中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

400 records (took 0.024 seconds)

    2-SUBSTITUTED 1,2-BENZISOTHIAZOLE DERIVAYIVES AND THEIR USE AS SEROTONIN ANTAGONISTS (5-HT1A, 5-HT1B AND 5-HT1D)
    13.
    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

    Control of cocaine addiction comprises administration of N-substituted azabicycloalkane derivative
    15.
    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.

Patent Agency Ranking