- COMPOSITIONS AND METHODS FOR MODULATING FXR
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The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).
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- Substituted acrylamido-penicillanic acid derivatives
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Compounds of formula (I) and their derivatives: wherein X is hydrogen or a group NHR1, wherein R1 is hydrogen or an amino protecting group, and R is an optionally substituted spiro, fused or bridged bicyclic group optionally containing one or more heteroatoms selected from oxygen, nitrogen and sulphur, are new and useful in the treatment of bacterial infections in humans and animals.
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- THIAZOLE CARDIOVASCULAR AGENTS
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1-Alkylamino-3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2-propan ol;5-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxymethylene-N-alkyloxazol idin e and/or 2-substituted oxazolidine derivatives thereof, and methods of making such compounds. The compounds exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions in mammals. The compounds are also useful in the treatment of hypertension in mammals. The 5-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolid ines and derivatives are also intermediates for the 1-alkylamino-3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2-propanols . The 1-alkylamino-3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2-propanols can be prepared by base or acid hydrolysis of the corresponding 5-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolid ine or derivative; or by treatment of the corresponding 3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2,3-epoxypropane with the desired alkylamine. Similarly the 5-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxymethylene)-N-alkyloxazolid ine or derivative can be prepared from the corresponding 1-alkylamino-3-(5-carbocyclicalkylaminocarbonylthiazol-2-yloxy)-2-propanols via treatment with an aldehyde or ketone.
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