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1. 发明授权

US09938269B2 Inhibitor compounds of phosphodiesterase type 10A 有权
公开(公告)号：US09938269B2
公开(公告)日：2018-04-10
申请号：US13534127
申请日：2012-06-27
申请人： Hervé Geneste , Michael Ochse , Karla Drescher , Berthold Behl , Loic Laplanche , Jürgen Dinges , Clarissa Jakob , Katja Jantos
发明人： Hervé Geneste , Michael Ochse , Karla Drescher , Berthold Behl , Loic Laplanche , Jürgen Dinges , Clarissa Jakob , Katja Jantos
IPC分类号： C07D471/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
CPC分类号： C07D471/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

2. 发明申请

US20130005705A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20130005705A1
公开(公告)日：2013-01-03
申请号：US13534127
申请日：2012-06-27
申请人： Hervé Geneste , Michael Ochse , Karla Drescher , Berthold Behl , Loic Laplanche , Jürgen Dinges , Clarissa Jakob
发明人： Hervé Geneste , Michael Ochse , Karla Drescher , Berthold Behl , Loic Laplanche , Jürgen Dinges , Clarissa Jakob
IPC分类号： A61K31/4709 , C07D401/14 , A61K31/517 , C07D413/14 , C07D495/04 , A61K31/444 , C07D405/14 , A61K31/506 , A61K31/5377 , A61K31/496 , C07D417/14 , A61K31/541 , C07D491/107 , A61K31/501 , A61P25/28 , A61P3/04 , A61P25/16 , A61P25/22 , A61P25/00 , A61P25/18 , C07D471/04
CPC分类号： C07D471/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
摘要翻译：本发明涉及新的羧酰胺化合物，含有它们的药物组合物及其在治疗中的用途。所述化合物具有有价值的治疗性质，并且特别适用于治疗或控制选自神经障碍和精神障碍的医学病症，用于改善与此类疾病相关的症状并降低此类疾病的风险。

3. 发明授权

US08664214B2 Small molecule potentiators of metabotropic glutamate receptors I 有权
标题翻译：代谢型谷氨酸受体的小分子增效剂I
公开(公告)号：US08664214B2
公开(公告)日：2014-03-04
申请号：US13071753
申请日：2011-03-25
申请人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker , Jayne Froggett
发明人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker , Jayne Froggett
IPC分类号： C07D231/12 , C07D409/04 , A61K31/4164
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I and variables defined herein.
摘要翻译：本发明涉及代谢型受体特别是mGlu2受体的小分子增效剂。本发明还涉及这些化合物用于预防或治疗与谷氨酸功能障碍相关的神经和精神疾病以及涉及代谢型谷氨酸受体的疾病的用途。因此，本发明提供式I化合物和本文定义的变量。

4. 发明授权

US08314120B2 Small molecule potentiators of metabotropic glutamate receptors 有权
公开(公告)号：US08314120B2
公开(公告)日：2012-11-20
申请号：US13073087
申请日：2011-03-28
申请人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker
发明人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker
IPC分类号： A61K31/4375 , A61K31/4725 , A61K31/403 , C07D471/04 , C07D217/22 , C07D487/04 , C07D209/46
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14
摘要： The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I wherein X1 is N or C—R1, X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X1, X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is Y1, Y2, N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2 has one of the meanings given for R1; R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2; and the N-oxides and the pharmaceutically acceptable salts thereof.

5. 发明申请

US20110245232A1 NOVEL SMALL MOLECULE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS I 有权
公开(公告)号：US20110245232A1
公开(公告)日：2011-10-06
申请号：US13071753
申请日：2011-03-25
申请人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker , Jayne Froggett
发明人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker , Jayne Froggett
IPC分类号： A61K31/553 , C07D401/12 , A61K31/4439 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/496 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/08 , A61P25/06
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I wherein X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2, R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2, Rb is hydrogen, halogen or C1-C4-alkyl; and the N-oxides and the pharmaceutically acceptable salts thereof.

6. 发明申请

US20110245247A1 NOVEL SMALL MOLECULE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS 有权
公开(公告)号：US20110245247A1
公开(公告)日：2011-10-06
申请号：US13073087
申请日：2011-03-28
申请人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker
发明人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker
IPC分类号： A61K31/5377 , C07D401/12 , C07D401/14 , C07D413/14 , C07D403/12 , A61K31/4439 , A61K31/496 , A61K31/4725 , A61K31/497 , A61K31/4709 , A61K31/498 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/08 , A61P25/06
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14
摘要： The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I wherein X1 is N or C—R1, X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X1, X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is Y1, Y2, N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2 has one of the meanings given for R1; R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2; and the N-oxides and the pharmaceutically acceptable salts thereof.

7. 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。

8. 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.

9. 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。

10. 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。

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