SALTS AND POLYMORPHS OF A POTENT ANTIDIABETIC COMPOUND
    5.
    发明授权
    SALTS AND POLYMORPHS OF A POTENT ANTIDIABETIC COMPOUND 有权
    盐类和多晶型有效的抗糖尿病化合物

    公开(公告)号:EP1677797B1

    公开(公告)日:2012-02-22

    申请号:EP04794053.1

    申请日:2004-10-04

    申请人: Amgen Inc.

    IPC分类号: A61K31/47 C07D215/16

    CPC分类号: C07D215/20

    摘要: Salts and polymorphs of a compound useful in the treatment of inflammatory and metabolic conditions and diseases are provided herein. In particular, the invention provides salts and polymorphs of a compound which modulates the expression and/or function of a peroxisome proliferator-activated receptor. The salts and polymorphs are useful for the treatment or prevention of conditions and disorders associated with energy homeostasis such as type II diabetes, lipid metabolism, adipocyte differentiation and inflammation.

    PPAR-GAMMA MODULATORS
    9.
    发明授权
    PPAR-GAMMA MODULATORS 有权
    PPAR-γ调节剂

    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.

    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.

    SALTS AND POLYMORPHS OF A POTENT ANTIDIABETIC COMPOUND
    10.
    发明公开
    SALTS AND POLYMORPHS OF A POTENT ANTIDIABETIC COMPOUND 有权
    盐类和多晶型有效的抗糖尿病化合物

    公开(公告)号:EP1677797A2

    公开(公告)日:2006-07-12

    申请号:EP04794053.1

    申请日:2004-10-04

    申请人: Amgen Inc.

    IPC分类号: A61K31/47 C07D215/16

    CPC分类号: C07D215/20

    摘要: Salts and polymorphs of a compound useful in the treatment of inflammatory and metabolic conditions and diseases are provided herein. In particular, the invention provides salts and polymorphs of a compound which modulates the expression and/or function of a peroxisome proliferator-activated receptor. The salts and polymorphs are useful for the treatment or prevention of conditions and disorders associated with energy homeostasis such as type II diabetes, lipid metabolism, adipocyte differentiation and inflammation.