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公开(公告)号:US09127003B2
公开(公告)日:2015-09-08
申请号:US14416937
申请日:2012-07-26
申请人: Stephen John Atkinson , Michael David Barker , Matthew Campbell , Hawa Diallo , Clement Douault , Neil Stuart Garton , John Liddle , Robert John Sheppard , Ann Louise Walker , Christopher Wellaway , David Matthew Wilson
发明人: Stephen John Atkinson , Michael David Barker , Matthew Campbell , Hawa Diallo , Clement Douault , Neil Stuart Garton , John Liddle , Robert John Sheppard , Ann Louise Walker , Christopher Wellaway , David Matthew Wilson
IPC分类号: C07D471/04 , A61K31/407 , A61K31/4184
CPC分类号: A61K31/4545 , A61K31/407 , A61K31/4184 , C07D471/04
摘要: Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6 alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
摘要翻译: 式(I)的化合物:其中; R1是氢或C1-6烷基; R 2是氢,C 1-6烷基,全卤代甲基C 0-5烷基-O-或C 1-6烷氧基; R3是氢,C1-6烷基或C1-6烷氧基C1-6烷基; R 4是氢,C 1-6烷基,全卤代甲基C 1-6烷基; 或未取代的C 3-6环烷基C 1-6烷基; A为C-R5或N; B为C-R6或N; D为C-R7或N; 条件是A,B和D中的至少一个为N; R5是氢或C1-6烷基; R6是氢或C1-6烷基; R7是氢,C1-6烷基,C1-6烷氧基或羟基; R8是氢或C1-6烷基,条件是R4和R8中的一个是氢; R9是氢或羟基; R 10是氢或C 1-6烷基; 其盐是PAD4抑制剂,并且可用于治疗各种疾病,例如类风湿性关节炎,血管炎,系统性红斑狼疮,溃疡性结肠炎,癌症,囊性纤维化,哮喘,皮肤红斑狼疮和牛皮癣。
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公开(公告)号:US20140005188A1
公开(公告)日:2014-01-02
申请号:US14004375
申请日:2012-03-08
申请人: Francis Louis Atkinson , Stephen John Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander G. Preston , Tracy Jane Shipley , David Matthew Wilson , Robert J. Watson
发明人: Francis Louis Atkinson , Stephen John Atkinson , Michael David Barker , Clement Douault , Neil Stuart Garton , John Liddle , Vipulkumar Kantibhai Patel , Alexander G. Preston , Tracy Jane Shipley , David Matthew Wilson , Robert J. Watson
IPC分类号: C07D471/04 , C07D487/04
CPC分类号: C07D471/04 , C07D487/04 , C07D519/00
摘要: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.
摘要翻译: 式(I)的化合物或其盐; 其是脾脏酪氨酸激酶(Syk)的抑制剂,因此潜在地用于治疗由肥大细胞,巨噬细胞和B细胞的不适当活化引起的疾病以及相关的炎症反应和组织损伤,例如炎性疾病和/或过敏性疾病 ,以及癌症治疗,特别是血红素恶性肿瘤和自身免疫病症。
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