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PE20050415A1 - ALPHA CARBOXYL ACIDS SUBSTITUTED AS PPAR MODULATORS - Google Patents

ALPHA CARBOXYL ACIDS SUBSTITUTED AS PPAR MODULATORS

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Publication number
PE20050415A1
PE20050415A1 PE2004000361A PE2004000361A PE20050415A1 PE 20050415 A1 PE20050415 A1 PE 20050415A1 PE 2004000361 A PE2004000361 A PE 2004000361A PE 2004000361 A PE2004000361 A PE 2004000361A PE 20050415 A1 PE20050415 A1 PE 20050415A1
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PE
Peru
Prior art keywords
methyl
alkyl
oxazol
phenyl
substituted
Prior art date
Application number
PE2004000361A
Other languages
Spanish (es)
Inventor
Simon Bailey
Paul Stuart Humphries
Wei-Guo Su
Luke Raymond Zehnder
Donald James Skalitzky
Original Assignee
Pfizer
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Publication of PE20050415A1 publication Critical patent/PE20050415A1/en

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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/65One oxygen atom attached in position 3 or 5
    • C07D213/66One oxygen atom attached in position 3 or 5 having in position 3 an oxygen atom and in each of the positions 4 and 5 a carbon atom bound to an oxygen, sulphur, or nitrogen atom, e.g. pyridoxal
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Abstract

SE REFIERE A COMPUESTOS ACIDOS CARBOXILICOS ALFA SUSTITUIDOS DE FORMULA (I), DONDE Q ES ARILO(C6-C10) O HETEROCICLILO DE 4 A 10 ESLABONES; R1 ES H, HALO, ALQUILO(C1-C8), ALCOXI(C1-C8), CN, CF3, -O-CF3-, -O-SO2-ALQUILO(C1-C8), ENTRE OTROS; R2 ES H, ALQUILO(C1-C8), -(CR11R12)t-CICLOALQUILO(C3-C10), ENTRE OTROS DONDE LOS ATOMOS DE C ESTAN OPCIONALMENTE SUSTITUIDOS CON 1 A 3 GRUPOS R13 Y LOS ATOMOS DE N DE R2 PUEDEN ESTAR SUSTITUIDOS POR ALQUILO(C1-C8); R3 ES -R4-Ar1-Ar2-R5-C(R6R7)-R8, -R4-Y-Y"-(C)p(R11R12)-Ar3-R5-C(R6R7R8), ENTRE OTROS, DONDE CADA Ar ES ARILO(C6-C10) O HETEROCICLILO(C5-C10) ESLABONES OPCIONALMENTE SUSTITUIDOS. SON COMPUESTOS PREFERIDOS: ACIDO 1-({3´-[2-(5-METIL-2-FENIL-1,3-OXAZOL-4-IL)ETOXI]-1,1´-BIFENIL-3-IL}OXI)CICLOBUTANOCARBOXILICO, ACIDO 2-METIL-2-{3-[({[2-(5-METIL-2-FENIL-1,3-OXAZOL-4-IL)ETOXI]CARBONIL}AMINO)METIL]FENOXI}PROPANOICO, ACIDO 2-ETOXI-3-{6-{2-(5-METIL-2-FENIL-1,3-OXAZOL-4-IL)ETOXI]PIRIDIN-3-IL}PROPANOICO, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS MODULAN LA ACTIVIDAD DEL RECEPTOR ACTIVADO-PROLIFERADOR DE PEROXISOMAS (PPAR) Y SON UTILES PARA MODULAR LA GLUCOSA EN SANGRE E INCREMENTAR LA SENSIBILIDAD A INSULINA, PARA EL TRATAMIENTO DE DIABETES, DISLIPIDEMIA OBESIDAD Y TRANSTORNOS INFLAMATORIOSREFERS TO ALPHA CARBOXYL ACID COMPOUNDS SUBSTITUTED FOR FORMULA (I), WHERE Q IS ARYL (C6-C10) OR 4 TO 10-LINK HETEROCICLYL; R1 IS H, HALO, ALKYL (C1-C8), ALCOXY (C1-C8), CN, CF3, -O-CF3-, -O-SO2-ALKYL (C1-C8), AMONG OTHERS; R2 IS H, ALKYL (C1-C8), - (CR11R12) t-CYCLOALKYL (C3-C10), AMONG OTHERS WHERE THE C ATOMS ARE OPTIONALLY REPLACED WITH 1 TO 3 R13 GROUPS AND THE N ATOMS OF R2 MAY BE SUBSTITUTED BY ALKYL (C1-C8); R3 IS -R4-Ar1-Ar2-R5-C (R6R7) -R8, -R4-YY "- (C) p (R11R12) -Ar3-R5-C (R6R7R8), AMONG OTHERS, WHERE EACH Ar IS ARYL ( C6-C10) OR HETERO CYCLYL (C5-C10) OPTIONALLY SUBSTITUTED LINKS ARE PREFERRED COMPOUNDS: ACID 1 - ({3´- [2- (5-METHYL-2-PHENYL-1,3-OXAZOL-4-IL) ETOXY ] -1,1'-BIPHENYL-3-IL} OXY) CYCLOBUTANOCARBOXYL, 2-METHYL-2- {3 - [({[2- (5-METHYL-2-PHENYL-1,3-OXAZOL-4- IL) ETOXY] CARBONYL} AMINO) METHYL] PHENOXY} PROPANOIC, 2-ETHOXY-3- {6- {2- (5-METHYL-2-PHENYL-1,3-OXAZOL-4-IL) ETHOXY] PYRIDIN- 3-IL} PROPANOIC, AMONG OTHERS. ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. THESE COMPOUNDS MODULATE THE ACTIVITY OF THE ACTIVATED PEROXISOME-PROLIFERATOR-RECEPTOR (PPAR) AND ARE USEFUL TO MODULATE BLOOD GLUCOSE AND INCREASE SENSIN TREATMENT OF DIABETES, DYSLIPIDEMIA, OBESITY AND INFLAMMATORY DISORDERS

PE2004000361A 2003-04-15 2004-04-12 ALPHA CARBOXYL ACIDS SUBSTITUTED AS PPAR MODULATORS PE20050415A1 (en)

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EP (1) EP1615899A1 (en)
JP (1) JP2006523671A (en)
KR (1) KR20060009846A (en)
CN (1) CN1805943A (en)
AP (1) AP2005003418A0 (en)
AR (1) AR044514A1 (en)
AU (1) AU2004230316A1 (en)
BR (1) BRPI0409429A (en)
CA (1) CA2521915A1 (en)
CL (1) CL2004000800A1 (en)
EA (1) EA200501462A1 (en)
EC (1) ECSP056105A (en)
IS (1) IS8033A (en)
MA (1) MA27764A1 (en)
MX (1) MXPA05010967A (en)
NL (1) NL1025946C2 (en)
NO (1) NO20055370L (en)
OA (1) OA13157A (en)
PA (1) PA8600201A1 (en)
PE (1) PE20050415A1 (en)
TN (1) TNSN05262A1 (en)
TW (1) TW200510353A (en)
UY (1) UY28266A1 (en)
WO (1) WO2004092145A1 (en)
ZA (1) ZA200508362B (en)

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