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1. 发明公开

EP0853617A1 NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES 失效
标题翻译： 2,3-DIOXO-1,2,3,4-四氢 - 二氢喹啉衍生物
公开(公告)号：EP0853617A1
公开(公告)日：1998-07-22
申请号：EP96929275.0
申请日：1996-08-19
申请人： Novartis AG
发明人： ACKLIN, Pierre , ALLGEIER, Hans , AUBERSON, Yves , BIOLLAZ, Michel , MORETTI, Robert , OFNER, Silvio , VEENSTRA, Siem, Jacob
IPC分类号： A61K31 , A61P25 , A61P43 , C07D241 , C07D401 , C07D403 , C07D405 , C07D409 , C07D413 , C07D417 , C07D491 , C07F9
CPC分类号： C07D401/06 , C07D241/44 , C07D401/12 , C07D417/12 , C07F9/650994
摘要： 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N+(R8)(R9)-X-R7A- (Id), -alk-O-X-R¿7? (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A?-¿ being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R¿7? and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.

2. 发明公开

EP0837864A1 NOVEL QUINOXALINE- AND QUINOXALINYLALKANE-PHOSPHONIC ACIDS 失效
标题翻译：新的喹喔啉和喹喔啉基烷基膦酸
公开(公告)号：EP0837864A1
公开(公告)日：1998-04-29
申请号：EP96924829.0
申请日：1996-07-01
申请人： Novartis AG
发明人： MORETTI, Robert , ALLGEIER, Hans
IPC分类号： A61K31 , A61P9 , A61P25 , C07D241 , C07F9
CPC分类号： C07F9/650994 , C07D241/44
摘要： Quinoxaline- and quinoxalinylalkane-phosphonic acids of formula (I), wherein R1 is free or esterified carboxy or free or partially esterified phosphono, R2 and R3 are each independently of the other hydrogen or an aliphatic radical, the radicals R4, R5 and R6 are each independently of the others hydrogen, an aliphatic hydrocarbon radical, free or etherified hydroxy, free or etherified mercapto or oxidised free or etherified mercapto, unsubstituted or aliphatically substituted amino, nitro, free or esterified or amidated carboxy, cyano, free or amidated sulfamoyl, halogen or trifluoromethyl and X is a divalent aliphatic radical, and their tautomers and/or salts have NMDA-antagonistic properties and can be used in the treatment of pathological conditions that are responsive to blocking of NMDA-sensitive receptors.
摘要翻译：其中R 1为游离或酯化的羧基或游离或部分酯化的膦酰基的式（I）的喹喔啉 - 和喹喔啉基烷烃 - 膦酸，R 2和R 3各自独立地为氢或脂族基团，基团R 4，R 5和R 6为游离或醚化的巯基或氧化的游离或醚化的巯基，未取代或脂族取代的氨基，硝基，游离或酯化或酰胺化的羧基，氰基，游离或酰胺化的氨磺酰基，卤素或三氟甲基，并且X是二价脂族基团，并且它们的互变异构体和/或盐具有NMDA拮抗特性，并且可以用于治疗对阻断NMDA敏感性受体有响应的病理状况。

3. 发明授权

EP0853617B1 NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES 失效
标题翻译： 2,3-二氧代-1,2,3,4-四氢喹喔啉衍生物
公开(公告)号：EP0853617B1
公开(公告)日：2004-03-03
申请号：EP96929275.4
申请日：1996-08-19
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ACKLIN, Pierre , ALLGEIER, Hans , AUBERSON, Yves , BIOLLAZ, Michel , MORETTI, Robert , OFNER, Silvio , VEENSTRA, Siem, Jacob
IPC分类号： C07D241/44 , C07D401/06 , A61K31/495
CPC分类号： C07D401/06 , C07D241/44 , C07D401/12 , C07D417/12 , C07F9/650994
摘要： 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N+(R8)(R9)-X-R7A- (Id), -alk-O-X-R¿7? (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A?-¿ being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R¿7? and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.

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