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9 条记录 (耗时 0.039 秒)

    Imidazopyridines pyrimidines and triazines for enhancing cognition as gaba-a-alphas 5 receoptor subtype ligands
    2.
    发明申请
    Imidazopyridines pyrimidines and triazines for enhancing cognition as gaba-a-alphas 5 receoptor subtype ligands 审中-公开

    公开(公告)号：US20060040940A1

    公开(公告)日：2006-02-23

    申请号：US10497002

    申请日：2002-11-27

    申请人： Michela Bettati ,  Mark Chambers ,  Alexander Humphries ,  Philip Jones ,  Richard Lewis ,  Robert Maxey ,  Helen Szekeres ,  Martin Teall

    发明人： Michela Bettati ,  Mark Chambers ,  Alexander Humphries ,  Philip Jones ,  Richard Lewis ,  Robert Maxey ,  Helen Szekeres ,  Martin Teall

    IPC分类号： A61K31/53 ,  A61K31/519 ,  A61K31/4745

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present invention provides a pharmaceutical composition providing a compound of formula I or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable excipient: (I), in which: X and Y independently represent CH or N, with the proviso that if X is CH then Y is also CH; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, —CO2Ra, —CONRaRb or CRa═NORb; Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; V and W are independently selected from H, halogen, C11-6alkyl, OH and C-1-6alkoxy; Z represents H, halogen, CN, NO2, CF3, OCF3, CF2H, SCF3, R2, OR3, SR3, (CH2)pN(R3)2, O(CH2)pN(R3)2, SO2R2, SO2N(R3)2, COR4, CO2R3, CON(R3)2, NHCOR4, NR1(CH2)nheteroaryl or O(CH2)nheteroaryl the heteroaryl is optionally substituted by one, two or three groups chosen from C1-6alkyl, benzyl, (CH2)pN(R3)2, halogen and CF3, R1 is C1-6alkyl, where n is 1 or 2 and p is 0, 1 or 2; with the proviso that at least one of V, W and Z is other than H; R2 represents C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-4alkyl, C2-6alkenyl, C2-6alkynyl or heteroaryl, any of which may bear a substituent selected from halogen, CN, NO2, CF3, OCF3, CF2H, SCF3, OH, C1-4alkoxy, C1-4alkoxycarbonyl, amino, C1-4alkylamino, or di(C1-4alkyl)amino; R3 represents H or R2; or two R3 groups bonded to the same nitrogen atom may complete a 5-7 membered nonaromatic heterocyclic ring; and R4 represents R3 or heteroaryl; the compounds are ligands for GABA-A receptors containing the alpha 5 subtype and thus are useful for enhancing cognition in individuals suffering from conditions such as Alzheimer's Disease.

    2/3-(heterocyclic alkyl amino)-1-(subst.-phenyl-methoxy)-ethanes/propanes as tachykinin-receptor antagonists
    9.
    发明授权
    2/3-(heterocyclic alkyl amino)-1-(subst.-phenyl-methoxy)-ethanes/propanes as tachykinin-receptor antagonists 失效
    2-（3-（杂环烷基氨基）-1-（邻 - 苯基 - 甲氧基） - 乙烷/丙烷作为速激肽受体拮抗剂

    公开(公告)号：US5494926A

    公开(公告)日：1996-02-27

    申请号：US338484

    申请日：1994-11-18

    申请人： Andrew P. Owens ,  Martin Teall ,  Brian Williams

    发明人： Andrew P. Owens ,  Martin Teall ,  Brian Williams

    IPC分类号： C07D233/54 ,  C07D233/76 ,  C07D249/08 ,  C07D249/14 ,  C07D257/04 ,  C07D271/06 ,  C07D271/07 ,  A61K31/42 ,  C07D263/10

    CPC分类号： C07D249/08 ,  C07D233/76 ,  C07D257/04 ,  C07D271/07

    摘要： Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents phenyl or benzhydryl; X and Y each represent H or X and Y together form a group =0; Z is O, S or NR.sup.8 (R.sup.8 is H or C.sub.1-6 alkyl); R.sup.1 is H, optionally substituted C.sub.1-6 alkyl, phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkylene, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-4 alkylNR.sup.a R.sup.b, or CONR.sup.a C.sub.1-4 alkylCONR.sup.a R.sup.b ; R.sup.2 is C.sub.1-4 alkyl substituted by an optionally substituted aromatic heterocycle; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 is H, C.sub.1-6 alkyl or optionally substituted phenyl; R.sup.5 represents optionally substituted phenyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy. ##STR1##

    摘要翻译： 式（I）化合物及其盐和前药，其中Q表示苯基或二苯甲基; X和Y各自表示H或X和Y一起形成基团= 0; Z是O，S或NR8（R8是H或C1-6烷基）; R 1是H，任选取代的C 1-6烷基，苯基（C 1-4烷基），C 2-6亚烷基，CORa，COORA，CONHRa，COC 1-4烷基NR a R b或CONR a C 1-4烷基CONR a R b; R2是被任选取代的芳族杂环取代的C 1-4烷基; R3是H，C1-6烷基或C2-6烯基; R4是H，C1-6烷基或任选取代的苯基; R5代表任选取代的苯基; q为0,1,2或3; 是用于治疗的速激肽拮抗剂。 （一）