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61. 发明授权

EP1521749B8 PHENYL-(4-(3-PHENYL-1H-PYRAZOL-4-YL)-PYRIMIDIN-2-Yl)-AMINE DERIVATIVES 有权
标题翻译：苯基 - （4-（3-苯基-1H-吡唑-4-基） - 嘧啶-2-基）AMINDERIVATE
公开(公告)号：EP1521749B8
公开(公告)日：2010-12-22
申请号：EP03762663.7
申请日：2003-07-08
申请人： Novartis AG
发明人： FURET, Pascal , IMBACH, Patricia , RAMSEY, Timothy, Michael , SCHLAPBACH, Achim , SCHOLZ, Dieter , CARAVATTI, Giorgio
IPC分类号： C07D403/04 , A61K31/505
CPC分类号： C07D403/04 , A61K31/505

62. 发明公开

EP2004653A1 3-SUBSTITUTED N-(ARYL- OR HETEROARYL)-PYRAZO[1,5-a]PYRIMIDINES AS KINASE INHIBITORS 有权
标题翻译： 3-取代的N-（芳基 - 或杂芳基）吡唑并[1,5-A]嘧啶类作为激酶抑制剂的
公开(公告)号：EP2004653A1
公开(公告)日：2008-12-24
申请号：EP07723895.4
申请日：2007-04-02
申请人： NOVARTIS AG
发明人： MASUYA, Keiichi , VAUPEL, Andrea , IMBACH, Patricia , FURET, Pascal
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to 3-substituted N-(aryl- or heteroaryl)-pyrazolo[1 ,5-a]pyrimidine compounds, their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warmblooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.

63. 发明公开

EP1173413A1 USE OF 2,4-DIAMINO-3-HYDROXYCARBOXYLIC ACID DERIVATIVES AS PROTEASOME INHIBITORS 有权
标题翻译： 2,4-二氨基-3-HYDROXYCARBOXYLSÄUREDERIVATEALS蛋白酶体抑制剂
公开(公告)号：EP1173413A1
公开(公告)日：2002-01-23
申请号：EP00927038.0
申请日：2000-04-25
申请人： Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
发明人： FRANCE, Dennis , FÜRST, Peter , ZIMMERMANN, Johann , GARCIA-ECHEVERRIA, Carlos , SCHOLZ, Dieter , FURET, Pascal , IMBACH, Patricia
IPC分类号： C07C271/22 , A61P43/00 , A61K31/325
CPC分类号： C07C271/22 , Y02P20/55
摘要： The present invention relates to the new use of 2,4-diamino-3-hydroxycarboxylic acids of formula (I), in which A and B independently represent a bond or an unsubstituted or substituted amino acyl moiety; R1 represents hydrogen; an amino protecting group; or a group of formula R5Y- wherein R5 represents hydrogen or an unsubstituted or substituted alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl group; and Y represents -CO-; -NH-CO-; -NH-CS-; -SO2-; -O-CO-; or -O-CS-; R2 represents the side chain of a natural amino acid; an alkyl, arylalkyl, heteroarylalkyl or cycloalkylalkyl group; or trimethylsilylmethyl, 2-thienylmethyl or styrylmethyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; and R4 represents 2(R)-hydroxyindan-1(S)-yl; (S)-2-hydroxy-1-phenylethyl; or 2-hydroxy-benzyl unsubstituted or substituted in 4-position by methoxy; in the manufacture of a pharmaceutical composition for the treatment of a proliferative disease, e.g. of a solid tumor; to a method of treatment of warm-blooded animals; and to 2,4-diamino-3-hydroxycarboxylic acids of formula (I*), wherein A and B independently represent an unsubstituted or substituted amino acyl moiety; R2 represents arylalkyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; R4 represents 2-hydroxy-benzyl unsubstituted or substituted in 4 position by methoxy; and R5 represents arylalkyl and Y represents -CO-; or R5 represents alkyl substituted by cycloalkyl, naphthyl, pyridyl or phenyl in which phenyl is substituted by alkyl or amino; and Y represents -O-CO; pharmaceutically acceptable salts thereof; and the use of such compounds of formula (I*) for the therapeutic treatment of the human or animal body, especially the treatment of proliferative diseases.

64. 发明公开

EP1153024A1 2-AMINO-6-ANILINO-PURINES AND THEIR USE AS MEDICAMENTS 有权
标题翻译： 2-氨基-6-苯胺基嘌呤及其作为药物的用途
公开(公告)号：EP1153024A1
公开(公告)日：2001-11-14
申请号：EP00916840.2
申请日：2000-02-16
申请人： Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
发明人： IMBACH, Patricia , CAPRARO, Hans-Georg , ZIMMERMANN, Jürg , CARAVATTI, Giorgio , FURET, Pascal , BRILL, Wolfgang, Karl-Diether
IPC分类号： C07D473/16 , C07D473/40 , A61K31/52 , A61P35/00
CPC分类号： C07D473/16 , C07D473/40
摘要： 2-Amino-6-anilino-purine derivatives of formula (I) in which R1 is -S(O)k-NR6R7 or-N(aryl lower alkyl) carbamoyl or -NH-S(O)i-R8 or -NH-C(O)-R9; 9 is 1-5; These compounds inhibit p34cdc2/cyclin Bcdc13 kinase and protein tyrosine kinase pp60c-src and can be used for treatment of hyperproliferative diseases, for example tumour diseases, and diseases which respond to inhibition of the activity of protein tyrosine kinase pp60c-src, in particular osteoporosis.

65. 发明公开

EP0874846A1 PURINE DERIVATIVES AND PROCESSES FOR THEIR PREPARATION 失效
标题翻译：嘌呤衍生物及其制备方法
公开(公告)号：EP0874846A1
公开(公告)日：1998-11-04
申请号：EP96934774.0
申请日：1996-10-22
申请人： Novartis AG
发明人： ZIMMERMANN, Jürg , CAPRARO, Hans-Georg , IMBACH, Patricia , FURET, Pascal
IPC分类号： A61K31 , A61P35 , C07D473
CPC分类号： C07D473/16
摘要： 2-Amino-6-anilino-purine derivatives of formula (1) in which the symbols are as defined in claim 1, are described. These compounds inhibit p34cdc2/cyclin Bcdc13 kinase and can be used for treatment of hyperproliferative diseases, for example tumour diseases.

66. 发明公开

EP0819129A1 PYRAZOLE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF 失效转让
标题翻译：吡唑衍生物和方法及其
公开(公告)号：EP0819129A1
公开(公告)日：1998-01-21
申请号：EP96909115.0
申请日：1996-03-22
申请人： Novartis AG
发明人： TRAXLER, Peter , FURET, Pascal , BOLD, Guido , FREI, Jörg , LANG, Marc
IPC分类号： C07D231 , A61K31 , A61P35 , A61P43 , C07D487
CPC分类号： C07D487/04
摘要： 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula (I) wherein the symbols are as defined in claim (1), and intermediates for their manufacture are described. The compounds of formula (I) inhibit especially the tyrosine kinase activity of the receptor for epidermal growth factor and can be used, for example, in the case of epidermal hyperproliferation (psoriasis) and as anti-tumour agents.

67. 发明公开

EP4237417A1 INTERLEUKIN-17 INHIBITORS 审中-实审
公开(公告)号：EP4237417A1
公开(公告)日：2023-09-06
申请号：EP21801650.9
申请日：2021-11-01
申请人： Novartis AG
发明人： TROXLER, Thomas Josef , ORAIN, David , FURET, Pascal , WEIGAND, Klaus , SCHLAPBACH, Achim
IPC分类号： C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D487/04 , A61K31/4427 , A61P17/02 , A61P17/06 , A61P37/00

69. 发明授权

EP2790705B1 USE OF INHIBITORS OF THE ACTIVITY OR FUNCTION OF PI3K 有权
标题翻译：使用PI3K的活性或功能的抑制剂
公开(公告)号：EP2790705B1
公开(公告)日：2017-12-06
申请号：EP12818825.7
申请日：2012-12-14
申请人： Novartis AG
发明人： COOKE, Nigel Graham , FERNANDES GOMES DOS SANTOS, Paulo Antonio , FURET, Pascal , HEBACH, Christina , HÖGENAUER, Klemens , HOLLINGWORTH, Gregory , KALIS, Christoph , LEWIS, Ian , SMITH, Alexander Baxter , SOLDERMANN, Nicolas , STAUFFER, Frédéric , STRANG, Ross , STOWASSER, Frank , TUFILLI, Nicola , VON MATT, Anette , WOLF, Romain , ZECRI, Frédéric
IPC分类号： A61K31/517 , A61K31/519 , A61P33/00
CPC分类号： A61K31/519 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K31/551 , C07D239/74 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/14 , C07D487/08 , Y02A50/409 , Y02A50/411 , Y02A50/414
摘要： The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.

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