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1. 发明申请

US20080242713A1 Novel 5-cyano-prostacyclin derivatives as agents for the treatment of autoimmune diseases 审中-公开
标题翻译：新型5-氰基 - 前列环素衍生物作为治疗自身免疫性疾病的药物
公开(公告)号：US20080242713A1
公开(公告)日：2008-10-02
申请号：US12079598
申请日：2008-03-27
申请人： William Guilford , Werner Skuballa , Daryl H. Faulds , Monica Kochanny , Wheeseong Lee , Bernd Raduchel
发明人： William Guilford , Werner Skuballa , Daryl H. Faulds , Monica Kochanny , Wheeseong Lee , Bernd Raduchel
IPC分类号： A61K31/41 , A61K31/343 , C07D307/77 , A61P37/00 , C07D405/02
CPC分类号： C07D307/937 , C07D405/06
摘要： This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating autoimmune diseases. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
摘要翻译：本发明涉及式（I）化合物：其中A，B，D，E，m和R 1 -R 5如本文所述，作为单立体异构体或其立体异构体或其药学上可接受的盐，包合物或前药的混合物，其可用于治疗自身免疫性疾病。还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。

2. 发明申请

US20050147563A1 Metal complexes that contain perfluoroalkyl, process for their production and their use in NMR diagnosis 失效
标题翻译：含有全氟烷基的金属络合物，其制备方法及其在核磁共振诊断中的应用
公开(公告)号：US20050147563A1
公开(公告)日：2005-07-07
申请号：US10957628
申请日：2004-10-05
申请人： Johannes Platzek , Ulrich Niedballa , Bernd Raduchel , Wolfgang Schlecker , Hanns-Joachim Weinmann , Thomas Frenzel , Bernd Misselwitz , Wolfgang Ebert
发明人： Johannes Platzek , Ulrich Niedballa , Bernd Raduchel , Wolfgang Schlecker , Hanns-Joachim Weinmann , Thomas Frenzel , Bernd Misselwitz , Wolfgang Ebert
IPC分类号： C07D295/22 , A61K49/00 , A61K49/10 , A61P35/00 , A61P43/00 , B65D25/16 , B65D47/08 , B65D83/00 , C07C229/16 , C07C229/22 , C07C229/76 , C07C235/10 , C07C237/08 , C07C237/10 , C07C311/05 , C07C311/06 , C07D257/02 , C07D295/26 , C07F5/00 , C07F13/00
CPC分类号： C07D295/26 , A61K49/0002 , A61K49/0004 , B65D25/16 , B65D47/0847 , B65D83/0055 , C07C229/76 , C07C237/10 , C07D257/02
摘要： The invention relates to new, monomeric, perfluoroalkyl-substituted metal complexes, processes for their production, and their use in diagnosis and therapy. The compounds according to the invention are suitable especially as in vivo contrast media in nuclear spin tomography (MRT). They can preferably be used as blood-pool agents and as lymphographic agents.
摘要翻译：本发明涉及新的单体，全氟烷基取代的金属络合物，其生产方法及其在诊断和治疗中的应用。根据本发明的化合物特别适用于核自旋断层扫描（MRT）中的体内造影剂。它们可优选用作血液池剂和淋巴药剂。

3. 发明授权

US5919431A 1,4,7,10-tetraazacyclododecane derivatives, their use, pharmaceutical agents containing these compounds and process for their production 失效
标题翻译： 1,4,7,10-四氮杂环十二烷衍生物，它们的用途，含有这些化合物的药剂及其生产方法
公开(公告)号：US5919431A
公开(公告)日：1999-07-06
申请号：US649672
申请日：1996-12-06
申请人： Christoph-Stephan Higler , Wolfgang Ebert , Mary Lee-Vaupel , Johannes Platzek , Jurgen Conrad , Bernd Raduchel
发明人： Christoph-Stephan Higler , Wolfgang Ebert , Mary Lee-Vaupel , Johannes Platzek , Jurgen Conrad , Bernd Raduchel
IPC分类号： A61K49/00 , A61K49/06 , A61K51/00 , C07C311/03 , C07C311/04 , C07D257/02 , A61B5/055
CPC分类号： C07D257/02 , A61K49/06 , Y10S514/836
摘要： The invention relates to new 1,4,7,10-tetraazacyclododecane derivatives of formula I ##STR1## in which R.sup.1, R.sup.2, X and V have various meanings, their metal complexes, pharmaceutical agents containing these compounds, their use in diagnosis and treatment as well as process for the production of these compounds and agents.
摘要翻译： PCT No.PCT / EP94 / 03718 Sec。 371日期1996年12月6日第 102（e）日期1996年12月6日PCT 1994年11月10日PCT PCT。公开号WO95 / 14678 日期：1995年6月1日本发明涉及式Ⅰ的新的1,4,7,10-四氮杂环十二烷衍生物，其中R1，R2，X和V具有各种含义，它们的金属络合物，含有这些化合物的药剂，它们在诊断中的应用以及用于生产这些化合物和试剂的处理以及方法。

4. 发明授权

US5744616A Process for the production of 1,4,7,10-tetraazacyclododecane and its derivatives 失效
标题翻译：生产1,4,7,10-四氮杂环十二烷及其衍生物的方法
公开(公告)号：US5744616A
公开(公告)日：1998-04-28
申请号：US805585
申请日：1997-02-25
申请人： Orlin Petrov , Annette Prelle , Klaus Graske , Klaus Nickisch , Bernd Raduchel , Johannes Platzek
发明人： Orlin Petrov , Annette Prelle , Klaus Graske , Klaus Nickisch , Bernd Raduchel , Johannes Platzek
IPC分类号： C07D257/02 , C07D229/02
CPC分类号： C07D257/02
摘要： A process for the production of 1,4,7,10-tetraazacyclododecane (cyclene) and its derivatives on an industrial scale comprises cyclotetramerizing of benzylaziridine that is produced in situ.
摘要翻译：在工业规模上生产1,4,7,10-四氮杂环十二烷（环己烯）及其衍生物的方法包括原位生产的苄基氮丙啶的环型四聚反应。

5. 发明授权

US4692464A Novel prostacyclin derivatives and a process for the preparation thereof 失效
公开(公告)号：US4692464A
公开(公告)日：1987-09-08
申请号：US352411
申请日：1982-02-26
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
IPC分类号： C07D309/12 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61P7/02 , A61P25/02 , A61P43/00 , C07C45/59 , C07C45/67 , C07C45/71 , C07C51/00 , C07C51/353 , C07C59/46 , C07C62/32 , C07C67/00 , C07C67/343 , C07C69/732 , C07C401/00 , C07C405/00 , C07D317/72 , C07D319/12 , C07C177/00
CPC分类号： C07D317/72 , A61K31/557 , C07C405/0083 , C07C45/59 , C07C45/673 , C07C45/71 , C07C62/32 , C07D319/12
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is (a) hydrogen, (b) C.sub.1-10 alkyl, (c) C.sub.1-10 alkyl substituted by halogen; C.sub.1-4 alkoxy; C.sub.6-10 aryl; C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; di-C.sub.1-4 -alkylamino; or tri-C.sub.1-4 -alkylammonium, (d) C.sub.4-10 cycloalkyl, (e) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (f) C.sub.6-10 aryl, (g) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group, or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C--;W is hydroxymethylene, RO-methylene, CH.sub.3 or CH.sub.3, ##STR2## wherein OH or OR is in the .alpha.- or .beta.-position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins;D and E together are a direct bond, orD is C.sub.1-10 alkylene, C.sub.1-10 alkenylene or C.sub.1-10 alkynylene or one of these groups substituted by fluorine, andE is oxygen, --C.tbd.C-- or a direct bond;R.sub.2 is (a) a C.sub.1-10 hydrocarbon aliphatic radical, (b) a C.sub.6-10 hydrocarbon aliphatic radical substituted by C.sub.6-10 aryl or by C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; (c) C.sub.4-10 cycloalkyl, (d) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (e) C.sub.6-10 aryl, (f) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S; andR.sub.3 is OH or OR; and, when R.sub.1 is hydrogen, the salts thereof with physiologically compatible bases, are effective as antihypertensive, bronchiodilators, thrombocyte aggregation inhibitors, inter alia.

6. 发明授权

US4364950A 5-Cyano-prostacyclin derivatives and use as medicines 失效
标题翻译： 5-Cyano-prostacyclin衍生物用作药物
公开(公告)号：US4364950A
公开(公告)日：1982-12-21
申请号：US317621
申请日：1981-11-02
申请人： Werner Skuballa , Helmut Vorbruggen , Bernd Raduchel , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Helmut Vorbruggen , Bernd Raduchel , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： A61K31/557 , A61P7/02 , A61P9/12 , A61P11/08 , A61P43/00 , C07D307/935 , C07D307/937 , C07F7/18 , C07F9/40
CPC分类号： C07D307/935 , C07D307/937 , C07F7/1856 , C07F9/4015
摘要： 5-cyano-prostacyclins of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ; R.sub.2 and R.sub.3 each independently is (a) H, (b) C.sub.1-10 -alkyl, (c) C.sub.1-10 -alkyl substituted by halo, C.sub.1-4 -alkoxy or phenyl, 1-naphthyl or 2-naphthyl, each optionally substituted as defined below, (d) C.sub.4-10 -cycloalkyl, (e) C.sub.4-10 -cycloalkyl substituted by C.sub.1-4 -alkyl, (f) phenyl, 1-naphthyl or 2-naphthyl, (g) phenyl, 1-naphthyl or 2-naphthyl substituted by 1-3 halogen atoms, phenyl, 1-3 alkyl groups of 1-4 C atoms each, or a chloromethyl-, fluoromethyl-, trifluoromethyl-, carboxyl-, hydroxy- or alkoxy-group of 1-4 C atoms, or (h) an aromatic, 5- or 6-membered heterocyclic ring containing one hetero atom which is O, N or S, the remaining atoms being carbon; R.sub.3 also possibly being an acyl group of a C.sub.1-15 -hydrocarbon carboxylic or sulfonic acid;B is straight chain or branched alkylene of 2-10 C atoms;W is hydroxymethylene or ##STR2## wherein the OH group may be in the alpha or beta position, and is optionally modified by replacement of the H atom of the OH with an ether or acyl group which is conventional for such replacements in prostaglandins and which is readily cleavable at physiological pH's;R.sub.4 is hydroxy, optionally modified as described for W above;R.sub.5, R.sub.6, R.sub.7 and R.sub.8 each independently is hydrogen, alkyl of 1-5 C atoms or methoxy; andR.sub.9 is alkyl of 1-5 C atoms orfor compounds wherein R.sub.2 is H, the salts thereof with physiologically compatible bases have valuable pharmacalogical properties, e.g., hypertonic and bronchodilatory activities.
摘要翻译：其中R1是OR2或NHR3的式“IMAGE”的5-氰基 - 前列环素; R 2和R 3各自独立地为（a）H，（b）C 1-10 - 烷基，（c）被卤素，C 1-4 - 烷氧基或苯基，1-萘基或2-萘基取代的C 1-10 - 烷基，（d）C 4-10 - 环烷基，（e）被C 1-4 - 烷基取代的C 4-10 - 环烷基，（f）苯基，1-萘基或2-萘基，（g）苯基，萘基或被1-3个卤素原子取代的2-萘基，苯基，1-4个C原子的1-3个烷基，或1个氯甲基 - ，氟甲基 - ，三氟甲基 - ，羧基 - ，羟基或烷氧基 -4个C原子，或（h）含有一个杂原子的芳族的5或6元杂环，它是O，N或S，其余的原子是碳; R3也可能是C1-15-烃羧酸或磺酸的酰基; B是2-10个C原子的直链或支链亚烷基; W是羟基亚甲基或其中OH基团可以在α或β位置，并且任选地通过用在前列腺素中这种替代物常规的醚或酰基取代OH的H原子来任意修饰，并且其是在生理pH值下易于切割; R4是羟基，任选地按照上述W所述进行改性; R5，R6，R7和R8各自独立地为氢，1-5个C原子的烷基或甲氧基; 并且R 9为1-5个C原子的烷基，或对于其中R 2为H的化合物，其与生理上相容的碱的盐具有有价值的药理学性质，例如高渗和支气管扩张活性。

7. 发明授权

US4004020A Novel prostanoic acid derivatives and process for the preparation thereof 失效
标题翻译：新型前列腺酸衍生物及其制备方法
公开(公告)号：US4004020A
公开(公告)日：1977-01-18
申请号：US534483
申请日：1974-12-19
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
IPC分类号： C07D317/14 , C07D317/46 , C07D317/70 , C07D319/06 , C07D319/08 , C07F9/40 , C07F9/54 , A01N9/28 , A61K31/335
CPC分类号： C07F9/4006 , C07D317/46 , C07D317/70 , C07D319/06 , C07F9/5407
摘要： Prostaglandins of the formula ##STR1## wherein R.sub.1 is hydroxymethyl, carboxy, aryloxycarbonyl, alkoxycarbonyl of 1-8 carbon atoms in the alkoxy group, or the group -COO-CH.sub.2 -U-V wherein U is a direct C-C bond, carbonyl or carbonyloxy and V is phenyl substituted by phenyl, alkoxy of 1-2 carbon atoms or halogen; R.sub.2 is hydroxy and R.sub.3 is a hydrogen atom or R.sub.2 and R.sub.3 collectively are an oxygen atom; A is -CH.sub.2 -CH.sub.2 or trans-CH=CH; B is -CH.sub.2 -CH.sub.2 or CH=CH; one of R.sub.4 and R.sub.5 is hydroxy and the other is a hydrogen atom; R.sub.6 and R.sub.7 each are alkyl of 1-10 carbon atoms or collectively are alkylene of up to 7 carbon atoms and with 2-3 carbon atoms in the chain, phenylene or naphthylene; R.sub.8 is a hydrogen atom or alkyl of 1-5 carbon atoms; ##STR2## when R.sub.2 is hydroxy and R.sub.3 is a hydrogen atom or is ##STR3## or -CH=CH- when R.sub.2 and R.sub.3 collectively are an oxygen atom; or, when R.sub.1 is carboxy, a physiologically acceptable salt thereof with a base, possess the activity of the corresponding natural prostaglandins, including a luteolytic effect, and are useful in triggering abortions and syncronizing the conception cycle of mammals.
摘要翻译：其中R1是羟甲基，羧基，芳氧基羰基，烷氧基中1-8个碳原子的烷氧基羰基或基团-COO-CH2-UV，其中U是直接的CC键，羰基或羰基氧基和V 是被苯基，1-2个碳原子的烷氧基或卤素取代的苯基; R2是羟基，R3是氢原子，R2和R3一起是氧原子; A是-CH 2 -CH 2或反式-CH = CH; B是-CH 2 -CH 2或CH = CH; R4和R5之一是羟基，另一个是氢原子; R6和R7各自为1-10个碳原子的烷基，或者统称为至多7个碳原子的亚烷基，链中有2-3个碳原子，亚苯基或亚萘基; R8是氢原子或1-5个碳原子的烷基; 当R2和R3共同为氧原子时，当R 2为羟基且R 3为氢原子或者为或者-CH = CH-时，或者，当R 1为羧基时，其与碱的生理上可接受的盐具有相应的天然前列腺素的活性，包括溶血性作用，并且可用于触发哺乳动物的受孕循环的流产和同步化。

8. 发明申请

US20070014725A1 Conjugates of macrocyclic metal complexes with biomolecules and their use for the production of agents for NMR diagnosis and radiodiagnosis as well as radiotherapy 审中-公开
标题翻译：大环金属配合物与生物分子的共轭物及其用于生产核磁共振诊断和放射诊断以及放射治疗剂的用途
公开(公告)号：US20070014725A1
公开(公告)日：2007-01-18
申请号：US11390414
申请日：2006-03-28
申请人： Johannes Platzek , Heribert Schmitt-Willich , Gunther Michl , Thomas Frenzel , Detlev Sulzle , Hans Bauer , Bernd Raduchel , Hanns-Joachim Weinmann , Heiko Schirmer
发明人： Johannes Platzek , Heribert Schmitt-Willich , Gunther Michl , Thomas Frenzel , Detlev Sulzle , Hans Bauer , Bernd Raduchel , Hanns-Joachim Weinmann , Heiko Schirmer
IPC分类号： A61K51/00 , A61K49/10 , C07K14/47 , C07F5/00
CPC分类号： A61K49/14 , A61K49/0002 , A61K49/085 , A61K49/143
摘要： The invention relates to conjugates that consist of macrocyclic metal complexes with biomolecules and their production. The conjugates are suitable as contrast media in NMR diagnosis and radiodiagnosis as well as as agents for radiotherapy. High relaxivity is achieved by a special liganding of macrocyclic compounds, and a fine-tuning of the relaxivity is made possible.
摘要翻译：本发明涉及由大环金属配合物与生物分子组成的共轭物及其生产。缀合物适用于核磁共振诊断和放射诊断中的造影剂以及放射治疗剂。通过大环化合物的特殊结合实现高的放松性，并且可以进行微调的松弛度。

9. 发明申请

US20070009442A1 Macrocyclic metal complexes and their use for the production of conjugates with biomolecules 审中-公开
公开(公告)号：US20070009442A1
公开(公告)日：2007-01-11
申请号：US11390472
申请日：2006-03-28
申请人： Johannes Platzek , Heribert Schmitt-Willich , Gunther Michl , Thomas Frenzel , Detlev Sulzle , Hans Bauer , Bernd Raduchel , Hanns-Joachim Weinmann , Heiko Schirmer
发明人： Johannes Platzek , Heribert Schmitt-Willich , Gunther Michl , Thomas Frenzel , Detlev Sulzle , Hans Bauer , Bernd Raduchel , Hanns-Joachim Weinmann , Heiko Schirmer
IPC分类号： A61K49/10 , C07K14/47 , C07H21/04 , C07D257/02 , C07D487/22
CPC分类号： A61K49/10 , A61K47/54 , A61K47/547 , A61K49/0002 , A61K49/085 , A61K49/14 , A61K49/143 , C07D257/02
摘要： The invention relates to macrocyclic metal complexes and their production and use for the production of conjugates with biomolecules. The conjugates are suitable as contrast media in NMR diagnosis and radiodiagnosis as well as for radiotherapy. High relaxivity is achieved by a special liganding of macrocyclic compounds, and a fine-tuning of the relaxivity is made possible.

10. 发明授权

US6019959A Oligomeric compounds that contain perfluoroalkyl, process for their production, and their use in NMR diagnosis 失效
标题翻译：含有全氟烷基的低聚化合物，其制备方法及其在NMR诊断中的应用
公开(公告)号：US6019959A
公开(公告)日：2000-02-01
申请号：US106146
申请日：1998-06-29
申请人： Johannes Platzek , Ulrich Niedballa , Bernd Raduchel , Wolfgang Schlecker , Hanns-Joachim Weinmann , Thomas Frenzel , Bernd Misselwitz , Wolfgang Ebert
发明人： Johannes Platzek , Ulrich Niedballa , Bernd Raduchel , Wolfgang Schlecker , Hanns-Joachim Weinmann , Thomas Frenzel , Bernd Misselwitz , Wolfgang Ebert
IPC分类号： A61K49/08 , C07D257/02 , A61K51/00 , A61B5/055 , C07F15/00 , C07F19/00
CPC分类号： A61K49/10 , A61K49/085 , A61K51/0497 , C07D257/02
摘要： Oligomeric compounds that contain perfluoroalkyl of general formula IA--R.sup.F (I)in whichA is a molecule portion that contains 2-6 metal complexes that are connected directly or via a linker to a nitrogen atom of an annular skeleton chain, andR.sup.F is a perfluorinated, straight-chain or branched carbon chain with formula --C.sub.n F.sub.2n E, in which E represents a terminal fluorine, chlorine, bromine, iodine, or hydrogen atom and n stands for numbers 4-30,are valuable compounds for diagnosis, especially as in-vivo contrast media.
摘要翻译：含有通式IA-RF（I）的全氟烷基的低聚化合物，其中A是含有直接或通过连接基与环状骨架链的氮原子连接的2-6个金属络合物的分子部分，RF是具有式-CnF 2 nE的全氟化，直链或支链碳链，其中E表示末端氟，氯，溴，碘或氢原子，n代表4-30，是用于诊断的有价值的化合物，体内造影剂。

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