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1. 发明申请

WO2008148867A3 QUINOXALINE DERIVATIVES AS INHIBITORS OF THE TYROSINE KINASE ACTIVITY OF JANUS KINASES 审中-公开
公开(公告)号：WO2008148867A3
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057058
申请日：2008-06-06
申请人： NOVARTIS AG , GERSPACHER, Marc , FURET, Pascal , VANGREVELINGHE, Eric , PISSOT SOLDERMANN, Carole , GAUL, Christoph , HOLZER, Philipp
发明人： GERSPACHER, Marc , FURET, Pascal , VANGREVELINGHE, Eric , PISSOT SOLDERMANN, Carole , GAUL, Christoph , HOLZER, Philipp
IPC分类号： A61K31/498 , A61K31/5377 , A61K31/541 , C07D241/42 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/14 , A61P35/00 , A61P35/02 , A61P21/00 , A61P17/06 , A61P17/00 , A61P19/02
摘要： The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R; R2 is caryl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8 R3, R4, and R5 are each independently hydrogen or R9; R6 is hydrogen; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases.

2. 发明申请

WO2009098236A1 PYRROLO [2, 3-D] PYRIDINES AND USE THEREOF AS TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：吡咯并[2,3-D]吡啶并以其作为酪氨酸激酶抑制剂的用途
公开(公告)号：WO2009098236A1
公开(公告)日：2009-08-13
申请号：PCT/EP2009/051281
申请日：2009-02-04
申请人： NOVARTIS AG , GAUL, Christoph , GERSPACHER, Marc , HOLZER, Philipp , PISSOT SOLDERMANN, Carole
发明人： GAUL, Christoph , GERSPACHER, Marc , HOLZER, Philipp , PISSOT SOLDERMANN, Carole
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The invention relates to compounds of formula (I) and salts thereof formula (I), wherein the substituens are as defined in the specification, processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
摘要翻译：本发明涉及式（I）化合物及其式（I）的盐，其中取代基如说明书中所定义，其制备方法; 涉及含有这些化合物的药物，特别是用于一种或多种蛋白质酪氨酸激酶介导的疾病。

3. 发明申请

WO2011076786A1 SUBSTITUTED ISOQUINOLINONES AND QUINAZOLINONES 审中-公开
标题翻译：取代的异喹啉和喹唑啉酮
公开(公告)号：WO2011076786A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070364
申请日：2010-12-21
申请人： NOVARTIS AG , BERGHAUSEN, Joerg , BUSCHMANN, Nicole , FURET, Pascal , GESSIER, François , HERGOVICH LISZTWAN, Joanna , HOLZER, Philipp , JACOBY, Edgar , KALLEN, Joerg , MASUYA, Keiichi , PISSOT SOLDERMANN, Carole , REN, Haixia , STUTZ, Stefan
发明人： BERGHAUSEN, Joerg , BUSCHMANN, Nicole , FURET, Pascal , GESSIER, François , HERGOVICH LISZTWAN, Joanna , HOLZER, Philipp , JACOBY, Edgar , KALLEN, Joerg , MASUYA, Keiichi , PISSOT SOLDERMANN, Carole , REN, Haixia , STUTZ, Stefan
IPC分类号： A61P35/00 , A61K31/495 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D405/14 , C07D413/14 , C07D217/24
CPC分类号： C07D239/82 , C07D217/24 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I): wherein Z is CH 2 or N-R 4 and X, R 1 , R 2 , R 4 , R 6 , R 7 and n 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 MDM2 and/or MDM4, or variants thereof.
摘要翻译：本发明涉及式（I）的取代的含氮双环杂环：其中Z是CH 2或N-R 4，X，R 1，R 2，R 4，R 6，R 7和n如说明书中所定义。这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。

4. 发明申请

WO2006034833A1 CYCLIC DIARLY UREAS SUITABLE AS TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：适用于酪氨酸激酶抑制剂的循环性尿路炎
公开(公告)号：WO2006034833A1
公开(公告)日：2006-04-06
申请号：PCT/EP2005/010408
申请日：2005-09-27
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , CARAVATTI, Giorgio , FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, W. , PISSOT SOLDERMANN, Carole , VAUPEL, Andrea
发明人： BOLD, Guido , CARAVATTI, Giorgio , FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, W. , PISSOT SOLDERMANN, Carole , VAUPEL, Andrea
IPC分类号： C07D401/12 , C07D403/12 , A61K31/505 , A61K31/506 , A61P35/00 , C07D407/12 , C07D417/12 , C07D413/12 , C07D409/12
CPC分类号： C07D417/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D417/14
摘要： The invention relates to novel compounds of Formula (I): wherein p is 1, 2 or 3; n is 0, 1, 2 or 3; mis0,1,2or3; A is CR c , S, NR c or O, where R c is H or lower alkyl; X, Y and Z are each independently selected fro N or C-R 3 , wherein at least two of X, Y and Z are N; and each R a is independently selected from hydrogen and lower-alkyl; each R b is hydrogen or lower-alkyl; G is a group Ar or represents CN or unsubstituted or substituted lower alkyl; Ar is a saturated or unsaturated cyclic group, which is substituted or unsubstituted and maybe a five or six membered monocyclic or a 8, 9, 10, 11 or 12 membered bicyclic or tricyclic ring and may contain 0, 1, 2 or 3 heteroatoms selected from O, N and S; and wherein the radicals have R 1 , R 2 , R 3 and R 4 have the meanings as defined herein, to salts, esters, N-oxides or prodrugs thereof; and their use in the treatment of protein kinase dependent diseases, their use in the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diaryl urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.
摘要翻译：本发明涉及新的式（I）化合物：其中p为1,2或3; n为0,1,2或3; mis0,1,2or3; A是CR

5. 发明申请

WO2007104538A1 HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES 审中-公开
标题翻译：作为杀虫剂的杀生物剂
公开(公告)号：WO2007104538A1
公开(公告)日：2007-09-20
申请号：PCT/EP2007/002213
申请日：2007-03-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , VAUPEL, Andrea , PISSOT SOLDERMANN, Carole , MANLEY, Paul, W.
发明人： BOLD, Guido , VAUPEL, Andrea , PISSOT SOLDERMANN, Carole , MANLEY, Paul, W.
IPC分类号： C07D239/30 , C07D239/34 , C07D239/36 , C07D239/42 , C07D239/46 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/06 , A61K31/495 , A61P35/00
CPC分类号： C07D413/12 , C07D239/34 , C07D239/36 , C07D239/42 , C07D239/47 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D471/06
摘要： The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
摘要翻译：本发明涉及新的式（I）化合物及其在治疗动物或人体中的用途，包括式（I）化合物的药物组合物和式（I）化合物在制备中的用途用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病，特别是肿瘤疾病的药物组合物。

6. 发明申请

WO2006059234A2 BICYCLIC AMIDES AS KINASE INHIBITORS 审中-公开
标题翻译：双酚A作为激酶抑制剂
公开(公告)号：WO2006059234A2
公开(公告)日：2006-06-08
申请号：PCT/IB2005/004030
申请日：2005-09-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , CAPRARO, Hans-georg , CARAVATTI, Giorgio , FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, W. , VAUPEL, Andrea , PISSOT SOLDERMANN, Carole , GESSIER, François , SCHNELL, Christian , LITTLEWOOD-EVANS, Amanda, Jane , KAPA, Prasad Koteswara , BAJWA, Joginder, S. , JIANG, Xinglong
发明人： BOLD, Guido , CAPRARO, Hans-georg , CARAVATTI, Giorgio , FLOERSHEIMER, Andreas , FURET, Pascal , MANLEY, Paul, W. , VAUPEL, Andrea , PISSOT SOLDERMANN, Carole , GESSIER, François , SCHNELL, Christian , LITTLEWOOD-EVANS, Amanda, Jane , KAPA, Prasad Koteswara , BAJWA, Joginder, S. , JIANG, Xinglong
IPC分类号： C07D403/12 , C07D413/12 , C07D239/46 , A61K31/505
CPC分类号： C07D239/47 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
摘要翻译：本发明涉及式（I）化合物及其在治疗动物或人体中的用途，包括式I化合物的药物组合物和式I化合物用于制备药物组合物的用途用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病，特别是肿瘤疾病。

7. 发明申请

WO2015181747A1 NOVEL PYRAZOLO PYRIMIDINE DERIVATIVES AND THEIR USE AS MALT1 INHIBITORS 审中-公开
标题翻译：新型吡咯并吡啶衍生物及其作为MALT1抑制剂的用途
公开(公告)号：WO2015181747A1
公开(公告)日：2015-12-03
申请号：PCT/IB2015/053975
申请日：2015-05-27
申请人： NOVARTIS AG , PISSOT SOLDERMANN, Carole , QUANCARD, Jean , SCHLAPBACH, Achim , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , ZOLLER, Thomas
发明人： PISSOT SOLDERMANN, Carole , QUANCARD, Jean , SCHLAPBACH, Achim , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , ZOLLER, Thomas
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377
摘要： The present invention describes new pyrazolo-pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein, R1 is halogen, cyano, or C 1 -C 3 alkyl optionally substituted by halogen; R2 is C 1 -C 6 alkyl optionally substituted one or more times by C 1 -C 6 alkyl, C 2 -C 6 alkenyl, hydroxyl, N,N-di-C 1 -C 6 alkyl amino, N-mono-C 1 -C 6 alkyl amino, O-Rg, Rg, phenyl, or by C 1 -C 6 alkoxy wherein said alkoxy again may optionally be substituted by C 1 -C 6 alkoxy, N,N-di-C 1 -C 6 alkyl amino, Rg or phenyl; C 3 -C 6 cycloalkyl optionally substituted by C 1 -C 6 alkyl, N,N-di-C 1 -C 6 alkyl amino or C 1 -C 6 alkoxy-C 1 -C 6 alkyl, and/or two of said optional substituents together with the atoms to which they are bound may form an annulated or spirocyclic 4 - 6 membered saturated heterocyclic ring comprising 1 - 2 O atoms; phenyl optionally substituted by C 1 -C 6 alkoxy; a 5 - 6 membered heteroaryl ring having 1 to 3 heteroatoms selected from N and O said ring being optionally substituted by C 1 -C 6 alkyl which may be optionally substituted by amino or hydroxy; Rg; or N,N-di-C 1 -C 6 alkyl amino carbonyl; and R is phenyl independently substituted two or more times by Ra, 2-pyridyl independently substituted one or more times by Rb, 3-pyridyl independently substituted one or more times by Rc, or 4-pyridyl independently substituted one or more times by Rd; which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.
摘要翻译：本发明描述了式（I）的新的吡唑并嘧啶衍生物或其药学上可接受的盐; （I）其中，R 1为卤素，氰基或任选被卤素取代的C 1 -C 3烷基; R2是任选被C 1 -C 6烷基，C 2 -C 6烯基，羟基，N，N-二-C 1 -C 6烷基氨基，N-单-C 1 -C 6烷基氨基，O-R g，R g，苯基，或C 1 -C 6烷氧基，其中所述烷氧基再次可任选被C 1 -C 6烷氧基，N，N-二-C 1烷基氨基，R g或苯基取代; 任选地被C 1 -C 6烷基，N，N-二-C 1 -C 6烷基氨基或C 1 -C 6烷氧基-C 1 -C 6烷基取代的C 3 -C 6环烷基和/或所述任选取代基中的两个与它们所键合的原子一起形成环状或包含1〜2个O原子的螺环4-6元饱和杂环; 任选被C 1 -C 6烷氧基取代的苯基; 具有1至3个选自N和O的杂原子的5-6元杂芳基环，所述环任选被可被氨基或羟基任选取代的C 1 -C 6烷基取代; RG; 或N，N-二-C 1 -C 6烷基氨基羰基; R为独立地被R a取代两次或更多次的苯基，R 2独立地取代一次或多次的2-吡啶基，R c独立地取代一次或多次的3-吡啶基，或被Rd独立地取代一次或多次的4-吡啶基; 其通常与MALT1蛋白水解和/或自发蛋白水解活性相互作用，特别是可能抑制所述活性。本发明还描述了所述新的吡唑并嘧啶衍生物的合成，它们作为药物的用途，特别是通过与MALT1蛋白水解和/或自身蛋白水解活性的相互作用。

8. 发明申请

WO2006000420A1 PYRIMIDINE UREA DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的吡嗪类尿素衍生物
公开(公告)号：WO2006000420A1
公开(公告)日：2006-01-05
申请号：PCT/EP2005/006815
申请日：2005-06-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , IRM LLC , DING, Qiang , GRAY, Nathanael, Schiander , LI, Bing , LIU, Yi , SIM, Taebo , UNO, Tetsuo , ZHANG, Guobao , PISSOT SOLDERMANN, Carole , BREITENSTEIN, Werner , BOLD, Guido , CARAVATTI, Giorgio , FURET, Pascal , GUAGNANO, Vito , LANG, Marc , MANLEY, Paul, W. , SCHOEPFER, Joseph , SPANKA, Carsten
发明人： DING, Qiang , GRAY, Nathanael, Schiander , LI, Bing , LIU, Yi , SIM, Taebo , UNO, Tetsuo , ZHANG, Guobao , PISSOT SOLDERMANN, Carole , BREITENSTEIN, Werner , BOLD, Guido , CARAVATTI, Giorgio , FURET, Pascal , GUAGNANO, Vito , LANG, Marc , MANLEY, Paul, W. , SCHOEPFER, Joseph , SPANKA, Carsten
IPC分类号： C07D239/48
CPC分类号： C07D239/48 , C07D251/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention relates to compounds of formula (I) wherein the substituents X 1 , R 1 , R 2 , R 3 and R 4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.
摘要翻译：本发明涉及式（I）的化合物，其中取代基X 1，R 1，R 2，R 3， SUP＆gt;和R 4具有本发明的描述中阐述和解释的含义，这些化合物的制备方法，含有它们的药物组合物，其用途可任选地与一种或多种用于治疗对蛋白激酶活性的抑制作出反应的疾病的更多其它药物活性化合物，以及治疗这种疾病的方法。

9. 发明申请

WO2007071393A2 SULPHONAMIDOANILINE DERIVATIVES BEING JANUS KINASES INHIBITORS 审中-公开
标题翻译：磺酰胺衍生物是JANUS KINASES抑制剂
公开(公告)号：WO2007071393A2
公开(公告)日：2007-06-28
申请号：PCT/EP2006/012311
申请日：2006-12-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CAPRARO, Hans-Georg , COUPEZ, Bernard , FURET, Pascal , MANLEY, Paul, W. , PISSOT SOLDERMANN, Carole
发明人： CAPRARO, Hans-Georg , COUPEZ, Bernard , FURET, Pascal , MANLEY, Paul, W. , PISSOT SOLDERMANN, Carole
IPC分类号： C07D473/16 , C07D473/18 , C07D487/04 , C07D519/00 , A61K31/5377
CPC分类号： C07D473/16 , C07D473/18 , C07D487/04 , C07D519/00
摘要： The invention relates to sulphonamidoanilines of formula (I) wherein A is N or CH, W, X, Y and Z are N or CH under the proviso that at least one of the three symbols W, X and Y represent CH, R 1 represents NR 4 R 5 or OR 4 , wherein R 4 represents optionally substituted alkyl, optionally substituted cycloalkyl optionally comprising one or two nitrogen or oxygen atoms, or substituted aryl, and R 5 represents hydrogen or unsubstituted or substituted alkyl, or R 4 and R 5 together with the nitrogen to which they are attached represent an optionally substituted five- or six-membered nitrogen containing monocyclic ring, an optionally substituted nitrogen containing fully saturated bicyclic ring, or an spirocyclic fully saturated ring system containing one or two nitrogen atoms, R 2 is hydrogen, lower alkenyl or alkyl, R 3 is alkyl which is unsubstituted or mono-, di- or trisubstituted by halogen; alkenyl or aryl, and their salts; processes for their preparation, their application in the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment of diseases, a method for the treatment of such a disease and the use of such a compound - alone or in combination with one or more other pharmaceutically active compounds - for the manufacture of a pharmaceutical preparation for the treatment of a proliferative disease.
摘要翻译：
本发明涉及式（I）其中A是N或CH，W，X，Y和Z的sulphonamidoanilines是N或CH，条件下，所述三个符号W，X中的至少一个 Y代表CH，R 1代表NR 4 R 5或OR 4，其中R 4 表示任选取代的烷基，任选包含一个或两个氮或氧原子的任选取代的环烷基或取代的芳基，并且R5表示氢或未取代或取代的烷基，或R 4 R 5和它们所连接的氮一起代表任选取代的五元或六元含氮单环，任选取代的含氮完全饱和双环或含有一个或两个氮原子的螺环全饱和环体系，R 2是氢，低级链烯基或烷基，R 3是未取代的或者单 - ，二 - 或三 - trisubstit 被卤素所阻挡; 烯基或芳基，及其盐; 它们的制备方法，它们在人体或动物体的治疗中的应用，单独或与一种或多种其它药物活性化合物组合用于治疗疾病的方法，治疗这种疾病的方法和单独或与一种或多种其它药物活性化合物组合使用这样的化合物用于制备用于治疗增殖性疾病的药物制剂。

10. 发明授权

EP2155201B1 QUINOXALINE DERIVATIVES AS INHIBITORS OF THE TYROSINE KINASE ACTIVITY OF JANUS KINASES 有权
标题翻译：喹喔啉衍生物作为Janus激酶酪氨酸激酶抑制剂
公开(公告)号：EP2155201B1
公开(公告)日：2012-08-01
申请号：EP08760632.3
申请日：2008-06-06
申请人： Novartis AG
发明人： GERSPACHER, Marc , FURET, Pascal , VANGREVELINGHE, Eric , PISSOT SOLDERMANN, Carole , GAUL, Christoph , HOLZER, Philipp
IPC分类号： A61K31/498 , A61K31/5377 , A61K31/541 , C07D241/42 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/14 , A61P35/00 , A61P35/02 , A61P21/00 , A61P17/06 , A61P17/00 , A61P19/02
CPC分类号： A61K31/498 , A61K31/5377 , A61K31/541 , C07D241/42 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14
摘要： The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R; R2 is caryl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8 R3, R4, and R5 are each independently hydrogen or R9; R6 is hydrogen; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases.

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