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1. 发明申请

WO2006108591A1 1H-QUINAZ0LINE-2,4-DIONES AND THEIR USE AS AMPA-RECEPTOR LIGANDS 审中-公开
标题翻译： 1H-QUINAZ0LINE-2,4-DIONES及其作为AMPA受体配体的用途
公开(公告)号：WO2006108591A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003251
申请日：2006-04-10
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ALLGEIER, Hans , AUBERSON, Yves , CARCACHE, David , FLOERSHEIM, Philipp , GUIBOURDENCHE, Christel , FROESTL, Wolfgang , KALLEN, Jörg , KOLLER, Manuel , MATTES, Henri , NOZULAK, Joachim , ORAIN, David , RENAUD, Johanne
发明人： ALLGEIER, Hans , AUBERSON, Yves , CARCACHE, David , FLOERSHEIM, Philipp , GUIBOURDENCHE, Christel , FROESTL, Wolfgang , KALLEN, Jörg , KOLLER, Manuel , MATTES, Henri , NOZULAK, Joachim , ORAIN, David , RENAUD, Johanne
IPC分类号： C07D239/96 , A61K31/517 , A61P25/08 , A61P25/18 , C07D405/04 , C07D403/04 , C07D401/04 , C07D413/04 , C07D307/16 , C07D309/12 , C07D231/12 , C07D249/06 , C07D207/32 , C07D307/54 , C07D237/08
CPC分类号： C07D239/96 , C07C207/00 , C07C229/56 , C07C229/64 , C07C229/66 , C07C255/18 , C07C265/12 , C07C271/58 , C07D207/337 , C07D231/12 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/06 , C07D263/32 , C07D307/16 , C07D307/54 , C07D309/12 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04
摘要： The present invention relates to l H-Quinazoline-2,4-diones of formula (I) wherein R 1 and R 2 are as defined in the specification, their preparation, their use as AMPA-receptor ligands, in particular for the treatment of epilepsy or schizophrenia, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) and combinations comprising compounds of formula (I) are disclosed.
摘要翻译：本发明涉及式（I）的1H-喹唑啉-2,4-二酮，其中R 1和R 2如说明书中所定义，它们的制备，它们用作AMPA受体配体，特别是用于治疗癫痫或精神分裂症，以及含有它们的药物组合物。此外，公开了用于制备式（I）化合物的中间体和包含式（I）化合物的组合。

2. 发明申请

WO2011048150A1 USE OF 1H-QUINAZOLINE-2,4-DIONES 审中-公开
标题翻译：使用1H-喹唑啉-2,4-二酮
公开(公告)号：WO2011048150A1
公开(公告)日：2011-04-28
申请号：PCT/EP2010/065805
申请日：2010-10-20
申请人： NOVARTIS AG , ALLGEIER, Hans , AUBERSON, Yves , AVRAMEAS, Alexandre , BLAETTLER, Thomas , CARCACHE, David , FLOERSHEIM, Philipp , FROESTL, Wolfgang , GUIBOURDENCHE, Christel , KALKMAN, Hans, O. , KALLEN, Joerg , KOLLER, Manuel , LINGENHÖHL, Kurt , MA, Shenglin , MATTES, Henri , NOZULAK, Joachim , ORAIN, David , RENAUD, Johanne , STROHMAIER, Christine
发明人： ALLGEIER, Hans , AUBERSON, Yves , AVRAMEAS, Alexandre , BLAETTLER, Thomas , CARCACHE, David , FLOERSHEIM, Philipp , FROESTL, Wolfgang , GUIBOURDENCHE, Christel , KALKMAN, Hans, O. , KALLEN, Joerg , KOLLER, Manuel , LINGENHÖHL, Kurt , MA, Shenglin , MATTES, Henri , NOZULAK, Joachim , ORAIN, David , RENAUD, Johanne , STROHMAIER, Christine
IPC分类号： A61K31/517 , A61P25/08
CPC分类号： A61K31/517 , A61K31/34
摘要： The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of Rasmussen's encephalitis and/or certain forms of epilepsy.
摘要翻译：本发明涉及竞争性AMPA受体拮抗剂用于治疗，预防或延缓拉斯穆森脑炎和/或某些形式的癫痫发展的用途。

3. 发明申请

WO2006010591A2 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹唑啉衍生物
公开(公告)号：WO2006010591A2
公开(公告)日：2006-02-02
申请号：PCT/EP2005/008113
申请日：2005-07-26
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ALLGEIER, Hans , FROESTL, Wolfgang , KOLLER, Manuel , MATTES, Henri , NOZULAK, Joachim , OFNER, Silvio , ORAIN, David , RASETTI, Vittorio , RENAUD, Johanne , SOLDERMANN, Nicolas , FLOERSHEIM, Philipp
发明人： ALLGEIER, Hans , FROESTL, Wolfgang , KOLLER, Manuel , MATTES, Henri , NOZULAK, Joachim , OFNER, Silvio , ORAIN, David , RASETTI, Vittorio , RENAUD, Johanne , SOLDERMANN, Nicolas , FLOERSHEIM, Philipp
IPC分类号： C07D239/96 , C07D403/04 , C07D409/12 , C07D401/12 , A61K31/517 , A61P25/00 , A61P25/18 , A61P25/28
CPC分类号： C07D409/12 , C07D239/96 , C07D401/12 , C07D403/04
摘要： The present invention relates to 1H-Quinazoline-2,4-dione derivatives of formula (I) wherein the substituents are defined as in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them.
摘要翻译：本发明涉及其中取代基如说明书中所定义的式（I）的1H-喹唑啉-2,4-二酮衍生物，它们的制备，它们作为药物的用途和药物组合物，其含有它们。

4. 发明授权

EP2468732B1 1H-Quinazoline-2,4-diones 有权
标题翻译： 1 H-Chinazolin -2,4-二酮
公开(公告)号：EP2468732B1
公开(公告)日：2014-08-20
申请号：EP12158895.8
申请日：2006-04-10
申请人： Novartis AG
发明人： ALLGEIER, Hans , NOZULAK, Joachim , ORAIN, David , RENAUD, Johanne , AUBERSON, Yves , CARCACHE, David , FLOERSHEIM, Philipp , GUIBOURDENCHE, Christel , FROESTL, Wolfgang , KALLEN, Joerg , KOLLER, Manuel , MATTES, Henri
IPC分类号： C07D239/96 , C07D403/04 , C07D405/04 , A61K31/517 , A61P25/08 , A61P25/18
CPC分类号： C07D239/96 , C07C207/00 , C07C229/56 , C07C229/64 , C07C229/66 , C07C255/18 , C07C265/12 , C07C271/58 , C07D207/337 , C07D231/12 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/06 , C07D263/32 , C07D307/16 , C07D307/54 , C07D309/12 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04

5. 发明授权

EP1773788B1 Quinazoline derivatives 有权
标题翻译：喹唑啉衍生物
公开(公告)号：EP1773788B1
公开(公告)日：2012-11-14
申请号：EP05768294.0
申请日：2005-07-26
申请人： Novartis AG
发明人： FLOERSHEIM, Philipp , ALLGEIER, Hans , FROESTL, Wolfgang , KOLLER, Manuel , MATTES, Henri , NOZULAK, Joachim , OFNER, Silvio , ORAIN, David , RASETTI, Vittorio , RENAUD, Johanne , SOLDERMANN, Nicolas
IPC分类号： C07D239/96 , C07D403/04 , C07D409/12 , C07D401/12 , A61K31/517 , A61P25/00 , A61P25/18 , A61P25/28
CPC分类号： C07D409/12 , C07D239/96 , C07D401/12 , C07D403/04

6. 发明授权

EP1871749B1 Selurampanel 有权
公开(公告)号：EP1871749B1
公开(公告)日：2012-08-01
申请号：EP06724185.1
申请日：2006-04-10
申请人： Novartis AG
发明人： ALLGEIER, Hans , AUBERSON, Yves , CARCACHE, David , FLOERSHEIM, Philipp , GUIBOURDENCHE, Christel , FROESTL, Wolfgang , KALLEN, Jörg , KOLLER, Manuel , MATTES, Henri , NOZULAK, Joachim , ORAIN, David , RENAUD, Johanne
IPC分类号： C07D239/96 , A61K31/517 , A61P25/08 , A61P25/18
CPC分类号： C07D239/96 , C07C207/00 , C07C229/56 , C07C229/64 , C07C229/66 , C07C255/18 , C07C265/12 , C07C271/58 , C07D207/337 , C07D231/12 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/06 , C07D263/32 , C07D307/16 , C07D307/54 , C07D309/12 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04
摘要： The present invention relates to l H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as AMPA-receptor ligands, in particular for the treatment of epilepsy or schizophrenia, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) and combinations comprising compounds of formula (I) are disclosed.
摘要翻译：本发明涉及式（I）的1H-喹唑啉-2,4-二酮，其中R 1和R 2如说明书中所定义，它们的制备，它们作为AMPA-受体配体的用途，特别是用于治疗癫痫症或精神分裂症和含有它们的药物组合物。此外，公开了用于制造式（I）化合物的中间体和包含式（I）化合物的组合。

7. 发明公开

EP1773788A2 QUINAZOLINE DERIVATIVES 有权
标题翻译：喹唑啉衍生物
公开(公告)号：EP1773788A2
公开(公告)日：2007-04-18
申请号：EP05768294.0
申请日：2005-07-26
申请人： NOVARTIS-PHARMA GMBH , Novartis AG
发明人： FLOERSHEIM, Philipp , ALLGEIER, Hans , FROESTL, Wolfgang , KOLLER, Manuel , MATTES, Henri , NOZULAK, Joachim , OFNER, Silvio , ORAIN, David , RASETTI, Vittorio , RENAUD, Johanne , SOLDERMANN, Nicolas
IPC分类号： C07D239/96 , C07D403/04 , C07D409/12 , C07D401/12 , A61K31/517 , A61P25/00 , A61P25/18 , A61P25/28
CPC分类号： C07D409/12 , C07D239/96 , C07D401/12 , C07D403/04
摘要： The present invention relates to 1H-Quinazoline-2,4-dione derivatives of formula (I) wherein the substituents are defined as in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them.
摘要翻译：本发明涉及其中取代基如说明书中所定义的式（I）的1H-喹唑啉-2,4-二酮衍生物，它们的制备，它们作为药物的用途以及含有它们的药物组合物。

8. 发明授权

EP0934326B1 SUBSTITUIERTE AMINOALKANPHOSPHONSÄUREN 失效
标题翻译：取代aminoalkanephosphonic酸
公开(公告)号：EP0934326B1
公开(公告)日：2006-05-03
申请号：EP97946755.2
申请日：1997-10-22
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ACKLIN, Pierre , ALLGEIER, Hans , AUBERSON, Yves , OFNER, Silvio , VEENSTRA, Siem, Jacob
IPC分类号： C07F9/6509 , A61K31/675
CPC分类号： C07F9/650994
摘要： Compounds have the formula (I), in which R1 stands for hydroxy or an aliphatic, araliphatic or aromatic radical; X stands for a bivalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical; R2 stands for hydrogen or an aliphatic or araliphatic radical; alk stands for lower alkylidene; and R3, R4 and R5 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro. These compounds and their salts may be used for treating pathological conditions which respond to the blocking of exciter amino acid receptors, and for producing pharmaceutical compositions.

9. 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.

10. 发明公开

EP0934326A1 SUBSTITUIERTE AMINOALKANPHOSPHONSÄUREN 失效
标题翻译： SUBSTITUIERTEAMINOALKANPHOSPHONSÄUREN
公开(公告)号：EP0934326A1
公开(公告)日：1999-08-11
申请号：EP97946755.0
申请日：1997-10-22
申请人： Novartis AG
发明人： ACKLIN, Pierre , ALLGEIER, Hans , AUBERSON, Yves , OFNER, Silvio , VEENSTRA, Siem, Jacob
IPC分类号： A61K31 , A61P9 , A61P25 , A61P43 , C07F9
CPC分类号： C07F9/650994
摘要： Compounds have the formula (I), in which R1 stands for hydroxy or an aliphatic, araliphatic or aromatic radical; X stands for a bivalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical; R2 stands for hydrogen or an aliphatic or araliphatic radical; alk stands for lower alkylidene; and R3, R4 and R5 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro. These compounds and their salts may be used for treating pathological conditions which respond to the blocking of exciter amino acid receptors, and for producing pharmaceutical compositions.
摘要翻译：化合物具有式（I），其中R 1代表羟基或脂族，芳脂族或芳族基团; X代表二价脂族，脂环族，脂环族 - 脂族，芳脂族，杂芳脂族或芳族基团; R2代表氢或脂族或芳脂族基团; alk代表低级亚烷基; 并且R3，R4和R5独立地表示氢，低级烷基，卤素，三氟甲基，氰基或硝基。这些化合物及其盐可用于治疗对激动剂氨基酸受体的阻断作出反应的病理状态，并用于制备药物组合物。

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