知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

163 条记录 (耗时 0.037 秒)

    Novel polyketide derivatives
    71.
    发明申请
    Novel polyketide derivatives 有权

    公开(公告)号：US20030144315A1

    公开(公告)日：2003-07-31

    申请号：US10331047

    申请日：2002-12-27

    发明人： Daniel Chu ,  Maria Fardis ,  Chaitan Khosla ,  Christopher Reeves ,  Daniel Santi ,  Andreas Schirmer

    IPC分类号： A61K031/5377 ,  A61K031/4745 ,  C07D267/22

    CPC分类号： C07D498/18

    摘要： The present invention relates to novel polyketides, host cells that produce the novel compounds, and methods fort their use. The compounds of the present invention are cyclic polyketides (also referred to as a nullmacrolidesnull or nullmacrolactonesnull) that include 1 as part of their structure and bind to a FK binding protein wherein R4 and R5 are each selected from the group consisting of hydrogen, methyl, ethyl, and methoxy, provided that at least one of R4 and R5 is hydrogen, methyl, or ethyl. As will be explained in greater detail below, the compounds of the present invention have properties such as favorable P450 enzyme activity profiles that are desirable for use of these compounds as drugs.

    Aryl, alkyl, alkenyl and alkynylmacrolides having immunosuppressive activity
    75.
    发明授权
    Aryl, alkyl, alkenyl and alkynylmacrolides having immunosuppressive activity 失效
    具有免疫抑制活性的芳基，烷基，烯基和炔基羟基丙烯酰胺

    公开(公告)号：US5880280A

    公开(公告)日：1999-03-09

    申请号：US259831

    申请日：1994-06-15

    申请人： Helen M. Organ ,  Mark A. Holmes

    发明人： Helen M. Organ ,  Mark A. Holmes

    IPC分类号： A61K31/435 ,  A61P31/04 ,  A61P37/06 ,  C07D498/18 ,  C07D267/22 ,  C07D281/18 ,  C07D337/16 ,  C07D513/00

    CPC分类号： C07D498/18

    摘要： Aryl, alkyl, alkenyl and alkynyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by modification at C-30, C-33, and/or C-34 of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

    摘要翻译： 通过在环己基环的C-30，C-33和/或C-34上进行修饰，由合适的前体制备通式结构式Ⅰ的芳基，烷基，烯基和炔基大环内酯：。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病和/或预防外来器官移植排斥和/或相关疾病，疾病和疾病。

    Condensed cyclic compounds and their use
    77.
    发明授权
    Condensed cyclic compounds and their use 失效
    缩合的环状化合物及其用途

    公开(公告)号：US5698691A

    公开(公告)日：1997-12-16

    申请号：US311932

    申请日：1994-09-26

    申请人： Hidefumi Yukimasa ,  Ryuichi Tozawa ,  Yasuo Sugiyama ,  Masakuni Kori

    发明人： Hidefumi Yukimasa ,  Ryuichi Tozawa ,  Yasuo Sugiyama ,  Masakuni Kori

    IPC分类号： C12N9/99 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  A61P3/06 ,  A61P43/00 ,  C07D223/16 ,  C07D243/04 ,  C07D243/10 ,  C07D243/12 ,  C07D243/14 ,  C07D243/16 ,  C07D243/24 ,  C07D245/06 ,  C07D255/04 ,  C07D257/04 ,  C07D267/14 ,  C07D267/22 ,  C07D281/10 ,  C07D285/00 ,  C07D417/06 ,  C07D417/12 ,  C07D498/04 ,  C07D267/02

    CPC分类号： C07D223/16 ,  C07D243/04 ,  C07D243/12 ,  C07D243/24 ,  C07D255/04 ,  C07D267/14 ,  C07D281/10 ,  C07D417/06 ,  C07D417/12

    摘要： Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R.sub.1 is hydrogen or an optionally substituted hydrocarbon group; R.sub.2 is hydrogen, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic ring group; X' is a substituent comprising an optionally esterified carboxyl group, an optionally substituted carbamoyl group, an optionally substituted hydroxyl group, an optionally substituted amino group or an optionally substituted heterocyclic radical having a protonizable hydrogen; Ring A is an optionally substituted benzene ring or an optionally substituted aromatic heterocyclic ring; Ring J' is a 7- to 8-membered heterocyclic ring containing at most three ring constituting hetero atoms; D is C or N; the Ring J' optionally having, besides R.sub.1, R.sub.2 and X', a further substituent; provided that the condensed ring composed of Ring A and ring J' is not a 2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine ring, or a pharmaceutically acceptable salt thereof, and which is useful for the prophylaxis or therapy of hypercholesteremia or coronary sclerosis of mammals.

    摘要翻译： 公开了一种角鲨烯合成酶抑制剂，其包含由通式取代的烃基表示的化合物; R2是氢，任选取代的烷基，任选取代的苯基或任选取代的芳族杂环基; X'是包含任选酯化的羧基，任选取代的氨基甲酰基，任选取代的羟基，任选取代的氨基或具有可质子化氢的任选取代的杂环基的取代基; 环A是任选取代的苯环或任选取代的芳族杂环; 环J'是含有至多三个环构成杂原子的7-至8-元杂环; D为C或N; 除了R1，R2和X'之外，环J'还可以具有另外的取代基; 条件是由环A和环J'组成的稠环不是2-氧代-1,2,3,5-四氢-4,1-苯并氧氮杂环，或其药学上可接受的盐，并且其可用于 预防或治疗哺乳动物的高胆固醇血症或冠状动脉硬化。