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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

US20140228303A1 NOVEL SGLT INHIBITORS 审中-公开
公开(公告)号：US20140228303A1
公开(公告)日：2014-08-14
申请号：US14126268
申请日：2012-06-13
申请人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Gurmeet Kaur Nanda , Sastry V. R. S Thungathurthi , Nishan Singh , Sudhir Kumar Sharma
发明人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Gurmeet Kaur Nanda , Sastry V. R. S Thungathurthi , Nishan Singh , Sudhir Kumar Sharma
IPC分类号： A61K31/7048 , A61K31/70 , C07H19/01 , C07H7/04
CPC分类号： A61K31/7048 , A61K31/70 , C07D309/10 , C07D401/04 , C07D493/08 , C07H7/04 , C07H9/04 , C07H13/04 , C07H13/12 , C07H15/04 , C07H19/01
摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).

3. 发明授权

US08455479B2 Heterocyclic compounds 有权
标题翻译：杂环化合物
公开(公告)号：US08455479B2
公开(公告)日：2013-06-04
申请号：US12863016
申请日：2009-01-23
申请人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Nishan Singh , Gurmeet Kaur Nanda , Sitaram Kumar Magadi , Sudhir Kumar Sharma
发明人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Nishan Singh , Gurmeet Kaur Nanda , Sitaram Kumar Magadi , Sudhir Kumar Sharma
IPC分类号： C07D243/14 , C07D403/06 , C07D413/12 , C07D487/04 , A61K31/551 , A61P3/10
CPC分类号： C07D243/14 , C07D403/06 , C07D413/12 , C07D487/04
摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).
摘要翻译：本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体，包括R和S异构体，多晶型物，前药，代谢物，盐或溶剂化物。本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。本发明还提供包含式I化合物的药物组合物以及通过抑制二肽基肽酶IV（DPP-IV）来治疗或预防可被调节或归一化的一种或多种病症的方法。

4. 发明授权

US08906913B2 Azabicyclohexanes 有权
标题翻译：氮杂双环己烷
公开(公告)号：US08906913B2
公开(公告)日：2014-12-09
申请号：US13380744
申请日：2010-06-22
申请人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Gurmeet Kaur , Sandeep Kanwar , Nishan Singh , Gurmeet Kaur Nanda , Sitaram Kumar Magadi , Sudhir Kumar Sharma
发明人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Gurmeet Kaur , Sandeep Kanwar , Nishan Singh , Gurmeet Kaur Nanda , Sitaram Kumar Magadi , Sudhir Kumar Sharma
IPC分类号： A61K31/5355 , C07D413/10 , C07D209/52 , C07D417/14 , C07D491/08 , C07D221/22 , C07D487/04 , C07D413/14 , C07D409/04 , C07D471/04 , C07D417/10 , C07D401/10
CPC分类号： C07D221/22 , C07D209/52 , C07D401/10 , C07D409/04 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/08
摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.
摘要翻译：本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体，包括R和S异构体，多晶型物，前药，代谢物，盐或溶剂化物。本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。

5. 发明授权

US08841306B2 Antimicrobials 有权
标题翻译：抗生素
公开(公告)号：US08841306B2
公开(公告)日：2014-09-23
申请号：US13130440
申请日：2009-11-18
申请人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Sandeep Kanwar , Sitaram Kumar Magadi , Sudhir Kumar Sharma
发明人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Sandeep Kanwar , Sitaram Kumar Magadi , Sudhir Kumar Sharma
IPC分类号： A61K31/33 , C07D413/14 , C07D417/12 , C07D487/04 , C07D413/12 , C07D263/20
CPC分类号： C07D487/04 , C07D263/20 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H. influenza, Moraxella, acid-fast organisms such as Mycobacterium tuberculosis as well as Linezolid resistant species of Staphylococcus and Enterococcus.
摘要翻译：本发明涉及式I的新型苯基恶唑烷酮化合物，其药学上可接受的类似物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂化物。本发明还涉及合成新型式I化合物或其药学上可接受的类似物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。本发明还提供了包含新颖的式I化合物和使用它们的方法的药物组合物。本发明的化合物可用作抗微生物剂，对许多需氧和/或厌氧革兰氏阳性和/或革兰氏阴性病原体有效，如葡萄球菌，链球菌，肠球菌，细菌，梭菌，流感嗜血杆菌，莫拉氏菌，耐酸菌，如结核分枝杆菌，以及耐盐霉菌属的霉菌和肠球菌。

6. 发明授权

US09133116B2 Bicyclic compounds 有权
标题翻译：双环化合物
公开(公告)号：US09133116B2
公开(公告)日：2015-09-15
申请号：US13876757
申请日：2011-09-27
申请人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Nishan Singh , Sudhir Kumar Sharma
发明人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Nishan Singh , Sudhir Kumar Sharma
IPC分类号： C07D209/52 , A61K31/403 , A61K45/06
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06
摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention further provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more disorders of the central and/or peripheral nervous system, preferably by modulating neurological and/or psychiatric targets (GPCR and/or non-GPCR).
摘要翻译：本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂化物。本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。本发明还提供包含式I化合物的药物组合物和治疗或预防中枢和/或周围神经系统的一种或多种病症的方法，优选通过调节神经和/或精神病学靶标（GPCR和/或非GPCR）。

7. 发明授权

US09018249B2 SGLT inhibitors 有权
标题翻译： SGLT抑制剂
公开(公告)号：US09018249B2
公开(公告)日：2015-04-28
申请号：US14344628
申请日：2012-09-12
申请人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Gurmeet Kaur Nanda , Sastry V. R. S. Thungathurthi , Nishan Singh , Sudhir Kumar Sharma
发明人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Gurmeet Kaur Nanda , Sastry V. R. S. Thungathurthi , Nishan Singh , Sudhir Kumar Sharma
IPC分类号： A61K31/352 , C07D311/00 , C07D309/10 , C07D493/08
CPC分类号： C07D309/10 , C07D493/08 , C07H7/04
摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
摘要翻译：本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂化物。本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。本发明还提供包含式I的新化合物和治疗或预防一种或多种可通过抑制葡萄糖转运蛋白-2（SGLT-2）调节或归一化的病症或疾病的药物组合物。

8. 发明申请

US20100311732A1 NOVEL HETEROCYCLIC COMPOUNDS 有权
标题翻译：新型杂环化合物
公开(公告)号：US20100311732A1
公开(公告)日：2010-12-09
申请号：US12863016
申请日：2009-01-23
申请人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Nishan Singh , Gurmeet Kaur Nanda , Sitaram Kumar Magadi , Sudhir Kumar Sharma
发明人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Nishan Singh , Gurmeet Kaur Nanda , Sitaram Kumar Magadi , Sudhir Kumar Sharma
IPC分类号： A61K31/5517 , C07D243/14 , C07D487/04 , A61K31/5513 , A61P3/10 , A61P3/06 , A61P9/10 , A61P9/12 , A61P1/00 , A61P1/04 , A61P25/28 , A61P35/00 , A61P35/04 , A61P19/10 , A61P29/00 , A61P15/16 , A61P17/00 , A61P31/18
CPC分类号： C07D243/14 , C07D403/06 , C07D413/12 , C07D487/04
摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).
摘要翻译：本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构体，立体异构体，包括R和S异构体，多晶型物，前药，代谢物，盐或溶剂化物。本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。本发明还提供包含式I化合物的药物组合物以及通过抑制二肽基肽酶IV（DPP-IV）来治疗或预防可被调节或归一化的一种或多种病症的方法。

9. 发明申请

US20130253029A1 NOVEL BICYCLIC COMPOUNDS 有权
标题翻译：新型双环化合物
公开(公告)号：US20130253029A1
公开(公告)日：2013-09-26
申请号：US13876757
申请日：2011-09-27
申请人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Nishan Singh , Sudhir Kumar Sharma
发明人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Nishan Singh , Sudhir Kumar Sharma
IPC分类号： C07D209/52 , A61K45/06 , A61K31/403
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06
摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention further provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more disorders of the central and/or peripheral nervous system, preferably by modulating neurological and/or psychiatric targets (GPCR and/or non-GPCR).
摘要翻译：本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂化物。本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。本发明还提供包含式I化合物的药物组合物和治疗或预防中枢和/或周围神经系统的一种或多种病症的方法，优选通过调节神经和/或精神病学靶标（GPCR和/或非GPCR）。

10. 发明申请

US20140378540A1 NOVEL SGLT INHIBITORS 有权
标题翻译：新型SGLT抑制剂
公开(公告)号：US20140378540A1
公开(公告)日：2014-12-25
申请号：US14344628
申请日：2012-09-12
申请人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Gurmeet Kaur Nanda , Sastry V. R. S Thungathurthi , Nishan Singh , Sudhir Kumar Sharma
发明人： Rajesh Jain , Sanjay Trehan , Jagattaran Das , Gurmeet Kaur Nanda , Sastry V. R. S Thungathurthi , Nishan Singh , Sudhir Kumar Sharma
IPC分类号： C07D309/10 , C07D493/08
CPC分类号： C07D309/10 , C07D493/08 , C07H7/04
摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).
摘要翻译：本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂化物。本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。本发明还提供包含式I的新化合物和治疗或预防一种或多种可通过抑制葡萄糖转运蛋白-2（SGLT-2）调节或归一化的病症或疾病的药物组合物。

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