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    ALKYLENEDIOXYPHENYL ETHER DERIVATIVES HAVING ANTI-ISCHAEMIC, MEMORY ENHANCING AND ANTI-CONVULSIVE ACTIVITY
    1.
    发明专利
    ALKYLENEDIOXYPHENYL ETHER DERIVATIVES HAVING ANTI-ISCHAEMIC, MEMORY ENHANCING AND ANTI-CONVULSIVE ACTIVITY 未知

    公开(公告)号：CA2063314A1

    公开(公告)日：1992-09-21

    申请号：CA2063314

    申请日：1992-03-18

    Applicant: DUPHAR INT RES

    Inventor： LANGE JOSEPHUS H M ,  TOOROP GERRIT P ,  VAN WIJNGAARDEN INEKE ,  DEN HARTOG JACOBUS A J

    IPC: C07D317/64 ,  C07D319/18 ,  C07D405/06 ,  A61K31/36 ,  A61K31/445 ,  A61K31/495

    Abstract: DIR 0482 The invention relates to compounds having anti-ischaemic activity, memory enhancing activity and anti-convulsive activity of the formulae 1A and 1B (1A) (1B) wherein -R1 + R2 together form an alkylene group having 1-3 C-atoms which may be substituted with one or more alkyl group(s) having 13 C-atoms; -Z is methylene optionally substituted with one alkyl group having 1-3 C-atoms, or with one phenylalkyl group with 1-3 C-atoms in the alkyl group, which phenyl group may be substituted with a group (R5)p wherein. R6 is halogen, hydroxy, alkyl or hydroxyalkyl having 1-5 C-atoms, alkoxy having 1-3 C-atoms, S-alkyl, S(O)-alkyl or S(O)2-alkyl having 1-3 Catoms, amino, mono- or dialkylamino having 1-3 C-atoms per alkyl group, trifluoromethyl, trifluoromethoxy, a sulphonylamido group SO2NHR or a carbalkoxy group COOR wherein R is alkyl having 1-4 C-atoms, the group COOH, SO3H,CONH2, the amidino group or cyano group, and p has the value 0-3; -R3 and R4 independent of each other represent hydrogen, alkyl having 1-10 C-atoms, alkenyl or alkynyl having 3-10 Catoms, cycloalkyi having 3-8 C-atoms, cycloalkyl-alkyl having 3-8 ring atoms and 1-5 C-atoms in the alkyl group, phenylalkyl or heteroaryl-alkyl having 1-5 C-atoms in the alkyl group, phenylalkenyl, heteroaryl-alkenyl, phenylalkynyl or heteroaryl-alkynyl group having 3-5 C-atoms in the alkenyl group or alkynyl group, which groups R3 and R4 may be substituted with a group (R8)p wherein R6 and p have the above mentioned meanings, or wherein R3+R4 together with DIR 0482 the nitrogen atom form a saturated or unsaturated heterocyclic group of 5-7 ring atoms, which may contain a second hetero-atom from the group consisting of oxygen, sulphur and nitrogen, which ring may be substituted with a group (R5)p wherein R6 and p have the above mentioned meanings, or with phenylalkyl, heteroarylalkyl, phenylalkenyl, heteroaryl-alkenyl, phenylalkynyl or heteroaryl-alkynyl having at most 3 C-atoms in the alkyl, alkenyl or alkynyl part, which groups may be substituted with a group (R6)p wherein R6 and p have the above-mentioned meanings, or which ring may be annelated with a phenyl group; -R5 is alkyl having 1-12 C-atoms, alkenyl or alkynyl having 3-12 C-atoms, cycloalkyl having 3-8 C-atoms, cycloalkyl-alkyl having 3-8 ring atoms and 1-5 C-atoms in the alkyl group, phenylalkyl or heteroaryl-alkyl having 1-5 C-atoms in the alkyl sub-group, phenylalkenyl, heteroaryl-alkenyl, phenylalkynyl or heteroaryl-alkynyl having 3-5 C-atoms in the alkenyl subgroup or alkynyl sub-group, which groups may be substituted with a group (R6)p, wherein R6 and p have the abovementioned meanings, and which alkyl sub-groups, alkenyl sub-groups and alkynyl sub-groups may contain a group -O-, S- or CO, or a pharmacologically acceptable salt thereof

    QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONIST ACTIVITY
    7.
    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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