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    2-SUBSTITUTED 1,2-BENZISOTHIAZOLE DERIVAYIVES AND THEIR USE AS SEROTONIN ANTAGONISTS (5-HT1A, 5-HT1B AND 5-HT1D)
    34.
    发明专利
    2-SUBSTITUTED 1,2-BENZISOTHIAZOLE DERIVAYIVES AND THEIR USE AS SEROTONIN ANTAGONISTS (5-HT1A, 5-HT1B AND 5-HT1D) 未知

    公开(公告)号：BG104332A

    公开(公告)日：2001-02-28

    申请号：BG10433200

    申请日：2000-04-11

    Applicant: BASF AG

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

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

    Abstract: The invention relates to 2-substituted 1,2-benzisothiazole derivatives of formula wherein R1 and R2 represent (C1-C6) alkyl, independently of each other; A represents branched or unbranched (C1-10)-alkylene or straight-chained or branched (C2-10)-alkylene comprising at least one group Z which is selected from O, S, NR7, cyclopropyl, CHOH, a double or triple bond; B represents 4-piperidine, 4-tetrahydro-1, 2, 3, 6 pyridine, 4-piperazine and the corresponding ring compounds enlarged with a methylene group, an N-atom of B providing the link with A; Ar represents phenyl which is optionally substituted by (C1-6) alkyl -branched or unbranched-, O-(C1-6)-alkyl-branched or unbranched-, FH, F, Cl, Br, I, fluoromethyl, NR5R6, CO2R7, cyano or phenyl; tetralin, indan, highly condensed aromatics such as naphthalin optionally substituted by (C1-4) alkyl or O(C1-4) alkyl, anthracene or 5- or 6-membered aromatic heterocyclene with 1 to 2 heteroatoms which are selected independently of each other from O and N and which can still be anellated with further aromatic radicals such as quinoline, isoquinoline, phthalazine, indole and quinazoline which can itself be substituted again with phenyl; and R3 and R4 have the meanings given in the description. The invention also relates to the production of the inventive derivatives and to their use as serotonin antagonists. 7 claims

    3-substituted 3,4 dihydro-thieno[2,3-d]pyrimidine for treating depression
    35.
    发明专利
    3-substituted 3,4 dihydro-thieno[2,3-d]pyrimidine for treating depression 未知

    公开(公告)号：NZ502238A

    公开(公告)日：2001-02-23

    申请号：NZ50223898

    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: 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.

    DERIVADOS DE PIRIDO [3 ,4 :4,5] TIENO [2,3-D]PIRIMIDINA 3-SUSTITUIDOS Y SU OBTENCION
    36.
    发明专利
    DERIVADOS DE PIRIDO [3 ,4 :4,5] TIENO [2,3-D]PIRIMIDINA 3-SUSTITUIDOS Y SU OBTENCION 未知

    公开(公告)号：CO4940481A1

    公开(公告)日：2000-07-24

    申请号：CO98033543

    申请日：1998-06-11

    Applicant: BASF AG

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

    IPC: A61K31/38 ,  A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14

    Abstract: Derivados de 3,4,5,6,7,8- hexahidro-pirido [3´, 4´: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, grupos C1 -C4 -alquilo, trifluorometilo, hidroxi, C1 -C4 -alcoxi, amino-, ciano o nitro, o un radical fenilalcanona, pudiendo el grupo fenilo estar sustituido por halógeno.R2 significa un grupo fenilo, piridilo, pirimidinilo o piracinilo eventualmente mono o disustituido por átomos de halógeno, C1 -C4 -alquilo, trifluorometilo, trifluorometoxi, hidroxi, C1 -C4 -alcoxi, amino-, monometilamino, dimetilamino, ciano o nitro, que puede estar anhelado con un núcleo benceno, que eventualmente está mono o disustituido por átomos de halógeno, C1 -C4 -alquilo, hidroxi, trifluorometilo C1 -C4 -alcoxi, amino, ciano- o nitro y contiene, eventualmente, un átomo de nitrógeno, o con un anillo de cinco o seis miembros que puede contener 1-2 átomos de oxígeno,A significa NH o un átomo de oxígeno, Y es CH2 , CH2 -CH2 , CH2 -CH2 -CH2 ó CH2 -CH,Z significa un átomo de nitrógeno, un átomo de carbono o CH, pudiendo el enlace entre Y y Z ser también un doble enlace, y n representa la cifra 2, 3 ó 4, así como sus sales con ácidos fisiológicamente toleradas.

    Control of cocaine addiction comprises administration of N-substituted azabicycloalkane derivative
    38.
    发明专利
    Control of cocaine addiction comprises administration of N-substituted azabicycloalkane derivative 未知

    公开(公告)号：DE19854147A1

    公开(公告)日：2000-05-25

    申请号：DE19854147

    申请日：1998-11-24

    Applicant: BASF AG

    Inventor： STEINER GERD ,  MUNSCHAUER RAINER ,  GROSS GERHARD ,  TRAUT MARTIN ,  UNGER LILIANE ,  TESCHENDORF HANS-JUERGEN

    IPC: C07D403/06 ,  A61K31/403 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/424 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/542 ,  A61P25/00 ,  A61P25/28 ,  A61P25/30 ,  A61P25/36 ,  C07D209/52 ,  C07D407/12 ,  C07D409/12 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/415 ,  A61K31/425

    Abstract: Use of N-substituted 3-azabicycloalkane derivatives (I) and their salts for the control of cocaine addiction is new. Use of N-substituted 3-azabicycloalkane derivatives of formula (I) and their salts for the control of cocaine addiction is new. B = 4-6 membered ring optionally containing a double bond; R1 = phenyl, naphthyl, phenanthryl or thienyl optionally mono- or disubstituted by halo, 1-4C alkyl, CF3, OH, 1-4C alkoxy, NH2, NHCH3, N(CH3)2; CN or NO2; R2 = naphthyl optionally mono- or disubstituted by halo; -C(R3)(R4)(R5); -NR6-C(O)-R7; -NR6-SO2-Q; -NR6-C(S)-Q; -O-C(O)-Q; -O-Q; or a group of formula (a)-(k): Q = phenyl optionally monosubstituted by F, Cl, 1-4C alkyl, OCH3 or NH2; R3 = H; OH; or phenyl optionally monosubstituted by F, Cl or Br; R4 = H; or R3+R4 = oxo; R5 = phenyl, naphthyl or thienyl optionally mono- or disubstituted by F, Cl, Br, OH, NO2, NH2, NH(1-4C alkanoyl), NH(1-4C alkyl), 1-4C alkyl or OCH3; R6 = H or CH3; R7 = phenyl, naphthyl, benzofuryl, benzothienyl, thienyl, indolyl or N-methylindolyl optionally mono- or disubstituted by F, Cl, Br, 1-4C alkyl, OH, OCH3, NO2, CN, CF3, NH2 or N(1-4C alkyl)2; or 3-7C cycloalkyl; R8 = H; F; Cl; 1-4C alkyl; OCH3; or NH2; R9 = H or CH3; R10 = H or CH3; or CR9R10 forms a spirocyclopropane ring; R11 = H; OH; 1-4C alkyl; or 1-4C alkoxy; or together with the C atom to which it is attached forms C=O or C=S; X, Y = C; CH; CH2; NH; N(1-4C alkyl); or N; Z = direct bond; C(O); C(S); or CH or CH2 in which 1 H atom is optionally replaced with OH, NH2, 1-4C alkoxy or halo; A = H; OH; NH2; SH; NH(1-4C alkyl), N(1-4C alkyl)2; 1-4C alkylthio; or 1-4C alkoxy; or together with the C atom to which it is attached forms C=O; or A+Y = 3-4C alkylene which (a) optionally contains 1 or 2 non-adjacent double bonds, (b) optionally contains N, S, NH or N(CH3) in place of 1 CH or CH2 and (c) is optionally monosubstituted by F, Cl, CH3, OCH3, NO2 or NH2 or, when the ring formed is a benzene ring, is optionally mono-, di- or trisubstituted by F, Cl, CH3, CF3, NO2, OH, OCH3, NH2, NHCH3 or N(CH3)2; W = N; N(1-4C alkyl); N(allyl); or N(benzyl); and the ring containing W can contain 1-3 non-adjacent double bonds.

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