公开(公告)号：WO2014105664A1

公开(公告)日：2014-07-03

申请号：PCT/US2013/076775

申请日：2013-12-20

Applicant: MERCK SHARP & DOHME CORP. ,  ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  BERLIN, Michael ,  TING, Pauline ,  ZHOU, Gang ,  YU, Tao ,  BOYCE, Christopher ,  KELLY, Joseph Michael ,  TAGAT, Jayaram, R. ,  ZHENG, Junying ,  HUANG, Xianhai ,  ZHOU, Wei ,  KIM, Jae-Hun ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda, V. ,  WON, Walter ,  WU, Heping ,  ANAND, Rajan

Inventor： ALI, Amjad ,  LO, Michael Man-Chu ,  LIM, Yeon-Hee ,  STAMFORD, Andrew ,  KUANG, Rongze ,  TEMPEST, Paul ,  YU, Younong ,  BERLIN, Michael ,  TING, Pauline ,  ZHOU, Gang ,  YU, Tao ,  BOYCE, Christopher ,  KELLY, Joseph Michael ,  TAGAT, Jayaram, R. ,  ZHENG, Junying ,  HUANG, Xianhai ,  ZHOU, Wei ,  KIM, Jae-Hun ,  ZORN, Nicolas ,  XIAO, Dong ,  GALLO, Gioconda, V. ,  WON, Walter ,  WU, Heping ,  ANAND, Rajan

IPC: A61K31/4985 ,  A61K31/519

CPC classification number: C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

Abstract: Disclosed are compounds of Formula A: (structurally represented) where "RG1", "RG2a", "RG4", "RG5", "MG1", "n" and "m" are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Abstract translation: 公开了式A化合物（结构上表示），其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：WO2014055311A1

公开(公告)日：2014-04-10

申请号：PCT/US2013/061786

申请日：2013-09-26

Applicant: MERCK SHARP & DOHME CORP. ,  HUANG, Xianhai ,  PALANI, Anandan ,  RAO, Ashwin, U. ,  ZHANG, Hongjun ,  ZHOU, Wei

Inventor： HUANG, Xianhai ,  PALANI, Anandan ,  RAO, Ashwin, U. ,  ZHANG, Hongjun ,  ZHOU, Wei

IPC: A61K31/4245 ,  A61K31/47 ,  A01N43/42

CPC classification number: C07D217/24 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/496 ,  A61K45/06 ,  C07D401/06 ,  C07D401/12 ,  C07D413/04 ,  C07D413/14 ,  A61K2300/00

Abstract: The invention provides certain substituted isoquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.

Abstract translation: 本发明提供某些式（I）的取代的异喹啉及其药学上可接受的盐和酯。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能有关的疾病或病症的方法。

公开(公告)号：WO2012087861A1

公开(公告)日：2012-06-28

申请号：PCT/US2011/065716

申请日：2011-12-19

Applicant: MERCK SHARP & DOHME CORP. ,  SCHERING CORPORATION ,  BOYCE, Christopher, W. ,  DEGRADO, Sylvia Joanna ,  CHEN, Xiao ,  QIN, Jun ,  MAZZOLA, Robert, D., Jr. ,  YU, Younong ,  MCCORMICK, Kevin, D. ,  PALANI, Anandan ,  XIAO, Dong ,  ASLANIAN, Robert George ,  WU, Jie ,  RAO, Ashwin Umesh ,  SILIPHAIVANH, Phieng ,  METHOT, Joey Lee ,  ZHANG, Hongjun ,  KELLEY, Elizabeth Helen ,  BROWN, William Colby ,  JIANG, Qin ,  GAUUAN, Jolicia Polivina ,  LEYHANE, Andrew, J. ,  BIJU, Purakkattle Johny ,  DHONDI, Pawan, K. ,  DONG, Li ,  FEVRIER, Salem ,  HUANG, Xianhai ,  VACCARO, Henry, M.

Inventor： BOYCE, Christopher, W. ,  DEGRADO, Sylvia Joanna ,  CHEN, Xiao ,  QIN, Jun ,  MAZZOLA, Robert, D., Jr. ,  YU, Younong ,  MCCORMICK, Kevin, D. ,  PALANI, Anandan ,  XIAO, Dong ,  ASLANIAN, Robert George ,  WU, Jie ,  RAO, Ashwin Umesh ,  SILIPHAIVANH, Phieng ,  METHOT, Joey Lee ,  ZHANG, Hongjun ,  KELLEY, Elizabeth Helen ,  BROWN, William Colby ,  JIANG, Qin ,  GAUUAN, Jolicia Polivina ,  LEYHANE, Andrew, J. ,  BIJU, Purakkattle Johny ,  DHONDI, Pawan, K. ,  DONG, Li ,  FEVRIER, Salem ,  HUANG, Xianhai ,  VACCARO, Henry, M.

IPC: C07D241/36 ,  A61K31/498

CPC classification number: C07D241/42 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/55 ,  A61K45/06 ,  C07D241/38 ,  C07D241/44 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/048 ,  C07D491/107 ,  C07D498/04 ,  C07D498/10

Abstract: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J 1 , J 2 , R 1 , R 2 , R 3 , R 22 , R a , R b , R c , R d , X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with with uncontrolled or inappropriate stimulation of CRTH 2 function.

Abstract translation: 本发明提供了式（I）的某些喹喔啉和氮杂 - 喹喔啉及其药学上可接受的盐，其中J1，J2，R1，R2，R3，R22，Ra，Rb，Rc，Rd，X，Y，b，n ，和q如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能有关的疾病或病症的方法。

公开(公告)号：WO2011041181A1

公开(公告)日：2011-04-07

申请号：PCT/US2010/049778

申请日：2010-09-22

Applicant: SCHERING CORPORATION ,  MCCORMICK, Kevin, D. ,  SHAO, Ning ,  YU, Younong ,  HUANG, Xianhai ,  DE LERA RUIZ, Manuel ,  PALANI, Anandan ,  ZHENG, Junying ,  BOYCE, Christopher, W. ,  ASLANIAN, Robert, G. ,  CHAO, Jianhua

Inventor： MCCORMICK, Kevin, D. ,  SHAO, Ning ,  YU, Younong ,  HUANG, Xianhai ,  DE LERA RUIZ, Manuel ,  PALANI, Anandan ,  ZHENG, Junying ,  BOYCE, Christopher, W. ,  ASLANIAN, Robert, G. ,  CHAO, Jianhua

IPC: A01N43/76 ,  A61K31/42

CPC classification number: C07D413/10 ,  A61K31/42 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/537 ,  A61K31/56 ,  A61K38/02 ,  A61K45/06 ,  C07D263/52 ,  C07D413/04 ,  C07D417/04 ,  A61K2300/00

Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的联芳基螺氨基恶唑啉类似物作为α2C肾上腺素能受体激动剂的调节剂，制备此类化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法 以及使用这些化合物或药物组合物治疗，预防，抑制或改善与α2肾上腺素能受体相关的一种或多种病症的方法。

公开(公告)号：WO2010147973A1

公开(公告)日：2010-12-23

申请号：PCT/US2010/038655

申请日：2010-06-15

Applicant: SCHERING CORPORATION ,  HUANG, Xianhai ,  ZHU, Zhaoning ,  GREENLEE, William, J. ,  PALANI, Anandan ,  ASLANIAN, Robert, G.

Inventor： HUANG, Xianhai ,  ZHU, Zhaoning ,  GREENLEE, William, J. ,  PALANI, Anandan ,  ASLANIAN, Robert, G.

IPC: C07D471/04 ,  A61K31/437 ,  A61P25/28

CPC classification number: C07D471/04

Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula I: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula I.

Abstract translation: 本发明提供了γ分泌酶调节剂的新化合物。 所述化合物具有式I：还公开了调节γ分泌酶活性的方法和使用式I化合物治疗阿尔茨海默病的方法。

公开(公告)号：WO2010075069A1

公开(公告)日：2010-07-01

申请号：PCT/US2009/068022

申请日：2009-12-15

Applicant: SCHERING CORPORATION ,  XIAO, Dong ,  PALANI, Anandan ,  HUANG, Xianhai ,  ZHU, Xiaohong ,  ASLANIAN, Robert G.

Inventor： XIAO, Dong ,  PALANI, Anandan ,  HUANG, Xianhai ,  ZHU, Xiaohong ,  ASLANIAN, Robert G.

IPC: C07D491/052 ,  A61K31/4162 ,  A61P9/00 ,  A61P29/00 ,  A61P7/00 ,  A61P11/00 ,  A61P25/00 ,  A61P1/00 ,  A61P35/00 ,  A61P3/00

CPC classification number: C07D491/052

Abstract: The present invention relates to Bicyclic Pyranone Derivatives, their compositions and uses for treating or preventing a metabolic disorder, dyslipidemia, a cardiovascular disease, a neurological disorder, a hematological disease, cancer, inflammation, a respiratory disease, a gastroenterological disease, diabetes, a diabetic complicaton, obesity, an obesity-related disorder or non-alcoholic fatty liver disease.Formula (I). Y is -C- when an optional and additional bond is present and Y is -CH- when an optional and additional bond is not present; Z is -O-, -NH- or -N(alkyl)- when the optional and additional bond between Y and Z Is absent, and Z Is -N- when the optional and additional bond between Y and Z is present; R 1 is H1 halo or -CN; R 2 is alkyl, alkenyl or -(alkyleneVcydoalkyl; t is 0 or 1; R 3 is O when the optional and additional bond between Y and R 3 is present, and R 3 is alkyl. haloalkyl. -C(O)OR 5 . -alkylene-O-alkyt or -O-alkyl when the optional and additional bond between Y and R 3 is absent: R 4 is H, alkyl or aryl, wherein an aryl group can be unsubstituted or optionally substituted.

Abstract translation: 本发明涉及双环吡喃酮衍生物，其组合物和用于治疗或预防代谢紊乱，血脂异常，心血管疾病，神经障碍，血液病，癌症，炎症，呼吸系统疾病，胃肠病，糖尿病， 糖尿病并发症，肥胖症，肥胖相关障碍或非酒精性脂肪性肝病。（I）。 当不存在任选和另外的键时，当存在任选的附加键且Y是-CH-时，Y是-C-; 当Y和Z之间的任选和另外的键不存在时，Z是-O - ， - NH-或-N（烷基），当存在Y和Z之间的任选的和另外的键时，Z是 - R1为H1卤素或-CN; R 2是烷基，链烯基或 - （亚烷基环烷基; t是0或1;当存在Y和R 3之间的任选和另外的键时，R 3是O，并且R 3是烷基卤代烷基-C（O）OR 5 - 亚烷基-O - 烷基或 - 烷基，当Y和R3之间的任选和另外的键不存在时：R 4是H，烷基或芳基，其中芳基可以是未取代的或任选被取代的。

公开(公告)号：WO2010009210A3

公开(公告)日：2010-01-21

申请号：PCT/US2009/050660

申请日：2009-07-15

Applicant: SCHERING CORPORATION ,  TENDOLKAR, Amol ,  PALANI, Anandan ,  HUANG, Xianhai ,  ASLANIAN, Robert, G.

Inventor： TENDOLKAR, Amol ,  PALANI, Anandan ,  HUANG, Xianhai ,  ASLANIAN, Robert, G.

IPC: C07D213/55 ,  C07D241/52 ,  C07D307/32 ,  C07D403/04 ,  C07D487/04 ,  C07D491/04 ,  A61K31/435 ,  A61K31/519 ,  A61K31/341 ,  A61P35/00 ,  A61P29/00 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00

Abstract: The present invention provides compounds of the Formula I: (I) wherein G represents a hydrolysable or metabolizable linker group; and R represents a recoverable residue of a nicotinic acid receptor agonist; and salts, solvates, esters and prodrugs thereof, as well as pharmaceutical compositions containing them, and methods of using them to treat metabolic syndrome, dyslipidemia, cardiovascular diseases, disorders of the peripheral and central nervous system, hematological diseases, cancer, inflammation, respiratory diseases, gastroenterological diseases, diabetes, and non-alcoholic fatty liver diseases.

公开(公告)号：WO2009076337A1

公开(公告)日：2009-06-18

申请号：PCT/US2008/086030

申请日：2008-12-09

Applicant: SCHERING CORPORATION ,  HUANG, Xianhai ,  ASLANIAN, Robert, G. ,  PALANI, Anandan

Inventor： HUANG, Xianhai ,  ASLANIAN, Robert, G. ,  PALANI, Anandan

IPC: C07D455/02 ,  A61K31/4375 ,  A61P25/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D455/02

Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).

Abstract translation: 本发明提供了作为γ分泌酶调节剂的新型化合物。 化合物具有式（I）。 还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

公开(公告)号：WO2009073779A1

公开(公告)日：2009-06-11

申请号：PCT/US2008/085520

申请日：2008-12-04

Applicant: SCHERING CORPORATION ,  HUANG, Xianhai ,  PALANI, Anandan ,  QIN, Jun ,  ASLANIAN, Robert G. ,  ZHU, Zhaoning ,  GREENLEE, William J.

Inventor： HUANG, Xianhai ,  PALANI, Anandan ,  QIN, Jun ,  ASLANIAN, Robert G. ,  ZHU, Zhaoning ,  GREENLEE, William J.

IPC: C07D401/10 ,  C07D403/10 ,  C07D471/04 ,  C07D491/04 ,  C07D498/04 ,  A61K31/4738 ,  A61P25/28

CPC classification number: C07D471/04 ,  C07D401/10 ,  C07D403/10 ,  C07D491/04 ,  C07D498/04

Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R 2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).

Abstract translation: 本发明提供了作为γ分泌酶调节剂的新型化合物。 所述化合物具有式（I），其中R 2是式（II）的稠合双环。 还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

公开(公告)号：WO2009005729A1

公开(公告)日：2009-01-08

申请号：PCT/US2008/008042

申请日：2008-06-27

Applicant: SCHERING CORPORATION ,  ZHU, Zhaoning ,  GREENLEE, William, J. ,  MAZZOLA, Robert, D. ,  QIN, Jun ,  HUANG, Xianhai ,  PALANI, Anandan

Inventor： ZHU, Zhaoning ,  GREENLEE, William, J. ,  MAZZOLA, Robert, D. ,  QIN, Jun ,  HUANG, Xianhai ,  PALANI, Anandan

IPC: C07D401/10 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/519 ,  A61P25/28

CPC classification number: C07D487/04 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.