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    QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONIST ACTIVITY
    11.
    发明专利
    QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONIST ACTIVITY 未知

    公开(公告)号：CA2270777C

    公开(公告)日：2008-04-22

    申请号：CA2270777

    申请日：1998-09-07

    Applicant: DUPHAR INT RES

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

    IPC: C07D239/94 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61P25/00 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D215/42 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  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, ri ng 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, C3-46-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), SO 2- (C1-6-alkyl), hydroxy, cyano, nitro, trifluoromethyl, SO2NH2, SO2N(mono- or di-C1-4-alkyl), formyl, CO-(C1-6-alkyl), COOH, COO-(C1 -6- alkyl), CONH2, CON(mono- or di-C1-4-alkyl),amino, N(mono or di-C1-4-alkyl), NHCO(C1-46-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) R 5 is 2,4,6-trimethylphenyl, and salts thereof have good CRF antagonist activity.

    PHENYLALKYL AMINE DERIVATIVES HAVING ANTIISCHAEMIC ACTIVITY
    19.
    发明专利
    PHENYLALKYL AMINE DERIVATIVES HAVING ANTIISCHAEMIC ACTIVITY 未知

    公开(公告)号：CA2025731A1

    公开(公告)日：1991-03-23

    申请号：CA2025731

    申请日：1990-09-19

    Applicant: DUPHAR INT RES

    Inventor： WITIAK DONALD T ,  VAN WIJNGAARDEN INEKE ,  NAIR RAGHUNATHAN V ,  LANGE JOSEPHUS H M ,  DEN HARTOG JACOBUS A J

    IPC: A61K31/357 ,  A61K31/36 ,  A61K31/443 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07C217/58 ,  C07D295/096 ,  C07D317/64 ,  C07D319/18 ,  C07D321/10 ,  C07D405/06 ,  C07D317/46 ,  A61K31/335 ,  A61K31/395 ,  C07D405/10 ,  C07D413/10

    Abstract: DIR 0444 The invention relates to compounds having anti-ischaemic activity of the formula (1) 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 1-3 C-atoms; -Z is methylene optionally substituted with one or two alkyl group(s) having 1-3 C-atoms, or with one phenyl group or phenylalkyl group with 1-3 C-atoms in the alkyl group, which phenyl groups may be substituted with a group (R6)p wherein R6 is halogen, hydroxyl 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 C-atoms, amino, mono- or dialkylamino having 1-3 Catoms per alkyl group, trifluoromethyl, trifluoromethoxy, a sulphonylamido group SO2NHR or a carbalkoxy group COOR wherein R is alkyl having 1-4 Catoms, the group COOH, SO3H,COHN2, 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 310 C-atoms, cycloalkyl having 3-8 C atoms, cycloalkylalkyl having 3-8 ring atoms and 1-5 C-atoms in the alkyl group, phenylalkyl or heteroaryl-alkyl having 1-5 Catoms in the alkyl group, phenylalkenyl, heteroarylalkenyl, phenylalkynyl or heteroaryl-alkynyl group having 3-5 C-atoms in the alkenyl group or alkynyl DIR 0444 group, which groups R3 and R4 may be substituted with a group (R6)p wherein R6 and p have the above mentioned meanings, or wherein R3+R4 together with 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 (R6)p wherein R6 and p have the above mentioned meanings, or with phenylalkyl, phenylalkenyl, thienylalkenyl, pyridinylalkenyl, phenylalkynyl, thienylalkynyl or pyridinylalXynyl 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 sub-group or alkynyl sub-group, which groups may be substituted with a group (R6)p, wherein R6 and p have the above-mentioned meanings, and which alkyl subgroups, alkenyl sub-groups and alkynyl sub-groups may contain a group -O-, -S- or CO, or a pharmacologically acceptable salt thereof.

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