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1. 发明授权

US4987133A Salicylic acid derivatives 失效
标题翻译：水杨酸衍生物
公开(公告)号：US4987133A
公开(公告)日：1991-01-22
申请号：US338822
申请日：1989-04-17
申请人： Hans-Adolf Kurmeier , Wolf-Dietrich Weber , Hans-Eckart Radunz , Hans-Jochen Schliep
发明人： Hans-Adolf Kurmeier , Wolf-Dietrich Weber , Hans-Eckart Radunz , Hans-Jochen Schliep
IPC分类号： A61K31/625 , A61P9/12 , C07D209/14 , C07D211/58 , C07D217/04 , C07D217/20 , C07D233/60 , C07D233/61 , C07D233/68 , C07D277/20 , C07D277/28 , C07D277/42 , C07D307/16 , C07D307/24 , C07D417/04 , C07D521/00
CPC分类号： C07D249/08 , C07D209/14 , C07D211/58 , C07D217/04 , C07D231/12 , C07D233/56 , C07D233/68 , C07D277/42 , C07D307/24
摘要： New salicylic acid derivatives of the general formula I ##STR1## in which R.sup.1 is H or CH.sub.3,R.sup.2 is 4-(4-methyl-2-thiazolyl)-piperazino, 4-(tetrahydro-2-furoyl)-piperazino, 4-(4-methyl-2-thiazolyl)-homopiperazino, 4-benzamidopiperidino, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolino, 1-imidazolyl, tribromo-1-imidazolyl or 2-(3-indolyl-1,1-dimethyl-ethylamino andR.sup.3 is alkoxy having 1-C atoms, NH.sub.2 or alkylamino having 1-4 C atoms,as well as the physiologically acceptable acid addition salts thereof, exhibit effects on the circulation, especially effects lowering the blood pressure and relieving the heart, and diuretic effects.
摘要翻译： R1为H或CH3，R2为4-（4-甲基-2-噻唑基） - 哌嗪基，4-（四氢-2-呋喃甲酰基） - 哌嗪子基，4-（四氢-2-呋喃甲酰基） - 哌嗪子基的通式I的新水杨酸衍生物 4-（4-甲基-2-噻唑基） - 高哌啶子基，4-苯甲酰基哌啶子基，6,7-二甲氧基-1,2,3,4-四氢异喹啉，1-咪唑基，三溴-1-咪唑基或2-（3-吲哚基 - 1,1-二甲基 - 乙基氨基和R3是具有1-C原子的烷氧基，具有1-4个C原子的NH 2或烷基氨基，以及其生理上可接受的酸加成盐，对循环具有影响，特别是降低血压的作用缓解心脏和利尿作用。

2. 发明授权

US4289768A Phenothiazine derivatives and a process for their preparation 失效
标题翻译：吩噻嗪衍生物及其制备方法
公开(公告)号：US4289768A
公开(公告)日：1981-09-15
申请号：US145652
申请日：1980-05-02
申请人： Joachim Gante , Hans-Eckart Radunz , Dieter Orth , Hans-Jochen Schliep , Ernst Schorscher
发明人： Joachim Gante , Hans-Eckart Radunz , Dieter Orth , Hans-Jochen Schliep , Ernst Schorscher
IPC分类号： C07D417/06 , A61K31/54 , A61K31/5415 , A61P7/10 , A61P9/12 , C07D417/12 , C07D521/00 , A61K31/415 , C07D279/30
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Phenothiazine derivatives of the formula ##STR1## wherein R is H, F, Cl, Br, I, CH.sub.3, CF.sub.3, CN, CH.sub.3 O or CH.sub.3 CO; Y is S, SO, or SO.sub.2 ; Z is imidazol-1-yl, 2-methyl-imidazol-1-yl, pyrazol-1-yl or benzimidazol-1-yl; and n is 1, 2 or 3; or the physiologically acceptable acid addition salts thereof; are useful as antihypertensive agents, for example.
摘要翻译：其中R是H，F，Cl，Br，I，CH 3，CF 3，CN，CH 3 O或CH 3 CO的式IV的吩噻嗪衍生物; Y是S，SO或SO2; Z是咪唑-1-基，2-甲基 - 咪唑-1-基，吡唑-1-基或苯并咪唑-1-基; n为1,2或3; 或其生理上可接受的酸加成盐; 例如可用作抗高血压药。

3. 发明授权

US4309441A 13-Thiaprostaglandin derivatives 失效
标题翻译： 13-Thiaprostaglandin衍生物
公开(公告)号：US4309441A
公开(公告)日：1982-01-05
申请号：US96348
申请日：1979-11-21
申请人： Hans-Eckart Radunz , Dieter Orth , Manfred Baumgarth , Hans-Jochen Schliep , Hans-Joachim Enenkel
发明人： Hans-Eckart Radunz , Dieter Orth , Manfred Baumgarth , Hans-Jochen Schliep , Hans-Joachim Enenkel
IPC分类号： A61K31/557 , A61K31/215 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D303/04 , C07D303/40 , C07F9/54 , C07C177/00
CPC分类号： C07D303/04 , C07C323/00 , C07C405/00 , C07C405/0033 , C07D303/40 , C07F9/5407
摘要： 13-Thiaprostanoic acid derivatives of the general formula I ##STR1## wherein A is --CO-- or --CHOH--; B is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--; Q is 1,4-phenylene or 1,4-naphthylene; R.sup.1 is H or OH; R.sup.2 is H or CH.sub.3 ; R.sup.3 is alkyl with 1-8 carbon atoms or alkyl with 1-8 carbon atoms substituted by (a) phenyl, (b) phenyl substituted by at least one of CH.sub.3, F, Cl, Br, OH, OCH.sub.3 or CF.sub.3 ; (c) phenoxy or (d) phenoxy substituted by at least one of CH.sub.3, F, Cl, Br, OH, OCH.sub.3 or CF.sub.3 ; and R.sup.4 is NH.sub.2, CH.sub.3, phenyl, p-acetylaminophenyl, p-benzoylaminophenyl or phenylamino. These compounds are useful for lowering blood pressure as well as for other pharmaceutical purposes. They also are useful intermediates for the preparation of other known pharmaceuticals such s the 13-thiaprostaglandins.
摘要翻译：其中A是-CO-或-CHOH-的通式I（I）的13-十三十二烷酸衍生物; B是-CH 2 CH 2 - 或-CH = CH-; Q是1,4-亚苯基或1,4-亚萘基; R1是H或OH; R2是H或CH3; R3是具有1-8个碳原子的烷基或具有1-8个碳原子的烷基，被（a）苯基取代，（b）被至少一个CH 3，F，Cl，Br，OH，OCH 3或CF 3取代的苯基; （c）苯氧基或（d）被至少一个CH 3，F，Cl，Br，OH，OCH 3或CF 3取代的苯氧基; 并且R 4是NH 2，CH 3，苯基，对乙酰氨基苯基，对苯甲酰基氨基苯基或苯基氨基。这些化合物可用于降低血压以及其它药物目的。它们也是制备其它已知药物如十三硫代前列腺素的有用的中间体。

4. 发明申请

US20090297613A1 Nanoparticles Designed for Drug Delivery 审中-公开
标题翻译：设计用于药物输送的纳米颗粒
公开(公告)号：US20090297613A1
公开(公告)日：2009-12-03
申请号：US12223420
申请日：2007-02-02
申请人： Kerstin Ringe , Hans-Eckart Radunz , Julia Kubasch
发明人： Kerstin Ringe , Hans-Eckart Radunz , Julia Kubasch
IPC分类号： A61K9/14
CPC分类号： A61K9/5138 , A61K9/5192 , A61K49/0043 , A61K49/0054 , A61K49/0093
摘要： The present invention is directed to a method of producing nanoparticles by the miniemulsion method, said nanoparticles being made by adding a defined amount of stabilizer to the reaction system. The present invention is further directed to nanoparticles made by this method and their use for the treatment of diseases and conditions, requiring a pharmaceutical agent to cross one or more physiological barriers, in particular the blood-brain barrier.
摘要翻译：本发明涉及通过细乳液法制备纳米颗粒的方法，所述纳米颗粒通过向反应体系中加入限定量的稳定剂而制备。本发明还涉及通过该方法制备的纳米颗粒及其用于治疗疾病和病症的用途，需要药剂穿过一个或多个生理屏障，特别是血脑屏障。

5. 发明授权

US5026642A Process for the enzymatic production of ketones 失效
标题翻译：用于酶生产酮的方法
公开(公告)号：US5026642A
公开(公告)日：1991-06-25
申请号：US223051
申请日：1988-07-22
申请人： Hans-Eckart Radunz , Harry Schwartz , Martin Heinrich
发明人： Hans-Eckart Radunz , Harry Schwartz , Martin Heinrich
IPC分类号： C07C67/00 , C07C227/16 , C07C229/22 , C07C229/28 , C07C229/34 , C07C239/00 , C07C271/22 , C07D521/00 , C07K5/06 , C07K14/195 , C07K14/41 , C07K14/81 , C12P7/42 , C12P7/62 , C12P13/00 , C12P17/00 , C12P41/00
CPC分类号： C12P13/001 , C07C227/16 , C12P13/002 , C12P13/005 , C12P13/008 , C12P13/02 , C12P13/04 , C12P17/00 , C12P41/002 , C12P7/42 , C12P7/62 , Y10S435/93 , Y10S435/942
摘要： In a process for the reduction of ketones, the keto compounds are enantioselectively reduced to give secondary alcohols by means of microorganisms. Keto compounds of the formulaR.sup.3 NH--CHR.sup.1 --CO--CH.sub.2 --COOR.sup.2in which R.sup.1, R.sup.2 and R.sup.3 have the meanings defined herein are used as starting compounds.
摘要翻译：在还原酮的方法中，酮化合物被对映选择性地还原以通过微生物产生仲醇。其中R1，R2和R3具有本文定义的含义的式R3NH-CHR1-CO-CH2-COOR2的酮基化合物用作起始化合物。

6. 发明授权

US4125622A 1,4-Oxathianes 失效
公开(公告)号：US4125622A
公开(公告)日：1978-11-14
申请号：US860355
申请日：1977-12-14
申请人： Hans-Eckart Radunz , Dieter Orth , Manfred Baumgarth , Reinhard Lissner , Jurgen Maisenbacher
发明人： Hans-Eckart Radunz , Dieter Orth , Manfred Baumgarth , Reinhard Lissner , Jurgen Maisenbacher
IPC分类号： A61K31/39 , A61P7/02 , C07D327/06
CPC分类号： C07D327/06 , Y10S514/822
摘要： 1,4-Oxathianes of the formula ##STR1## and the physiologically-acceptable salts thereof wherein R.sup.1 is H or alkyl with 1-4 C-atoms; R.sup.2 is H or alkyl with 1-4 C-atoms; R.sup.3 is H, alkyl with 1-8 C-atoms, phenyl or phenyl substituted by F, Cl, Br, OH, OCH.sub.3, CF.sub.3 or NO.sub.2 ; R.sup.4 is H or CH.sub.3 ; B is a single bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --CH.sub.2 O--; and a wavy line ( ) indicates that these bonds can be in the .alpha.- or .beta.- positions possess thrombocyte inhibition properties.
摘要翻译：具有式“IMAGE”的1,4-氧硫辛酸和其生理学上可接受的盐，其中R 1是H或具有1-4个C原子的烷基; R2是H或具有1-4个C原子的烷基; R3是H，具有1-8个C原子的烷基，被F，Cl，Br，OH，OCH3，CF3或NO2取代的苯基或苯基; R4是H或CH3; B是单键，-CH 2 - ， - CH 2 CH 2 - 或-CH 2 O- 和波浪线（）表示这些键可以在α或β位具有血细胞抑制性质。

7. 发明授权

US4680288A Sulfur-containing 6-ketoprostaglandins 失效
标题翻译：含硫6孔松脂腺苷
公开(公告)号：US4680288A
公开(公告)日：1987-07-14
申请号：US692490
申请日：1985-01-18
申请人： Klaus Irmscher , Hans-Eckart Radunz , Ernst Schulze , Bernhard Riefling
发明人： Klaus Irmscher , Hans-Eckart Radunz , Ernst Schulze , Bernhard Riefling
IPC分类号： C07D333/18 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D213/70 , C07D309/12 , C07F7/18 , C07C177/00
CPC分类号： C07C405/0033
摘要： Sulfur-containing 6-ketoprostaglandins of the formula I ##STR1## in which D is a bond, alkylene having 1-3 C atoms, cis-alkenylene having 2-5 C atoms or alkinylene having 2-5 C atoms,R.sup.1 is H, alkyl having 1-4 C atoms, aryl having 6-12 C atoms or --C.sub.6 H.sub.4 NHCOC.sub.6 H.sub.5,R.sup.2 is alkyl having 1-7 C atoms, alkyl having 1-7 C atoms which is substituted by halogen, cycloalkyl having 5-6 C atoms, cycloalkyl having 5-6 C atoms which is substituted by alkyl having 1-4 C atoms, phenyl, phenyl which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3, pyridyl, naphthyl, thienyl or, if D is alkylene having 1-3 C atoms, also is alkoxy having 1-4 C atoms, alkylthio having 1-4 C atoms, phenoxy or phenoxy which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3,R.sup.3 and R.sup.4 each are H, alkyl having 1-7 C atoms, tetrahydro-2-pyranyl, trialkylsilyl having a total of 3-12 C atoms, aryldialkylsilyl having a total of 8-18 C atoms, alkoxymethyl having 2-5 C atoms, aryloxymethyl having 7-11 C atoms or acyl having 1-10 C atoms, andR.sup.5 is H or alkyl having 1-3 C atoms, and.... indicates that this bond is .alpha., indicates that this bond is .beta.,and, where R.sub.1 is H, their salts, show effects on the circulation, in particular hypotensive effects, as well as effects on the force of myocardial contraction.
摘要翻译：其中D为键的式I化合物I-I，含有1-3个C原子的亚烷基，具有2-5个C原子的顺式亚烯基或具有2-5个C原子的亚炔基的含硫的6-酮基前列腺素，R1为H 具有1-4个C原子的烷基，具有6-12个碳原子的芳基或-C6H4NHCOC6H5的芳基，R2是具有1-7个C原子的烷基，具有1-7个C原子的被卤素取代的烷基，具有5-6个C原子的环烷基由具有1-4个C原子的烷基取代的具有5-6个碳原子的环烷基，苯基，被F，Cl，Br，具有1-4个C原子的烷基取代的苯基，OH，OCH3或CF3，吡啶基，萘基，噻吩基或如果D是具有1-3个C原子的亚烷基，也是具有1-4个C原子的烷氧基，具有1-4个C原子的烷硫基，被F，Cl，Br取代的苯氧基或苯氧基， 4个C原子，OH，OCH 3或CF 3，R 3和R 4各自为H，具有1-7个C原子的烷基，四氢-2-吡喃基，总共3-12个C原子的三烷基甲硅烷基，共有8-18个芳基二烷基甲硅烷基 C原子，具有2-5个C原子的烷氧基甲基，芳氧基甲基具有1-10个碳原子的7-11个C原子或酰基，R5是H或具有1-3个C原子的烷基，...表示该键为α，表示该键为β，并且其中 R1是H，它们的盐，对循环有显着影响，特别是降压作用，以及对心肌收缩力的影响。

8. 发明授权

US4622316A 13-thiaprostaglandins having cytoprotective activity 失效
标题翻译：具有细胞保护活性的13-thiaprostaglandins
公开(公告)号：US4622316A
公开(公告)日：1986-11-11
申请号：US669407
申请日：1984-11-08
申请人： Bernd Simon , Hanns-Gerd Dammann , Peter Muller , Hans-Jurgen Legeler , Dieter Orth , Hans-Eckart Radunz
发明人： Bernd Simon , Hanns-Gerd Dammann , Peter Muller , Hans-Jurgen Legeler , Dieter Orth , Hans-Eckart Radunz
IPC分类号： A61K31/557 , A61P1/00 , A61K31/615 , A61K31/215
CPC分类号： A61K31/557
摘要： 13-thiaprostaglandins of Formula I ##STR1## wherein B is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,R.sup.1 is phenyl, CH.sub.3, or NH.sub.2,R.sup.2 is H or CH.sub.3, andR.sup.3 is pentyl, hexyl, 1-methylpentyl, or 1,1-dimethylpentylhave valuable pharmacological properties, e.g., as cytoprotective agents.
摘要翻译：其中B是-CH 2 -CH 2 - 或-CH = CH-，R 1是苯基，CH 3或NH 2，R 2是H或CH 3，并且R 3是戊基，己基，1-甲基戊基或1,1-二甲基戊基具有有价值的药理学性质，例如作为细胞保护剂。

9. 发明授权

US4113863A Prostenoic acid derivatives 失效
标题翻译：前列腺酸衍生物
公开(公告)号：US4113863A
公开(公告)日：1978-09-12
申请号：US739142
申请日：1976-11-05
申请人： Manfred Baumgarth , Hans-Eckart Radunz , Dieter Orth , Reinhard Lissner , Hans-Joachim Enenkel , Filippus Johannes Zeelen
发明人： Manfred Baumgarth , Hans-Eckart Radunz , Dieter Orth , Reinhard Lissner , Hans-Joachim Enenkel , Filippus Johannes Zeelen
IPC分类号： C07C405/00 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07C405/00 , Y10S514/926 , Y10S514/927
摘要： Prostenoic acid derivatives of the general formula ##STR1## wherein R.sup.1 is H or alkyl of 1-4 carbon atoms;R.sup.2 is alkyl of 5 - 9 carbon atoms, phenoxymethyl or phenoxymethyl substituted by up to 3 of F, Cl, Br, CH.sub.3, CF.sub.3, or OCH.sub.3 ;R.sup.3 is H or alkyl of 1 - 5 carbon atoms, and physiologically acceptable salts thereof, as well as intermediates therefore are blood-pressure lowering, vasodilatory, diuretic, and nasal mucosa decongesting agents and are produced from intermediates of the formula ##STR2## wherein R.sup.4 is H or acyl of up to 5 carbon atoms and A is CH.sub.2 D or CH.dbd.C(OR.sup.5); D is carbonyl or dialkoxypolymethylene of up to 7 carbon atoms.

10. 发明授权

US4080458A Thiaprostaglandins 失效
公开(公告)号：US4080458A
公开(公告)日：1978-03-21
申请号：US576140
申请日：1975-05-09
申请人： Hans-Eckart Radunz , Josef Kramer , Manfred Baumgarth , Dieter Orth
发明人： Hans-Eckart Radunz , Josef Kramer , Manfred Baumgarth , Dieter Orth
IPC分类号： C07D333/34 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C20060101 , C07C67/00 , C07C401/00 , C07C405/00 , C07D213/32 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07C405/0033 , Y02P20/55
摘要： 13-Thiaprostanoic acid derivatives of the formula ##STR1## wherein A is --CO-- or --CHOH--, B is --CH.sub.2 --CH.sub.2 -- or --CH=CH--, R.sup.1 is H or alkyl of 1 to 4 carbon atoms, m is a whole number from 0 to 5, n is a whole number from 0 to 3 or, when B is --CH=CH--, additionally 4, 5, 6, 7, 8 or 9, R.sup.2 is alkoxy of 1 to 4 carbon atoms, phenoxy, pyridyl, thienyl, naphthyl, phenyl substituted by F, Cl, Br, OH, OCH.sub.3 or OF.sub.3 or phenoxy substituted by F, Cl, Br, OH, OCH.sub.3, CH.sub.3 or CF.sub.3 or, when B is --CH=CH--, additionally hydrogen, phenyl or tolyl, R.sup.3 is H, methyl or ethyl, possess pharmacological activity, including blood pressure lowering activity.
摘要翻译：其中A是-CO-或-CHOH-，B是-CH 2 -CH 2 - 或-CH = CH-，R 1是H或1-4个碳原子的烷基，m是 0至5的整数，n为0至3的整数，或当B为-CH = CH-时，另外为4，5，6，7，8或9，R 2为1至4个碳原子的烷氧基苯氧基，吡啶基，噻吩基，萘基，被F，Cl，Br，OH，OCH3或OF3取代的苯基或被F，Cl，Br，OH，OCH3，CH3或CF3取代的苯氧基，或当B为-CH = CH- ，另外是氢，苯基或甲苯基，R3是H，甲基或乙基，具有药理活性，包括降血压活性。

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