公开(公告)号：US20110130403A1

公开(公告)日：2011-06-02

申请号：US12531045

申请日：2008-03-13

申请人： Sonali Rudra ,  Nidhi Gupta ,  Lalit Kumar Baregama ,  Ritu Agarwal ,  Mandadapu Raghuramaiah ,  Vinayak Vasantrao Khairnar ,  Venkata P. Palle ,  Sarala Balachandran ,  Abhijit Ray ,  Sunada G. Dastidar ,  Lalitha Vijaykrishnan

发明人： Sonali Rudra ,  Nidhi Gupta ,  Lalit Kumar Baregama ,  Ritu Agarwal ,  Mandadapu Raghuramaiah ,  Vinayak Vasantrao Khairnar ,  Venkata P. Palle ,  Sarala Balachandran ,  Abhijit Ray ,  Sunada G. Dastidar ,  Lalitha Vijaykrishnan

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61P29/00 ,  A61P37/06 ,  A61P25/00

CPC分类号： C07D471/04

摘要： The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed hereinf having the structure of Formula I: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE t e 4/PDE t e 7 inhibitors are rovided.

摘要翻译： 本发明涉及磷酸二酯酶（PDE）4型，磷酸二酯酶（PDE）7型和双重PDE型4 / PDE型7型抑制剂。 本文公开的具有式I结构的化合物可用于治疗，预防，抑制或抑制CNS疾病，例如多发性硬化; 各种病理状况如影响免疫系统的疾病，包括艾滋病，移植排斥反应，自身免疫性疾病如T细胞相关疾病，例如类风湿性关节炎; 炎性疾病如呼吸道炎症疾病，包括慢性阻塞性肺疾病（COPD），哮喘，支气管炎，过敏性鼻炎，成人呼吸窘迫综合征（ARDS）和其他炎性疾病，包括但不限于银屑病，休克，特应性皮炎，嗜酸性肉芽肿，过敏性 结膜炎，骨关节炎; 胃肠道炎症性疾病如克罗恩病，结肠炎，胰腺炎以及不同类型的癌症，包括白血病; 特别是在人类。 制备所公开的化合物的方法，包含所公开的化合物的药物组合物及其作为PDE 4型，PDE型7和双重PDE 4 / PDE 7抑制剂的用途是有争议的。