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1. 发明申请

US20080114005A1 Fibrate Compounds Having Ppar Agonist Activity 审中-公开
标题翻译：具有Ppar激动剂活性的纤维化合物
公开(公告)号：US20080114005A1
公开(公告)日：2008-05-15
申请号：US11574702
申请日：2005-09-06
申请人： Saibal Kumar Das , Sunil Kumar Singh , Gurram Ranga Madhavan , Debnath Bhuniya , Javed Iqbal , Sudhir Kumar Sharma , Ranjan Chakrabarti
发明人： Saibal Kumar Das , Sunil Kumar Singh , Gurram Ranga Madhavan , Debnath Bhuniya , Javed Iqbal , Sudhir Kumar Sharma , Ranjan Chakrabarti
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D487/04 , C07D239/90
摘要： 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.
摘要翻译：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。

2. 发明申请

US20110105748A1 Novel beta-phenyl-alpha-oxysubstituted propionic derivatives: process for its preparation and their use in the preparation of pharmaceutically important compounds 审中-公开
标题翻译：新型β-苯基-α-氧代取代的丙酸衍生物：其制备方法及其在制备药学上重要的化合物中的应用
公开(公告)号：US20110105748A1
公开(公告)日：2011-05-05
申请号：US10492452
申请日：2002-10-15
申请人： Debnath Bhuniya , Saibal Kumar Das , Gurram Ranga Madhavan , Javed Iqbal , Ranjan Chakrabarti , Sankar Mohan , Mohan Chander
发明人： Debnath Bhuniya , Saibal Kumar Das , Gurram Ranga Madhavan , Javed Iqbal , Ranjan Chakrabarti , Sankar Mohan , Mohan Chander
IPC分类号： C07D265/36 , C07C229/42
CPC分类号： C07C229/42 , C07C229/34 , C07D265/36 , C07D279/16
摘要： The present invention relates to novel propionic acid derivatives. More particularly, the present invention relates to beta-phenyl alpha-oxysubstituted propionic acids of the general formula (I). The present invention also relates to processes for the preparation of compounds of the formula (I) and their use in the preparation of compounds of formula (II).
摘要翻译：本发明涉及新型丙酸衍生物。更具体地说，本发明涉及通式（I）的β-苯基α-氧代取代丙酸。本发明还涉及制备式（I）化合物及其在制备式（II）化合物中的用途的方法。

3. 发明授权

US07365064B2 Benzoxazine and benzothiazine derivatives and pharmaceutical compositions containing them 失效
标题翻译：苯并嗪和苯并噻嗪衍生物和含有它们的药物组合物
公开(公告)号：US07365064B2
公开(公告)日：2008-04-29
申请号：US10492454
申请日：2002-10-15
申请人： Debnath Bhuniya , Saibal Kumar Das , Gurram Ranga Madhavan , Javed Iqbal , Ranjan Chakrabarti
发明人： Debnath Bhuniya , Saibal Kumar Das , Gurram Ranga Madhavan , Javed Iqbal , Ranjan Chakrabarti
IPC分类号： C07D265/36 , C07D279/16 , A61K31/5415 , A61K31/538
CPC分类号： C07C229/42 , C07C229/34 , C07D265/36 , C07D279/16
摘要： 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
摘要翻译：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

4. 发明授权

US07314889B2 Compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：化合物及其在医药中的应用，其制备方法和含有它们的药物组合物
公开(公告)号：US07314889B2
公开(公告)日：2008-01-01
申请号：US10306898
申请日：2002-11-27
申请人： Bhuniya Debnath , Saibal Kumar Das , Gurram Ranga Madhavan , Javed Iqbal , Ranjan Chakrabarti , Reeba Kannimel Vikramadithyan
发明人： Bhuniya Debnath , Saibal Kumar Das , Gurram Ranga Madhavan , Javed Iqbal , Ranjan Chakrabarti , Reeba Kannimel Vikramadithyan
IPC分类号： A61K31/195 , C07C229/34
CPC分类号： A61K31/353 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C309/66 , C07C309/73 , C07C311/53
摘要： 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.
摘要翻译：本发明涉及式（I）的新型抗糖尿病，降血脂，抗胆固醇和低胆固醇血症化合物，其衍生物，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药学上可接受的组合物，其含有他们。

5. 发明授权

US07348334B2 Monocyclic derivatives of aryl alkanoic acids and their use in medicine: process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：芳基链烷酸的单环衍生物及其在医药中的应用：其制备方法和含有它们的药物组合物
公开(公告)号：US07348334B2
公开(公告)日：2008-03-25
申请号：US10119300
申请日：2002-04-08
申请人： Javed Iqbal , Gurram Ranga Madhavan , Saibal Kumar Das , Debnath Bhunia , Ranjan Chakrabarti , Ramanujam Rajagopalan
发明人： Javed Iqbal , Gurram Ranga Madhavan , Saibal Kumar Das , Debnath Bhunia , Ranjan Chakrabarti , Ramanujam Rajagopalan
IPC分类号： A61K31/506 , C07D239/22
CPC分类号： C07D239/36
摘要： The present invention relates to novel hypolipidemic, antihyperglycemic compounds, 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. More particularly, the present invention relates to novel β-aryl-α-oxysubstituted alkylcarboxylic acids of the general 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.
摘要翻译：本发明涉及新型降血脂，抗高血糖化合物，其衍生物，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化物和含有它们的药学上可接受的组合物。更具体地，本发明涉及通式（I）的新型β-芳基-α-氧代取代的烷基羧酸，其衍生物，它们的类似物，其互变异构形式，它们的立体异构体，它们的多晶型物，其药学上可接受的盐，它们的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。

6. 发明申请

US20080221088A1 3,4-Substituted Thiazoles as Ampk Activators 审中-公开
标题翻译： 3,4-取代的噻唑作为Ampk活化剂
公开(公告)号：US20080221088A1
公开(公告)日：2008-09-11
申请号：US11917229
申请日：2006-06-23
申请人： Vijay Kumar Potluri , Saibal Kumar Das , Pradip Kumar Sasmal , Javed Iqbal , Parimal Misra , Ranjan Chakrabarti , Rashmi Talwar
发明人： Vijay Kumar Potluri , Saibal Kumar Das , Pradip Kumar Sasmal , Javed Iqbal , Parimal Misra , Ranjan Chakrabarti , Rashmi Talwar
IPC分类号： A61K31/541 , C07D277/587 , C07D401/12 , C07D417/12 , A61K31/427 , A61K31/4439
CPC分类号： C07D277/42 , C07D417/12
摘要： 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.
摘要翻译：本申请提供了可用作腺苷5'-单磷酸激活蛋白激酶的激活剂的新型噻唑衍生物和含有这些化合物的药物组合物。

7. 发明授权

US08080668B2 Thiazoles derivatives as AMPK activator 失效
标题翻译：噻唑衍生物作为AMPK活化剂
公开(公告)号：US08080668B2
公开(公告)日：2011-12-20
申请号：US11480032
申请日：2006-06-30
申请人： Vijay Kumar Potluri , Saibal Kumar Das , Pradip Kumar Sasmal , Javed Iqbal , Parimal Misra , Ranjan Chakrabarti , Rashmi Talwar
发明人： Vijay Kumar Potluri , Saibal Kumar Das , Pradip Kumar Sasmal , Javed Iqbal , Parimal Misra , Ranjan Chakrabarti , Rashmi Talwar
IPC分类号： A61K31/426 , C07D277/38 , C07D277/56
CPC分类号： C07D277/42
摘要： 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.
摘要翻译：本申请提供了可用作腺苷5'-单磷酸激活蛋白激酶的激活剂的新型噻唑衍生物和含有这些化合物的药物组合物。

8. 发明授权

US07598293B2 Compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：化合物及其在医药中的应用，其制备方法和含有它们的药物组合物
公开(公告)号：US07598293B2
公开(公告)日：2009-10-06
申请号：US11674465
申请日：2007-02-13
申请人： Bhuniya Debnath , Saibal Kumar Das , Gurram Ranga Madhaven , Javed Iqbal , Ranjan Chakrabarti , Reeba Kannimel Vikramadithyan
发明人： Bhuniya Debnath , Saibal Kumar Das , Gurram Ranga Madhaven , Javed Iqbal , Ranjan Chakrabarti , Reeba Kannimel Vikramadithyan
IPC分类号： A61K31/195 , C07C229/34
CPC分类号： A61K31/353 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C309/66 , C07C309/73 , C07C311/53
摘要： 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.
摘要翻译：本发明涉及式（I）的新型抗糖尿病，降血脂，抗胆固醇和低胆固醇血症化合物，其衍生物，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药学上可接受的组合物，其含有他们。

9. 发明授权

US06444816B1 Fused 7-oxo-pyrimidinyl compounds, preparation, composition and use thereof 失效
标题翻译：融合的7-氧代 - 嘧啶基化合物，其制备，组成和用途
公开(公告)号：US06444816B1
公开(公告)日：2002-09-03
申请号：US09507373
申请日：2000-02-18
申请人： Saibal Kumar Das , Papi Reddy Purma , Venkateswarlu Akella , Rajagopalan Ramanujam , Ranjan Chakrabarti , Vidya Bhushan Lohray , Braj Bhushan Lohray , Rao Bheema Paraselli
发明人： Saibal Kumar Das , Papi Reddy Purma , Venkateswarlu Akella , Rajagopalan Ramanujam , Ranjan Chakrabarti , Vidya Bhushan Lohray , Braj Bhushan Lohray , Rao Bheema Paraselli
IPC分类号： C07D23902
CPC分类号： C07C217/22 , C07C237/32 , C07C247/04 , C07D239/36 , C07D239/90
摘要： The present invention relates to novel antiobesity and hypocholesterolemic compounds, 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. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general 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. The present invention also relates to a process for the preparation of the above said novel compounds, their analogs, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to novel intermediates, processes for their preparation and their use in the preparation of compounds of formula (I).
摘要翻译：本发明涉及新型抗肥胖和低胆固醇血症化合物，其衍生物，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。更具体地，本发明涉及通式（I）的新型β-芳基-α-氧代取代的烷基羧酸，其衍生物，它们的类似物，其互变异构形式，它们的立体异构体，它们的多晶型物，其药学上可接受的盐，它们的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。本发明还涉及制备上述新化合物，其类似物，其衍生物，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，药学上可接受的溶剂化物和含有它们的药物组合物的方法。本发明还涉及新型中间体，其制备方法及其在制备式（I）化合物中的用途。

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