CYCLOHEXYL(ALKYL)PROPANOLAMINES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

    公开(公告)号:US20080261949A1

    公开(公告)日:2008-10-23

    申请号:US12144843

    申请日:2008-06-24

    摘要: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen atom, a (C1-C6)alkyl group, a (C1-C4)alkoxy group, a —COO(C1-C4)alkyl group, a —CO(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl groups, —NO2, —CN, —CONR4R5, —COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; R4 and R5 represent, independently, a hydrogen atom, a phenyl, a (C1-C4)alkyl group or a phenyl-(C1-C4)alkyl group or R4 and R5 with the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.

    2-aminoethyl-benzofuran derivatives, preparation thereof and
therapeutical use thereof
    13.
    发明授权
    2-aminoethyl-benzofuran derivatives, preparation thereof and therapeutical use thereof 失效
    2-氨基乙基 - 苯并呋喃衍生物,其制备及其治疗用途

    公开(公告)号:US6063810A

    公开(公告)日:2000-05-16

    申请号:US125947

    申请日:1998-08-31

    CPC分类号: C07D307/79

    摘要: Compounds of formula (I), wherein A is a hydrogen atom or a hydroxyl group; B is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group; each of R.sub.1, R.sub.2 and R.sub.5, which are the same or different, is a hydrogen atom, a halogen such as chlorine, bromine or fluorine, a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl, C.sub.6, C.sub.10 or C.sub.14 aryl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 hydroxyalkyl, C.sub.1-6 alkoxyalkyl, C.sub.1-6 alkoxy, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group, or R.sub.1 and R.sub.2 taken together form a C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl or C.sub.6, C.sub.10 or C.sub.14 aryl ring, except for compounds in which R.sub.1 and R.sub.2 are both hydrogen; each of R.sub.3 and R.sub.4, which are the same or different, is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl or C.sub.3-8 cycloalkenyl group, or R.sub.3 and R.sub.4 taken together form a C.sub.2-6 cycloalkyl or C.sub.3-6 cycloalkenyl ring, e.g., piperidyl, azetidinyl or pyrrolidyl; in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures;, as well as pharmaceutically acceptable acid addition salts thereof. The compounds may be used in therapy.

    摘要翻译: PCT No.PCT / FR97 / 00383 Sec。 371日期1998年8月31日 102(e)日期1998年8月31日PCT 1997年3月5日PCT公布。 公开号WO97 / 32870 日期:1997年9月12日,式(I)的化合物,其中A为氢原子或羟基; B是氢原子或C 1-8烷基,C 1-8烯基,C 1-8氟烷基或C 1-8全氟烷基; R 1,R 2和R 5各自相同或不同,为氢原子,卤素如氯,溴或氟,C 1-8烷基,C 1-8烯基,C 3-8环烷基,C 3-8环烯基 ,C 6,C 10或C 14芳基,C 1-6烷氧基羰基,C 1-6羟基烷基,C 1-6烷氧基烷基,C 1-6烷氧基,C 1-8氟代烷基或C 1-8全氟烷基,或者R 1和R 2一起形成C 3-8 环烷基,C3-8环烯基或C6,C10或C14芳基环,其中R1和R2均为氢的化合物; R 3和R 4各自相同或不同,为氢原子或C 1-8烷基,C 1-8烯基,C 3-8环烷基或C 3-8环烯基,或者R 3和R 4一起形成C2- 6环烷基或C 3-6环烯基环,例如哌啶基,氮杂环丁烷基或吡咯烷基; 以对映异构体,非对映异构体或其混合物的形式,包括外消旋混合物,以及其药学上可接受的酸加成盐。 该化合物可用于治疗。

    Cyclohexyl(alkyl)propanolamines, preparation method and pharmaceutical compositions containing same

    公开(公告)号:US07718646B2

    公开(公告)日:2010-05-18

    申请号:US12144843

    申请日:2008-06-24

    摘要: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen atom, a (C1-C6)alkyl group, a (C1-C4)alkoxy group, a —COO(C1-C4)alkyl group, a —CO(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl groups, —NO2, —CN, —CONR4R5, —COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; R4 and R5 represent, independently, a hydrogen atom, a phenyl, a (C1-C4)alkyl group or a phenyl-(C1-C4)alkyl group or R4 and R5 with the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.

    Cyclohexyl(alkyl)-propanolamines, preparation method and pharmaceutical compositions containing same

    公开(公告)号:US07388031B2

    公开(公告)日:2008-06-17

    申请号:US10432493

    申请日:2001-11-30

    IPC分类号: A61K31/18 C07C311/08

    摘要: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1–C4)alkyl group, an —NHSO2(C1–C4)alkyl group, an —SO2NH(C1–C4)alkyl group, an —NHSO2phenyl-(C1–C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1–C4)alkyl group or with a (C1–C4)alkoxy group; R1 represents a hydrogen atom or a (C1–C4)alkyl group, a —CO(C1–C4)alkyl group, a phenyl-(C1–C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1–C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1–C4)alkyl group, an —SO2phenyl-(C1–C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1–C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen atom, a (C1–C6)alkyl group, a (C1–C4)alkoxy group, a —COO(C1–C4)alkyl group, a —CO(C1–C4)alkyl group, an —NHSO2(C1–C4)alkyl group, an —NHSO2phenyl-(C1–C4)alkyl groups, —NO2, —CN, —CONR4R5, —COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; R4 and R5 represent, independently, a hydrogen atom, a phenyl, a (C1–C4)alkyl group or a phenyl-(C1–C4)alkyl group or R4 and R5 with the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.

    Compositions of silico-sodo-calcic glasses and their applications
    18.
    发明授权
    Compositions of silico-sodo-calcic glasses and their applications 失效
    硅钙石眼镜组合及其应用

    公开(公告)号:US5958812A

    公开(公告)日:1999-09-28

    申请号:US991558

    申请日:1997-12-16

    摘要: This invention concerns a thermally stable glass composition, which comprises the following constituents in the following proportions by weight:______________________________________ SiO.sub.2 45 to 68% Al.sub.2 O.sub.3 0 to 20% ZrO.sub.2 0 to 20% B.sub.2 O.sub.3 0 to 10% Na.sub.2 O 2 to 12% K.sub.2 O 3.5 to 9% CaO 1 to 13% MgO 0 to 8%______________________________________the sum of the contents of the oxides SiO.sub.2, Al.sub.2 O.sub.3 and ZrO.sub.2 remaining equal to or less than 70%, the sum of the oxides Al.sub.2 O.sub.3 and ZrO.sub.2 being equal to or greater than 2%, the sum of the alkaline oxides Na.sub.2 O and K.sub.2 O being equal to or greater than 8%, said composition comprising, if desired, the oxides BaO and/or SrO in proportions such that:11%.ltoreq.MgO+CaO--BaO+SrO>30%This glass composition may be used for the production of substrates for an emissive screen or for that of a fire-resistant pane.

    摘要翻译: 本发明涉及一种热稳定性玻璃组合物,其包含以下重量比的以下组分: - SiO 2 45至68%-Al 2 O 3 0至20%-ZrO 2 0至20%-B 2 O 3 0至10%Na 2 O 2至12 % - K2O 3.5〜9% - CaO 1〜13% - MgO 0〜8% - 氧化物SiO 2,Al 2 O 3和ZrO 2的含量的总和等于或小于70%,氧化物Al 2 O 3和ZrO 2的总和 等于或大于2%,碱性氧化物Na 2 O和K 2 O的总和等于或大于8%,如果需要,所述组合物包含氧化物BaO和/或SrO,其比例使得:11% = MgO + CaO-BaO + SrO> 30%该玻璃组合物可用于生产用于发射屏幕或耐火玻璃板的基板。