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21. 发明授权

US5891910A 9-halogen-(Z) prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
标题翻译： 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。

22. 发明授权

US4721729A Novel carbacyclins, process for the preparation thereof, and their use as medicinal agents 失效
标题翻译：新型碳环霉素，其制备方法及其作为药剂的用途
公开(公告)号：US4721729A
公开(公告)日：1988-01-26
申请号：US702092
申请日：1985-02-08
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Robert Nickolson , Martin Haberey , Olaf Loge , Claus-Steffen Stuerzebecher
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Robert Nickolson , Martin Haberey , Olaf Loge , Claus-Steffen Stuerzebecher
IPC分类号： C07C43/14 , A61K31/557 , A61P43/00 , C07C27/00 , C07C35/31 , C07C35/52 , C07C41/00 , C07C45/00 , C07C49/24 , C07C49/255 , C07C49/76 , C07C67/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0083 , Y10S514/829
摘要： Carbacyclins of Formula I ##STR1## wherein R.sub.1 is an alkyl, cycloalkyl, aryl, aralkyl, or heterocyclic group,Y is a keto group or a hydroxymethylene group,X is a --CH.sub.2 -- group or an oxygen atom,A is a --CH.sub.2 --CH.sub.2 --, a trans--CH.dbd.CH-- or a --C.tbd.C-- group,W is a hydroxymethylene group or a ##STR2## D is the group ##STR3## a straight-chain or branched, saturated alkylene group or unsaturated alkylene group of up to 5 carbon atoms which can optionally be substituted by 1-2 fluorine atoms,n is 1, 2 or 3,E is a direct bond, a --C.tbd.C-- group or a --CR.sub.4 .dbd.CR.sub.5 -- group wherein R.sub.4 is hydrogen or an alkyl group and R.sub.5 is hydrogen, halogen or an alkyl group,R.sub.2 is an alkyl, cycloalkyl, aryl, or heterocyclic group, andR.sub.3 is a hydroxy group,are valuable, e.g., as cytoprotective agents.
摘要翻译：式I的卡巴菌素其中R 1是烷基，环烷基，芳基，芳烷基或杂环基，Y是酮基或羟亚甲基，X是-CH 2 - 基或氧原子，A是 -CH 2 -CH 2 - ，反式-CH = CH-或-C 3 C C基团，W是羟基亚甲基基团，或者D是基团，即直链或支链饱和亚烷基或至多5个碳原子的不饱和亚烷基，其可任选被1-2个氟原子取代，n为1,2或3，E为直接键，-C 3位C基团或-CR 4 = CR 5 - 基团，其中R 4是氢或烷基，R 5是氢，卤素或烷基，R 2是烷基，环烷基，芳基或杂环基，并且R 3是羟基，是有价值的，例如作为细胞保护剂。

23. 发明授权

US4560786A .DELTA..sup.8,9 -Prostaglandin derivatives, their preparation and use as medicinal agents 失效
标题翻译： 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。

24. 发明授权

US4454339A 9-Fluoroprostaglandin derivatives, and use as medicinal agents 失效
标题翻译： 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。

25. 发明授权

US4073934A Novel acetylenic prostaglandin analogs 失效
标题翻译：新型炔类前列腺素类似物
公开(公告)号：US4073934A
公开(公告)日：1978-02-14
申请号：US677861
申请日：1976-04-16
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Eckehard Schillinger
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Eckehard Schillinger
IPC分类号： A61K31/23 , C07C67/00 , C07C401/00 , C07C405/00 , C07D213/30 , C07D213/55 , C07D307/38 , C07D307/54 , C07D307/935 , C07D333/06 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07D307/935 , C07C405/00
摘要： Optically active and racemic prostaglandin derivatives of the formula ##STR1## wherein R.sub.1 is --OR.sub.5 ; --NHSO.sub.2 CH.sub.3 ; or --O--CH.sub.2 --U--V; R.sub.5 is hydrogen, alkyl, aryl, or a heterocyclic group; U is a direct bond, carbonyl or carbonyloxy; and V is phenyl substituted by 1-3 phenyl, alkoxy of 1-2 carbon atoms, or halogen, preferably bromine;R.sub.2 is hydrogen or alkyl of 1-5 carbon atoms;R.sub.3 is alkyl, substituted or unsubstituted cycloalkyl, straight-chain or branched alkyl of 1-5 carbon atoms substituted by aryl or substituted aryl, when R.sub.1 is as above; or R.sub.3 is aryl or substituted aryl group when R.sub.1 is --OR.sub.5 ', --NHSO.sub.2 CH.sub.3, or --O--CH.sub.2 --U--V and R.sub.5 ' is aryl or a heterocyclic group and U and V are as above;R.sub.4 is hydrogen or an ether or acyl residue;A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--;B is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--;D is a direct bond, oxygen, or sulfur;Z is carbonyl or >CH OR.sub.4 wherein OR.sub.4 is in the .alpha.- or .beta.-position; andX y is ##STR2## when Z is >CH OR.sub.4 --, or ##STR3## or --CH.dbd.CH-- when Z is carbonyl; AND, WHEN R.sub.1 is hydroxy, the physiologically compatible salts thereof with bases, have more prolonged activity than naturally-occurring prostaglandins.
摘要翻译：式（Ⅰ）的光学活性和外消旋前列腺素衍生物，其中R1为-OR5; -NHSO 2 CH 3; 或-O-CH 2 -U-V; R5是氢，烷基，芳基或杂环基; U是直接键，羰基或羰氧基; 并且V是被1-3个苯基，1-2个碳原子的烷氧基或卤素，优选溴取代的苯基; R2是氢或1-5个碳原子的烷基; R 3为烷基，取代或未取代的环烷基，被芳基或取代芳基取代的1-5个碳原子的直链或支链烷基，当R 1如上所述时; 或当R 1为-OR 5'，-NHSO 2 CH 3或-O-CH 2 -U-V且R 5'为芳基或杂环基时，R 3为芳基或取代的芳基，U和V如上所述; R4是氢或醚或酰基残基; A是-CH 2 -CH 2 - 或顺式-CH = CH-; B是-CH 2 -CH 2 - 或反式-CH = CH-; D是直接键合，氧或硫; Z是羰基或> CH OR 4，其中OR 4在α或β-位; 当Z为羰基时Z为> CH OR4-或或-CH = CH-时，X Y为当R1是羟基时，其与碱的生理上相容的盐比天然存在的前列腺素具有更长的活性。

26. 发明授权

US5047525A 9-haloprostaglandin clathrates and their use as medicines 失效
标题翻译： 9-卤代前列腺素包合物及其作为药物的用途
公开(公告)号：US5047525A
公开(公告)日：1991-09-10
申请号：US549045
申请日：1990-07-06
申请人： Bernd Raduechel , Werner Skuballa , Olaf Loge , Johann-Wilhelm Tack
发明人： Bernd Raduechel , Werner Skuballa , Olaf Loge , Johann-Wilhelm Tack
IPC分类号： A61K31/557 , A61K47/48 , C08B37/00 , C08B37/16
CPC分类号： B82Y5/00 , A61K31/557 , A61K47/48969 , C08B37/0015
摘要： The present application encompasses pharmaceutical preparations, characterized in that they contain as the active component a cyclodextrin clathrate of a prostaglandin of general Formula I ##STR1## wherein R.sub.1 is a hydrogen atom or a straight-chain or branched alkyl residue of up to 10 carbon atoms,R.sub.2 is an alkyl, cycloalkyl, or optionally substituted phenyl group,A and B jointly mean a direct bond orA means a straight- or branched-chain alkylene group of up to 10 carbon atoms andB means an oxygen atom, a direct bond, or a --C.tbd.C--bond, andX means a chlorine or fluorine atom.
摘要翻译：本申请包括药物制剂，其特征在于它们作为活性组分含有通式I的前列腺素的环糊精包合物，其中R 1是氢原子或至多10个碳原子的直链或支链烷基残基，R2是烷基，环烷基或任选取代的苯基，A和B联合表示直接键，或A表示至多10个碳原子的直链或支链亚烷基，B表示氧原子，直接键或-C 3 C C键，X表示氯或氟原子。

27. 发明授权

US07074387B2 DTPA monoamides, pharmaceutical agents containing these compounds, their use and process for their production 失效
标题翻译： DTPA单酰胺，含这些化合物的药剂，它们的用途和制备方法
公开(公告)号：US07074387B2
公开(公告)日：2006-07-11
申请号：US10395080
申请日：2003-03-25
申请人： Heinz Gries , Erich Klieger , Bernd Raduechel , Heribert Schmitt-Willich , Hanns-Joachim Weinmann , Hubert Vogler , Gabriele Schuhmann-Giampieri , Juergen Conrad
发明人： Heinz Gries , Erich Klieger , Bernd Raduechel , Heribert Schmitt-Willich , Hanns-Joachim Weinmann , Hubert Vogler , Gabriele Schuhmann-Giampieri , Juergen Conrad
IPC分类号： A61B5/055
CPC分类号： C07F5/003 , A61K49/06 , C07C237/04 , C07C237/12 , C07F15/025 , Y10S514/836
摘要： Compounds of formula I wherein Z1, Z2, X, R2 and R3 are as defined herein, are suitable as NMR shift reagents.
摘要翻译：其中Z 1，Z 2，X，R 2和R 3的式I化合物如本文所定义，适用于NMR转移试剂。

28. 发明申请

US20060093554A1 Galenical formulations 审中-公开
标题翻译：盖仑制剂
公开(公告)号：US20060093554A1
公开(公告)日：2006-05-04
申请号：US11223203
申请日：2005-09-12
申请人： Johannes Platzek , Ulrich Niedballa , Bernd Raduechel , Peter Mareski , Bernd Misselwitz , Thomas Frenzel , Hanns-Joachim Weinmann
发明人： Johannes Platzek , Ulrich Niedballa , Bernd Raduechel , Peter Mareski , Bernd Misselwitz , Thomas Frenzel , Hanns-Joachim Weinmann
IPC分类号： A61K51/00
CPC分类号： A61K49/10 , A61K49/06 , A61K49/085
摘要： This invention describes new galenical formulations that contain paramagnetic and diamagnetic perfluoroalkyl-containing compounds. The new formulations are suitable as contrast media for nuclear spin tomography.
摘要翻译：本发明描述了含有顺磁性和反抗磁性全氟烷基的化合物的新的盖仑制剂。新制剂适用于核自旋层析成像的造影剂。

29. 发明授权

US06676928B2 Perfluoroalkyl-containing complexes with polar radicals, process for their production and their use 失效
标题翻译：具有极性基团的含全氟烷基的络合物，其制备及其用途
公开(公告)号：US06676928B2
公开(公告)日：2004-01-13
申请号：US09925420
申请日：2001-08-10
申请人： Johannes Platzek , Peter Mareski , Ulrich Niedballa , Bernd Raduechel , Hanns-Joachim Weinmann , Bernd Misselwitz
发明人： Johannes Platzek , Peter Mareski , Ulrich Niedballa , Bernd Raduechel , Hanns-Joachim Weinmann , Bernd Misselwitz
IPC分类号： A61B5055
CPC分类号： C07D295/26 , A61K49/0438 , A61K49/085 , A61K49/10 , C07D257/02
摘要： Perfluoroalkyl-containing complexes with polar radicals of general formula I (K)1-G-(Z-Rf)m(R)p (I) in which R means the polar radical, Rf means a perfluorinated carbon chain, K is a metal complex, and Z represents a linker group, are suitable for intravenous lymphography, for tumor diagnosis and for infarction and necrosis imaging.
摘要翻译：含有通式Iin的极性基团的全氟烷基配合物，其中R表示极性基团，Rf表示全氟化碳链，K为金属络合物，Z为连接基团，适用于静脉内淋巴造影，肿瘤诊断和梗死和坏死成像。

30. 发明授权

US6146615A Contrast agents for image enhancement in magnetic resonance imaging 失效
标题翻译：磁共振成像中图像增强的对比剂
公开(公告)号：US6146615A
公开(公告)日：2000-11-14
申请号：US227962
申请日：1999-01-11
申请人： Julian A. Davies , Wolfgang Ebert , Bernd Raduechel
发明人： Julian A. Davies , Wolfgang Ebert , Bernd Raduechel
IPC分类号： A61K49/10 , A61B5/055
CPC分类号： A61K49/101 , Y10S514/836
摘要： A compound of formula (I): ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected independently from hydrogen, alkyl, and alkyl substituted with one or more --O-- atoms, or where R.sup.1, R.sup.2 and R.sup.3, R.sup.4 are ring residues. The compound is capable of functioning as a ligand and complexing with paramagnetic Fe(III) ion for use as a second-sphere contrast enhancing agent for magnetic resonance imaging of tissue, and a method of administering the second sphere contrast agent.
摘要翻译：式（I）化合物：其中，R 1，R 2，R 3和R 4独立地选自氢，烷基和被一个或多个-O-原子取代的烷基，或其中R 1，R 2和R 3，R 4为环残基。该化合物能够用作配体并与顺磁性Fe（III）离子络合，用作组织磁共振成像的第二球对比增强剂，以及施用第二球形造影剂的方法。

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