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    • 3. 发明申请
    • NEW HETEROCYCLIC COMPOUNDS
    • 新的杂环化合物
    • WO2008110891A2
    • 2008-09-18
    • PCT/IB2008/000536
    • 2008-03-07
    • ORCHID RESEARCH LABORATORIES LIMITED,SHARMA, Ganapavarapu, Veera, RaghavaREDDY, Gaddam, OmRAJAGOPAL, SriramRAMACHANDRAN, UmaNARAYANAN, SukunathPICHIKA, NagalakshmiNEMMARA VISWANATHAN, VenkateshANDIAPPAN, LavanyaTHIRUNAVUKKARASU, Saravanan
    • SHARMA, Ganapavarapu, Veera, RaghavaREDDY, Gaddam, OmRAJAGOPAL, SriramRAMACHANDRAN, UmaNARAYANAN, SukunathPICHIKA, NagalakshmiNEMMARA VISWANATHAN, VenkateshANDIAPPAN, LavanyaTHIRUNAVUKKARASU, Saravanan
    • C07D401/12
    • C07D239/24C07D413/14
    • Provided herein are heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, wherein R 1 , R 2 , R 3 , R 4 and R 5 are as described herein. Further described herein in particular are heterocyclic compounds of the formula (I) for treating various diseases and disorders by administering in a patient one or more TNF-α, Thromboxane synthase, 5-LOX, and PDE4 inhibitors. In particular described herein are methods for treating immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; ischemic heart disease; atherosclerosis; cancer; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; cachexia; asthma; bone resorption diseases; ischemia reperfusion injury; brain trauma; multiple sclerosis; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection and diseases mediated by HIV-1; HIV-2; HIV-3; cytomegalovirus (CMV); influenza; adenovirus; the herpes viruses (including HSV-1, HSV-2) and herpes zoster viruses in a mammal comprising administering an effective amount of a compound of formula (I).
    • 本文提供了通式(I)的杂环化合物,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,药学上可接受的盐和组合物,其代谢物和前药,其中R 1, R 2,R 3,R 4和R 5如本文所述。 本文进一步描述的是通过在患者中给予一种或多种TNF-α,血栓烷合成酶,5-LOX和PDE4抑制剂来治疗各种疾病和病症的式(I)的杂环化合物。 本文特别描述的是用于治疗免疫疾病,炎症,疼痛障碍,类风湿性关节炎的方法; 骨质疏松症; 多发性骨髓瘤 uveititis; 急性和慢性粒细胞白血病; 缺血性心脏病; 动脉粥样硬化; 癌症; 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; 成人呼吸窘迫综合征(ARDS); 银屑病; 克罗恩病; 过敏性鼻炎; 溃疡性结肠炎 过敏性反应; 接触性皮炎; 肌肉退化; 恶病质; 哮喘; 骨吸收疾病; 缺血再灌注损伤; 脑外伤; 多发性硬化症 败血症; 败血性休克 中毒性休克综合征 由于HIV-1介导的感染和疾病引起的发热和肌痛; HIV-2; HIV-3; 巨细胞病毒(CMV); 流感; 腺病毒; 哺乳动物中的疱疹病毒(包括HSV-1,HSV-2)和带状疱疹病毒,包括施用有效量的式(I)化合物。