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1. 发明申请

US20110112097A1 Substituted imidazoline-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof 审中-公开
标题翻译：取代的咪唑啉-2,4-二酮，其制备方法，包含这些化合物的药物及其用途
公开(公告)号：US20110112097A1
公开(公告)日：2011-05-12
申请号：US12852084
申请日：2010-08-06
申请人： Gerhard Jaehne , Peter Below , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Irvin Winkler
发明人： Gerhard Jaehne , Peter Below , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Irvin Winkler
IPC分类号： A61K31/5377 , C07D233/72 , A61K31/415 , C07D413/10 , C07D471/10 , A61K31/438 , C07D487/10 , C07D401/04 , A61K31/4439 , A61P3/00 , A61P3/10 , A61P3/04 , A61P25/34 , A61P25/32 , A61P25/00 , A61P25/18 , A61P25/28
CPC分类号： C07D401/04 , C07D233/74 , C07D235/02 , C07D405/04 , C07D409/04 , C07D471/04
摘要： The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
摘要翻译：本发明涉及式（I）化合物，其中基团R和R'，A，D，E，G，L，p和R 1至R 10具有所述含义及其生理上相容的盐。所述化合物例如适合作为抗肥胖药物。

2. 发明申请

US20110046105A1 Heterocycle-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising them and use thereof 审中-公开
标题翻译：杂环取代的咪唑烷-2,4-二酮，其制备方法，包含它们的药物及其用途
公开(公告)号：US20110046105A1
公开(公告)日：2011-02-24
申请号：US12852233
申请日：2010-08-06
申请人： Gerhard Jaehne , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Irvin Winkler
发明人： Gerhard Jaehne , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Irvin Winkler
IPC分类号： A61K31/4178 , C07D401/12 , A61K31/497 , A61P3/04 , A61P3/10 , A61P25/28 , A61P25/18 , A61P25/32 , A61P25/34 , A61K31/4184 , A61K31/501 , C07D413/14 , A61K31/5355 , A61K31/454
CPC分类号： C07D233/72 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
摘要翻译：本发明涉及式（I）化合物，其中基团R和R'，A，D，E，G，L，p和R 1至R 10具有所述含义及其生理上相容的盐。所述化合物例如适合作为抗肥胖药物。

3. 发明授权

US07759366B2 Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use 有权
标题翻译：芳基氨基芳基 - 烷基取代的咪唑烷-2,4-二酮，其制备方法，包含这些化合物的药物及其用途
公开(公告)号：US07759366B2
公开(公告)日：2010-07-20
申请号：US12365940
申请日：2009-02-05
申请人： Gerhard Jaehne , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Irvin Winkler
发明人： Gerhard Jaehne , Siegfried Stengelin , Matthias Gossel , Thomas Klabunde , Irvin Winkler
IPC分类号： A61K31/4439 , A61K31/4166 , C07D401/04 , C07D233/72 , C07D233/74 , C07D209/54
CPC分类号： C07D233/72
摘要： This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R′, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.
摘要翻译：本发明涉及式（I）的芳基氨基芳基 - 烷基取代的咪唑烷酮-2,4-二酮，也涉及其生理上耐受的盐：其中R，R'，R 1至R 10，A，D，E，G，L和p 如本文所定义。本发明还涉及制备它们的方法，包含它们的药物组合物及其治疗用途。该化合物例如适合作为抗肥胖药物和治疗心脏代谢综合征。

4. 发明授权

US5457091A N1-substituted 1H-1,2,3-triazolo[4,5,-D]pyrimidines, a process for their preparation and their use as antiviral agents 失效
标题翻译： N1取代的1H-1,2,3-三唑并[4,5，-D]嘧啶，其制备方法及其作为抗病毒剂的用途
公开(公告)号：US5457091A
公开(公告)日：1995-10-10
申请号：US125195
申请日：1993-09-23
申请人： Gerhard Jaehne , Matthias Helsberg , Irvin Winkler , Gerhard Gross , Thomas Scholl
发明人： Gerhard Jaehne , Matthias Helsberg , Irvin Winkler , Gerhard Gross , Thomas Scholl
IPC分类号： A61K31/505 , A61P31/12 , C07D487/04 , C07F9/6561 , C07D239/00
CPC分类号： C07D487/04
摘要： N1-Substituted 1H-1,2,3-triazolo[4,5-d]pyrimidine compounds of the formula I ##STR1## in which the substituents X, Y, R.sup.1, R.sup.2 and R.sup.3 have the meanings recited in the specification, are described as pharmaceutical compositions containing them and processes for their preparation. The compounds are effective antiviral agents.
摘要翻译：取代基X，Y，R 1，R 2和R 3具有式I（I）中所述的取代基的N 1 - 取代的1 H-1,2,3-三唑并[4,5-d]嘧啶化合物描述为含有它们的药物组合物及其制备方法。这些化合物是有效的抗病毒剂。

5. 发明授权

US5789383A Bradykinin antagonists for the prophylaxis or treatment of virus diseases 失效
标题翻译：缓激肽拮抗剂用于预防或治疗病毒性疾病
公开(公告)号：US5789383A
公开(公告)日：1998-08-04
申请号：US366598
申请日：1994-12-29
申请人： Klaus Wirth , Irvin Winkler , Fred Lembeck , Gerhard Breipohl , Stephan Henke , Jochen Knolle
发明人： Klaus Wirth , Irvin Winkler , Fred Lembeck , Gerhard Breipohl , Stephan Henke , Jochen Knolle
IPC分类号： A61K38/17 , A61K38/04 , A61K38/08 , A61P31/12 , A61K38/00 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： A61K38/043
摘要： Bradykinin antagonists and their physiologically tolerated salts are suitable for the treatment or prophylaxis of virus diseases.
摘要翻译：缓激肽拮抗剂及其生理耐受盐适用于治疗或预防病毒病。

6. 发明授权

US5242908A Use of benzylphosphonic acid derivatives for the treatment of diseases caused by viruses 失效
标题翻译：用于治疗病毒引起的疾病的苯并恶唑酸衍生物的应用
公开(公告)号：US5242908A
公开(公告)日：1993-09-07
申请号：US648622
申请日：1991-02-01
申请人： Anuschirwan Peyman , Eugen Uhlmann , Karlheinz Budt , Jochen Knolle , Irvin Winkler , Matthias Helsberg
发明人： Anuschirwan Peyman , Eugen Uhlmann , Karlheinz Budt , Jochen Knolle , Irvin Winkler , Matthias Helsberg
IPC分类号： A61K31/66 , A61P31/12 , C07F9/38 , C07F9/40 , C07F9/6574
CPC分类号： C07F9/65742 , C07F9/3882 , C07F9/4056
摘要： The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.
摘要翻译：使用其中V为烷基，氟，氯，溴或碘的式I化合物I，其为1至5的整数，W为烷基，烯基，炔基或烷氧基，氰基，硝基，羧基，氢或环烷基，芳基，芳烷基或烷氧基，R1和R2是烷基，烯基，炔基，环烷基或卤代烷基，钠，钾，钙，镁，铝，锂，铵，或氢，R1和R2一起形成环状二酯，R3和R4是烷基，烯基，炔基，烷氧羰基，环烷基或烷氧基，氢，氟，氯，溴或碘，X，Y和Z是氧或硫，描述了用于治疗由DNA病毒或RNA病毒引起的疾病。

7. 发明授权

US6033909A Oligonucleotide analogs, their preparation and use 失效
标题翻译：寡核苷酸类似物，其制备和用途
公开(公告)号：US6033909A
公开(公告)日：2000-03-07
申请号：US281203
申请日：1994-07-27
申请人： Eugen Uhlmann , Anuschirwan Peyman , Gerard O'Malley , Matthias Helsberg , Irvin Winkler
发明人： Eugen Uhlmann , Anuschirwan Peyman , Gerard O'Malley , Matthias Helsberg , Irvin Winkler
IPC分类号： C07H21/00 , C12Q1/68 , C07H21/04
CPC分类号： C07H21/00 , C07B2200/11
摘要： The invention relates to compounds of the formula I ##STR1## where R.sup.1 is H, alkyl, acyl, aryl, or a phosphate residue; R.sup.2 is H, OH, alkoxy, NH.sub.2, or halogen; B is a base customary in nucleotide chemistry; a is O or CH.sub.2 ; n is an integer from 1 to 100; W=O, S or Se; V=O, S, or NH; Y=O, S, NH, or CH.sub.2 ; Y'=O, S, NH, or alkylene; X=OH or SH; U=OH, SH, SeH, alkyl, alkoxy, aryl, aryloxy, or amine, and Z=OH, SH, SeH, an optionally substituted radical from the group comprising alkyl, aryl, heteroaryl, alkoxy, or amino, or a group which favors intracellular uptake or serves as the label of a DNA probe or attacks the target nucleic acid during hybridization, where if Z=OH, SH, CH.sub.3, or OC.sub.2 H.sub.5, at least one of the groups X, Y, Y', V, or W is not OH or O or R.sup.1 is not H; a process for their preparation and their use as inhibitors of gene expression, as probes for detecting nucleic acids and as aids in molecular biology.
摘要翻译：本发明涉及式Ⅰ化合物，其中R1是H，烷基，酰基，芳基或磷酸酯残基; R2是H，OH，烷氧基，NH2或卤素; B是核苷酸化学中常规的基础; a是O或CH2; n为1〜100的整数， W = O，S或Se; V = O，S或NH; Y = O，S，NH或CH 2; Y'= O，S，NH或亚烷基; X = OH或SH; U = OH，SH，SeH，烷基，烷氧基，芳基，芳氧基或胺，Z = OH，SH，SeH，任选取代的基团，其包含烷基，芳基，杂芳基，烷氧基或氨基，其有利于细胞内吸收或用作DNA探针的标记或在杂交期间攻击靶核酸，其中如果Z = OH，SH，CH 3或OC 2 H 5，X，Y，Y'，V，或W不是OH或O或R 1不是H; 其制备方法及其作为基因表达抑制剂的用途，作为检测核酸的探针和分子生物学的辅助工具。

8. 发明授权

US5798365A Substituted quinoline derivatives, a process for their preparation, and their use 失效
标题翻译：取代的喹啉衍生物，其制备方法及其用途
公开(公告)号：US5798365A
公开(公告)日：1998-08-25
申请号：US515556
申请日：1995-08-14
申请人： Reinhard Kirsch , Jorg-Peter Kleim , Gunther Riess , Manfred Rosner , Irvin Winkler
发明人： Reinhard Kirsch , Jorg-Peter Kleim , Gunther Riess , Manfred Rosner , Irvin Winkler
IPC分类号： A61K31/47 , A61P31/12 , A61P31/18 , C07D215/22 , C07D215/227 , C07D215/24 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/58 , C07D221/20 , C07D401/06 , C07D401/12 , C07D401/14
CPC分类号： C07D215/227 , C07D215/22 , C07D215/26 , C07D215/36 , C07D215/38 , C07D221/20 , C07D401/06 , C07D401/12
摘要： Compounds of the formula I, ##STR1## and also their tautomeric forms of the formula Ia, ##STR2## in which the substituents R.sup.1 to R.sup.6 and X have said meanings, exhibit antiviral activity.
摘要翻译：式Ⅰ化合物，（Ⅰ）化合物及其互变异构形式的式Ia，其中取代基R 1至R 6和X具有所述含义，具有抗病毒活性。

9. 发明授权

US6114349A Substituted quinoline derivatives with antiviral action 有权
标题翻译：取代喹啉衍生物与抗病毒作用
公开(公告)号：US6114349A
公开(公告)日：2000-09-05
申请号：US155647
申请日：1999-03-03
申请人： Reinhard Kirsch , Jorg-Peter Kleim , Gunther Riess , Bernd Rosenstock , Manfred Rosner , Irvin Winkler
发明人： Reinhard Kirsch , Jorg-Peter Kleim , Gunther Riess , Bernd Rosenstock , Manfred Rosner , Irvin Winkler
IPC分类号： A61K31/00 , A61K31/47 , A61K31/4704 , A61K31/4709 , A61P31/00 , A61P31/12 , C07D215/22 , C07D215/227 , C07D215/50 , C07D401/12 , C07D491/04 , C07D491/06 , C07D215/12 , C07D215/16 , C07D215/20 , C07D215/38
CPC分类号： C07D215/227 , A61K31/47 , A61K31/4704 , A61K31/4709 , C07D215/50 , C07D401/12 , C07D491/04 , C07D491/06
摘要： Substituted quinoline derivatives, processes for their preparation, and their use.Compounds of the formula I ##STR1## and their tautomeric forms, of the formula Ia ##STR2## in which m, n and the substituents X and R.sup.1 to R.sup.5 have the meanings mentioned, have an action against viruses.
摘要翻译： PCT No.PCT / EP97 / 01496 Sec。 371日期1999年3月3日 102（e）1999年3月3日PCT 1997年3月25日PCT公布。公开号WO97 / 37977 PCT 日期1997年10月16日取代喹啉衍生物，其制备方法及其用途。其中m，n和取代基X和R 1至R 5具有上述含义的式Ⅰ化合物及其互变异构形式具有抗病毒作用。

10. 发明授权

US5804559A Prodrug derivatives of enzyme inhibitors having hydroxyl groups, a process for preparing them, and their use 失效
标题翻译：具有羟基的酶抑制剂的前药衍生物，其制备方法及其应用
公开(公告)号：US5804559A
公开(公告)日：1998-09-08
申请号：US525525
申请日：1995-09-12
申请人： Karl-Heinz Budt , Bernd Stowasser , Anuschirwan Peyman , Jochen Knolle , Irvin Winkler , Hans Gerd Berscheid
发明人： Karl-Heinz Budt , Bernd Stowasser , Anuschirwan Peyman , Jochen Knolle , Irvin Winkler , Hans Gerd Berscheid
IPC分类号： C07D295/08 , A61K31/215 , A61K31/27 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/4427 , A61K31/47 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/66 , A61K38/00 , A61P31/12 , A61P37/00 , A61P43/00 , C07C317/44 , C07C323/52 , C07D207/16 , C07D213/40 , C07D215/48 , C07D235/14 , C07D277/04 , C07D401/12 , C07F9/53 , C07K5/02 , C07K7/02 , C07K5/00
CPC分类号： C07K7/02 , C07C317/44 , C07C323/52 , C07F9/5304 , C07K5/0207 , C07K5/021 , A61K38/00
摘要： The invention concerns prodrugs of enzyme inhibitors in which at least one OH-- group in the enzyme inhibitor has been converted into a derivative grouping of the formula III, IV or V: ##STR1## in which the groups R.sup.11 to R.sup.25 and s,l, m, o, q, and r are as defined in the description. Such prodrugs exhibit an improved solubility in water and improved pharmaco-kinetic characteristics.
摘要翻译： PCT No.PCT / EP94 / 00561 Sec。 371 1995年9月12日第 102（e）1995年9月12日PCT PCT 1994年2月25日PCT公布。公开号WO94 / 21604 日期1994年9月29日本发明涉及酶抑制剂的前药，其中酶抑制剂中的至少一个OH-基团已转化为式III，IV或V的衍生基团：（IMAGE）（III） IV）其中组R11至R25和s，l，m，o，q和r如说明书中所定义的（V）。这些前药在水中表现出改善的溶解性和改善的药物动力学特征。

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