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    Method of inhibiting aortal smooth muscle cell proliferation using naphthyl compounds
    51.
    发明授权
    Method of inhibiting aortal smooth muscle cell proliferation using naphthyl compounds 失效
    使用萘基化合物抑制大动脉平滑肌细胞增殖的方法

    公开(公告)号：US5691353A

    公开(公告)日：1997-11-25

    申请号：US567635

    申请日：1995-12-05

    申请人： Henry U. Bryant ,  Jeffrey A. Dodge

    发明人： Henry U. Bryant ,  Jeffrey A. Dodge

    IPC分类号： C07D295/08 ,  A61K31/40 ,  A61K31/445 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/55 ,  A61P3/02 ,  A61P3/06 ,  A61P5/00 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00 ,  A61P43/00 ,  C07D207/06 ,  C07D295/092 ,  C07D211/14

    CPC分类号： C07D295/088

    摘要： The present invention provides a compound of formula I ##STR1## wherein R.sub.1 is H, OH, halo, OCO(C.sub.1 -C.sub.6 alkyl), OCO(aryl), OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), OCOO(C.sub.1 -C.sub.6 alkyl), OCOO(aryl), OCONH (C.sub.1 -C.sub.6 alkyl), or OCON(C.sub.1 -C.sub.6 alkyl).sub.2 ; R.sub.2 is aryl, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or 4-cyclohexanol; R.sub.3 is O(CH.sub.2).sub.2 or O(CH.sub.2).sub.3 ; R.sub.4 and R.sub.5 are optionally CO(CH.sub.2).sub.3,CO(CH.sub.2).sub.4, C.sub.1 -C.sub.6 alkyl, or R.sub.4 and R.sub.5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrollidine, 3-methylpyrollidine, 3,3-dimethylpyrollidine, 3,4-dimethylpyrollidine, azepine, or pipecoline; R.sub.6 is >CH(C.sub.1 -C.sub.5 alkyl), >CH(C.sub.2 -C.sub.5 alkenyl), >C.dbd.CH(C.sub.1 -C.sub.5 alkyl), >CH(aryl), >C(OH)(C.sub.1 -C.sub.5 alkyl), >C(OH)(C.sub.2 -C.sub.5 alkenyl), C(OH)aryl; and phamaceutically acceptable salts thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, optionally containing estrogen or progestin, and the use of such compounds alone, or in combination with estrogen or progestin, for alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer. As used herein, the term "progestin" includes compounds having progestational activity such as, for example, progesterone, norethylnodrel, nongestrel, megestrol acetate, norethindrone, and the like. The compounds of the present invention also are useful for inhibiting uterine fibroid disease and endometriosis in women and aortal smooth muscle cell proliferation, particularly restenosis, in humans.

    摘要翻译： 本发明提供式I化合物其中R 1是H，OH，卤素，OCO（C 1 -C 6烷基），OCO（芳基），OSO 2（C 4 -C 6烷基），OCOO（C 1 -C 6 烷基），OCOO（芳基），OCONH（C1-C6烷基）或OCON（C1-C6烷基）2; R2是芳基，C1-C6烷基，C3-C6环烷基或4-环己醇; R3是O（CH2）2或O（CH2）3; R4和R5任选是CO（CH 2）3，CO（CH 2）4，C 1 -C 6烷基或R 4和R 5与它们所连接的氮键合形成哌啶，吗啉，吡咯烷，3-甲基吡咯烷，3 ，3-二甲基吡咯烷，3,4-二甲基吡咯烷，吖庚因或哌可乐; R6是CH（C1-C5烷基），> CH（C2-C5烯基），> C = CH（C1-C5烷基），> CH（芳基），> C（OH） C（OH）（C 2 -C 5烯基），C（OH）芳基;及其药学上可接受的盐。 本发明进一步提供含有式I化合物，任选含有雌激素或孕激素的药物组合物，以及单独或与雌​​激素或孕激素组合使用此类化合物，用于减轻绝经后综合征，特别是骨质疏松症的心血管相关症状 病理状况和雌激素依赖性癌症。 如本文所用，术语“孕激素”包括具有促孕活性的化合物，例如孕酮，去甲肾上腺素，非诺司定，醋酸甲地孕酮，炔诺酮等。 本发明的化合物还可用于抑制妇女子宫肌瘤和子宫内膜异位症以及主动脉平滑肌细胞增殖，特别是人类的再狭窄。

    Methods for lowering serum cholesterol
    53.
    发明授权
    Methods for lowering serum cholesterol 失效
    降低血清胆固醇的方法

    公开(公告)号：US5446061A

    公开(公告)日：1995-08-29

    申请号：US148038

    申请日：1993-11-05

    申请人： Henry U. Bryant ,  Timothy A. Grese

    发明人： Henry U. Bryant ,  Timothy A. Grese

    IPC分类号： C07D311/60 ,  A61K31/40 ,  A61K31/445 ,  A61P3/06 ,  A61P9/10 ,  A61K31/35

    CPC分类号： A61K31/445 ,  A61K31/40

    摘要： A method of lowering serum cholesterol levels, comprising administering an effective amount of a compound having the formula ##STR1## wherein: R.sup.1 and R.sup.2 are, independently, --H, --OH, halo, --OC.sub.1 -C.sub.17 alkyl, --OC.sub.3 -C.sub.6 cycloalkyl, --O(CO)C.sub.1 -C.sub.17 alkyl, --O(CO) aryl, --O(CO)O aryl, or --OSO.sub.2 -(n-butyl or n-pentyl);R.sup.3 is ##STR2## and R.sup.4 is --H, methyl, ethyl, propyl, ethenyl or ethynyl; or a pharmaceutically acceptable salt or solvate thereof, to an animal in need of lower cholesterol levels.

    摘要翻译： 一种降低血清胆固醇水平的方法，包括施用有效量的具有下式的化合物（I）其中：R 1和R 2独立地是-H，-OH，卤素，-OC 1 -C 17烷基，-OC 3 -C（C）环烷基，-O（CO）C 1 -C 17烷基，-O（CO）芳基，-O（CO）O芳基或-OSO 2 - （正丁基或正戊基） R3为;，R4为-H，甲基，乙基，丙基，乙烯基或乙炔基; 或其药学上可接受的盐或溶剂化物施用于需要降低胆固醇水平的动物。

    Method of inhibiting demineralization of bone
    55.
    发明授权
    Method of inhibiting demineralization of bone 失效
    抑制骨质疏松的方法

    公开(公告)号：US5063234A

    公开(公告)日：1991-11-05

    申请号：US684524

    申请日：1991-04-11

    申请人： Henry U. Bryant ,  James A. Clemens

    发明人： Henry U. Bryant ,  James A. Clemens

    IPC分类号： A61K31/47 ,  A61K31/48 ,  A61P3/00 ,  A61P19/10 ,  A61P43/00 ,  C07D457/02 ,  C07D471/06

    CPC分类号： A61K31/48

    摘要： A method of inhibiting bone demineralization comprising administration of an effective amount of a compound having the formula ##STR1## where X is CH or N;Y is O or S;R.sup.1 is 2-propenyl, C.sub.1 -C.sub.3 alkyl, benzyl or substituted benzyl where the substitutents are one or two of the same or different and are selected from methyl, ethyl, methoxy, ethoxy, hydroxy, chloro, bromo, or fluoro;R.sup.2 is C.sub.2 -C.sub.3 alkyl, allyl or cyclopropylmethyl;R.sup.3 and R.sup.4 are both hydrogen or combine to form a carbon-carbon bond; and pharmaceutically acceptable acid addition salts thereof to a mammal requiring bone demineralization inhibition.