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US RE40,558 E1Granted
Therapeutic uses of di-aryl acid derivatives
AssigneeSanofi-Aventis Deutschland GmbH
InventorsZaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko
Life of this patent
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Abstract
The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
Claims42
A compound of formula (I)
- wherein:
- is oxazolyl or quinolinyl, which are optionally substituted by one or more ring system substituents;
- is phenyl, which is optionally substituted by one or more ring system substituents, in addition to being substituted by group Z;
- A is
- B and E are a chemical bond;
- a is 1;
- b is 0 or 1;
- c is 0;
- d is 0;
- g is 1-5;
- R1, R2, R3 and R4 are, independently, hydrogen, halogen or alkyl, wherein alkyl is optionally substituted by one or more alkyl group substituents;
- Z is R21O2C—, R21OC—, —CN, R21O2SHNCO—, R21O2SHN—, (R21)2NCO— or R21O—;
- R21 is independently
- hydrogen,
- alkyl, which is optionally substituted by one or more alkyl group substituents,
- aryl, which is optionally substituted by one or more ring system substituents,
- cycloalkyl, which is optionally substituted by one or more ring system substituents, or
- aralkyl, wherein the aryl portion is optionally substituted by one or more ring system substituents and the alkyl portion is optionally substituted by one or more alkyl group substituents;
- R15, R16 are independently
- hydrogen,
- alkyl, which is optionally substituted by one or more alkyl group substituents,
- aralkyl, wherein the aryl portion is optionally substituted by one or more ring system substituents and the alkyl portion is optionally substituted by one or more alkyl group substituents, or
- alkoxycarbonyl, wherein the alkyl portion is optionally substituted by one or more alkyl group substituents;
- or a pharmaceutically acceptable salt thereof, or an N-oxide thereof, a hydrate thereof or a solvate thereof,
- wherein
- alkyl is an aliphatic hydrocarbon group which is straight or branched having 1 to about 20 carbon atoms;
- aryl is an aromatic monocyclic or multicyclic ring system of about 6 to about 14 carbon atoms;
- a ring system substituent is halo, unsubstituted lower alkyl of 1 to about 4 carbon atoms, unsubstituted alkoxy, unsubstituted aryloxy, unsubstituted aralkyloxy or unsubstituted cycloalkylalkyloxy;
- and
- an alkyl group substituent is unsubstituted acyl, carboxyl, unsubstituted carboxymethyl, unsubstituted methoxycarbonylethyl, unsubstituted benzyloxycarbonylmethyl, unsubstituted pyridylmethyloxycarbonylmethyl or unsubstituted alkoxycarbonyl.
27 more elements
A compound of formula (I)
- wherein:
- is a oxazolyl or quinolinyl, which are optionally substituted by one or more substituents selected from
- phenyl optionally substituted by one or more ring system substituents,
- thienyl optionally substituted by one or more ring system substituents,
- cycloalkyl optionally substituted by one or more ring system substituents,
- lower alkyl optionally substituted by one or more alkyl group substituents,
- branched alkyl optionally substituted by one or more alkyl group substituents,
- fluoro,
- chloro,
- alkoxy wherein the alkyl portion is optionally substituted by one or more alkyl group substituents,
- aralkyloxy wherein the aryl portion is optionally substituted with one or more ring system substituents and the alkyl portion is optionally substituted with one or more alkyl group substituents,
- trifluoromethyl, and
- trifluoromethyloxy;
- is phenyl, which is optionally substituted by one or more ring system substituents, in addition to being substituted by group Z;
- a is 1;
- b is 0 or 1;
- g is 1-5;
- R1, R2, R3 and R4 are, independently, hydrogen, halogen or alkyl, wherein alkyl is optionally substituted by one or more alkyl group substituents;
- Z is R21O2C—, R21OC—, —CN, R21O2SHNCO—, R21O2SHN—, (R21)2NCO— or R21O—;
- R21 is independently
- hydrogen,
- alkyl, which is optionally substituted by one or more alkyl group substituents,
- aryl, which is optionally substituted by one or more ring system substituents,
- cycloalkyl, which is optionally substituted by one or more ring system substituents, or
- aralkyl, wherein the aryl portion is optionally substituted by one or more ring system substituents and the alkyl portion is optionally substituted by one or more alkyl group substituents;
- R15, R16 are independently
- hydrogen,
- alkyl, which is optionally substituted by one or more alkyl group substituents,
- aralkyl, wherein the aryl portion is optionally substituted by one or more ring system substituents and the alkyl portion is optionally substituted by one or more alkyl group substituents, or
- alkoxycarbonyl, wherein the alkyl portion is optionally substituted by one or more alkyl group substituents;
- or a pharmaceutically acceptable salt thereof, or an N-oxide thereof,
- wherein
- alkyl is an aliphatic hydrocarbon group which is straight or branched having 1 to about 20 carbon atoms;
- aryl is an aromatic monocyclic or multicyclic ring system of about 6 to about 14 carbon atoms;
- a ring system substituent is halo, unsubstituted lower alkyl of 1 to about 4 carbon atoms, unsubstituted alkoxy, unsubstituted aryloxy, unsubstituted aralkyloxy or unsubstituted cycloalkylalkyloxy;
- and
- an alkyl group substituent is unsubstituted acyl, carboxyl, unsubstituted carboxymethyl, unsubstituted methoxycarbonylethyl, unsubstituted benzyloxycarbonylmethyl, unsubstituted pyridylmethyloxycarbonylmethyl or unsubstituted alkoxycarbonyl.
34 more elements
A compound, wherein the compound is
- or a pharmaceutically acceptable salt thereof, or an N-oxide thereof.
A compound, wherein the compound is
- or a pharmaceutically acceptable salt thereof, or an N-oxide thereof.
Dependencies are inferred from the claim text.