公开(公告)号：US20100168110A1

公开(公告)日：2010-07-01

申请号：US12224168

申请日：2008-06-02

申请人： Laxmikant Chhipa ,  Shitalkumar Zambad ,  Ramesh Gupta ,  Davinder Tuli ,  Ashok Kasundra ,  Siralee Munshi ,  M. Amir Siddiqui ,  Subrat Kumar Bhattamisra ,  C. Dutt ,  Vijay Chauthaiwale

发明人： Laxmikant Chhipa ,  Shitalkumar Zambad ,  Ramesh Gupta ,  Davinder Tuli ,  Ashok Kasundra ,  Siralee Munshi ,  M. Amir Siddiqui ,  Subrat Kumar Bhattamisra ,  C. Dutt ,  Vijay Chauthaiwale

IPC分类号： A61K31/5377 ,  C07D231/20 ,  A61K31/415 ,  C07D403/06 ,  A61K31/4155 ,  C07D403/04 ,  C07D413/04 ,  A61K31/4245 ,  A61K31/506 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P3/00 ,  A61P5/14 ,  A61P17/00 ,  A61P9/00 ,  A61P25/24

CPC分类号： C07D403/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D403/10 ,  C07D403/12 ,  C07D409/04 ,  C07D413/06

摘要： The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.

摘要翻译： 本发明公开了一种新颖的甲状腺样化合物，其中R1 R2，R3，R4和Z如本说明书中所定义，其制备方法，含有这些化合物的组合物以及这些化合物的用途和组合物作为药物。 此外，式（I）化合物对甲状腺受体具有显着低的结合亲和力，因此显着缺乏甲状腺毒性作用。 本发明还涉及式（I）化合物在制备用于治疗各种疾病状况如肥胖，血脂异常，代谢综合征和与代谢综合征相关的并发症的药物中的用途。

公开(公告)号：US20120202816A1

公开(公告)日：2012-08-09

申请号：US13346968

申请日：2012-01-10

申请人： Laxmikant Chhipa ,  Shitalkumar Pukharaj Zambad ,  Ramesh Gupta ,  Davinder Tuli ,  Ashok Kasundra ,  Siralee Munshi ,  M. Amir Siddiqui ,  Subrat Kumar Bhattamisra ,  C. Dutt ,  Vijay Chauthaiwale

发明人： Laxmikant Chhipa ,  Shitalkumar Pukharaj Zambad ,  Ramesh Gupta ,  Davinder Tuli ,  Ashok Kasundra ,  Siralee Munshi ,  M. Amir Siddiqui ,  Subrat Kumar Bhattamisra ,  C. Dutt ,  Vijay Chauthaiwale

IPC分类号： A61K31/415 ,  C07D403/06 ,  A61K31/4155 ,  C07D409/04 ,  C07D413/06 ,  A61K31/4245 ,  C07D413/04 ,  A61K31/5377 ,  A61P3/04 ,  A61P5/48 ,  A61P3/10 ,  A61P3/06 ,  A61P3/00 ,  A61P5/14 ,  A61P3/08 ,  A61P25/24 ,  A61P9/00 ,  A61P17/00 ,  C07D231/18

CPC分类号： C07D403/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D403/10 ,  C07D403/12 ,  C07D409/04 ,  C07D413/06

摘要： The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.

摘要翻译： 本发明公开了一种新颖的甲状腺样化合物，其中R1 R2，R3，R4和Z如本说明书中所定义，其制备方法，含有这些化合物的组合物以及这些化合物的用途和作为药物的组合物。 此外，式（I）化合物对甲状腺受体具有显着低的结合亲和力，因此显着缺乏甲状腺毒性作用。 本发明还涉及式（I）化合物在制备用于治疗各种疾病状况如肥胖，血脂异常，代谢综合征和与代谢综合征相关的并发症的药物中的用途。

公开(公告)号：US08378118B2

公开(公告)日：2013-02-19

申请号：US13346968

申请日：2012-01-10

申请人： Laxmikant Chhipa ,  Shitalkumar Pukharaj Zambad ,  Ramesh Gupta ,  Davinder Tuli ,  Ashok Kasundra ,  Siralee Munshi ,  M. Amir Siddiqui ,  Subrat Kumar Bhattamisra ,  C. Dutt ,  Vijay Chauthaiwale

发明人： Laxmikant Chhipa ,  Shitalkumar Pukharaj Zambad ,  Ramesh Gupta ,  Davinder Tuli ,  Ashok Kasundra ,  Siralee Munshi ,  M. Amir Siddiqui ,  Subrat Kumar Bhattamisra ,  C. Dutt ,  Vijay Chauthaiwale

IPC分类号： A61K31/5377 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4245 ,  A61K31/506 ,  C07D231/20 ,  C07D403/06 ,  C07D403/04 ,  C07D413/04 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P3/00 ,  A61P5/14 ,  A61P17/00 ,  A61P9/00 ,  A61P25/24

CPC分类号： C07D403/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D403/10 ,  C07D403/12 ,  C07D409/04 ,  C07D413/06

摘要： The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.

摘要翻译： 本发明公开了一种新颖的甲状腺样化合物，其中R1 R2，R3，R4和Z如本说明书中所定义，其制备方法，含有这些化合物的组合物以及这些化合物的用途和组合物作为药物。 此外，式（I）化合物对甲状腺受体具有显着低的结合亲和力，因此显着缺乏甲状腺毒性作用。 本发明还涉及式（I）化合物在制备用于治疗各种疾病状况如肥胖，血脂异常，代谢综合征和与代谢综合征相关的并发症的药物中的用途。

公开(公告)号：US08143424B2

公开(公告)日：2012-03-27

申请号：US12224168

申请日：2008-06-02

申请人： Laxmikant Chhipa ,  Shitalkumar Pukharaj Zambad ,  Ramesh Gupta ,  Davinder Tuli ,  Ashok Kasundra ,  Siralee Munshi ,  M. Amir Siddiqui ,  Subrat Kumar Bhattamisra ,  Chaitanya Dutt ,  Vijay Chauthaiwale

发明人： Laxmikant Chhipa ,  Shitalkumar Pukharaj Zambad ,  Ramesh Gupta ,  Davinder Tuli ,  Ashok Kasundra ,  Siralee Munshi ,  M. Amir Siddiqui ,  Subrat Kumar Bhattamisra ,  Chaitanya Dutt ,  Vijay Chauthaiwale

IPC分类号： A61K31/5377 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4245 ,  A61K31/506 ,  C07D231/20 ,  C07D403/06 ,  C07D403/04 ,  C07D413/04 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P3/00 ,  A61P5/14 ,  A61P17/00 ,  A61P9/00 ,  A61P25/24

CPC分类号： C07D403/06 ,  C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D403/10 ,  C07D403/12 ,  C07D409/04 ,  C07D413/06

摘要： A novel thyroid like compounds of formula (I), wherein R1, R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition and use thereof. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions including obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.

摘要翻译： 一种新型甲状腺类似式（I）的化合物，其中R1，R2，R3，R4和Z如说明书中所定义，其制备方法，组合物和用途。 此外，式（I）化合物对甲状腺受体具有显着低的结合亲和力，因此显着缺乏甲状腺毒性作用。 本发明还涉及式（I）化合物在制备用于治疗各种疾病状况，包括肥胖，血脂异常，代谢综合征和与代谢综合征相关的并发症的药物中的用途。

公开(公告)号：US20080207608A1

公开(公告)日：2008-08-28

申请号：US11578354

申请日：2005-04-11

申请人： Prabhat Kumar ,  Uttam Mane ,  Ramesh Gupta ,  Sunil Nadkarni ,  Anookh Mohanan ,  Ruchi Tandon ,  Siralee Munshi

发明人： Prabhat Kumar ,  Uttam Mane ,  Ramesh Gupta ,  Sunil Nadkarni ,  Anookh Mohanan ,  Ruchi Tandon ,  Siralee Munshi

IPC分类号： A61K31/5377 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61P29/00 ,  A61P9/00 ,  C07D215/00 ,  C07D239/72 ,  C07D241/36 ,  C07D295/00 ,  C07D241/00 ,  C07D239/02 ,  C07D213/00 ,  A61P43/00 ,  A61P25/00 ,  A61K31/495 ,  A61K31/517

CPC分类号： C07D215/42 ,  C07D213/72 ,  C07D215/14 ,  C07D241/12 ,  C07D241/18 ,  C07D241/44 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to novel compounds of 2-propene-1-one series, of general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, wherein R5, R6, Q and Y are as defined in the specification. The present invention also relates to a process for preparing such compounds, compositions containing such compounds, and use of such compound and composition in medicine. The compounds of the general formula (I) induce HSP-70 and are useful for the treatment of diseases accompanying pathological stress in a living mammalian organism, including a human being, such as stroke, myocardial infarction, inflammatory disorder, hepatotoxicity, sepsis, diseases of viral origin, allograft rejection, tumourous diseases, gastric mucosal damage, brain haemorrhage, endothelial dysfunctions, diabetic complications, neuro-degenerative diseases, post-traumatic neuronal damage, acute renal failure, glaucoma and aging related skin degeneration.

摘要翻译： 本发明涉及通式（I）的2-丙烯-1-酮系列的新化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，药学上可接受的盐，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， 其中R 5，R 6，Q和Y如说明书中所定义。 本发明还涉及制备这种化合物的方法，含有这些化合物的组合物，以及这些化合物和组合物在医药中的用途。 通式（I）的化合物诱导HSP-70，并且可用于治疗活的哺乳动物生物体中伴随病理应激的疾病，包括人类，如中风，心肌梗死，炎性疾病，肝毒性，败血症，疾病 病毒来源，同种异体移植排斥，肿瘤性疾病，胃粘膜损伤，脑出血，内皮功能障碍，糖尿病并发症，神经退行性疾病，创伤后神经元损伤，急性肾功能衰竭，青光眼和衰老相关的皮肤退化。