C3A receptor ligands
    1.
    发明授权
    C3A receptor ligands 失效
    C3A受体配体

    公开(公告)号:US06489339B1

    公开(公告)日:2002-12-03

    申请号:US09762459

    申请日:2001-02-07

    IPC分类号: A61K3147

    CPC分类号: C07C279/14

    摘要: A compound according to Formula (I): wherein: A represents C1-4 alkylene, unsubstituted or optionally substituted by C1-4 alkyl or aryl; or A forms a 5-8 membered fused aliphatic ring with the adjacent phenyl ring; m is an integer from 1 to 3; each R1 is independently selected form the group consisting of halo, C1-4 alkyl, methanesulfonyl, alkoxy, nitrile, dimethylamine, methylenedioxy and CF3; and R2 is hydrogen or methyl is provided.

    摘要翻译: 根据式(I)的化合物:其中:A表示未被取代或任选被C 1-4烷基或芳基取代的C 1-4亚烷基; 或A与相邻的苯环形成5-8元稠合的脂族环; m为1至3的整数;每个R 1独立地选自卤素,C 1-4烷基,甲磺酰基,烷氧基,腈,二甲胺 ,亚甲二氧基和CF 3; 并且R 2是氢或甲基。

    Integrin receptor antagonists
    7.
    发明授权
    Integrin receptor antagonists 失效
    整合素受体拮抗剂

    公开(公告)号:US6008213A

    公开(公告)日:1999-12-28

    申请号:US722095

    申请日:1997-12-19

    摘要: Compounds of formula (I) ##STR1## wherein A.sub.1 is C or N; E is a five- or six-membered heteroaromatic or six-membered aromatic ring optionally substituted by R.sup.3 or R.sup.4 ; X.sup.1 --X.sup.2 is CHR.sup.1 --CH, CR.sup.1 .dbd.CH, NR.sup.1 --CH, S(O).sub.u --CH or O--CH; X.sup.3 is CR.sup.5 R.sup.5 ', NR.sup.5, S(O).sub.u or O; R.sup.2 is --OR', --NR'R", --NR'SO.sub.2 R'", --NR'OR', --OCR'.sub.2 C(O)OR', --OCR'.sub.2 OC(O)--R', --OCR'.sub.2 C(O)NR'.sub.2, CF.sub.3 or --COCR'.sub.2 R.sup.2 '; R.sup.3, R.sup.4 and R.sup.7 are independently H, halo, --OR.sup.12, --SR.sup.12, --CN, --NR'R.sup.12, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r --, --CO.sub.2 R', --CONR'.sub.2, R.sup.14 --C.sub.0-6 alky-, R.sup.14 --C.sub.1-6 oxoalkyl-, R.sup.14 --C.sub.2-6 alkenyl-, R.sup.14 --C.sub.2-6 alkynyl-, R.sup.14 --C.sub.0-6 alkyloxy-, R.sup.14 --C.sub.0-6 alkylamino- or R.sup.14 --C.sub.0-6 alkyl--S(O).sub.r --; R.sup.6 is W--(CR'.sub.2).sub.q --Z--(CR'R.sup.10)--U--(CR'.sub.2).sub.s --V-- or W'--(CR'.sub.2).sub.q --U--(CR'.sub.2).sub.s -- U and V are absent or CO, CR'.sub.2, C(.dbd.CR.sup.15.sub.2), S(O).sub.n, O, NR.sup.15, CR.sup.15 'OR.sup.15, CR'(OR")CR'.sub.2, CR'.sub.2 CR'(OR") C(O)CR'.sub.2, CR.sup.15.sub.2 C(O), CONR.sup.15, NR.sup.15 CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR.sup.15, NR.sup.15 C(S), SO.sub.2 NR.sup.15, NR.sup.15 SO.sub.2, N.dbd.N, NR.sup.15 NR.sup.15, NR.sup.15 CR.sup.15.sub.2, NR.sup.15 CR.sup.15.sub.2, CR.sup.15.sub.2 O, OCR.sup.15.sub.2, C$(m)ZC, CR.sup.15 .dbd.CR.sup.15, Het, or Ar, provided that U and V are not simultaneously absent, and W and W' are a nitrogen-containing substituent, and integrin receptor antagonists.

    摘要翻译: PCT No.PCT / US96 / 11108 Sec。 371 1997年12月19日第 102(e)1997年12月19日PCT PCT 1996年6月28日PCT公布。 出版物WO97 / 01540 日期1997年1月16日其中A1为C或N的式(I)化合物; E是任选被R 3或R 4取代的五元或六元杂芳族或六元芳环; X1-X2是CHR1-CH,CR1 = CH,NR1-CH,S(O)u-CH或O-CH; X3是CR5R5',NR5,S(O)u或O; R2是-OR',-NR'R“,-NR'SO2R”',-NR'OR',-OCR'2C(O)OR',-OCR'2OC(O)-R',-OCR '2C(O)NR'2,CF 3或-COCR'2R2'; R3,R4和R7独立地是H,卤素,-OR12,-SR12,-CN,-NR'R12,-NO2,-CF3,CF3S(O)r-,-CO2R',-CONR'2,R14-C0 烷基 - ,R14-C 1-6氧基烷基 - ,R 14 -C 2-6烯基 - ,R 14 -C 2-6炔基 - ,R 14 -C 0-6烷氧基 - ,R 14 -C 0-6烷基氨基 - 或R 14 -C 0-6烷基-S(O)r - ; R6是W-(CR'2)qZ-(CR'R10)-U-(CR'2)sV-或W' - (CR'2)qU-(CR'2)s- U和V不存在 CO,CR'2,C(= CR152),S(O)n,O,NR15,CR15'OR15,CR'(OR“)CR'2,CR'2CR'(OR” CR(O),CONR 15,NR 15 CO,OC(O),C(O)O,C(S)O,OC(S),C(S)NR 15,NR 15 C(S),SO 2 NR 15,NR 15 SO 2, N = N,NR15NR15,NR15CR152,NR15CR152,CR152O,OCR152,C $(m)ZC,CR15 = CR15,Het或Ar,条件是U和V不同时不存在,W和W' 取代基和整联蛋白受体拮抗剂。