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

    公开(公告)号：BG63602B1

    公开(公告)日：2002-06-28

    申请号：BG10312299

    申请日：1999-01-27

    Applicant: BASF AG

    Inventor： STEINER GERD ,  LUBISCH WILFRIED ,  BACH ALFRED ,  EMLING FRANZ ,  WICKE KARSTEN ,  TESCHENDORF HANS-JUERGEN ,  BEHL BERTHOLD ,  KERRIGAN FRANK ,  CHEETHAM SHARON

    IPC: A61K31/435 ,  A61K31/519 ,  A61P25/24 ,  A61P43/00 ,  C07D211/00 ,  C07D239/00 ,  C07D333/00 ,  C07D495/14

    Abstract: The 3-substituted 3,4,5,6,7.8-hexahydro-pyrido[4', 3': 4,5]-thieno [2,3-d] pyrimidine derivatives can be used as medicamentous forms for diseases where there is redud serotonin concentration and where, within the therapy, the activity of the presnaptic receptors 5-HT1B-, 5-HT1A-, 5-HT1D-, should be blocked without seriously affecting any other receptors. Depression is an example for such morbid state. The compounds have formula in which R1 is hydrogen, C1-C4-alkyl group, acetyl, benzoyl, phenylalkyl-C1-C4-residue where the aromatic residue is optionally substituted with halogen, C1-C4-alkyl, trifluoromethyl, hydroxy-, C1-C4-alkoxy-, amino-, cyano- or nitrogroups or is naphtalene-C1-C4-alkyl residue, phenylalkanon-C2-C4-residue or phenylcarbamoylalkyl-C2-residue where the phenyl group can be substituted by halogen; R2 optionally is mono-, di- or trisubstituted with halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluormethoxy, hydroxy, C1-C4-alkoxy, amino-, monomethylamino-, diethylamino-, cyano- or nitrogroup, phenyl, pyridyl, pyrimidinyl or pyrasinyl reside which can optionally be ringed by one benzene ring which optionally can be mono- or disubstituted with halogen atom, C1-C4-alkyl, hydroxy, trifluormethyl, C1-C4-alkoxy, amino-, cyano- or nitrogroup, and optionally can contain one nitrogen atom or be ringed by 5- or 6-member ring which can contain one to two oxygen atoms, or can be substituted by phenyl-C1-C2-alkyl, or alkoxygroup, respectively, where the phenyl residue can be substituted with halogen, methyl, trifluormethyl or methoxygroup. A is NH or oxygen, B is hydrogen or methyl, C is hydrogen, methyl or hydroxy, X is nitrogen atom, Y is the group CH2, CH2- CH2, CH2-CH2-CH2 or CH2-CH, Z is nitrogen atom, carbon or CH where the bond between Y and Z can be double, n has the value of 2, 3 or 4. The invention also relates to physiologically acceptable salts of the above compounds. 6 claims

    3-Substituted 3,4,5,7-tetrahydropyrrolo[3',4':4,5]thieno[2,3-d]pyrimidine derivatives, their preparation and use as 5HT antagonists
    8.
    发明专利
    3-Substituted 3,4,5,7-tetrahydropyrrolo[3',4':4,5]thieno[2,3-d]pyrimidine derivatives, their preparation and use as 5HT antagonists 未知

    公开(公告)号：NZ502657A

    公开(公告)日：2001-06-29

    申请号：NZ50265798

    申请日：1998-07-23

    Applicant: BASF AG

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

    IPC: A61K31/435 ,  A61P25/24 ,  C07D495/14

    Abstract: A 3-substituted 3,4,5,7-tetrahhydropyrrolo[3',4':4,5]-thieno[2,3-d]pyrimidine derivative of the formula I, wherein, R1is a hydrogen atom, a C1-C4 alkyl group, an acetyl group, a phenylalkyl c1-c4 radical where the aromatic ring is unsubstituted or substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxyl, C1-C4 alkoxy, amino, cyano or nitro groups, or is a C1-C3 alkyl carboxylate radical, 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, monoethylamino, dimethylamino, cyano or nitro groups, and may be fused to a benzene nucleus which may be 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, where the linkage between Y and Z may also be a double bond, and n is 2,3 or 4, or a physiologically tolerated salt thereof. These compounds are useful as selective 5HT1B and/or 5HT1A antagonists.

    DERIVADOS DE TETRAHIDROPIRIDOPIRIMIDINONA 3-SUSTITUIDOS .
    9.
    发明专利
    DERIVADOS DE TETRAHIDROPIRIDOPIRIMIDINONA 3-SUSTITUIDOS . 未知

    公开(公告)号：CO4980862A1

    公开(公告)日：2000-11-27

    申请号：CO98061508

    申请日：1998-10-22

    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: A61K31/505 ,  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

    Abstract: Derivados de tetrahidropiridopirimidinona 3-sustituidos de la fórmula (I)caracterizados porque uno de los radicales X, Y significa CH2 y el otro significa NR1 , R1 significa hidrógeno, (C1-6 ) alquilo ramificado o sin ramificar, CO-(C1-4 )-ALQUILO, CO2 -tBu, CO-arilo y un radical fenilalquilo C1-4 , 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. A Significa (C1 -10 )-alquiteno ramificado o sin ramificar, (C2 -10 )-alquileno lineal o ramificado, que comprende al menos un grupo 2, seleccionado de entre 0, S. NR2 ciclopropilo, CHOH, un enlace doble o triple, R2 significa hidrógeno y C1 -C4 alquilo B significa 4-piperidina, 4-tetrahidro- 1,2,3,6 piridina, 4-piperacina y los compuestos anulares correspondientes, amplios por un grupo metileno, realizándose el enlace entre A y B por vía de un átomo de N, 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, I, trifluorometilo, NR2 2 , CO2 R2 , ciano o fenilo, tetralina, indano, aromáticos de alto grado de condensación como p. ej. naftalina, que eventualmente está sustituida por (C1-4 )-alquilo o O(C1-4 )-alquilo, entraceno o heterociclos aromáticos de 5 ó 6 miembros con 1 a 2 heteroátomos, heteroátomos seleccionados independientemente de entre O y N, y que pueden estar aún fusionados con otros radicales aromáticos, así como sus sales con ácidos fisiológicamente tolerados.

    10.
    发明专利
    未知

    公开(公告)号：BR9810017A

    公开(公告)日：2000-09-19

    申请号：BR9810017

    申请日：1998-05-29

    Applicant: BASF AG

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

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

    Abstract: PCT No. PCT/EP98/03230 Sec. 371 Date Dec. 6, 1999 Sec. 102(e) Date Dec. 6, 1999 PCT Filed May 29, 1998 PCT Pub. No. WO98/56792 PCT Pub. Date Dec. 17, 19983-Substituted 3,4-dihydrothieno[2,3-d]pyrimidine derivatives of the formula I where R1 and R2 are a hydrogen atom or a C1-C4-alkyl group, R3 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 may 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 being possible for the linkage between Y and Z also to be a double bond, and n is 2, 3 or 4, and the physiologically tolerated salts thereof.

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