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11. 发明申请

WO2003076417A3 OXO-AZABICYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2003076417A3
公开(公告)日：2003-09-18
申请号：PCT/EP2003/002277
申请日：2003-03-06
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , KOSTLAN, Catherine , LI, Jack , YUE, Wen-Song
IPC分类号： C07D239/91
摘要： A compound selected from those of formula (I) wherein: X 1 , X 2 , and X 3 , represent N or -CR 3 in which R 3 is as described in the description, G 1 represents a group selected from those of formulae (i/a) and (i/b) in which R 4 , R 5 , and R 6 are as defined in the description, G 2 represents a group selected from carbon-carbon triple bond, -CH=C=CH-, C=O, C=S, S(O) n1 in which nl represents an integer from 0 to 2 inclusive, or a group of formula (i/c) in which Y 1 represents O, S, -NH or -Nalkyl, and Y 2 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, Z 1 represents -CR 9 R 10 ,wherein R 9 and R 10 are as defined in the description, A represents a ring system, R 1 represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d) in which p, Z 2 , B, q and G 3 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.

12. 发明申请

WO2003033478A1 ALKYNYLATED FUSED RING PYRIMIDINE COMPOUNDS AS MATRIX METALLOPROTEASE-13 INHIBITORS 审中-公开
标题翻译：作为基质METALLOPROTEASE-13抑制剂的烷基化的环烯丙基化合物
公开(公告)号：WO2003033478A1
公开(公告)日：2003-04-24
申请号：PCT/EP2002/012194
申请日：2002-10-11
申请人： WARNER-LAMBERT COMPANY LLC , GAUDILLIERE, Bernard , JACOBELLI, Henry , WILSON, Michael, William , PICARD, Joseph, Armand
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry , WILSON, Michael, William , PICARD, Joseph, Armand
IPC分类号： C07D239/96
CPC分类号： C07D231/12 , A61K31/517 , C07D233/56 , C07D239/96 , C07D249/08 , C07D403/06 , C07D471/04 , C07D487/04 , C07F7/1856
摘要： A compound selected from those of formula (I), wherein W 1 represents O, S, or -NR 3 in which R 3 represents hydrogen, alkyl, OH or CN; W 2 represents a group selected from hydrohen, CF 3 , NH 2 , monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W 1 and W 2 form together a group of formula -N=X 4 -W 3 - as defined in the description, X 1 , X 2 and X 3 represent N or C optionally substituted, n is 0 to 8, Z represents -CR 12 R 13 , wherein R 12 and R 13 are as defined in the description, A represents a ring system, the groups R 2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R 1 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，其中W 1表示O，S或-NR 3，其中R 3表示氢，烷基，OH或CN; W2代表选自氢化物，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，这些基团任选取代的基团，或者W1和W2一起形成式-N = X4 -W3-如说明书中所定义，X 1，X 2和X 3表示N或C任选取代，n为0至8，Z表示-CR 12 R 13，其中R 12和R 13如说明书中所定义，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，以及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。

13. 发明申请

WO2003033477A1 ALKYNLATED FUSED RING PYRIMIDINE COMPOUNDS AS MATRIX METALLOPROTEASE-13 INHIBITOR 审中-公开
标题翻译：碱性金属环化合物作为基质金属蛋白酶-13抑制剂
公开(公告)号：WO2003033477A1
公开(公告)日：2003-04-24
申请号：PCT/EP2001/011824
申请日：2001-10-12
申请人： WARNER-LAMBERT COMPANY , GAUDILLIERE, Bernard , JACOBELLI, Henry
发明人： GAUDILLIERE, Bernard , JACOBELLI, Henry
IPC分类号： C07D239/96
CPC分类号： C07D231/12 , C07D233/56 , C07D239/96 , C07D249/08 , C07D403/06 , C07D471/04 , C07D487/04 , C07F7/1856
摘要： A compound selected from those of formula (I) : wherein W 1 represents O, S, or -NR 3 in which R 3 represents hydrogen, alkyl, OH or CN; W 2 represents a group selected from hydrogen, CF 3 , NH 2 , monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W 1 and W 2 form together a group of formula -N=X 4- W 3- as defined in the description, X 1 , X 2 and X 3 represent N or C optionally substituted, n is 0 to 8, Z represents -CR 12 R 13 , wherein R 12 and R 13 are as defined in the description, A represents a ring system, the groups R 2 represent hydrogen, alkyl, halogen, cyano, nitro, trihalogenoalkyl, -NR 10 R 11 , -OR 14 , -SR 14 , -SOR 14 , -SO 2 R 14 , acyl, -(CH 2 ) k NR 10 R 11 , -X 5 (CH 2 ) k NR 10 R 11 , -(CH 2 ) k SO 2 NR 14 R 15 , -X 5 (CH 2 ) k C(=O)OR 14 , -(CH 2 ) k C(=O)OR 14 , -X 5 (CH 2 ) k C(=O)NR 14 R 15 , -(CH 2 ) k C(=O)NR 14 R 15 and -X 6 -R 16 in which X 5 , k; R 10 , R 11 , R 14 , R 15 , X 6 , and R 16 are as defined in the description, q is 0 to 7; R 1 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 mettaloprotease.
摘要翻译：选自式（I）的化合物：其中W 1表示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，这些基团任选取代的基团，或者W1和W2一起形成式-N = X4 -W3-如说明书中所定义，X 1，X 2和X 3表示N或C任选取代，n为0至8，Z表示-CR 12 R 13，其中R 12和R 13如说明书中所定义，A表示环系，基团R 2表示氢，烷基，卤素，氰基，硝基，三卤代烷基，-NR 10 R 11，-OR 14，-SR 14，-SOR 14，-SO 2 R 14，酰基， - （CH 2）k NR 10 R 11，-X 5（CH 2）k NR 10 R 11， - （CH 2）k SO 2 NR 14 R 15 ，-X5（CH2）kC（= O）OR14， - （CH2）kC（= O）OR14，-X5（CH2）kC（= O）NR14R15， - （CH2）kC（= O）NR14R15和-X6- R16，其中X5，k; R 10，R 11，R 14，R 15，X 6和R 16如说明书中所定义，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，以及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。

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