公开(公告)号：US20170362225A1

公开(公告)日：2017-12-21

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

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

摘要： The present disclosure relates to a class of 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. 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 retinoic acid-related orphan receptor gamma (RORγ) such as 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, erythematosus or other disorders.

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。

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.

公开(公告)号：US20150064196A1

公开(公告)日：2015-03-05

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： C07D519/00 ,  C07D487/04 ,  A61K31/5377 ,  A61K31/553 ,  A61K31/519 ,  C07D471/04 ,  A61K45/06

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，多发性硬化症，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。