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    Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
    3.
    发明授权
    Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof 有权
    取代的杂双环化合物，组合物及其药用应用

    公开(公告)号：US09233983B2

    公开(公告)日：2016-01-12

    申请号：US14509793

    申请日：2014-10-08

    申请人： ADVINUS THERAPEUTICS LIMITED

    发明人： Mahesh Thakkar ,  Summon Koul ,  Debnath Bhuniya ,  Kasim Mookhtiar ,  Santosh Kurhade ,  Yogesh Munot ,  Tanaji Mengawade ,  Bheemashankar A. Kulkarni

    IPC分类号： C07D403/04 ,  C07D413/14 ,  C07D519/00 ,  C07D403/14 ,  A61K45/06 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/553 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

    摘要： The present disclosure provides hetero-bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.

    摘要翻译： 本公开提供式（I）的异双环化合物，其互变异构体，多晶型物，立体异构体，前药，溶剂合物，水合物，N-氧化物，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 这是由Bruton的酪氨酸激酶（Btk）活性介导的。本公开还涉及式（I）化合物的制备方法。 这些化合物可用于治疗，预防，预防，治疗或辅助治疗与抑制Bruton酪氨酸激酶（Btk）相关的所有医学病症，如炎性和/或自身免疫性疾病，细胞增殖，类风湿性关节炎，牛皮癣，牛皮癣 关节炎，移植排斥反应，移植物抗宿主病，多发性硬化，炎性肠病，过敏性疾病，哮喘，1型糖尿病，重症肌无力，造血功能障碍，B细胞恶性肿瘤，系统性红斑狼疮，红斑狼疮或其他疾病。

    FUSED TRICYCLIC COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONIST
    4.
    发明申请
    FUSED TRICYCLIC COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONIST 有权
    作为腺苷受体拮抗剂的融合三聚体化合物

    公开(公告)号：US20130252885A1

    公开(公告)日：2013-09-26

    申请号：US13825665

    申请日：2011-09-22

    申请人： Barawkar Dinesh ,  Basu Sujay ,  Ramdas Vidya ,  Naykodi Minakshi ,  Patel Meena ,  Shejul Yogesh ,  Thorat Sachin ,  Panmand Anil

    发明人： Barawkar Dinesh ,  Basu Sujay ,  Ramdas Vidya ,  Naykodi Minakshi ,  Patel Meena ,  Shejul Yogesh ,  Thorat Sachin ,  Panmand Anil

    IPC分类号： C07D487/14 ,  A61K31/5377 ,  A61K31/519 ,  C07D519/00 ,  A61K45/06

    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。

    Bicyclic compounds, compositions and medicinal applications thereof
    5.
    发明授权
    Bicyclic compounds, compositions and medicinal applications thereof 有权

    公开(公告)号：US10435402B2

    公开(公告)日：2019-10-08

    申请号：US15541875

    申请日：2016-01-08

    申请人： Advinus Therapeutics Limited

    发明人： Partha Mukhopadhyay ,  Yogesh Munot ,  Nadim Shaikh ,  Bheemashankar A. Kulkarni ,  Kasim Mookhtiar

    IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/437

    摘要： Substituted bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts and pharmaceutical compositions containing them are disclosed, as well as processes for preparing and using the compounds. These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of retinoic acid-related orphan receptor gamma (RORy). Representative conditions include inflammatory and/or autoimmune disorder, rheumatoid arthritis, psoriasis, psoriatic arthritis, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, COPD, cancer, cell proliferation, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, systemic lupus, crythematosus or other disorders.

    Substituted fused tricyclic compounds, compositions and medicinal applications thereof
    7.
    发明授权
    Substituted fused tricyclic compounds, compositions and medicinal applications thereof 有权
    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。

    Fused tricyclic compounds as adenosine receptor antagonist
    9.
    发明授权
    Fused tricyclic compounds as adenosine receptor antagonist 有权
    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。