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29 条记录 (耗时 0.106 秒)

    Benzothiophenes
    11.
    发明授权
    Benzothiophenes 失效
    苯并噻吩

    公开(公告)号：US06291484B1

    公开(公告)日：2001-09-18

    申请号：US09482432

    申请日：2000-01-13

    申请人： Henry Uhlman Bryant ,  Jeffrey Alan Dodge

    发明人： Henry Uhlman Bryant ,  Jeffrey Alan Dodge

    IPC分类号： A61K31445

    CPC分类号： C07D409/12 ,  C07D333/56

    摘要： This invention provides novel benzothiophene compounds of the formula I: which are useful for the treatment of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further relates to pharmaceutical formulations of compounds of formula I.

    摘要翻译： 本发明提供了式I的新型苯并噻吩化合物：其可用于治疗与绝经后综合征相关的各种医学病症，以及雌激素依赖性疾病，包括乳腺癌，子宫癌和子宫颈癌。 本发明还涉及式I化合物的药物制剂。

    Indene compounds having activity as SERMS
    14.
    发明授权
    Indene compounds having activity as SERMS 失效
    具有SERMS活性的茚化合物

    公开(公告)号：US5994370A

    公开(公告)日：1999-11-30

    申请号：US64548

    申请日：1998-04-22

    申请人： Henry Uhlman Bryant ,  Charles David Jones ,  Pamela Ann Pennington

    发明人： Henry Uhlman Bryant ,  Charles David Jones ,  Pamela Ann Pennington

    IPC分类号： C07D295/08 ,  A61K31/138 ,  A61K31/40 ,  A61K31/4453 ,  A61K31/5375 ,  A61P3/06 ,  A61P5/30 ,  A61P19/10 ,  C07B61/00 ,  C07C41/18 ,  C07C43/23 ,  C07D295/092 ,  C07D339/08 ,  A61K31/445 ,  A61K31/55 ,  C07D207/08 ,  C07D211/06

    CPC分类号： C07D295/088 ,  C07C43/23 ,  C07D339/08 ,  C07C2102/08

    摘要： The present invention provides a class of substituted indene compounds and their pharmaceutically acceptable salts which possess selective estrogen receptor modulator (SERM) activity and are thus useful in the treatment of osteoporosis and cardiovascular disease, particularly hyperlipidemia in women. The compounds possess the structure ##STR1## in which R.sup.1 is hydrogen, hydroxy, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.2 is hydrogen, hydroxy, halo, alkoxy, phenylcarbonyloxy, alkylcarbonyloxy, or alkylsulfonyloxy. R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexa-methyleneimino, and n is 2 or 3. The dashed line bond between the carbon atoms at positions 1 and 2 of the indene nucleus represent an optional double bond with the proviso that when the double bond is absent, the parenthetic hydroxy group at position 1 is present and vice versa. Certain 2,3-dihydro-1H-indene precursors to the disclosed indene compounds also possess SERM activity and are useful for the same purposes.

    摘要翻译： 本发明提供一类具有选择性雌激素受体调节剂（SERM）活性的取代茚化合物及其药学上可接受的盐，因此可用于治疗骨质疏松症和心血管疾病，特别是妇女高脂血症。 该化合物具有其中R 1为氢，羟基，烷氧基，苯基羰基氧基，烷基羰基氧基或烷基磺酰氧基的结构。 R2是氢，羟基，卤素，烷氧基，苯基羰基氧基，烷基羰基氧基或烷基磺酰氧基。 R3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，二异丙基氨基或1-己亚甲基亚氨基，n是2或3.虚线键 在茚核位置1和2之间的碳原子之间代表任选的双键，条件是当双键不存在时，存在位置1的支链羟基，反之亦然。 所公开的茚化合物的某些2,3-二氢-1H-茚前体也具有SERM活性，并且可用于相同的目的。

    Pyridine compounds intermediates processes compositions and methods
    20.
    发明授权
    Pyridine compounds intermediates processes compositions and methods 失效
    吡啶化合物中间体处理组合物和方法

    公开(公告)号：US5750708A

    公开(公告)日：1998-05-12

    申请号：US838098

    申请日：1997-04-15

    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 ,  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，取代的苯甲酰氧基轴承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。