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    BENZIMADAZOLES SUSTITUIDOS POR CICLOALQUILO, SU OBTECION Y SU USO
    71.
    发明专利
    BENZIMADAZOLES SUSTITUIDOS POR CICLOALQUILO, SU OBTECION Y SU USO 未知

    公开(公告)号：CO5170500A1

    公开(公告)日：2002-06-27

    申请号：CO00028650

    申请日：2000-04-18

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  KOCK MICHAEL ,  HOGER THOMAS ,  GRANDEL ROLAND ,  SCHULT SABINE ,  MULLER REINHOLD

    IPC: C07D235/08 ,  A61K31/165 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/496 ,  A61K31/551 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P19/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D401/08 ,  C07D403/08

    Abstract: Compuestos de las fórmulas I ó II: dondeA significa un carbociclo saturado o monoinsaturado con 3 a 8 átomos de carbono, que pueden tener adicionalmente un anillo benceno condensado, cuyos anillos pueden estar sustituidos adicionalmente por uno o dos radicales R3 idénticos o diferentes, así como el radical R4, yR1 hidrógeno, cloro, fluoro, bromo, yodo, C1-C6-alquilo ramificado y sin ramificar, OH, nitro, CF3, CN, NR11R12, NH-CO-R13, O-C1-C4-alquilo, significando R11 y R12, cada uno independientemente del otro, hidrógeno o C1-C4-alquilo yR13 hidrógeno, C1-C4-alquilo, C1-C4-alquil-fenilo o fenilo,YR2 significa hidrógeno, C1-C6-alquilo ramificado y sin ramificar, C1-C4-alquilo, fenilo yR3 significa C1-C6-alquilo, OH, O-C1-C4-alquilo, OC1-C4-alquil-fenilo, NR11R12, fenilo, C1-C4-alquil-fenilo, CF3, COOH, COOC1-C4-alquilo, CONH-C1-C4-alquilo, CONH2, pudiendo los anillos fenilo estar sustituidos aún por, como máximo, dos radicales R31 idénticos o diferentes, yR31 significa OH, C1-C6-alquilo, OC1-C4-alquilo, cloro, bromo, yodo, fluoro, CF3, nitro, NH2, y R4 significa -(O)p.(CH2)q-B, dondeB es NR41R42 SignificandoP 0 y 1 yq 0, 1, 2 ó 3, pudiendo, cuando q = 0 p también ser igual a 0, y- 2 -R41 significa hidrógeno, C1-C6-alquilo, (CH2)r-E yR42 significa hidrógeno, C1-C6-alquilo, -CO-R8, SO2-R8, -(C=N)-R8 y -(C=N)- NHR8 yr es 0,1,2,3,4 yE significa fenilo, que puede llevar aún, como máximo dos radicales R72, y, cuando r ? 0, 1, también NR11R12, NH-C1-C4-alquil-fenilo, pirrolidina, piperidina, dihidropiperidina, morfolina, homopiperidina, piperacina, que puede estar sustituída aún por C1-C6-alquilo y C1-C6-alquil-fenilo, y homopiperacina, que puede estar sustituída aún por C1-C6-alquilo y C1-C4-alquil-fenilo, yR7 significa hidrógeno, C1-C6-alquilo, fenilo, pudiendo el anillo estar sustituido aún por hasta dos radicales R71 idénticos o diferentes, yR71 significa OH, C1-C6-alquilo, O-C1-C4-alquilo, cloro, bromo, yodo, fluoro, CF3, nitro, NR11R12, yR72 significa OH, C1-C6-alquilo, O-C1-C4-alquilo, cloro, bromo, yodo, fluoro, CF3, nitro, NR11R12, yR8 significa C1-C6-alquilo, fenilo, C1-C4-alquil-fenilo, pudiendo el anillo estar sustituído aún por hasta dos radicales R81 idénticos o diferentes, yR81 significa OH, C1-C6-alquilo, O-C1-C4-alquilo, cloro, bromo, yodo, fluoro, CF3, nitro, NR11R12, yR9 significa hidrógeno, C1-C6-alquilo, C1-C4-alquil-fenilo, fenilo, pudiendo el anillo estar sustituido aún por hasta dos radicales R91 idénticos o diferentes, y R91 significa OH, C1-C6-alquilo, O-C1-C4-alquilo, cloro, bromo, yodo, fluoro, CF3, nitro NR11R12,así como sus formas tautómeras, sus formas enantiómeras y diastereómeras posibles, los isómeros cis.-trans en los anillos A y sus prodrogas.

    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
    74.
    发明专利
    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

    公开(公告)号：DE10039610A1

    公开(公告)日：2002-02-28

    申请号：DE10039610

    申请日：2000-08-09

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  GRANDEL ROLAND ,  KOCK MICHAEL ,  MUELLER REINHOLD ,  HOEGER THOMAS ,  SCHULT SABINE

    IPC: A61P35/00 ,  C07D487/06 ,  A61K31/437 ,  A61K31/55 ,  C07D471/06

    Abstract: 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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