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    BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY
    32.
    发明专利
    BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY 未知

    公开(公告)号：CA2320120C

    公开(公告)日：2009-08-11

    申请号：CA2320120

    申请日：1999-02-05

    Applicant: DUPHAR INT RES

    Inventor： VISSER GERBEN M ,  DEN HARTOG JACOBUS A J ,  LANGE JOSEPHUS H M ,  TULP MARTINUS T M ,  VAN STEEN BARTHOLOMEUS J ,  RONKEN ERIC ,  KRUSE CORNELIS G

    IPC: C07D413/14 ,  A61K31/445 ,  A61K31/454 ,  A61K31/55 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00

    Abstract: The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C1-2)-amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1- 2)- amino, X is O, S, NH or NCH3, Y represents CH2 or (CH2)2, (R2)m represents 0, 1, or 2 substituents, which can be the same or different , from the group methyl and ethyl, or (R2)m is a methylene bridge or ethylene bridge, A is a group -CH2-(CRH)p- wherein R is hydrogen o r methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C1-2)amino, sulfonyl-(C1- 3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino.

    33.
    发明专利
    未知

    公开(公告)号：DE69936572T2

    公开(公告)日：2008-06-19

    申请号：DE69936572

    申请日：1999-02-05

    Applicant: DUPHAR INT RES

    Inventor： DEN HARTOG JACOBUS A J ,  VISSER GERBEN M ,  VAN STEEN BARTHOLOMEUS J ,  TULP MARTINUS T ,  RONKEN ERIC ,  KRUSE CORNELIS G ,  LANGE JOSEPHUS H M

    IPC: C07D413/14 ,  A61K31/445 ,  A61K31/454 ,  A61K31/55 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00

    Abstract: The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C1-2)-amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino, X is O, S, NH or NCH3, Y represents CH2, or (CH2)2, (R2)m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)m is a methylene bridge or ethylene bridge, A is a group -CH2-(CRH)p- wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C1-2)amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino.

    QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONIST ACTIVITY
    38.
    发明专利
    QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONIST ACTIVITY 未知

    公开(公告)号：CA2270777A1

    公开(公告)日：1999-03-18

    申请号：CA2270777

    申请日：1998-09-07

    Applicant: DUPHAR INT RES

    Inventor： RONKEN ERIC ,  TULP MARTINUS T M ,  REINDERS JAN H ,  JANSEN JOHANNES W C M ,  TOOROP GERRIT P ,  VISSER GERBEN M ,  DEN HARTOG JACOBUS A J

    IPC: A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/519 ,  A61P25/00 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D215/42 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04

    Abstract: The invention relates to novel quinoline and quinazoline derivatives having corticotropin releasing factor (CRF) antagonist activity. It has been found that compounds having formula (I) wherein A is CH or N, ring Q is phenyl, pyridyl, pyrimidinyl or pyridazinyl, optionally substituted with one or two groups R4; ring Y is phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 and R2 are optionally branched C1-6-alkyl, C3-6-alkenyl, C3-6-alkynyl, C3-6-cycloalkyl-C1-4-alkyl, phenyl-C1-4-alkyl, 5- or 6-membered saturated or unsaturated heterocyclyl-C1-4-alkyl, which groups R1 and R2 can be substituted with OH, C1-3-alkoxy, C1-3-alkoxycarbonyl, optionally mono- or di-(C1-3-alkyl)substituted amino, halogen or cyano; R3 is H, C1-3-alkyl optionally substituted with one or more fluorine atoms, or R3 is halogen, methoxy or ethoxy; R4 is C1-3-alkyl optionally substituted with one or more fluorine atoms, or R4 is halogen, methoxy, ethoxy, amino, mono- or di-substituted amino, or cyano; R5 is halogen, optionally branched C1-6-alkyl, C3-6-alkenyl, C3-6-alkynyl, C3-6-cycloalkyl-C1-4-alkyl, O-(C1-6-alkyl), S-(C1-6-alkyl), SO2 (C1-6-alkyl), hydroxy, cyano, nitro, trifluoromethyl, SO2NH2, SO2N(mono- or diC1-4-alkyl), formyl, CO-(C1-6-alkyl), COOH, COO-(C1-6-alkyl), CONH2, CON(monoor di-C1-4-alkyl), amino, N(mono or di-C1-4-alkyl), NHCO(C1-6-alkyl), NHSO2 (C1-6-alkyl), which groups R5 can be identical or different; and n has the value 0 to 4; with the proviso that the group NR1R2 is not diethylamino, ethyl,n-propylamino or ethyl,n-butylamino, if A is CH, Q is unsubstituted phenyl, R3 is methyl, and substituent Y with the group(s) R5 is 2,4,6trimethylphenyl, and salts thereof have good CRF antagonist activity.

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