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1. 发明申请

WO2004087684A1 BENZO[1,2,5]OXADIAZOLES AND BENZO [1,2,5]THIADIAZOLES USEFUL AS HISTOPATHOLOGICAL STAINING AGENTS, IMAGING AGENTS AND BIOMARKERS 审中-公开
标题翻译：苯并[1,2,5]氧化氮和苯甲[1,2,5]噻吗啉有利于组织病理学染色剂，成像剂和生物标志物
公开(公告)号：WO2004087684A1
公开(公告)日：2004-10-14
申请号：PCT/EP2004/003517
申请日：2004-04-02
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , HINTERMANN, Samuel , ZIMMERMANN, Kaspar
发明人： AUBERSON, Yves , HINTERMANN, Samuel , ZIMMERMANN, Kaspar
IPC分类号： C07D271/12
CPC分类号： C07D271/12 , A61K47/6813 , C07D285/14
摘要： The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R 1 is 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2- 18 F-ethylamino)- thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R 2 is NHCH 3 , NH 11 CH 3 , N(CH 3 ) 11 CH 3 , N(CH 3 ) 2 , N( 11 CH 3 ) 2 , NH(CH 2 ) n F, NH(CH 2 ) n 18 F, N(CH 3 )(CH 2 ) n F, N(CH 3 )-(CH 2 ) n 18 F, O-(CH 2 ) n F, O-(CH 2 ) n 18 F, CONH(CH 2 )nF or CONH(CH 2 ) n 18 F (n being in each case 2 to 4) and R 3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.
摘要翻译：本发明涉及式（I）的新的苯并[1,2,5]恶二唑和苯并[1,2,5]噻二唑，其中X是O或S，R 1是5-（2-氟 - 乙基氨基） - 噻唑 -2-基，其中Y是CH或N，R 2是NHCH 3，NH 11 CH 3，N（C 1-6烷基， CH 3）CH 2，N（CH 3）2，NH（CH 2）n F，NH（CH 2）n 18 F，N（CH 3）） - （CH 2）n 18 F，O-（CH 2）n F，O-（CH 2）n 18 F，CONH（CH 2）n F或CONH（CH 2）n 18 F（n分别为 2〜4），R3为羟基，（C1-4）烷氧基，氢或硝基，为游离碱或酸加成盐形式; 它们的制备，它们在诊断中的用途和含有它们的组合物。

2. 发明申请

WO2003015780A3 ISOXAZOLOPYRIDINONES AND USE THEREOF IN THE TREATMENT OF PARKINSON'S DISEASE 审中-公开
公开(公告)号：WO2003015780A3
公开(公告)日：2003-02-27
申请号：PCT/EP2002/009134
申请日：2002-08-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , HINTERMANN, Samuel , HENGERER, Bastian , VON KROSIGK, Ulrike
发明人： HINTERMANN, Samuel , HENGERER, Bastian , VON KROSIGK, Ulrike
IPC分类号： A61K31/437
摘要： The invention provides compounds of formula I , wherein X, Y, R 1 , R 2 , and R 3 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals for the treatment of perkinson's disease.

3. 发明申请

WO2004072050A1 HETEROCYCLIC COMPOUNDS USEFUL AS NURR-1 ACTIVATORS 审中-公开
标题翻译：杂环化合物可用作N-1个活化剂
公开(公告)号：WO2004072050A1
公开(公告)日：2004-08-26
申请号：PCT/EP2004/001372
申请日：2004-02-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , HINTERMANN, Samuel , HENGERER, Bastian
发明人： HINTERMANN, Samuel , HENGERER, Bastian
IPC分类号： C07D261/02
CPC分类号： C07D271/06 , C07D261/08 , C07D263/32 , C07D413/04
摘要： The present invention relates to compounds of formula (I) : wherein R 1 is hydroxy, C 1-4 alkoxy ,amino, C 1-4 alkyl-amino, di C 1-4 alkylamino , benzyloxy or C 2- C 7 alkanoyl, R 2 is C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkoxy C 1-4 alkoxy, CF 3 , halogen, C 1-4 alkylamino, di C 1-4 alkylamino, di C 1-4 alkylamino C 1-4 alkoxy or N-C 1-4 alkoxy C 1-4 alkyl-N-C 1-4 alkylamino, N-C 1-4 alkyl-piperazinyl, morpholinyl or pyrrolidinyl-C 1-4 alkoxy, wherein the C 1-4 alkyl radicals in R 2 are optionally further substituted by C 1-4 alkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) R 1 is not hydroxy or C 1-4 alkoxy when R 2 is CF 3 , X is O, Y is CH, Z is N and W is CH, (b) R 1 is not hydroxy or C 1-4 alkoxy when R 2 is CF 3 or chloro, X is N, Y is O, Z is CH and W is CH, (c) R 1 is not hydroxy when R 2 is CF 3 , X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）化合物：其中R1是羟基，C1-4烷氧基，氨基，C1-4烷基 - 氨基，二C1-4烷基氨基，苄氧基或C2-C7烷酰基，R2是C1-4烷基，C 1-4烷氧基，C 1-4烷氧基C 1-4烷氧基，CF 3，卤素，C 1-4烷基氨基，二C 1-4烷基氨基，二C 1-4烷基氨基C 1-4烷氧基或N-C 1-4烷氧基C 1-4烷基-N C 1-4烷基氨基，N-C 1-4烷基 - 哌嗪基，吗啉基或吡咯烷基-C 1-4烷氧基，其中R 2中的C 1-4烷基任选进一步被C 1-4烷基，卤素，氰基，氨基，烷氧基或烷硫基，X为N或O，Y为N，O或CH，Z为N或CH，W为N或CH，条件是（a）当R 2为CF 3时，R 1不为羟基或C 1-4烷氧基，X 是O，Y是CH，Z是N，W是CH，（b）当R 2是CF 3或氯时，R 1不是羟基或C 1-4烷氧基，X是N，Y是O，Z是CH，W是CH，（c）当R 2为CF 3时，R 1不为羟基，X为O，Y为N，Z为CH且W为CH，（d）X和Y不同时为O，它们的制备，它们的用途和含有它们的药物组合物。

4. 发明申请

WO2008028958A1 CYCLIC SULFONES USEFUL AS MITOCHONDRIAL SODIUM-CALCIUM EXCHANGERS 审中-公开
标题翻译：循环硫磺有助于作为麻醉钠钙交换剂
公开(公告)号：WO2008028958A1
公开(公告)日：2008-03-13
申请号：PCT/EP2007/059394
申请日：2007-09-07
申请人： NOVARTIS AG , HINTERMANN, Samuel , CHIESI, Michele
发明人： HINTERMANN, Samuel , CHIESI, Michele
IPC分类号： C07D281/10 , A61K31/554 , A61P3/00 , A61P25/00 , A61P9/00
CPC分类号： C07D281/10
摘要： The invention relates to novel heterocyclic compounds of the formula ( I ), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及式（I）的新型杂环化合物，其游离碱形式或酸加成盐形式，用于制备它们作为药物和包含它们的药物的用途。

5. 发明申请

WO2002076968A1 MALONATES AS INHIBITORS OF THE ICE/CED-6 FAMILY OF CYSTEINE PROTEASES 审中-公开
标题翻译：作为ICE / CED-6家族蛋白家族的抑制剂的雄激素
公开(公告)号：WO2002076968A1
公开(公告)日：2002-10-03
申请号：PCT/EP2002/003194
申请日：2002-03-21
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , ROGGO, Silvio , HINTERMANN, Samuel , RASETTI, Vittorio , VON KROSIGK, Ulrike
发明人： ROGGO, Silvio , HINTERMANN, Samuel , RASETTI, Vittorio , VON KROSIGK, Ulrike
IPC分类号： C07D307/20
CPC分类号： C07D295/185 , C07C237/22 , C07C311/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2603/74 , C07D295/32 , C07F9/46
摘要： The invention provides compounds of formula I, wherein Q, R, S, T, U, V, X and Y are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.
摘要翻译：本发明提供式I化合物，其中Q，R，S，T，U，V，X和Y如说明书中所定义，及其制备。式I的化合物可用作药物。

6. 发明申请

WO2012055888A1 DIAZA-SPIRO[5.5]UNDECANES USEFUL AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译： DIAZA-SPIRO [5.5]有机质作为OREXIN受体拮抗剂
公开(公告)号：WO2012055888A1
公开(公告)日：2012-05-03
申请号：PCT/EP2011/068689
申请日：2011-10-25
申请人： NOVARTIS AG , BADIGER, Sangamesh , BEHNKE, Dirk , BETSCHART, Claudia , COTESTA, Simona , HINTERMANN, Samuel , OFNER, Silvio , PANDIT, Chetan , ROY, Bernard Lucien
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; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

7. 发明申请

WO2015010641A1 SUBSTITUTED QUINAZOLIN-4-ONE DERIVATIVES 审中-公开
标题翻译：取代的喹唑啉-4-酮衍生物
公开(公告)号：WO2015010641A1
公开(公告)日：2015-01-29
申请号：PCT/CN2014/082946
申请日：2014-07-24
申请人： NOVARTIS AG , DU, Zhenxing , HINTERMANN, Samuel , HURTH, Konstanze , JACQUIER, Sebastien , LEHMANN, Hansjoerg , MOEBITZ, Henrik , SOLDERMANN, Nicolas , STOJANOVIC, Aleksandar
发明人： DU, Zhenxing , HINTERMANN, Samuel , HURTH, Konstanze , JACQUIER, Sebastien , LEHMANN, Hansjoerg , MOEBITZ, Henrik , SOLDERMANN, Nicolas , STOJANOVIC, Aleksandar
IPC分类号： C07D401/14 , C07D403/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D473/16 , C07D487/04 , C07D513/04 , A61K31/536 , A61K31/52 , A61K31/53 , A61P37/00 , A61P35/00 , A61P33/00
CPC分类号： C07D403/14 , A61K31/517 , A61K31/52 , C07D401/14 , C07D417/14 , C07D473/16
摘要： Provided are substituted quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein R 1 ,R 2 ,R 3 ,R 5 ,R 6 and L are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the class I PI3K kinases.
摘要翻译：提供式（I）的取代喹唑啉-4-酮化合物和/或其药学上可接受的盐和/或溶剂合物，其中R1，R2，R3，R5，R6和L如说明书中所定义。这些化合物适用于治疗由I型PI3K激酶的活性介导的病症或疾病。

8. 发明申请

WO2014128612A1 QUINAZOLIN-4-ONE DERIVATIVES 审中-公开
标题翻译：喹唑啉-4-酮衍生物
公开(公告)号：WO2014128612A1
公开(公告)日：2014-08-28
申请号：PCT/IB2014/059071
申请日：2014-02-18
申请人： NOVARTIS AG , GUIBOURDENCHE, Christel , HINTERMANN, Samuel , HURTH, Konstanze , JACQUIER, Sébastien , KALIS, Christoph , MOEBITZ, Henrik , SOLDERMANN, Nicolas
发明人： GUIBOURDENCHE, Christel , HINTERMANN, Samuel , HURTH, Konstanze , JACQUIER, Sébastien , KALIS, Christoph , MOEBITZ, Henrik , SOLDERMANN, Nicolas
IPC分类号： C07D401/14 , C07D403/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D473/16 , C07D473/34 , C07D487/04 , C07D513/04 , A61K31/517 , A61K31/52 , A61K31/53 , A61P37/00 , A61P35/00 , A61P33/00
CPC分类号： C07D401/14 , C07D403/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D473/16 , C07D473/34 , C07D487/04 , C07D513/04
摘要： The invention relates to quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, Formula (I) wherein R 1 , R 2 , R 3 , R 5 , R 6 and L are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the class I PI3K kinases.
摘要翻译：本发明涉及式（I）的喹唑啉-4-酮化合物和/或其药学上可接受的盐和/或溶剂合物，式（I）其中R 1，R 2，R 3，R 5，R 6和L如说明书中所定义。这些化合物适用于治疗由I型PI3K激酶的活性介导的病症或疾病。

9. 发明申请

WO2010086366A1 4-ARYL-BUTANE-1,3-DIAMIDES 审中-公开
标题翻译： 4-芳基 - 丁烷-1,3-二酰胺
公开(公告)号：WO2010086366A1
公开(公告)日：2010-08-05
申请号：PCT/EP2010/050991
申请日：2010-01-28
申请人： NOVARTIS AG , BEHNKE, Dirk , BETSCHART, Claudia , COTESTA, Simona , GERSPACHER, Marc , HINTERMANN, Samuel , ROY, Bernard Lucien , VON MATT, Anette , WAGNER, Jürgen
发明人： BEHNKE, Dirk , BETSCHART, Claudia , COTESTA, Simona , GERSPACHER, Marc , HINTERMANN, Samuel , ROY, Bernard Lucien , VON MATT, Anette , WAGNER, Jürgen
IPC分类号： C07C233/78 , C07D207/34 , C07D209/08 , C07D213/81 , C07D215/48 , C07D215/50 , C07D235/24 , C07D277/56 , C07D307/79 , C07D317/68 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12
CPC分类号： C07C233/78 , C07D207/416 , C07D209/08 , C07D213/81 , C07D215/48 , C07D215/50 , C07D217/26 , C07D233/66 , C07D235/24 , C07D277/56 , C07D307/79 , C07D317/68 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; m 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; m形式或盐形式; 作为其制备，用作药物和包含它的药物。

10. 发明申请

WO2011073316A1 4-ARYL-BUTANE-1,3-DIAMIDES 审中-公开
标题翻译： 4-芳基 - 丁烷-1,3-二酰胺
公开(公告)号：WO2011073316A1
公开(公告)日：2011-06-23
申请号：PCT/EP2010/069889
申请日：2010-12-16
申请人： NOVARTIS AG , BETSCHART, Claudia , COTESTA, Simona , HINTERMANN, Samuel , WAGNER, Jürgen , ROY, Bernard, Lucien , GERSPACHER, Marc , VON MATT, Anette , BEHNKE, Dirk
发明人： BETSCHART, Claudia , COTESTA, Simona , HINTERMANN, Samuel , WAGNER, Jürgen , ROY, Bernard, Lucien , GERSPACHER, Marc , VON MATT, Anette
IPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/048 , C07D513/04 , A61K31/4184 , A61K31/4188 , A61K31/416 , A61K31/47 , A61K31/437 , A61P25/00
CPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/048 , C07D513/04
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）的化合物：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。

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