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1. 发明授权

EP0810991B1 1-ARYL-2-ACYLAMINO-ETHANE COMPOUNDS AND THEIR USE AS NEUROKININ ESPECIALLY NEUROKININ 1 ANTAGONISTS 失效
标题翻译： 1-芳基-2-酰氨基乙烷化合物和它们作为神经激肽尤其是作为神经激肽-1拮抗剂的用途
公开(公告)号：EP0810991B1
公开(公告)日：1999-04-14
申请号：EP96901800.1
申请日：1996-02-09
申请人： Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
发明人： GERSPACHER, Marc , VON SPRECHER, Andreas , ROGGO, Silvio , MAH, Robert , OFNER, Silvio , VEENSTRA, Siem, Jacob , BETSCHART, Claudia , AUBERSON, Yves , SCHILLING, Walter
IPC分类号： C07C237/22 , A61K31/16 , C07D213/40 , C07D209/08 , C07D211/58 , C07C311/51 , C07D295/185 , C07D295/13 , C07D209/12 , C07D209/20
CPC分类号： C07D213/40 , C07C237/22 , C07C255/29 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/22 , C07D211/44 , C07D211/48 , C07D211/58 , C07D213/70 , C07D215/46 , C07D223/12 , C07D231/12 , C07D231/38 , C07D233/56 , C07D235/16 , C07D235/28 , C07D239/42 , C07D241/20 , C07D249/08 , C07D295/13 , C07D295/135 , C07D295/185 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/10
摘要： 1-Aryl-2-acylamino-ethane compounds of formula (I), wherein R1 is aryl or heteroaryl; R2 is hydrogen, lower alkyl or aryl-lower alkyl; R3 is hydrogen, lower alkyl, aryl or heteroaryl; R4 is aryl or heteroaryl; X is C1-C7alkylene, C2-C7 alkenyline or C4-C7 alkanedienylene, and Am is an unsubstituted or mono- or di-substituted amino group, a disubstituted amino group being understood as including also an amino group in which the amino nitrogen is bonded into a ring, or a salt thereof, have valuable pharmaceutical properties and are especially effective as NK1 antagonists. They are prepared in a manner known per se.

2. 发明授权

EP0783490B1 1-ACYL-4-ALIPHATIC AMINOPIPERIDINE COMPOUNDS 失效
标题翻译： 1-酰基-4-氨基哌啶的脂族化合物
公开(公告)号：EP0783490B1
公开(公告)日：2002-02-06
申请号：EP95933394.9
申请日：1995-09-19
申请人： Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
发明人： OFNER, Silvio , VEENSTRA, Siem, Jacob
IPC分类号： C07D211/58 , A61K31/445
CPC分类号： C07D211/58
摘要： The invention relates to novel 1-acyl-4-aliphatylaminopiperidine compounds of formula (I), in which R1 is a benzoyl, naphthoyl or cycloalkanoyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl; R2 is cycloalkyl or a phenyl or naphthyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen, nitro, cyano and/or trifluoromethyl; R3 and R4 together are lower alkylene or aza-, oxa- or thia-lower alkylene; or R3 is lower alkyl, lower alkoxy-lower alkyl, di-lower alkylamino-lower alkyl or a radical of the formula -(CH2)n-C(=O)-R5 (Ia); and R4 is hydrogen, lower alkyl or a radical of the formula -(CH2)n-C(=O)-R5 (Ia); R5 is (i) hydrogen, alkyl or alkyl which is substituted by halogen, lower alkoxy, amino or amino substituted by lower alkyl, amino-lower alkyl, mono- or di-lower alkylaminoalkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene, (ii) hydroxyl, cycloalkoxy, lower alkoxy or lower alkoxy which is substituted by lower alkoxy, amino or amino substituted by lower alkyl, amino-lower alkyl, mono- or di-lower alkylamino-alkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene, or (iii) amino or amino substituted by lower alkyl, cycloalkyl, amino-lower alkyl, mono- or di-lower alkylaminoalkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene; X1 is methyelene, ethylene, a direct bond, a free or ketalized carbonyl group or a free or etherified hydroxymethylene group and n is 0 or 1, and their salts, processes for the preparation of the compounds according to the invention, pharmaceutical compositions containing these and their use as pharmaceutical active ingredients.

3. 发明公开

EP1037876A1 BIPHENYL DERIVATIVES AS PHARMACEUTICALS 审中-公开
标题翻译：联苯作为药品
公开(公告)号：EP1037876A1
公开(公告)日：2000-09-27
申请号：EP98958884.3
申请日：1998-10-30
申请人： Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
发明人： POMBO VILLAR, Esteban , KOLLER, Manuel , OFNER, Silvio , SWOBODA, Robert
IPC分类号： C07D211/70 , C07D211/22 , C07C211/29 , C07D207/08 , C07D491/18 , A61K31/40 , A61K31/445
CPC分类号： C07D295/096 , C07C211/29 , C07C217/60 , C07D211/22 , C07D211/70
摘要： Compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the description, are useful as pharmaceuticals.

4. 发明公开

EP2516439A1 DIAZA-SPIRO[5.5]UNDECANES AS OREXIN RECEPTOR ANTAGONISTS 有权
标题翻译： DIAZA-SPIRO [5.5] UNDECANE ALS OREXINREZEPTORANTAGONISTEN
公开(公告)号：EP2516439A1
公开(公告)日：2012-10-31
申请号：EP10805703.5
申请日：2010-12-20
申请人： Novartis AG
发明人： BADIGER, Sangamesh , BEHNKE, Dirk , BETSCHART, Claudia , CHAUDHARI, Vinod , COTESTA, Simona , HINRICHS, Jürgen Hans-Hermann , OFNER, Silvio , PANDIT, Chetan , WAGNER, Jürgen
IPC分类号： C07D471/10 , A61K31/438 , A61P25/00
CPC分类号： C07D471/10
摘要： The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

5. 发明授权

EP2516439B1 DIAZA-SPIRO[5.5]UNDECANES AS OREXIN RECEPTOR ANTAGONISTS 有权
标题翻译：氮杂 - 螺[5.5]十一烷ALS食欲素受体拮抗剂
公开(公告)号：EP2516439B1
公开(公告)日：2014-01-22
申请号：EP10805703.5
申请日：2010-12-20
申请人： Novartis AG
发明人： BADIGER, Sangamesh , BEHNKE, Dirk , BETSCHART, Claudia , CHAUDHARI, Vinod , COTESTA, Simona , HINRICHS, Jürgen Hans-Hermann , OFNER, Silvio , PANDIT, Chetan , WAGNER, Jürgen
IPC分类号： C07D471/10 , A61K31/438 , A61P25/00
CPC分类号： C07D471/10

6. 发明授权

EP1773788B8 Quinazoline derivatives 有权
标题翻译：喹唑啉衍生物
公开(公告)号：EP1773788B8
公开(公告)日：2013-01-09
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

7. 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.

8. 发明公开

EP2655326A1 4- (HETERO) ARYL - ETHYNYL - OCTAHYDRO - INDOLE - 1 - CARBOXYLIC ACID ESTERS 审中-公开
标题翻译： 4-（异丙基） - 乙基 - 乙烯基 - 甲氧基 - 吲哚-1-碳三烯
公开(公告)号：EP2655326A1
公开(公告)日：2013-10-30
申请号：EP11802917.2
申请日：2011-12-19
申请人： Novartis AG
发明人： CARCACHE, David , GASPARINI, Fabrizio , KOLLER, Manuel , OFNER, Silvio , ORAIN, David , RENAUD, Johanne
IPC分类号： C07D209/08 , C07D401/06 , C07D417/06 , A61K31/404 , A61K31/427 , A61K31/4439 , A61P25/00 , A61P13/02 , A61P1/00
CPC分类号： C07D209/08 , A61K31/403 , A61K31/427 , A61K31/4439 , A61K45/06 , C07D401/06 , C07D401/08 , C07D417/06 , C07D417/08
摘要： The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.

9. 发明公开

EP2632924A1 DIAZA-SPIRO[5.5]UNDECANES USEFUL AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译： DIAZA-SPIRO [5.5] UNDECANE ASL OREXINREZEPTORANTAGONISTEN
公开(公告)号：EP2632924A1
公开(公告)日：2013-09-04
申请号：EP11779607.8
申请日：2011-10-25
申请人： Novartis AG
发明人： BADIGER, Sangamesh , BEHNKE, Dirk , BETSCHART, Claudia , COTESTA, Simona , HINTERMANN, Samuel , OFNER, Silvio , PANDIT, Chetan , ROY, Bernard Lucien
IPC分类号： C07D471/10 , C07D519/00 , A61K31/438 , A61P25/00
CPC分类号： C07D471/10 , A61K31/444 , A61K31/506 , A61K45/06 , C07D519/00
摘要： The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译：本发明涉及式I化合物，其中取代基如说明书中所定义; 游离形式或盐形式; 用于其制备，用作药物和包含它的药物。

10. 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.

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