公开(公告)号：EP1192137B1

公开(公告)日：2013-10-23

申请号：EP00946961.0

申请日：2000-06-28

申请人： Amgen Inc. ,  Japan Tobacco Inc.

发明人： MCGEE, Lawrence, R. ,  HOUZE, Jonathan, B. ,  RUBENSTEIN, Steven, M. ,  HAGIWARA, Atsushi ,  FURUKAWA, Noboru ,  SHINKAI, Hisashi

IPC分类号： C07D213/65 ,  C07D215/36 ,  C07D215/20 ,  C07D277/74 ,  C07D211/82 ,  C07D235/28 ,  C07C311/21 ,  A61K31/18 ,  A61K31/44 ,  A61K31/415 ,  A61K31/425

CPC分类号： C07D213/70 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C311/29 ,  C07C317/34 ,  C07C323/49 ,  C07D213/65 ,  C07D213/89 ,  C07D215/20 ,  C07D215/36 ,  C07D215/48 ,  C07D235/14 ,  C07D235/28 ,  C07D263/56 ,  C07D263/58 ,  C07D277/64 ,  C07D277/68 ,  C07D277/74 ,  C07D277/82 ,  C07D307/80 ,  C07D401/12 ,  C07D413/04 ,  C07D413/12 ,  C07D513/04

公开(公告)号：EP1296967B1

公开(公告)日：2006-05-31

申请号：EP01950669.0

申请日：2001-06-27

申请人： Amgen Inc. ,  Japan Tobacco Inc.

发明人： MCGEE, Lawrence, R. ,  HOUZE, Jonathan, B. ,  RUBENSTEIN, Steven, M. ,  HAGIWARA, Atsushi ,  FURUKAWA, Noboru ,  SHINKAI, Hisashi

IPC分类号： C07D277/82 ,  C07D277/68 ,  C07D215/36 ,  C07D277/64 ,  C07D215/20 ,  C07D215/48 ,  C07D215/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  A61K31/428 ,  A61K31/47 ,  A61P29/00 ,  A61P3/10

CPC分类号： C07D277/68 ,  C07D215/12 ,  C07D215/20 ,  C07D215/36 ,  C07D215/48 ,  C07D277/64 ,  C07D277/82 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： Compounds having the formula (I) wherein Ar is substituted or unsubstituted 2-benzothiazolyl or substituted or unsubstituted quinolinyl; X is -O-, -C(O)-, -CH(R )-, -N(R )-, or -S(O)k-; Y is -N(R )-S(O)2-; R is hydrogen or a specified substituent; R is substituted or unsubstituted aryl; and R is halogen or (C1-C8)alkoxy are useful in the treatment or prevention of a condition or disorder mediated by PPAR gamma . In particular, the compounds of the invention modulate the function of PPAR gamma . The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.

公开(公告)号：EP1192137A1

公开(公告)日：2002-04-03

申请号：EP00946961.0

申请日：2000-06-28

申请人： Tularik Inc. ,  JAPAN TOBACCO INC.

发明人： MCGEE, Lawrence, R. ,  HOUZE, Jonathan, B. ,  RUBENSTEIN, Steven, M. ,  HAGIWARA, Atsushi ,  FURUKAWA, Noboru ,  SHINKAI, Hisashi

IPC分类号： C07D213/65 ,  C07D215/36 ,  C07D215/20 ,  C07D277/74 ,  C07D211/82 ,  C07D277/68 ,  C07D235/28 ,  C07C311/21 ,  A61K31/18 ,  A61K31/44 ,  A61K31/415 ,  A61K31/425

CPC分类号： C07D213/70 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C311/29 ,  C07C317/34 ,  C07C323/49 ,  C07D213/65 ,  C07D213/89 ,  C07D215/20 ,  C07D215/36 ,  C07D215/48 ,  C07D235/14 ,  C07D235/28 ,  C07D263/56 ,  C07D263/58 ,  C07D277/64 ,  C07D277/68 ,  C07D277/74 ,  C07D277/82 ,  C07D307/80 ,  C07D401/12 ,  C07D413/04 ,  C07D413/12 ,  C07D513/04

摘要： Modulators of PPARη activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

公开(公告)号：EP1296967A1

公开(公告)日：2003-04-02

申请号：EP01950669.0

申请日：2001-06-27

申请人： Tularik Inc. ,  Japan Tobacco Inc.

发明人： MCGEE, Lawrence, R. ,  HOUZE, Jonathan, B. ,  RUBENSTEIN, Steven, M. ,  HAGIWARA, Atsushi ,  FURUKAWA, Noboru ,  SHINKAI, Hisashi

IPC分类号： C07D277/82 ,  C07D277/68 ,  C07D215/36 ,  C07D277/64 ,  C07D215/20 ,  C07D215/48 ,  C07D215/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  A61K31/428 ,  A61K31/47 ,  A61P29/00 ,  A61P3/10

CPC分类号： C07D277/68 ,  C07D215/12 ,  C07D215/20 ,  C07D215/36 ,  C07D215/48 ,  C07D277/64 ,  C07D277/82 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： Compounds having the formula (I) wherein Ar is substituted or unsubstituted 2-benzothiazolyl or substituted or unsubstituted quinolinyl; X is -O-, -C(O)-, -CH(R )-, -N(R )-, or -S(O)k-; Y is -N(R )-S(O)2-; R is hydrogen or a specified substituent; R is substituted or unsubstituted aryl; and R is halogen or (C1-C8)alkoxy are useful in the treatment or prevention of a condition or disorder mediated by PPAR gamma . In particular, the compounds of the invention modulate the function of PPAR gamma . The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.

公开(公告)号：EP1053227B1

公开(公告)日：2008-11-05

申请号：EP99901492.1

申请日：1999-01-20

申请人： AMGEN INC.

发明人： DE LA BROUSE-ELWOOD, Fabienne ,  JAEN, Juan, C. ,  MCGEE, Lawrence, R. ,  MIAO, Shi-Chang ,  RUBENSTEIN, Steven, Marc ,  CHEN, Jin-Long ,  CUSHING, Timothy, D. ,  FLYGARE, John, A. ,  HOUZE, Jonathan, B. ,  KEARNEY, Patrick, C.

IPC分类号： C07D213/65 ,  A61K31/435 ,  C07D239/34 ,  C07D213/643 ,  C07D233/70 ,  C07D413/12

CPC分类号： C07D213/70 ,  C07C311/21 ,  C07D213/65 ,  C07D215/20 ,  C07D217/04 ,  C07D405/12

摘要： Modulators of PPARη activity are provided having formula (I): in which the symbol Ar represents an aryl group; the letter X represents a divalent linkage selected from the group consisting of =C1-C6alkylene, -(C1-C6)alkylenoxy, -O-, -C(O)-, -N(R11)-, -N(R11)C(O)-, -S(O)¿k?- and a single bond, in which R?11¿ is a member selected from the group consisting of hydrogen, alkyl, heteroalkyl, and arylalkyl and the subscript k is an integer of from 0 to 2. The letter Y, in formula (I) represents a divalent linkage selected from the group consisting of alkylene, -O-, -C(O)-, -N(R12)-S(O)¿m?-, -N(R?13¿)-S(O)¿m-N(R?13)-, -N(R12)C(O)-, -S(O)¿n?-, a single bond, and combinations thereof in which R?12 and R13¿ are members independently selected from the group consisting of hydrogen, alkyl, heteroalkyl and arylalkyl; and the subscripts m and n independently integers of from 0 to 2. The symbol R1 represents a member selected from the group consisting of hydrogen, alkyl, heteroalkyl, aryl, arylalkyl, -CO¿2R?14, -CO(R)14, -C(O)NR15R16, -S(O)¿p-R?14, -S(O)¿q?-NR?15R16¿, -O-C(O)-OR17, -O-C(O)-R17, -O-C(O)-NR?15R16, -N(R14¿)-C(O)-NR?15R16, -N(R14¿)-C(O)-R17 and -N(R14)-C(O)-OR17, in which R14 is a member selected from the group consisting of hydrogen, alkyl, heteroalkyl, aryl and arylalkyl, and R?15 and R16¿ are members independently selected from the group consisting of hydrogen, alkyl, heteroalkyl, aryl and arylalkyl, or taken together with the nitrogen to which each is attached from a 5-, 6- or 7-membered ring. The symbol R17 represents a member selected from the group consisting of alkyl, heteroalkyl, aryl and arylalkyl. Additionally, for the R1 groups described above, the subscript p is an integer of from 0 to 3, and the subscript q is an integer of from 1 to 2. The symbol R2 represents a member selected from the group consisting of alkyl, heteroalkyl, aryl and arylalkyl. In another aspect, the present invention provides compounds of formula (I), as well as pharmaceutical compositions containing the compounds described above for the treatment of conditions such as type II diabetes and obesity.

公开(公告)号：EP4146222A1

公开(公告)日：2023-03-15

申请号：EP21800538.7

申请日：2021-05-04

申请人： Amgen Inc. ,  Vigil Neuoscience, Inc.

发明人： CZABANIUK, Lara, C. ,  HOPPER, Timothy ,  HOUZE, Jonathan, B. ,  PANTELEEV, Jane ,  RESCOURIO, Gwenaella ,  SANTORA, Vincent ,  WANG, Haoxuan ,  WHITE, Ryan D. ,  WONG, Alice, R. ,  WU, Yongwei ,  BOS, Maxence ,  MANCUSO, John ,  FRANZONI, Ivan

IPC分类号： A61K31/5375 ,  C07D239/72 ,  C07D265/28 ,  C07D243/34 ,  A61K31/517 ,  C07H19/22 ,  A61K31/47

公开(公告)号：EP2001844A2

公开(公告)日：2008-12-17

申请号：EP07752941.0

申请日：2007-03-12

申请人： Amgen, Inc

发明人： SHARMA, Rajiv ,  AKERMAN, Michelle ,  CARDOZO, Mario, G. ,  HOUZE, Jonathan, B. ,  LI, An-Rong ,  LIU, Jinqian ,  LIU, Jiwen ,  MA, Zhihua ,  MEDINA, Julio, C. ,  SCHMITT, Michael, J. ,  SUN, Ying ,  WANG, Yingcai ,  WANG, Zhongyu ,  ZHU, Liusheng

IPC分类号： C07D209/08 ,  C07D209/46 ,  C07D215/22 ,  C07D277/24 ,  C07D311/74 ,  C07D313/08 ,  C07D417/12 ,  C07D498/04 ,  C07C59/54 ,  C07C59/72 ,  A61K31/426 ,  A61P3/10

CPC分类号： C07C57/62 ,  C07C59/64 ,  C07C59/72 ,  C07D209/08 ,  C07D209/46 ,  C07D215/20 ,  C07D215/227 ,  C07D277/24 ,  C07D311/58 ,  C07D311/74 ,  C07D311/76 ,  C07D313/08 ,  C07D417/12 ,  C07D498/04

摘要： Compounds having the general formula I and/or the general formula II are useful, for example, for treating metabolic disorders in a subject formula (I) (II) where the variables are provided herein. Compositions and methods for using the compounds for preparing medicaments and for treating metabolic disorders such as, for instance, type II diabetes are disclosed.

公开(公告)号：EP1924546A1

公开(公告)日：2008-05-28

申请号：EP06814336.1

申请日：2006-09-08

申请人： Amgen, Inc

发明人： AKERMAN, Michelle ,  BROWN, Sean ,  HOUZE, Jonathan, B. ,  LIU, Jinqian ,  MA, Zhihua ,  MEDINA, Julio, C. ,  QIU, Wei ,  SCHMITT, Michael, J. ,  WANG, Yingcai ,  ZHU, Liusheng ,  LIU Jiwen ,  SHARMA, Rajiv

IPC分类号： C07C59/72

CPC分类号： C07D333/24 ,  C07C59/72 ,  C07D231/12 ,  C07D233/26 ,  C07D233/64 ,  C07D239/26 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/04 ,  C07D261/08 ,  C07D263/32 ,  C07D317/54 ,  C07D333/16

摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: (F) where the definitions of the variables Q, L1, , L2, M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.