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    • 7. 发明申请
    • HETEROCYCLIC COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY
    • 具有CXCR3拮抗剂活性的杂环化合物
    • US20120157466A1
    • 2012-06-21
    • US12519970
    • 2007-12-20
    • Qingbei ZengStuart B. RosenblumJoseph A. KozlowskiNeng-Yang ShihBrian F. McGuinnessDouglas W. Hobbs
    • Qingbei ZengStuart B. RosenblumJoseph A. KozlowskiNeng-Yang ShihBrian F. McGuinnessDouglas W. Hobbs
    • A61K31/519C07D401/14C07D473/32A61K31/52A61K31/496A61P29/00A61P37/00C07D471/04A61K31/506
    • C07D401/14
    • The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1 or Formula 5: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non limiting example(s) include, psoriasis), autoimmune diseases (non limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
    • 本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐,溶剂合物或酯的化合物或对映异构体,立体异构体,旋转异构体,互变异构体或前药,所述化合物具有式1所示的一般结构 或式5:或其药学上可接受的盐,溶剂合物或酯。 还公开了治疗趋化因子介导的疾病的方法,例如姑息治疗,治疗疗法,某些疾病和疾病如炎性疾病的预防性治疗(非限制性实例,包括牛皮癣),自身免疫疾病(非限制性实例( 传染性疾病(例如结核性麻风病),固定药物爆发,皮肤迟发型超敏反应,眼部炎症反应(例如,类风湿性关节炎,多发性硬化症),移植物排斥反应(非限制性实例包括同种异体移植物排斥反应, ,I型糖尿病,病毒性脑膜炎和使用式1的化合物的肿瘤。