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1. 发明授权

US08350055B2 Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them 有权
公开(公告)号：US08350055B2
公开(公告)日：2013-01-08
申请号：US12839612
申请日：2010-07-20
申请人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Andrea Hager-Wernet, legal representative , Liliane Unger , Wilfried Lubisch
发明人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Liliane Unger , Wilfried Lubisch
IPC分类号： C07D411/00
CPC分类号： C07D401/14 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.

2. 发明申请

US20110294817A1 N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR 失效
标题翻译：具有多巴胺D3受体亲和性的N- [哌嗪基]维生素A亚磺酰胺化合物
公开(公告)号：US20110294817A1
公开(公告)日：2011-12-01
申请号：US13117269
申请日：2011-05-27
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
IPC分类号： A61K31/496 , A61P13/12 , A61P25/00 , C07D401/04 , A61K31/4995
CPC分类号： C07D213/74 , C07D213/76 , C07D239/48 , C07D239/50 , C07D403/04 , C07D403/14 , C07D487/08
摘要： The invention related 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.
摘要翻译：本发明涉及通式（I）的N - [（哌嗪基）杂芳基]芳基磺酰胺化合物，其中Q是具有1或2个N原子作为环成员的二价，6元杂芳族基团，并且任选地带有一个或两个被卤素，CN，NO 2，CO 2 R 4，COR 5，C 1 -C 4 - 烷基和C 1 -C 4卤代烷基独立地选择的取代基R a; Ar是苯基或6元杂芳族基，其具有1或2个N原子作为环成员，并且任选地带有一个或两个选自卤素，NO 2，CN，CO 2 R 4，COR 5，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 4 - 烷基和C 1 -C 4卤代烷基，与Ar的相邻C原子一起C3-C4-亚烷基; R 1是氢，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 3 -C 6环烷基，C 3 -C 6环烷基-C 1 -C 4烷基，C 1 -C 4羟烷基，C 1 -C 4烷氧基-C 1 -C 4 - 烷基，C 3 -C 4 - 烯基或C 3 -C 4 - 炔基; 具有如专利权利要求中给出的含义的基团n，R 1，R 2，R 3，R 4和R 5与这些化合物的N-氧化物和生理上耐受的酸加成盐以及包含至少一种N- 和/或至少一种I的生理学耐受的酸加成盐和/或I的N-氧化物，其中适宜地与生理上可接受的载体和/或用于治疗对多巴胺D3受体拮抗剂或激动剂影响的疾病的辅助物质，特别是用于治疗中枢神经系统疾病和肾功能障碍。

3. 发明授权

US07960386B2 Pyridin-2-one compounds and their use as modulators of the dopamine D3 receptor 有权
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：US07960386B2
公开(公告)日：2011-06-14
申请号：US11628633
申请日：2005-06-03
申请人： Herve Geneste , Wilfried Braje , Andreas Haupt
发明人： Herve Geneste , Wilfried Braje , Andreas Haupt
IPC分类号： C07D401/12 , A61K31/506
CPC分类号： C07D401/12
摘要： The invention relates to 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 and the physiologically acceptable salts of the compounds I and their tautomers.The invention also relates to the use of these compounds 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）的吡啶-2-酮化合物，其中A表示可以具有1或2个甲基作为取代基的4至6元烃链，其中1或2个碳原子可以被氧，羰基或硫，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的互变异构体和化合物I及其互变异构体的生理上可接受的盐。本发明还涉及这些化合物用于治疗对多巴胺D3受体拮抗剂或激动剂的影响作出反应的疾病的用途。

4. 发明申请

US20100311755A1 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，-TRIAZIN-3,5-DIONE适用于治疗多巴胺D3受体调节障碍的化合物
公开(公告)号：US20100311755A1
公开(公告)日：2010-12-09
申请号：US12740714
申请日：2008-10-31
申请人： Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Herve' Geneste , Karla Drescher , Liliane Unger , Ana Lucia Jongen-Relo , Anton Bespalov
发明人： Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Herve' Geneste , Karla Drescher , Liliane Unger , Ana Lucia Jongen-Relo , Anton Bespalov
IPC分类号： A61K31/53 , C07D253/07 , A61P25/00 , A61P25/18 , A61P25/30 , A61P13/12
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。

5. 发明申请

US20100048536A1 Novel Substituted Diaryl Azepine Derivatives as Integrin Ligands 审中-公开
标题翻译：新型取代的二芳基Azepine衍生物作为整合素配体
公开(公告)号：US20100048536A1
公开(公告)日：2010-02-25
申请号：US12396698
申请日：2009-03-03
申请人： Herve Geneste , Andreas Kling , Arnulf Lauterbach , Claudia Isabella Graef , Thomas Subkoski , Wilfried Hornberger
发明人： Herve Geneste , Andreas Kling , Arnulf Lauterbach , Claudia Isabella Graef , Thomas Subkoski , Wilfried Hornberger
IPC分类号： A61K31/55 , C07D403/02
CPC分类号： A61K45/06
摘要： The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the αvβ3 integrin receptor, and pharmaceutical preparations comprising these compounds.
摘要翻译：本发明涉及结合整联蛋白受体的新化合物，它们作为整联蛋白受体的配体，特别是作为αv＆bgr 3整联蛋白受体的配体的用途，以及包含这些化合物的药物制剂。

6. 发明申请

US20090105224A1 Tetrahydrobenzazepines and their use in the modulation of the dopamine d3 receptor 失效
标题翻译：四氢苯并吖嗪及其在调节多巴胺d3受体中的用途
公开(公告)号：US20090105224A1
公开(公告)日：2009-04-23
申请号：US10583590
申请日：2004-12-17
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
IPC分类号： C07D223/16 , A61K31/55 , A61P25/00
CPC分类号： C07D223/16 , C07D409/12
摘要： The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides.The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.
摘要翻译：本发明涉及通式Ⅰ的四氢苯并吖庚因，其中变量Ar，A，B，Y，R 1和R 2具有权利要求1所示的含义，以及这些化合物的N-氧化物，生理上耐受的酸加成盐的这些化合物和N-氧化物的生理上耐受的酸加成盐。本发明还涉及药物组合物，其包含至少一种式I的四氢苯并氮杂化合物，I的物理耐受的酸加成盐，式I化合物的N-氧化物和/或其物理上耐受的酸加成盐 I的N-氧化物，并且进一步使用根据本发明的化合物用于治疗有益于多巴胺D3受体拮抗剂或多巴胺D3激动剂的病症。根据本发明的化合物优选可用于治疗中枢神经系统疾病如精神分裂症和抑郁症以及治疗肾功能障碍。

7. 发明申请

US20080221082A1 Ligands of Integrin Receptors 审中-公开
标题翻译：整合素受体配体
公开(公告)号：US20080221082A1
公开(公告)日：2008-09-11
申请号：US10297202
申请日：2001-06-06
申请人： Herve Geneste , Andreas Kling , Udo Lange , Werner Seitz , Claudia Isabella Graef , Thomas Subkowski , Wilfried Hornberger , Arnulf Lauterbach
发明人： Herve Geneste , Andreas Kling , Udo Lange , Werner Seitz , Claudia Isabella Graef , Thomas Subkowski , Wilfried Hornberger , Arnulf Lauterbach
IPC分类号： A61K31/55 , C07D487/14 , C07D235/30 , C07D277/02 , A61K31/426 , A61K31/4168
CPC分类号： A61K45/06
摘要： The invention relates to the use of cyclic compounds as ligands of integrin receptors, in particular as ligands of the αVβ3 integrin receptor, the novel compounds themselves, their use, and pharmaceutical preparations comprising these compounds.
摘要翻译：本发明涉及环状化合物作为整联蛋白受体的配体的用途，特别是作为α3β3整联蛋白受体的配体，新化合物本身，其用途，和包含这些化合物的药物制剂。

8. 发明授权

US07125883B1 Integrin receptor ligands 有权
标题翻译：整合素受体配体
公开(公告)号：US07125883B1
公开(公告)日：2006-10-24
申请号：US09958491
申请日：2000-03-29
申请人： Johann-Christian Zechel , Andreas Kling , Herve Geneste , Udo Lange , Arnulf Lauterbach , Claudia Isabella Graef , Thomas Subkowski , Jens Sadowski , Wilfried Hornberger
发明人： Johann-Christian Zechel , Andreas Kling , Herve Geneste , Udo Lange , Arnulf Lauterbach , Claudia Isabella Graef , Thomas Subkowski , Jens Sadowski , Wilfried Hornberger
IPC分类号： C07D401/14 , A61K31/505
CPC分类号： C07D405/14 , A61K45/06 , C07D239/34 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D409/14 , C07D417/12 , C07D417/14
摘要： The invention relates to novel compounds which bind to integrin receptors, to their preparation, to their use as integrin receptor ligands and for treating diseases, to pharmaceutical preparations comprising these compounds, and to pharmaceutical preparations comprising at least one other active compound.
摘要翻译：本发明涉及结合整联蛋白受体，其制备，其作为整联蛋白受体配体和用于治疗疾病的药物，包含这些化合物的药物制剂以及包含至少一种其它活性化合物的药物制剂的新型化合物。

9. 发明申请

US20060160809A1 N-[(piperazinyl)hetaryl]arylsulfonamide compounds 失效
公开(公告)号：US20060160809A1
公开(公告)日：2006-07-20
申请号：US10823317
申请日：2004-04-13
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer , Sean Turner
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer , Sean Turner
IPC分类号： A61K31/53 , A61K31/506 , A61K31/501
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

US09242933B2 Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (mGlu2 receptor) 有权
标题翻译：杂环化合物作为代谢型谷氨酸受体2（mGlu2受体）的阳性调节剂
公开(公告)号：US09242933B2
公开(公告)日：2016-01-26
申请号：US12126174
申请日：2008-05-23
申请人： Herve Geneste , Daryl Sauer , Wilfried Braje , Wilhelm Amberg , Mario Mezler , Margaretha Henrica Maria Bakker
发明人： Herve Geneste , Daryl Sauer , Wilfried Braje , Wilhelm Amberg , Mario Mezler , Margaretha Henrica Maria Bakker
IPC分类号： C07D207/335 , C07D409/06 , C07D215/12 , C07D231/12 , A61K31/44 , C07D209/14 , C07D209/26 , C07D213/36 , C07D213/38 , C07D233/58 , C07D239/26 , C07D261/08 , C07D277/28 , C07D307/14 , C07D307/54 , C07D333/20 , C07D333/58 , C07D407/04 , C07D409/04
CPC分类号： C07D209/14 , C07D207/335 , C07D209/26 , C07D213/36 , C07D213/38 , C07D215/12 , C07D231/12 , C07D233/58 , C07D239/26 , C07D261/08 , C07D277/28 , C07D307/14 , C07D307/54 , C07D333/20 , C07D333/58 , C07D407/04 , C07D409/04 , C07D409/06
摘要： The present invention relates to heterocyclic compounds which are positive modulators of metabotropic glutamate receptor. The present invention also relates to the use of these compounds for preparing a pharmaceutical composition and to a method of treating a medical disorder, selected from neurological and psychiatric disorders associated with glutamate dysfunction.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的阳性调节剂的杂环化合物。本发明还涉及这些化合物用于制备药物组合物和治疗选自与谷氨酸功能障碍相关的神经和精神障碍的医学病症的方法的用途。

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