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    • 2. 发明申请
    • OXO-AZABICYCLIC COMPOUNDS
    • OXO-AZABICYCLIC化合物
    • WO2003076417A2
    • 2003-09-18
    • PCT/EP2003/002277
    • 2003-03-06
    • WARNER-LAMBERT COMPANY LLCGAUDILLIERE, BernardJACOBELLI, HenryKOSTLAN, CatherineLI, JackYUE, Wen-Song
    • GAUDILLIERE, BernardJACOBELLI, HenryKOSTLAN, CatherineLI, JackYUE, Wen-Song
    • C07D239/91
    • C07D471/04C07D239/91
    • A compound selected from those of formula (1): ~',Xi Gi X 2 (7l) I ,N - R 1 (I) 11 - G 2 X3 wherein: 5 • X,, X2, and X3, represent N or -CR3 in which R3 is as described in the description, • G, represents a group selected from those of formulae (i/a) and (i/b): R4 R6 \ R4 N (i/a) (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, 10 C=S, S(O) n , in which nl represents an integer from 0 to 2 inclusive, or a group of formula (i/c): 11-1y -r ( i/c ) Y 1 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, 15 • Z, represents -CRgR,o, wherein R9 and R I O areas defined in the description, • A represents a ring system, • R, represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d) (G3)q~(Z2 )~ (i/d) 20 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.
    • 选自式(I)的化合物的化合物,其中:X 1,X 2和X 3表示N或-CR 3,其中R 3如描述中所述,G 1表示选自式(i / a)和( 其中R 4,R 5和R 6如说明书中所定义,R 2表示选自碳 - 碳三键,-CH = C = CH-,C = O,C = S,S(O )n1,其中n1表示0〜2的整数,或其中Y1表示O,S,-NH或-N烷基的式(i / c)基团,Y2表示O,S,-NH或-N烷基 n为0以上6以下的整数,m为0以上7以下的整数,Z1为-CR9R10,其中,R9和R10如说明书中所定义,A表示环系,R1表示选自 H,烷基,烯基,炔基,任选被取代的基团和其中p,Z2,B,q和G3如说明书中所定义的任选的其光学异构体,N-氧化物和加成 其盐与药学上可接受的 le酸或碱,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。
    • 3. 发明申请
    • OXO AZABICYCLIC COMPOUNDS
    • OXO AZABICYCLIC化合物
    • WO2003076416A1
    • 2003-09-18
    • PCT/EP2002/003240
    • 2002-03-08
    • WARNER-LAMBERT COMPANY LLCGAUDILLIERE, BernardJACOBELLI, HenryKOSTLAN, CatherineLI, JackYUE, Wen-Song
    • GAUDILLIERE, BernardJACOBELLI, HenryKOSTLAN, CatherineLI, JackYUE, Wen-Song
    • C07D239/91
    • C07D471/04C07D239/91
    • A compound selected from those of formula (I): 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): formula (II) 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) nt in which n1 represents an integer from 0 to 2 inclusive, or a group of formula (i/c): formula (III) 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): formula (IV) 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.
    • 选自式(I)的化合物:式(I)其中:-X 1,X 2和X 3表示其中R 3如描述中所述的N或CR 3,-G1表示选自式 I / a)和(i / b):其中R 4,R 5和R 6如说明书中所定义的式(II),-G2表示选自碳 - 碳三键,-CH = C = CH- ,C = O,C = S,S(O)nt,其中n1表示0〜2的整数,或式(i / c):式(III)的基团,其中Y1表示O,S, NH或N烷基,Y2表示O,S,-NH或N烷基,-n为0〜6的整数,m为0〜7的整数,Z1表示CR9R10,其中R9和R10如 描述,-A表示环系,-R 1表示选自H,烷基,烯基,炔基,任选取代的基团和式(I / d)的基团:式(IV)其中p,Z2,B, q和G3如说明书中所定义,并且任选地,其光学异构体, 和其药学上可接受的酸或碱的加成盐和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。