ANDREW

Inventor： CLASBY MARTIN C ,  CHACKALAMANNIL SAMUEL ,  STAMFORD ANDREW

IPC: C07D487/04 ,  A61K31/522 ,  A61P25/16

CPC classification number: C07D487/04

Abstract: 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.

Abstract translation: 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。

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

Applicant: SCHERING CORP ,  CHACKALAMANNIL SAMUEL ,  CHELLIAH MARIAPPAN V ,  XIA YAN

Inventor： CHACKALAMANNIL SAMUEL ,  CHELLIAH MARIAPPAN V ,  XIA YAN

IPC: C07D263/52 ,  A61K31/4184 ,  A61P7/02 ,  A61P9/00

CPC classification number: C07D263/52 ,  C07D413/08

Abstract: 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.

Abstract translation: 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。

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

Applicant: SCHERING CORP ,  XIA YAN ,  CHACKALAMANNIL SAMUEL

Inventor： XIA YAN ,  CHACKALAMANNIL SAMUEL

IPC: A61K31/416 ,  A61K31/443 ,  A61K31/5377 ,  A61K45/06 ,  A61P7/02 ,  A61P9/00 ,  A61P25/28 ,  A61P35/00

CPC classification number: A61K31/443 ,  A61K31/416 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2007120730A3

公开(公告)日：2008-02-28

申请号：PCT/US2007008978

申请日：2007-04-11

Applicant: SCHERING CORP ,  XIA YAN ,  CHELLIAH MARIAPPAN V ,  CHACKALAMANNIL SAMUEL

Inventor： XIA YAN ,  CHELLIAH MARIAPPAN V ,  CHACKALAMANNIL SAMUEL

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

CPC classification number: C07D405/06 ,  C07D498/04

Abstract: 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 A n , E n , M n , G n , J n , R 3 , n 7 , R 8 , R 9 , R 10 , R 11 , R 32 , R 33 , 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.

Abstract translation: 式（I）的稠环，杂环取代三环或所述化合物的药学上可接受的盐或溶剂合物，异构体或外消旋混合物，其中式（II）表示任选的双键，并且其中A n N，N，N，N，N，N，N，N，N， >，n 7，R 8，R 9，R 10，R 11， >，R 32，R 33，X，Y，B和Het在本文中定义，并且其余取代基如说明书中所定义，以及药物 含有它们的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，心律失常，心力衰竭和癌症相关的疾病的方法。 还要求与其它心血管药物联合治疗。

公开(公告)号：WO2005030712A8

公开(公告)日：2007-12-21

申请号：PCT/US2004031495

申请日：2004-09-23

Applicant: SCHERING CORP ,  CHACKALAMANNIL SAMUEL ,  CHELLIAH MARIAPPAN V ,  XIA YAN

Inventor： CHACKALAMANNIL SAMUEL ,  CHELLIAH MARIAPPAN V ,  XIA YAN

IPC: C07D405/06 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D521/00

CPC classification number: C07D417/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14

Abstract: A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.

Abstract translation: 公开了一系列由结构式表示的化合物及其药学上可接受的异构体，盐，溶剂化物和多晶型物。 还公开了含有所述化合物的药物组合物及其作为大麻素受体的凝血酶受体拮抗剂和粘合剂的用途。

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

Applicant: 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

Inventor： 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: 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 classification number: A61K31/4525 ,  A61K31/343 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2009023664A3

公开(公告)日：2009-07-23

申请号：PCT/US2008072889

申请日：2008-08-12

Applicant: SCHERING CORP ,  NEELAMKAVIL SANTHOSH ,  BOYLE CRAIG D ,  CHACKALAMANNIL SAMUEL

Inventor： NEELAMKAVIL SANTHOSH ,  BOYLE CRAIG D ,  CHACKALAMANNIL SAMUEL

IPC: C07D223/08 ,  A61K31/55 ,  A61K31/551 ,  A61P3/00 ,  C07D223/12 ,  C07D243/08 ,  C07D401/12 ,  C07D409/04

CPC classification number: C07D223/08 ,  C07D223/04 ,  C07D223/12 ,  C07D223/30 ,  C07D243/08 ,  C07D401/12 ,  C07D409/04

Abstract: In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11BETA-hydroxysteroid dehydrogenase type-1, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11BETA-hydroxysteroid dehydrogenase type-1 using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明涉及可用于抑制11BETA-羟基类固醇脱氢酶-1型的新类别的取代的氮杂 - 和二氮杂 - 磺酰胺化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善 与使用此类化合物或药物组合物的11BETA-羟基类固醇脱氢酶1型的表达相关的一种或多种病症。

公开(公告)号：WO2008042422A2

公开(公告)日：2008-04-10

申请号：PCT/US2007021277

申请日：2007-10-02

Applicant: SCHERING CORP ,  CHACKALAMANNIL SAMUEL ,  CHELLIAH MARIAPPAN V ,  WANG YUGUGUANG ,  XIA YAN

Inventor： CHACKALAMANNIL SAMUEL ,  CHELLIAH MARIAPPAN V ,  WANG YUGUGUANG ,  XIA YAN

CPC classification number: C07D401/06 ,  C07D417/06

Abstract: 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 E, A, G M, Het, B, X, R 3 , R 10 , R 11 , R 32 and R 33 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.

Abstract translation: 式（I）的杂环取代三环或所述化合物，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，虚线任选是键或无键，得到双键或 单价，如价格要求所允许的，其中E，A，GM，Het，B，X，R 3，R 10，R 11， 本文定义了本发明的限制性实施方案，其中R 32，R 32和R 33，并且其余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，心律失常，心力衰竭和癌症相关的疾病。 还要求与其它心血管药物联合治疗。

公开(公告)号：WO2007075809A2

公开(公告)日：2007-07-05

申请号：PCT/US2006048646

申请日：2006-12-20

Applicant: SCHERING CORP ,  CHACKALAMANNIL SAMUEL ,  WANG YUGUANG

Inventor： CHACKALAMANNIL SAMUEL ,  WANG YUGUANG

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: Heterocyclic-substituted bi or 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 An, 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.

Abstract translation: 式（I）的杂环取代的二环或三环或所述化合物，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，虚线任选是键或无键，得到双键 或单价键，如价格要求所允许的，其中An，Mn，Un，Gn，Jn，Kn，R9，R10，R11，R32，R33，B和Het在本文中定义，其余取代基如 说明书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。 还要求与其它心血管药物联合治疗。