公开(公告)号：WO2005063697A2

公开(公告)日：2005-07-14

申请号：PCT/US2004/042934

申请日：2004-12-21

Applicant: SCHERING CORPORATION ,  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: C07C257/00

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 D 1 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D 1 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: 本发明提供化合物，其为D 1受体的新型拮抗剂以及制备此类化合物的方法。 在另一个实施方案中，本发明提供了包含这种D 1受体拮抗剂的药物组合物以及使用它们治疗CNS病症，肥胖症，代谢病症，进食障碍例如食欲过盛和糖尿病的方法。 p>

公开(公告)号：WO2011149874A3

公开(公告)日：2014-03-20

申请号：PCT/US2011037651

申请日：2011-05-24

Applicant: MERCK SHARP & DOHME ,  TSUI HON-CHUNG ,  PALIWAL SUNIL ,  KIM HYUNJIN M ,  KEREKES ANGELA D ,  CAPLEN MARY ANN ,  ESPOSITE SARA J ,  MCKITTRICK BRIAN A ,  FISCHMANN THIERRY OLIVIER ,  DOLL RONALD J ,  RAINKA MATTHEW PAUL ,  LI ANG

Inventor： TSUI HON-CHUNG ,  PALIWAL SUNIL ,  KIM HYUNJIN M ,  KEREKES ANGELA D ,  CAPLEN MARY ANN ,  ESPOSITE SARA J ,  MCKITTRICK BRIAN A ,  FISCHMANN THIERRY OLIVIER ,  DOLL RONALD J ,  RAINKA MATTHEW PAUL ,  LI ANG

IPC: A61K31/497

CPC classification number: A61K45/06 ,  A61K31/4178 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/69 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D491/10 ,  C07D498/08 ,  A61K2300/00

Abstract: The present invention provides Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.

Abstract translation: 本发明提供式（I）的咪唑羧酰胺化合物：其中D，T，R 1，R 2，R 3和R 6如本文所定义，以及这些咪唑羧酰胺化合物的药学上可接受的盐。 咪唑羧酰胺化合物可用于治疗由过度刺激PDK-1信号通路引起的癌症和其他异常病症。

公开(公告)号：WO2010059611A2

公开(公告)日：2010-05-27

申请号：PCT/US2009/064762

申请日：2009-11-17

Applicant: SCHERING CORPORATION ,  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 ,  C07D401/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D493/10 ,  A61K31/422 ,  A61K31/427

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 below: (We bring to your attention that the illustrative compound of the invention is not provided on this electronic version as it is provided in the abstract of the paper copy)

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。 本发明的示例性化合物如下所示：（我们提请您注意，本发明的说明性化合物不是在该电子版本上提供的，如在本文摘要中提供的）

公开(公告)号：WO2010059602A2

公开(公告)日：2010-05-27

申请号：PCT/US2009/064738

申请日：2009-11-17

Applicant: SCHERING CORPORATION ,  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 ,  A61P9/00 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

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甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含该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，代谢病症 ，肥胖或肥胖相关病症，糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量受损或空腹血糖受损。 下面显示了本发明的说明性化合物：式（I）。

公开(公告)号：WO2018034917A1

公开(公告)日：2018-02-22

申请号：PCT/US2017/046183

申请日：2017-08-10

Applicant: MERCK SHARP & DOHME CORP. ,  CALDWELL, John, P. ,  CAPLEN, Mary Ann ,  CUMMING, Jared, N. ,  DYKSTRA, Kevin, D. ,  HRUZA, Alan ,  LANKIN, Claire ,  LI, Derun ,  LIU, Hong ,  MCCRACKEN, Amy ,  MCKITTRICK, Brian ,  RAO, Ashwin ,  TAGAT, Jayaram, R. ,  TANG, Haiqun ,  TAOKA, Brandon, M. ,  VERRAS, Andreas ,  WALSH, Shawn, P. ,  WU, Wen-Lian ,  ZHANG, Tianyuan

Inventor： CALDWELL, John, P. ,  CAPLEN, Mary Ann ,  CUMMING, Jared, N. ,  DYKSTRA, Kevin, D. ,  HRUZA, Alan ,  LANKIN, Claire ,  LI, Derun ,  LIU, Hong ,  MCCRACKEN, Amy ,  MCKITTRICK, Brian ,  RAO, Ashwin ,  TAGAT, Jayaram, R. ,  TANG, Haiqun ,  TAOKA, Brandon, M. ,  VERRAS, Andreas ,  WALSH, Shawn, P. ,  WU, Wen-Lian ,  ZHANG, Tianyuan

IPC: A61K31/445 ,  A61K31/47 ,  C07D215/16

Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.

Abstract translation: 本文描述了式I的化合物或其药学上可接受的盐。 式I化合物作为Cyp8b1抑制剂，可用于预防，治疗或作为糖尿病和心血管疾病的治疗剂。

公开(公告)号：WO2011149874A2

公开(公告)日：2011-12-01

申请号：PCT/US2011/037651

申请日：2011-05-24

Applicant: SCHERING CORPORATION ,  TSUI, Hon-Chung ,  PALIWAL, Sunil ,  KIM, Hyunjin, M. ,  KEREKES, Angela, D. ,  CAPLEN, Mary Ann ,  ESPOSITE, Sara, J. ,  MCKITTRICK, Brian, A. ,  FISCHMANN, Thierry Olivier ,  DOLL, Ronald, J. ,  RAINKA, Matthew Paul ,  LI, Ang

Inventor： TSUI, Hon-Chung ,  PALIWAL, Sunil ,  KIM, Hyunjin, M. ,  KEREKES, Angela, D. ,  CAPLEN, Mary Ann ,  ESPOSITE, Sara, J. ,  MCKITTRICK, Brian, A. ,  FISCHMANN, Thierry Olivier ,  DOLL, Ronald, J. ,  RAINKA, Matthew Paul ,  LI, Ang

IPC: C07D403/02

CPC classification number: A61K45/06 ,  A61K31/4178 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/69 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D491/10 ,  C07D498/08 ,  A61K2300/00

Abstract: The present invention provides Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R 1 , R 2 , R 3 , and R 6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.

Abstract translation: 本发明提供式（I）的咪唑羧酰胺化合物：其中D，T，R 1，R 2，R 3和R 6如本文所定义，以及这些咪唑羧酰胺化合物的药学上可接受的盐。 咪唑羧酰胺化合物可用于治疗由过度刺激PDK-1信号通路引起的癌症和其他异常病症。

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：WO2005021528A1

公开(公告)日：2005-03-10

申请号：PCT/US2004/027240

申请日：2004-08-23

Applicant: SCHERING CORPORATION ,  WU, Wen-Lian ,  BURNETT, Duane, A. ,  CAPLEN, Mary, Ann

Inventor： WU, Wen-Lian ,  BURNETT, Duane, A. ,  CAPLEN, Mary, Ann

IPC: C07D401/06

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

Abstract: The present invention discloses compounds of formula (I) wherein Ar, X, R 1 and 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.

Abstract translation: 本发明公开了本文定义的其中Ar，X，R 1和R 11的式（I）化合物，所述化合物是黑色素浓缩激素（MCH）的新型拮抗剂，以及制备此类化合物的方法 。 在另一个实施方案中，本发明公开了包含这样的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。

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：WO2010059606A2

公开(公告)日：2010-05-27

申请号：PCT/US2009/064747

申请日：2009-11-17

Applicant: SCHERING CORPORATION ,  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 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

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甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含该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，代谢病症 ，肥胖或肥胖相关病症，糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量受损或空腹血糖受损。 下面显示了本发明的说明性化合物。