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11 条记录 (耗时 0.019 秒)

    Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their pharmaceutical uses
    2.
    依法登记的发明
    Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their pharmaceutical uses 有权

    公开(公告)号：USH1992H1

    公开(公告)日：2001-09-04

    申请号：US09372064

    申请日：1999-08-11

    申请人： Steven L. Bender ,  Arlindo L. Castelhano

    发明人： Steven L. Bender ,  Arlindo L. Castelhano

    IPC分类号： C07D21132

    摘要： The present invention relates to compounds of formula I: wherein Ar is an aryl group or a heteroaryl group; X is —NH—OH or —OH; R1 is H, —CH(R3)(R4), —C(O)R3, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group, wherein R3 is H or any suitable substituent and R4 is H, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group; R2 is CH2-R5, wherein R5 is H or any suitable substituent, or wherein R5 and R4 are optionally substituted carbon atoms singly- or double-bonded to one another; and pharmaceutically acceptable prodrugs, salts, and solvates thereof. The invention further relates to methods of using these compounds, particularly as metalloproteinase inhibitors.

    Processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto
    3.
    发明授权
    Processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto 有权
    制备周围阿片样物质拮抗剂化合物及其中间体的方法

    公开(公告)号：US06794510B2

    公开(公告)日：2004-09-21

    申请号：US10216158

    申请日：2002-08-08

    申请人： Bertrand Le Bourdonnec ,  Roland Ellwood Dolle

    发明人： Bertrand Le Bourdonnec ,  Roland Ellwood Dolle

    IPC分类号： C07D21132

    CPC分类号： C07D211/22 ,  C07C231/02 ,  C07C235/34

    摘要： Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.

    摘要翻译： 用于制备外周阿片样物质拮抗剂化合物及其中间体的新方法。 通过本发明方法制备的化合物可用作例如mu，κ和δ阿片样物质受体的拮抗剂，因此可用于治疗胃肠动力障碍，以及用于预防外周鸦片诱导的副作用。 本发明方法可以提供改善的产率，纯度，中间体和最终产物的制备和/或分离的容易性，以及更具有工业上有用的反应条件和可加工性。

    Methods for production of piperidyl acetamide stereoisomers
    6.
    发明授权
    Methods for production of piperidyl acetamide stereoisomers 有权
    哌啶乙酰胺立体异构体的生产方法

    公开(公告)号：US06359139B1

    公开(公告)日：2002-03-19

    申请号：US09707524

    申请日：2000-11-07

    申请人： Vikram Khetani ,  William Konnecke ,  Chuansheng Ge

    发明人： Vikram Khetani ,  William Konnecke ,  Chuansheng Ge

    IPC分类号： C07D21132

    CPC分类号： C07D211/34

    摘要： Synthetic methods are provided comprising the steps of racemizing l-threo-piperidyl acetamides to form a mixture of d-threo, l-threo, d-erythro, and l-erythro-piperidyl acetamides by reacting said l-threo-piperidyl acetamides with alkanoic acid.

    摘要翻译： 提供了合成方法，包括以下步骤：使1-苏式 - 哌啶基乙酰胺进行外消旋化以形成d-苏，1-苏，d-赤型和1-赤型 - 哌啶基乙酰胺的混合物，通过使所述1-苏 - 哌啶基乙酰胺与链烷酸 酸。

    Process and intermediates for production of donepezil and related compounds
    8.
    发明授权
    Process and intermediates for production of donepezil and related compounds 失效
    生产多奈哌齐和相关化合物的方法和中间体

    公开(公告)号：US06492522B1

    公开(公告)日：2002-12-10

    申请号：US09763245

    申请日：2001-05-24

    申请人： Arie L. Gutman ,  Eleonora Shkolnik ,  Boris Tishin ,  Genady Nisnevich ,  Igor Zaltzman

    发明人： Arie L. Gutman ,  Eleonora Shkolnik ,  Boris Tishin ,  Genady Nisnevich ,  Igor Zaltzman

    IPC分类号： C07D21132

    CPC分类号： C07D211/32 ,  C07D211/34

    摘要： The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R1 is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-(&ohgr;-aralkyl)-4-piperidyl; 4-pyridyl; R4, R5, R6, and R7 are identical or different and each represents hydrogen, straight-chain or branched alkyl, aryl, hydroxy, alkoxy, aryloxy, benzyloxy, acyloxy, alkylthio, arylthio, benzylthio, acylamino, phthalimido or halogen; n is 1, 2 or 3; m is 1, 2, 3, 4, or 5. This process comprises cyclisation of a compound of formula (II) or salts thereof, wherein R1, R4, R5, R6 and R7, m and n are as defined above; R2 is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R3 is selected from a derivatised or non-derivatised carboxyl, cyano or N-substituted aminocarbonyl groups, optionally in the presence of acids and/or solvents. One of the most potent acetylcholinesterase inhibitors of the class of compounds prepared according to the present invention is donepezil.

    摘要翻译： 本发明涉及制备式（I）的乙酰胆碱酯酶抑制剂或其盐的新方法，其中：R1是N-酰基-4-哌啶基; N-烷氧基羰基-4-哌啶基; N-烷基-4-哌啶基; N-苄基-4-哌啶基; N-（ω-芳烷基）-4-哌啶基; 4-吡啶基; R 4，R 5，R 6和R 7相同或不同，各自表示氢，直链或支链烷基，芳基，羟基，烷氧基，芳氧基，苄氧基，酰氧基，烷硫基，芳硫基，苄硫基，酰氨基，苯二酰亚胺基或卤素; n为1,2或3; 该方法包括式（II）化合物或其盐的环化，其中R 1，R 4，R 5，R 6和R 7，m和n如上所定义; R2选自衍生的或非衍生的羧基，氰基，N-取代的氨基羰基或氢; R3选自衍生化或非衍生的羧基，氰基或N-取代的氨基羰基，任选在酸和/或溶剂的存在下。 根据本发明制备的化合物类别中最有效的乙酰胆碱酯酶抑制剂之一是多奈哌齐。