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    • 68. 发明专利
      DE10039610A1 Azepinoindole derivatives are PARP inhibitors and are useful for the treatment of neurodegenerative diseases, ischemia, tumor, septic shock, inflammation, rheumatic diseases, ARDS and diabetes mellitus 未知
    • Azepinoindole derivatives are PARP inhibitors and are useful for the treatment of neurodegenerative diseases, ischemia, tumor, septic shock, inflammation, rheumatic diseases, ARDS and diabetes mellitus
    • DE10039610A1
    • 2002-02-28
    • DE10039610
    • 2000-08-09
    • BASF AG
    • LUBISCH WILFRIED , GRANDEL ROLAND , KOCK MICHAEL , MUELLER REINHOLD , HOEGER THOMAS , SCHULT SABINE
    • A61P35/00 , C07D487/06 , A61K31/437 , A61K31/55 , C07D471/06
    • Azepinoindole derivatives are new. The azepinoindole derivatives of formula (I) and their tautomers, enantiomers, diastereomers, salts and prodrugs are new: A = 1-3C chain optionally substituted on each C by 1 or 2 1-4C alkyl, OH, 1-4C alkoxy, COOH, COO-1-4C alkyl or phenyl or optionally substituted with 1 oxo; X = S, O, or NH; X = C optionally carrying a 1-4C chain; or N; X = N, or CR ; R = H, 1-6C alkyl, phenyl-1-4C alkyl, or phenyl; R = H, Cl, Br, I, 1-6C alkyl, OH, NO2, CF3, CN; NR R , NHCOR , or 1-4C alkoxy; R , R = H or 1-4C alkyl; R = H, 1-4C alkyl, phenyl-1-4C alkyl, or phenyl; B = an unsaturated, saturated or partly unsaturated mono-, bi- or tricyclic ring with up to 15C which (a) optionally contains up to 5 N atoms or 1 or 2 O or S atoms when it has up to 14C, (b) is substituted with 1 R and up to 3 R ; and (c) is optionally substituted with =O on 1 or 2 C or S atoms; R = -(D)p-(E)s-(F )q-G -(F )r-(G )-G ; G = a bond or an unsaturated, saturated or partly unsaturated mono-, bi- or tricyclic ring with up to 15C which (a) optionally contains up to 5 N atoms or 1 or 2 O or S atoms when it has up to 14C, (b) is substituted with up to 3 R ; and (c) is optionally substituted with =O on 1 or 2 C or S atoms; G = NR R , a bond; or pyrrolidin-1-yl, piperidin-1-yl, 1,2,5,6-tetrahydropyridin-1-yl, 4-R -piperazin-1-yl, 4-R -1,4-diazepin-1-yl, azepin-1-yl or morpholin-1-yl (each ring-substituted with R ); G = H; or an unsaturated, saturated or partly unsaturated mono-, bi- or tricyclic ring with up to 15C which (a) optionally contains up to 5 N atoms or 1 or 2 O or S atoms when it has up to 14C, (b) is substituted with up to 3 R ; and (c) is optionally substituted with =O on 1 or 2 C or S atoms; D = S, NR , or O; E = phenyl, -C(O)-, -SO2-, -SO2NH-, -NHCO-, -CONH-, -NHSO2-, or -NHCOCH2X -; X = S, O, or NH; F , F = saturated or unsaturated 1-8C chain; p, q, r and s = 0 or 1; R = H, 1-6C alkyl optionally substituted on each C with 1 or 2R , phenyl optionally substituted with 1 or 2 R , or (CH2)t-K; R = H, 1-6C alkyl, COR , CO2R , SO2NH2, SO2R8, -(C=N)-R , or -(C=N)-NHR ; R = H or 1-4C alkyl; t = 1-4; K = NR R , NR -(1-4C alkyl)-phenyl, pyrrolidinyl, piperidinyl, 1,2,5,6-tetrahydropyridinyl, morpholinyl, homopiperidinyl, or piperazinyl or homopipearzinyl (each optionally substituted with 1 1-6C alkyl); R = H, Cl, F, Br, I, OH, NO2, CF3, CN; NR R , NHCOR , (1-4C alkyl)-CONHR , COR , (0-4C alkyl)-OCOR , phenyl-1-4C alkyl; phenyl, CO2-1-4C alkyl, or saturated or unsaturated 1-6C alkyl, 1-4C alkoxy or 1-4C alkylthio (each optionally substituted with 1 or 2 R ); R = H, Cl, F, Br, I, 1-6C alkyl, OH, NO2, CF3, CN, NR R , NHCOR , or 1-4C alkoxy; R = H, 1-6C alkyl, phenyl optionally substituted with 1-3 Q, NR R , or a saturated 3-7 membered cyclic amino group or homopiperazinyl (each optionally substituted with 1 1-6C alkyl); Q = OH, 1-6C alkyl, 1-4C alkoxy, Cl, Br, I, F, CF3, NO2, or NH2; R = 1-6C alkyl, CF3, phenyl, or phenyl-1-4C alkyl optionally substituted with 1 or 2 Q; R = H, 1-6C alkyl, Ph-1-4C alkyl, CO2-(1-4C alkyl)-Ph, CO2-1-4C alkyl, SO2-Ph, COR , or Ph; Ph = phenyl optionally substituted 1 or 2 Q; compounds are excluded when: (a) X = X = N; (b) G = G = G = H or a bond; and (c) two of G -G = H or a bond when p = s = 0 and q or r = 1 or p. q and r = 0.
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