发明名称 SUBSTITUTED 4-HYDROXY-PHENYLALCANOIC ACID DERIVATIVES WITH AGONIST ACTIVITY TO PPAR-GAMMA
摘要 A COMPOUND HAVING THE FORMULA (I):(FORMULA 1)WHEREIN @A IS SELECTED FROM THE GROUP CONSISTING OF:(I)PHENYL, WHEREIN SAID PHENYL IS OPTIONALLY SUBSTITUTED BY ONE OR MORE HALOGEN ATOMS, C1-6ALKYL, C1-3 ALKOXY, C1-3 FLUOROALKOXY, NITRILE, OR -NR7R8 WHERE R7 AND R8 ARE INDEPENDENTLY HYDROGEN OR C1-3ALKYL;(II)A 5- OR 6- MEMBERED HETEROCYCLIC GROUP CONTAINING AT LEAST ONE HETEROATOM SELECTED FROM OXYGEN, NITROGEN AND SULFUR; AND(III)A FUSED BICYCLIC RING (FORMULA) WHEREIN RING C REPRESENTS A HETEROCYCLIC GROUPS DEFINED IN POINT (II) ABOVE, WHICH BICYCLIC RING IS ATTACHED TO GROUP B VIA A RING ATOM OF RING C;B IS SELECTED FROM THE GROUP CONSISTING OF:(IV) C1-6 ALKYLENE;(V)-MC1-6 ALKYLENE OR C1-6 ALKYLENEMC1-6ALKYLENE, WHEREIN M IS O, S, OR-NR2 WHEREIN R2 REPRESENTS HYDROGEN OR C1-3ALKYL;(VI)A 5- OR 6- MEMBERED HETEROCYCLIC GROUP CONTAINING AT LEAST ONE NITROGEN HETEROATOM AND OPTIONALLY AT LEAST ONE FURTHER HETEROATOM SELECTED FROM OXYGEN, NITROGEN AND SULFURAND OPTIONALLY SUBSTOTUTED BY C1-3 ALKYL; AND (VIII) HET-C1-6ALKYLENE, WHEREIN HET REPRESENTS A HETEROCYCLIC GROUP AS DEFINED IN POINT (VI) ABOVE;ALK REPRESENTS C1-3ALKYLENE;R1REPRESENTS HYDROGEN OR C1-3 ALKYL;Z IS SELECTED FROM THE GROUP CONSISTING OF:(VIII)-(C1-3 ALKYLENE) PHENYL, WHICH PHENYL IS OPTIONALLY SUBSTITUTED BY ONE OR MORE HALOGEN ATOMS; AND(IX)-NR3R4, WHEREIN R3 REPRESENTS HYDROGEN OR C1-3 ALKYL, AND R4 EPRESENTS -Y- (C=O)-T-R5, OR -Y-(CH(OH))-T-R5, WHEREIN:(A) Y REPRESENTS A BOND, C1-6 ALKYLENE, C2-6 ALKENYLENE, C4-6 CYCLOALKYLENE OR CYCLOALKENYLENE, A HETEROCYCLIC GROUP AS DEFINED IN POINT (VI) ABOVE, OR PHENYL OPTIONALLY SUBSTITUTED BY ONE OR MORE C1-3 ALKYL GROUPS AND/OR ONE OR MORE HALOGEN ATOMS;(B)T REPRESENTS A BOND, C1-3 ALKYLENEOXY, -0- OR -N(R6)-, WHEREIN R6 REPRESENTS HYDROGEN OR C1-3 ALKYL;(C) R5 REPRESENTS C1-6 ALKYL, C4-6 CYCLOALKYL OR CYCLOALKENYL, PHENYL (OPTIONALLY SUBSTITUTED BY ONE OR MORE: HALOGEN ATOMS, C1-3 ALKYL, C1-3 ALKOXY GRUPS, C0-3 ALKYLENENR9R10 WHERE EACH R9 AND R10 IS INDEPENDENTLY HYDROGEN, C1-3 ALKYL, -SO2C1-3ALKYL, OR -CO2C1-3ALKYL, -SONHC1-3ALKYL, C0-3ALKYLENECO2H, C0- ALKYLENECO2C1-3ALKYL, OR -OCH2(O)NH2), A 5- OR 6- MEMBERED HETEROCYCLIC GROUP AS DEFINED IN PINT (II) ABOVE, OR A BICYLIC FUSED RING (FORMULA) WHEREIN RING D REPRESENTS A 5- OR 6- MEMBERED HETEROCYCLIC GROUP CONTAINING AT LEAST ONE HETEROATOM SELECTED FROM OXYGEN, NITROGEN AND SULFUR AND OPTIONALLY SUBSTITUTED BY (=O), WHICH BICYCLIC RING IS ATTACHED TO T VIA A RING ATOM OF RING D, OR -C1-6 ALKYLENEMR11 M IS O, S, OR -NR2 WHEREIN R2 AND R11 ARE INDEPENDENTLY HYDROGEN OR C1-3 ALKYL;OR A TAUTOMERIC FORM THEREOF, AND/OR A PHARMACEUTICALLY ACCEPTABLE SALT OR SOLVATE THEREOF.
申请公布号 MY119425(A) 申请公布日期 2005.05.31
申请号 MYPI9700725 申请日期 1997.02.25
申请人 GLAXO GROUP LIMITED 发明人 TIMOTHY MARK WILLSON;JOHN MARK O'CALLAGHAN;GREG ALAN ERICKSON;GRADY EVAN BOSWELL;ROBERT ANTHONY MOOK, JR;ISTVAN KALDOR;BRAD RICHARD HENKE;DAVID NORMAN DEATON;JON LOREN COLLINS;JEFFREY EDMOND COBB;MARKUS BRACKEEN;MATTHEW JUDE SHARP
分类号 C07D263/56;C07D295/18;A61K31/00;A61K31/192;A61K31/195;A61K31/215;A61K31/216;A61K31/353;A61K31/38;A61K31/381;A61K31/40;A61K31/415;A61K31/4164;A61K31/4184;A61K31/42;A61K31/421;A61K31/422;A61K31/423;A61K31/425;A61K31/426;A61K31/427;A61K31/44;A61K31/4402;A61K31/4439;A61K31/445;A61K31/4453;A61K31/454;A61K31/495;A61K31/496;A61K31/535;A61K31/5375;A61K31/5377;A61P3/00;A61P3/06;A61P3/10;A61P9/00;A61P9/04;A61P9/10;A61P9/12;C07C229/36;C07C229/56;C07C235/30;C07C237/40;C07C255/54;C07C323/12;C07D207/08;C07D207/12;C07D213/64;C07D213/65;C07D213/70;C07D213/74;C07D231/12;C07D233/54;C07D233/64;C07D235/12;C07D237/14;C07D249/08;C07D261/08;C07D263/32;C07D277/24;C07D277/42;C07D311/22;C07D333/36;C07D401/04;C07D405/04;C07D413/04;C07D413/12;C07D417/04 主分类号 C07D263/56
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