Imidazole derivatives as phosphodiesterase VII inhibitors
    5.
    发明授权
    Imidazole derivatives as phosphodiesterase VII inhibitors 失效
    咪唑衍生物作为磷酸二酯酶VII抑制剂

    公开(公告)号:US07491742B2

    公开(公告)日:2009-02-17

    申请号:US10750878

    申请日:2004-01-05

    IPC分类号: A61K31/415

    CPC分类号: C07D491/04 C07D495/04

    摘要: Imidazole derivatives of the formula I in which R1 is H, A, benzyl, indan-5-yl, 1,2,3,4-tetrahydronaphthalen-5-yl, dibenzothien-2-yl, or phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, A-CO—NH, benzyloxy, alkoxy, COOH or COOA, R2 is H or A, X is O or S, Hal is F, Cl, Br or I, A is alkyl with 1 to 6 C atoms, and the physiologically acceptable salts and/or solvates thereof as phosphodiesterase VII inhibitors and the use thereof for producing a pharmaceutical.

    摘要翻译: 式I的咪唑衍生物,其中R 1是H,A,苄基,茚满-5-基,1,2,3,4-四氢萘-5-基,二苯并噻吩-2-基或未取代或单 - ,Hal,A,A-CO-NH,苄氧基,烷氧基,COOH或COOA二取代或三取代,R 2为H或A,X为O或S,Hal为F,Cl,Br或I, 1至6个C原子,以及其作为磷酸二酯酶VII抑制剂的生理学上可接受的盐和/或溶剂合物及其用于制备药物的用途。

    Benzoylpyridazines
    6.
    发明授权
    Benzoylpyridazines 失效
    苯甲酰哒嗪

    公开(公告)号:US06376493B1

    公开(公告)日:2002-04-23

    申请号:US09830957

    申请日:2001-05-03

    IPC分类号: A61K3150

    CPC分类号: C07D237/04

    摘要: A group of compounds of, the preparation of, and the methods of use of benzoylpyridazine derivatives and the physiologically acceptable salts and solvates thereof, which have valuable pharmacological properties while well tolerated. They selectively inhibit phosphodiesterase IV with an intracellular increase in the CAMP level, and have an inhibitory effect on the formation of tumor necrosis factor.

    摘要翻译: 苯甲酰基哒嗪衍生物的一组化合物,其制备方法和使用方法及其生理上可接受的盐和溶剂合物,其具有有价值的药理学性质,同时具有良好的耐受性。 它们选择性抑制磷酸二酯酶IV,细胞内CAMP水平升高,对肿瘤坏死因子的形成具有抑制作用。

    Arylalkylpyridazinones
    7.
    发明授权
    Arylalkylpyridazinones 失效
    芳基哒嗪酮

    公开(公告)号:US06399611B1

    公开(公告)日:2002-06-04

    申请号:US08634830

    申请日:1996-04-19

    IPC分类号: C07D23704

    CPC分类号: C07D237/04

    摘要: Aralkylpyridazinone derivatives of the formula I and their physiologically acceptable salts in which R1, R2, R3, R4, R5 and Q have the meanings indicated in claim 1, show inhibition of phosphodiesterase IV and can be employed for the treatment of inflammatory processes and of allergies, asthma and autoimmune disorders.

    摘要翻译: 式I的芳烷基哒嗪酮衍生物及其生理上可接受的盐,其中R 1,R 2,R 3,R 4,R 5和Q具有权利要求1所示的含义,表示磷酸二酯酶IV的抑制,并且可用于治疗炎症过程和过敏性哮喘 和自身免疫性疾病。

    Isoxazole derivatives to be used as phosphodiesterase VII inhibitors
    9.
    发明授权
    Isoxazole derivatives to be used as phosphodiesterase VII inhibitors 失效
    异恶唑衍生物用作磷酸二酯酶VII抑制剂

    公开(公告)号:US06531498B1

    公开(公告)日:2003-03-11

    申请号:US10129270

    申请日:2002-05-03

    IPC分类号: C07D26106

    CPC分类号: A61K31/42

    摘要: The invention relates to compounds of formula I and to their physiologically acceptable salts and solvates which act as phosphodiesterse VII inhibitors and are thus useful for the treatment of allergic disorders, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin disorders, inflammatory disorders, autoimmune diseases, rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumor growth, tumor metastases, sepsis, memory disturbances, atherosclerosis and AIDS.

    摘要翻译: 本发明涉及式I化合物及其作为磷酸二酯VII抑制剂的生理上可接受的盐和溶剂合物,因此可用于治疗过敏性疾病,哮喘,慢性支气管炎,特应性皮炎,牛皮癣和其他皮肤病,炎症性疾病, 自身免疫疾病,类风湿性关节炎,多发性硬化,克罗恩病,糖尿病或溃疡性结肠炎,骨质疏松症,移植排斥反应,恶病质,肿瘤生长,肿瘤转移,败血症,记忆障碍,动脉粥样硬化和艾滋病。

    Pyrrole derivatives as phosphodiesterase VII inhibitors
    10.
    发明授权
    Pyrrole derivatives as phosphodiesterase VII inhibitors 失效
    吡咯衍生物作为磷酸二酯酶VII抑制剂

    公开(公告)号:US06737436B1

    公开(公告)日:2004-05-18

    申请号:US10129261

    申请日:2002-05-03

    IPC分类号: A61K31402

    CPC分类号: C07D207/34

    摘要: Compounds of the formula I in which R1 and R2, independently of one another, each denote H, A, OA, SA or HaI, R3 denotes H or A, R4 denotes A or NH2, R5 denotes H, NH2, NHA or NA2, A denotes alkyl having 1 to 10 carbon atoms, alkenyl, cycloalkyl or alkylenecycloalkyl, Hal denotes F, Cl, Br or I, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors.

    摘要翻译: R 1和R 2彼此独立的式Iin的化合物各自表示H,A,OA,SA或HaI,R 3表示H或A,R 4表示A或NH 2, R 5表示H,NH 2,NHA或NA 2,A表示具有1至10个碳原子的烷基,烯基,环烷基或亚烷基环烷基,Hal表示F,Cl,Br或I及其生理学上可接受的盐和/或溶剂化物, 磷酸二酯酶VII抑制剂。