发明名称 Indol-3-YL derivatives
摘要 Indol-3-yl derivatives of the formula I, where A and B are each, independently of one another, O, S, NH, NR7, CO, CONH, NHCO or a direct bond, X is alkylene having 1 to 2 carbon atoms which is unsubstituted or monosubstituted by R4 or R5, or a direct bond, R1 is H, Z or -(CH2)o-Ar, R2 is H, R7 or -C(O)Z, R3 is NHR6, -NR6-C(=NR6)-NHR6, -C(=NR6)-NHR6, -NR6-C(=NR9)- NHR6, -C(=NR9)-NHR6 or Het1, R4 and R5 are each, independently of one another, H, oxo, R7, -(CH2)o-Ar, -C(O)-(CH2)o-Ar, -C(O)-(CH2)o-R-C(O)-(CH2)o- Het, Het, NHR6, NHAr, NH-Het, CONH-R7, CONH-(CH2)o-Ar, CONH- (CH2)o-Het, OR7, OAR, OR6 or O-Het1, R6 is H, -C(O)R, -C(O)-Ar, -C(O)-Het, R7, COOR7, COO-(CH2)o- Ar, COO-(CH2)o-Het, SO2-Ar, SO2R7 or SO2-Het, R7 is alkyl having 1 to 10 carbon atoms or cycloalkyl having 3 to 10 carbon atoms, R8 is Hal, NO2, CN, Z, -(CH2)o-Ar, COOR1, OR1, CF3, OCF3, SO2R1, NHR1, N(R1)2, NH-C(O)R1, NHCOOR1, COOH, COOZ or C(O)R1, R9 is CN or NO2, Z is alkyl having 1 to 6 carbon atoms, Ar is aryl which is unsubstituted or monosubstituted or polysubstituted by R8, Hal is F, Cl, Br or I, Het is a saturated, partially or fully unsaturated monocyclic or bicyclic heterocyclic radical having 5 to 10 ring members, where 1 or 2 N and/or 1 or 2 S or O atoms may be present and the heterocyclic radical may be monosubstituted or disubstituted by R8, Het1 is a saturated, partially or fully unsaturated monocyclic or bicyclic heterocyclic radical having 5 to 10 ring members and 1 to 4 N atoms which may be unsubstituted or monosubstituted or disubstituted by Hal, R7, OR7, CN, NHZ, oxo or NO2, n is 0, 1 or 2, m is 0, 1, 2, 3, 4, 5 or 6, and o is 0, 1 or 2. A process for preparing compounds of formula I is also disclosed. Also disclosed are their use in medicines for the treatment of thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, rheumatic arthritis, macular degenerative disease, diabetic retinopathy, tumour diseases, osteoporosis, infections and restenosis after angioplasty.
申请公布号 NZ521260(A) 申请公布日期 2004.02.27
申请号 NZ20010521260 申请日期 2001.01.05
申请人 MERCK PATENT GMBH 发明人 GOODMAN, SIMON;GOTTSCHLICH, RUDOLF;WIESNER, MATTHIAS
分类号 C07D401/06;A61K31/405;A61K31/4178;A61K31/4184;A61K31/4439;A61K31/506;A61P7/02;A61P9/00;A61P9/10;A61P19/02;A61P19/10;A61P25/00;A61P27/02;A61P29/00;A61P31/00;A61P35/00;A61P43/00;C07D209/18;C07D209/20;C07D401/12;C07D401/14;C07D403/06;C07D403/12;C07D409/06;C07D417/06;C07D417/14;(IPC1-7):A61K31/405 主分类号 C07D401/06
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