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    Serotonin antagonists 3-substituted tetrahydropyridopyrimidinone derivatives for treating 5HT, depression and related disorders
    103.
    发明专利
    Serotonin antagonists 3-substituted tetrahydropyridopyrimidinone derivatives for treating 5HT, depression and related disorders 未知

    公开(公告)号：NZ503486A

    公开(公告)日：2001-04-27

    申请号：NZ50348698

    申请日：1998-10-05

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  DULLWEBER UTA ,  STARCK DOROTHEA ,  STEINER GERD ,  BACH ALFRED ,  EMLING FRANZ ,  GARCIA-LADONA XAVIER ,  TESCHENDORF HANS-JURGEN ,  WICKE KARSTEN

    IPC: A61K31/519 ,  A61P1/00 ,  A61P1/14 ,  A61P3/04 ,  A61P5/00 ,  A61P9/12 ,  A61P15/00 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D471/00 ,  C07D471/04 ,  C07D295/04

    Abstract: A 3-substituted tetrahydropyridopyrimidione derivative of the formula shown as a therapeutic composition having a high affinity for 5-HT1B, 5-HT1D and 5-HT1A serotonin receptors. The compounds are suitable for treating pathological states in which the serotonin concentration is reduced such as depression, mood disturbances with central nervous causation (dysthymia), anxiety such as panic attacks, sociophobia, obsessive-compulsive neuroses and post-traumatic stress symptoms, memory disturbances such as dementia, amnesias and age-related loss of memory and psychogenic eating disorders such as anorexia nervosa and bulimia nervosa. Wherein; one of the two radicals X and Y is CH2 and the other is NR1, R1 is hydrogen, C1-6alkyl branched or unbranched, CO-C1-4alkyl, CO2tBu, CO-phenyl and a phenylalkyl-C1-4 radical which in turn may be substituted on the aromatic system by F, Cl, Br, I, C1-4alkyl, C1-4alkoxy, trifluoromethyl, hydroxyl, amino, cyano or nitro, A is branched or unbranched C1-10alkylene or straight-chain or branched C2-10alkylene which comprises at least one group Z which is selected from O, S, NR2, cyclopropyl, CO2, CHOH, a double or triple bond, R2 is hydrogen and C1-4alkyl, B is 4-piperidine, 4-tetrahydro-1,2,3,6 pyridine, 4-piperazine or the corresponding cyclic compounds enlarged by one methylene group, with the linkage to A being via an N atom of B, and Ar is phenyl which is unsubstituted or substituted by C1-6alkyl branched or unbranched, O-C1-6alkyl branched or unbranched, OH, F, Cl, Br, I, trifluoromethyl, NR22, CO2R2, cyano or phenyl, or is tetralin, indan, naphthalene which is unsubstituted or substituted by C1-4alkyl or O-C1-4alkyl, anthracene or 5- or 6-membered aromatic heterocycles having 1 or 2 heteroatoms which are selected, independently of one another, from O and N.

    DERIVADOS DE 3,4,5,7-TETRAHIDRO-PIRROLO(3´, 4´:4,5)-TIENO [2,3-d] PIRIMIDINA 3-SUSTITUIDOS
    107.
    发明专利
    DERIVADOS DE 3,4,5,7-TETRAHIDRO-PIRROLO(3´, 4´:4,5)-TIENO [2,3-d] PIRIMIDINA 3-SUSTITUIDOS 未知

    公开(公告)号：CO4960665A1

    公开(公告)日：2000-09-25

    申请号：CO98045546

    申请日：1998-08-10

    Applicant: BASF AG

    Inventor： STEINER GERD ,  UTA DULLWEBER ,  DOROTHEA STARCK ,  BACH ALFRED ,  KARSTEN WICKE ,  TESCHENDORF HANS-JURGEN ,  EMLING FRANZ

    IPC: A61K31/38 ,  A61K31/395 ,  A61K31/435 ,  A61K31/505 ,  A61P25/24 ,  C07D495/14

    Abstract: Derivados de 3,4,5,7- tetrahidro-pirrolo[3´,4´5]-tieno[2,3-d]pirimidina 3-sustituidos de la fórmula I donde R1 significa un átomo de hidrógeno, un grupo C1 -C4 -alquilo, un grupo acetilo, un radical fenilalquilo C1 -C4 , pudiendo el aromático estar sustituido, eventualmente, por halógeno, un grupo C1 -C4 -alquilo, trifluorometilo, hidroxi, C1 -C4 -alcoxi, amino, ciano o nitro, o un radical de carboxilato de C1 -C3 -alquilo, R2 significa un grupo fenilo, pirrodilo, pirimidinilo o piracinilo eventualmente mono o disustituido por átomos de halógeno, grupos C1 -C4 - alquilo, trifluorometilo, trifluorometoxi, hidroxi, C1 -C4 -alcoxi, amino, monometilamino, dimetilamino, ciano o nitro, que puede estar anelado con un núcleo benceno que puede estar mono o disustituido, eventualmente por átomos de halógeno, grupos C1 -C4 - alquilo, hidroxi, trifluorometilo, C1 -C4 -alcoxi, amino, ciano o nitro y que puede contener, eventualmente, un átomo de nitrógeno, o que puede estar anhelado con un anillo de cinco o seis miembros que puede contener 1 a 2 átomos de oxígeno, A representa NH o un átomo de oxígeno, Y significa CH2 , CH2 -CH2 , CH2 -CH2 -CH2 o bien CH2 -CH, Z significa un átomo de nitrógeno, un átomo de carbono o CH, pudiendo el enlace entre Y y Z también puede ser un doble enlace, y n representa los números 2, 3 ó 4 y sus sales con ácidos fisiológicamente tolerados.

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