公开(公告)号：EP1664022B1

公开(公告)日：2011-06-15

申请号：EP04782252.3

申请日：2004-08-26

申请人： Schering Corporation ,  Pharmacopeia, LLC

发明人： BURNETT, Duane, A. ,  WU, Wen-Lian ,  SASIKUMAR, Thavalakulamgara, K. ,  GREENLEE, William, J. ,  CAPLEN, Mary, Ann ,  GUO, Tao ,  HUNTER, Rachael

IPC分类号： C07D401/12 ,  C07D401/06 ,  A61K31/454 ,  A61P3/04 ,  A61P3/10

CPC分类号： C04B35/632 ,  C07D401/06 ,  C07D401/12

摘要： The present invention discloses compounds of formula (I); wherein Ar, Y, m, n, R1 and R4 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：EP1664022A1

公开(公告)日：2006-06-07

申请号：EP04782252.3

申请日：2004-08-26

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： BURNETT, Duane, A. ,  WU, Wen-Lian ,  SASIKUMAR, Thavalakulamgara, K. ,  GREENLEE, William, J. ,  CAPLEN, Mary, Ann ,  GUO, Tao ,  HUNTER, Rachael

IPC分类号： C07D401/12 ,  C07D401/06 ,  A61K31/454 ,  A61P3/04 ,  A61P3/10

CPC分类号： C04B35/632 ,  C07D401/06 ,  C07D401/12

摘要： The present invention discloses compounds of formula (I); wherein Ar, Y, m, n, R1 and R4 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：EP1444200B1

公开(公告)日：2006-05-03

申请号：EP02778840.5

申请日：2002-11-14

申请人： SCHERING CORPORATION

发明人： BURNETT, Duane, A. ,  CAPLEN, Mary, Ann ,  CZARNIECKI, Michael, F. ,  DOMALSKI, Martin, S. ,  HO, Ginny, D. ,  TULSHIAN, Deen ,  WU, Wen-Lian

IPC分类号： C07D205/04 ,  C07D401/06 ,  C07D417/06 ,  C07D405/06 ,  C07D403/04 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  A61K31/397 ,  A61P11/06 ,  A61P11/14

CPC分类号： C07D231/12 ,  C07D205/04 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： 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 R¿7? 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.

公开(公告)号：EP1444200A1

公开(公告)日：2004-08-11

申请号：EP02778840.5

申请日：2002-11-14

申请人： SCHERING CORPORATION

发明人： BURNETT, Duane, A. ,  CAPLEN, Mary, Ann ,  CZARNIECKI, Michael, F. ,  DOMALSKI, Martin, S. ,  HO, Ginny, D. ,  TULSHIAN, Deen ,  WU, Wen-Lian

IPC分类号： C07D205/04 ,  C07D401/06 ,  C07D417/06 ,  C07D405/06 ,  C07D403/04 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  A61K31/397 ,  A61P11/06 ,  A61P11/14

CPC分类号： C07D231/12 ,  C07D205/04 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： 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 R¿7? 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.

公开(公告)号：EP1706375A2

公开(公告)日：2006-10-04

申请号：EP04815055.1

申请日：2004-12-21

申请人： SCHERING CORPORATION

发明人： BURNETT, Duane, A. ,  WU, Wen-Lian ,  DOMALSKI, Martin, S. ,  CAPLEN, Mary, Ann ,  SPRING, Richard ,  LACHOWICZ, Jean, E.

IPC分类号： C07C257/14

CPC分类号： 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

摘要： 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.

公开(公告)号：EP1660478A1

公开(公告)日：2006-05-31

申请号：EP04781845.5

申请日：2004-08-23

申请人： SCHERING CORPORATION

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

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

CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D417/14

摘要： The present invention discloses compounds of formula (I) wherein Ar, X, R1 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.