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1. 发明申请

WO2003010159A1 PIPERIDINE DERIVATIVES AS NMDA RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NMDA受体拮抗剂的哌啶衍生物
公开(公告)号：WO2003010159A1
公开(公告)日：2003-02-06
申请号：PCT/HU2002/000071
申请日：2002-07-23
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , DOMÁNY, György , HORVÁTH, Csilla , FARKAS, Sándor , BARTÁNÉ SZALAI, Gisella , NAGY, József , KOLOK, Sándor , KOVÁCSNÉ BOZÓ, Éva , BORZA, István , VÁGÓ, István , BIELIK, Attila , IGNÁCZNÉ SZENDREI, Györgyi , KESERÚ, György
发明人： DOMÁNY, György , HORVÁTH, Csilla , FARKAS, Sándor , BARTÁNÉ SZALAI, Gisella , NAGY, József , KOLOK, Sándor , KOVÁCSNÉ BOZÓ, Éva , BORZA, István , VÁGÓ, István , BIELIK, Attila , IGNÁCZNÉ SZENDREI, Györgyi , KESERÚ, György
IPC分类号： C07D401/12
CPC分类号： C07D211/14 , C07D211/16 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to new carboxylic acid amide derivatives of formula (I), wherein U, V, W, X, Y, Z, n and m are as defined as in Claim 1. A further object of the invention are the processes for producing of carboxylic acid amide compounds of formula (I), and the pharmaceutical manufacture of medicaments containing these compounds, as well as the process of treatments with these compounds, which means administering to a mammal to be treated including human - effective amount/amounts of compounds of formula (I) of the present invention as such or as medicament. The new carboxylic acid amide derivatives of formula (I) of the present invention are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.
摘要翻译：本发明涉及式（I）的新的羧酸酰胺衍生物，其中U，V，W，X，Y，Z，n和m如权利要求1所定义。本发明的另一个目的是制备式（I）的羧酸酰胺化合物，以及含有这些化合物的药物的药物制造，以及用这些化合物处理的方法，这意味着对待治疗的哺乳动物施用包括人 - 有效量/ 本发明的式（I）化合物本身或作为药物。本发明式（I）的新羧酸酰胺衍生物是NMDA受体的高效和选择性拮抗剂，而且大部分化合物是NMDA受体NR2B亚型的选择性拮抗剂。

2. 发明申请

WO2006010968A1 NEW ARYLOXY ACETIC ACID AMIDE DERIVATIVES 审中-公开
标题翻译：新ARYLOXY乙酸酰胺衍生物
公开(公告)号：WO2006010968A1
公开(公告)日：2006-02-02
申请号：PCT/HU2005/000081
申请日：2005-07-21
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , KESERÛ, György , VÁGÓ, István , FARKAS, Sándor , HORVÁTH, Csilla , BIELIK, Attila , BORZA, István , WÉBER, Csaba , KOLOK, Sándor , NAGY, József
发明人： KESERÛ, György , VÁGÓ, István , FARKAS, Sándor , HORVÁTH, Csilla , BIELIK, Attila , BORZA, István , WÉBER, Csaba , KOLOK, Sándor , NAGY, József
IPC分类号： C07C235/34 , C07D211/08 , C07D235/06 , C07D263/56 , A61K31/16 , A61K31/18 , A61K31/445 , A61K31/4184
CPC分类号： C07D211/22 , C07D211/16 , C07D211/18 , C07D211/46 , C07D211/52 , C07D211/58 , C07D211/70 , C07D401/12 , C07D413/12
摘要： The new aryloxy acetic acid amide derivatives of formula (I) where R 1 and R 2 are the same or different and can be hydrogen atom or C 1-4 alkanoylamido group optionally substituted by halogen atom or C 1-4 alkyl-sulfonylamido group or N'-( C 1-4 alkyl)-ureido group C 1-6 alkoxy-carbonyl-amido or di-( C 1-4 alkyl)-amino group with the proviso that only one of them can be hydrogen atom, or R 1 and R 2 form together a -NH-CO-NH-, -NH-N=CH- or -NH-CO-O- chain attached to two neighbouring carbon atoms of the benzyl group, R 3 and R 4 mean the same or different C 1-4 alkyl groups which are substituted by phenyl group, or R 3 and R 4 mean together a C 4-6 alkylene chain which can be interrupted optionally by a nitrogen atom and which can contain a C-C double bound and which C 4-6 alkylene chain can substituted by one or two substituents from the following hydroxy group, phenyl or phenoxy group optionally substituted by a C 1-4 alkyl or trifluoro methyl group, =CH-phenyl group which can be substituted by halogen atom or C 1-4 alkyl group, C 1-4 alkyl group optionally substituted by hydroxy groµp and one or two phenyl groups which can be substituted by halogen atom or C 1-4 alkyl group, C 1-4 alkyl amino group which is substituted by a phenyl or naphtyl group which can be substituted optionally by a halogen atom or a C 1-4 alkyl group, as well as their salts formed with organic or inorganic acids or bases and solvates of these compounds are functional antagonists of NMDA receptors, which target the NMDA receptors primarily via binding to the ifenprodil binding site. Furthermore objects of the present invention are the pharmaceutical compositions containing new aryloxy acetic acid amide derivatives of formula (I) or optical antipodes or racemates or the salts thereof as active ingredients and processes for producing these compounds and pharmaceutical compositions.
摘要翻译：式（I）的新的芳氧基乙酸酰胺衍生物，其中R

3. 发明申请

WO2003028728A1 4-(4-SUBSTITUTED PIPERAZINYL-1YL)-BUTYLCARBOXAMIDES AS D3 DOPAMINE SUBTYPE SELECTIVE LIGANDS 审中-公开
标题翻译： 4-（4-取代的哌嗪-1-基） - 丁醛作为D3多巴胺亚型选择性配体
公开(公告)号：WO2003028728A1
公开(公告)日：2003-04-10
申请号：PCT/HU2002/000095
申请日：2002-09-25
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , NÓGRÁDI, Katalin , GALAMBOS, János , ÁCS, Tibor , BORZA, István , BIELIK, Attila , DOMÁNY, György , KISS, Béla , GYERTYÁN, István , LASZLOVSZKY, István , HORVÁTH, Attila
发明人： NÓGRÁDI, Katalin , GALAMBOS, János , ÁCS, Tibor , BORZA, István , BIELIK, Attila , DOMÁNY, György , KISS, Béla , GYERTYÁN, István , LASZLOVSZKY, István , HORVÁTH, Attila
IPC分类号： A61K31/496
CPC分类号： C07D209/48 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/519 , A61K31/542 , C07D207/34 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/50 , C07D215/54 , C07D233/64 , C07D239/26 , C07D295/073 , C07D295/096 , C07D295/13 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to new D 3 dopamine receptor subtype selective ligands of Formula (I), wherein R 1 , R 2 and R 3 independently represent substituents selected from hydrogen, halogen, C 1-6 alkyl, C 1-6 alkoxy, cyano, hydroxy, trifluoromethyl, C 1-6 alkylsulfonyloxy, trifluoromethanesulfonyloxy, optionally substituted C 1-6 alkanoyloxy, amino, aminoalkyl, carboxy, aminocarbonyl, N-hydroxycarbamimidoyl, carbamimidoyl, hydroxycarbamoyl, thiocarbamoyl, sulfamoyl, optionally substituted phenyl or naphthyl, optionally substituted mono or bicyclic heterocyclic group, two adjacent groups of R 1 , R 2 and R 3 may combine to form an optionally substituted fused mono or bicyclic heterocyclic group, with the exception of compounds wherein a) R 1 = R 2 = R 3 = H, b) R 1 = R 2 = H and R 3 = C 1-6 alkoxy in the position 2 or R 3 is in the position 4 of the piperazinylphenyl moiety, c) R¿1 ?= H and R 2 = R 3 = C 1-6 alkoxy; Q represents an optionally substituted C 1-6 alkyl, C 1-6 alkenyl, phenyl or heteroaryl group.
摘要翻译：本发明涉及式（I）的新的D3多巴胺受体亚型选择性配体，其中R 1，R 2和R 3独立地表示选自氢，卤素，C 1-6烷基，C 1-6烷氧基，氰基，羟基，三氟甲基，C 1-6烷基磺酰氧基，三氟甲磺酰氧基，任选取代的C 1-6烷酰氧基，氨基，氨基烷基，羧基，氨基羰基，N-羟基甲脒基，氨基甲酰基，氨基甲酰基，硫代氨基甲酰基，氨磺酰基，任选取代的苯基或萘基，任选取代的单或双环杂环基，并且R 3可以结合形成任选取代的稠合单或双环杂环基，除了其中a）R 1 = R 2 = R 3 = H，b）R 1 = R 2 = H和R 3 = C 1-6烷氧基在位置2或 R3在哌嗪基苯基部分的位置4，c）R1 = H，R2 = R3 = C1-6烷氧基; Q表示任选取代的C 1-6烷基，C 1-6烯基，苯基或杂芳基。

4. 发明申请

WO2007072093A1 QUINOLINE DERIVATIVES USEFUL IN THE TREATMENT OF MGLUR5 RECEPTOR-MEDIATED DISORDERS 审中-公开
标题翻译：喹诺酮衍生物用于治疗MGLUR5受体介导的疾病
公开(公告)号：WO2007072093A1
公开(公告)日：2007-06-28
申请号：PCT/HU2006/000121
申请日：2006-12-19
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , KESERÜ, György , WÉBER, Csaba , BIELIK, Attila , BOBOK, Amrita, Ágnes , GÁL, Krisztina , MESZLÉNYINÉ SIPOS, Márta , MOLNÁR, László , VASTAG, Mónika
发明人： KESERÜ, György , WÉBER, Csaba , BIELIK, Attila , BOBOK, Amrita, Ágnes , GÁL, Krisztina , MESZLÉNYINÉ SIPOS, Márta , MOLNÁR, László , VASTAG, Mónika
IPC分类号： A61K31/4706 , A61K31/4709 , A61K31/4741 , C07D215/42 , C07D215/44 , C07D215/46 , C07D401/04 , C07D405/12 , C07D405/14 , A61P25/00
CPC分类号： C07D215/42 , C07D215/44 , C07D215/46 , C07D405/12 , C07D491/04 , C07D491/10
摘要： Compounds of formula (I): and/or enantiomers and/or racemates and/or diastereomers and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the process for their preparation, to the intermediates of the preparation process, to the pharmaceutical formulations containing these compounds and to their use in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
摘要翻译：与酸或碱形成的式（I）化合物和/或其对映异构体和/或外消旋体和/或非对映异构体和/或其药学上可接受的盐，其制备方法，制备方法的中间体，含有这些化合物的制剂及其在预防和/或治疗mGluR5受体介导的病症中的用途。

5. 发明申请

WO2007072094A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2007072094A1
公开(公告)日：2007-06-28
申请号：PCT/HU2006/000122
申请日：2006-12-19
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , NÓGRÁDI, Katalin , WÁGNER, Gábor , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , HÁDA, Viktor , KÓTI, János , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
发明人： NÓGRÁDI, Katalin , WÁGNER, Gábor , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , HÁDA, Viktor , KÓTI, János , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
IPC分类号： C07D495/04 , A61K31/4365 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention relates to new mGluRl and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from CO, SO, SO 2 ; Y represents a group selected from 0, OCH 2 , (CH 2 )n, NH, NHCH 2 ; n is an integer of 0 to 2; R 1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R 2 is an optionally substituted phenyl, heterocyclyl or NR 3 R 4 group wherein R 3 and R 4 are independently selected from the group of hydrogen, alkyl, or R 3 and R 4 together with the N atom to which they are attached can form an optionally substituted C 5-7 heterocyclyl group, containing one or more heteroatom(s) selected from the group of N, O, S, and/or tautomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluRl and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.
摘要翻译：本发明涉及新的mGluR1和mGluR5受体亚型优选式（I）的配体，其中X表示选自CO，SO，SO 2的基团; Y表示选自0，OCH 2，（CH 2）2，NH，NHCH 2的基团。 n为0〜2的整数， R 1是任选取代的烷基，环烷基，苯基，联苯基，杂环基; R 2是任选取代的苯基，杂环基或NR 3 R 4 R 4基团，其中R 3'和R“_{> 4个独立地选自氢，烷基或R 3和R 4和它们所连接的N原子的基团可以形成含有一个或多个选自N，O，S和/或互变异构体和/或盐和/或水合物的杂原子和/或杂原子的任选取代的C 5-7杂环基，和/或其制备方法涉及含有该组合物的药物组合物及其在治疗和/或预防需要调节mGluR1和mGluR5受体如神经系统疾病，精神疾病，急性和慢性的病理状况中的用途疼痛，下尿路神经肌肉功能障碍和胃肠道疾病。}

6. 发明申请

WO2007072095A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2007072095A1
公开(公告)日：2007-06-28
申请号：PCT/HU2006/000123
申请日：2006-12-19
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , NÓGRÁDI, Katalin , WÁGNER, Gábor , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , HÁDA, Viktor , KÓTI, János , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
发明人： NÓGRÁDI, Katalin , WÁGNER, Gábor , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , HÁDA, Viktor , KÓTI, János , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
IPC分类号： C07D495/04 , A61K31/4365 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention relates to new mGluRl and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from SO, SO2; Y represents a group selected from (CH 2 ) n , NH, NHCH 2 ; n is an integer of 0 to 1; Z is H or monosubstituted by alkyl, nitro, halogen, alkoxy, trifluoromethyl, cyano, amino, alkylamino, dialkylamino, aminomethyl, alkylaminomethyl, dialkylaminomethyl, hydroxyl, alkylsulfonylamino; R 1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R 2 is an optionally substituted phenyl, heterocyclyl, or NR 3 R 4 group wherein R 3 and R 4 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R 3 and R 4 together with the N atom to which they are attached form an optionally substituted C 5-7 heterocyclyl group, containing one or more heteroatom(s), or NH-CO-NR 5 R 6 group, wherein R 5 and R 6 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R 5 and R 6 together with the N atom to which they are attached form an optionally substituted C 5-7 heterocyclyl group, containing one or more heteroatom(s); and/or hydrates and/or solvates and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluRl and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.
摘要翻译：本发明涉及新的mGluR1和mGluR5受体亚型优选式（I）的配体，其中X表示选自SO，SO 2的基团; Y表示选自（CH 2）n，NH，NHCH 2， n为0〜1的整数; Z是H或被烷基，硝基，卤素，烷氧基，三氟甲基，氰基，氨基，烷基氨基，二烷基氨基，氨基甲基，烷基氨基甲基，二烷基氨基甲基，羟基，烷基磺酰基氨基等单取代。 R 1是任选取代的烷基，环烷基，苯基，联苯基，杂环基; R 2是任选取代的苯基，杂环基或NR 3 R 4 R 4基团，其中R 3和R 3，独立地选自氢和任选取代的烷基，或R 3和R 4与它们所在的N原子一起连接形成任选取代的C 5-7杂环基，其含有一个或多个杂原子或NH-CO-NR 5 R 6 >基，其中R 5和R 6独立地选自氢和任选取代的烷基，或R 5和R 5， SUB> 6与它们所连接的N原子一起形成含有一个或多个杂原子的任选取代的C 5-7杂环基; 和/或与酸或碱形成的水合物和/或其溶剂合物和/或其药学上可接受的盐与其制备方法相同的药物组合物及其在治疗和/或预防需要的病理状况中的用途 mGluR1和mGluR5受体的调节如神经障碍，精神疾病，急性和慢性疼痛，下尿路神经肌肉功能障碍和胃肠道疾病。

7. 发明申请

WO2007072091A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2007072091A1
公开(公告)日：2007-06-28
申请号：PCT/HU2006/000119
申请日：2006-12-19
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , NÓGRÁDI, Katalin , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
发明人： NÓGRÁDI, Katalin , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
IPC分类号： C07D495/04 , A61K31/4365 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I); wherein Y represents a subtituent selected from hydrogen, methyl, fluoro, chloro, bromo, methoxy; Z is hydrogen or methyl; R is an optionally substituted heteroaryl, and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.
摘要翻译：本发明涉及新的mGluR1和mGluR5受体亚型优选式（I）的配体; 其中Y表示选自氢，甲基，氟，氯，溴，甲氧基的取代基; Z是氢或甲基; R是任选取代的杂芳基，和/或其盐和/或其水合物和/或溶剂合物，其制备方法，含有其的药物组合物及其在治疗和/或预防需要的病理状况中的用途 mGluR1和mGluR5受体的调节，如神经系统疾病，精神疾病，急性和慢性疼痛以及下泌尿道的神经肌肉功能障碍。

8. 发明申请

WO2007072090A1 THIENOPYRIDINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：作为代谢型谷氨酸受体的调节剂的三硝基吡啶衍生物
公开(公告)号：WO2007072090A1
公开(公告)日：2007-06-28
申请号：PCT/HU2006/000118
申请日：2006-12-19
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , NÓGRÁDI, Katalin , WÁGNER, Gábor , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , HÁDA, Viktor , KÓTI, János , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
发明人： NÓGRÁDI, Katalin , WÁGNER, Gábor , KESERÜ, György , BIELIK, Attila , GÁTI, Tamás , HÁDA, Viktor , KÓTI, János , GÁL, Krisztina , VASTAG, Mónika , BOBOK, Amrita, Ágnes
IPC分类号： C07D495/04 , A61K31/4365 , A61P25/28
CPC分类号： C07D495/04
摘要： The present invention relates to new mGluRl and niGluR5 receptor subtype preferring ligands of formula (I): wherein X represents a group selected from (CH 2 ) n , CH=CH, NH, N(CH 3 ), NHCH 2 , N(CH 3 )CH 2 , O, OCH 2 , CH 2 COO, NHCH 2 COO; n is an integer of O to 2; Y represents a subtituent selected from H, CH 3 , F, Cl, Br; Z is H or CH 3 ; R is alkyl, cycloalkyl, an optionally substituted phenyl or an optionally substituted heteroaryl, and/or geometric isomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluRl mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.
摘要翻译：本发明涉及新的mGluR1和niGluR5受体亚型优选式（I）的配体：其中X表示选自（CH 2）n，CH = CH， NH，N（CH 3）3，NHCH 2，N（CH 3 3）CH 2，O，OCH CH 2 CO 2，NHCH 2 COO，CH 2 COO，NHCH 2 COO; n为0〜2的整数; Y表示选自H，CH 3，F，Cl，Br的取代基; Z是H或CH 3 N; R是烷基，环烷基，任选取代的苯基或任选取代的杂芳基，和/或其几何异构体和/或其盐和/或水合物和/或溶剂化物，其制备方法，包含其的药物组合物和用于治疗和/或预防需要调节mGluR1 mGluR5受体的病理状况，例如神经系统疾病，精神疾病，急性和慢性疼痛以及下泌尿道的神经肌肉功能障碍。

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