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34 条记录 (耗时 0.029 秒)

    Phenoxypropanolamines, preparation and therapeutic use thereof
    32.
    发明授权
    Phenoxypropanolamines, preparation and therapeutic use thereof 失效
    苯氧基丙胺胺，其制备和治疗用途

    公开(公告)号：US06852736B2

    公开(公告)日：2005-02-08

    申请号：US10149626

    申请日：2000-12-15

    申请人： Philippe R. Bovy ,  Roberto Cecchi ,  Olivier Venier

    发明人： Philippe R. Bovy ,  Roberto Cecchi ,  Olivier Venier

    IPC分类号： A61K31/4545 ,  A61K31/5377 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10 ,  A61P15/00 ,  A61P17/02 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P27/06 ,  C07D401/04 ,  C07D401/14 ,  A61K31/445 ,  C07D211/06 ,  C07D401/06

    CPC分类号： C07D401/04 ,  C07D401/14

    摘要： The invention concerns phenoxypropanolamines of formula (I) in which R1 represents a hydrogen, a group —S(O)z—(C1-C4)alk-R′, (R′ being H, phenyl or (C1-C4)alkoxy), —NHSO2—(C1-C4)alk or NHCO(C1-C4)alk; m and n are each independently 0, 1 or 2; R2 and R3 independently represent a hydrogen, a (C5-C6)alkyl, (C3-C6)cycloalkyl, (C1-C4)alkoxy, hydrogen(C1-C4)alkoxy-(C1-C4)alkyl, mono- or di(C1-C4)alkamino(C1-C4)alkyl, pyrrolidino(C1-C4)alkyl, phenylamino or (C2-C4)alkenyl group, an aromatic or heteroaromatic group optionally substituted with a group R4, an aralkyl or heteroaralkyl group optionally substituted with a group R4, R2 and R3 can also together constitute a saturated or unsaturated ring of 3 to 8 atoms possibly bearing a (C1-C4)alkyl, amino (C1-C4)alkyl, carbamoyl or benzyl substituent; R4 represents a hydrogen or a halogen, or a group —CO(C1-C4)alk or a group —NHSO2—(C1-C4)alk; a group (C1-C4)alk, a group (C1-C4)alkoxy, a halogen, —COOH, —COO(C1-C4)alk, —CN, —CONR3R4, —NO2, —SO2NH2 or —NHSO2(C1-C4)alk; z is 1 or 2; and the salts or solvates thereof. The compounds have agonist activity toward β-3 adrenergic receptors.

    摘要翻译： 本发明涉及式（I）的苯氧基丙醇胺，其中R 1表示氢，-S（O）z - （C 1 -C 4）烷基-R'，（R'为H，苯基或（C 1 -C 4）烷氧基） ，-NHSO 2 - （C 1 -C 4）烷基或NHCO（C 1 -C 4）烷基; m和n各自独立地为0,1或2; R2和R3独立地表示氢，（C5-C6）烷基，（C3-C6）环烷基，（C1-C4）烷氧基，氢（C1-C4）烷氧基 - （C1-C4）烷基， C 1 -C 4烷基，吡咯烷子基（C 1 -C 4）烷基，苯基氨基或（C 2 -C 4）烯基，任选被基团R 4取代的芳族或杂芳族基团，任选被 基团R4，R2和R3也可以一起构成3至8个可能带有（C 1 -C 4）烷基，氨基（C 1 -C 4）烷基，氨基甲酰基或苄基取代基的饱和或不饱和环; R4表示氢或卤素，或基团-CO（C1-C4）烷基或基团-NHSO2-（C1-C4）烷基; （C1-C4）烷基，（C1-C4）烷氧基，卤素，-COOH，-COO（C1-C4）烷基，-CN，-CONR3R4，-NO2，-SO2NH2或-NHSO2（C1- C4）烷基; z为1或2; 及其盐或溶剂合物。 该化合物对β-3肾上腺素能受体具有激动作用。

    Cycloheptimidazolone compounds as angiotensin II antagonists for control of hypertension
    33.
    发明授权
    Cycloheptimidazolone compounds as angiotensin II antagonists for control of hypertension 失效
    环庚咪唑酮化合物作为血管紧张素II拮抗剂用于控制高血压

    公开(公告)号：US5281615A

    公开(公告)日：1994-01-25

    申请号：US840471

    申请日：1992-02-24

    申请人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

    发明人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

    IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/675 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  A61P43/00 ,  C07D235/02 ,  C07D403/10 ,  C07F9/6558 ,  C07D257/04

    CPC分类号： C07D235/02 ,  C07D403/10

    摘要： A class of cycloheptimidazolone compounds is described as angiotensin II antagonists for use in control of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, alkyl, halo, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, haloalkyl, alkoxyalkyl, formyl, cyano, alkoxy, phenoxy, phenylthio, alkylthio; wherein R.sup.3 is alkyl, alkenyl, alkynyl, hydroxyalkyl and alkoxyalkyl; wherein each of R.sup.5 through R.sup.13 is independently selected from hydrido, alkyl, haloalkyl, halo, nitro, cyano, hydroxy, alkoxy, alkylthio, aryl, aryloxy, arythio, and acidic groups such as carboxylic acid, with the proviso that at least one of R.sup.9 through R.sup.13 substituents is an acidic group; or a pharmaceutically-acceptable ester, amide or salt thereof.

    摘要翻译： 一类环庚咪唑酮化合物被描述为用于控制高血压的血管紧张素II拮抗剂。 特别感兴趣的化合物是式（*化学结构*）的化合物，其中R 1和R 2各自独立地选自氢，烷基，卤素，烷酰基，羧基，烷氧基羰基，苯基，卤代烷基，烷氧基烷基，甲酰基，氰基，烷氧基，苯氧基 ，苯硫基，烷硫基; 其中R3是烷基，烯基，炔基，羟基烷基和烷氧基烷基; 其中R 5至R 13中的每一个独立地选自氢，烷基，卤代烷基，卤素，硝基，氰基，羟基，烷氧基，烷硫基，芳基，芳氧基，仲氨基和酸性基团如羧酸，条件是至少一个 R9至R13取代基是酸性基团; 或其药学上可接受的酯，酰胺或其盐。