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    • 2. 发明授权
    • Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity
    • 具有CXCR3拮抗活性的杂环取代的吡啶化合物
    • US08017616B2
    • 2011-09-13
    • US12642931
    • 2009-12-21
    • Stuart B. RosenblumJoseph A. KozlowskiNeng-Yang ShihBrian F. McGuinnessDouglas W. Hobbs
    • Stuart B. RosenblumJoseph A. KozlowskiNeng-Yang ShihBrian F. McGuinnessDouglas W. Hobbs
    • A61K31/496C07D413/14
    • C07D401/14C07D413/14
    • 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 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, xenograft 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,疗效治疗,某些疾病和疾病如炎性疾病的预防性治疗(非限制性实例,牛皮癣),自身免疫性疾病(非限制性的 例如,类风湿性关节炎,多发性硬化症),移植排斥反应(非限制性实例包括,同种异体移植排斥反应,异种移植物排斥),感染性疾病(例如结核性麻风病),固定药物爆发,皮肤迟发型超敏反应 应答,眼部炎症,I型糖尿病,病毒性脑膜炎和使用式1的化合物的肿瘤。
    • 3. 发明申请
    • HETEROCYCLIC SUBSTITUTED PIPERAZINE COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY
    • 具有CXCR3拮抗剂活性的杂环取代的哌嗪化合物
    • US20080058343A1
    • 2008-03-06
    • US11776901
    • 2007-07-12
    • Stuart RosenblumJoseph KozlowskiNeng-Yang ShihBrian McGuinnessDouglas Hobbs
    • Stuart RosenblumJoseph KozlowskiNeng-Yang ShihBrian McGuinnessDouglas Hobbs
    • A61K31/497A61P25/00C07D401/02
    • 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 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,治疗性治疗,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(非限制性实例包括类风湿性关节炎,多发性硬化症),移植物排斥(非限制性实例,包括同种异体移植物排斥,移植排斥),感染性疾病(例如,结节性麻风病 ),固定药物喷发,皮肤迟发型超敏反应,眼部炎症,I型糖尿病,病毒性脑膜炎和使用组合物的肿瘤 和式1。