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    Novel carbacyclin esters, process for the preparation thereof, and their use as medicinal agents
    1.
    发明授权
    Novel carbacyclin esters, process for the preparation thereof, and their use as medicinal agents 失效
    新型卡巴环素酯，其制备方法及其作为药剂的用途

    公开(公告)号：US4618626A

    公开(公告)日：1986-10-21

    申请号：US777535

    申请日：1985-09-16

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Bob Nieuweboer ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Bob Nieuweboer ,  Michael-Harold Town

    IPC分类号： C07C69/708 ,  A61K31/557 ,  A61P1/04 ,  A61P9/08 ,  A61P9/12 ,  A61P11/08 ,  C07C67/10 ,  C07C69/732 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/0083

    摘要： Carbacyclin esters of Formula I ##STR1## wherein R.sub.1 is an unsubstituted or substituted aromatic residue,R.sub.2 is a free or functionally modified hydroxy group,R.sub.3 is an alkyl or cycloalkyl group, or an optionally substituted aryl group, or a heterocyclic group,X is an oxygen atom or the group --CH.sub.2 --,A is a --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--group,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 is the group ##STR3## a straight-chain saturated alkylene group of 1-5 carbon atoms, a branched, saturated or a straight-chain or branched, unsaturated alkylene group of 2-5 carbon atoms, which groups can optionally be substituted by fluorine atoms,E is a direct bond, a --C.tbd.C--group, or a --CR.sub.4 .dbd.CR.sub.5 -- group wherein R.sub.2 and R.sub.5 mean a hydrogen atom or an alkyl group of 1-5 carbon atoms;are useful as blood-pressure-lowering agents, inter alia.

    摘要翻译： 式I的卡巴环素酯其中R 1是未取代或取代的芳族残基，R 2是游离或官能改性的羟基，R 3是烷基或环烷基，或任选取代的芳基或杂环基 ，X是氧原子或基团-CH 2 - ，A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3 C C基，W是游离或官能改性的羟基亚甲基， 功能修饰的“IMAGE”，其中OH基可以在α或β位D是基团，即1-5个碳原子的直链饱和亚烷基，支链，饱和或直链 或2-5个碳原子的支链不饱和亚烷基，该基团可任选被氟原子取代，E是直接键，-C 3 C C基或-CR 4 = CR 5 - 基，其中R 2和R 5表示 氢原子或1-5个碳原子的烷基; 作为降血压剂特别有用。

    9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents
    2.
    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。

    .DELTA..sup.8,9 -Prostaglandin derivatives, their preparation and use as medicinal agents
    3.
    发明授权
    .DELTA..sup.8,9 -Prostaglandin derivatives, their preparation and use as medicinal agents 失效
    DELTA 8,9-前列腺素衍生物，其制备和用作药物

    公开(公告)号：US4560786A

    公开(公告)日：1985-12-24

    申请号：US391734

    申请日：1982-06-24

    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： A61K31/045 ,  A61K31/557 ,  A61K31/5575 ,  A61P25/04 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00

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

    摘要： .DELTA..sup.8,9 -Prostane 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 ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 ; 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 or free or functionally modified ##STR4## 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, 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 free or functionally modified hydroxy andR.sub.5 is an optionally substituted aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group, and when R.sub.2 is hydrogen, physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g. luteolytic and abortifacient activities.

    摘要翻译： DELTA 8,9-式I的前驱体衍生物其中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; 或R 1为，其中R 3为酸残基或R 2; A是-CH 2 -CH 2 - 或顺式-CH = CH; B是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3BOND 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-基团可以是α或β - 位置 D和E共同是直接键合，或D是可以任选被氟原子取代的1-10个碳原子的直链或支链亚烷基或亚烯基，并且E是氧，硫，直接键，-C 3 D或 -CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自为氢，氯或烷基; R4是游离的或官能改性的羟基，R 5是任选取代的脂族基，环烷基，任选取代的芳基或杂环基，当R 2是氢时，其与碱的生理上相容的盐具有有价值的药理学性质。 luteolytic和流产活动。

    9-Fluoroprostaglandin derivatives, and use as medicinal agents
    4.
    发明授权
    9-Fluoroprostaglandin derivatives, and use as medicinal agents 失效
    9-氟前列腺素衍生物，用作药物

    公开(公告)号：US4454339A

    公开(公告)日：1984-06-12

    申请号：US395448

    申请日：1982-07-06

    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, 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。

    5-fluorocarbacyclins, their preparation and pharmaceutical use
    5.
    发明授权
    5-fluorocarbacyclins, their preparation and pharmaceutical use 失效
    5-氟卡巴环素，其制备和药物用途

    公开(公告)号：US5190964A

    公开(公告)日：1993-03-02

    申请号：US480448

    申请日：1990-02-15

    申请人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Martin Haberey ,  Claus-Steffen Sturzebecher ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbruggen ,  Martin Haberey ,  Claus-Steffen Sturzebecher ,  Michael-Harold Town

    IPC分类号： C07C405/00 ,  C07D263/14

    CPC分类号： C07D263/14 ,  C07C405/0083

    摘要： 5-fluorocarbacyclin derivatives of the Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH orA 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 free or functionally modified ##STR2## in which the OH group can be in the .alpha.-- or .beta.-position, D is ##STR3## a C.sub.1-10 -aliphatic group (e.g., alkyl or alkenyl) which optionally can be substituted by fluorine atoms,n is 1, 2 or 3,E is a direct bond, --C.tbd.C-- or --CR.sub.6 .tbd.CR.sub.7 -- in which R.sub.6 represents a hydrogen atom or an alkyl group with 1-5 atoms and R.sub.7 represents a hydrogen atom, a halogen atom or an alkyl group with 1-5 C atoms,R.sub.4 is alkyl, cycloalkyl or optionally substituted aryl or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy groupand, when R.sub.2 is a hydrogen atom, its salts with physiologically compatible bases,have valuable pharmacological properties.

    摘要翻译： 其中R 1是CH 2 OH或A是-CH 2 -CH 2 - ，反式-CH = CH-或-CB 3 C，其中W是游离的或官能改性的羟基亚甲基，或游离或官能改性的羟基亚甲基， 官能改性的“IMAGE”，其中OH基团可以是α或β-位，D是可任选被氟原子取代的C 1-10脂族基团（例如烷基或烯基），n 是1,2或3，E是直接键，-C 3 D或-CR 6 3BOND CR 7 - ，其中R 6表示氢原子或具有1-5个原子的烷基，R 7表示氢原子，卤素原子 或具有1-5个C原子的烷基，R4是烷基，环烷基或任选取代的芳基或杂环基，R5是游离或官能改性的羟基，当R2是氢原子时，其与生理上相容的碱的盐， 具有宝贵的药理性质。

    Process and reagent for the determination of substrates or enzyme activities
    8.
    发明授权
    Process and reagent for the determination of substrates or enzyme activities 失效
    用于测定底物或酶活性的方法和试剂

    公开(公告)号：US5196314A

    公开(公告)日：1993-03-23

    申请号：US661271

    申请日：1991-02-26

    申请人： Michael-Harold Town ,  Joachim Siedel ,  Joachim Ziegenhorn

    发明人： Michael-Harold Town ,  Joachim Siedel ,  Joachim Ziegenhorn

    IPC分类号： C07D257/04 ,  C12Q1/26 ,  C12Q1/28

    CPC分类号： C07D257/04 ,  C12Q1/26 ,  C12Q1/28 ,  C12Q2326/92 ,  Y10S435/805

    摘要： 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.

    摘要翻译： 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。

    Method for determining iron in a body fluid sample
    9.
    发明授权
    Method for determining iron in a body fluid sample 失效
    用于测定体液样品中铁的方法

    公开(公告)号：US4961970A

    公开(公告)日：1990-10-09

    申请号：US238620

    申请日：1988-08-30

    申请人： Joachim Siedel ,  Lieselotte Schellong ,  Johnny Staepels ,  Uwe Herrmann ,  Michael-Harold Town

    发明人： Joachim Siedel ,  Lieselotte Schellong ,  Johnny Staepels ,  Uwe Herrmann ,  Michael-Harold Town

    IPC分类号： G01N33/84

    CPC分类号： G01N33/84 ,  Y10S436/91

    摘要： The present invention provides a process for the determination of iron in body fluids by liberation of the bound iron, reduction to Fe.sup.2+, addition of a color system appropriate for the detection of iron and photometric measurement in a tenside-containing sample solution, wherein a fatty acid polyethylene glycol ester, an alkanol polyglycol ether and at least 1 mole/liter quanidine hydrochloride are added to the sample solution. The present invention also provides a reagent for the determination of iron in serum, containing a reducing agent, a color material system appropriate for the detection of iron and guanidine hydrochloride and at least one tenside, wherein it contains a fatty acid polyethylene glycol ester and a alkanol polyglycol ether.

    摘要翻译： 本发明提供了一种通过释放结合的铁，还原成Fe2 +，添加适合于检测铁的颜色系统和在含有表面活性剂的样品溶液中进行光度测量来测定体液中铁的方法，其中脂肪 酸性聚乙二醇酯，链烷醇聚乙二醇醚和至少1摩尔/升盐酸氢化物加入到样品溶液中。 本发明还提供了一种用于测定血清中含铁的试剂，其含有还原剂，适用于检测铁和胍盐酸盐和至少一种表面活性剂的着色材料体系，其中它含有脂肪酸聚乙二醇酯和 链烷醇聚乙二醇醚。