SUBSTITUTED CYCLOPENTYL-AZINES AS CASR-ACTIVE COMPOUNDS
    44.
    发明申请
    SUBSTITUTED CYCLOPENTYL-AZINES AS CASR-ACTIVE COMPOUNDS 有权
    取代的环己基作为CASR活性化合物

    公开(公告)号:US20130345194A1

    公开(公告)日:2013-12-26

    申请号:US13977408

    申请日:2012-01-06

    CPC classification number: C07D487/04 A61K31/519 A61K31/5377 A61K45/06

    Abstract: The invention relates to compounds of general Formula (I), Wherein R1, R2, R3, R4, R5, m, n are defined herein, and pharmaceutically acceptable salts, prodrugs, 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 disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.

    Abstract translation: 本发明涉及通式(I)的化合物,其中R1,R2,R3,R4,R5,m,n如本文所定义,及其药学上可接受的盐,前体药物,水合物或溶剂化物,单独使用或组合使用 与治疗中的一种或多种其它药物活性化合物一起作为用于预防,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和适应症,如免疫抑制在器官 移植。

    CALCIUM-SENSING RECEPTOR-ACTIVE COMPOUNDS
    45.
    发明申请
    CALCIUM-SENSING RECEPTOR-ACTIVE COMPOUNDS 审中-公开
    钙敏感受体活性化合物

    公开(公告)号:US20130245084A1

    公开(公告)日:2013-09-19

    申请号:US13989447

    申请日:2011-11-21

    Abstract: Compounds of general formula (I) their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

    Abstract translation: 通式(I)的化合物作为钙受体活性化合物用于预防,治疗或改善与CaSR活性相关的生理障碍或疾病如甲状旁腺功能亢进,包含所述化合物的药物组合物和用于治疗疾病的方法 所述化合物。

    Vitamin d analogues, compositions comprising said analogues and their use
    46.
    发明授权
    Vitamin d analogues, compositions comprising said analogues and their use 有权
    维生素d类似物,包含所述类似物的组合物及其用途

    公开(公告)号:US08455466B2

    公开(公告)日:2013-06-04

    申请号:US10532019

    申请日:2003-10-23

    CPC classification number: C07C401/00

    Abstract: Compounds according to formula I in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6)hydrocarbyl, optionally substituted with one or two hydroxyl group or one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C3-C6)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C1-C3)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.

    Abstract translation: 根据式I的化合物,其中可以相同或不同的式R 1和R 2表示卤素,(C 1 -C 6)烃基,任选被一个或两个羟基或一个或多个氟原子取代,或者与 碳原子,R 1和R 2形成(C 3 -C 6)碳环,R 1和R 2中的一个与R 3一起形成直接键,从而构成三键,或者R 1和R 2表示 氢; 当不与R 1和R 2中的一个直接键合时,R 3表示氢或(C 1 -C 3)烃基; X表示(E) - 亚乙基,(Z) - 亚乙基,亚乙炔基或键; Y和Z独立地表示氢或甲基; 并且其前体药物和立体异构形式与其在治疗中的用途一起提供,以及它们在制备药物中的用途。

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