公开(公告)号：US07820654B2

公开(公告)日：2010-10-26

申请号：US11234695

申请日：2005-09-23

申请人： Manojit Pal ,  Srinivas Kalleda ,  Srinivas Padakanti ,  Nalivela Kumara Swamy ,  Koteswar Rao Yeleswarapu ,  Christopher W. Alexander ,  Ish Khanna ,  Javed Iqbal ,  Sivaram Pillarisetti ,  Deepak Barange

发明人： Manojit Pal ,  Srinivas Kalleda ,  Srinivas Padakanti ,  Nalivela Kumara Swamy ,  Koteswar Rao Yeleswarapu ,  Christopher W. Alexander ,  Ish Khanna ,  Javed Iqbal ,  Sivaram Pillarisetti ,  Deepak Barange

IPC分类号： A61K31/54 ,  A61K31/535 ,  A61K31/497 ,  A61K31/505 ,  C07D417/00 ,  C07D413/00 ,  C07D403/00 ,  C07D239/02

CPC分类号： C07D405/14 ,  C07D239/30 ,  C07D239/40 ,  C07D239/42 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D239/54 ,  C07D401/04 ,  C07D403/12 ,  C07D405/12

摘要： The present invention is directed to a compounds, methods and compositions for making the compounds and methods of treating a variety of diseases and disease states including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan, comprising the administration of new heterocyclic compounds, particularly substituted pyrimidines. The present invention is directed to novel compounds represented by the general formula:

摘要翻译： 本发明涉及用于制备化合物的化合物，方法和组合物以及治疗各种疾病和疾病状态的方法，包括动脉粥样硬化，关节炎，再狭窄，糖尿病性肾病或血脂异常或由Perlecan低表达介导的疾病 包括施用新的杂环化合物，特别是取代的嘧啶。 本发明涉及由以下通式表示的新化合物：

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：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。

公开(公告)号：US07202254B2

公开(公告)日：2007-04-10

申请号：US11120617

申请日：2005-05-03

申请人： Jagattaran Das ,  Selavakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Naga Venkata Srinivasa Rao Mamidi ,  Rajagopalan Ramanujam

发明人： Jagattaran Das ,  Selavakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Kumar Magadi ,  Naga Venkata Srinivasa Rao Mamidi ,  Rajagopalan Ramanujam

IPC分类号： C07D401/10 ,  C07D401/14 ,  A61K31/4439 ,  A61P31/04

CPC分类号： C07D249/06 ,  C07D295/135 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D491/10

摘要： The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. More particularly, the present invention relates to novel triazoles of the general formula (I) their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

摘要翻译： 本发明涉及式（I）的新型三唑化合物，其衍生物，其类似物，其互变异构形式，其区域异构体，其旋转异构体，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物组合物 。 更具体地说，本发明涉及通式（I）的新型三唑，

公开(公告)号：US20060270628A1

公开(公告)日：2006-11-30

申请号：US10554472

申请日：2004-04-29

申请人： Jagattaran Das ,  Selvakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Magadi

发明人： Jagattaran Das ,  Selvakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Magadi

IPC分类号： A61K31/695 ,  A61K31/655 ,  A61K31/4192 ,  C07D403/02 ,  C07F7/02

CPC分类号： C07D403/10

摘要： The present invention relates to novel triazole compounds of formula (I), thie pharmaceutically acceptable salts and their pharmaceutical compositions, where all symbols have meaning as defined in the description, for use in the treatment of bacterial infections.

摘要翻译： 本发明涉及式（I）的新型三唑化合物，其药学上可接受的盐及其药物组合物，其中所有符号具有如说明书中定义的含义，用于治疗细菌感染。

公开(公告)号：US20050209223A1

公开(公告)日：2005-09-22

申请号：US11120617

申请日：2005-05-03

申请人： Jagattaran Das ,  Selavakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Magadi ,  Naga Venkata Srinivasa Rao Mamidi ,  Rajagopalan Ramanujam

发明人： Jagattaran Das ,  Selavakumar Natesan ,  Sanjay Trehan ,  Javed Iqbal ,  Sitaram Magadi ,  Naga Venkata Srinivasa Rao Mamidi ,  Rajagopalan Ramanujam

IPC分类号： A61K31/4192 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/655 ,  A61P31/00 ,  A61P31/04 ,  C07D249/06 ,  C07D295/12 ,  C07D295/135 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/10 ,  C07D413/02 ,  C07D413/14 ,  C07D417/02 ,  C07D417/10 ,  C07D417/14

CPC分类号： C07D249/06 ,  C07D295/135 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D491/10

摘要： The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. More particularly, the present invention relates to novel triazoles of the general formula (I) their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

摘要翻译： 本发明涉及式（I）的新型三唑化合物，其衍生物，其类似物，其互变异构形式，其区域异构体，其旋转异构体，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物组合物 。 更具体地，本发明涉及通式（I）的新型三唑衍生物，其类似物，其互变异构体，其区域异构体，其旋转异构体，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物 含有它们的组合物。

公开(公告)号：US06846824B2

公开(公告)日：2005-01-25

申请号：US09816584

申请日：2001-03-23

申请人： Braj Bhushan Lohray ,  Vidya Bhushan Lohray ,  Ashok Channaveerappa Bajji ,  Shivaramayya Kalchar ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Javed Iqbal ,  Ranga Madhavan Gurram

发明人： Braj Bhushan Lohray ,  Vidya Bhushan Lohray ,  Ashok Channaveerappa Bajji ,  Shivaramayya Kalchar ,  Rajagopalan Ramanujam ,  Ranjan Chakrabarti ,  Javed Iqbal ,  Ranga Madhavan Gurram

IPC分类号： A61K9/08 ,  A61K9/10 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/538 ,  A61K31/5415 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/00 ,  A61P9/10 ,  A61P13/12 ,  A61P17/06 ,  A61P19/10 ,  A61P25/28 ,  C07D265/36 ,  C07D279/16 ,  C07D413/06 ,  A61K31/495 ,  C07D241/38

CPC分类号： C07D413/06 ,  A61K31/5415 ,  C07D265/36 ,  C07D279/16

摘要： Compounds of formula (I) its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates can be used to prevent or treat diabetes caused by insulin resistance or impaired glucose tolerance or complications of diabetes caused by insulin resistance or impaired glucose tolerance. The compounds can also be used to reduce cholesterol, body weight, blood glucose, triglycerides and free fatty acids in the blood.

摘要翻译： 式（I）化合物其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐或其药学上可接受的溶剂化物可用于预防或治疗由胰岛素抵抗或糖耐量受损或由胰岛素抵抗引起的糖尿病并发症引起的糖尿病， 葡萄糖耐量降低。 该化合物也可用于降低血液中的胆固醇，体重，血糖，甘油三酯和游离脂肪酸。

公开(公告)号：US09216943B2

公开(公告)日：2015-12-22

申请号：US14114305

申请日：2012-04-27

申请人： Srinivas Katkam ,  Rajeswar Reddy Sagyam ,  Raghavendar Rao Morthala ,  Babu Ireni ,  Krishna Vinigari ,  Suresh Kumar Ramdoss ,  Srinivasulu Rangineni ,  Arjunkumar Tummala ,  Javed Iqbal ,  Srinivas Oruganti ,  Bhaskar Kandagatla

发明人： Srinivas Katkam ,  Rajeswar Reddy Sagyam ,  Raghavendar Rao Morthala ,  Babu Ireni ,  Krishna Vinigari ,  Suresh Kumar Ramdoss ,  Srinivasulu Rangineni ,  Arjunkumar Tummala ,  Javed Iqbal ,  Srinivas Oruganti ,  Bhaskar Kandagatla

IPC分类号： C07C205/45 ,  C07C201/10 ,  C07C201/12 ,  C07C213/02 ,  C07C215/28 ,  C07C213/00 ,  C07C213/10

CPC分类号： C07C205/45 ,  C07C201/10 ,  C07C201/12 ,  C07C213/00 ,  C07C213/02 ,  C07C213/10 ,  C07C215/28 ,  C07C205/04

摘要： 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.

摘要翻译： 本申请提供了芬戈莫德及其药学上可接受的盐的制备方法，盐酸芬戈莫德的纯化方法和用于制备无定形芬戈莫德盐酸盐的方法。

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。