利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

11 条记录 (耗时 0.039 秒)

    Alkynylated fused ring pyrimidine compounds
    5.
    发明申请
    Alkynylated fused ring pyrimidine compounds 审中-公开
    炔烃基稠环嘧啶化合物

    公开(公告)号：US20050245548A1

    公开(公告)日：2005-11-03

    申请号：US11148880

    申请日：2005-06-09

    申请人： Bernard Gaudilliere ,  Henri Jacobelli ,  Joseph Picard ,  Michael Wilson

    发明人： Bernard Gaudilliere ,  Henri Jacobelli ,  Joseph Picard ,  Michael Wilson

    IPC分类号： A61K31/517 ,  A61K31/519 ,  A61P1/02 ,  A61P1/04 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P27/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D239/96 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04 ,  C07D521/00 ,  C07F7/18

    CPC分类号： C07D231/12 ,  A61K31/517 ,  C07D233/56 ,  C07D239/96 ,  C07D249/08 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04 ,  C07F7/1804

    摘要： A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N═X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.

    摘要翻译： 选自式（I）的化合物的化合物：其中W 1代表O，S或-NR 3，其中R 3表示氢 ，烷基，OH或CN; W 2表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳基烷基， 环烷基烷基，杂环，这些基团任选被取代，或者W 1和W 2 2一起形成式-NX 4 -W 3 < - >如描述中所定义，X 1，X 2和X 3表示N或C任选取代的n 是0至8，Z表示-CR 12 R 13，其中R 12和R 13定义同上 在描述中，A表示环系，基团R 2表示氢或如说明书中定义的各种化学基团，q为0至7; R 1表示氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和药物产品 含有它们的特异性抑制剂可用作13型基质金属蛋白酶的特异性抑制剂。

    Alkynylated quinazoline compounds
    7.
    发明授权
    Alkynylated quinazoline compounds 失效
    炔烃基喹唑啉化合物

    公开(公告)号：US06962922B2

    公开(公告)日：2005-11-08

    申请号：US10269197

    申请日：2002-10-11

    申请人： Bernard Gaudilliere ,  Henri Jacobelli ,  Joseph Armand Picard ,  Michael William Wilson

    发明人： Bernard Gaudilliere ,  Henri Jacobelli ,  Joseph Armand Picard ,  Michael William Wilson

    IPC分类号： C07D239/96 ,  C07D403/06 ,  C07D471/04 ,  A61K31/517 ,  A61P19/02 ,  C07D401/10

    CPC分类号： C07D403/06 ,  C07D239/96 ,  C07D471/04

    摘要： A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N═X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.

    摘要翻译： 选自式（I）的化合物的化合物：其中W 1代表O，S或-NR 3，其中R 3表示氢 ，烷基，OH或CN; W 2表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳基烷基， 环烷基烷基，杂环，这些基团任选被取代，或者W 1和W 2 2一起形成式-NX 4 -W 3 < - >如描述中所定义，X 1，X 2和X 3表示N或C任选取代的n 是0至8，Z表示-CR 12 R 13，其中R 12和R 13定义同上 在描述中，A表示环系，基团R 2表示氢或如说明书中定义的各种化学基团，q为0至7; R 1表示氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和药物产品 含有它们的特异性抑制剂可用作13型基质金属蛋白酶的特异性抑制剂。

    1-Amino triazoloc4,3-a! quinazoline-5-ones and/or -5-thiones inhibiting phosphodiesterase IV
    8.
    发明授权
    1-Amino triazoloc4,3-a! quinazoline-5-ones and/or -5-thiones inhibiting phosphodiesterase IV 失效
    1-氨基三唑并[3,4-a] 喹唑啉-5-酮和/或5-硫代磷酸二酯酶IV

    公开(公告)号：US06828315B1

    公开(公告)日：2004-12-07

    申请号：US09980540

    申请日：2001-10-25

    申请人： Bernard Gaudilliere ,  Remi Lavalette ,  Charles Andrianjara ,  Francine Breuzard

    发明人： Bernard Gaudilliere ,  Remi Lavalette ,  Charles Andrianjara ,  Francine Breuzard

    IPC分类号： C07D48704

    CPC分类号： C07D487/04

    摘要： The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives. The compounds act as inhibitors of phosphodiesterase IV (PDE-4) and, as such, have utility in treating asthma, chronic bronchitis, acutte pulmonary attack, atopic dermatitis, pulmonary hypertension, pulmonary insufficiency, cardiac insufficiency, psoriasis, inflammatory conditions of the digestive system such as haemorrhagic rectocolitis and Crohn's disease, acute respiratory distress syndrome, acute pancreatitis, benign hypertrophy of the prostate, rheumatoid arthritis, multiple sclerosis, depression, ischaemia-induced neuronal damage, partial cerebral ischaemia, and cancer such as malignant tumor and chronic lymphoid leukemia.

    摘要翻译： 本发明涉及式I和式II的三唑并[4,3-a]喹唑啉-5-酮和5-硫杂，其中I和II是氮3或4上基团R的位置异构体。任选地，本发明也 涉及其外消旋形式，异构体和药学上可接受的盐。 本发明还涉及其制备方法和含有所述衍生物的组合物。 这些化合物作为磷酸二酯酶IV（PDE-4）的抑制剂，因此可用于治疗哮喘，慢性支气管炎，急性肺部发作，特应性皮炎，肺动脉高压，肺功能不全，心功能不全，牛皮癣，消化道炎症状况 系统如出血性直肠结肠炎和克罗恩病，急性呼吸窘迫综合征，急性胰腺炎，前列腺良性肥大，类风湿性关节炎，多发性硬化症，抑郁症，局部缺血诱发的神经元损伤，部分脑缺血和恶性肿瘤和慢性淋巴细胞癌 白血病。

    Oxo-azabicyclic compounds
    9.
    发明授权
    Oxo-azabicyclic compounds 失效
    氧氮杂双环化合物

    公开(公告)号：US06894057B2

    公开(公告)日：2005-05-17

    申请号：US10384115

    申请日：2003-03-07

    申请人： Bernard Gaudilliere ,  Henry Jacobelli ,  Catherine Kostlan ,  Jack Jie Li ,  Wen-Song Yue

    发明人： Bernard Gaudilliere ,  Henry Jacobelli ,  Catherine Kostlan ,  Jack Jie Li ,  Wen-Song Yue

    IPC分类号： C07D239/91 ,  C07D401/06 ,  C07D403/06 ,  C07D403/10 ,  C07D471/04 ,  A61K31/5025

    CPC分类号： C07D401/06 ,  C07D239/91 ,  C07D403/06 ,  C07D403/10 ,  C07D471/04

    摘要： A compound selected from those of formula (I): wherein: X1, X2, and X3, represent N or —CR3 in which R3 is as described in the description, G1 represents a group selected from those of formulae (i/a) and (i/b): in which R4, R5, and R6 are as defined in the description, G2 represents a group selected from carbon—carbon triple bond, —CH═C═CH—, C═O, C═S, S(O)n1 in which n1 represents an integer from 0 to 2 inclusive, or a group of formula (i/c): in which Y1 represents O, S, —NH or -Nalkyl, and Y2 represents O, S, —NH or -Nalkyl, n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, Z1 represents —CR9R10, wherein R9 and R10 are as defined in the description, A represents a ring system, R1 represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d): in which p, Z2, B, q and G3 are as defined in the description and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.

    摘要翻译： 选自式（I）的化合物：其中：X 1，X 2和X 3代表N或-CR 3， 其中R 3 3如说明书中所述，其中G 1表示选自式（i / a）和（i / b）：其中R 4，R 5和R 6如描述中所定义，G 2， 表示选自碳 - 碳三键，-CH-C-CH-，CO，CS，S（O）n1N的基团，其中n1表示0〜2的整数，或者 式（I / c）的基团：其中Y 1表示O，S，-NH或-N烷基，Y 2表示O，S，-NH或 -N烷基，n为0〜6的整数，m为0〜7的整数，Z 1表示-CR 9 R 10， 其中R 9和R 10如在说明书中所定义，A表示环系，R 1表示所选择的基团 由H，烷基，烯基，炔基，任选的 其中p，Z 2，B，q和G 3 3如在说明书中所定义，并且任选地，其 光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用作13型基质金属蛋白酶的特异性抑制剂。

    Triazolo compounds as MMP inhibitors
    10.
    发明授权
    Triazolo compounds as MMP inhibitors 失效
    三唑酚化合物作为MMP抑制剂

    公开(公告)号：US06849637B2

    公开(公告)日：2005-02-01

    申请号：US10075654

    申请日：2002-02-14

    申请人： Charles Andrianjara ,  Francine Breuzard ,  Bernard Gaudilliere ,  Henri Jacobelli

    发明人： Charles Andrianjara ,  Francine Breuzard ,  Bernard Gaudilliere ,  Henri Jacobelli

    IPC分类号： A61K31/519 ,  A61P1/02 ,  A61P1/04 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： A compound selected from those of formula (I): in which: W represents N or C—R1; in which R1 is as defined in the description, X represents N or C—R2 in which R2 is as defined in the description, Y represents a group selected from oxygen, sulfur, —NH, and —Nalkyl, Z represents a group selected from oxygen, sulphur, —NR8 in which R8 is as defined in the description, and optionally carbon depending the definition of Y, n is an integer from 0 to 8 inclusive, Z1 represents a group —CR9R10 wherein R9 and R10, are as defined in the description, which group contains optionally multiple bonds or heteroatomes, A represents a cyclic group, m is an integer from 0 to 7 inclusive, the group(s) R4 is (are) as defined in the description, R3 represents a group selected from hydrogen, alkyl, alkenyl, alkynyl, and the group of formula: in which p, Z2, B, q, and R13 are as defined in the description, optionally, its racemic forms, isomers thereof, N-oxydes thereof, and its the pharmaceutically acceptable salts thereof, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.

    摘要翻译： 选自式（I）的化合物：其中：W表示N或C-R 1; 其中R1如说明书中所定义，X表示N或C-R2，其中R2如说明书中所定义，Y表示选自氧，硫，-NH和-N烷基的基团，Z表示选自 氧，硫，-NR 8，其中R8如说明书中所定义，可选地取决于Y的定义，n为0至8的整数，其中Z 1为基团-CR 9 R 10，其中R 9和R 10如 描述，该组包含任选的多个键或杂原子，A表示环状基团，m是0至7的整数，包括端值，其中R 4是如在说明书中所定义的（是），R 3表示选自 氢，烷基，烯基，炔基和下式的基团：其中p，Z2，B，q和R13如说明书中所定义，任选地，其外消旋形式，异构体，其N-氧化物及其 其药学上可接受的盐和含有它们的药物可用作特异性抑制剂 的13型基质金属蛋白酶。