2-amino-7-hydroxytetralin carboxylalkyl ethers
    1.
    发明授权
    2-amino-7-hydroxytetralin carboxylalkyl ethers 失效
    2-氨基-7-羟基四氢萘基羧基烷基醚

    公开(公告)号:US5312961A

    公开(公告)日:1994-05-17

    申请号:US905483

    申请日:1992-06-29

    摘要: The invention relates to 2-amino-7-hydroxytetralin carboxyalkyl ethers of formula ##STR1## wherein Alk represents a straight or branched (C.sub.3 -C.sub.5)alkylene group, and R is hydrogen or (C.sub.1 -C.sub.4)alkyl, useful as starting materials in the synthesis of 7-substituted phenylethanolaminotetralins of formula (XII) ##STR2## wherein X represents hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl, or trifluoromethyl which are useful as spasmolytics and anti-glaucoma agents.The new 7-substituted phenylethanolaminotetralins (XII) as well as the intermediates in the preparation of the compounds (I), the N-protected 2-amino-7-hydroxytetralin carboxyalkyl ethers, are also claimed.

    摘要翻译: 本发明涉及式(I)的2-氨基-7-羟基四氢萘羧酸烷基醚,其中Alk表示直链或支链(C3-C5)亚烷基,R是氢或(C1-C4)烷基,可用作 合成式(XII)的7-取代苯乙醇氨基十氢化萘(XII)的原料,其中X代表氢,卤素,(C1-C4)烷基或三氟甲基,其可用作解聚物和抗青光眼剂。 还要求保护新的7-取代苯乙醇氨基十氢化萘(XII)以及化合物(I),N-保护的2-氨基-7-羟基四氢萘烷羧基烷基醚的制备中的中间体。

    Phenoxylpropanolamines, method for the production thereof and pharmaceutical compositions containing the same
    3.
    发明授权
    Phenoxylpropanolamines, method for the production thereof and pharmaceutical compositions containing the same 失效
    苯氧基丙醇胺,其制备方法和含有它们的药物组合物

    公开(公告)号:US06649627B1

    公开(公告)日:2003-11-18

    申请号:US09719640

    申请日:2001-03-26

    IPC分类号: A61K31445

    摘要: The invention concerns compounds of formula (Ia) wherein R1a represents hydrogen, an —S(O)z —(C1-C4)Alk group, a —CO(C1-C4)Alk group, an —NHSO2—(C1-C4)Alk group, an NCHl (C1-C4) Alk group, a 2-furyl group or a halogen; R2 represents hydrogen or a (C1-C4)Alk group, a (C1-C4) alkoxyl group, a halogen, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NH2, —NHSO2(C1-C4)Alk; m and n are independently 0, 1 or 2; R3 and R4 independently represent hydrogen or a (C1-C4)Alk group; Z is 1 or 2 and their salts or solvates, the pharmaceutical compositions that contain them, the process for their preparation, and intermediate synthesis products.

    摘要翻译: 本发明涉及式(Ia)化合物,其中R 1a表示氢,-S(O)z - (C 1 -C 4)Alk基,-CO(C 1 -C 4)Alk基,-NHSO 2 - (C 1 -C 4) 基团,NCH1(C1-C4)Alk基团,2-呋喃基或卤素; R2表示氢或(C1-C4)Alk基团,(C1-C4)烷氧基,卤素,-COOH, COO(C1-C4)Alk,-CN,-CONR3R4,-NO2,-SO2NH2,-NHSO2(C1-C4)Alk; m和n分别为0,1或2; R3和R4独立地表示氢或(C1 -C4)Alk基; Z为1或2及其盐或溶剂化物,含有它们的药物组合物,其制备方法和中间合成产物。

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

    公开(公告)号:US07622460B2

    公开(公告)日:2009-11-24

    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.