会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明授权
    • 9-fluoroprostaglandin derivatives, their preparation and use as
medicinal agents
    • 9-氟前列腺素衍生物,其制备和用作药物
    • US4789685A
    • 1988-12-06
    • US4733
    • 1987-01-20
    • Werner SkuballaBernd RaduechelNorbert SchwarzHelmut VorbrueggenWalter ElgerOlaf LogeMichael-Harold Town
    • Werner SkuballaBernd RaduechelNorbert SchwarzHelmut VorbrueggenWalter ElgerOlaf LogeMichael-Harold Town
    • A61K31/557A61K31/5575A61P43/00C07C67/00C07C401/00C07C405/00C07C177/00
    • C07C405/00C07C405/0016C07C405/0041
    • 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.
    • 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。
    • 6. 发明授权
    • 9-Fluoroprostaglandin derivatives, and use as medicinal agents
    • 9-氟前列腺素衍生物,用作药物
    • US4454339A
    • 1984-06-12
    • US395448
    • 1982-07-06
    • Werner SkuballaBernd RaduechelNorbert SchwarzHelmut VorbrueggenWalter ElgerOlaf LogeMichael-Harold Town
    • Werner SkuballaBernd RaduechelNorbert SchwarzHelmut VorbrueggenWalter ElgerOlaf LogeMichael-Harold Town
    • A61K31/557A61K31/5575A61P43/00C07C67/00C07C401/00C07C405/00C07C177/00
    • C07C405/00C07C405/0016C07C405/0041
    • 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, physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g., as luteolytics or abortifacients.
    • 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1-氟代衍生物(Ⅰ) 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,任选取代的芳基或杂环基,当R 2是H时,其生理上相容的盐 具有碱性,具有有价值的药理学性质,例如作为纤溶素或流产。
    • 9. 发明授权
    • Process and reagent for the determination of substrates or enzyme
activities
    • 用于测定底物或酶活性的方法和试剂
    • US5196314A
    • 1993-03-23
    • US661271
    • 1991-02-26
    • Michael-Harold TownJoachim SiedelJoachim Ziegenhorn
    • Michael-Harold TownJoachim SiedelJoachim Ziegenhorn
    • C07D257/04C12Q1/26C12Q1/28
    • C07D257/04C12Q1/26C12Q1/28C12Q2326/92Y10S435/805
    • A process for the determination of substrate or enzyme activities by the use of a redox reaction as a measurement reaction is carried out in the presence of one or more additionally added tetrazolium salts to remove disturbing substances. The tetrazolium salts have the formula ##STR1## in which R.sup.1 is a hydrogen atom, a carboxyl group or an alkyl, phenyl, nitrophenyl, dinitrophenyl, carboxyl-substituted phenyl or trialkylammoniumphenyl radical, R.sup.2 is a phenyl, nitrophenyl, biphenylyl or naphthyl radical, R.sup.3 is a phenyl, carboxyl-substituted phenyl, carboxyl-substituted hydroxyphenyl or dimethylthiazolyl radical, and A.sup..crclbar. is a monovalent anion. The formazanes formed by reaction with reducing substances do not absorb light at all, or absorb light only to a negligible extent, at the measurement wavelength of the redox reaction.New compounds included within the structural formula are those in which R.sup.1 is carboxy, phenyl, 2-carboxyphenyl, 4-carboxyphenyl, 2,4-dinitrophenyl or 4-trimethylammoniumphenyl, R.sup.2 is phenyl, and R.sup.3 is phenyl or 2-carboxyphenyl; with the proviso that, when R.sup.3 is unsubstituted phenyl or 2-carboxyphenyl, R.sup.1 may not be unsubstituted phenyl.
    • 通过使用氧化还原反应作为测量反应来测定底物或酶活性的方法在一种或多种另外加入的四唑鎓盐的存在下进行以除去扰乱物质。 所述四唑鎓盐具有其中R 1为氢原子,羧基或烷基,苯基,硝基苯基,二硝基苯基,羧基取代的苯基或三烷基铵苯基的式(I),R 2为苯基,硝基苯基,联苯基或 萘基,R3是苯基,羧基取代的苯基,羧基取代的羟基苯基或二甲基噻唑基,A( - )是一价阴离子。 通过与还原物质反应而形成的甲烷在氧化还原反应的测定波长下根本不吸收光,或仅吸收光可忽略的程度。 包括在结构式中的新化合物是其中R1是羧基,苯基,2-羧基苯基,4-羧基苯基,2,4-二硝基苯基或4-三甲基铵苯基,R2是苯基,R3是苯基或2-羧基苯基的化合物; 条件是当R3是未取代的苯基或2-羧基苯基时,R 1可以不是未被取代的苯基。