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。

公开(公告)号：US20070129409A1

公开(公告)日：2007-06-07

申请号：US10580078

申请日：2004-11-08

申请人： Lain-Yen Hu ,  Daniel Du ,  Huangshu Lei ,  Wen-Song Yue

发明人： Lain-Yen Hu ,  Daniel Du ,  Huangshu Lei ,  Wen-Song Yue

IPC分类号： C07D213/84 ,  A61K31/44

CPC分类号： C07D213/85

摘要： The present invention is directed to a new class of 5-cyano-2-amino pyridines and to their use as androgen receptor modulators. A further aspect of the invention is directed to a new animal model for finding compounds capable of alleviating androgenic alopecia.

摘要翻译： 本发明涉及一类新的5-氰基-2-氨基吡啶并且其用作雄激素受体调节剂。 本发明的另一方面涉及一种用于发现能够减轻雄激素性脱发的化合物的新动物模型。