NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF
    73.
    发明申请
    NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF 有权
    新型双酚A衍生物作为蛋白酪氨酸激酶抑制剂及其药物用途

    公开(公告)号:US20130172325A1

    公开(公告)日:2013-07-04

    申请号:US13809059

    申请日:2011-07-08

    CPC classification number: C07D487/04 A61K31/5513 A61K45/00

    Abstract: The invention relates to compounds of general formula (I) wherein R1, R2, R3, R4, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immuno-suppression would be desirable for example in organ transplantation.

    Abstract translation: 本发明涉及通式(I)的化合物,其中R 1,R 2,R 3,R 4,m和n如本文所定义,及其药学上可接受的盐,水合物或溶剂合物,其单独使用或与 更多其他药物活性化合物 - 在治疗中,作为用于预防,治疗或改善疾病及其并发症的JAK激酶和蛋白酪氨酸激酶抑制剂,包括例如牛皮癣,特应性皮炎,酒渣鼻,狼疮,多发性硬化,类风湿性关节炎,I型 糖尿病,哮喘,癌症,自身免疫性甲状腺疾病,溃疡性结肠炎,克罗恩病,阿尔茨海默氏病,白血病,眼睛疾病如糖尿病性视网膜病变和黄斑变性以及其他自身免疫性疾病以及免疫抑制在器官移植中是理想的适应症 。

    Pyridyl cyanoguanidine compounds
    78.
    发明授权
    Pyridyl cyanoguanidine compounds 有权
    吡啶氰腈化合物

    公开(公告)号:US07807682B2

    公开(公告)日:2010-10-05

    申请号:US11998575

    申请日:2007-11-30

    CPC classification number: C07D213/89 A61K31/4439 A61K45/06 C07D401/12

    Abstract: Compounds according to formula I wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, 0, C(O), S, S(O), S(0)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, aminoalkyl or straight or branched, saturated or unsaturated C1-4 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl or aminoalkyl; provided that R1 is not attached to the nitrogen-atom in the pyridyl ring; and pharmaceutically acceptable salts, solvates, hydrates, N-oxides and prodrugs thereof are disclosed. The compounds are useful in therapy.

    Abstract translation: 根据式I的化合物,其中R 1表示氢,卤素或一个或多个直链或支链的饱和或不饱和C 1-6烃基,任选被卤素,羟基,氰基,硝基,羧基,烷氧基,烷氧基羰基,烷基羰基,甲酰基,氨基 氨基烷基,氨基羰基,烷基羰基氨基,磺基,氨基磺酰基,烷基磺酰基氨基,羟基磺酰氧基,二氢氧膦基氧基或膦酰基; X代表直链或支链饱和或不饱和的C 1 -C 12烃基,其任选被卤素,羟基,氰基,硝基,羧基,烷氧基,烷氧基羰基,烷基羰基,甲酰基,氨基,氨基烷基,氨基羰基,烷基羰基氨基,磺基,氨基磺酰基,烷基磺酰基氨基 ,羟基磺酰氧基,二羟基磷酰氧基或膦酰基; Y表示0,C(O),S,S(O),S(O)2,C(O)O,NH,C(O)NH,OC(O)或NHC(O) 羟基,氰基,硝基,烷氧基,烷氧基羰基,烷基羰基,甲酰基,氨基烷基或直链或支链,饱和或不饱和的C 1-4烃基,其中Z代表具有5-12个环原子的芳族或非芳族杂环基团 羟基,氰基,硝基,烷氧基,烷氧基羰基,烷基羰基,甲酰基或氨基烷基; 条件是R1不连接在吡啶环中的氮原子上; 及其药学上可接受的盐,溶剂化物,水合物,N-氧化物和前体药物。 这些化合物可用于治疗。

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