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41. 发明申请

WO2014072956A1 OXAZOLIDIN-2-ONE-PYRIMIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2014072956A1
公开(公告)日：2014-05-15
申请号：PCT/IB2013/060052
申请日：2013-11-11
申请人： NOVARTIS AG , FAIRHURST, Robin Alec , FURET, Pascal , KALTHOFF, Frank Stephan , LERCHNER, Andreas , RUEEGER, Heinrich
发明人： FAIRHURST, Robin Alec , FURET, Pascal , KALTHOFF, Frank Stephan , LERCHNER, Andreas , RUEEGER, Heinrich
IPC分类号： C07D413/14 , C07D417/14 , A61K31/506 , A61P35/00
CPC分类号： C07D417/14 , A61K31/5377 , A61K45/06 , C07D413/14
摘要： The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
摘要翻译：本发明涉及作为PI3K（磷脂酰肌醇-3-激酶）抑制剂的恶唑烷-2-酮取代的嘧啶化合物及其药物组合物，其制备方法和用于治疗依赖于 PI3K。

42. 发明申请

WO2011157793A1 PIPERIDINYL SUBSTITUTED 1,3-DIHYDRO-BENZOIMIDAZOL-2-YLIDENEAMINE DERIVATIVES 审中-公开
标题翻译：哌啶基取代的1,3-二氢苯并咪唑-2-甲酰胺衍生物
公开(公告)号：WO2011157793A1
公开(公告)日：2011-12-22
申请号：PCT/EP2011/060032
申请日：2011-06-16
申请人： NOVARTIS AG , BERST, Frederic , FURET, Pascal , MARZINZIK, Andreas , STAUFFER, Frédéric
发明人： BERST, Frederic , FURET, Pascal , MARZINZIK, Andreas , STAUFFER, Frédéric
IPC分类号： C07D235/30 , C07D401/04 , A61K31/4184 , A61P5/00
CPC分类号： C07D401/04 , A61K31/454 , A61K31/4545 , A61K45/06 , C07D401/14
摘要： The invention relates to new derivatives of formula (I) wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.
摘要翻译：本发明涉及式（I）的新衍生物，其中取代基如说明书中所定义; 制备此类衍生物的方法; 包含这些衍生物的药物组合物; 这种衍生物作为药物; 用于治疗一种或多种IGF-1R介导的病症或疾病的衍生物。

43. 发明申请

WO2011015652A1 3-HETEROARYLMETHYL-IMIDAZO[1,2-B]PYRIDAZIN-6-YL DERIVATIVES AS C-MET TYROSINE KINASE MODULATORS 审中-公开
标题翻译：作为C-MET酪氨酸激酶调节剂的3-异丙基甲基咪唑并[1,2-B]吡啶-6-基衍生物
公开(公告)号：WO2011015652A1
公开(公告)日：2011-02-10
申请号：PCT/EP2010/061485
申请日：2010-08-06
申请人： NOVARTIS AG , FURET, Pascal , McCARTHY, Clive , SCHOEPFER, Joseph , STUTZ, Stefan
发明人： FURET, Pascal , McCARTHY, Clive , SCHOEPFER, Joseph , STUTZ, Stefan
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to compounds of formula (I) and salts thereof, wherein the substituents are as defined in the specification, the application of a compound of formula (I) in a process for the treatment of the human or animal body, in particular with regard to C-Met tyrosine kinase mediated disease; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharamaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner; processes for the preparation of a compound of formula (I).
摘要翻译：本发明涉及式（I）化合物及其盐，其中取代基如本说明书中所定义，式（I）化合物在治疗人或动物体的方法中的应用，特别是用涉及C-Met酪氨酸激酶介导的疾病; 使用式（I）化合物制备用于治疗这些疾病的药物; 药物组合物，其包含式（I）的化合物，任选地在组合配偶体的存在下; 制备式（I）化合物的方法。

44. 发明申请

WO2008119741A2 3-IMIDAZOLYL-INDOLES FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于治疗增殖性疾病的3-咪唑啉吲哚
公开(公告)号：WO2008119741A2
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053667
申请日：2008-03-27
申请人： NOVARTIS AG , BOETTCHER, Andreas , BUSCHMANN, Nicole , FURET, Pascal , GROELL, Jean-Marc , KALLEN, Jörg , HERGOVICH LISZTWAN, Joanna , MASUYA, Keiichi , MAYR, Lorenz , VAUPEL, Andrea
发明人： BOETTCHER, Andreas , BUSCHMANN, Nicole , FURET, Pascal , GROELL, Jean-Marc , KALLEN, Jörg , HERGOVICH LISZTWAN, Joanna , MASUYA, Keiichi , MAYR, Lorenz , VAUPEL, Andrea
IPC分类号： C07D403/04 , A61K31/4164 , A61P35/00
CPC分类号： C07D403/04
摘要： The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula (I) wherein R 1 , R 2 , R 3 , R 4 , R A , Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.
摘要翻译：本发明涉及能够分别抑制p53或其变体和MDM2和/或MDM4或其变体之间的相互作用的3-杂环基吲哚基化合物，所述具有式（I）的化合物其中R 1， R 2，R 2，R 3，R 4，R A，Y和Y定义如下：规格。由于它们的活性，所述化合物可用于治疗由MDM2和/或MDM4或其变体如炎性或增殖性疾病或保护细胞的活性介导的各种疾病和疾病。

45. 发明申请

WO2007071752A3 PYRIMIDINYL ARYL UREA DERIVATIVES BEING FGF INHIBITORS 审中-公开
公开(公告)号：WO2007071752A3
公开(公告)日：2007-06-28
申请号：PCT/EP2006/070046
申请日：2006-12-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , BOLD, Guido , FURET, Pascal , GUAGNANO, Vito
发明人： BOLD, Guido , FURET, Pascal , GUAGNANO, Vito
IPC分类号： C07D401/04 , C07D239/32 , C07D413/10 , A61K31/506
摘要： The invention relates to heteroaryl aryl ureas of the formula (IA), wherein the radicals and symbols have the meanings as defined herein, the use of such compounds in the treatment of protein kinase dependent diseases; to pharmaceutical preparations comprising said heteroaryl aryl ureas, to processes for the manufacture of such novel compounds and to methods of treatment comprising the use of such heteroaryl aryl ureas.

46. 发明申请

WO2006108640A1 PHENYLACETAMIDES SUITABLE AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：适用于蛋白激酶抑制剂的苯乙烯胺
公开(公告)号：WO2006108640A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003380
申请日：2006-04-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , FURET, Pascal , GUAGNANO, Vito , MCCARTHY, Clive , VAUPEL, Andrea
发明人： BOLD, Guido , FURET, Pascal , GUAGNANO, Vito , MCCARTHY, Clive , VAUPEL, Andrea
IPC分类号： C07D471/04 , C07D235/04 , A61K31/4184 , A61K31/4188 , A61P35/00 , A61P35/02
CPC分类号： C07D235/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D473/00
摘要： The invention relates to compounds of the formula (I) wherein the moieties R1 , R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof; as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.
摘要翻译：本发明涉及式（I）化合物，其中部分R 1，R 2，R 3，R 9，R 10和Q和X，Y和Z如说明书中所定义，及其盐; 以及它们的使用，它们的使用方法及其合成方法等。这些化合物是蛋白激酶抑制剂，尤其可用于治疗各种增殖性疾病。

47. 发明申请

WO2004052884A1 ANTHRANILIC ACID AMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：氨基酸衍生物及其药物用途
公开(公告)号：WO2004052884A1
公开(公告)日：2004-06-24
申请号：PCT/EP2003/014086
申请日：2003-12-11
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
发明人： BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
IPC分类号： C07D409/04
CPC分类号： C07D405/04 , C07D213/38 , C07D213/50 , C07D213/61 , C07D213/64 , C07D213/74 , C07D401/12 , C07D409/04 , C07D417/04
摘要： The present invention relates to new anthranilic acid amide derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds.
摘要翻译：本发明涉及新的邻氨基苯甲酸酰胺衍生物，其制备方法，其在人或动物体的治疗方法中的应用，其用途 - 单独使用或与一种或多种其它药学活性化合物组合。

48. 发明申请

WO2003040101A1 ANTHRANILIC ACID AMIDES AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：氨基酸和其药物用途
公开(公告)号：WO2003040101A1
公开(公告)日：2003-05-15
申请号：PCT/EP2002/012445
申请日：2002-11-07
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
发明人： BOLD, Guido , FURET, Pascal , MANLEY, Paul, William
IPC分类号： C07D213/38
CPC分类号： C07C237/40 , C07D213/38 , C07D213/89
摘要： The invention relates to anthranilic acid amide derivatives of formula (I), wherein Ar is represented by the subformula (I a ), wherein R a represents H or lower alkyl, and R 1 represents H or perfluoro lower alkyl, R 2 represents H, halogen, C 2 -C 7 alkyl, C 2 -C 7 alkenyl or lower aklynyl; or Ar is represented by the subformula (I b ) and R 1 represents perfluoro lower alkyl, and R 2 represents bromo, iodo, C 2 -C 7 alkyl, C 2 -C 7 alkenyl or lower alkynyl, or R 1 represents H, and R 2 represents fluoro, bromo, iodo, ethyl, C 5 -C 7 alkyl, C 2 -C 7 alkenyl or lower alkynyl; to N-oxides and tautomers thereof, and to salts of such anthranilic acid amides, its N-oxides and tautomers; to processes for their preparation; to their application in the treatment of the human or animal body, to the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age-related macular degeneration; to a method for the treatment of such diseases in animals; and to 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 neoplastic disease, of retinopathy or age-related macular degeneration.
摘要翻译：本发明涉及式（I）的邻氨基苯甲酰胺衍生物，其中Ar由亚式（Ia）表示，其中Ra表示H或低级烷基，R1表示H或全氟低级烷基，R2表示H，卤素，C2- C7烷基，C2-C7链烯基或低级甲酰胺基; 或Ar由亚式（Ib）表示，R 1表示全氟低级烷基，R 2表示溴，碘，C 2 -C 7烷基，C 2 -C 7链烯基或低级炔基，或R 1表示H，R 2表示氟，溴，碘，乙基 C 5 -C 7烷基，C 2 -C 7链烯基或低级炔基; 其N-氧化物和互变异构体，以及这种邻氨基苯甲酰胺，其N-氧化物和互变异构体的盐; 进行准备; 其用于治疗人或动物体的用途，其单独使用或与一种或多种其它药学活性化合物组合用于特别是治疗视网膜病变或年龄的肿瘤疾病如肿瘤疾病的治疗相关性黄斑变性; 涉及在动物中治疗这些疾病的方法; 以及使用这样的化合物 - 单独或与一种或多种其它药学活性化合物组合用于制备用于治疗肿瘤性疾病，视网膜病变或年龄相关性黄斑变性的药物制剂。

49. 发明申请

WO2016054483A1 USE OF RING-FUSED BICYCLIC PYRIDYL DERIVATIVES AS FGFR4 INHIBITORS 审中-公开
标题翻译：用FGFR4抑制剂使用环状双键二吡啶衍生物
公开(公告)号：WO2016054483A1
公开(公告)日：2016-04-07
申请号：PCT/US2015/053677
申请日：2015-10-02
申请人： NOVARTIS AG , FAIRHURST, Robin, Alec , FURET, Pascal , KNÖPFEL, Thomas , LEBLANC, Catherine , LIAO, Lv , MAH, Robert , NIMSGERN, Pierre , RIPOCHE, Sebastien , XIONG, Jing , ZHAO, Xianglin , HAN, Bo , WANG, Can , PORTER, Dale , BUSCHMANN, Nicole , GRAUS PORTA, Diana , HAEFLIGER, Carolina , MURAKAMI, Masato , PALMER, Michael , WANG, Youzhen , WEISS, Andreas
发明人： FAIRHURST, Robin, Alec , FURET, Pascal , KNÖPFEL, Thomas , LEBLANC, Catherine , LIAO, Lv , MAH, Robert , NIMSGERN, Pierre , RIPOCHE, Sebastien , XIONG, Jing , ZHAO, Xianglin , HAN, Bo , WANG, Can , PORTER, Dale , BUSCHMANN, Nicole , GRAUS PORTA, Diana , HAEFLIGER, Carolina , MURAKAMI, Masato , PALMER, Michael , WANG, Youzhen , WEISS, Andreas
IPC分类号： A61K31/4375 , A61K31/437 , A61K31/4353 , A61K31/506 , A61K31/5383 , A61K31/5377 , A61K31/501 , A61P35/00
CPC分类号： A61K31/4375 , A61K31/4545 , A61K31/496 , A61K31/55 , A61P35/00
摘要： The present invention relates to therapeutic uses of compounds of formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐的治疗用途。

50. 发明申请

WO2014132220A1 SOLID FORMS OF BICYCLIC HETEROCYCLIC DERIVATIVES AS PDGF RECEPTOR MEDIATORS 审中-公开
标题翻译：作为PDGF受体介质的双相杂环衍生物的固体形式
公开(公告)号：WO2014132220A1
公开(公告)日：2014-09-04
申请号：PCT/IB2014/059304
申请日：2014-02-27
申请人： NOVARTIS AG , BRUCE, Ian , CHAMOIN, Sylvie , COLLINGWOOD, Stephen Paul , FURET, Pascal , FURMINGER, Vikki , LEWIS, Sarah , LOREN, Jon , LV, Lin , MOLTENI, Valentina , SAUNDERS, Alex Michael , SHAW, Duncan , TURNER, Roy , YEH, Vince
发明人： BRUCE, Ian , CHAMOIN, Sylvie , FURET, Pascal , FURMINGER, Vikki , LEWIS, Sarah , LOREN, Jon , LV, Lin , MOLTENI, Valentina , SAUNDERS, Alex Michael , SHAW, Duncan , TURNER, Roy , YEH, Vince
IPC分类号： C07D471/04 , A61K31/44
CPC分类号： C07D471/04 , A61K45/06
摘要： The present invention provides novel solid forms of pharmaceutically active agents and therapeutic uses thereof. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供药物活性剂的新型固体形式及其治疗用途。本发明还提供药理活性剂和药物组合物的组合。

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