公开(公告)号：EP2794600B1

公开(公告)日：2017-12-06

申请号：EP12823036.4

申请日：2012-12-20

申请人： Novartis AG

发明人： CARAVATTI, Giorgio ,  CHAMOIN, Sylvie ,  FURET, Pascal ,  HÖGENAUER, Klemens ,  HURTH, Konstanze ,  KALIS, Christoph ,  KAMMERTOENS, Karen ,  LEWIS, Ian ,  MOEBITZ, Henrik ,  SMITH, Alexander Baxter ,  SOLDERMANN, Nicolas ,  WOLF, Romain ,  ZECRI, Frédéric

IPC分类号： C07D413/14 ,  C07D498/04 ,  A61K31/536 ,  A61K31/5365 ,  A61P19/02 ,  A61P37/08 ,  A61P35/00 ,  A61P33/06

CPC分类号： A61K31/5383 ,  A61K31/538 ,  C07D413/14 ,  C07D498/04 ,  C12N9/12 ,  C12Q1/25 ,  C12Q1/686 ,  Y02A50/409 ,  Y02A50/411

摘要： The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 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 PI3K enzymes.

公开(公告)号：EP2794600A1

公开(公告)日：2014-10-29

申请号：EP12823036.4

申请日：2012-12-20

申请人： Novartis AG

发明人： CARAVATTI, Giorgio ,  CHAMOIN, Sylvie ,  FURET, Pascal ,  HÖGENAUER, Klemens ,  HURTH, Konstanze ,  KALIS, Christoph ,  KAMMERTOENS, Karen ,  LEWIS, Ian ,  MOEBITZ, Henrik ,  SMITH, Alexander Baxter ,  SOLDERMANN, Nicolas ,  WOLF, Romain ,  ZECRI, Frédéric

IPC分类号： C07D413/14 ,  C07D498/04 ,  A61K31/536 ,  A61K31/5365 ,  A61P19/02 ,  A61P37/08 ,  A61P35/00 ,  A61P33/06

CPC分类号： A61K31/5383 ,  A61K31/538 ,  C07D413/14 ,  C07D498/04 ,  C12N9/12 ,  C12Q1/25 ,  C12Q1/686 ,  Y02A50/409 ,  Y02A50/411

摘要： The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 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 PI3K enzymes.

摘要翻译： 本发明涉及式（I）的二氢 - 苯并恶嗪和二氢 - 吡啶并 - 恶嗪化合物和/或其药学上可接受的盐和/或溶剂合物，其中Y，V，W，U，Q，R 1，R 5，R 7 和R30如说明书中所定义。 此类化合物适用于治疗由PI3K酶的活性介导的疾病或疾病。

公开(公告)号：EP1753712A1

公开(公告)日：2007-02-21

申请号：EP05752742.6

申请日：2005-05-25

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： HINTERDING, Klaus ,  HÖGENAUER, Klemens ,  NUSSBAUMER, Peter

IPC分类号： C07C217/64 ,  C07F9/09 ,  A61P17/00 ,  A61P31/00 ,  A61K31/137 ,  A61K31/661

CPC分类号： C07C217/64 ,  C07C271/16 ,  C07F9/094

摘要： A compound of formula (I) wherein R1, R2, R3, Ra and R5 are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.

公开(公告)号：EP2794594A1

公开(公告)日：2014-10-29

申请号：EP12823037.2

申请日：2012-12-20

申请人： Novartis AG

发明人： HÖGENAUER, Klemens ,  HURTH, Konstanze ,  KALIS, Christoph ,  MOEBITZ, Henrik ,  SOLDERMANN, Nicolas ,  ZECRI, Frédéric

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  A61K31/498 ,  A61P35/00

CPC分类号： C07D409/14 ,  A61K31/4709 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  Y02A50/409 ,  Y02A50/411

摘要： The invention relates to quinoline compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, W, U, Q, R1, R5 R7 and R30 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 PI3K enzymes.

公开(公告)号：EP2790705A1

公开(公告)日：2014-10-22

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.

摘要翻译： 本发明涉及PI3K抑制剂的新用途，其中所述抑制剂对PI3K同种型δ具有抑制作用，用于治疗患有选自疟疾，利什曼病，锥虫病，弓形虫病和/或神经囊尾erc病的疾病或病症的受试者的免疫病理学， 通过功能抑制受感染受试者的TLR9。

公开(公告)号：EP2590974B1

公开(公告)日：2014-05-21

申请号：EP11730637.3

申请日：2011-07-06

申请人： Novartis AG

发明人： COOKE, Nigel Graham ,  FERNANDES GOMES DOS SANTOS, Paulo ,  GRAVELEAU, Nadege ,  HEBACH, Christina ,  HÖGENAUER, Klemens ,  HOLLINGWORTH, Gregory ,  SMITH, Alexander Baxter ,  SOLDERMANN, Nicolas ,  STOWASSER, Frank ,  STRANG, Ross ,  TUFILLI, Nicola ,  VON MATT, Anette ,  WOLF, Romain ,  ZECRI, Frédéric

IPC分类号： C07D471/04 ,  A61K31/517 ,  A61P29/00

CPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  C07B2200/05

摘要： wherein Y, R1, R2 and m 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 PI3K enzymes.

摘要翻译： 本发明涉及式（I）的取代的四氢 - 吡啶并 - 嘧啶衍生物，其中Y，R 1，R 2和m如说明书中所定义。 此类化合物适用于治疗由PI3K酶的活性介导的疾病或疾病。

公开(公告)号：EP2723740A1

公开(公告)日：2014-04-30

申请号：EP12738616.7

申请日：2012-06-25

申请人： Novartis AG

发明人： FERNANDES GOMES DOS SANTOS, Paulo Antonio ,  HÖGENAUER, Klemens ,  HOLLINGWORTH, Gregory ,  SOLDERMANN, Nicolas ,  STOWASSER, Frank ,  TUFILLI, Nicola ,  ZECRI, Frédéric

IPC分类号： C07D471/04 ,  A61K31/517 ,  A61P29/00

CPC分类号： C07D471/04

摘要： The invention relates to crystalline anhydrous forms, crystalline solvate forms and/or salt forms including crystalline salt forms of {(S)-3-[6-(6-methoxy-5-methyl-pyridin-3-yl)-5,6,7,8- tetrahydro-pyrido[4,3-d]pyrimidin-4-yloxy]-pyrrolidin-1-yl}-(tetrahydro-pyran-4-yl)-methanone or salt forms including crystalline salt forms of 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl- pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}-propan-1-on; pharmaceutical compositions and combinations including these forms as well as to methods of using these forms, including their pharmaceutical compositions and combinations for the treatment of diseases.

公开(公告)号：EP1753712B1

公开(公告)日：2009-05-13

申请号：EP05752742.6

申请日：2005-05-25

申请人： NOVARTIS AG ,  Novartis Pharma GmbH

发明人： HINTERDING, Klaus ,  HÖGENAUER, Klemens ,  NUSSBAUMER, Peter

IPC分类号： C07C217/64 ,  C07F9/09 ,  A61P17/00 ,  A61P31/00 ,  A61K31/137 ,  A61K31/661

CPC分类号： C07C217/64 ,  C07C271/16 ,  C07F9/094

摘要： A compound of formula (I) wherein R1, R2, R3, Ra and R5 are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.

公开(公告)号：EP2044100A2

公开(公告)日：2009-04-08

申请号：EP07786106.0

申请日：2007-07-16

申请人： NOVARTIS AG

发明人： SCHREINER, Erwin Paul ,  HÖGENAUER, Klemens

IPC分类号： C07J41/00 ,  A61K31/575 ,  A61P37/06

CPC分类号： C07J41/0061

摘要： 4-(3-hydroxy-10,13-climethyl-hexaclecahyclro-cyclopenta[a]phenanthren-17-yl)-pentanoic acid amides wherein the nitrogen of the amide group is substituted by a sulfonylaminocarbonyl- (C14)-alkyl group; and the use of such compounds as pharmaceuticals.

摘要翻译： 其中酰胺基的氮被磺酰氨基羰基 - （C 14） - 烷基取代的4-（3-羟基-10,13-二甲基 - 六羧基环 - 环戊[a]菲-17-基） - 戊酸酰胺; 以及这些化合物作为药物的用途。

公开(公告)号：EP2001851A2

公开(公告)日：2008-12-17

申请号：EP07723709.7

申请日：2007-03-28

申请人： NOVARTIS AG

发明人： ARISTA, Luca ,  HÖGENAUER, Klemens ,  SCHMIEDEBERG, Niko ,  WERNER, Gudrun ,  JAKSCHE, Herbert

IPC分类号： C07D213/81 ,  C07D213/89 ,  C07D401/12 ,  C07D215/50 ,  C07D237/24 ,  C07D261/18 ,  C07D413/12 ,  C07D513/04 ,  C07D233/90 ,  A61K31/435 ,  A61K31/41 ,  A61P29/00 ,  A61P25/00 ,  A61P9/00 ,  A61P37/00

CPC分类号： C07D213/81 ,  C07D213/89 ,  C07D215/50 ,  C07D233/90 ,  C07D237/24 ,  C07D261/18 ,  C07D401/12 ,  C07D413/12 ,  C07D513/04

摘要： Compounds of Formula (I) wherein R1 is aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R2 is defined heterocyclyl, R3 is alkyl, aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R4 is H or alkyl, or R3 and R4 together with the carbon atom to which they are attached are cycloalkyl fused with aryl, and their use as pharmaceuticals.