发明公开
EP1077929A1 2,3,5-SUBSTITUTED BIPHENYLS USEFUL IN THE TREATMENT OF INSULIN RESISTANCE AND HYPERGLYCEMIA
审中-公开
2,3,5-SUBSTITUIERTE BIPHENYLENÜTZLICHIN DIE BEHANDLUNG VON INSULINRESISTENZ UNDHYPERGLYKÄMIE
- 专利标题： 2,3,5-SUBSTITUTED BIPHENYLS USEFUL IN THE TREATMENT OF INSULIN RESISTANCE AND HYPERGLYCEMIA
- 专利标题（中）： 2,3,5-SUBSTITUIERTE BIPHENYLENÜTZLICHIN DIE BEHANDLUNG VON INSULINRESISTENZ UNDHYPERGLYKÄMIE
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申请号： EP99924158.1申请日： 1999-05-10
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公开(公告)号： EP1077929A1公开(公告)日： 2001-02-28
- 发明人: BUTERA, John, Anthony , CAUFIELD, Craig, Eugene , GRACEFFA, Russell, Francis , GREENFIELD, Alexander , GUNDERSEN, Eric, Gould , HAVRAN, Lisa, Marie , KATZ, Alan, Howard , LENNOX, Joseph, Richard , MAYER, Scott, Christian , McDEVITT, Robert, Emmett
- 申请人： AMERICAN HOME PRODUCTS CORPORATION
- 申请人地址： Five Giralda Farms Madison, New Jersey 07940-0874 US
- 专利权人： AMERICAN HOME PRODUCTS CORPORATION
- 当前专利权人： AMERICAN HOME PRODUCTS CORPORATION
- 当前专利权人地址： Five Giralda Farms Madison, New Jersey 07940-0874 US
- 代理机构： Walters, Philip Bernard William
- 优先权： US76709 19980512
- 国际公布： WO9961410 19991202
- 主分类号： C07C235/44
- IPC分类号： C07C235/44 ; C07C59/70 ; C07D307/80 ; C07F9/38 ; C07F9/40 ; A61K31/165 ; A61K31/19
摘要：
This invention provides compounds of Formula (I) having structure (I) wherein: B and D are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, aryl, heteroaryl, aralkyl of 6-12 carbon atoms, or heteroaralkyl of 6-12 carbon atoms except where B and D both are hydrogen; R1 is hydrogen, alkyl of 1-6 carbon atoms, -SO¿2?Ph(OH)(CO2H), -CH(R?2¿)W, -CH¿2?CH2Y, or -CH2CH2CH2Y; R?2¿ is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, -CH¿2?(1H-imidazol-4-yl), -CH2(3-1H-indolyl), -CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), -CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or -CH2(3-pyridyl); W is -CO2R?3¿, -CONHOH, -CN, -CONHR3, aryl, heteroaryl, -CHO, -CH=NOR3, or -CH=NHNHR3; Y is -W, -OCH¿2CO2R?3, aryl, heteroaryl, -C(=NOH)NH¿2, -OR?3, -O(C=O)NR?4R5, -NR3(C=O)OR3, -NR3(C=O)NR4R5¿, or -NR4R5; R3 is hydrogen or alkyl of 1-6 carbon atoms; R?4 and R5¿ are each, independently, hydrogen, or alkyl of 1-6 carbon atoms or R?4 and R5¿ are, together, -(CH¿2?)n-, or -CH2CH2XCH2CH2-; X is O, S, SO, SO2, NR?3¿, or CH¿2?; n is 2 to 5; C is alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, -CONR?6R7, -NR3CONR6R7, -NR3COR6, -OR6, -O¿2CNR?6R7, -NR3CO¿2R6, -O2CR6, -CH2OR?6, -NR6R7, -CR3=CR3R8¿, -CPh¿3?, -CH2NR?6R7¿, or Formula (1); R?6 and R7¿ are each, independently, hydrogen, alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, cycloalkyl of 3-10 carbon atoms, -(CH¿2?CH2O)nCH3, -(CH2)mA or R?6 and R7¿ are, together, -(CH¿2?)p-, -(CH2)2N(CH3)(CH2)4-, -(CH2)2N(R?8)(CH¿2)2-, or -(CH2)2CH(R8)-(CH2)2-; R8 is hydrogen, alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, cycloakyl or 3-10 carbon atoms, -(CH¿2?CH2O)nCH3, -(CH2CH2CH2O)nCH3, or -(CH2)mA; A is aryl, heteroaryl, aryloxy, heteroaryloxy, arylthio, heteroarylthio, arylsulfoxy, heteroarylsulfoxy, arylsulfonyl, heteroarylsulfonyl, -CHF2, -CH2F, -CF3, -(CH2CH2O)nCH3, -(CH2CH2CH2O)nCH3, -CO2R?3¿, -O(C=O)NR6R7, aralkyloxy, or heteroaralkyloxy; m is 2 to 16; p is 2 to 12; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
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