2-amino-7-hydroxytetralin carboxylalkyl ethers
    3.
    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
    4.
    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。

    Propanolaminomethyltetralines, their preparation and pharmaceutical composition comprising same

    公开(公告)号:US07115780B2

    公开(公告)日:2006-10-03

    申请号:US10497379

    申请日:2002-12-02

    CPC分类号: C07C311/08 C07C2602/10

    摘要: The invention concerns compounds of formula (I), wherein A is a group of formula (a) or (b), wherein: R represents a hydrogen or halogen atom, a —S(O)z(C1–C4)Alk wherein z is 0, 1 or 2, a —NHSO2(C1–C4)Alk, —SO2NH(C1–C4)Alk, —NHSO2—(C1–C4)Alk-phenyl or —NHSO2-phenyl group, said phenyl capable of bearing a halogen atom, a (C1–C4)Alk group or a (C1–C6)alkoxy group; R1 represents a hydrogen atom or a —(C1–C4)Alk, —CO(C1–C4)Alk, —(C1–C4)Alk-phenyl or —CO-phenyl group, said phenyl capable of bearing a halogen atom or a —(C1–C4)Alk or (C1–C6)alkoxy group; R2 is a hydrogen atom, a —SO2(C1–C4)Alk, —SO2—(C1–C4)Alk-phenyl, —SO2-phenyl group, or a —(C1–C4)Alk group; X completes a saturated or unsaturated cycle of 5 to 8 atoms, capable of bearing one or two —(C1–C4)Alk groups and/or two carbonyl groups; R3 and R′3 represent each independently a hydrogen or halogen atom, a —(C1–C6)Alk, hydroxy, —CN, —(C1–C6)alkoxy, —COR4 or Y—CR8R9—COR4 group; Y represents O or CH2; R4 represents a hydroxy, (C1–C6)alkoxy or —NR5R6 group; R5 and R6 independently represent a hydrogen atom, a —(C1–C4)Alk, group, aryl or heteroaryl optionally substituted by a R7 group, aralkyl or heteroaralkyl optionally substituted by a R7 group; or R5 and R6, with the nitrogen atom which bears them, form a saturated or unsaturated cycle of 5 to 7 atoms optionally substituted by a R7 group; and R7 represents a hydrogen or halogen atom, a hydroxy, —(C1–C4)Alk, —(C1–C6)alkoxy, —NH(C1–C4)Alk, —N(C1–C4)Alk2, —COO(C1–C4)Alk, aralkyl or heteroaryl group; R8 and R9 independently represent a hydrogen atom or a —(C1–C4)Alk group; their salts or solvates, the pharmaceutical compositions containing them, a method for preparing them and synthesis intermediates