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1. 发明授权

EP1963337B1 THIENO[2,3-b]PYRIDINE DERIVATIVES 无效
标题翻译：噻吩[2,3-b]吡啶衍生物
公开(公告)号：EP1963337B1
公开(公告)日：2010-09-01
申请号：EP06831522.5
申请日：2006-12-19
申请人： Richter Gedeon Nyrt.
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 (CH2)n, NH, NHCH2; 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; R1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R2 is an optionally substituted phenyl, heterocyclyl, or NR3R4 group wherein R3 and R4 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R3 and R4 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s), or NH-CO-NR5R6 group, wherein R5 and R6 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R5 and R6 together with the N atom to which they are attached form an optionally substituted C5-7 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.

2. 发明公开

EP2074083A1 NEW SULFONAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS 无效
标题翻译：新磺胺ALS缓激肽拮抗剂
公开(公告)号：EP2074083A1
公开(公告)日：2009-07-01
申请号：EP07824996.8
申请日：2007-10-27
申请人： Richter Gedeon Nyrt.
发明人： BOZÓ, Éva , BEKE, Gyula , ÉLES, János , FARKAS, Sándor , HORNOK, Katalin , KESERÜ, György , SCHMIDT, Éva , SZENTIRMAY, Éva , VÁGÓ, István , VASTAG, Mónika
IPC分类号： C07C311/21 , A61K31/18 , A61P29/00 , C07D207/26 , C07D211/26 , C07D211/34 , C07D211/56 , C07D211/62 , C07D211/76 , C07D213/38 , C07D213/74 , C07D213/75 , C07D233/54 , C07D239/04 , C07D239/42
CPC分类号： C07C311/21 , C07D207/26 , C07D211/26 , C07D211/34 , C07D211/56 , C07D211/62 , C07D211/76 , C07D213/38 , C07D213/74 , C07D213/75 , C07D233/54 , C07D239/04 , C07D239/42 , C07D241/20 , C07D243/08 , C07D295/12 , C07D295/20 , C07D401/04 , C07D401/06 , C07D401/12
摘要： The present invention relates to new sulfonamide derivatives of formula (I), wherein R1 -R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

3. 发明公开

EP2057116A1 NEW PHENYLSULFAMOYL BENZAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS 无效
标题翻译：新的苯基氨基磺酰基苯甲酰胺衍生物作为BRADYKININ ANTAGONISTS
公开(公告)号：EP2057116A1
公开(公告)日：2009-05-13
申请号：EP07824995.0
申请日：2007-10-27
申请人： Richter Gedeon Nyrt.
发明人： BEKE, Gyula , BOZÓ, Éva , FARKAS, Sándor , HORNOK, Katalin , KESERÜ, György , SCHMIDT, Éva , SZENTIRMAY, Éva , VÁGÓ, István , VASTAG, Mónika
IPC分类号： C07C311/21 , A61K31/18 , A61P29/00 , C07D209/08 , C07D211/26 , C07D211/58 , C07D213/40 , C07D231/40 , C07D233/54 , C07D235/30 , C07D261/14 , C07D277/46 , C07D277/62 , C07D277/82 , C07D285/12
CPC分类号： C07C311/21 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D209/08 , C07D211/26 , C07D211/58 , C07D213/40 , C07D213/75 , C07D231/40 , C07D233/54 , C07D233/64 , C07D235/30 , C07D241/08 , C07D261/14 , C07D277/46 , C07D277/62 , C07D277/82 , C07D285/135 , C07D295/13 , C07D295/135 , C07D317/46
摘要： The present invention relates to new sulfonamide derivatives of formula (I), wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
摘要翻译：本发明涉及式（I）的新型磺酰胺衍生物，其中R1-R8和Z如权利要求中所定义，以及作为选择性拮抗剂的光学对映体或外消旋体和/或盐和/或水合物和/或溶剂合物缓激肽B1，制备这些相同化合物的方法，含有它们的药物组合物，以及它们在治疗或预防疼痛和炎症状况中的用途。

4. 发明授权

EP1409477B1 PIPERIDINE DERIVATIVES AS NMDA RECEPTOR ANTAGONISTS 有权
标题翻译：哌啶，NMDA受体拮抗剂
公开(公告)号：EP1409477B1
公开(公告)日：2008-09-17
申请号：EP02753161.5
申请日：2002-07-23
申请人： Richter Gedeon NYRT
发明人： DOMANY, György , HORVATH, Csilla , FARKAS, Sándor , BARTANE SZALAI, Gizella , NAGY, József , KOLOK, Sándor , BOZO, Eva , BORZA, István , VAGO, István , BIELIK, Attila , IGNACZNE SZENDREI, Györgyi , KESERÜ, György
IPC分类号： C07D401/12 , C07D413/12 , C07D295/185 , C07D407/12 , C07D417/12 , C07D451/02 , A61K31/445 , A61P25/28
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.

5. 发明公开

EP1963338A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：EP1963338A1
公开(公告)日：2008-09-03
申请号：EP06842192.4
申请日：2006-12-19
申请人： Richter Gedeon NYRT
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：本发明涉及式（I）的新的mGluR1和mGluR5受体亚型优选配体; 其中Y代表选自氢，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/或水合物和/或溶剂化物，涉及其制备方法，涉及含有该化合物的药物组合物及其在治疗和/或预防需要 mGluR1和mGluR5受体的调节，例如神经障碍，精神障碍，急性和慢性疼痛以及下尿路的神经肌肉功能障碍。

6. 发明公开

EP1963336A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：EP1963336A1
公开(公告)日：2008-09-03
申请号：EP06831521.7
申请日：2006-12-19
申请人： Richter Gedeon NYRT
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, SO2; Y represents a group selected from 0, OCH2, (CH2)n, NH, NHCH2; n is an integer of 0 to 2; R1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R2 is an optionally substituted phenyl, heterocyclyl or NR3R4 group wherein R3 and R4 are independently selected from the group of hydrogen, alkyl, or R3 and R4 together with the N atom to which they are attached can form an optionally substituted C5-7 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：本发明涉及新的式（I）的mGluR1和mGluR5受体亚型优选配体，其中X代表选自CO，SO，SO2的基团; Y代表选自O，OCH 2，（CH 2）n，NH，NHCH 2的基团; n是0至2的整数; R1是任选取代的烷基，环烷基，苯基，联苯基，杂环基; R 2为任选取代的苯基，杂环基或NR 3 R 4基团，其中R 3和R 4独立地选自氢，烷基或R 3和R 4与它们所连接的N原子一起可形成任选取代的C 5-7杂环基，其含有一种或多种选自N，O，S和/或互变异构体和/或盐和/或水合物和/或溶剂合物的杂原子，涉及其制备方法，涉及药物组合物以及它们在治疗和/或预防需要调节mGluR1和mGluR5受体如神经障碍，精神障碍，急性和慢性疼痛，下尿路神经肌肉功能障碍和胃肠病症的病理状况中的用途。

7. 发明公开

EP1962849A1 QUINOLINE DERIVATIVES USEFUL IN THE TREATMENT OF MGLUR5 RECEPTOR-MEDIATED DISORDERS 有权
标题翻译：喹啉衍生物对mGluR5受体介导的疾病的治疗
公开(公告)号：EP1962849A1
公开(公告)日：2008-09-03
申请号：EP06831520.9
申请日：2006-12-19
申请人： Richter Gedeon NYRT
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.

9. 发明授权

EP2167469B1 SULFONYL-QUINOLINE DERIVATIVES 有权
标题翻译：磺酰基 - 喹啉衍生物
公开(公告)号：EP2167469B1
公开(公告)日：2012-08-15
申请号：EP08762671.9
申请日：2008-06-17
申请人： Richter Gedeon Nyrt.
发明人： GALAMBOS, János , KESERÜ, György , GÁL, Krisztina , BOBOK, Amrita, Ágnes , WÉBER, Csaba , PRAUDA, lbolya , WÁGNER, Gábor, András , VASTAG, Mónika
IPC分类号： C07D215/36 , C07D409/12 , A61K31/4706 , A61K31/4709 , A61P25/00
CPC分类号： C07D215/36 , C07D409/12
摘要： New mGluRl and mGluR5 receptor subtype preferring ligands of formula: (I) and/or salts and/or hydrates and/or solvates thereof, to the processes and intermediates for their preparation, to pharmaceutical compositions containing these compounds and to their use in therapy and/or prevention of a condition which requires modulation of mGluRl and mGluR5 receptors.FORMULE (I) wherein Ar
1 represents an optionally substituted phenyl or heteroaryl group; Ar
2 represents a substituted phenyl or an optionally substituted heteroaryl group; R
1 , R
2 , R
3 and R
4 represent independently a substituent selected from hydrogen, halogen, cyano, alkyl, alkoxy, hydroxy, trifluoromethyl, amino, alkylamino, dialkylamino, aminomethyl, alkylaminomethyl, dialkylaminomethyl
摘要翻译：新的mGluR1和mGluR5受体亚型偏好式的配位体：（I）和/或盐和/或水合物和/或溶剂化物，涉及它们的制备方法和中间体，含有这些化合物的药物组合物以及它们的使用在治疗和 /或预防需要调节mGluR1和mGluR5受体的病症。方案（I）其中Ar 1代表任选取代的苯基或杂芳基; Ar 2表示取代的苯基或任选取代的杂芳基; R 1，R 2，R 3和R 4独立地表示选自氢，卤素，氰基，烷基，烷氧基，羟基，三氟甲基，氨基，烷基氨基，二烷基氨基，氨基甲基，烷基氨基，二烷基氨基甲基的取代基

10. 发明公开

EP2215055A1 NEW NON-PEPTIDE DERIVATIVES AS BRADYKININ B1 ANTAGONISTS 审中-公开
标题翻译：新的非肽衍生物作为缓激肽B1受体拮抗剂
公开(公告)号：EP2215055A1
公开(公告)日：2010-08-11
申请号：EP07824993.5
申请日：2007-10-27
申请人： Richter Gedeon Nyrt.
发明人： VÁGÓ, István , FARKAS, Sándor , HORNOK, Katalin , BEKE, Gyula , BOZÓ, Éva , VASTAG, Mónika , SZENTIRMAY, Éva , KESERÜ, György , SCHMIDT, Éva
IPC分类号： C07C311/21 , A61K31/18 , A61P29/00 , C07D207/12 , C07D211/22 , C07D211/26 , C07D211/44 , C07D211/58 , C07D211/62 , C07D241/06 , C07D243/08 , C07D279/12 , C07D295/20 , C07D401/04
CPC分类号： C07C311/21 , C07D207/36 , C07D211/22 , C07D211/26 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/74 , C07D241/08 , C07D295/096 , C07D295/185
摘要： The present invention relates to new non-peptide derivatives of formula (I), wherein R
1 -R
5 , Q and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

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