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    3-SUBSTITUTED PYRIDO [3',4': 4,5] THIENO [2,3-D] PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND USE
    42.
    发明专利
    3-SUBSTITUTED PYRIDO [3',4': 4,5] THIENO [2,3-D] PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND USE 未知

    公开(公告)号：MY132993A

    公开(公告)日：2007-10-31

    申请号：MYPI9802644

    申请日：1998-06-13

    Applicant: BASF AG

    Inventor： BACH ALFRED ,  STARCK DOROTHEA DR ,  GARCIA-LADONA FRANCISCO-JAVIER ,  EMLING FRANZ ,  STEINER GERD DR ,  TESCHENDORF HANS-JURGEN ,  WICKE KARSTEN ,  DULLWEBER UTA

    IPC: A61K31/495 ,  A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14

    Abstract: 3-SUBSTITUTED 3,4,S,6,7,8-HEXAHYDROPYRIDO [3',4':4,5]-THIENO[2,3-D]PYRIRNIDINE DERIVATIVES OF THE FORMULA I WHERE RL IS A HYDROGEN ATOM, A CL-C4-ALKYL GROUP, AN ACETYL GROUP, A PHENYLALKYL CL-C4 RADICAL, THE AROMATIC SYSTEM BEING UNSUBSTITUTED OR SUBSTITUTED BY HALOGEN, CL-C4-ALKYL, TRIFLUOROMETHYL, HYDROXYL, CL-C4-ALKOXY, AMINO, CYANO OR NITRO GROUPS, OR IS A PHENYLALKANONE RADICAL, IT BEING POSSIBLE FOR THE PHENYL GROUP TO BE SUBSTITUTED BY HALOGEN, R2 IS A PHENYL, PYRIDYL, PYRIMIDINYL OR PYRAZINYL GROUP WHICH IS UNSUBSTITUTED OR'MONO- OR DISUBSTITUTED BY HALOGEN ATOMS, CL-C4-ALKYL, TRIFLUOROMETHYL, TRIFLUOROMETHOXY, HYDROXYL, CL-C4- ALKOXY, AMINO, MONOMETHYLAMINO, DIMETHYLAMINO, CYANO OR NITRO GROUPS AND WHICH MAY BE FUSED TO A BENZENE NUCLEUS WHICH CAN BE UNSUBSTITUTED OR MONO- OR DISUBSTITUTED BY HALOGEN ATOMS, CL-C4 ALKYL, HYDROXYL, TRIFLUOROMETHYL, CL-C4-ALKOXY, AMINO, CYANO OR NITRO GROUPS AND MAY CONTAIN 1 NITROGEN ATOM, OR TO A 5- OR 6-MEMBERED RING WHICH MAY CONTAIN 1-2 OXYGEN ATOMS, A IS NH OR AN OXYGEN ATOM, Y IS CH2, CH2-CH2, CH2-CH2-CH2 OR CH2-CH, Z IS A NITROGEN ATOM, CARBON ATOM OR CH, IT ALSO BEING POSSIBLE FOR THE LINKAGE BETWEEN Y AND Z TO BE A DOUBLE BOND, AND N IS 2, 3 OR 4, AND THE PHYSIOLOGICALLY TOLERATED SALTS THEREOF.

    3-Substituted 3,4-dihydrothieno[2,3-d]pyrimidine derivatives, process of their preparation and use
    43.
    发明专利
    3-Substituted 3,4-dihydrothieno[2,3-d]pyrimidine derivatives, process of their preparation and use 未知

    公开(公告)号：CZ290464B6

    公开(公告)日：2002-07-17

    申请号：CZ443199

    申请日：1998-05-29

    Applicant: BASF AG

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

    IPC: A61K31/495 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/04

    Abstract: In the present invention there are disclosed 3-substituted 3,4-dihydrothieno[2,3-d]pyrimidine derivatives of the general formula I, in which Re1 and Re2 represent a hydrogen atom or an alkyl group containing 1 to 4 carbon atoms, Re3 represents a phenyl, pyridyl, pyrimidinyl or pyrazinyl group, which can be optionally mono- or disubstituted with a halogen atom or with the following groups; alkyl containing 1 to 4 carbon atoms, trifluoromethyl, trifluoromethoxy, hydroxy, alkoxy containing 1 to 4 carbon atoms, amino, monomethylamino, dimethylamino, cyano or nitro and which can be condensed with a benzene nucleus that can be optionally mono- or disubstituted with a halogen atom or with the following groups; alkyl containing 1 to 4 carbon atoms, hydroxy, trifluoromethyl, alkoxy containing 1 to 4 carbon atoms, amino, cyano or nitro and which can optionally contain 1 nitrogen atom, or with 5- or 6-membered ring that can contain 1 to 2 oxygen atoms, A represents NH or an oxygen atom, Y represents CHi2, CHi2-CHi2, CHi2-CHi2-CHi2 or CHi2-CH, Z represents a nitrogen atom, a carbon atom or CH, whereby the bond between Y and Z can be also a double bond and n is 2, 3 or 4, and their physiologically acceptable salts. The invented derivatives are intended for treating depressions and related disorders with activity as selective antagonist 5-HTi1B and 5-HTi1A.

    3-substituted pyrido {3',4':4,5} thieno {2,3-D} pyrimidine derivatives, and production and use of the same
    45.
    发明专利
    3-substituted pyrido {3',4':4,5} thieno {2,3-D} pyrimidine derivatives, and production and use of the same 未知

    公开(公告)号：AU748697B2

    公开(公告)日：2002-06-13

    申请号：AU8535798

    申请日：1998-05-29

    Applicant: BASF AG

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

    IPC: A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14

    Abstract: PCT No. PCT/EP98/03231 Sec. 371 Date Dec. 8, 1999 Sec. 102(e) Date Dec. 8, 1999 PCT Filed May 29, 1998 PCT Pub. No. WO98/56793 PCT Pub. Date Dec. 17, 19983-Substituted 3,4,5,6,7,8-hexahydropyrido [3',4':4,5]-thieno[2,3-d]pyrimidine derivatives of the formula I where R1 is a hydrogen atom, a C1-C4-alkyl group, an acetyl group, a phenylalkyl C1-C4 radical, the aromatic system being unsubstituted or substituted by halogen, C1-C4-alkyl, trifluoromethyl, hydroxyl, C1-C4-alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen, R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4-alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which can be unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, hydroxyl, trifluoromethyl, C1-C4-alkoxy, amino, cyano or nitro groups and may contain 1 nitrogen atom, or to a 5- or 6-membered ring which may contain 1-2 oxygen atoms, A is NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is a nitrogen atom, carbon atom or CH, it also being possible for the linkage between Y and Z to be a double bond, and n is 2, 3 or 4, and the physiologically tolerated salts thereof.

    3-substituted pyrido [3',4':4,5] thieno [2,3-d] pyrimidine derivatives for treating 5-HT1B/D receptor related disorders which increases serotonin release in the brain
    47.
    发明专利
    3-substituted pyrido [3',4':4,5] thieno [2,3-d] pyrimidine derivatives for treating 5-HT1B/D receptor related disorders which increases serotonin release in the brain 未知

    公开(公告)号：NZ502237A

    公开(公告)日：2001-08-31

    申请号：NZ50223798

    申请日：1998-05-29

    Applicant: BASF AG

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

    IPC: A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14

    Abstract: A 3-substituted 3,4,5,6,7,8-hexahydropyrido[3',4':4,5]thieno-[2,3-d]pyrimidine derivative of the formula described useful for treating pathological states in which the serotonin concentration is reduced by specifically blocking the activity of the presynaptic 5-HT1B, 5-HT1A, 5-HT1D receptors. The compounds are useful for treating mood disorders with a central nervous causation, such as seasonal affective disorders and dysthymia, including anxiety states disorders, sociophobia, obsessive-compulsive neuroses, post traumatic stress symptoms, memory disturbances, age-related memory loss, and psychogenic eating disorders. Wherein; R1 is a hydrogen atom, a C1-4alkyl group, an acetyl group, a phenylalkylC1-4 radical, the aromatic system being unsubstituted or substituted by halogen, C1-4alkyl, trifluoromethyl, hydroxyl, C1-4alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen; R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C1-4alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-4alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which can be unsubstituted or mono- or disubstituted by halogen atoms, C1-4alkyl, hydroxyl, trifluoromethyl, C1-4alkoxy, amino, cyano or nitro groups and may contain 1 nitrogen atom, or to a 5- or 6-membered ring which may contain 1-2 oxygen atoms A is NH or an oxygen atom; Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH; Z is a nitrogen atom, carbon atom or CH, it also being possible for the linkage between Y and Z to be a double bond; and n is 2, 3 or 4.

    DERIVADOS DE 1,2, BENZISOTIAZOL 2-SUSTITUIDOS, SU OBTENCION Y USO
    50.
    发明专利
    DERIVADOS DE 1,2, BENZISOTIAZOL 2-SUSTITUIDOS, SU OBTENCION Y USO 未知

    公开(公告)号：CO4980863A1

    公开(公告)日：2000-11-27

    申请号：CO98060934

    申请日：1998-10-20

    Applicant: BASF AG

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

    IPC: A61K31/40 ,  A61K31/425 ,  A61K31/428 ,  A61K31/495 ,  A61P25/24 ,  A61P43/00 ,  C07D275/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

    Abstract: Derivados de 1,2-benzisotiazol 2 sustituidos, de lafórmula (1)donde R1 , R2 significan, cada uno independientemente del otro, (C1-6 )alquilo, R3 , R4 significan, cada uno independientemente del otro, hidrógeno, (C1-6 )alquilo ramificado o sin ramificar, OH, O-(C1-6 )-alquilo ramificado o sin ramificar, F, Cl, Br, Y, trifluorometilo, NR5 R6 , CO2 R7 , nitro, ciano, pirrol, un radical fenilalquilo con 1 a 4 átomos de carbono, que a su vez puede estar sustituido en el aromático por F, Cl, Br, Y, C1 -C4 alquilo, C1 -C4 alcoxi, trifluorometilo, hidroxi, amino, ciano o nitro, R5 , R6 significan, cada uno independientemente de otro, hidrógeno, (C1-6 ) alquilo ramificado o sin ramificar, COPh, CO2 tBu, CO-(C1-4 ) alquilo o forman juntos un anillo de 5 ó 6 miembros, que eventualmente contiene otro nitrógeno (p. ej. piperacina), R7 significa hidrógeno y (C1-6 )alquilo ramificado o sin ramificar, A significa un (C1-6 )alquilo ramificado o sin ramificar, o un (C2-10 )-alquileno lineal o ramificado, que comprende al menos un gupo Z, que está seleccionado de entre O, S, NR7 ciclopropilo, CHOH, o un doble o triple enlace,B significa 4-piperidina, 4-tetrahidro-1,2,3,6 piridina, -4-piperacina y los compuestos anulares correspondientes ampliados por un grupo metileno, realizándose el enlace entre A y B por vía del átomo de nitrógeno, y Ar significa fenilo, que eventualmente está sustituido por (C1-6 )alquilo ramificado o sin ramificar, O-(C1-6 )-alquilo ramificado o sin ramificar, OH, F, Cl, Br, Y, trifluorometilo, NR5 R6 , CO2 R7 , ciano o fenilo, tetralina, indano, aromáticos de alto gado de condensación, como p. ej. naftalina, que eventualmente está sustituida por (C1-6 )alquilo o O(C1-4 )alquilo, antraceno o heterociclos aromáticos de 5 ó 6 miembros con uno a dos heteroátomos, seleccionados independientemente de O y N, y que pueden estar fusionados con otros radicales aromáticos, y sus enantiómeros y diastereómeros, sus formas tautómeras, asi como sus sales con ácido fisiológicamente tolerados.

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