公开(公告)号：WO2014093230A2

公开(公告)日：2014-06-19

申请号：PCT/US2013/073895

申请日：2013-12-09

Applicant: MERCK PATENT GMBH ,  LIU-BUJALSKI, Lesley ,  JOHNSON, Theresa L. ,  GOUTOPOULOS, Andreas ,  QIU, Hui

Inventor： LIU-BUJALSKI, Lesley ,  JOHNSON, Theresa L. ,  GOUTOPOULOS, Andreas ,  QIU, Hui

IPC: C07D403/12 ,  C07D401/14 ,  C07D413/14 ,  C07D213/73 ,  C07D213/74 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/14 ,  C07D239/34 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D413/12 ,  C07D495/04 ,  C07D213/68 ,  A61K31/506 ,  A61K31/513 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/4418 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D403/12 ,  A61K31/4418 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  C07D213/68 ,  C07D213/73 ,  C07D213/74 ,  C07D239/34 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/08 ,  C07D471/10 ,  C07D487/10 ,  C07D495/04

Abstract: The present invention provides novel pyrimidine and pyridine compounds which are attached to a warhead, and the manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. The invention also describes kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.

Abstract translation: 本发明提供附着于弹头的新型嘧啶和吡啶化合物，以及用于治疗过度增殖性疾病的制造和用途，包括但不限于癌症，狼疮，过敏性疾病，干燥病和类风湿性关节炎。 本发明还描述了激酶抑制剂，包括但不限于Bruton酪氨酸激酶的抑制剂。

公开(公告)号：WO2013012848A1

公开(公告)日：2013-01-24

申请号：PCT/US2012/047038

申请日：2012-07-17

Applicant: YU, Henry ,  LI, Jiezhen ,  RICHARDSON, Thomas E. ,  BHARATHI, Pandi ,  HEASLEY, Brian H. ,  GOUTOPOULOS, Andreas ,  MERCK PATENT GMBH

Inventor： YU, Henry ,  LI, Jiezhen ,  RICHARDSON, Thomas E. ,  BHARATHI, Pandi ,  HEASLEY, Brian H. ,  GOUTOPOULOS, Andreas

IPC: C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/496 ,  A61P15/08

CPC classification number: C07D417/12 ,  A61K31/454 ,  A61K31/496 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D233/64 ,  C07D263/34 ,  C07D307/68 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: Novel benzamide derivatives of formula (I) wherein W 1 , W 2 , R 1 to R 7 , R 6 , X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.

Abstract translation: 其中W 1，W 2，R 1至R 7，R 6，X和Y具有根据权利要求的含义的式（I）的新型苯甲酰胺衍生物是FSH受体的正变构调节剂，并且可以用于治疗 的生育障碍。

公开(公告)号：WO2007123939A2

公开(公告)日：2007-11-01

申请号：PCT/US2007009461

申请日：2007-04-18

Applicant: APPLIED RESEARCH SYSTEMS ,  GOUTOPOULOS ANDREAS ,  ASKEW BENNY C ,  DIEP NHUT KIET ,  KARRA SRINIVASA ,  SCHWARZ MATTHIAS ,  YU HENRY

Inventor： GOUTOPOULOS ANDREAS ,  ASKEW BENNY C ,  DIEP NHUT KIET ,  KARRA SRINIVASA ,  SCHWARZ MATTHIAS ,  YU HENRY

IPC: C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D213/84 ,  C07D237/24

CPC classification number: C07D213/84 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D237/24 ,  C07D405/12

Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed. is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.

Abstract translation: 本发明提供了式（I）的新型芳基氨基N-杂芳基MEK抑制剂：此类化合物是用于治疗过度增殖性疾病例如癌症和炎症的MEK抑制剂。 还披露。 是治疗哺乳动物中的过度增殖性疾病，以及含有这些化合物的药物组合物。

公开(公告)号：WO0128498A3

公开(公告)日：2001-09-13

申请号：PCT/US0041248

申请日：2000-10-18

Applicant: UNIV CONNECTICUT ,  MAKRIYANNIS ALEXANDROS ,  LIU QIAN ,  GOUTOPOULOS ANDREAS

Inventor： MAKRIYANNIS ALEXANDROS ,  LIU QIAN ,  GOUTOPOULOS ANDREAS

IPC: C07D295/20 ,  A61K31/16 ,  A61K31/166 ,  A61K31/17 ,  A61K31/27 ,  A61K31/5375 ,  A61P1/00 ,  A61P9/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P27/06 ,  A61P31/18 ,  A61P35/00 ,  A61P43/00 ,  C07C233/05 ,  C07C233/09 ,  C07C233/65 ,  C07C235/06 ,  C07C271/12 ,  C07C275/20 ,  C07D295/215 ,  C07C233/00 ,  A01N37/18

CPC classification number: C07D295/215 ,  C07C233/05 ,  C07C233/09 ,  C07C233/65 ,  C07C235/06 ,  C07C271/12 ,  C07C275/20

Abstract: Novel retro-anandamides are presented which have high affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy, as well as suppression of the immune system, enhancement of appetite and in treatment of certain mental disorders.

Abstract translation: 提出了对大麻素CB1和/或CB2受体位点具有高度亲和力的新颖的逆anandamides。 此外，大部分类似物比花生四烯酸乙醇酰胺显示更高的代谢稳定性。 改善的受体亲和力和选择性和/或更高的代谢稳定性使得这些类似物在个体和动物中用作治疗疼痛，青光眼，癫痫，与化疗相关的恶心以及抑制免疫系统，增强食欲和 用于治疗某些精神疾病。

公开(公告)号：WO2016057500A1

公开(公告)日：2016-04-14

申请号：PCT/US2015/054221

申请日：2015-10-06

Applicant: MERCK PATENT GMBH ,  GAILLARD, Pascale ,  SEENISAMY, Jeyaprakashnarayanan ,  LIU-BUJALSKI, Lesley ,  POTNICK, Justin ,  CALDWELL, Richard D. ,  QIU, Hui ,  NEAGU, Constantin ,  JONES, Reinaldo ,  WON, Annie Cho ,  GOUTOPOULOS, Andreas ,  SHERER, Brian A. ,  JOHNSON, Theresa L. ,  GARDBERG, Anna

Inventor： GAILLARD, Pascale ,  SEENISAMY, Jeyaprakashnarayanan ,  LIU-BUJALSKI, Lesley ,  POTNICK, Justin ,  CALDWELL, Richard D. ,  QIU, Hui ,  NEAGU, Constantin ,  JONES, Reinaldo ,  WON, Annie Cho ,  GOUTOPOULOS, Andreas ,  SHERER, Brian A. ,  JOHNSON, Theresa L. ,  GARDBERG, Anna

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/437 ,  A61K31/553 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to imidazopyridine compounds of formula I, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

Abstract translation: 本发明涉及式I的咪唑并吡啶化合物及其药学上可接受的组合物，其可用作BTK抑制剂。

公开(公告)号：WO2014143612A1

公开(公告)日：2014-09-18

申请号：PCT/US2014/022479

申请日：2014-03-10

Applicant: MERCK PATENT GMBH ,  LAN, Ruoxi ,  CHEN, Xiaoling ,  XIAO, Yufang ,  HUCK, Bayard R. ,  GOUTOPOULOS, Andreas

Inventor： LAN, Ruoxi ,  CHEN, Xiaoling ,  XIAO, Yufang ,  HUCK, Bayard R. ,  GOUTOPOULOS, Andreas

IPC: C07D401/14 ,  A61K31/506 ,  A61P35/00

CPC classification number: A61K31/519 ,  A61K31/506 ,  C07D401/14 ,  C07D487/04

Abstract: The invention provides heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. Formula (I).

Abstract translation: 本发明提供式（I）的杂环胺，其用于治疗过度增殖性疾病如癌症的制造和用途。 式（I）。

公开(公告)号：WO2014085528A1

公开(公告)日：2014-06-05

申请号：PCT/US2013/072141

申请日：2013-11-27

Applicant: MERCK PATENT GMBH ,  HUCK, Bayard R. ,  LAN, Ruoxi ,  POTNICK, Justin ,  DESELM, Lizbeth Celeste ,  CRONIN, Mark W., Jr. ,  NEAGU, Constantin ,  CHEN, Xiaoling ,  BOIVIN, Roch ,  JOHNSON, Theresa L. ,  GOUTOPOULOS, Andreas

Inventor： HUCK, Bayard R. ,  LAN, Ruoxi ,  POTNICK, Justin ,  DESELM, Lizbeth Celeste ,  CRONIN, Mark W., Jr. ,  NEAGU, Constantin ,  CHEN, Xiaoling ,  BOIVIN, Roch ,  JOHNSON, Theresa L. ,  GOUTOPOULOS, Andreas

IPC: C07D403/12 ,  A61K31/519 ,  A61K31/53 ,  C07D401/12 ,  C07D471/04 ,  C07D253/08 ,  A61P35/00

CPC classification number: C07D253/08 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04

Abstract: Novel azaquinazoline carboxamide derivatives of formula (I) wherein W 1 , W 2 , W 3 , W 4 , R 1 , R 2 , R 3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.

Abstract translation: 式（I）的新型氮杂喹唑啉羧酰胺衍生物，其中上述定义的W1，W2，W3，W4，R1，R2，R3和m是p70S6K抑制剂，并且可以特别用于治疗过度增殖性疾病。

公开(公告)号：WO2013028715A1

公开(公告)日：2013-02-28

申请号：PCT/US2012/051785

申请日：2012-08-22

Applicant: MERCK PATENT GMBH ,  DONNELLY, Marianne ,  QIU, Hui ,  YU, Henry ,  LIU-BUJALSKI, Lesley ,  GOUTOPOULOS, Andreas

Inventor： DONNELLY, Marianne ,  QIU, Hui ,  YU, Henry ,  LIU-BUJALSKI, Lesley ,  GOUTOPOULOS, Andreas

IPC: C07D513/04 ,  A61K31/429

CPC classification number: C07D513/04 ,  A61K31/429 ,  A61K31/4439 ,  A61K31/454

Abstract: Novel compounds of formula (I), wherein R 1 to R 4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.

Abstract translation: 式（I）的新型化合物，其中R 1至R 4和X具有根据权利要求的含义，其为葡糖苷酶抑制剂，并且可用于治疗阿尔茨海默氏病。

公开(公告)号：WO2007123936A1

公开(公告)日：2007-11-01

申请号：PCT/US2007/009456

申请日：2007-04-18

Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. ,  GOUTOPOULOS, Andreas ,  ASKEW, Benny, C., Jr. ,  CHEN, Xiaoling ,  KARRA, Srinivasa ,  YU, Henry

Inventor： GOUTOPOULOS, Andreas ,  ASKEW, Benny, C., Jr. ,  CHEN, Xiaoling ,  KARRA, Srinivasa ,  YU, Henry

IPC: C07D213/79 ,  C07D213/81 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  A61K31/4427 ,  A61K31/4439 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D213/79 ,  C07D213/81 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: The invention provides novel heteroaryl-substituted arylaminopyridine derivative MEK inhibitors of Formula (Ia) Formula (Ia) Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.

Abstract translation: 本发明提供式（Ia）式（Ia）的新颖的杂芳基取代的芳基氨基吡啶衍生物MEK抑制剂。这些化合物是可用于治疗过度增殖性疾病如癌症和炎症的MEK抑制剂。 还公开了哺乳动物中过度增殖性疾病的治疗和含有这些化合物的药物组合物。

公开(公告)号：WO2016127025A1

公开(公告)日：2016-08-11

申请号：PCT/US2016/016709

申请日：2016-02-05

Applicant: MERCK PATENT GMBH ,  CHEN, Xiaoling ,  YU, Henry ,  LAN, Ruoxi ,  JORAND-LEBRUN, Catherine ,  JOHNSON, Theresa L. ,  GOUTOPOULOS, Andreas

Inventor： CHEN, Xiaoling ,  YU, Henry ,  LAN, Ruoxi ,  JORAND-LEBRUN, Catherine ,  JOHNSON, Theresa L. ,  GOUTOPOULOS, Andreas

IPC: C07D487/18 ,  A61P35/00

CPC classification number: C07D471/22 ,  C07D487/18 ,  C07D498/18 ,  C07D498/22 ,  C07D513/22

Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors. Wherein: Ring A is a 5-membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5- membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted; Ring B is a 6-membered aryl, or a 6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted; Ring C is a 5-membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5- membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted.

Abstract translation: 本发明涉及可用作IRAK抑制剂的式（I）化合物及其药学上可接受的组合物。 其中环A是具有1-4个独立地选自氮，氧或硫的杂原子的5元杂环，或具有1-4个独立地选自氮，氧或硫的杂原子的5-元单环杂芳基环; 它们各自任选被取代; 环B是6元芳基或具有1-4个独立地选自氮，氧或硫的杂原子的6元单环杂芳基环; 它们各自任选被取代; 环C是具有1-4个独立地选自氮，氧或硫的杂原子的5元杂环，或具有1-4个独立地选自氮，氧或硫的杂原子的5-元单环杂芳基环; 它们各自任选被取代。