Heterocyclic compounds useful as Nurr-1 activators
    12.
    发明授权
    Heterocyclic compounds useful as Nurr-1 activators 失效
    用作Nurr-1激活剂的杂环化合物

    公开(公告)号:US07432293B2

    公开(公告)日:2008-10-07

    申请号:US10545245

    申请日:2004-02-13

    摘要: The present invention relates to compounds of formula (I): wherein R1 is hydroxy, C1-4 alkoxy, amino, C1-4 alkyl-amino, di C1-4alkylamino, benzyloxy or C2-C7 alkanoyl, R2 is C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxy C1-4alkoxy, CF3, halogen, C1-4alkylamino, di C1-4alkylamino, di C1-4 alkylamino C1-4 alkoxy or N—C1-4 alkoxy C1-4 alkyl-N—C1-4 alkylamino, N—C1-4 alkyl-piperazinyl, morpholinyl or pyrrolidinyl-C1-4 alkoxy, wherein the C1-4 alkyl radicals in R2 are optionally further substituted by C1-4 alkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3, X is O, Y is CH, Z is N and W is CH, (b) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3 or chloro, X is N, Y is O, Z is CH and W is CH, (c) R1 is not hydroxy when R2 is CF3, X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them.

    摘要翻译: 本发明涉及式(I)的化合物:其中R 1是羟基,C 1-4烷氧基,氨基,C 1-4 烷基 - 氨基,二C 1-4烷基氨基,苄氧基或C 2 -C 7烷酰基,R 2 为C 1-4烷基,C 1-4烷氧基,C 1-4烷氧基C 1-4烷基 烷氧基,CF 3,卤素,C 1-4烷基氨基,二C 1-4烷基氨基,二C 1-4 烷基氨基C 1-4烷氧基或NC 1-4烷氧基C 1-4烷基-NC 1-4 烷基氨基,NC 1-4烷基 - 哌嗪基,吗啉基或吡咯烷基-C 1-4烷氧基,其中C 1-4 - R 2中的烷基任选进一步被C 1-4烷基,卤素,氰基,氨基,烷氧基或烷硫基取代,X是N或O,Y是N ,O或CH,Z是N或CH,W是N或CH,条件是当R(R)不为羟基或C 1-4烷氧基时, 2是CF 3,X是O,Y是C H,Z是N,W是CH,(b)当R 2是CF时,R 1不是羟基或C 1-4烷氧基 3是或氯,X是N,Y是O,Z是CH,W是CH,(c)R 1不是羟基, SUB>是CF 3,X是O,Y是N,Z是CH,W是CH,(d)X和Y不同时为O,其盐; 它们的制备,它们的用途和含有它们的药物组合物。

    Organic Compounds
    14.
    发明申请
    Organic Compounds 审中-公开
    有机化合物

    公开(公告)号:US20110195950A1

    公开(公告)日:2011-08-11

    申请号:US12673365

    申请日:2008-08-12

    CPC分类号: C07D471/04 C07D491/04

    摘要: The invention relates to compound of the formula I in which R1 represents an optionally substituted aryl group or an optionally substituted heteroaryl group; R2 represents hydrogen or a substituent different from hydrogen; R3 represents an optionally substituted aryl group, cycloalkyl group, heteroaryl group, heterocyclyl group; X1 represents O, S, NR4, CR42; X2 represents O, S, NR4, CR42; X3 represents O, S, NR4, CR42; X4 represents O, S, NR4, CR42; R4 represents hydrogen or a substituent different from hydrogen; R5 represents hydrogen or alkyl; Y represents O or S; m represents 0, 1, 2 or 3; n represents 0, 1, 2 or 3 in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.

    摘要翻译: 本发明涉及式I化合物,其中R 1表示任选取代的芳基或任选取代的杂芳基; R2代表氢或不同于氢的取代基; R 3表示任选取代的芳基,环烷基,杂芳基,杂环基; X1表示O,S,NR4,CR42; X2表示O,S,NR4,CR42; X3表示O,S,NR4,CR42; X 4表示O,S,NR 4,CR 42; R4表示氢或不同于氢的取代基; R5代表氢或烷基; Y表示O或S; m表示0,1,2或3; n表示游离碱形式或酸加成盐形式的0,1,2或3; 作为其制备,用作药物和包含它的药物。

    Benzo[1,2,5]oxadiazoles and benzol[1,2,5]thiadiazoles useful as histopathological staining agents, imaging agents and biomarkers
    15.
    发明授权
    Benzo[1,2,5]oxadiazoles and benzol[1,2,5]thiadiazoles useful as histopathological staining agents, imaging agents and biomarkers 失效
    可用作组织病理学染色剂的苯并[1,2,5]恶二唑和苯并[1,2,5]噻二唑,成像剂和生物标志物

    公开(公告)号:US07632851B2

    公开(公告)日:2009-12-15

    申请号:US10549248

    申请日:2004-04-02

    摘要: The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R1 is 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-18F-ethylamino)-thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R2 is NHCH3, NH11CH3, N(CH3)11CH3, N(CH3)2, N(11CH3)2, NH(CH2)nF, NH(CH2)n18F, N(CH3)(CH2)nF, N(CH3)—(CH2)n18F, O—(CH2)nF, O—(CH2)n18F, CONH(CH2)nF or CONH(CH2)n18F (n being in each case 2 to 4) and R3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.

    摘要翻译: 本发明涉及式(I)的新的苯并[1,2,5]恶二唑和苯并[1,2,5]噻二唑,其中X是O或S,R 1是5-(2-氟 - 乙基氨基) - 噻唑 -2-基,或其中Y是CH或N的式(a)基团,R 2是NHCH 3,NH 11 CH 3,N(CH 3)11 CH 3,N(CH 3) )2,N(11CH3)2,NH(CH2)nF,NH(CH2)n18F,N(CH3)(CH2)nF,N(CH3) - (CH2)n18F,O-(CH2) CH2)n18F,CONH(CH2)nF或CONH(CH2)n18F(n分别为2〜4),R3为羟基,(C1-4)烷氧基,氢或硝基,为游离碱或酸加成盐形式; 它们的制备,它们在诊断中的用途和含有它们的组合物。

    Heterocyclic compounds useful as nurr-1 activators
    16.
    发明申请
    Heterocyclic compounds useful as nurr-1 activators 失效
    用作护士1激活剂的杂环化合物

    公开(公告)号:US20060089365A1

    公开(公告)日:2006-04-27

    申请号:US10545245

    申请日:2004-02-13

    摘要: The present invention relates to compounds of formula (I): wherein R1 is hydroxy, C1-4 alkoxy, amino, C1-4 alkyl-amino, di C1-4alkylamino, benzyloxy or C2-C7 alkanoyl, R2 is C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxy C1-4alkoxy, CF3, halogen, C1-4alkylamino, di C1-4alkylamino, di C1-4 alkylamino C1-4 alkoxy or N—C1-4 alkoxy C1-4 alkyl-N—C1-4 alkylamino, N—C1-4 alkyl-piperazinyl, morpholinyl or pyrrolidinyl-C1-4 alkoxy, wherein the C1-4 alkyl radicals in R2 are optionally further substituted by C1-4 alkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3, X is O, Y is CH, Z is N and W is CH, (b) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3 or chloro, X is N, Y is O, Z is CH and W is CH, (c) R1 is not hydroxy when R2 is CF3, X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them.

    摘要翻译: 本发明涉及式(I)的化合物:其中R 1是羟基,C 1-4烷氧基,氨基,C 1-4 烷基 - 氨基,二C 1-4烷基氨基,苄氧基或C 2 -C 7烷酰基,R 2 为C 1-4烷基,C 1-4烷氧基,C 1-4烷氧基C 1-4烷基 烷氧基,CF 3,卤素,C 1-4烷基氨基,二C 1-4烷基氨基,二C 1-4 烷基氨基C 1-4烷氧基或NC 1-4烷氧基C 1-4烷基-NC 1-4 烷基氨基,NC 1-4烷基 - 哌嗪基,吗啉基或吡咯烷基-C 1-4烷氧基,其中C 1-4 - R 2中的烷基任选进一步被C 1-4烷基,卤素,氰基,氨基,烷氧基或烷硫基取代,X是N或O,Y是N ,O或CH,Z是N或CH,W是N或CH,条件是当R(R)不为羟基或C 1-4烷氧基时, 2是CF 3,X是O,Y是C H,Z是N,W是CH,(b)当R 2是CF时,R 1不是羟基或C 1-4烷氧基 3是或氯,X是N,Y是O,Z是CH,W是CH,(c)R 1不是羟基, SUB>是CF 3,X是O,Y是N,Z是CH,W是CH,(d)X和Y不同时为O,其盐; 它们的制备,它们的用途和含有它们的药物组合物。