利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

134 条记录 (耗时 0.026 秒)

    9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents
    21.
    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。

    9-Bromoprostaglandins, their preparation, and their use as medicaments
    23.
    发明授权
    9-Bromoprostaglandins, their preparation, and their use as medicaments 失效
    9-溴前列​​腺素，其制剂及其用作药物

    公开(公告)号：US4487953A

    公开(公告)日：1984-12-11

    申请号：US446888

    申请日：1982-12-06

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger

    IPC分类号： A61K31/16 ,  A61K31/19 ,  A61K31/20 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D309/12 ,  C07C177/00

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

    摘要： Compounds of Formula (I) ##STR1## wherein the 9-bromine atom can be in the .alpha.- or .beta.-position,R.sub.1 is CH.sub.2 OH or C(O)OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is C(O)NHR.sub.3 wherein R.sub.3 is an acid residue or R.sub.2 ; andA 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 or a free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D and E together are a direct bond; orD is straight-chain, branched, or cyclic alkylene of 1-10 carbon atoms, optionally substituted by fluorine atoms; andE is oxygen, sulfur, a direct bond --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 and R.sub.7 are different from each other and each is hydrogen, chlorine, or C.sub.1 -C.sub.4 -alkyl;R.sub.4 is a free or functionally modified hydroxy group;R.sub.5 is hydrogen, alkyl, halo-substituted alkyl, cycloalkyl, optionally substituted aryl, or a heterocyclic group; and, when R.sub.2 is hydrogen, the salts thereof with physiologically compatible bases,are pharmacologically active compounds, e.g., as abortifacients.

    摘要翻译： 式（I）化合物其中9-溴原子可以是α或β-位，R1是CH2OH或C（O）OR2，其中R2是氢，烷基，环烷基，芳基， 或杂环残基; 或R 1为C（O）NHR 3，其中R 3为酸残基或R 2; 并且A是-CH 2 -CH 2 - 或顺式-CH = CH-; B是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; W是游离或官能改性的羟基亚甲基或游离或官能改性的“IMAGE”，其中OH基可以是α-或β-位; D和E一起是直接的债券; 或D是1-10个碳原子的直链，支链或环状亚烷基，任选被氟原子取代; 并且E是氧，硫，直接键-C 3或C 6或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自是氢，氯或C 1 -C 4 - 烷基; R4是游离的或官能改性的羟基; R5是氢，烷基，卤素取代的烷基，环烷基，任选取代的芳基或杂环基; 并且当R 2为氢时，其与生理上相容的碱的盐是药理活性化合物，例如作为流产者。

    Crystalline prostanoic acid esters
    26.
    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。

    COMPOUNDS WITH A SULPHONAMIDE GROUP AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS
    29.
    发明申请
    COMPOUNDS WITH A SULPHONAMIDE GROUP AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS 审中-公开
    具有磺酰胺基团的化合物和含有这些化合物的药物组合物

    公开(公告)号：US20090023896A1

    公开(公告)日：2009-01-22

    申请号：US12142332

    申请日：2008-06-19

    申请人： Walter Elger ,  Alexander Hillisch ,  Annemarie Hedden ,  Sigfrid Schwarz ,  Klaus Schollkopf

    发明人： Walter Elger ,  Alexander Hillisch ,  Annemarie Hedden ,  Sigfrid Schwarz ,  Klaus Schollkopf

    IPC分类号： C07K7/06 ,  C07J1/00

    CPC分类号： C07J41/0044 ,  C07J41/0038 ,  C07J41/005

    摘要： This invention relates to compounds that as prodrugs and/or vehicles make it possible for an active ingredient to be taken up into erythrocytes and/or an active ingredient to bind to erythrocytes, whereby the uptake of the compounds into erythrocytes and/or the binding of the compounds to erythrocytes is made possible by a group —SO2NR1R2, whereby R1 and R2, independently of one another, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. By the prodrugs according to the invention, active ingredients, such as endogenous substances, natural substances and synthetic substances with therapeutically valuable properties with a high “first pass” effect are made available orally to a reasonable extent or are decisively improved relative to oral activity.

    摘要翻译： 本发明涉及作为前药和/或载体的化合物，使活性成分能够摄入红细胞和/或活性成分以结合红细胞，由此将化合物摄入红细胞和/或结合 对于红细胞的化合物可以通过基团-SO 2 NR 1 R 2来实现，其中R 1和R 2彼此独立地表示氢原子，酰基，烷基，环烷基，芳基，氰基或羟基 组。 通过根据本发明的前药，可以以合理的方式口服提供活性成分，例如内源物质，天然物质和具有高“第一道”效果的治疗有价值的性质的合成物质，或者相对于口服活性而言是有显着改善的。

    8Beta-Hydrocarbyl-Substituted Estratrienes As Selectively Active Estrogens
    30.
    发明申请
    8Beta-Hydrocarbyl-Substituted Estratrienes As Selectively Active Estrogens 审中-公开
    8Beta-Hydrocarbyl-Substituted Estratrienes As Selective Active Estrogens

    公开(公告)号：US20080182829A1

    公开(公告)日：2008-07-31

    申请号：US12045979

    申请日：2008-03-11

    申请人： Olaf Peters ,  Alexander Hillisch ,  Ina Thieme ,  Walter Elger ,  Christa Hegele-Hartung ,  Uwe Kollenkirchen ,  Karl-Heinrich Fritzemeier ,  Vladimir Patchev

    发明人： Olaf Peters ,  Alexander Hillisch ,  Ina Thieme ,  Walter Elger ,  Christa Hegele-Hartung ,  Uwe Kollenkirchen ,  Karl-Heinrich Fritzemeier ,  Vladimir Patchev

    IPC分类号： A61K31/58 ,  A61K31/565 ,  A61P25/28 ,  A61P19/02 ,  A61P1/00 ,  A61P15/00

    CPC分类号： C07J1/007 ,  C07J1/0059 ,  C07J1/0062 ,  C07J1/0074 ,  C07J41/0072

    摘要： This invention describes the new 8β-substituted estratrienes of general formula I in which R2, R3, R6, R6′, R7, R7′, R9, R11, R11′, R12, R14, R15, R15′, R16, R16′, R17, R17′ have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8β-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.

    摘要翻译： 本发明描述了通式I的新的8-取代的雌三烯，其中R 2，R 3，R 6，R 6， R 7，R 7，R 9，R 11，R 11， > 11'，R 12，R 14，R 15，R 15'，R 15， R 16，R 16，R 17，R 17，R 17具有在说明书中指出的含义， R 8是指具有至多5个碳原子的直链或支链，任选部分或完全卤代的烷基或烯基，乙炔基或丙-1-基基团作为药物活性物质 具有体外对大鼠前列腺的雌激素受体制剂的亲和力高于大鼠子宫雌激素受体制剂的体内成分，并且在体内优选对骨骼而不是子宫的优先作用和/或对刺激表达的显着作用 5HT2a受体和5HT2a转运蛋白，它们的产物 n，其治疗用途和含有新化合物的药物分配形式。 本发明还描述了这些化合物用于治疗雌激素缺乏诱导的疾病和病症的用途，以及在具有有利于其雌激素作用的解离的化合物的总体结构中使用8-取代的雌三醇结构部分 骨头而不是子宫。