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1. 发明授权

US06509493B1 Method for producing atropic acid ethyl ester 有权
标题翻译：生产阿托酸乙酯的方法
公开(公告)号：US06509493B1
公开(公告)日：2003-01-21
申请号：US09743894
申请日：2001-01-17
申请人： Wolfgang Falkenberg , Marco Thyes , Conny Wenz , Ulrich Schneider
发明人： Wolfgang Falkenberg , Marco Thyes , Conny Wenz , Ulrich Schneider
IPC分类号： C07C6976
CPC分类号： C07C67/343 , C07C69/618
摘要： A process for preparing ethyl atropate by reacting ethyl phenylacetate with paraformaldehyde in the presence of a base is described and entails employing as ethyl phenylacetate a product which contains not more than 0.03% of the corresponding methyl phenylacetate, and carrying out the reaction in N-methyl-pyrrolidone or N,N-dimethylformamide.
摘要翻译：描述了通过在碱存在下使苯乙酸乙酯与多聚甲醛反应来制备乙酸乙酯的方法，并且需要使用苯乙酸乙酯作为相应的苯基乙酸苯酯不超过0.03％的产物，并在N-甲基 - 吡咯烷酮或N，N-二甲基甲酰胺。

2. 发明授权

US07273947B1 Method for reducing 3-dimethylamnio-2-phenylpropion-acid ethyl ester-content in solutions of 2-dimethylamino-1-phenyl-3-cyclohexene-1-carboxylic acid ethyl ester 失效
标题翻译： 2-二甲基氨基-1-苯基-3-环己烯-1-羧酸乙酯溶液中3-二甲基亚氨基-2-苯基丙酸乙酯含量的降低方法
公开(公告)号：US07273947B1
公开(公告)日：2007-09-25
申请号：US09889383
申请日：2000-01-15
申请人： Marco Thyes , Wolfgang Falkenberg , Ulrich Schneider
发明人： Marco Thyes , Wolfgang Falkenberg , Ulrich Schneider
IPC分类号： C07C229/00
CPC分类号： C07C227/40 , C07C2601/16 , C07C229/48
摘要： A process for reducing the content of ethyl 3-dimethylamino-2-phenylpropionate in a solution, contaminated therewith, of ethyl 2-dimethylamino-1-phenyl-3-cyclohexene-1-carboxylate in a water-immiscible solvent, which comprises adding from 0.5 to 2.0 equivalents of a carboxylic acid per mole of ethyl 2-dimethylamino-1-phenyl-3-cyclohexene-1-carboxylate to this solution, and stirring this mixture at a temperature of from 50° C. to 100° C., is described.
摘要翻译：在与水不混溶的溶剂中的2-二甲基氨基-1-苯基-3-环己烯-1-羧酸乙酯的溶液中降低3-二甲基氨基-2-苯基丙酸乙酯的含量的方法，该方法包括从将0.5-2.0当量羧酸/摩尔2-二甲基氨基-1-苯基-3-环己烯-1-羧酸乙酯加入到该溶液中，并在50℃至100℃的温度下搅拌该混合物，被描述。

3. 发明授权

US4937308A Preparation of alkyl O,O-dialkyl-.gamma.-phosphonotiglates 失效
标题翻译：烷基O，O-二烷基-γ-膦酸吡啶的制备
公开(公告)号：US4937308A
公开(公告)日：1990-06-26
申请号：US205283
申请日：1988-06-10
申请人： Guenter H. Knaus , Hansgeorg Ernst , Marco Thyes , Joachim Paust
发明人： Guenter H. Knaus , Hansgeorg Ernst , Marco Thyes , Joachim Paust
IPC分类号： C07F9/40
CPC分类号： C07F9/4015
摘要： Alkyl .gamma.-halotiglates of the general formula I ##STR1## where X is Cl or Br and R.sup.2 is alkyl of 1 to 3 carbon atoms, having a high E isomer content, are prepared by a process in which(a) the corresponding 2-methyl-but-3-enoate of the general formula II ##STR2## is reacted with chlorine or bromine in the absence of a solvent and (b) the resulting 2-methyl-3,4-dihalobutyrate of the general formula III ##STR3## is dehydrohalogenated by reaction with a solution of an alkali metal hydroxide in an alcohol R.sup.2 OH, where R.sup.2 has the stated meaning, or in a mixture of water and an alcohol R.sup.2 OH, and the products are further processed to give O,O-dialkyl-.gamma.-phosphonotiglates of the general formula IV ##STR4## where R.sup.1 is alkyl of 1 to 4 carbon atoms and R.sup.2 is alkyl of 1 to 3 carbon atoms, preferably ethyl, by reaction with a trialkyl phosphite and thermal isomerization. The process gives C.sub.5 building blocks which are extremely interesting for polyene chemistry, the said building blocks being obtained in good yields and essentially in the form of the required E isomers.
摘要翻译：通过以下方法制备通式I的烷基γ-卤代吡咯烷酮，其中X是Cl或Br，R2是具有高E异构体含量的1至3个碳原子的烷基，其中（a）在不存在溶剂的情况下，使通式II（II）的相应的2-甲基 - 丁-3-烯酸酯与氯或溴反应，和（b）所得的2-甲基-3,4-二卤代丁酸酯通过与碱金属氢氧化物在醇R2OH中的溶液（其中R2具有所述含义）或在水和醇R2OH的混合物中进行反应脱卤化氢，并将产物进一步加工得到通式IV（IV）的O，O-二烷基-γ-膦腈吡咯烷酮，其中R 1为1至4个碳原子的烷基，R 2为1至3个碳原子的烷基，优选为乙基，通过与亚磷酸三烷基酯和热异构化。该方法提供了对多烯化学非常有趣的C5构建块，所述构建块以良好的产率获得并且基本上以所需的E异构体的形式获得。

4. 发明授权

US4772598A 2-aryl-3,4-diazabicyclo(4.n.O)alk-2-en-5-ones for the preparation of an agent for treating cardiac insufficiency 失效
标题翻译： 2-芳基-3,4-二氮杂双环（4.n.O）烷-2-烯-5-酮用于制备治疗心功能不全的药物
公开(公告)号：US4772598A
公开(公告)日：1988-09-20
申请号：US914729
申请日：1986-10-01
申请人： Karl-Heinz Geiss , Phillip A. Rossy , Marco Thyes , Horst Koenig , Hans D. Lehmann , Martin Traut , Josef Gries
发明人： Karl-Heinz Geiss , Phillip A. Rossy , Marco Thyes , Horst Koenig , Hans D. Lehmann , Martin Traut , Josef Gries
IPC分类号： C07D401/04 , A61K31/50 , A61K31/55 , A61P3/02 , A61P9/04 , A61P9/08 , A61P9/10 , C07D209/34 , C07D215/22 , C07D223/16 , C07D237/00 , C07D403/04 , C12N9/99 , A61K31/495
CPC分类号： A61K31/55 , A61K31/50
摘要： 2-aryl-3,4-diazabicyclo[4.n.0]-alk-2-en-5-ones of the formula ##STR1## where m, n, R, R.sup.1, R.sup.2 and R.sup.3 have the stated meanings, are used for the treatment of cardiac insufficiency.
摘要翻译：其中m，n，R，R 1，R 2和R 3具有所述含义，其中m，n，R 1，R 2，R 3，R 3，R 3，用于治疗心功能不全。

5. 发明授权

US07030247B2 Method for the production of biperidin 失效
标题翻译：生产丁吡啶的方法
公开(公告)号：US07030247B2
公开(公告)日：2006-04-18
申请号：US10477761
申请日：2002-05-17
申请人： Peter Klein , Marco Thyes , Markus Grosse , Klaus Martin Weber
发明人： Peter Klein , Marco Thyes , Markus Grosse , Klaus Martin Weber
IPC分类号： C07D211/06
CPC分类号： C07D295/088 , C07D295/108
摘要： The invention relates to a method for the production of biperiden by reacting an exo/endo mixture of 1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-3-piperidino-1-propanone with a phenyl magnesium compound to form an isomer mixture of 1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-piperidino-1-propanol, whereby biperiden is obtained therefrom by conversion of said mixture into corresponding hydrochloride, isolation of said hydrochloride, reconversion to the free base and crystallization of said biperiden.
摘要翻译：本发明涉及一种通过使1-（双环[2.2.1]庚-5-烯-2-基）-3-哌啶子基-1-丙酮的外部/内部混合物与苯基镁化合物形成1-（双环[2.2.1]庚-5-烯-2-基）-1-苯基-3-哌啶-1-基-1-异丙醇的异构体混合物，由此通过转化得到二哌啶的所述混合物转化成相应的盐酸盐，分离所述盐酸盐，重新转化为游离碱并结晶所述双倍哌啶。

6. 发明授权

US4873246A 6-(acylaminoaryl)-3(2H)-pyridazinone derivatives, and their use 失效
标题翻译： 6-（酰基氨基芳基）-3（2H） - 哒嗪酮衍生物及其用途
公开(公告)号：US4873246A
公开(公告)日：1989-10-10
申请号：US916843
申请日：1986-10-08
申请人： Philip A. Rossy , Marco Thyes , Albrecht Franke , Horst Koenig , Hans D. Lehmann , Josef Gries , Ludwig Friedrich , Dieter Lenke
发明人： Philip A. Rossy , Marco Thyes , Albrecht Franke , Horst Koenig , Hans D. Lehmann , Josef Gries , Ludwig Friedrich , Dieter Lenke
IPC分类号： A61K31/50 , A61K31/502 , A61K31/535 , A61K31/55 , A61P1/04 , A61P7/02 , A61P9/12 , C07D237/04 , C07D237/14 , C07D237/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D237/04 , C07D237/14 , C07D237/26 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Novel 6-(acylaminaryl)-3(2H)-pyridazinones of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and B have the meanings given in the description, and their preparation are described.The compounds have thrombocyte aggregation-inhibiting activity.
摘要翻译：其中R 1，R 2，R 3，R 4，A和B具有本说明书中给出的含义的新颖的6-（酰基氨基芳基）-3（2H） - 哒嗪酮及其制备。该化合物具有血细胞聚集抑制活性。

7. 发明授权

US4857658A Preparation of (Z)-2-(2-arylethenyl)arylcarboxylic acids 失效
标题翻译：（Z）-2-（2-芳基乙烯基）芳基羧酸的制备
公开(公告)号：US4857658A
公开(公告)日：1989-08-15
申请号：US134108
申请日：1987-12-17
申请人： Marco Thyes , Gerd Steiner
发明人： Marco Thyes , Gerd Steiner
IPC分类号： C07C63/331 , C07C51/00 , C07C51/353 , C07C63/66 , C07C63/74 , C07C65/28 , C07C67/00 , C07C201/00 , C07C205/06 , C07C205/56 , C07C253/00 , C07C255/50 , C07C255/57
CPC分类号： C07C51/353
摘要： (Z)-2-(2-arylethenyl)arylcarboxylic acids of the general formula I ##STR1## where A is a group for completing an aromatic ring system and Ar is an aromatic radical, are prepared by reacting a 2-formylarylcarboxylic acid of the general formula II ##STR2## with an (arylmethyl)phosphonium salt of the general formula III ##STR3## where R.sup.1, R.sup.2 and R.sup.3 are each organic radicals and X is halogen, in the presence of a base at from (-20.degree.) to +30.degree. C. by carrying out the reaction in the presence of a C.sub.1 -C.sub.5 -alkanol and/or a C.sub.2 -C.sub.4 -alkanediol.
摘要翻译：（I）的（Z）-2-（2-芳基乙烯基）芳基羧酸，其中A是用于完成芳族环系统的基团，Ar是芳族基团，其通过使2-甲酰基芳基羧酸通式II（II）的酸与通式III（III）的（芳基甲基）鏻盐反应，其中R 1，R 2和R 3各自为有机基团，X为卤素，在通过在C1-C5链烷醇和/或C 2 -C 4 - 链烷二醇的存在下进行反应，从（-20℃）至+ 30℃进行反应。

8. 发明授权

US4636504A 6-(acylaminoaryl)-3(2H)-pyridazinone derivatives and their use 失效
标题翻译： 6-（酰氨基芳基）-3（2H） - 哒嗪酮衍生物及其用途
公开(公告)号：US4636504A
公开(公告)日：1987-01-13
申请号：US571675
申请日：1984-01-17
申请人： Phillip A. Rossy , Marco Thyes , Albrecht Franke , Horst Koenig , Hans Dieter Lehmann , Josef Gries , Ludwig Friedrich , Dieter Lenke
发明人： Phillip A. Rossy , Marco Thyes , Albrecht Franke , Horst Koenig , Hans Dieter Lehmann , Josef Gries , Ludwig Friedrich , Dieter Lenke
IPC分类号： A61K31/50 , A61K31/502 , A61K31/535 , A61K31/55 , A61P1/04 , A61P7/02 , A61P9/12 , C07D237/04 , C07D237/14 , C07D237/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14 , C07D521/00 , C07D237/06
CPC分类号： C07D231/12 , C07D233/56 , C07D237/04 , C07D237/14 , C07D237/26 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Novel 6-(acylaminoaryl)-3(2H)-pyridazinones of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and B have the meanings given in the description, and their preparation are described and inhibiting thrombocyte aggregation and gastric secretion.The compounds are useful for treating disorders.
摘要翻译：式（Ⅰ）的新型6-（酰基氨基芳基）-3（2H） - 哒嗪酮其中R 1，R 2，R 3，R 4，A和B具有说明书中给出的含义及其制备，并描述并抑制血小板聚集和胃分泌。该化合物可用于治疗疾病。

9. 发明授权

US06486162B2 2-{3-[4-(2-t-butyl-6-trifluoromethyl-4-pyrimidinyl)-1- piperazinyl] propylthio}-4-pyrimidinol fumarate 有权
标题翻译： 2- {3- [4-（2-叔丁基-6-三氟甲基-4-嘧啶基）-1-哌嗪基]丙硫基} -4-嘧啶醇富马酸盐
公开(公告)号：US06486162B2
公开(公告)日：2002-11-26
申请号：US10039974
申请日：2002-01-08
申请人： Thomas Höger , Dorothea Starck , Hans-Jorg Treiber , Stefan Koser , Bernd Schaefer , Marco Thyes , Stefan Blank
发明人： Thomas Höger , Dorothea Starck , Hans-Jorg Treiber , Stefan Koser , Bernd Schaefer , Marco Thyes , Stefan Blank
IPC分类号： A61K31506
CPC分类号： C07D239/42
摘要： The fumaric acid salt of 2-{3-[4-(2-t-butyl-6-trifluoromethyl-4-pyrimidinyl)-1-piperazinyl]propylthio}-4-pyrimidinol is useful for treating disorders which respond to dopamine D3 ligands. It has higher stability at low pH and is therefore particularly suitable for oral administration in pharmaceutical compositions comprising this salt.
摘要翻译： 2- {3- [4-（2-叔丁基-6-三氟甲基-4-嘧啶基）-1-哌嗪基]丙硫基} -4-嘧啶醇的富马酸盐可用于治疗对多巴胺D3配体。它在低pH下具有较高的稳定性，因此特别适用于包含该盐的药物组合物中的口服给药。

10. 再颁专利

USRE33476E 6-(alkanolaminoaryl)-3(2H)-pyridazinone derivatives, and their use 失效
标题翻译： 6-（链烷醇氨基芳基）-3（2H） - 哒嗪酮衍生物及其用途
公开(公告)号：USRE33476E
公开(公告)日：1990-12-04
申请号：US189136
申请日：1988-05-02
申请人： Phillip A. Rossy , Marco Thyes , Albrecht Franke , Horst Koenig , Hans D. Lehmann , Josef Gries , Ludwig Friedrich , Dieter Lenke
发明人： Phillip A. Rossy , Marco Thyes , Albrecht Franke , Horst Koenig , Hans D. Lehmann , Josef Gries , Ludwig Friedrich , Dieter Lenke
IPC分类号： A61K31/50 , A61K31/502 , A61K31/535 , A61K31/55 , A61P1/04 , A61P7/02 , A61P9/12 , C07D237/04 , C07D237/14 , C07D237/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D237/04 , C07D237/14 , C07D237/26 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Novel 6-(acylaminoaryl)-3(2H)-pyridazinones of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and B have the meanings given in the description, and their preparation are described.[.and inhibiting thrombocyte aggregation and gastric secretion.]..The compounds are useful for treating disorders .Iadd.and inhibiting thrombocyte aggregation and gastric secretion.Iaddend..

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