公开(公告)号：US20100329998A1

公开(公告)日：2010-12-30

申请号：US12863796

申请日：2009-01-30

申请人： Visweswara Akella Satya Surya Srinivas ,  Ravikumar Tadiparthi ,  Ganapavarapu Veera Raghava Sharma ,  Thirunavukkarasu Sappanimuthu ,  Durairaj Peter Bhakiaraj ,  Virendra Kachhadia ,  Kilambi Narasimhan ,  Sathya Narayana Thara ,  Sriram Rajagopal ,  Om Gaddam ,  Nishikanth Reddy Gaddam ,  Sukunath Narayanan ,  Venkatesan Parameswaran ,  Venkatesan Janarthanam ,  Maruthikumar Narayanam ,  Sathyanarayana Gadde ,  Uma Ramachandran ,  Gopalan Balasubramanian ,  Narayanan Surendran ,  Shridhar Narayanan ,  Lolaknath Santosh Vishwakarma ,  Sanjeev Saxena

发明人： Visweswara Akella Satya Surya Srinivas ,  Ravikumar Tadiparthi ,  Ganapavarapu Veera Raghava Sharma ,  Thirunavukkarasu Sappanimuthu ,  Durairaj Peter Bhakiaraj ,  Virendra Kachhadia ,  Kilambi Narasimhan ,  Sathya Narayana Thara ,  Sriram Rajagopal ,  Om Gaddam ,  Nishikanth Reddy Gaddam ,  Sukunath Narayanan ,  Venkatesan Parameswaran ,  Venkatesan Janarthanam ,  Maruthikumar Narayanam ,  Sathyanarayana Gadde ,  Uma Ramachandran ,  Gopalan Balasubramanian ,  Narayanan Surendran ,  Shridhar Narayanan ,  Lolaknath Santosh Vishwakarma ,  Sanjeev Saxena

IPC分类号： A61K9/12 ,  A61K31/505 ,  C07D239/02 ,  C07D401/14 ,  A61K31/506 ,  A61K31/497 ,  C07D417/04 ,  C07D403/04 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/54 ,  A61P37/00 ,  A61P29/00 ,  A61P19/02 ,  A61P19/10 ,  A61P35/02 ,  A61P35/04 ,  A61P9/00 ,  A61P1/00 ,  A61P11/00

CPC分类号： C07D239/42 ,  A61K31/5377 ,  C07D265/28 ,  C07D401/04

摘要： Described are novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are useful in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever. More particularly these compounds are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases.

摘要翻译： 描述了通式（I）的新型杂环化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐，药物组合物，代谢物和前药。 这些化合物可用于治疗免疫疾病，炎症，疼痛障碍，类风湿性关节炎; 骨质疏松症 多发性骨髓瘤 葡萄膜炎 急性和慢性粒细胞白血病; 动脉粥样硬化 癌症; 恶病质 缺血诱导的细胞损伤; 胰腺β细胞破坏; 骨关节炎 类风湿性脊柱炎; 痛风性关节炎 炎症性肠病; ARDS; 银屑病; 克罗恩病; 过敏性鼻炎; 溃疡性结肠炎 过敏反应 接触性皮炎; 肌肉退化; 哮喘; COPD; 骨吸收疾病; 多发性硬化症 败血症 败血性休克 中毒性休克综合征和发烧。 更特别地，这些化合物可用作PDE4抑制剂，并且可用于治疗PDE4介导的疾病。

公开(公告)号：US08420653B2

公开(公告)日：2013-04-16

申请号：US12863796

申请日：2009-01-30

申请人： Visweswara Akella Satya Surya Srinivas ,  Ravikumar Tadiparthi ,  Ganapavarapu Veera Raghava Sharma ,  Thirunavukkarasu Sappanimuthu ,  Durairaj Peter Bhakiaraj ,  Virendra Kachhadia ,  Kilambi Narasimhan ,  Sathya Narayana Thara ,  Sriram Rajagopal ,  Sukunath Narayanan ,  Venkatesan Parameswaran ,  Venkatesan Janarthanam ,  Maruthikumar Narayanam ,  Sathyanarayana Gadde ,  Uma Ramachandran ,  Gopalan Balasubramanian ,  Narayanan Surendran ,  Shridhar Narayanan ,  Lolaknath Santosh Vishwakarma ,  Sanjeev Saxena ,  Nishikanth Reddy Gaddam

发明人： Visweswara Akella Satya Surya Srinivas ,  Ravikumar Tadiparthi ,  Ganapavarapu Veera Raghava Sharma ,  Thirunavukkarasu Sappanimuthu ,  Durairaj Peter Bhakiaraj ,  Virendra Kachhadia ,  Kilambi Narasimhan ,  Sathya Narayana Thara ,  Sriram Rajagopal ,  Om Reddy Gaddam ,  Sukunath Narayanan ,  Venkatesan Parameswaran ,  Venkatesan Janarthanam ,  Maruthikumar Narayanam ,  Sathyanarayana Gadde ,  Uma Ramachandran ,  Gopalan Balasubramanian ,  Narayanan Surendran ,  Shridhar Narayanan ,  Lolaknath Santosh Vishwakarma ,  Sanjeev Saxena

IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

CPC分类号： C07D239/42 ,  A61K31/5377 ,  C07D265/28 ,  C07D401/04

摘要： Described are novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are useful in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever. More particularly these compounds are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases.

摘要翻译： 描述了通式（I）的新型杂环化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐，药物组合物，代谢物和前药。 这些化合物可用于治疗免疫疾病，炎症，疼痛障碍，类风湿性关节炎; 骨质疏松症 多发性骨髓瘤 葡萄膜炎 急性和慢性粒细胞白血病; 动脉粥样硬化 癌症; 恶病质 缺血诱导的细胞损伤; 胰腺β细胞破坏; 骨关节炎 类风湿性脊柱炎; 痛风性关节炎 炎症性肠病; ARDS; 银屑病; 克罗恩病; 过敏性鼻炎; 溃疡性结肠炎 过敏反应 接触性皮炎; 肌肉退化; 哮喘; COPD; 骨吸收疾病; 多发性硬化症 败血症 败血性休克 中毒性休克综合征和发烧。 更特别地，这些化合物可用作PDE4抑制剂，并且可用于治疗PDE4介导的疾病。

公开(公告)号：US20140187594A1

公开(公告)日：2014-07-03

申请号：US13809604

申请日：2011-03-28

申请人： Shridhar Narayanan ,  Jeyamurugan Mookkan ,  Jayanarayan Kulathingal ,  Narayanan Surendran ,  Gajendra Singh ,  Gopalan Balasubramanian

发明人： Shridhar Narayanan ,  Jeyamurugan Mookkan ,  Jayanarayan Kulathingal ,  Narayanan Surendran ,  Gajendra Singh ,  Gopalan Balasubramanian

IPC分类号： A61K31/426

CPC分类号： A61K31/426

摘要： Described herein are compounds of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, for use in treating liver diseases such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH), and other fibrotic diseases of the liver; diabetic complications such as macro (ischemic heart disease, cerebrovascular disease and peripheral vascular disease) and micro (cataract, retinopathy nephropathy neuropathy, maculopathy and glaucoma) vascular complication; and cardiovascular diseases such as atherosclerosis, restenosis, hypertension, vasospasm, and cardiac hypertrophy; and lung disorders and lung fibrosis.

摘要翻译： 本文描述了用于治疗肝脏疾病如非酒精性脂肪肝的式（I）化合物，其衍生物，类似物，互变异构体形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐和组合物，其代谢物和前药 疾病（NAFLD）和非酒精性脂肪性肝炎（NASH）等肝纤维化疾病; 糖尿病并发症如宏观（缺血性心脏病，脑血管疾病和外周血管疾病）和微（白内障，视网膜病变肾病，神经病变，黄斑病变和青光眼）血管并发症; 心血管疾病如动脉粥样硬化，再狭窄，高血压，血管痉挛和心脏肥大; 和肺部疾病和肺纤维化。