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1. 发明授权

US6156890A Process for the production of cyclene 有权
标题翻译：生产环烯烃的工艺
公开(公告)号：US6156890A
公开(公告)日：2000-12-05
申请号：US451702
申请日：1999-12-01
申请人： Johannes Platzek , Karsten Hoyer , Klaus-Dieter Graske , Bernd Raduechel
发明人： Johannes Platzek , Karsten Hoyer , Klaus-Dieter Graske , Bernd Raduechel
IPC分类号： C07D257/02 , C07D255/02
CPC分类号： C07D257/02
摘要： A new single-pot process for the production of cyclene is described.
摘要翻译：描述了用于生产环烯烃的新的单锅法。

2. 发明授权

US5693310A Amide complexes 失效
标题翻译：酰胺配合物
公开(公告)号：US5693310A
公开(公告)日：1997-12-02
申请号：US614947
申请日：1990-11-19
申请人： Heinz Gries , Bernd Raduechel , Hans-Joachim Weinmann , Wolfgang Muetzel , Ulrich Speck
发明人： Heinz Gries , Bernd Raduechel , Hans-Joachim Weinmann , Wolfgang Muetzel , Ulrich Speck
IPC分类号： C07F5/00 , A61K49/00 , A61K49/04 , A61K49/06 , A61K51/00 , A61K51/04 , C07B59/00 , C07C231/00 , C07C231/02 , C07C237/04 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/22 , C07C273/10 , C07D211/22 , C07D265/32 , C07D265/33 , C07D295/18 , C07D295/185 , C07D521/00 , C07F13/00 , C07C229/00
CPC分类号： C07D295/185 , A61K49/06 , A61K51/048 , C07C237/08 , C07C237/22 , C07D211/22 , C07D265/33 , A61K2123/00
摘要： Compounds of general Formula I ##STR1## wherein R.sup.3 is a saturated, unsaturated, straight- or branched-chain or cyclic aliphatic hydrocarbon residue of up to 16 carbon atoms or, if R.sup.4 is a hydrogen atom, a cycloalkyl group or an aryl or aralkyl group optionally substituted by one or several C.sub.1 -C.sub.6 -dialkylamino groups or by one or several C.sub.1 -C.sub.6 -alkoxy groups, R.sup.4 is a hydrogen atom, a saturated, unsaturated, straight- or branched-chain or cyclic hydrocarbon residue of up to 16 carbon atoms, or R.sup.3 and R.sup.4 jointly mean a saturated or unsaturated 5- or 6-membered ring optionally substituted or containing an O, S, N atom or oxo substituent, and Y is COOX or CONR.sub.3 R.sub.4, are valuable complexing agents, complexes or complex salts, e.g., for use as NMR or X-ray diagnostic image-enhancement agents or radioactive diagnostic agents.
摘要翻译：通式Ⅰ的化合物其中R 3是至多16个碳原子的饱和的，不饱和的，直链或支链或环状脂族烃残基，或者如果R 4是氢原子，则环烷基或任选被一个或多个C 1 -C 6 - 二烷基氨基或一个或多个C 1 -C 6 - 烷氧基取代的芳基或芳烷基，R 4是氢原子，饱和的，不饱和的，直链的或支链的或环状的烃基至16个碳原子，或者R 3和R 4共同表示饱和或不饱和的5或6元环，其任选地被取代或含有O，S，N原子或氧取代基，Y是COOX或CONR3R4，是有价值的络合剂，络合物或复盐，例如用作NMR或X射线诊断图像增强剂或放射性诊断剂。

3. 发明授权

US5523321A Prostacyclins, their analogs or prostaglandins and thromboxane antagonists for treatment of thrombotic and thromboembolic syndromes 失效
标题翻译：前列环素，其类似物或前列腺素和血栓素拮抗剂用于治疗血栓形成和血栓栓塞综合征
公开(公告)号：US5523321A
公开(公告)日：1996-06-04
申请号：US504071
申请日：1990-04-02
申请人： Claus-Steffen Stuerzebecher , Werner Witt , Bernd Raduechel , Werner Skuballa , Helmut Vorbrueggen
发明人： Claus-Steffen Stuerzebecher , Werner Witt , Bernd Raduechel , Werner Skuballa , Helmut Vorbrueggen
IPC分类号： A61K31/557 , A61K31/355 , A61K31/19 , A61K31/34
CPC分类号： A61K31/557
摘要： Combination products containing a prostaglandin (PG), prostacyclin (PC) or a prostacyclin analog (PCA) and a thromboxane receptor antagonist (TXAA) are suitable for joint application to thrombotic and thromboembolic syndromes.
摘要翻译：包含前列腺素（PG），前列环素（PC）或前列环素类似物（PCA）和血栓素受体拮抗剂（TXAA）的组合产品适用于联合应用于血栓形成和血栓栓塞综合征。

4. 发明授权

US5204371A Pharmaceutically active 9-chloroprostaglandins 失效
标题翻译：药用活性9-氯前列腺素
公开(公告)号：US5204371A
公开(公告)日：1993-04-20
申请号：US792574
申请日：1991-11-15
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
IPC分类号： C07C405/00
CPC分类号： C07C405/0041 , C07C405/00
摘要： Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.-or .beta.-position,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 --CH.tbd.C--, W is hydroxymethylene orD and E together represent a direct bond orD is a straight-chain or branched alkylene group of 1-10 carbon atoms, optionally substituted by fluorine, andE is oxygen or sulfur or a direct bond, andR.sub.4 is hydroxy or hydroxy etherified or esterified as defined for W above;R.sub.5 is a C.sub.1-10 hydrocarbon aliphatic group; a C.sub.1-10 hydrocarbon aliphatic group substituted by aryl, a substituted aryl as defined for R.sub.2 above, or halogen; or cycloalkyl, substituted cycloalkyl, aryl, substituted aryl or aromatic heterocyclic, all as defined for R.sub.2 above;or a physiologically acceptable salt thereof with a base when R.sub.1 is OH,have valuable pharmacologoical properties.
摘要翻译：其中9-氯原子可以是α-或β-位的式为“IMAGE”的化合物，A为-CH 2 -CH 2 - 或顺式-CH = CH-，B为-CH 2 -CH 2， - ， CH = CH-或-CH 3 B - ，W是羟基亚甲基或D和E一起代表直接键，或D是1-10个碳原子的直链或支链亚烷基，任选被氟取代，E是氧或硫或直接键，并且R4是如上定义的羟基或羟基醚化或酯化; R5是C1-10烃脂族基团; 被芳基取代的C1-10烃脂族基，对上述R2定义的取代芳基或卤素; 或环烷基，取代的环烷基，芳基，取代的芳基或芳族杂环，全部如上述R2所定义; 或其生理上可接受的盐，当R1为OH时，具有有价值的药理学性质。

5. 发明授权

US5004752A Novel 9-haloprostaglandins, processes for their preparation, and their use as medicinal agents 失效
标题翻译：新型9-卤代前列腺素，其制备方法及其作为药物的用途
公开(公告)号：US5004752A
公开(公告)日：1991-04-02
申请号：US350951
申请日：1989-05-08
申请人： Bernd Raduechel , Werner Skuballa , Helmut Vorbrueggen , Olaf Loge , Ekkehard Schilliner
发明人： Bernd Raduechel , Werner Skuballa , Helmut Vorbrueggen , Olaf Loge , Ekkehard Schilliner
IPC分类号： A61K31/557 , A61K31/5575 , A61P1/04 , A61P7/02 , A61P9/06 , A61P9/12 , C07C67/00 , C07C401/00 , C07C405/00
CPC分类号： C07C405/00
摘要： The invention relates to 9-halo-15-cycloalkyl prostaglandin derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen or methyl,R.sub.2 is fluorine or chlorine,n is 0 or 1,and, if R.sub.1 is hydrogen, the salts thereof with physiologically compatible bases or the cyclodextrin clathrates thereof, processes for their preparation, and their pharmaceutical usage.
摘要翻译：本发明涉及式I的9-卤代-15-环烷基前列腺素衍生物，其中R1是氢或甲基，R2是氟或氯，n是0或1，如果R1是氢，其与生理上相容的碱或其环糊精包合物，其制备方法及其药物用途。

6. 发明授权

US4444788A Pharmaceutically active 9-chloroprostaglandins 失效
标题翻译：药用活性9-氯前列腺素
公开(公告)号：US4444788A
公开(公告)日：1984-04-24
申请号：US387140
申请日：1982-06-10
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00 , C07C405/0041
摘要： Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.- or .beta.-position,R.sub.1 is OR.sub.2, or NHR.sub.3 wherein R.sub.3 is H or the acyl group ofa C.sub.1-15 hydrocarbon carboxylic or sulfonic acid;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--, ##STR2## wherein the OH-group in each case can be in the .alpha.- or .beta.-position, and can be etherified or esterified by tetrahydropyranyl, tetrahydrofuranyl, .alpha.-ethoxyethyl, trimethylsilyl dimethyl, tert-butylsilyl, tribenzylsilyl, acetyl, propionyl, butyryl or benzoyl;D and E together represent a direct bond orD is a straight-chain or branched alkylene group of 1-10 carbon atoms, optionally substituted by fluorine, andE is oxygen or sulfur or a direct bond, andR.sub.4 is hydroxy or hydroxy etherified or esterified as defined for W above;R.sub.5 is a C.sub.1-10 hydrocarbon aliphatic group; a C.sub.1-10 hydrocarbon, aliphatic group substituted by aryl, a substituted aryl as defined for R.sub.2 above, or halogen; or cycloalkyl, substituted cycloalkyl, aryl, substituted aryl or aromatic heterocyclic, all as defined for R.sub.2 above;or a physiologically acceptable salt thereof with a base when R.sub.1 is OH,have valuable pharmacological properties.
摘要翻译：其中9-氯原子可以是α-或β-位，R1是OR2或NHR3，其中R3是H或C1-15烃羧酸或磺酸的酰基; 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，，其中每种情况下的OH-基团可以是四氢呋喃基，α-乙氧基乙基，三甲基甲硅烷基二甲基，叔丁基甲硅烷基，三苄基甲硅烷基，乙酰基，丙酰基，丁酰基或苯甲酰基可以醚化或酯化。 D和E一起代表直接键或D是1-10个碳原子的直链或支链亚烷基，任选被氟取代，E是氧或硫或直接键，并且R 4是羟基或羟基醚化或酯化如上述W所定义; R5是C1-10烃脂族基团; C1-10烃基，被芳基取代的脂族基团，对上述R2定义的取代芳基或卤素; 或环烷基，取代的环烷基，芳基，取代的芳基或芳族杂环，全部如上述R2所定义; 或其生理上可接受的盐，当R1为OH时，具有有价值的药理学性质。

7. 发明授权

US4359581A Process for the production of caracyclin intermediates 失效
标题翻译：生产青蒿素中间体的方法
公开(公告)号：US4359581A
公开(公告)日：1982-11-16
申请号：US270716
申请日：1981-06-05
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen
IPC分类号： C07C67/30 , C07C69/757 , C07C405/00 , C07D307/935 , C07F7/08 , C07D309/12 , C07C69/76 , C07D37/20
CPC分类号： C07C405/0083
摘要： A process for preparing a 3-oxo-7-hydroxy-bicyclo[3,3,0]octan-2-ylcarboxylic acid ester of the formula ##STR1## wherein R.sub.1 is alkyl of 1-6 carbon atoms or phenalkyl of 7-10 carbon atoms andR.sub.2 is hydrogen, alkyl or 1-6 carbon atoms, phenalkyl of 7-10 carbon atoms, tetrahydropyranyl, tetrahydrofuranyl, .alpha.-ethoxyethyl, tri-C.sub.1-4 -alkylsilyl, wherein the alkyl moieties can optionally be substituted by phenyl, or ##STR2## wherein R.sub.3 is alkyl of 1-6 carbon atoms or aryl of 6-12 carbon atoms, comprises oxidizing the corresponding 7-hydroxy-2-oxabicyclo [3,3,0]octan-3-ylideneacetic acid ester of the formula ##STR3## wherein R.sub.1 and R.sub.2 are as defined above, to form the corresponding ketone, reacting the latter with a base which opens the ether oxygen containing ring, and then reducing the resultant product to prepare the 3-oxo-7-hydroxy-bicyclo[3,3,0]octan-2-ylcarboxylic acid ester.
摘要翻译：制备下式的“3-氧代-7-羟基 - 双环[3,3,0]辛-2-基羧酸酯的方法，其中R1是1-6个碳原子的烷基或7-10的苯基烷基碳原子，R 2是氢，烷基或1-6个碳原子，7-10个碳原子的苯基烷基，四氢吡喃基，四氢呋喃基，α-乙氧基乙基，三-C 1-4 - 烷基甲硅烷基，其中烷基部分可以任选被苯基取代，或者其中R 3为1-6个碳原子的烷基或6-12个碳原子的芳基，包括将相应的7-羟基-2-氧杂双环[3,3,0]辛-3-基亚乙基乙酸酯氧化为其中R 1和R 2如上定义，以形成相应的酮，使后者与打开醚氧环的碱反应，然后还原所得产物以制备3-氧代-7-羟基 - 双环[3,3,0]辛-2-基羧酸酯。

8. 发明授权

US4346228A Novel 11-oxoprostaglandin derivatives 失效
标题翻译：新型11-氧代前列腺素衍生物
公开(公告)号：US4346228A
公开(公告)日：1982-08-24
申请号：US677420
申请日：1976-04-15
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 , C07D307/20 , C07D307/935 , C07D309/12 , C07D521/00 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12
摘要： 11-Oxoprostaglandin derivatives of the formula ##STR1## wherein R.sub.2 is a hydrogen atom or alkyl of 1-5 carbon atoms,R.sub.3 is alkyl of 1-5 carbon atoms, alkylaryl, cycloalkyl of 5-6 ring carbon atoms and a total of 5-10 carbon atoms; benzodioxol-2-yl, phenyl, naphthyl or phenyl or naphthyl substituted by phenyl, halogen, alkyl of 1-4 carbon atoms, chloromethyl, fluoromethyl, carboxyl or hydroxy;A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, or trans--CH.dbd.CH--;B is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--,D and E collectively are a direct bond or D is alkylene of 1-5 carbon atoms and E is an oxygen or sulfur atom; esters thereof; readily cleavable 9,15 and 9,15 ethers thereof; methanesulfonylamides thereof, and physiologically acceptable salts thereof with bases; possess the activity of the corresponding natural prostaglandins with a surprisingly longer duration of effectiveness, greater selectivity, and better effects, and can be produced, e.g., by oxidation of the corresponding 9-hydroxy prostaglandins.
摘要翻译：其中R2是氢原子或1-5个碳原子的烷基，R3是1-5个碳原子的烷基，烷基芳基，5-6个环碳原子的环烷基和总共5个碳原子的11-前列酰乳糖衍生物 -10个碳原子; 苯基二氧杂环戊烯-2-基，苯基，萘基或被苯基，卤素，1-4个碳原子的烷基取代的苯基或萘基，氯甲基，氟甲基，羧基或羟基; A是-CH 2 -CH 2 - ，顺式-CH = CH-或反式-CH = CH-; B是-CH 2 -CH 2 - 或反式-CH = CH-，D和E共同是直接键或D是1-5个碳原子的亚烷基，E是氧或硫原子; 其酯; 易于切割的9,15和9,15醚; 甲磺酰胺及其与碱的生理学上可接受的盐; 具有相当的天然前列腺素的活性，具有惊人的更长的有效期，更高的选择性和更好的效果，并且可以例如通过相应的9-羟基前列腺素的氧化来产生。

9. 发明授权

US06294152B1 Iron(III) complexes as contrast agents for image enhancement in magnetic resonance imaging 失效
标题翻译：铁（III）配合物作为磁共振成像中图像增强的造影剂
公开(公告)号：US06294152B1
公开(公告)日：2001-09-25
申请号：US09227961
申请日：1999-01-11
申请人： Julian A. Davies , Wolfgang Ebert , Bernd Raduechel , Heribert Schmitt-Willich
发明人： Julian A. Davies , Wolfgang Ebert , Bernd Raduechel , Heribert Schmitt-Willich
IPC分类号： A61B5055
CPC分类号： A61K49/101
摘要： A compound of formula (I): wherein, R1 is independently selected from methyl and ethyl and R2 is independently selected from hydrogen, alkyl, and substituted alkyl. 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. The present invention also relates to a method of administering the second sphere contrast agent.
摘要翻译：式（I）化合物：其中，R 1独立地选自甲基和乙基，R 2独立地选自氢，烷基和取代的烷基。该化合物能够作为配体并与顺磁性Fe（III）离子络合，用作组织磁共振成像的第二球对比增强剂。本发明还涉及施用第二球形造影剂的方法。

10. 发明授权

US06083479A Contrast media for infarction and necrosis imaging 失效
标题翻译：对照介质用于梗死和坏死成像
公开(公告)号：US06083479A
公开(公告)日：2000-07-04
申请号：US157959
申请日：1998-09-22
申请人： Johannes Platzek , Ulrich Niedballa , Bernd Raduechel , Wolfgang Ebert , Hanns Joachim Weinmann
发明人： Johannes Platzek , Ulrich Niedballa , Bernd Raduechel , Wolfgang Ebert , Hanns Joachim Weinmann
IPC分类号： A61K49/00 , A61K49/06 , A61K51/00 , A61K51/04 , C07B59/00 , C07D257/02 , A61B5/055 , A61K49/04
CPC分类号： A61K51/0478 , A61K49/103 , A61K49/106 , A61K51/0482 , C07B59/004 , C07D257/02 , Y10S514/836
摘要： The invention relates to new compounds that are suitable as contrast media especially for infarction and necrosis imaging, process for their production and pharmaceutical agents that contain these compounds.
摘要翻译：本发明涉及适用于特别用于梗塞和坏死成像的造影剂，其生产方法和含有这些化合物的药剂的新化合物。

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