Abstract:
There are provided derivatives having PPAR agonist activity. The derivatives include compounds and/or their pharmaceutically acceptable salts; the compounds having the formula (I) wherein A has the structure (II) or (III); X is chosen from -CH 2 -, -O-, -NH-, and -S-; Y is chosen from -O-, -NH-, and -S-; Z, which may be located in any position of substitution, is hydrogen or halogen; R 1 and R 2 , which may be the same or different, are independently chosen from hydrogen and C 1 -C 8 alkyl, or R 1 and R 2 together form a carbocyclic ring having from 4 to 6 carbon atoms; R 3 is chosen from hydrogen and C 1 -C 8 alkyl; R 4 , R 5 , and R 6 , which may be the same or different, are independently chosen from hydrogen and C 1 -C 8 alkyl; and n is 1 to 6. Various embodiments and variants are provided. In accordance with other aspects, the invention also provides methods of producing a PPARa agonist activity in a mammal, the methods including administering to the mammal an effective amount of certain derivative(s) of the first aspect of the invention, a method of producing a PPARa agonist activity and a PPARa agonist activity in a mammal, the method including administering to the mammal an effective amount of certain derivative(s); and a pharmaceutical composition that includes the derivative(s) of the first aspect of the invention and one or more pharmaceutically-acceptable excipients. Various embodiments and variants are provided.
Abstract translation:提供具有PPAR激动剂活性的衍生物。 衍生物包括化合物和/或其药学上可接受的盐; 具有式(I)的化合物其中A具有结构(II)或(III); X选自-CH 2 - , - O - , - N - 和-S-; Y选自-O - , - NH-和-S-; 可以位于任何取代位置的Z是氢或卤素; R 1和R 2可以相同或不同,独立地选自氢和C 1 -C 8烷基, 或者R 1和R 2一起形成具有4至6个碳原子的碳环; R 3选自氢和C 1 -C 8烷基; R 4,R 5,R 5和R 6可以相同或不同,独立地选自氢和C 1 C 8 -C 14烷基; 并且n为1至6.提供了各种实施方案和变体。 根据其它方面,本发明还提供了在哺乳动物中产生PPARα激动剂活性的方法,所述方法包括向哺乳动物施用有效量的本发明第一方面的某些衍生物, PPARα激动剂活性和PPARα激动剂活性,所述方法包括向哺乳动物施用有效量的某些衍生物; 和包含本发明第一方面的衍生物和一种或多种药学上可接受的赋形剂的药物组合物。 提供了各种实施例和变型。
Abstract:
A method for identifying an AMPK activator is provided. The method includes providing a sample of cells that include AMPK and perilipin, providing a sample of an AMPK activator-candidate, contacting the cell sample and the activator-candidate, and measuring a quantitative indicator of the AMPK activation within the cell sample after the contacting step.
Abstract:
The present application provides novel thiazole derivatives that are useful as activators of Adenosine 5'-Monophosphate-Activated Protein Kinase and pharmaceutical compositions containing such compounds.
Abstract:
Provided are novel processes for preparation of (1S, 3aR, 6aS)-octahydrocyclopenta[c]pyrrole-1-carboxylic acid and its derivatives; land their use in preparation of Telaprevir.
Abstract:
The present invention relates to novel triazole compounds of formula (I), where all symbols are as defined in the detailed description; their pharmaceutically acceptable salts their stereosiomers thereof, their prodrugs, their rotamers, their pharmaceutical compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds.
Abstract:
The present application relates to processes for preparing intermediates of Boceprevir and their use in preparation of Boceprevir or its pharmaceutically acceptable salts thereof.
Abstract:
The present application provide processes for the preparation of fingolimod and its pharmaceutically acceptable salts, process for the purification of fingolimod hydrochloride and process for the preparation of amorphous fingolimod hydrochloride.
Abstract:
The present invention relates to novel triazole compounds of formula (I), their prodrugs, their pharmaceutically acceptable salts and their stereoisomers thereof. The present invention also relates to a process for the preparation of the novel compound of the formula (I).
Abstract:
The present invention relates to novel anticancer agents, their pharmaceutically acceptable salts, their geometrical isomers and their pharmaceutically acceptable compositions containing them. the present invention more particularly relates to novel quinazoline compounds, their pharmaceutically acceptable salts and their pharmaceutically acceptable compositions containing them. the novel quinazoline compounds have the general formula (I), where all symbols are as defined in the specification.