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    • 6. 发明申请
    • Fibrate Compounds Having Ppar Agonist Activity
    • 具有Ppar激动剂活性的纤维化合物
    • US20080114005A1
    • 2008-05-15
    • US11574702
    • 2005-09-06
    • Saibal Kumar DasSunil Kumar SinghGurram Ranga MadhavanDebnath BhuniyaJaved IqbalSudhir Kumar SharmaRanjan Chakrabarti
    • Saibal Kumar DasSunil Kumar SinghGurram Ranga MadhavanDebnath BhuniyaJaved IqbalSudhir Kumar SharmaRanjan Chakrabarti
    • A61K31/519C07D487/02
    • C07D487/04C07D239/90
    • 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 —CH2—, —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; R1 and R2, which may be the same or different, are independently chosen from hydrogen and C1-C8 alkyl, or R1 and R2 together form a carbocyclic ring having from 4 to 6 carbon atoms; R3 is chosen from hydrogen and C1-C8 alkyl; R4, R5, and R6, which may be the same or different, are independently chosen from hydrogen and C1-C8 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 PPARα 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 PPARα agonist activity and a PPARα 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.
    • 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激动剂活性和哺乳动物中的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。
    • 7. 发明授权
    • Benzoxazine and benzothiazine derivatives and pharmaceutical compositions containing them
    • 苯并嗪和苯并噻嗪衍生物和含有它们的药物组合物
    • US07365064B2
    • 2008-04-29
    • US10492454
    • 2002-10-15
    • Debnath BhuniyaSaibal Kumar DasGurram Ranga MadhavanJaved IqbalRanjan Chakrabarti
    • Debnath BhuniyaSaibal Kumar DasGurram Ranga MadhavanJaved IqbalRanjan Chakrabarti
    • C07D265/36C07D279/16A61K31/5415A61K31/538
    • C07C229/42C07C229/34C07D265/36C07D279/16
    • The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, to a process for preparing such compounds. More particularly, the present invention relates to novel alkyl carboxylic acids of the general, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, to a process for preparing such compounds. The present invention also relates to processes for the preparation of the compounds of formula (I), novel intermediates, processes for their preparation, their use in the preparation of the above said compounds and their use as antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds
    • 本发明涉及式(I)衍生物,其类似物,其互变异构形式,其立体异构体,其多晶型物,其药学上可接受的盐,其药学上可接受的溶剂合物和含有它们的药学上可接受的组合物的新型抗糖尿病,降血脂,抗胆固醇和低胆固醇血症化合物 涉及制备这种化合物的方法。 更具体地说,本发明涉及通用的衍生物,其衍生物,它们的类似物,它们的互变异构形式,它们的立体异构体,它们的多晶型物,其药学上可接受的盐,其药学上可接受的溶剂化物和含有它们的药学上可接受的组合物的新型烷基羧酸, 制备此类化合物的方法。 本发明还涉及式(I)化合物的制备方法,新型中间体,其制备方法,它们在制备上述化合物中的用途及其作为抗糖尿病,降血脂,抗肥胖和低胆固醇血症化合物的用途