知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

40 条记录 (耗时 0.018 秒)

    Indole derivatives pharmaceutical preparations based thereon, and .beta.-receptor stimulation therewith
    3.
    发明授权
    Indole derivatives pharmaceutical preparations based thereon, and .beta.-receptor stimulation therewith 失效
    基于此的吲哚衍生物药物制剂和其中的β-受体刺激

    公开(公告)号：US4835175A

    公开(公告)日：1989-05-30

    申请号：US917445

    申请日：1986-10-10

    申请人： Josef Heindl ,  Olaf Loge

    发明人： Josef Heindl ,  Olaf Loge

    IPC分类号： A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  A61P37/08 ,  C07C205/37 ,  C07D209/08 ,  C07D209/42 ,  C07D413/14

    CPC分类号： C07C255/00 ,  C07C205/37 ,  C07D209/08 ,  C07D209/42

    摘要： Indole derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1-6 carbon atoms, or benzylR.sub.2 is hydrogen, alkyl of up to 4 carbon atoms, free or esterified hydroxyalkyl of up to 4 carbon atoms, or free, amidated or esterified carboxy or carboxyalkyl,R.sub.3 is hydrogen or alkyl containing 1-6 carbon atoms,R.sub.4 is hydrogen or alkyl containing 1-6 carbon atoms andR.sub.5 is hydrogen, or alkyl, alkenyl, or cycloalkyl, all of which per se contain up to 6 carbon atoms, and all of which are optionally substituted by a free or esterified carboxy group or by an optionally substituted phenyl group; or a polymethylene group of up to 8 carbon atoms linking the first indole residue to a second indole residue of Formula Ia ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as defined above,and the physiologically acceptable salts thereof with acids and, optionally, their alkali metal and alkaline earth metal salts,possess valuable pharmacological properties, such as stimulating .beta.-receptors and prevention of premature labor, are described.

    摘要翻译： 式I的吲哚衍生物其中R 1是氢，1-6个碳原子的烷基或苄基R 2是氢，至多4个碳原子的烷基，最多4个碳原子的游离或酯化的羟烷基，或 游离的，酰胺化的或酯化的羧基或羧基烷基，R3是氢或含有1-6个碳原子的烷基，R4是氢或含1-6个碳原子的烷基，R5是氢或烷基，烯基或环烷基，其本身都是 含有多达6个碳原子，并且所有这些都任选被游离或酯化的羧基或任选取代的苯基取代; 或至多8个碳原子的多亚甲基，其连接第一吲哚残基与式Ia的第二吲哚残基（Ia），其中R 1，R 2，R 3和R 4如上所定义，其生理上可接受的盐与 描述了酸和任选的其碱金属和碱土金属盐，具有有价值的药理学性质，例如刺激β-受体和预防早产。

    9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents
    4.
    发明授权
    9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents 失效
    9-氟前列腺素衍生物，其制备和用作药物

    公开(公告)号：US4789685A

    公开(公告)日：1988-12-06

    申请号：US4733

    申请日：1987-01-20

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    IPC分类号： A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/00 ,  C07C405/0016 ,  C07C405/0041

    摘要： 9-fluoroprostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is the residue ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 and A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,D and E jointly are a direct bond orD is straight-chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen or sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine, or alkyl,R.sub.4 is a free or functionally modified hydroxy group, andR.sub.5 is hydrogen, an optionally substituted aliphatic group, e.g., alkyl or halosubstituted alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group, and, when R.sub.2 is H, the physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g., as luteolytics or abortifacients.

    摘要翻译： 其中R 1是CH 2 OH或其中R 2是氢，烷基，环烷基，芳基或杂环残基的式I的α-氟仿烷基衍生物。 或R1是残基，其中R3是酸残基或R2和A是-CH2-CH2-或顺式-CH = CH-，B是-CH2-CH2-，反式-CH = CH-或-C3BOND C，W是游离的或官能改性的羟基亚甲基，其中OH基可以是α或β位，D和E共同是直接键，或D是1-10的直链或支链亚烷基或亚链烯基 可以任选被氟原子取代的碳原子，E是氧或硫，直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自是氢，氯或烷基 R4是游离的或官能改性的羟基，R5是氢，任意取代的脂族基团，例如烷基或卤代取代的烷基，环烷基，任选被取代的芳基或杂环基，当R2是H时，生理上相容的盐 具有有价值的药理学性质，例如作为骨质疏松症或流产者。

    Crystalline prostanoic acid esters
    6.
    发明授权
    Crystalline prostanoic acid esters 失效
    结晶前列腺酸酯

    公开(公告)号：US4154953A

    公开(公告)日：1979-05-15

    申请号：US826908

    申请日：1977-08-19

    申请人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Walter Elger ,  Olaf Loge ,  Wolfgang Losert

    发明人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Walter Elger ,  Olaf Loge ,  Wolfgang Losert

    IPC分类号： C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/00

    摘要： Prostanoic acid esters of the formulaPG-- CH.sub.2 -- X-- Ywherein PG is the prostanoyloxy radical of a prostaglandin, X is a carbon-carbon single bond, carbonyl or carbonyloxy, and Y is substituted phenyl are easily crystallized compounds at least as active as the unesterified prostanoic acid and useful for the purification of the parent prostaglandin are prepared by reacting, in the presence of an agent which splits off hydrogen halide, the unesterified prostaglandin with a halide of the formula Hal--CH.sub.2 --X--Y, wherein Hal is a halogen atom and X and Y have the values given above.

    摘要翻译： 式PG-CH2-X-Y的前列腺酸，其中PG是前列腺素的前烷氧基自由基，X是碳 - 碳单键，羰基或羰氧基，Y是取代的苯基，容易结晶化合物至少与 通过使未分解的前列腺素与式Hal-CH2-XY的卤化物反应，其中Hal是卤素，其中Hal是卤素 原子，X和Y具有上面给出的值。

    9-halogen-(Z)-prostaglandin derivatives, process for their production and their use as pharmaceutical agents
    9.
    发明授权
    9-halogen-(Z)-prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
    9-卤素 - （Z） - 前列腺素衍生物，其制备方法及其作为药剂的用途

    公开(公告)号：US06225347B1

    公开(公告)日：2001-05-01

    申请号：US08313667

    申请日：1994-09-27

    申请人： Bernd Buchmann ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Bernd Raduechel ,  Olaf Loge ,  Walter Elger ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    发明人： Bernd Buchmann ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Bernd Raduechel ,  Olaf Loge ,  Walter Elger ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    IPC分类号： C07C40500

    CPC分类号： C07C405/0016 ,  C07C405/00 ,  C07C405/0025

    摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I in which Z represents the radicals Hal represents a chlorine or fluorine atom in the alpha or beta position, R1 represents the radical with R2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl or heterocyclic radical or R1 represents the radical with R3 meaning an acid radical or the radical R2 and A represents a —CH2—CH2—, a trans-CH═CH or —C≡C group, W represents a free or a functionally modified group, and the respective OH groups can be in the alpha or beta position, D and E together represent a direct bond or D represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, and E represents an oxygen or sulfur atom, a direct bond, a C≡C bond or a —CR6═CR7 group, and R6 and R7 are different and mean a hydrogen atom, a chlorine atom or a C1-C4 alkyl group, R4 resents a free or functionally modified hydroxy group, R5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group, and if R2 means a hydrogen atom, its salts with physiologically compatible bases or its cyclodextrin chlathrates, process for their production and their pharmaceutical use.

    摘要翻译： 本发明涉及式Iin的9-卤素 - （Z）前列腺衍生物，其中Z代表基团.Hal表示α或β位上的氯或氟原子，R 1表示R 2表示氢原子，烷基，环烷基，芳基或 杂环基或R 1表示基团，其中R 3表示酸基或基团R 2且A表示-CH 2 -CH 2 - ，反式-CH = CH或-C = C基团，W表示游离或功能修饰基团， OH基可以是α或β位，D和E一起代表直接键或D表示具有1-10个C原子的直链亚烷基，具有2-10个C原子的支链亚烷基或环状亚烷基 具有3-10个C原子的基团，其任选地可以被氟原子取代，E表示氧或硫原子，直接键合，C = C键或-CR 6 = CR 7基团，并且R 6和R 7不同， 一个氢原子，一个氯原子或一个C 1 -C 4烷基，R 4是一个游离的 或官能改性的羟基，R 5表示氢原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基，如果R 2表示氢原子，则其与生理上相容的碱或其环糊精的盐 chlathrates，生产过程及其药物用途。

    9-halogen-(Z) prostaglandin derivatives, process for their production and their use as pharmaceutical agents
    10.
    发明授权
    9-halogen-(Z) prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
    9-卤素 - （Z）前列腺素衍生物，其制备方法及其作为药剂的用途

    公开(公告)号：US5891910A

    公开(公告)日：1999-04-06

    申请号：US467888

    申请日：1995-06-06

    申请人： Bernd Buchmann ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Bernd Raduechel ,  Olaf Loge ,  Walter Elger ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    发明人： Bernd Buchmann ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Bernd Raduechel ,  Olaf Loge ,  Walter Elger ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    IPC分类号： C07C405/00 ,  A61K31/557

    CPC分类号： C07C405/00 ,  C07C405/0016 ,  C07C405/0025

    摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I ##STR1## in which ##STR2## Z represents the radicals Hal represents a chlorine or fluorine atom,R.sub.1 represents ##STR3## A represents a --CH.sub.2 --CH.sub.2 --, a trans--CH=CH or --C.ident.C, W represents a free or a functionally modified ##STR4## group, D and E together represent a direct bond orD represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, andE represents an oxygen or sulfur atom, a direct bond, a C.ident.C bond or a --CR.sub.6 =CR.sub.7 group, and R.sub.6 and R.sub.7 are different and mean a hydrogen atom, a chlorine atom or a C.sub.1 -C.sub.4 alkyl group,R.sub.4 represents a free or functionally modified hydroxy,R.sub.5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group.

    摘要翻译： 本发明涉及式I的9-卤代 - （Z）前列腺衍生物，其中，Z表示基团，Hal表示氯或氟原子，R1表示A表示 -CH 2 -CH 2 - ，反式-CH = CH或-C = C，W表示游离或官能改性的基团，D和E一起表示直接键或D表示直链亚烷基，其中1 -10个C原子，具有2-10个碳原子的支链亚烷基或具有3-10个C原子的环状亚烷基，其任选可以被氟原子取代，E表示氧或硫原子，直接键 ，C = C键或-CR6 = CR7基，R6和R7不同，表示氢原子，氯原子或C1-C4烷基，R4表示游离或官能改性的羟基，R5表示氢 原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基。