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1. 发明授权

US08940751B2 Purine compounds as prodrugs of A2B adenosine receptor antagonists, their process and medicinal applications 有权
标题翻译：嘌呤化合物作为A2B腺苷受体拮抗剂的前药，其过程和药物应用
公开(公告)号：US08940751B2
公开(公告)日：2015-01-27
申请号：US13821481
申请日：2011-09-09
申请人： Dinesh Barawkar , Sujay Basu , Vidya Ramdas , Venkata Poornapragnacharyulu Palle , Yogesh Waman , Meena Patel , Anil Panmand
发明人： Dinesh Barawkar , Sujay Basu , Vidya Ramdas , Venkata Poornapragnacharyulu Palle , Yogesh Waman , Meena Patel , Anil Panmand
IPC分类号： A61K31/522 , C07D473/30 , C07F9/6561 , A61K31/675 , A61K45/06
CPC分类号： A61K31/522 , A61K31/675 , A61K45/06 , C07D473/30 , C07F9/65616
摘要： The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
摘要翻译：本公开内容涉及式（I）或式（II）的嘌呤化合物或其互变异构体，多晶型物，立体异构体，溶剂合物或其药学上可接受的盐或含有它们的药物组合物以及将由其介导的病症和疾病作为治疗方法 A2B腺苷受体拮抗剂。本公开的化合物可用于治疗，预防或抑制可能通过腺苷A2B受体的介导而改善的疾病和病症。本公开还涉及制备这些化合物的方法以及含有它们的药物组合物。

2. 发明申请

US20130172249A1 PURINE COMPOUNDS AS PRODRUGS OF A2B ADENOSINE RECEPTOR ANTAGONISTS, THEIR PROCESS AND MEDICINAL APPLICATIONS 有权
标题翻译：作为A2B腺苷受体拮抗剂的原料的嘌呤化合物，其方法和药物应用
公开(公告)号：US20130172249A1
公开(公告)日：2013-07-04
申请号：US13821481
申请日：2011-09-09
申请人： Dinesh Barawkar , Sujay Basu , Vidya Ramdas , Venkata Poornapragnacharyulu Palle , Yogesh Waman , Meena Patel , Anil Panmand
发明人： Dinesh Barawkar , Sujay Basu , Vidya Ramdas , Venkata Poornapragnacharyulu Palle , Yogesh Waman , Meena Patel , Anil Panmand
IPC分类号： A61K31/522 , A61K45/06 , A61K31/675 , C07D473/30 , C07F9/6561
CPC分类号： A61K31/522 , A61K31/675 , A61K45/06 , C07D473/30 , C07F9/65616
摘要： The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. Such conditions include, but are not limited to, 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 including inflammatory bowel disease, sickle cell disease, and/or autoimmune diseases, and to their use in treating mammals for various disease states, such as gastrointestinal disorders, immunological disorders, hypersensitivity disorders, neurological disorders, and cardiovascular diseases due to both cellular hyperproliferation and apoptosis, and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
摘要翻译：本公开内容涉及式（I）或式（II）的嘌呤化合物或其互变异构体，多晶型物，立体异构体，溶剂合物或其药学上可接受的盐或含有它们的药物组合物以及将由其介导的病症和疾病作为治疗方法 A2B腺苷受体拮抗剂。本公开的化合物可用于治疗，预防或抑制可能通过腺苷A2B受体的介导而改善的疾病和病症。这些病症包括但不限于哮喘，慢性阻塞性肺病，血管发生，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，肥胖症，包括炎症性肠病，镰状细胞病和/或自身免疫性疾病在内的炎性胃肠道疾病，以及它们在治疗哺乳动物用于各种疾病状态的用途，例如胃肠疾病，免疫学障碍，超敏反应性障碍，神经障碍和心血管疾病细胞过度增殖和细胞凋亡等。本公开还涉及制备这些化合物的方法以及含有它们的药物组合物。

3. 发明授权

US08252797B2 Heterocyclic compounds as adenosine receptor antagonist 有权
标题翻译：杂环化合物作为腺苷受体拮抗剂
公开(公告)号：US08252797B2
公开(公告)日：2012-08-28
申请号：US12411956
申请日：2009-03-26
申请人： Venkata Palle , Sujay Basu , Yogesh Waman , Vidya Ramdas , Dinesh Barawkar , Meena Patel , Anil Panmand
发明人： Venkata Palle , Sujay Basu , Yogesh Waman , Vidya Ramdas , Dinesh Barawkar , Meena Patel , Anil Panmand
IPC分类号： C07D473/06 , C07D473/04 , A61K31/522 , C07D231/14 , C07D261/04 , A61P11/06 , A61P37/08
CPC分类号： C07D473/06 , C07D473/08
摘要： Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.
摘要翻译：作为腺苷受体拮抗剂，本公开的化合物是式（I）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，溶剂合物或其药学上可接受的盐。本发明还描述了其制备方法。

4. 发明授权

US08859566B2 Substituted fused pyrimidine compounds 有权
标题翻译：取代的稠合嘧啶化合物
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。

5. 发明申请

US20120115864A1 Substituted Fused Pyrimidine Compounds 有权
标题翻译：取代的熔融嘧啶化合物
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。

6. 发明授权

US08796290B2 Substituted fused pyrimidine compounds, its preparation and uses thereof 有权
标题翻译：取代的稠合嘧啶化合物，其制备和用途
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。

7. 发明授权

US09006177B2 Fused tricyclic compounds as adenosine receptor antagonist 有权
标题翻译：融合三环化合物作为腺苷受体拮抗剂
公开(公告)号：US09006177B2
公开(公告)日：2015-04-14
申请号：US13825665
申请日：2011-09-22
申请人： Dinesh Barawkar , Sujay Basu , Vidya Ramdas , Minakshi Naykodi , Meena Patel , Yogesh Shejul , Sachin Thorat , Anil Panmand
发明人： Dinesh Barawkar , Sujay Basu , Vidya Ramdas , Minakshi Naykodi , Meena Patel , Yogesh Shejul , Sachin Thorat , Anil Panmand
IPC分类号： A61K38/28 , A61P5/50 , C07D487/14 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D519/00
CPC分类号： C07D487/14 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D519/00
摘要： The present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor. Such conditions include, but are not limited to, Parkinsons disease, restless leg syndrome, Alzheimers disease, neurodegenerative disorder, inflammation, wound healing, dermal fibrosis, nocturnal myoclonus, cerebral ischaemia, myocardial ischemia, Huntington's disease, multiple system atrophy, corticobasal degeneration, Wilson's disease or other disorders of basal ganglia which results in dyskinesias, post traumatic stress disorder, hepatic cirrhosis, sepsis, spinal cord injury, retinopathy, hypertension, social memory impairment, depression, neuroprotection, narcolepsy or other sleep related disorders, attention deficit hyperactivity disorder, drug addiction, post traumatic stress disorder and vascular injury and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
摘要翻译：本公开内容涉及式（I）的稠合三环化合物或其互变异构体，多晶型物，立体异构体，前药，溶剂合物或药学上可接受的盐或含有它们的药物组合物和将其作为A2A腺苷介导的病症和疾病的方法受体拮抗剂。本公开的化合物可用于治疗，预防或抑制可能通过腺苷A2A受体介导而改善的疾病和病症。这些病症包括但不限于：帕金森病，不宁腿综合征，阿尔茨海默病，神经变性疾病，炎症，伤口愈合，真皮纤维化，夜间肌阵挛，脑缺血，心肌缺血，亨廷顿舞蹈病，多系统萎缩，皮质基底变性，威尔逊病或基底节神经节的其他疾病，导致运动障碍，创伤后应激障碍，肝硬化，败血症，脊髓损伤，视网膜病变，高血压，社会记忆障碍，抑郁，神经保护，发作性睡眠或其他睡眠相关疾病，注意缺陷多动障碍，药物成瘾，创伤后应激障碍和血管损伤等。本公开还涉及制备这些化合物的方法以及含有它们的药物组合物。

8. 发明申请

US20090298744A1 HETEROCYCLIC COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONIST 有权
标题翻译：作为腺苷受体拮抗剂的杂环化合物
公开(公告)号：US20090298744A1
公开(公告)日：2009-12-03
申请号：US12411956
申请日：2009-03-26
申请人： Venkata Palle , Sujay Basu , Yogesh Waman , Vidya Ramdas , Dinesh Barawkar
发明人： Venkata Palle , Sujay Basu , Yogesh Waman , Vidya Ramdas , Dinesh Barawkar
IPC分类号： A61K38/28 , C07D473/04 , A61K31/522 , A61K31/496 , A61K31/56 , A61K31/60 , A61P9/00 , A61P29/00 , A61P37/08 , A61P3/00
CPC分类号： C07D473/06 , C07D473/08
摘要： Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.
摘要翻译：作为腺苷受体拮抗剂，本公开的化合物是式（I）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，溶剂合物或其药学上可接受的盐。本发明还描述了其制备方法。

9. 发明申请

US20120225812A1 SUBSTITUTED FUSED PYRIMIDINE COMPOUNDS, ITS PREPARATION AND USES THEREOF 有权
标题翻译：取代的熔融吡啶化合物，其制备及其用途
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。

10. 发明授权

US09115133B2 Substituted fused tricyclic compounds, compositions and medicinal applications thereof 有权
标题翻译：取代的稠合三环化合物，组合物及其药用应用
公开(公告)号：US09115133B2
公开(公告)日：2015-08-25
申请号：US14006630
申请日：2012-03-21
申请人： Dinesh Barawkar , Tanushree Bende , Robert Zahler , Anish Bandyopadhyay , Robindro Singh Sarangthem , Jignesh Doshi , Yogesh Waman , Rushikesh Jadhav , Umesh Prasad Singh
发明人： Dinesh Barawkar , Tanushree Bende , Robert Zahler , Anish Bandyopadhyay , Robindro Singh Sarangthem , Jignesh Doshi , Yogesh Waman , Rushikesh Jadhav , Umesh Prasad Singh
IPC分类号： C07D471/14 , A61K31/4375 , A61K31/5025 , A61K31/5377 , A61K31/519 , A61K45/06 , A61K31/496
CPC分类号： C07D471/14 , A61K31/4375 , A61K31/496 , A61K31/5025 , A61K31/519 , A61K31/5377 , A61K45/06 , Y02A50/475 , A61K2300/00
摘要： The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity. Such conditions include, but not limited to, arthritis, Alzheimer's disease, autoimmune thyroid disorders, cancer, diabetes, leukemia, T-cell prolymphocytic leukemia, lymphoma, myleoproliferation disorders, lupus, multiple myeloma, multiple sclerosis, osteoarthritis, sepsis, psoriatic arthritis, prostate cancer, T-cell autoimmune disease, inflammatory diseases, chronic and acute allograft transplant rejection, bone marrow transplant, stroke, asthma, chronic obstructive pulmonary disease, allergy, bronchitis, viral diseases, or Type I diabetes, complications from diabetes, rheumatoid arthritis, asthma, Crohn's disease, dry eye, uveitis, inflammatory bowel disease, organ transplant rejection, psoriasis and ulcerative colitis. The present disclosure also relates to process for the preparation of such compounds, and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）或（Ia）的取代的稠合三环化合物，其互变异构体，多晶型物，立体异构体，前药，溶剂合物，共晶体，药学上可接受的盐，含有它们的药物组合物和治疗病症和疾病的方法由JAK活动介导。本发明的化合物可用于治疗，预防或抑制由JAK活性介导的疾病和病症。这些病症包括但不限于关节炎，阿尔茨海默氏病，自身免疫性甲状腺疾病，癌症，糖尿病，白血病，T细胞淋巴细胞性白血病，淋巴瘤，组织增生障碍，狼疮，多发性骨髓瘤，多发性硬化，骨关节炎，败血症，牛皮癣关节炎，前列腺癌，T细胞自身免疫疾病，炎性疾病，慢性和急性同种异体移植排斥反应，骨髓移植，中风，哮喘，慢性阻塞性肺病，过敏，支气管炎，病毒性疾病或I型糖尿病，糖尿病并发症，类风湿关节炎，哮喘，克罗恩病，干眼症，葡萄膜炎，炎性肠病，器官移植排斥反应，牛皮癣和溃疡性结肠炎。本公开还涉及制备这些化合物的方法以及含有它们的药物组合物。

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