公开(公告)号：US20050096331A1

公开(公告)日：2005-05-05

申请号：US10499852

申请日：2002-12-17

申请人： Saibal Das ,  Debnath Bhuniya ,  Gurram, Ranga Madhavan ,  Javed Iqbal ,  Ranjan Chakrabarti

发明人： Saibal Das ,  Debnath Bhuniya ,  Gurram, Ranga Madhavan ,  Javed Iqbal ,  Ranjan Chakrabarti

IPC分类号： A61K31/395 ,  A61K31/519 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P19/10 ,  A61P29/02 ,  A61P35/00 ,  C07D231/40 ,  C07D473/00 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D231/40

摘要： The present invention relates to novel antidiabetic, hypolipidemic, 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 alkyl carboxylic 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： 本发明涉及新型抗糖尿病，降血脂症，抗肥胖症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）的新型烷基羧酸，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药学上可接受的组合物，其含有 他们。

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。

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。

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

公开(公告)号：US20080045580A1

公开(公告)日：2008-02-21

申请号：US11577031

申请日：2005-10-11

申请人： Gurram Madhavan ,  Javed Iqbal ,  Debnath Bhuniya ,  Saibal Das ,  Sudhir Sharma ,  Ranjan Chakrabarti

发明人： Gurram Madhavan ,  Javed Iqbal ,  Debnath Bhuniya ,  Saibal Das ,  Sudhir Sharma ,  Ranjan Chakrabarti

IPC分类号： A61K31/42 ,  A61P29/00 ,  A61P3/10 ,  A61P9/00 ,  A61P9/12 ,  C07D261/08 ,  C07D413/12

CPC分类号： C07D275/02 ,  C07D261/08 ,  C07D413/12

摘要： The present invention relates to novel isoxazole compounds of formula (I) having (PPAR) agonist activity, pharmaceutical compositions containing such compounds and methods for their use.

摘要翻译： 本发明涉及具有（PPAR）激动剂活性的式（I）的异恶唑化合物，含有这些化合物的药物组合物及其用途。

公开(公告)号：US20050113368A1

公开(公告)日：2005-05-26

申请号：US10492454

申请日：2002-10-15

申请人： Debnath Bhuniya ,  Saibal Das ,  Gurram Madhavan ,  Javed Iqbal ,  Ranjan Chakrabarti

发明人： Debnath Bhuniya ,  Saibal Das ,  Gurram Madhavan ,  Javed Iqbal ,  Ranjan Chakrabarti

IPC分类号： A61K9/08 ,  A61K9/10 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/538 ,  A61K31/5415 ,  A61P1/04 ,  A61P1/14 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/10 ,  A61P21/04 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07B61/00 ,  C07C227/04 ,  C07C227/18 ,  C07C229/34 ,  C07C229/42 ,  C07D265/36 ,  C07D279/16

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，降血脂症，抗肥胖症和低胆固醇血症化合物的用途。

公开(公告)号：US20070043035A1

公开(公告)日：2007-02-22

申请号：US10575122

申请日：2004-01-29

申请人： Ranga Gurram ,  Debnath Bhuniya ,  Saibal Das ,  Sudhir Sharma ,  Ranjan Chakrabarti ,  Javed Iqbal

发明人： Ranga Gurram ,  Debnath Bhuniya ,  Saibal Das ,  Sudhir Sharma ,  Ranjan Chakrabarti ,  Javed Iqbal

IPC分类号： A61K31/5415 ,  A61K31/5377 ,  A61K31/47 ,  A61K31/405 ,  A61K31/4035

CPC分类号： C07C69/757 ,  C07B2200/07 ,  C07C33/28 ,  C07C59/68 ,  C07C67/30 ,  C07C67/31 ,  C07C69/712 ,  C07C217/84 ,  C07C309/66 ,  C07C323/52 ,  C07C2601/08 ,  C07C2603/18 ,  C07D233/64 ,  C07D265/38 ,  C07D279/22

摘要： The present invention relates to novel hypolipidemic, antiobesity, hypocholesterolemic and antidiabetic compounds. More particularly, the present invention relates to novel alkyl carboxylic acids of the general formula (I), their stereoisomers, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing them where all symbols are as defined in the description.

摘要翻译： 本发明涉及新型降血脂，抗肥胖，低胆固醇血症和抗糖尿病化合物。 更具体地，本发明涉及通式（I）的新型烷基羧酸，其立体异构体，其药学上可接受的盐和含有它们的药物组合物，其中所有符号如说明书中所定义。

公开(公告)号：US08501955B2

公开(公告)日：2013-08-06

申请号：US12681845

申请日：2008-10-07

申请人： Debnath Bhuniya ,  Sandeep Bhausaheb Bhosale ,  Gobind Sing Kapkoti ,  Venkata Poornapragnacharyulu Palle ,  Siddhartha De ,  Kasim A. Mookhtiar ,  Bhavesh Dave ,  Anil Deshpande ,  Santosh Kurhade ,  Balasaheb Kobal ,  Keshav Naik ,  Sachin Kandalkar

发明人： Debnath Bhuniya ,  Sandeep Bhausaheb Bhosale ,  Gobind Sing Kapkoti ,  Venkata Poornapragnacharyulu Palle ,  Siddhartha De ,  Kasim A. Mookhtiar ,  Bhavesh Dave ,  Anil Deshpande ,  Santosh Kurhade ,  Balasaheb Kobal ,  Keshav Naik ,  Sachin Kandalkar

IPC分类号： C07D277/34 ,  C07D277/38 ,  C07D513/04 ,  A61K31/397 ,  A61K31/44 ,  A61K31/437 ,  A61K31/427

CPC分类号： C07D277/46 ,  C07D213/80 ,  C07D241/26 ,  C07D277/54 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

摘要： Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.

摘要翻译： 乙酰胺衍生物，它们的立体异构体，互变异构体，前药，药学上可接受的盐，多晶型物，溶剂化物及其制剂，用于预防，治疗，控制进展或辅助治疗葡萄糖激酶活化有益的疾病和/或医学病症 ，被披露。 本公开还提供了这些乙酰胺衍生物的制备方法。

公开(公告)号：US08299115B2

公开(公告)日：2012-10-30

申请号：US12600577

申请日：2008-06-05

申请人： Debnath Bhuniya ,  S. Gobind Kapkoti ,  S. Jayakumar Warrier ,  Gagan Kukrejka ,  N. Jagadeesh Mavinahalli ,  P. Venkata Palle ,  A. Kasim Mookhtiar

发明人： Debnath Bhuniya ,  S. Gobind Kapkoti ,  S. Jayakumar Warrier ,  Gagan Kukrejka ,  N. Jagadeesh Mavinahalli ,  P. Venkata Palle ,  A. Kasim Mookhtiar

IPC分类号： A61K31/4025 ,  C07D207/34

CPC分类号： C07D417/12 ,  C07D417/14

摘要： Pyrrole-2-carboxamide derivatives, their polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, beneficial for prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these pyrrole-2-carboxamides.

摘要翻译： 吡咯-2-甲酰胺衍生物，它们的多晶型物，立体异构体，前药，溶剂合物，其药学上可接受的盐和制剂，有利于预防，治疗，控制进展或辅助治疗疾病和/或医学状况，其中葡萄糖激酶 将是有益的，被披露。 本公开还提供了制备这些吡咯-2-甲酰胺的方法。

公开(公告)号：US20100144772A1

公开(公告)日：2010-06-10

申请号：US12528770

申请日：2008-02-25

申请人： Kasim A. Mookhtiar ,  Debnath Bhuniya ,  Bhavesh Dave ,  Gobind S. Kapkoti ,  Sujay Basu ,  Anita Chugh ,  Siddhartha De ,  Venkata P. Palle

发明人： Kasim A. Mookhtiar ,  Debnath Bhuniya ,  Bhavesh Dave ,  Gobind S. Kapkoti ,  Sujay Basu ,  Anita Chugh ,  Siddhartha De ,  Venkata P. Palle

IPC分类号： A61K31/427 ,  C07D417/12 ,  C07D277/38 ,  C07D239/22 ,  A61K31/4439 ,  A61K31/426 ,  A61K31/505 ,  A61P3/10 ,  A61P3/04 ,  C12Q1/48

CPC分类号： C07D277/46 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D213/80 ,  C07D213/82 ,  C07D239/42 ,  C07D257/06 ,  C07D261/14 ,  C07D277/82 ,  C07D285/135 ,  C07D417/12

摘要： Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.

摘要翻译： 本公开的化合物是可用作葡糖苷酶活化剂的式（I）的2,2,2-三取代乙酰胺衍生物，其多晶型物，立体异构体，前药，溶剂化物，药学上可接受的盐和制剂。 本发明还描述了其制备方法。 本公开还描述了表征部分葡糖激酶激活剂的方法。