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31. 发明授权

US4968717A Phenylacetonitriles which are substituted by basic groups, their preparation and drugs containing these substances 失效
标题翻译：由碱性基团取代的苯乙腈，其制剂和含有这些物质的药物
公开(公告)号：US4968717A
公开(公告)日：1990-11-06
申请号：US351036
申请日：1989-05-12
申请人： Liliane Unger , Manfred Raschack , Verena Baldinger , Ferdinand Dengel , Oskar Ehrmann , Hans J. Treiber , Werner Seitz
发明人： Liliane Unger , Manfred Raschack , Verena Baldinger , Ferdinand Dengel , Oskar Ehrmann , Hans J. Treiber , Werner Seitz
IPC分类号： A61K31/275 , A61K31/335 , A61K31/357 , A61P7/02 , A61P9/00 , A61P9/12 , A61P43/00 , C07C67/00 , C07C253/00 , C07C255/32 , C07C255/42 , C07C255/43 , C07C255/53 , C07C255/58 , C07D317/58 , C07D319/08 , C07D319/18 , C07D321/12 , C07D325/00
CPC分类号： C07D319/08 , C07C255/00 , C07D317/58 , C07D319/18
摘要： Compounds of the formula ##STR1## where R.sup.1 to R.sup.7, m, n and p have the meanings stated in the description, and certain derivatives which are p-substituted in the left-hand phenyl ring, are useful for the treatment of disorders.
摘要翻译：其中R 1至R 7，m，n和p具有说明书中所述的含义，以及在左侧苯环中被取代的某些衍生物可用于治疗疾病。

32. 发明授权

US5342839A 2-hydroxy-3-phenoxy-propyl-substituted piperazines, their preparation and use 失效
标题翻译： 2-羟基-3-苯氧基 - 丙基取代的哌嗪，其制备和用途
公开(公告)号：US5342839A
公开(公告)日：1994-08-30
申请号：US659365
申请日：1991-03-18
申请人： Hans-Joerg Treiber , Hans P. Hofmann , Laszlo Szabo , Liliane Unger , Manfred Raschack
发明人： Hans-Joerg Treiber , Hans P. Hofmann , Laszlo Szabo , Liliane Unger , Manfred Raschack
IPC分类号： C07D243/08 , A61K31/495 , A61K31/55 , A61P9/00 , A61P9/08 , A61P9/10 , C07D295/08 , C07D295/092 , C07D295/088
CPC分类号： C07D295/088
摘要： 2-Hydroxy-3-phenoxy-propyl-substituted piperazines of the formula I ##STR1## in which R.sup.1 -R.sup.5, Y, m and n have the meaning indicated in the description, and the preparation thereof are described. The novel compounds are suitable for the therapy of oxygen deficiency diseases of the brain.
摘要翻译： PCT No.PCT / EP89 / 01058 Sec。 371日期1991年3月18日 102（e）1991年3月18日PCT PCT 1989年9月12日PCT公布。公开号WO90 / 03371 日期：1990年4月5日，其中R1-R5，Y，m和n具有说明书中指出的含义及其制备的式I的2-羟基-3-苯氧基 - 丙基取代的哌嗪。该新型化合物适用于治疗脑缺氧症。

33. 发明授权

US4940780A Basically substituted phenylacetonitriles, their preparation and drugs containing these compounds 失效
标题翻译：基本取代的苯乙腈，其制备方法和含有这些化合物的药物
公开(公告)号：US4940780A
公开(公告)日：1990-07-10
申请号：US130954
申请日：1987-12-10
申请人： Werner Seitz , Liliane Unger , Manfred Raschack , Verena Baldinger , Klaus Ruebsmen , Josef Gries
发明人： Werner Seitz , Liliane Unger , Manfred Raschack , Verena Baldinger , Klaus Ruebsmen , Josef Gries
IPC分类号： A61K31/275 , A61K31/335 , A61K31/357 , A61K31/36 , A61P1/04 , A61P3/00 , A61P9/00 , A61P11/00 , A61P43/00 , C07C67/00 , C07C253/00 , C07C253/30 , C07C255/32 , C07C255/35 , C07C255/42 , C07C255/53 , C07C255/58 , C07D317/50 , C07D317/60 , C07D319/08 , C07D319/18 , C07D321/00
CPC分类号： C07C255/00 , C07D317/60 , C07D319/08
摘要： Basically substituted phenylacetonitriles ##STR1## where R.sup.1 to R.sup.6 and n have the meanings stated in the description, and their preparation are described. The compounds are useful for the treatment of disorders.
摘要翻译：基本取代的苯基乙腈其中R1至R6和n具有说明书中所述的含义，并描述其制备方法。该化合物可用于治疗疾病。

34. 发明授权

US08008488B2 Pyrimidin-2-one compounds and their use as dopamine D3 receptor ligands 有权
标题翻译：嘧啶-2-酮化合物及其作为多巴胺D3受体配体的用途
公开(公告)号：US08008488B2
公开(公告)日：2011-08-30
申请号：US10548931
申请日：2004-03-12
申请人： Hervé Geneste , Andreas Kling , Wilfried Braje , Andreas Haupt , Liliane Unger
发明人： Hervé Geneste , Andreas Kling , Wilfried Braje , Andreas Haupt , Liliane Unger
IPC分类号： C07D403/06 , C07D403/14 , C07D401/06 , C07D401/14 , A61K31/505 , A61K31/506 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/22 , A61P25/30
CPC分类号： C07D239/36 , C07D239/52 , C07D239/54 , C07D239/553 , C07D239/56 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C═CH, C═CH—CH2 or CH—CH═CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a pharmaceutical agent for treating diseases which respond to the influence of dopamine D3 receptor ligands.
摘要翻译：除了（I）的衍生物和互变异构体以及所述化合物的生理学上可接受的盐之外，本发明涉及通式（I）的嘧啶-2-酮化合物。在所述式中，A表示可以具有双键或三键的直链或支链C 3 -C 6烯基和/或不与嘧啶酮环的氮原子相邻并且选自O，S， C（O），NR 3，C（O）NR 3，NR 3 C（O），OC（O）和C（O）O; B表示式（II）的基团，其中X表示CH2或N，Y表示CH2或CH2CH2，或X-Y也可共同表示C = CH，C = CH-CH 2或CH-CH = CH ; R1和R2定义为在说明书和权利要求书中引用的; 并且Ar表示任选取代的芳族基团。本发明还涉及含有至少一种化合物（I）和所述化合物的互变异构体，衍生物和/或酸加成盐，任选地与生理上可接受的载体和/或辅助剂一起的药剂。本发明还涉及式（I）化合物及其互变异构体，衍生物和药理学上可接受的酸加成盐的用途，用于制备用于治疗对多巴胺D3受体配体的影响作出反应的疾病的药剂。

35. 发明授权

US09006276B2 Substituted oxindole derivatives, medicaments containing said derivatives and use thereof 有权
标题翻译：取代的羟吲哚衍生物，含有所述衍生物的药物及其用途
公开(公告)号：US09006276B2
公开(公告)日：2015-04-14
申请号：US13243166
申请日：2011-09-23
申请人： Thorsten Oost , Wilfried Lubisch , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Herve Geneste , Astrid Netz
发明人： Thorsten Oost , Wilfried Lubisch , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Herve Geneste , Astrid Netz
IPC分类号： C07D417/14 , C07D417/12 , C07D413/14 , C07D413/12 , C07D401/14 , C07D401/12 , A61K31/551 , A61K31/5377 , A61K31/496 , A61K31/4525 , A61K31/454 , A61K31/4439 , A61K31/427 , A61K31/422
CPC分类号： C07D413/14 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/4525 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
摘要翻译：本发明涉及通式（I）的新型羟基吲哚衍生物，其中取代基R 1，R 2，A，B和Y如权利要求1中所定义。本发明还涉及含有所述衍生物的药物及其用于预防和/或加压素依赖性疾病的治疗。

36. 发明授权

US08969552B2 Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译：芳基磺酰基甲基或芳基磺酰胺取代的芳族化合物，适用于治疗对多巴胺D3受体调节作用的疾病
公开(公告)号：US08969552B2
公开(公告)日：2015-03-03
申请号：US11665428
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry
IPC分类号： C07C311/44 , C07D207/10 , C07D211/10 , C07D215/38 , C07D263/32 , C07D413/04 , C07C311/21 , C07C311/29 , C07D239/84 , C07D277/82 , C07D311/04 , C07D491/04
CPC分类号： C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2602/10 , C07D207/10 , C07D211/10 , C07D215/38 , C07D239/84 , C07D263/32 , C07D277/82 , C07D311/04 , C07D413/04 , C07D491/04
摘要： The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH═N—, —CH═CH— or —N═CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
摘要翻译：本发明涉及式I的芳族化合物，其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基团，其中Ar可以带有1个基团R a，并且其中Ar也可以带有1个或2个基团Rb; X为N或CH; Y是O，S，-CH = N - ， - CH = CH-或-N = CH-; A是CH 2，O或S; E为CR6R7或NR3; R 1是C 1 -C 4烷基，C 3 -C 4环烷基，C 3 -C 4环烷基甲基，C 3 -C 4链烯基，氟化C 1 -C 4烷基，氟化C 3 -C 4环烷基，氟化C 3 -C 4环烷基甲基， C4-烯基，甲酰基或C1-C3-烷基羰基; R1a为H，C2-C4-烷基，C3-C4-环烷基，C3-C4-烯基，氟化C1-C4-烷基，氟化C3-C4-环烷基或R1a和R2一起为（CH2）n，n为2 或3，或R 1a和R 2a一起为（CH 2）n，其中n为2或3; R2和R2a彼此独立地为H，CH3，CH2F，CHF2或CF3; R3是H或C1-C4-烷基; R6，R7彼此独立地选自H，C1-C2-烷基和氟化C1-C2-烷基; 及其生理上耐受的酸加成盐。本发明还涉及式I化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。

37. 发明授权

US08703775B2 Amidomethyl-substituted oxindole derivatives and the use thereof for the treatment of vasopressin-dependent illnesses 有权
标题翻译：酰胺甲基取代的羟基吲哚衍生物及其用于治疗加压素依赖性疾病的用途
公开(公告)号：US08703775B2
公开(公告)日：2014-04-22
申请号：US12746700
申请日：2008-12-05
申请人： Thorsten Oost , Astrid Netz , Herve Geneste , Wilfried Braje , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch , Andrea Hager-Wernet
发明人： Thorsten Oost , Astrid Netz , Herve Geneste , Wilfried Braje , Wolfgang Wernet , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch
IPC分类号： A61K31/496 , A61K31/4545 , C07D401/14
CPC分类号： C07D401/14
摘要： The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.
摘要翻译：本发明涉及新的酰胺甲基取代的羟基吲哚衍生物，包含它们的药物组合物及其用于治疗加压素依赖性病症的用途。

38. 发明授权

US08546401B2 5,6-disubstituted oxindole-derivatives and use thereof for treating vasopressin-dependent diseases 有权
标题翻译： 5,6-二取代羟吲哚衍生物及其用于治疗加压素依赖性疾病的用途
公开(公告)号：US08546401B2
公开(公告)日：2013-10-01
申请号：US12746715
申请日：2008-12-05
申请人： Wilfried Braje , Thorsten Oost , Astrid Netz , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch , Andrea Hager-Wernet
发明人： Wilfried Braje , Thorsten Oost , Astrid Netz , Wolfgang Wernet , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch
IPC分类号： A61K31/497 , A61K31/445 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00
CPC分类号： C07D401/14
摘要： The present invention relates to novel 5,6-disubstituted oxindole derivatives and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising such derivatives, and to the use of such derivatives for the manufacture of a medicament, and methods of treating disorders in a subject in need thereof, such as vasopressin-dependent disorders, using 5,6-disubstituted oxindole derivatives.
摘要翻译：本发明涉及新的5,6-二取代羟吲哚衍生物及其药学上可接受的盐，以及包含这些衍生物的药物组合物，以及这些衍生物在制备药物中的用途，以及在需要治疗的受试者中治疗疾病的方法如使用5,6-二取代的羟吲哚衍生物的血管加压素依赖性疾病。

39. 发明申请

US20130029966A1 SUBSTITUTED OXINDOLE DERIVATIVES, MEDICAMENTS CONTAINING SAID DERIVATIVES AND USE THEREOF 有权
公开(公告)号：US20130029966A1
公开(公告)日：2013-01-31
申请号：US13243166
申请日：2011-09-23
申请人： Thorsten Oost , Wilfried Lubisch , Wilfried Hornberger , Liliane Unger , Herve Geneste , Astrid Netz
发明人： Thorsten Oost , Wilfried Lubisch , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Herve Geneste , Astrid Netz
IPC分类号： A61K31/496 , A61K31/454 , A61K31/5377 , A61K31/551 , C07D413/14 , C07D413/12 , A61K31/427 , C07D417/14 , A61K31/4439 , C07D401/14 , A61P3/10 , A61P13/02 , A61P7/02 , A61P9/00 , A61P9/10 , A61P13/12 , A61P1/00 , A61P1/16 , A61P1/04 , A61P1/08 , A61P25/28 , A61P25/24 , A61P25/30 , A61K31/422
CPC分类号： C07D413/14 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/4525 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/551 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.

40. 发明授权

US08362010B2 Benzenesulfonanilide compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor 有权
标题翻译：苯磺酰苯胺化合物适用于治疗对血清素5-HT6受体调节作用的疾病
公开(公告)号：US08362010B2
公开(公告)日：2013-01-29
申请号：US12769878
申请日：2010-04-29
申请人： Andreas Haupt , Frauke Pohlki , Karla Drescher , Karsten Wicke , Liliane Unger , Ana-Lucia Relo , Anton Bespalov , Barbara Vogg , Gisela Backfisch , Juergen Delzer , Min Zhang
发明人： Andreas Haupt , Frauke Pohlki , Karla Drescher , Karsten Wicke , Liliane Unger , Ana-Lucia Relo , Anton Bespalov , Barbara Vogg , Gisela Backfisch , Juergen Delzer , Min Zhang
IPC分类号： A61P3/04 , A61P25/18 , A61K31/551 , C07D243/08
CPC分类号： C07D243/08 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl; R2 is hydrogen or methyl and is positioned vicinal to the radical R1; R3 hydrogen, C1-C3 alkyl, halogen, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R4 is hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, C3-C4 cycloalkylmethyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, chlorine, C1-C4 alkyl, fluorinated C1-C4 alkyl, C1-C4 alkoxy or fluorinated C1-C4 alkoxy; and R6 is hydrogen, fluorine or chlorine.
摘要翻译：本发明涉及式I和I'的新型苯磺酰苯胺化合物和生理上耐受的酸加成盐及其N-氧化物。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT 6受体调节作出反应的疾病。其中R1是氢或甲基; R2是氢或甲基，并且位于基团R1的邻近位置; R3氢，C1-C3烷基，卤素，C1-C3烷氧基，氟化C1-C3烷基或氟化C1-C3烷氧基; R4是氢，C1-C4烷基，C3-C4环烷基，C3-C4环烷基甲基或氟化C1-C4烷基; R5是氢，氟，氯，C1-C4烷基，氟化C1-C4烷基，C1-C4烷氧基或氟化C1-C4烷氧基; R6是氢，氟或氯。

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