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14 条记录 (耗时 0.041 秒)

    Novel compounds as histone deacetylase inhibitors
    2.
    发明申请
    Novel compounds as histone deacetylase inhibitors 审中-公开
    新型化合物作为组蛋白脱乙酰酶抑制剂

    公开(公告)号：US20050176686A1

    公开(公告)日：2005-08-11

    申请号：US10624571

    申请日：2003-07-23

    申请人： Alexander Maurer ,  Sascha Hoevelmann ,  Elke Martin ,  Bernd Hentsch ,  Michael Gassen ,  Juergen Kraus ,  Rolf Krauss ,  Adam-Spencer Vincek

    发明人： Alexander Maurer ,  Sascha Hoevelmann ,  Elke Martin ,  Bernd Hentsch ,  Michael Gassen ,  Juergen Kraus ,  Rolf Krauss ,  Adam-Spencer Vincek

    IPC分类号： A61K31/19 ,  A61K31/66 ,  C07C259/04

    CPC分类号： C07C259/04 ,  C07C2601/08 ,  C07C2601/14

    摘要： The present invention is directed to compounds of the general formula (I) or pharmaceutical acceptable salts or physiologically functional derivatives thereof wherein: n is a non-aromatic ring system containing two to seven carbon atoms, wherein the ring system can contain one ore two double bonds; X is C, CH or CH2; Y is selected from C, CH, CH2, S, NR, CH2-CH2, H2C—CH, HC—CH2, C—CH2, H2C—C, or C—C; one or more of the hydrogen atoms can optionally be substituted by one or more substituents R′; each of the dotted lines means a single, a double or triple bond with the exclusion of a combination of a triple with triple bond and a double with a triple bond; R′ is independently H, —CN, alkyl, cycloalkyl, aminoalkyl, alkylamino, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, hydroxyalkylamino, halogene, haloalkyl, haloalkyloxy; R is H, an alkyl or cycloalkyl group; Z is CH, C, or P; p is 0 or 1.

    摘要翻译： 本发明涉及通式（I）的化合物或其药学上可接受的盐或生理功能衍生物，其中：n是含有2至7个碳原子的非芳族环系统，其中所述环体系可以包含一个二价双 债券 X是C，CH或CH 2; Y选自C，CH，CH 2，S，NR，CH 2 -CH 2，H 2， C-CH，HC-CH 2，C-CH 2，H 2 CC或CC; 一个或多个氢原子可以任选被一个或多个取代基R'取代; 每个虚线意味着单，双或三键，排除三元组与三键的组合和具有三键的双键; R'独立地是H，-CN，烷基，环烷基，氨基烷基，烷基氨基，烷氧基，-OH，-SH，烷硫基，羟基烷基，羟烷基氨基，卤素基，卤代烷基，卤代烷氧基。 R是H，烷基或环烷基; Z是CH，C或P; p为0或1。

    Pyrrole derivatives as phosphodiesterase VII inhibitors
    3.
    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

    申请人： Hans-Michael Eggenweiler ,  Rochus Jonas ,  Michael Wolf ,  Michael Gassen ,  Thomas Welge

    发明人： Hans-Michael Eggenweiler ,  Rochus Jonas ,  Michael Wolf ,  Michael Gassen ,  Thomas Welge

    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。

    Compounds as histone deacetylase inhibitors
    4.
    发明授权
    Compounds as histone deacetylase inhibitors 失效
    化合物作为组蛋白脱乙酰酶抑制剂

    公开(公告)号：US08227516B2

    公开(公告)日：2012-07-24

    申请号：US11778297

    申请日：2007-07-16

    申请人： Alexander B. Maurer ,  Sascha Hoevelmann ,  Elke Martin ,  Bernd Hentsch ,  Michael Gassen ,  Juergen Kraus ,  Rolf Krauss ,  Adam-Spencer Vincek

    发明人： Alexander B. Maurer ,  Sascha Hoevelmann ,  Elke Martin ,  Bernd Hentsch ,  Michael Gassen ,  Juergen Kraus ,  Rolf Krauss ,  Adam-Spencer Vincek

    IPC分类号： A61K31/16

    CPC分类号： C07C259/04 ,  C07C2601/08 ,  C07C2601/14

    摘要： The present invention relates to compounds as inhibitors of enzymes having histone deacetylase activity, to the processes for the preparation of those compounds, and to their use for the treatment of diseases which are associated with hypoacetylation of histones and/or other molecules, or in which induction of hyperacetylation has a beneficial effect for example by inhibition of proliferation and/or induction of differentiation and/or induction of apoptosis in transformed cells, such as cancer. Furthermore, the compounds are useful for the treatment of other proliferative diseases, for therapy or prophylaxis of conditions associated with abnormal gene expression.

    摘要翻译： 本发明涉及作为具有组蛋白脱乙酰酶活性的酶的抑制剂的化合物，这些化合物的制备方法及其用于治疗与组蛋白和/或其他分子的低乙酰化相关的疾病的用途，或其中 超乙酰化的诱导例如通过抑制转化细胞（例如癌症）的增殖和/或诱导分化和/或诱导细胞凋亡具有有益的作用。 此外，该化合物可用于治疗其他增殖性疾病，用于治疗或预防与异常基因表达相关的病症。

    Isoxazole derivatives to be used as phosphodiesterase VII inhibitors
    8.
    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

    申请人： Hans-Michael Eggenweiler ,  Rochus Jonas ,  Michael Wolf ,  Michael Gassen ,  Thomas Welge

    发明人： Hans-Michael Eggenweiler ,  Rochus Jonas ,  Michael Wolf ,  Michael Gassen ,  Thomas Welge

    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。

    Imidazole derivatives as phosphodiesterase VII inhibitors
    10.
    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

    申请人： Hans-Michael Eggenweiler ,  Rochus Jonas ,  Michael Wolf ,  Michael Gassen ,  Oliver Pöschke

    发明人： Hans-Michael Eggenweiler ,  Rochus Jonas ,  Michael Wolf ,  Michael Gassen ,  Oliver Pöschke

    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。