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1. 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。

2. 发明授权

US08492540B2 1,2,4,-triazin-3,5-dione compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译： 1,2,4-三嗪-3,5-二酮化合物，适用于治疗对多巴胺D3受体调节作用的疾病
公开(公告)号：US08492540B2
公开(公告)日：2013-07-23
申请号：US12740714
申请日：2008-10-31
申请人： Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Hervé Geneste , Karla Drescher , Liliane Unger , Ana Lucia Relo , Anton Bespalov
发明人： Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Hervé Geneste , Karla Drescher , Liliane Unger , Ana Lucia Relo , Anton Bespalov
IPC分类号： C07D253/075 , C07D403/14 , A61K31/53 , A61P25/18 , A61P25/30 , A61P25/00
CPC分类号： C07D403/12
摘要： The invention relates to compounds of the formula I: wherein A is a saturated or unsaturated hydrocarbon chain having a chain length of 4 to 6 carbon atoms, the hydrocarbon chain being unsubstituted or substituted by 1, 2 or 3 methyl groups; R1 is selected from the group consisting of hydrogen, C1-C3 alkyl and fluorinated C1-C3 alkyl; R2 is hydrogen, halogen, cyano, C1-C3 alkyl, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R3 is selected from the group consisting of branched C4-C6 alkyl and C3-C6 cycloalkyl, and R4 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C3-alkyl and fluorinated C3-C6 cycloalkyl. and the physiologically tolerated salts of these compounds and the N-oxides thereof. The invention also relates to a pharmaceutical composition that comprises at least one compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.
摘要翻译：本发明涉及式I化合物：其中A是链长为4-6个碳原子的饱和或不饱和烃链，烃链未被取代或被1,2或3个甲基取代; R1选自氢，C1-C3烷基和氟化C1-C3烷基; R2是氢，卤素，氰基，C1-C3烷基，C1-C3烷氧基，氟化C1-C3烷基或氟化C1-C3烷氧基; R3选自支链C4-C6烷基和C3-C6环烷基，R4为C1-C6烷基，C3-C6环烷基，氟化C1-C3-烷基和氟化C3-C6环烷基。以及这些化合物的生理上耐受的盐及其N-氧化物。本发明还涉及包含至少一种式I化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物，还涉及治疗有益于多巴胺D3受体拮抗剂或多巴胺D3的病症的方法所述方法包括向有需要的受试者施用有效量的至少一种式I化合物或生理学上耐受的酸加成盐。

3. 发明申请

US20110077253A1 AMIDOMETHYL-SUBSTITUTED OXINDOLE DERIVATIVES AND THE USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT ILLNESSES 有权
标题翻译：氨基取代的氧化衍生物及其用于治疗依赖于依赖性依赖性的药物的用途
公开(公告)号：US20110077253A1
公开(公告)日：2011-03-31
申请号：US12746700
申请日：2008-12-05
申请人： Thorsten Oost , Astrid Netz , Hervé Geneste , Wilfried Braje , Wolfgang Wernet , Andrea Hager-Wernet , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch
发明人： Thorsten Oost , Astrid Netz , Hervé Geneste , Wilfried Braje , Wolfgang Wernet , Andrea Hager-Wernet , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch
IPC分类号： A61K31/496 , C07D401/14 , A61K31/4545 , A61P25/00
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。

4. 发明申请

US20110065720A1 CARBAMATE-SUBSTITUTED OXINDOLE DERIVATIVES AND USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT DISEASES 有权
标题翻译：碳水化合物取代的氧化衍生物及其用于治疗依赖性依赖性疾病的用途
公开(公告)号：US20110065720A1
公开(公告)日：2011-03-17
申请号：US12746688
申请日：2008-12-05
申请人： Astrid Netz , Thorsten Oost , Hervé Geneste , Wilfried Braje , Wolfgang Wernet , Liliane Unger , Wilfried Homberger , Wilfried Lubisch
发明人： Astrid Netz , Thorsten Oost , Hervé Geneste , Wilfried Braje , Wolfgang Wernet , Liliane Unger , Wilfried Homberger , Wilfried Lubisch
IPC分类号： A61K31/496 , C07D401/14 , A61P11/00 , A61P13/12 , A61P3/00 , A61P1/08 , A61P25/22 , A61P25/18
CPC分类号： C07D401/14 , C07D401/04
摘要： The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.
摘要翻译：本发明涉及新的氨基甲酸酯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。

5. 发明授权

US08334289B2 Pyridin-2-one compounds and their use as modulators of the dopamine D3 receptor 失效
标题翻译：吡啶-2-酮化合物及其作为多巴胺D3受体调节剂的用途
公开(公告)号：US08334289B2
公开(公告)日：2012-12-18
申请号：US13103734
申请日：2011-05-09
申请人： Hervé Geneste , Wilfried Braje , Andreas Haupt
发明人： Hervé Geneste , Wilfried Braje , Andreas Haupt
IPC分类号： A61K31/506
CPC分类号： C07D401/12
摘要： The invention relates to novel pyridin-2-one compounds of general formula (I), in which A represents a 4- to 6-membered hydrocarbon chain that can have 1 or 2 methyl groups as substituents, wherein 1 or 2 carbon atoms can be replaced by oxygen, a carbonyl group or sulfur, and the hydrocarbon chain can have a double bond or a triple bond; R1, R2, R3 and R4 have the meanings as cited in the claims and in the description. The invention also relates to the tautomers of compounds I, the physiologically acceptable salts of compounds I, and to the physiologically acceptable salts of the tautomers of compounds I. The invention also relates to the use of compounds of general formula (I) and of the tautomers, and to the use of the physiologically acceptable salts of compounds I and of the tautomers for producing a pharmaceutical agent for treating diseases that respond to the influence of dopamine D3 receptor antagonists or agonists.
摘要翻译：本发明涉及通式（I）的新型吡啶-2-酮化合物，其中A表示可具有1或2个甲基作为取代基的4至6元烃链，其中1或2个碳原子可以是由氧，羰基或硫取代，烃链可以具有双键或三键; R1，R2，R3和R4具有权利要求书和说明书中引用的含义。本发明还涉及化合物I的互变异构体，化合物I的生理上可接受的盐，以及化合物I的互变异构体的生理上可接受的盐。本发明还涉及通式（I）的化合物和互变异构体，以及化合物I和互变异构体的生理上可接受的盐的用途，用于制备用于治疗对多巴胺D3受体拮抗剂或激动剂的影响作出反应的疾病的药剂。

6. 发明申请

US20110245266A1 PYRIDIN-2-ONE COMPOUNDS AND THEIR USE AS MODULATORS OF THE DOPAMINE D3 RECEPTOR 失效
标题翻译： PYRIDIN-2-ONE化合物及其作为DOPAMINE D3受体的调节剂
公开(公告)号：US20110245266A1
公开(公告)日：2011-10-06
申请号：US13103734
申请日：2011-05-09
申请人： Hervé Geneste , Wilfried Braje , Andreas Haupt
发明人： Hervé Geneste , Wilfried Braje , Andreas Haupt
IPC分类号： A61K31/497 , C07D403/14 , A61P25/18 , A61P25/24
CPC分类号： C07D401/12
摘要： The invention relates to novel pyridin-2-one compounds of general formula (I), in which A represents a 4- to 6-membered hydrocarbon chain that can have 1 or 2 methyl groups as substituents, wherein 1 or 2 carbon atoms can be replaced by oxygen, a carbonyl group or sulfur, and the hydrocarbon chain can have a double bond or a triple bond; R1, R2, R3 and R4 have the meanings as cited in the claims and in the description. The invention also relates to the tautomers of compounds I, the physiologically acceptable salts of compounds I, and to the physiologically acceptable salts of the tautomers of compounds I. The invention also relates to the use of compounds of general formula (I) and of the tautomers, and to the use of the physiologically acceptable salts of compounds I and of the tautomers for producing a pharmaceutical agent for treating diseases that respond to the influence of dopamine D3 receptor antagonists or agonists.
摘要翻译：本发明涉及通式（I）的新型吡啶-2-酮化合物，其中A表示可具有1或2个甲基作为取代基的4至6元烃链，其中1或2个碳原子可以是由氧，羰基或硫取代，烃链可以具有双键或三键; R1，R2，R3和R4具有权利要求书和说明书中引用的含义。本发明还涉及化合物I的互变异构体，化合物I的生理上可接受的盐，以及化合物I的互变异构体的生理上可接受的盐。本发明还涉及通式（I）的化合物和互变异构体，以及化合物I和互变异构体的生理上可接受的盐的用途，用于制备用于治疗对多巴胺D3受体拮抗剂或激动剂的影响作出反应的疾病的药剂。

7. 发明授权

US07465744B2 Triazole compounds and the therapeutic use thereof 失效
标题翻译：三唑化合物及其治疗用途
公开(公告)号：US07465744B2
公开(公告)日：2008-12-16
申请号：US10544550
申请日：2004-02-05
申请人： Dorothea Starck , Hans-Jörg Treiber , Thomas Zierke , Georg Kettschau , Hervé Geneste , Andreas Haupt , Liliane Unger , Kai Blumbach , Dietmar Schöbel , Hans-Jurgen Teschendorf
发明人： Dorothea Starck , Hans-Jörg Treiber , Thomas Zierke , Georg Kettschau , Hervé Geneste , Andreas Haupt , Liliane Unger , Kai Blumbach , Dietmar Schöbel , Hans-Jurgen Teschendorf
IPC分类号： A61K31/41 , C07D401/02
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The invention relates to triazole compounds of general formula (I), wherein A, B, R1, R2, R3 and R4 have the meaning cited in claim 1. The invention also relates to a pharmaceutical agent containing at least one compound of general formula (I) in addition to the use of the compound (I) for producing a pharmaceutical agent for treating illnesses, responding to the effects of dopamine-D3-receptor antagonists or dopamine-D3-receptor agonists, especially for treating disorders in the central nervous system.
摘要翻译：本发明涉及通式（I）的三唑化合物，其中A，B，R 1，R 2，R 3和R 4具有权利要求1中引用的含义。本发明还涉及含有至少一种通式（ I），除了使用化合物（I）制备用于治疗疾病的药剂之外，还应对多巴胺-D3受体拮抗剂或多巴胺-D 3受体激动剂的作用，特别是用于治疗中枢神经系统疾病。

8. 发明授权

US06919342B2 Triazole compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 失效
标题翻译：适用于治疗对多巴胺D3受体调节作出反应的三唑化合物
公开(公告)号：US06919342B2
公开(公告)日：2005-07-19
申请号：US10860823
申请日：2004-06-04
申请人： Andreas Haupt , Roland Grandel , Wilfried Braje , Hervé Geneste , Karla Drescher , Dorothea Starck , Hans-Jürgen Teschendorf
发明人： Andreas Haupt , Roland Grandel , Wilfried Braje , Hervé Geneste , Karla Drescher , Dorothea Starck , Hans-Jürgen Teschendorf
IPC分类号： A61K31/506 , C07D403/12 , C07D403/14
CPC分类号： C07D403/12
摘要： The invention relates to triazole compounds of the general formula I wherein R1 is hydrogen or methyl, and R2 is C3-C4 alkyl or C1-C2 fluoroalkyl, as well as the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.
摘要翻译：本发明涉及通式Ⅰ的三唑化合物，其中R 1是氢或甲基，R 2是C 3 -C 3 > 4个烷基或C 1 -C 2 - 氟代烷基，以及这些化合物的生理上耐受的酸加成盐。本发明还涉及一种药物组合物，其包含至少一种式I的三唑化合物和/或其至少一种生理上耐受的酸加成盐，还涉及治疗有益于多巴胺D 3的病症的方法受体拮抗剂或多巴胺D 3激动剂，所述方法包括向有需要的受试者施用有效量的至少一种式III的三唑化合物或生理耐受的酸加成盐。

9. 发明授权

US07320979B2 N-[(piperazinyl)hetaryl]arylsulfonamide compounds 失效
公开(公告)号：US07320979B2
公开(公告)日：2008-01-22
申请号：US10823317
申请日：2004-04-13
申请人： Wilfried M. Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Hervé Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
发明人： Wilfried M. Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Hervé Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
IPC分类号： A61K31/496 , A61K31/506 , C07D213/72 , C07D213/74 , C07D239/48
CPC分类号： C07D213/76 , C07D213/74 , C07D239/69 , C07D401/04 , C07D487/08
摘要： The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene; R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

10. 发明授权

US08129389B2 Substituted oxindole derivatives, medicaments containing the latter and use thereof 有权
标题翻译：取代的羟基吲哚衍生物，含有后者的药物及其用途
公开(公告)号：US08129389B2
公开(公告)日：2012-03-06
申请号：US11886729
申请日：2006-03-23
申请人： Wilfried Lubisch , Thorsten Oost , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Hervé Geneste
发明人： Wilfried Lubisch , Thorsten Oost , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Hervé Geneste
IPC分类号： A61K31/496 , A61K31/506 , C07D401/12 , C07D403/12 , C07D417/12
CPC分类号： C07D403/12 , C07D401/12 , C07D417/12
摘要： The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-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A，B，R 1，R 2和R 3如权利要求1中所定义，含有所述衍生物的药物及其用于预防的药物和/或加压素依赖性和/或催产素依赖性疾病的治疗。

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