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    Arylvinylazacycloalkane compounds and methods of preparation and use thereof
    6.
    发明授权
    Arylvinylazacycloalkane compounds and methods of preparation and use thereof 有权
    芳基乙烯基氮杂环烷烃化合物及其制备和使用方法

    公开(公告)号：US08633222B2

    公开(公告)日：2014-01-21

    申请号：US13033719

    申请日：2011-02-24

    申请人： Jeffrey Daniel Schmitt ,  Gary Maurice Dull ,  Arielle Genevois-Borella ,  Marc Capet ,  Michel Cheve ,  Craig Harrison Miller

    发明人： Jeffrey Daniel Schmitt ,  Gary Maurice Dull ,  Arielle Genevois-Borella ,  Marc Capet ,  Michel Cheve ,  Craig Harrison Miller

    IPC分类号： A61K31/351 ,  C07D401/02

    CPC分类号： A61K31/506 ,  C07D405/14

    摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

    摘要翻译： 公开了式（I）的新型乙烯基氮杂环烷化合物。 这些化合物是各种nAChR的配体。 化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。 可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。 化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments
    9.
    发明授权
    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments 失效
    法呢基转移酶抑制剂，它们的制备，含有它们的药物组合物及其在制备药物中的用途

    公开(公告)号：US06218406B1

    公开(公告)日：2001-04-17

    申请号：US09346303

    申请日：1999-07-02

    申请人： Jean-Dominique Bourzat ,  Alain Commerçon ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    发明人： Jean-Dominique Bourzat ,  Alain Commerçon ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    IPC分类号： A61K314439

    CPC分类号： C07D401/12 ,  C07D209/56 ,  C07D209/72 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14

    摘要： Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula —(CH2)m—X1—(CH2)n—Z in which X1=single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH2 radicals to be substituted; Z represents carboxyl, COOR6 (R6=alkyl), CON(R7)(R8) (R7=hydrogen or alkyl and R8=hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR9)2 (R9=hydrogen or alkyl), an —NH—CO—T (T=hydrogen or optionally substituted alkyl) radical, or else—a radical, R1 and R2=hydrogen or halogen or alkyl, alkyloxy, which is optionally substituted, alkylthio, alkyloxycarbonyl or else R1 and R2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R3 and R4=hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxyl or alkyloxycarbonyl, R5=hydrogen, alkyl, alkylthio, X=O or S or —NH—, —CO—, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.

    摘要翻译： 式（I）的新型产物，其制备方法，含有它们的药物组合物及其在制备药物中的用途。在式（I）中，以下取代基是优选的：Ar表示取代或缩合的苯基或 多环或杂环芳族基团，R表示通式为（CH 2）m -X1（CH 2）n Z的基团，其中X1 =单键，O，S; m = 0,1， n = 0,1,2; CH2基可以被取代; Z代表羧基，COOR6（R6 =烷基），CON（R7）（R8）（R7 =氢或烷基，R8 =氢，羟基，芳基磺酰基，杂环基，任选取代的氨基，任选取代的烷氧基或任选取代的烷基），PO OR 9）2（R 9 =氢或烷基），-NH-CO-T（T =氢或任选取代的烷基）基团，或不相关的，R 1和R 2 =氢或卤素或烷基，烷氧基，其被任选取代 ，烷硫基，烷氧基羰基或其它R1和R2在相邻的邻位形成含有1或2个杂原子的任选取代的杂环，R 3和R 4 =氢或卤素或烷基，烯基，烷氧基，烷硫基，羧基或烷氧基羰基 ，R5 =氢，烷基，烷硫基，X = O或S或-NH-，-CO-，亚甲基，乙烯基二烯基，烯-1,1-二基或环烷烃-1,1-二基，Y = O或S， 外消旋形式，以及光学异构体（非对映异构体和对映体）和式（I）的产物的盐。 式（I）化合物是具有显着的抗肿瘤和抗白血病性质的法呢基转移酶抑制剂。