公开(公告)号：WO2013010092A1

公开(公告)日：2013-01-17

申请号：PCT/US2012/046699

申请日：2012-07-13

Applicant: NOVARTIS AG ,  CHEUNG, Atwood, Kim ,  CHIN, Donoval, Noel ,  FAN, Jianmei ,  SHULTZ, Michael, David ,  TOMLINSON, Ronald, Charles

Inventor： CHEUNG, Atwood, Kim ,  CHIN, Donoval, Noel ,  FAN, Jianmei ,  SHULTZ, Michael, David ,  TOMLINSON, Ronald, Charles

IPC: C07D491/052 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D491/052 ,  A61K31/519

Abstract: The present invention provides for compounds of formula (I) wherein R 1 and R 2 are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

Abstract translation: 本发明提供式（I）化合物，其中R 1和R 2在本文中定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。

公开(公告)号：WO2003027069A1

公开(公告)日：2003-04-03

申请号：PCT/US2002/030543

申请日：2002-09-24

Applicant: BAYER PHARMACEUTICALS CORPORATION ,  SMITH, Roger, A. ,  KLUENDER, Harold, C. E. ,  SU, Ning ,  LAVOIE, Rico, C. ,  FAN, Jianmei

Inventor： SMITH, Roger, A. ,  KLUENDER, Harold, C. E. ,  SU, Ning ,  LAVOIE, Rico, C. ,  FAN, Jianmei

IPC: C07D207/34

CPC classification number: C07D401/06 ,  C07D207/34 ,  C07D401/12

Abstract: This invention relates to pyrrole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.

Abstract translation: 本发明涉及已被发现抑制食欲并引起体重减轻的吡咯衍生物。 本发明还提供了合成化合物的方法，包含该化合物的药物组合物，以及使用这些组合物诱导体重减轻和治疗肥胖症和肥胖相关疾病的方法。

公开(公告)号：WO2013012723A1

公开(公告)日：2013-01-24

申请号：PCT/US2012/046673

申请日：2012-07-13

Applicant: NOVARTIS AG ,  CHEN, Zhuoliang ,  CHEUNG, Atwood, Kim ,  CHIN, Donovan, Noel ,  FAN, Jianmei ,  MILLER-MOSLIN, Karen, Marie ,  SHULTZ, Michael, David ,  SMITH, Troy, D. ,  TOMLINSON, Ronald, Charles ,  TOURE, Bakary-Barry ,  VISSER, Michael, Scott

Inventor： CHEUNG, Atwood, Kim ,  CHIN, Donovan, Noel ,  FAN, Jianmei ,  MILLER-MOSLIN, Karen, Marie ,  SHULTZ, Michael, David ,  SMITH, Troy, D. ,  TOMLINSON, Ronald, Charles ,  TOURE, Bakary-Barry ,  VISSER, Michael, Scott

IPC: C07D401/12 ,  C07D409/14 ,  C07D491/052 ,  A61K31/519 ,  A61K31/517 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D491/052 ,  A61K31/453 ,  A61K31/4545 ,  C07D401/12 ,  C07D409/14 ,  C07D493/04

Abstract: The present invention provides for compounds of formula (I), wherein R 1 -R 5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

Abstract translation: 本发明提供式（I）化合物，其中R 1 -R 5和L如本文所定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。

公开(公告)号：WO2004078748A3

公开(公告)日：2004-11-11

申请号：PCT/US2004006287

申请日：2004-03-01

Applicant: BAYER PHARMACEUTICALS CORP ,  DUMAS JACQUES ,  BOYER STEPHEN ,  VERMA SHARAD ,  ADNANE LILA ,  CHEN YUANWEI ,  LEE WENDY ,  PHILLIPS BARTON ,  SMITH ROGER A ,  SCOTT WILLIAM J ,  BURKE JENNIFER ,  CHEN JIANQING ,  CHEN ZHI ,  FAN JIANMEI ,  MIRANDA KARL ,  RAUDENBUSH BRIAN ,  REDMAN ANIKO ,  SHAO JIANXING ,  SU NING ,  WANG GAN ,  YI LIN ,  ZHU QINGMING

Inventor： DUMAS JACQUES ,  BOYER STEPHEN ,  VERMA SHARAD ,  ADNANE LILA ,  CHEN YUANWEI ,  LEE WENDY ,  PHILLIPS BARTON ,  SMITH ROGER A ,  SCOTT WILLIAM J ,  BURKE JENNIFER ,  CHEN JIANQING ,  CHEN ZHI ,  FAN JIANMEI ,  MIRANDA KARL ,  RAUDENBUSH BRIAN ,  REDMAN ANIKO ,  SHAO JIANXING ,  SU NING ,  WANG GAN ,  YI LIN ,  ZHU QINGMING

IPC: A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61P35/00 ,  C07D213/89 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  C07D213/89 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: This invention relates to novel diary) ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.

Abstract translation: 本发明涉及新颖的日记尿素，含有这些化合物的药物组合物，以及这些化合物或组合物用于治疗高增殖和血管生成障碍，作为唯一试剂或与细胞毒性疗法组合的用途。

公开(公告)号：WO2009118305A1

公开(公告)日：2009-10-01

申请号：PCT/EP2009/053421

申请日：2009-03-24

Applicant: NOVARTIS AG ,  SHULTZ, Michael ,  CHEN, Christine, Hiu-Tung ,  CHO, Young Shin ,  JIANG, Lei ,  FAN, Jianmei ,  LIU, Gang ,  MAJUMDAR, Dyuti

Inventor： SHULTZ, Michael ,  CHEN, Christine, Hiu-Tung ,  CHO, Young Shin ,  JIANG, Lei ,  FAN, Jianmei ,  LIU, Gang ,  MAJUMDAR, Dyuti

IPC: C07D207/08 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D471/04 ,  A61K31/4025 ,  A61P35/00 ,  C07D401/06

CPC classification number: C07D207/08 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D471/04

Abstract: The present teachings relate to compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R 1 , R 2 , R 3 , Y, Z, and (A) are as defined herein. The present teachings also provide methods of preparing compounds of Formula (I) and methods of using compounds of Formula (I) in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐，水合物，酯和前药，其中R1，R2，R3，Y，Z和（A）如本文所定义。 本教导还提供了制备式（I）化合物的方法和使用式（I）化合物治疗，抑制或预防完全或部分由脱乙酰酶介导的病理状况或病症的方法。

公开(公告)号：WO2004078747A1

公开(公告)日：2004-09-16

申请号：PCT/US2004/006286

申请日：2004-03-01

Applicant: BAYER PHARMACEUTICALS CORPORATION ,  SCOTT, William, J. ,  DUMAS, Jacques ,  BOYER, Stephen ,  LEE, Wendy ,  CHEN, Yuanwei ,  PHILLIPS, Barton ,  VERMA, Sharad ,  CHEN, Jianqing ,  CHEN, Zhi ,  FAN, Jianmei ,  RAUDENBUSH, Brian ,  REDMAN, Aniko ,  YI, Lin ,  ZHU, Qingming

Inventor： SCOTT, William, J. ,  DUMAS, Jacques ,  BOYER, Stephen ,  LEE, Wendy ,  CHEN, Yuanwei ,  PHILLIPS, Barton ,  VERMA, Sharad ,  CHEN, Jianqing ,  CHEN, Zhi ,  FAN, Jianmei ,  RAUDENBUSH, Brian ,  REDMAN, Aniko ,  YI, Lin ,  ZHU, Qingming

IPC: C07D401/12

CPC classification number: C07D213/84 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

Abstract: This invention relates to novel diaryl ureas of Formula (I), pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper­proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.

Abstract translation: 本发明涉及式（I）的新型二芳基脲，含有这些化合物的药物组合物，以及这些化合物或组合物用于治疗过度增殖和血管生成障碍，作为唯一试剂或与细胞毒性疗法组合的用途。

公开(公告)号：WO2003072561A1

公开(公告)日：2003-09-04

申请号：PCT/US2003/005396

申请日：2003-02-21

Applicant: BAYER PHARMACEUTICALS CORPORATION ,  ZHANG, Chengzhi ,  BURKE, Michael ,  CHEN, Zhi ,  DUMAS, Jacques ,  FAN, Dongping ,  FAN, Jianmei ,  HATOUM-MOKDAD, Holia ,  JONES, Benjamin, D. ,  LADOUCEUR, Gaetan ,  LEE, Wendy ,  PHILLIPS, Barton

Inventor： ZHANG, Chengzhi ,  BURKE, Michael ,  CHEN, Zhi ,  DUMAS, Jacques ,  FAN, Dongping ,  FAN, Jianmei ,  HATOUM-MOKDAD, Holia ,  JONES, Benjamin, D. ,  LADOUCEUR, Gaetan ,  LEE, Wendy ,  PHILLIPS, Barton

IPC: C07D307/82

CPC classification number: C07D307/82 ,  C07D307/92 ,  C07D307/93 ,  C07D333/66 ,  C07D333/74 ,  C07D333/78 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D407/06 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D493/04

Abstract: This invention relates to novel benzofuran and benzothiophene derivatives of the general formula and their use for the treatment of hyper-proliferative disorders.

Abstract translation: 本发明涉及通式的新型苯并呋喃和苯并噻吩衍生物及其用于治疗高增殖性疾病的用途。

公开(公告)号：WO2004078747A8

公开(公告)日：2004-11-04

申请号：PCT/US2004006286

申请日：2004-03-01

Applicant: BAYER PHARMACEUTICALS CORP ,  SCOTT WILLIAM J ,  DUMAS JACQUES ,  BOYER STEPHEN ,  LEE WENDY ,  CHEN YUANWEI ,  PHILLIPS BARTON ,  VERMA SHARAD ,  CHEN JIANQING ,  CHEN ZHI ,  FAN JIANMEI ,  RAUDENBUSH BRIAN ,  REDMAN ANIKO ,  YI LIN ,  ZHU QINGMING

Inventor： SCOTT WILLIAM J ,  DUMAS JACQUES ,  BOYER STEPHEN ,  LEE WENDY ,  CHEN YUANWEI ,  PHILLIPS BARTON ,  VERMA SHARAD ,  CHEN JIANQING ,  CHEN ZHI ,  FAN JIANMEI ,  RAUDENBUSH BRIAN ,  REDMAN ANIKO ,  YI LIN ,  ZHU QINGMING

IPC: A61K31/335 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/423 ,  A61K31/428 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/53 ,  A61K31/538 ,  A61K31/5415 ,  A61P35/00 ,  C07D213/68 ,  C07D213/79 ,  C07D213/84 ,  C07D251/02 ,  C07D333/66 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

CPC classification number: C07D213/84 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

Abstract: This invention relates to novel diaryl ureas of Formula (I), pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper­proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.

公开(公告)号：WO2003027114A1

公开(公告)日：2003-04-03

申请号：PCT/US2002/030541

申请日：2002-09-24

Applicant: BAYER PHARMACEUTICALS CORPORATION ,  SMITH, Roger, A. ,  WONG, Wai, C. ,  O'CONNOR, Stephen, J. ,  CHOI, Soongyu ,  KLUENDER, Harold, C., E. ,  ZHANG, Zhonghua ,  LAVOIE, Rico, C. ,  FAN, Jianmei ,  PODLOGAR, Brent, L.

Inventor： SMITH, Roger, A. ,  WONG, Wai, C. ,  O'CONNOR, Stephen, J. ,  CHOI, Soongyu ,  KLUENDER, Harold, C., E. ,  ZHANG, Zhonghua ,  LAVOIE, Rico, C. ,  FAN, Jianmei ,  PODLOGAR, Brent, L.

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: This invention relates to 1,5,6,7-tetrahydropyrrolo[3,2-c]pyridine derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.

Abstract translation: 本发明涉及已被发现抑制食欲并引起体重减轻的1,5,6,7-四氢吡咯并[3,2-c]吡啶衍生物。 本发明还提供了合成化合物的方法，包含该化合物的药物组合物，以及使用这些组合物诱导体重减轻和治疗肥胖症和肥胖相关疾病的方法。

公开(公告)号：WO2005121147A1

公开(公告)日：2005-12-22

申请号：PCT/US2005/019472

申请日：2005-06-03

Applicant: BAYER PHARMACEUTICALS CORPORATION ,  DIXON, Julie, A. ,  BRENNAN, Catherine ,  MIRANDA, Karl ,  CHANDLER, Brent ,  PHILLIPS, Barton ,  FAN, Jianmei ,  BRANDS, Michael ,  MCCLURE, Andrea ,  JONES, Benjamin ,  FU, Wenlang ,  BIERER, Donald ,  MAGNUSON, Steven ,  KLUENDER, Harold, C. E.

Inventor： DIXON, Julie, A. ,  BRENNAN, Catherine ,  MIRANDA, Karl ,  CHANDLER, Brent ,  PHILLIPS, Barton ,  FAN, Jianmei ,  BRANDS, Michael ,  MCCLURE, Andrea ,  JONES, Benjamin ,  FU, Wenlang ,  BIERER, Donald ,  MAGNUSON, Steven ,  KLUENDER, Harold, C. E.

IPC: C07D487/04

CPC classification number: C07D491/113 ,  C07D487/04

Abstract: This invention relates to pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.

Abstract translation: 本发明涉及吡咯并三嗪化合物，含有这些化合物的药物组合物以及这些化合物和组合物用于预防和/或治疗与血管发生相关的高增殖性病症和疾病的用途。