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29 条记录 (耗时 0.072 秒)

    Methods for regulating trkA expression
    21.
    发明授权
    Methods for regulating trkA expression 失效
    调节trkA表达的方法

    公开(公告)号：US5990129A

    公开(公告)日：1999-11-23

    申请号：US150271

    申请日：1998-09-09

    申请人： Henry Uhlman Bryant ,  Robert Frank Santerre

    发明人： Henry Uhlman Bryant ,  Robert Frank Santerre

    IPC分类号： C07D333/64 ,  A61K31/38 ,  A61K31/4025 ,  A61K31/445 ,  A61K31/4535 ,  A61K31/55 ,  A61P5/32 ,  A61P15/12 ,  A61P25/00 ,  A61P25/28 ,  A61K31/40

    CPC分类号： A61K31/38 ,  A61K31/4025 ,  A61K31/445 ,  A61K31/4535

    摘要： The current invention provides methods for the up-regulation of trkA in a mammal, including humans, comprising the administration of an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.3 are, independently, --H, --CH.sub.3, --CO(C.sub.1 -C.sub.6 alkyl), or --COAr, where Ar is optionally substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine, piperidine, and hexamethyleneimino; ora pharmaceutically acceptable salt or solvate thereof.In addition, the current invention provides method to increase the effect of NGF (Nerve Growth Factor), NGF-like activities or NGF agonists, whether such is from endogenous or exogenous sources.Further, the current invention provides methods for maintaining the homeostasis and health of the hippocampus, hypothalamus, and cortex, thus maintaining their biological functions.

    摘要翻译： 本发明提供了包括人在内的哺乳动物中trkA上调的方法，包括施用有效量的式I化合物，其中R 1和R 3独立地是-H，-CH 3，-CO（C 1 -C 1-6烷基）或-COAr，其中Ar是任选取代的苯基; R2选自吡咯烷，哌啶和六亚甲基亚氨基; 或其药学上可接受的盐或溶剂合物。 此外，本发明提供了增加NGF（神经生长因子），NGF样活性或NGF激动剂的作用的方法，无论这些来自内源或外源来源。 此外，本发明提供了维持海马，下丘脑和皮质的稳态和健康的方法，从而保持其生物学功能。

    Benzothiophene compounds
    22.
    发明授权
    Benzothiophene compounds 失效
    苯并噻吩化合物

    公开(公告)号：US5728724A

    公开(公告)日：1998-03-17

    申请号：US692666

    申请日：1996-08-06

    申请人： Henry Uhlman Bryant ,  Timothy Alan Grese ,  Stephen Sung Yong Cho

    发明人： Henry Uhlman Bryant ,  Timothy Alan Grese ,  Stephen Sung Yong Cho

    IPC分类号： A61K31/00 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4523 ,  A61K31/4535 ,  A61P5/30 ,  A61P9/00 ,  A61P15/00 ,  A61P19/00 ,  A61P19/10 ,  A61P35/00 ,  C07D333/56 ,  A61K31/38 ,  C07D333/58 ,  C07D333/62

    CPC分类号： C07D333/56

    摘要： The present invention relates to compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl); R.sup.2 is 1-naphthyl, 2-naphthyl, 2-thienyl, 3-thienyl, benzothienyl, or --CH.sub.2 C.sub.6 H.sub.5 ; any of which may be optionally substituted with 1-3 substituents independently selected from the group halo, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl); X is --CH.sub.2 --, --CO--, or --CH(OH)--; n is 2 or 3; and R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical compositions containing compounds of formula I, and the use of such compounds, for alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer. 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： 本发明涉及式Ⅰ化合物其中R 1是-H，-OH，-O（C 1 -C 4烷基），-OCOC 6 H 5，-OCO（C 1 -C 6烷基）或-OSO 2（C 4 -C 6 烷基）; R2是1-萘基，2-萘基，2-噻吩基，3-噻吩基，苯并噻吩基或-CH2C6H5; 其中任何一个可以任选被1-3个独立地选自卤素，-OH，-O（C 1 -C 4烷基），-OCOC 6 H 5，-OCO（C 1 -C 6烷基）或-OSO 2（C 4 -C 6 烷基）; X是-CH 2 - ， - CO-或-CH（OH） - ; n为2或3; 并且R 3是1-哌啶基，1-吡咯烷基，甲基-1-吡咯烷基，二甲基-1-吡咯烷基，4-吗啉代，二甲基氨基，二乙基氨基或1-六亚甲基亚氨基; 或其药学上可接受的盐。 本发明还涉及包含式I化合物的药物组合物，以及这些化合物用于缓解绝经后综合征，特别是骨质疏松症，心血管相关病理状况和雌激素依赖性癌症的症状的用途。 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。

    Pyridine compounds, intermediates compositions and methods of use
    29.
    发明授权
    Pyridine compounds, intermediates compositions and methods of use 失效
    吡啶化合物，中间体组合物和使用方法

    公开(公告)号：US5672609A

    公开(公告)日：1997-09-30

    申请号：US683326

    申请日：1996-07-18

    申请人： Henry Uhlman Bryant ,  Don Richard Finley ,  Ken Matsumoto

    发明人： Henry Uhlman Bryant ,  Don Richard Finley ,  Ken Matsumoto

    IPC分类号： A61K31/565 ,  A61K31/57 ,  C07D213/30 ,  C07D401/02 ,  A61K31/44 ,  C07D213/02

    CPC分类号： C07D213/30 ,  A61K31/565 ,  A61K31/57

    摘要： The present invention is directed to compounds of Formula I: ##STR1## wherein: n is 2 or 3; R is dimethylamino, diethylamino, 1-piperidinyl, 1-pyrrolidinyl, 4-morpholinyl, or 1-hexamethyleneimino; R.sup.1 is hydrogen, loweralkyl of C.sub.1 -C.sub.4, phenyl, or mono or di-substituted phenyl wherein each substituent is independently halo, methyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.6 -alkylsulfonyloxy; R.sup.2 is hydrogen, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, C.sub.1 -C.sub.6 -alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C.sub.1 -C.sub.4 -loweralkyl, or C.sub.1 -C.sub.4 -loweralkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyloxy, or C.sub.4 -C.sub.6 -alkylsulfonyloxy; and the pharmaceutically acceptable acid addition salts, which are for the treatment of post menopausal symptoms such as osteoporosis, cardiovascular conditions such as hyperlipidaemia, and the like.

    摘要翻译： 本发明涉及式I化合物：其中：n为2或3; R是二甲基氨基，二乙基氨基，1-哌啶基，1-吡咯烷基，4-吗啉基或1-六亚甲基亚氨基; R1是氢，C1-C4，苯基或单或二取代苯基的低级烷基，其中每个取代基独立地是卤素，甲基，羟基，C 1 -C 6 - 烷氧基，苄氧基，C 1 -C 6 - 烷酰氧基，苯甲酰氧基，取代的苯甲酰氧基，带有1 至3个取代基，各自独立地为卤素，C 1 -C 4 - 低级烷基或C 1 -C 4 - 低级烷氧基，C 1 -C 5 - 烷氧基羰基氧基或C 4 -C 6烷基磺酰氧基; R2是氢，羟基，C1-C6-烷氧基，苄氧基，C1-C6-烷酰氧基，苯甲酰氧基，带有1至3个取代基的取代苯甲酰氧基，各自独立地是卤素，C 1 -C 4 - 低级烷基或C 1 -C 4 - 低级烷氧基，C 1 -C 5-烷氧基羰基氧基或C 4 -C 6烷基磺酰氧基; 和用于治疗绝经后症状如骨质疏松症，心血管疾病如高脂血症等的药学上可接受的酸加成盐。