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    Imidazoles for the treatment of atherosclerosis
    2.
    发明授权
    Imidazoles for the treatment of atherosclerosis 失效

    公开(公告)号：US5318984A

    公开(公告)日：1994-06-07

    申请号：US940372

    申请日：1992-09-03

    申请人： Jeffrey T. Billheimer ,  Peter J. Gillies ,  C. Anne Higley ,  Thomas P. Maduskuie, Jr. ,  Ruth R. Wexler

    发明人： Jeffrey T. Billheimer ,  Peter J. Gillies ,  C. Anne Higley ,  Thomas P. Maduskuie, Jr. ,  Ruth R. Wexler

    IPC分类号： C07D233/54 ,  C07D233/70 ,  C07D233/84 ,  C07D233/88 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D491/04 ,  A61K31/415 ,  C07D233/66

    CPC分类号： C07D233/64 ,  C07D233/70 ,  C07D233/84 ,  C07D233/88 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D491/04

    摘要： Disclosed are compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are selected independently from H, C.sub.1 -C.sub.8 unbranched alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 araalkyl, 2-, 3- or 4-pyridinyl, 2-thienyl, 2-furanyl, phenyl optionally substituted with 1 to 3 groups selected from F, Cl, Br, OH, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, CH.sub.3 S(O).sub.r, NO.sub.2, CF.sub.3, or NR.sup.7 R.sup.8 ; or ##STR2## where L is O, O(CH.sub.2).sub.m+1 O, or (CH.sub.2).sub.m where m is 0-4; R.sup.3 is H, C.sub.1 -C.sub.6 alkyl, allyl, benzyl, or phenyl optionally substituted with F, Cl, CH.sub.3, CH.sub.3 O, or CF.sub.3 ;R.sup.4 is straight chain C.sub.1 -C.sub.8 alkyl optionally substituted with F; C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; C.sub.3 --C.sub.6 alkenyl or alkynyl, C.sub.1 -C.sub.3 perfluoroalkyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.1 -C.sub.4 alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8 or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, pyrimidinyl, or biphenyl;R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, or benzyl;R.sup.6 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.8 alkenyl or alkynyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ;R.sup.7 and R.sup.8 are selected independently from H or C.sub.1 -C.sub.4 alkyl;X is S(O).sub.r, O, NR.sup.5, CH.sub.2 ;A is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl, or C.sub.3 -C.sub.10 alkynyl;Y is O, S, H.sub.2, or NH;Z is NHR.sup.4, OR.sup.4, or R.sup.4 ;r is 0-2,or a pharmaceutically acceptable salt thereof and their use as antihypercholesterolemic agents or antiatherosclerotic agents.

    Use of imidazoles for the treatment of atherosclerosis
    3.
    发明授权
    Use of imidazoles for the treatment of atherosclerosis 失效

    公开(公告)号：US5166214A

    公开(公告)日：1992-11-24

    申请号：US533241

    申请日：1990-06-04

    申请人： Jeffrey T. Billheimer ,  Peter J. Gillies ,  C. Anne Higley ,  Thomas P. Maduskuie, Jr. ,  Ruth R. Wexler

    发明人： Jeffrey T. Billheimer ,  Peter J. Gillies ,  C. Anne Higley ,  Thomas P. Maduskuie, Jr. ,  Ruth R. Wexler

    IPC分类号： C07D233/54 ,  C07D233/70 ,  C07D233/84 ,  C07D233/88 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D491/04

    CPC分类号： C07D233/64 ,  C07D233/70 ,  C07D233/84 ,  C07D233/88 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D491/04

    摘要： This invention relates to imidazoles as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), processes for their preparation, and their use as antihypercholesterolemic agents or antiatherosclerotic.The compounds for use in the described method are compounds of Formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are selected independently from H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 araalkyl, phenyl optionally substituted with 1 to 3 groups selected from F, Cl, Br, OH, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, CH.sub.3 S(O).sub.r, NO.sub.2, CF.sub.3, or NR.sup.7 R.sup.8 ; R.sup.3 is H, C.sub.1 -C.sub.6 alkyl, allyl, benzyl, or phenyl optionally substituted with F, Cl, CH.sub.3, CH.sub.3 O, or CF.sub.3 ; R.sup.4 is straight chain C.sub.1 -C.sub.8 alkyl optionally substituted with F; C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkylalkyl, C.sub.7 -C.sub.14 aralkyl where the aryl group is optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; C.sub.3 -C.sub.6 alkenyl or alkynyl, C.sub.1 -C.sub.3 perfluoroalkyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.1 -C.sub.4, alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8 or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; 2-, 3-, or 4- or pyrindinyl, pyrimidinyl, or biphenyl; R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, or benzyl; R.sup.6 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.8 alkenyl of alkynyl, phenyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; pentafluorophenyl, benzyl optionally substituted with 1 to 3 groups selected from C.sub.1 -C.sub.4 alkyl or alkoxy, F, Br, Cl, NH.sub.2, OH, CN, CO.sub.2 H, CF.sub.3, NO.sub.2, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.7 R.sup.8, or NCOR.sup.7 ; R.sup.7 and R.sup.8 are selected independently from H or C.sub.1 -C.sub.4 alkyl; A is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl, or C.sub.3 -C.sub.10 alkynyl; Y is O; Z is NHR.sup.4, OR.sup.4, or R.sup.4 ; r is 0-2, or a pharmaceutically acceptable salt thereof.

    Fused-ring heterocycles for the treatment of atherosclerosis
    4.
    发明授权
    Fused-ring heterocycles for the treatment of atherosclerosis 失效
    用于治疗动脉粥样硬化的融合环杂环

    公开(公告)号：US5478830A

    公开(公告)日：1995-12-26

    申请号：US889892

    申请日：1992-05-29

    申请人： C. Anne Higley ,  Ruth R. Wexler ,  Richard G. Wilde

    发明人： C. Anne Higley ,  Ruth R. Wexler ,  Richard G. Wilde

    IPC分类号： C07D487/04 ,  A61K31/44 ,  A61K31/505 ,  A61K31/52

    CPC分类号： C07D487/04

    摘要： This invention relates to pyrazolo pyrimidines for the treatment of atherosclerosis as inhibitors of acyl--CoA, cholesterol acyetransferase (ACAT), and their use as antihypercholesterolemic agents, pharmaceutical compositions and preparation, and having the formula (I): ##STR1## wherein: A and Q are selected independently from CH or N with no more than two nitrogens per ring:D, E, and G are selected independently from CR.sup.1 or N with no more than two nitrogens per ring;X is S(O).sub.r, O, NR.sup.4 or CH.sup.2 ;J is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl or C.sub.3 -C.sub.10 alkynyl;Y is O, S, H.sub.2 or NH:Z is NHR.sup.3, OR.sup.3 or R.sup.3 :R.sup.1 is selected independently from H, NO.sub.2, Br, Cl, F, CF.sub.3, CN, CH.sub.3 S(O).sub.r, C.sub.1 -C.sub.8 alkyl or alloxy, C.sub.3 -C.sub.8, branched alkyl, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.5 R.sup.6 or NR.sup.5 COR.sup.6 ;R.sup.2 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.8 alkenyl or alkynyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted; phenyl optionally substituted benzyl optionally substituted 2-, 3-, or 4- pyridinyl, pyrimidinyl: or biphenyl:R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloallylalkyl, C.sub.3 -C.sub.6 alkenyl or alkynyl, C.sub.1 -C.sub.3 perfluoroalkyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted phenyl optionally substituted benzyl optionally substituted 2-, 3-, or 4- pyridinyl, pyrimidinyl; or biphenyl:R.sup.4 is H, C.sub.1 -C.sub.6 alkyl or benzyl;R.sup.5 and R.sup.6 are selected independently from H or C.sub.1 -C.sub.4 alkyl;r is 0 to 2:or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及用于治疗动脉粥样硬化的吡唑并嘧啶作为酰基辅酶A，胆固醇转氨酶（ACAT）的抑制剂及其作为抗高胆固醇血症药物，药物组合物和制剂的用途，并具有式（I）：其中： A和Q独立地选自CH或N，每个环不多于两个氮：D，E和G独立地选自CR1或N，每个环不多于两个氮; X是S（O）r，O，NR 4或CH 2; J是C 2 -C 10烷基，C 3 -C 10支链烷基，C 3 -C 10链烯基或C 3 -C 10炔基; Y是O，S，H2或NH：Z是NHR3，OR3或R3：R1独立地选自H，NO2，Br，Cl，F，CF3，CN，CH3S（O）r，C1-C8烷基或烯氧基， C3-C8，支链烷基，C1-C4烷氧羰基，NR5R6或NR5COR6; R2是C1-C8烷基，C3-C8支链烷基，C3-C7环烷基，C3-C8链烯基或炔基，其中芳基任选被取代的C7-C14芳烷基; 苯基任选取代的苄基任选取代的2-，3-或4-吡啶基，嘧啶基或联苯基：R3是C1-C8烷基，C3-C8支链烷基，C3-C7环烷基，C4-C10环烯基烷基，C3-C6烯基或 炔基，C1-C3全氟烷基，C7-C14芳烷基，其中芳基是任选取代的苯基任选取代的苄基任选取代的2-，3-或4-吡啶基，嘧啶基; 或联苯基：R 4是H，C 1 -C 6烷基或苄基; R 5和R 6独立地选自H或C 1 -C 4烷基; r为0〜2：或其药学上可接受的盐。