利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

7 条记录 (耗时 0.036 秒)

    1-N-phenylamino-1H-imidazole derivatives as aromatase inhibitors and pharmaceutical compositions containing them
    5.
    发明授权
    1-N-phenylamino-1H-imidazole derivatives as aromatase inhibitors and pharmaceutical compositions containing them 失效
    1-N-苯基氨基-1H-咪唑衍生物作为芳香酶抑制剂和含有它们的药物组合物

    公开(公告)号：US06737433B1

    公开(公告)日：2004-05-18

    申请号：US10319840

    申请日：2002-12-16

    申请人： Nathalie Adje ,  Paule Bonnet ,  Denis Carniato ,  Remi Delansorne ,  Jean Lafay ,  Jean-Claude Pascal

    发明人： Nathalie Adje ,  Paule Bonnet ,  Denis Carniato ,  Remi Delansorne ,  Jean Lafay ,  Jean-Claude Pascal

    IPC分类号： A61K314164

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Imidazole derivatives of the formula: in which R1 and R2 are each independently hydrogen, (C1-C6)alkyl or (C3-C8)cycloalkyl; n is 0, 1 or 2; R3, R4, R5 and R6 are each independently hydrogen or a (C1-C6)alkyl, halogen, cyano, (C1-C6)alkoxy, trifluoromethyl, (C1-C6)alkylthio, (C1-C6)alkylsulfonyl, sulfonamido, acyl, (C1-C6)alkoxycarbonyl, or carboxamido group; R3 and R6 together with the phenyl ring bearing them can also form a benzofurane, or a N-methylbenzotriazole. The invention also relates to pharmaceutical compositions containing these derivatives, and to the uses thereof.

    摘要翻译： 下式的咪唑衍生物：其中R 1和R 2各自独立地为氢，（C 1 -C 6）烷基或（C 3 -C 8）环烷基; n为0,1或2; R 3，R 4，R 5和R 6各自独立地为氢或 （C1-C6）烷基，卤素，氰基，（C1-C6）烷氧基，三氟甲基，（C1-C6）烷硫基，（C1-C6）烷基磺酰基，亚磺酰氨基，酰基，（C1-C6）烷氧基羰基或甲酰氨基; R3 和R6与带有它们的苯环一起也可以形成苯并呋喃或N-甲基苯并三唑。 本发明还涉及含有这些衍生物的药物组合物及其用途。

    Conformationally constrained LH-RH analogues, their uses and pharmaceutical compositions containing them
    6.
    发明授权
    Conformationally constrained LH-RH analogues, their uses and pharmaceutical compositions containing them 失效
    构象约束的LH-RH类似物，其用途和含有它们的药物组合物

    公开(公告)号：US6153587A

    公开(公告)日：2000-11-28

    申请号：US317125

    申请日：1999-05-24

    申请人： Remi Delansorne ,  Jacques Paris

    发明人： Remi Delansorne ,  Jacques Paris

    IPC分类号： A61K45/00 ,  A61K38/00 ,  A61K38/09 ,  A61P15/10 ,  A61P35/00 ,  C07K7/23

    CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S930/13

    摘要： LH-RH analogues with excellent affinity for LH-RH receptors, of the formula A.sub.1 -A.sub.2 -W-A.sub.3 -A.sub.4 -SPL-A.sub.5 -A.sub.6 -Pro-Z(I) in which:-A.sub.1 is pGlu, AcSar or an aromatic D-amino acid;-A.sub.2 is a direct bond, His, DPhe, DpFPhe or DpClPhe;*W is an aromatic L- or D-amino acid;-A.sub.3 is Ala, Thr, Ser, DSer, Ser(OBzl) or MeSer;-A.sub.4 is Tyr, Phe, cPzACAla, L- or D-PicLys, L- or D-NicLys or L- or D-IprLys;*SPL is the spirolactam of formula: ##STR1## -A.sub.5 is an amino acid with a (C.sub.1 -C.sub.8)alkyl or (C.sub.3-C.sub.6)cycloalkyl side chain;-A.sub.6 is L- or D-(Arg, HArg, Lys, HLys, Orn, Cit, HCit or Aph), where L- or D-(Arg and HArg) can be substituted by one or two (C.sub.1 -C.sub.4)alkyl groups and L- or D-(Lys, HLys, Orn and Aph) can be substituted by an isopropyl, nicotinoyl or picolinoyl group; and*Z is GlyNH.sub.2, DAlaNH.sub.2, AzaGlyNH.sub.2 or --NHR.sub.1 where R.sub.1 is a (C.sub.1 -C.sub.4)alkyl optionally substituted by a hydroxy or one or several fluorine atoms, a (C.sub.3 -C.sub.6)cycloalkyl or a heterocyclic radical selected from the group consisting of morpholinyl, pyrrolidinyl and piperidyl;or its pharmaceutically acceptable salts.

    摘要翻译： 式A1-A2-W-A3-A4-SPL-A5-A6-Pro-Z（I）的LH-RH受体具有优异亲和力的LH-RH类似物，其中：-A1是pGlu，AcSar或芳香族 D-氨基酸; -A2是直接键，His，DPhe，DpFPhe或DpClPhe; * W是芳族L-或D-氨基酸; -A3是Ala，Thr，Ser，DSer，Ser（OBzl）或MeSer; -A4是Tyr，Phe，cPzACAla，L或D-PicLys，L或D-NicLys或L或D-IprLys; * SPL是下式的螺内酰胺：-A5是具有（C1-C8）烷基或（C3-C6）环烷基侧链的氨基酸; -A6是L-或D-（Arg，HArg，Lys，HLys，Orn，Cit，HCit或Aph），其中L-或D-（Arg和HArg）可被一个或两个（C 1 -C 4）烷基取代 基团和L-或D-（Lys，HLys，Orn和Aph）可以被异丙基，烟酰基或吡啶酰基取代; 和* Z是GlyNH 2，DAla NH 2，Aza GlyNH 2或-NHR 1，其中R 1是任选被羟基或一个或多个氟原子取代的（C 1 -C 4）烷基，（C 3 -C 6）环烷基或选自以下的杂环基： 吗啉基，吡咯烷基和哌啶基; 或其药学上可接受的盐。