公开(公告)号：US08859566B2

公开(公告)日：2014-10-14

申请号：US13256071

申请日：2010-03-12

申请人： Venkata Palle ,  Vidya Ramdas ,  Dinesh Barawkar ,  Sujay Basu ,  Summon Koul ,  Yogesh Waman ,  Meena Patel ,  Anil Panmand

发明人： Venkata Palle ,  Vidya Ramdas ,  Dinesh Barawkar ,  Sujay Basu ,  Summon Koul ,  Yogesh Waman ,  Meena Patel ,  Anil Panmand

IPC分类号： A61K31/522 ,  C07D473/28 ,  C07D473/18 ,  C07D473/06 ,  C07D473/30 ,  C07D473/40

CPC分类号： C07D473/40 ,  A61K31/522 ,  A61K31/5377 ,  C07D473/06 ,  C07D473/18 ,  C07D473/30

摘要： The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.

摘要翻译： 本发明公开了式（I）的取代的稠合嘧啶化合物，其互变异构体，多晶型物，立体异构体，溶剂化物，药学上可接受的盐或含有它们的药物组合物以及治疗由腺苷受体（AR）活性介导的病症和疾病的方法。 本发明的化合物可用于治疗，预防或抑制可能易受腺苷受体拮抗作用改善的疾病和病症，例如哮喘，慢性阻塞性肺病，血管生成，肺纤维化，肺气肿，过敏性疾病 ，炎症，再灌注损伤，心肌缺血，动脉粥样硬化，高血压，充血性心力衰竭，视网膜病变，糖尿病，肥胖，炎性胃肠道疾病和/或自身免疫性疾病。

公开(公告)号：US20120115864A1

公开(公告)日：2012-05-10

申请号：US13256071

申请日：2010-03-12

申请人： Venkata Palle ,  Vidya Ramdas ,  Dinesh Barawkar ,  Sujay Basu ,  Summon Koul ,  Yogesh Waman ,  Meena Patel ,  Anil Panmand

发明人： Venkata Palle ,  Vidya Ramdas ,  Dinesh Barawkar ,  Sujay Basu ,  Summon Koul ,  Yogesh Waman ,  Meena Patel ,  Anil Panmand

IPC分类号： A61K31/5377 ,  A61K31/522 ,  A61P11/06 ,  C07D473/30 ,  A61P35/00 ,  A61P37/08 ,  A61P29/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/00 ,  A61P3/04 ,  A61P3/10 ,  A61P1/00 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P3/06 ,  A61P11/00

CPC分类号： C07D473/40 ,  A61K31/522 ,  A61K31/5377 ,  C07D473/06 ,  C07D473/18 ,  C07D473/30

摘要： The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.

摘要翻译： 本发明公开了式（I）的取代的稠合嘧啶化合物，其互变异构体，多晶型物，立体异构体，溶剂化物，药学上可接受的盐或含有它们的药物组合物以及治疗由腺苷受体（AR）活性介导的病症和疾病的方法。 本发明的化合物可用于治疗，预防或抑制可能易受腺苷受体拮抗作用改善的疾病和病症，例如哮喘，慢性阻塞性肺病，血管生成，肺纤维化，肺气肿，过敏性疾病 ，炎症，再灌注损伤，心肌缺血，动脉粥样硬化，高血压，充血性心力衰竭，视网膜病变，糖尿病，肥胖，炎性胃肠道疾病和/或自身免疫性疾病。

公开(公告)号：US08796290B2

公开(公告)日：2014-08-05

申请号：US13508672

申请日：2010-11-09

申请人： Vidya Ramdas ,  Summon Koul ,  Sujay Basu ,  Yogesh Waman ,  Yogesh Shejul ,  Dinesh Barawkar ,  Venkata Poornapragnacharyulu Palle

发明人： Vidya Ramdas ,  Summon Koul ,  Sujay Basu ,  Yogesh Waman ,  Yogesh Shejul ,  Dinesh Barawkar ,  Venkata Poornapragnacharyulu Palle

IPC分类号： A61K31/522 ,  C07D473/30

CPC分类号： C07D473/18 ,  C07D473/06

摘要： The present invention provides substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The present invention also provides processes for preparation of compounds of formula (I).

摘要翻译： 本发明提供式（I）的取代的稠合嘧啶化合物，其互变异构体，多晶型物，立体异构体，前药，溶剂化物，药学上可接受的盐，含有它们的药物组合物和治疗由腺苷受体（AR）活性介导的病症和疾病的方法 。 本发明还提供式（I）化合物的制备方法。

公开(公告)号：US20120225812A1

公开(公告)日：2012-09-06

申请号：US13508672

申请日：2010-11-09

申请人： Vidya Ramdas ,  Summon Koul ,  Sujay Basu ,  Yogesh Waman ,  Yogesh Shejul ,  Dinesh Barawkar ,  Ventaka Poornapragnacharyulu Palle

发明人： Vidya Ramdas ,  Summon Koul ,  Sujay Basu ,  Yogesh Waman ,  Yogesh Shejul ,  Dinesh Barawkar ,  Ventaka Poornapragnacharyulu Palle

IPC分类号： A61K38/28 ,  A61K31/60 ,  A61K31/56 ,  A61K31/522 ,  A61P3/06 ,  C07D473/06 ,  A61P29/00 ,  A61P3/10 ,  A61P9/12 ,  A61K38/26 ,  A61K31/455

CPC分类号： C07D473/18 ,  C07D473/06

摘要： The present invention provides substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The present invention also provides process of preparation of compounds of formula (I).

摘要翻译： 本发明提供式（I）的取代的稠合嘧啶化合物，其互变异构体，多晶型物，立体异构体，前药，溶剂化物，药学上可接受的盐，含有它们的药物组合物和治疗由腺苷受体（AR）活性介导的病症和疾病的方法 。 本发明还提供式（I）化合物的制备方法。