利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

37 条记录 (耗时 0.039 秒)

    Process for preparing benzothiazepines from gamma-aminoalkylbenzenes
    22.
    发明授权
    Process for preparing benzothiazepines from gamma-aminoalkylbenzenes 有权
    从γ-氨基烷基苯制备苯并硫氮杂的方法

    公开(公告)号：US08618282B2

    公开(公告)日：2013-12-31

    申请号：US12397212

    申请日：2009-03-03

    申请人： Shixian Deng ,  Sandro Belvedere ,  Jiaming Yan ,  Donald Landry

    发明人： Shixian Deng ,  Sandro Belvedere ,  Jiaming Yan ,  Donald Landry

    IPC分类号： C07D281/08 ,  C07D281/10

    CPC分类号： C07D281/02 ,  C07D281/10 ,  C07D513/04 ,  Y02P20/55

    摘要： The invention provides a process for preparing a 2,3,4,5-tetrahydro[1,4]benzothiazepine of formula: by reacting a [2-(acylaminoethyl)thio]arene of formula with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2-(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula then treating the [N-hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahydro[1,4]benzothiazepine.

    摘要翻译： 本发明提供了制备下式的2,3,4,5-四氢[1,4]苯并硫氮杂的方法：通过使式的[2-（酰基氨基乙基）硫代]芳烃或其多聚体与 酸。 本发明还提供了使[2-（酰基氨基乙基）硫代]芳烃与其醛或多聚体和碱反应以形成式的[N-羟甲基-2- [酰氨基乙基]硫代]芳烃，然后将[N- 羟基甲基-2-（酰氨基乙基）硫代]芳烃与酸形成2,3,4,5-四氢[1,4]苯并硫氮杂。

    Pyridine Derivatives and Their Use in The Treatment of Psychotic Disorders
    24.
    发明申请
    Pyridine Derivatives and Their Use in The Treatment of Psychotic Disorders 有权

    公开(公告)号：US20100152175A1

    公开(公告)日：2010-06-17

    申请号：US12636849

    申请日：2009-12-14

    申请人： Giuseppe Alvaro ,  Daniele Andreotti ,  Sandro Belvedere ,  Romano Di Fabio ,  Alessandro Falchi ,  Riccardo Giovannini

    发明人： Giuseppe Alvaro ,  Daniele Andreotti ,  Sandro Belvedere ,  Romano Di Fabio ,  Alessandro Falchi ,  Riccardo Giovannini

    IPC分类号： A61K31/5383 ,  A61P25/30

    CPC分类号： C07D487/04 ,  C07D513/04

    摘要： There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein: X represents a nitrogen atom; Y represents —C(H2)—, (—C(H2)—)2, —S(O2)— or —C(═O)—; Z represents —C(H2)—, —S(O2)—, —N(Rz)—, or an oxygen or sulphur atom; A represents hydrogen or —CH2OH; Rz represents hydrogen, C1-6 alkyl, C1-6 alkoxy, —COR7 or —SO2R7; R1 represents halogen, C1-6 alkyl, C1-6 alkoxy, ═O, haloC1-6 alkyl, haloC1-6 alkoxy, hydroxyl or —CH2OH; m represents an integer from 0 to 3; R2 represents halogen, ═O, C1-6 alkyl (optionally substituted by one or more hydroxyl groups), —COOR7, —CONR7R8, C1-6 alkoxy, haloC1-6 alkyl, haloC1-6 alkoxy or C1-6alkylOC1-6alkyl; n represents an integer from 0 to 3; p and q independently represent an integer from 0 to 2; R3 represents an -aryl, -heteroaryl, -heterocyclyl, -aryl-aryl, -aryl-heteroaryl, -aryl-heterocyclyl, -heteroaryl-aryl, -heteroaryl-heteroaryl, -heteroaryl-heterocyclyl, -heterocyclyl-aryl, -heterocyclyl-heteroaryl or -heterocyclyl-heterocyclyl group, all of which may be optionally substituted by one or more (e.g. 1, 2 or 3) halogen, C1-6 alkyl (optionally substituted by one or more hydroxyl groups), C3-8 cycloalkyl, C1-6 alkoxy, hydroxyl, haloC1-6 alkyl, haloC1-6 alkoxy, cyano, —S—C1-6 alkyl, —SO—C1-6 alkyl, —SO2—C1-6 alkyl, —COR7, —CONR7R8, —NR7R8, —NR7COC1-6 alkyl, —NR7SO2—C1-6 alkyl, C1-6 alkyl-NR7R8, —OCONR7R8, —NR7CO2R8 or —SO2NR7R8 groups; R4 and R5 independently represent C1-6 alkyl, or R4 and R5 together with the carbon atom to which they are attached may together form a C3-8 cycloalkyl group; R6 represents halogen, C1-6 alkyl, C3-8 cycloalkyl, C1-6 alkoxy, haloC1-6 alkyl or haloC1-6 alkoxy; s represents an integer from 0 to 4; R7 and R8 independently represent hydrogen, C1-6 alkyl or C3-8 cycloalkyl; or solvates thereof.

    Hydroxamic acid compounds and methods of use thereof
    26.
    发明申请
    Hydroxamic acid compounds and methods of use thereof 失效
    羟肟酸化合物及其使用方法

    公开(公告)号：US20070155785A1

    公开(公告)日：2007-07-05

    申请号：US11710036

    申请日：2007-02-22

    申请人： Ronald Breslow ,  Thomas Miller ,  Sandro Belvedere ,  Paul Marks ,  Victoria Richon ,  Richard Rifkind

    发明人： Ronald Breslow ,  Thomas Miller ,  Sandro Belvedere ,  Paul Marks ,  Victoria Richon ,  Richard Rifkind

    IPC分类号： A61K31/4709 ,  C07D401/02

    CPC分类号： C07D211/02 ,  C07D215/38 ,  C07D401/12

    摘要： The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

    摘要翻译： 本发明涉及一类具有至少两个含芳基基团的异羟肟酸衍生物，其中至少一个是喹啉基，异喹啉基或苄基部分，通过亚甲基链与异羟肟酸基团连接。 异羟肟酸化合物可用于治疗癌症，例如脑癌。 异羟肟酸化合物也可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。 因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经变性 疾病