公开(公告)号：WO2010059606A3

公开(公告)日：2010-09-16

申请号：PCT/US2009064747

申请日：2009-11-17

Applicant: SCHERING CORP ,  TING PAULINE C ,  ASLANIAN ROBERT G ,  CAPLEN MARY ANN ,  CAO JIANHUA ,  KIM DAVID WON-SHIK ,  KIM HYUNJIN ,  KUANG RONGZE ,  LEE JOE F ,  SCHWERDT JOHN H ,  WU HEPING ,  ZHOU GANG ,  ZORN NICOLAS

Inventor： TING PAULINE C ,  ASLANIAN ROBERT G ,  CAPLEN MARY ANN ,  CAO JIANHUA ,  KIM DAVID WON-SHIK ,  KIM HYUNJIN ,  KUANG RONGZE ,  LEE JOE F ,  SCHWERDT JOHN H ,  WU HEPING ,  ZHOU GANG ,  ZORN NICOLAS

IPC: C07D401/12 ,  A61K31/422 ,  A61K31/427 ,  A61K31/506 ,  A61P3/00 ,  A61P9/00 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.

Abstract translation: 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物以及该化合物用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关障碍的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本发明的说明性化合物如下所示。

公开(公告)号：WO2010059611A3

公开(公告)日：2010-11-18

申请号：PCT/US2009064762

申请日：2009-11-17

Applicant: SCHERING CORP ,  TING PAULINE C ,  ASLANIAN ROBERT G ,  CAO JIANHUA ,  CAPLEN MARY ANN ,  CHAN TIN-YAU ,  KIM HYUNJIN ,  KIM JAE-HUN ,  KUANG RONGZE ,  LEE JOE F ,  WU HEPING

Inventor： TING PAULINE C ,  ASLANIAN ROBERT G ,  CAO JIANHUA ,  CAPLEN MARY ANN ,  CHAN TIN-YAU ,  KIM HYUNJIN ,  KIM JAE-HUN ,  KUANG RONGZE ,  LEE JOE F ,  WU HEPING

IPC: C07D213/74 ,  A61K31/422 ,  A61K31/427 ,  C07D401/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D493/10

CPC classification number: C07D413/12 ,  A61K31/422 ,  A61K31/427 ,  C07D213/74 ,  C07D401/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D493/10

Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown with this abstract.

Abstract translation: 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物以及该化合物用于治疗或预防心血管疾病，代谢障碍，肥胖症或肥胖相关病症的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本摘要显示了本发明的说明性化合物。

公开(公告)号：WO2010059602A3

公开(公告)日：2010-07-15

申请号：PCT/US2009064738

申请日：2009-11-17

Applicant: SCHERING CORP ,  TING PAULINE C ,  ASLANIAN ROBERT G ,  CAPLEN MARY ANN ,  CAO JIANHUA ,  CHAN TIN-YAU ,  KIM DAVID WON-SHIK ,  KIM HYUNJIN ,  KIM JAE-HUN ,  KUANG RONGZE ,  LEE JOE F ,  SCHWERDT JOHN H ,  WU HEPING ,  ZORN NICOLAS

Inventor： TING PAULINE C ,  ASLANIAN ROBERT G ,  CAPLEN MARY ANN ,  CAO JIANHUA ,  CHAN TIN-YAU ,  KIM DAVID WON-SHIK ,  KIM HYUNJIN ,  KIM JAE-HUN ,  KUANG RONGZE ,  LEE JOE F ,  SCHWERDT JOHN H ,  WU HEPING ,  ZORN NICOLAS

IPC: A61P3/00 ,  A61K31/422 ,  A61K31/427 ,  A61P9/00 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04

CPC classification number: C07D413/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04

Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).

Abstract translation: 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物以及该化合物用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关障碍的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本发明的说明性化合物如下所示：式（I）。

公开(公告)号：WO2007084595A3

公开(公告)日：2007-09-07

申请号：PCT/US2007001302

申请日：2007-01-18

Applicant: SCHERING CORP ,  ASBEROM THEODROS ,  BARA THOMAS ,  BENNETT CHAD E ,  BURNETT DUANE A ,  CAPLEN MARY ANN ,  CLADER JOHN W ,  COLE DAVID J ,  DOMALSKI MARTIN S ,  JOSIEN HUBERT B ,  KNUTSON CHAD E ,  LI HONGMEI ,  MCBRIAR MARK D ,  PISSARNITSKI DMITRI A ,  QIANG LI ,  RAJAGOPALAN MURALI ,  SASIKUMAR THAVALAKULAMGAR K ,  SU JING ,  TANG HAIQUN ,  WU WEN-LIAN ,  XU RUO ,  ZHAO ZHIQIANG

Inventor： ASBEROM THEODROS ,  BARA THOMAS ,  BENNETT CHAD E ,  BURNETT DUANE A ,  CAPLEN MARY ANN ,  CLADER JOHN W ,  COLE DAVID J ,  DOMALSKI MARTIN S ,  JOSIEN HUBERT B ,  KNUTSON CHAD E ,  LI HONGMEI ,  MCBRIAR MARK D ,  PISSARNITSKI DMITRI A ,  QIANG LI ,  RAJAGOPALAN MURALI ,  SASIKUMAR THAVALAKULAMGAR K ,  SU JING ,  TANG HAIQUN ,  WU WEN-LIAN ,  XU RUO ,  ZHAO ZHIQIANG

IPC: C07D311/22 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06

CPC classification number: C07D311/22 ,  C07C317/14 ,  C07C317/20 ,  C07C317/44 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D493/04

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R 2 and R 3 , or R 2 and R 4 , or R 3 and R 4 , together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Abstract translation: 本发明公开了下式的新型γ分泌酶抑制剂：R 2和R 3，或R 2和R 4 O / >或R 3和R 4以及它们所结合的原子可以形成稠合的环烷基或稠合的杂环烷基环。 环烷基环或杂环烷基环可任选被一个或多个取代基取代。 一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如， 治疗阿尔茨海默病。

公开(公告)号：WO2005063697A3

公开(公告)日：2005-12-22

申请号：PCT/US2004042934

申请日：2004-12-21

Applicant: SCHERING CORP ,  BURNETT DUANE A ,  WU WEN-LIAN ,  DOMALSKI MARTIN S ,  CAPLEN MARY ANN ,  SPRING RICHARD ,  LACHOWICZ JEAN E

Inventor： BURNETT DUANE A ,  WU WEN-LIAN ,  DOMALSKI MARTIN S ,  CAPLEN MARY ANN ,  SPRING RICHARD ,  LACHOWICZ JEAN E

IPC: A61K31/277 ,  A61K31/405 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K45/06 ,  C07C255/57 ,  C07C257/14 ,  C07C257/18 ,  C07D211/28 ,  C07D295/155 ,  C07D295/205 ,  C07D295/14

CPC classification number: C07D295/205 ,  A61K45/06 ,  C07C255/57 ,  C07C257/14 ,  C07C257/18 ,  C07D209/08 ,  C07D209/86 ,  C07D211/14 ,  C07D213/53 ,  C07D215/26 ,  C07D215/48 ,  C07D233/64 ,  C07D295/073 ,  C07D295/112 ,  C07D295/155 ,  C07D317/58 ,  C07D319/18 ,  C07D333/20 ,  C07D405/12

Abstract: The present invention provides compounds, which, are novel antagonists for D1 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract translation: 本发明提供了作为D1受体的新型拮抗剂的化合物以及这些化合物的制备方法。 在另一个实施方案中，本发明提供包含这种D1受体拮抗剂的药物组合物以及使用它们治疗CNS障碍，肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

公开(公告)号：JP2010047618A

公开(公告)日：2010-03-04

申请号：JP2009275958

申请日：2009-12-03

Applicant: Schering Corp ,  シェーリング コーポレイションSchering Corporation

Inventor： WU WEN-LIAN ,  BURNETT DUANE A ,  CAPLEN MARY ANN

IPC: C07D401/06 ,  A61K31/454 ,  A61K45/00 ,  A61P1/16 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  A61P35/00 ,  A61P43/00 ,  C07D401/08 ,  C07D401/14 ,  C07D417/14

CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D417/14

Abstract: PROBLEM TO BE SOLVED: To provide new biaryl-piperidin-4-ylidene-methylbenzimidazole derivatives with antagonists activity for MCH (melanin-concentrating hormone). SOLUTION: There are disclosed the compounds represented by formula (I) wherein Ar, X, R 1 and R 11 are specifically defined, the compounds being new antagonists for MCH, as well as methods for preparing such compounds. In another embodiment, there are disclosed pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. COPYRIGHT: (C)2010,JPO&INPIT

Abstract translation: 要解决的问题：提供具有MCH（黑色素浓缩激素）拮抗剂活性的新的联芳基 - 哌啶-4-亚基 - 甲基苯并咪唑衍生物。 解决方案：公开了由式（I）表示的化合物，其中Ar，X，R 11，R 11和R 11是特异性定义的，该化合物是新的拮抗剂 MCH，以及制备这些化合物的方法。 在另一个实施方案中，公开了包含这样的MCH拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。 版权所有（C）2010，JPO＆INPIT

公开(公告)号：NO20083598L

公开(公告)日：2008-10-20

申请号：NO20083598

申请日：2008-08-19

Applicant: SCHERING CORP

Inventor： ASBEROM THEODROS ,  LI HONGMEI ,  SU JING ,  TANG HAIQUN ,  BARA THOMAS A ,  BENNETT CHAD E ,  BURNETT DUANE A ,  CAPLEN MARY ANN ,  CLADER JOHN W ,  COLE DAVID J ,  DOMALSKI MARTIN S ,  JOSIEN HUBERT B ,  KNUTSON CHAD E ,  MCBRIAR MARK D ,  PISSARNITSKI DMITRI A ,  QIANG LI ,  RAJAGOPALAN MURALI ,  SASIKUMAR THAVALAKULAMGAR K ,  WU WEN-LIAN ,  XU RUO

IPC: C07D311/22 ,  C07C317/14

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

公开(公告)号：MXPA06002201A

公开(公告)日：2006-04-27

申请号：MXPA06002201

申请日：2004-08-23

Applicant: SCHERING CORP

Inventor： CAPLEN MARY ANN

IPC: A61K31/437 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D401/06 ,  C07D401/14 ,  C07D417/14

Abstract: La presente invencion describe compuestos de formula I (ver formula) en la cual Ar, X, R1 y R11 son tal como se definen aqui, dichos compuestos son nuevos antagonistas para la hormona concentradora de melanina (MCH), asi como tambien metodos para preparar dichos compuestos; en otra modalidad, la invencion describe composiciones farmaceuticas que comprenden dichos antagonistas de MCH, asi como tambien metodos para el uso de los mismos para tratar la obesidad, los desordenes metabolicos, los desordenes de la alimentacion, tales como hiperfagia y diabetes.

公开(公告)号：CA2536544A1

公开(公告)日：2005-03-10

申请号：CA2536544

申请日：2004-08-23

Applicant: SCHERING CORP

Inventor： BURNETT DUANE A ,  CAPLEN MARY ANN ,  WU WEN-LIAN

IPC: C07D401/06 ,  A61K31/437 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D401/14 ,  C07D417/14

Abstract: The present invention discloses compounds of formula (I) wherein Ar, X, R1 a nd R 11 are herein defined, said compounds being novel antagonists for melanin- concentrating hormone (MCH), as well as methods for preparing such compounds . In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

公开(公告)号：CA2466728C

公开(公告)日：2008-09-02

申请号：CA2466728

申请日：2002-11-14

Applicant: SCHERING CORP

Inventor： WU WEN-LIAN ,  TULSHIAN DEEN ,  DOMALSKI MARTIN S ,  HO GINNY D ,  CZARNIECKI MICHAEL F ,  BURNETT DUANE A ,  CAPLEN MARY ANN

IPC: C07D205/04 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K45/06 ,  A61P11/06 ,  A61P11/14 ,  A61P25/00 ,  A61P25/04 ,  A61P25/22 ,  A61P25/24 ,  A61P25/32 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06 ,  C07D521/00

Abstract: Disclosed are nociceptin ORL-1 receptor agonists of formula (I) wherein; (a) R1 is optionally substituted alkyl, fluorenyl, pyrimidinyl or optionally substituted piperidinyl; R2 is H; and R3 is -C(H)(R)-NR7R8; R is H, optionally substituted aryl or arylalkyl, or heteroaryl; R7 is -(CH2)xR9, optionally substituted tetrahydronaphthyl, or cycloalkyl; and R8 is H; or R7 and R8 together form a substituted piperidinyl or piperazinyl ring; x is 0- 10; and R9 is H, alkoxy, optionally substituted phenyl, naphthyl, heteroaryl, pyrrolidinyl, pyrrolidonyl, optionally substituted piperidinyl or diphenylmethyl; or (b) R2 is -NHR7 or formula (II) and R3 is H; pharmaceutical compositions; and methods of using the compounds to treat cough and pain.