Benzoyl-phenyl-piperidine derivatives
    2.
    发明授权
    Benzoyl-phenyl-piperidine derivatives 失效
    苯甲酰基 - 苯基 - 哌啶衍生物

    公开(公告)号:US4528294A

    公开(公告)日:1985-07-09

    申请号:US391915

    申请日:1982-06-24

    摘要: The present invention relates to new benzoyl-phenyl-piperidine derivatives selected from the group consisting of:(i) 2-piperidinobenzophenones of the general formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3, which are identical or different, each represent an atom of hydrogen, a hydroxy group, CF.sub.3, a halogen, a lower alkyl group or a lower alkoxy group;R.sub.4 represents an atom of hydrogen, a halogen, an NO.sub.2 group, an NR'R" group [where R' and R", which are identical or different, represent an atom of hydrogen, a lower alkyl group or a CO.sub.2 R group (where R represents a lower alkyl group or a benzyl group)];R.sub.5 and R.sub.6, which are identical or different, each represent an atom of hydrogen, a C.sub.1 -C.sub.4 -alkyl group, an OH group, a phenyl group or a benzyl group; and(ii) acid addition salts thereof.The invention also relates to the method for preparing these new derivatives and to their use in therapeutics, particularly as immunostimulant and immunoadjuvant agents.

    摘要翻译: 本发明涉及选自以下的新的苯甲酰基 - 苯基 - 哌啶衍生物:(i)具有以下通式的2-哌啶二苯甲酮:其中:R1,R2和R3相同或不同 各自表示氢原子,羟基,CF 3,卤素,低级烷基或低级烷氧基; R 4表示氢原子,卤素,NO 2基,NR'R“基[其中R'和R”相同或不同,表示氢原子,低级烷基或CO 2 R基团 (其中R表示低级烷基或苄基)]; R5,R6相同或不同,分别表示氢原子,C1-C4烷基,OH基,苯基或苄基。 和(ii)其酸加成盐。 本发明还涉及制备这些新衍生物及其在治疗学中的用途的方法,特别是作为免疫刺激剂和免疫佐剂。

    Asymmetrical ester derivatives of 1,4-dihydrophyridine-3,5-dicarboxylic
acid
    3.
    发明授权
    Asymmetrical ester derivatives of 1,4-dihydrophyridine-3,5-dicarboxylic acid 失效
    1,4-二氢吡啶-3,5-二羧酸的不对称酯衍生物

    公开(公告)号:US4806544A

    公开(公告)日:1989-02-21

    申请号:US27262

    申请日:1987-03-18

    CPC分类号: C07D491/10 C07D211/00

    摘要: The present invention relates to novel asymmetrical esters derived from 1,4-dihydrophyridine-3,5-dicarboxylic acid, of the formula: ##STR1## in which: R.sub.1 represents a C.sub.1 -C.sub.4 alkyl group, R.sub.2 represents a C.sub.1 -C.sub.4 alkyl group, a benzyl group, a benzoyl group or a phenyl group optionally substituted by one or more C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, cyano, nitro, hydroxyl or trifluoromethyl groups or by one or more halogen atoms, and R.sub.3 and R.sub.4, which are identical or different, each represent the hydrogen atom, a nitro group or a chlorine atom, their optical isomers and diastereoisomers and also the corresponding addition salts.These novel esters are useful in therapy, especially as antihypertensives.

    摘要翻译: 本发明涉及衍生自1,4-二氢吡啶-3,5-二羧酸的新型不对称酯,其具有下式:其中:R1表示C1-C4烷基,R2表示C1- C4烷基,苄基,苯甲酰基或任选被一个或多个C 1 -C 4烷氧基,C 1 -C 4烷基,氰基,硝基,羟基或三氟甲基取代或被一个或多个卤素原子取代的苯基, R 4相同或不同,各自表示氢原子,硝基或氯原子,它们的光学异构体和非对映异构体以及相应的加成盐。 这些新型酯可用于治疗,特别是抗高血压药。

    PROCESS FOR THE SYNTHESIS OF 2-AMINOTHIAZOLE COMPOUNDS AS KINASE INHIBITORS
    5.
    发明申请
    PROCESS FOR THE SYNTHESIS OF 2-AMINOTHIAZOLE COMPOUNDS AS KINASE INHIBITORS 有权
    合成2-氨基噻唑化合物作为激酶抑制剂的方法

    公开(公告)号:US20100121063A1

    公开(公告)日:2010-05-13

    申请号:US12526827

    申请日:2008-02-13

    IPC分类号: C07D417/14

    CPC分类号: C07D417/04

    摘要: The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula (1) which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or different, represent each a hydrogen, halogen atom, an alkyl, an alkoxy, a trifluoromethyl, an amino, an alkylamino, a dialkylamino, a solubilising group; m is 0-5 and n is 0-4; the group R3 represents an aryl or an heteroaryl group as described in claims herein.

    摘要翻译: 本发明涉及一种制备具有式(1)的药物化合物的工业方法,其可用作某些酪氨酸激酶抑制剂,更特别地涉及c-kit和bcr-abl抑制剂。 R1和R2相同或不同,各自表示氢,卤素原子,烷基,烷氧基,三氟甲基,氨基,烷基氨基,二烷基氨基,增溶基团; m为0-5,n为0-4; 基团R 3表示如权利要求书中所述的芳基或杂芳基。