公开(公告)号：WO2022135346A1

公开(公告)日：2022-06-30

申请号：PCT/CN2021/139694

申请日：2021-12-20

Applicant: NOVARTIS AG ,  LIU, Bo

Inventor： ASKOXYLAKIS, Vasileios ,  BRACHMANN, Saskia Maria ,  COTESTA, Simona ,  CUI, Xiaoming ,  ENGELMAN, Jeffrey ,  FARAGO, Anna ,  GERSPACHER, Marc ,  GRAUS PORTA, Diana ,  LEBLANC, Catherine ,  LORTHIOIS, Edwige Liliane Jeanne ,  MACHAUER, Rainer ,  MAH, Robert ,  MURA, Christophe ,  RIGOLLIER, Pascal ,  SCHNEIDER, Nadine ,  STUTZ, Stefan ,  VAUPEL, Andrea ,  WARIN, Nicolas ,  WEISS, Andreas ,  WILCKEN, Rainer ,  YERRAMILLI-RAO, Padmaja

IPC: A61K31/416 ,  A61K31/497 ,  C07D403/14 ,  A61P35/00

Abstract: It relates to a pharmaceutical combination comprising a KRAS G12C inhibitor, in particular 1- {6- [ (4M) -4- (5-Chloro-6-methyl-1H-indazol-4-yl) -5-methyl-3- (1-methyl -1H-indazol-5-yl) -1H-pyrazol-1-yl] -2-azaspiro [3.3] heptan-2-yl} prop- 2-en-1-one (Compound A) and one or more therapeutically active agents selected from a SHP2 inhibitor (e.g. TNO155) and a PD-1 inhibitor; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention of a cancer or a tumor, in particular wherein the cancer or tumor is KRAS G12C mutated.

公开(公告)号：WO2008009458A1

公开(公告)日：2008-01-24

申请号：PCT/EP2007/006452

申请日：2007-07-19

Applicant: NOVARTIS AG ,  NOVARTIS PHARMA GMBH ,  DUTHALER, Rudolf ,  GERSPACHER, Marc ,  HOLZER, Philipp ,  STREIFF, Markus ,  THOMA, Gebhard ,  WÄLCHLI, Rudolf ,  ZERWES, Hans-Günter

Inventor： DUTHALER, Rudolf ,  GERSPACHER, Marc ,  HOLZER, Philipp ,  STREIFF, Markus ,  THOMA, Gebhard ,  WÄLCHLI, Rudolf ,  ZERWES, Hans-Günter

IPC: C07D239/48 ,  A61K31/505 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00

CPC classification number: C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

Abstract: Disclosed are pyrimidine derivatives of formula (I) exhibiting JAK-3 and JAK-2 kinase inhibiting activities. wherein R 1 , R 2, R 3 and R 4 are as described herein.

Abstract translation: 公开了具有JAK-3和JAK-2激酶抑制活性的式（I）的嘧啶衍生物。 其中R 1'

公开(公告)号：WO2005068433A1

公开(公告)日：2005-07-28

申请号：PCT/EP2005/000291

申请日：2005-01-13

Applicant: NOVARTIS AG ,  NOVARTIS PHARMA GMBH ,  GERSPACHER, Marc ,  WEILER, Sven

Inventor： GERSPACHER, Marc ,  WEILER, Sven

IPC: C07D235/18

CPC classification number: C07D401/04 ,  C07D235/18 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof; wherein R1-R7 are as disclosed in the specification and pharmaceutical uses thereof.

Abstract translation: 式（I）的化合物或其药学上可接受的盐或前药酯; 其中R1-R7如说明书和其药物用途中所公开的。

公开(公告)号：WO2021220170A1

公开(公告)日：2021-11-04

申请号：PCT/IB2021/053486

申请日：2021-04-27

Applicant: NOVARTIS AG [CH]/[CH]

Inventor： FAIRHURST, Robin Alec ,  FRITSCH, Christine ,  GERSPACHER, Marc ,  HINRICHS, Jürgen Hans-Hermann ,  LANGLOIS, Jean-Baptiste Georges Armand ,  LEBLANC, Catherine ,  LI, Tengfei ,  LORTHIOIS, Edwige Liliane Jeanne ,  MURA, Christophe ,  NIETO-OBERHUBER, Cristina Montserrat ,  TODOROV, Milen ,  VAUPEL, Andrea ,  WARIN, Nicolas ,  WILCKEN, Rainer

IPC: C07D471/04 ,  C07D519/00 ,  A61P35/00 ,  A61K31/437

Abstract: The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease. The compounds are inhibitors or modulators of HIF2alpha.

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

Applicant: NOVARTIS AG ,  BEHNKE, Dirk ,  BETSCHART, Claudia ,  COTESTA, Simona ,  GERSPACHER, Marc ,  HINTERMANN, Samuel ,  ROY, Bernard Lucien ,  VON MATT, Anette ,  WAGNER, Jürgen

Inventor： BEHNKE, Dirk ,  BETSCHART, Claudia ,  COTESTA, Simona ,  GERSPACHER, Marc ,  HINTERMANN, Samuel ,  ROY, Bernard Lucien ,  VON MATT, Anette ,  WAGNER, Jürgen

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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。

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

Applicant: NOVARTIS AG ,  GAUL, Christoph ,  GERSPACHER, Marc ,  HOLZER, Philipp ,  PISSOT SOLDERMANN, Carole

Inventor： GAUL, Christoph ,  GERSPACHER, Marc ,  HOLZER, Philipp ,  PISSOT SOLDERMANN, Carole

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2007112913A3

公开(公告)日：2007-10-11

申请号：PCT/EP2007/002763

申请日：2007-03-28

Applicant: NOVARTIS AG ,  NOVARTIS PHARMA GMBH ,  GERSPACHER, Marc ,  KRAWINKLER, Karl, Heinz

Inventor： GERSPACHER, Marc ,  KRAWINKLER, Karl, Heinz

IPC: C07D401/06 ,  A61P19/10 ,  A61K31/4439

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R, X and Y are as disclosed in the specification, suitable for the treatment of osteoporosis.

公开(公告)号：WO2021124222A1

公开(公告)日：2021-06-24

申请号：PCT/IB2020/062144

申请日：2020-12-17

Applicant: NOVARTIS AG

Inventor： COTESTA, Simona ,  GERSPACHER, Marc ,  LEBLANC, Catherine ,  LIU, Bo ,  LORTHIOIS, Edwige Liliane Jeanne ,  MACHAUER, Rainier ,  MAH, Robert ,  MURA, Christophe ,  RIGOLLIER, Pascal ,  SCHNEIDER, Nadine ,  STUTZ, Stefan ,  VAUPEL, Andrea ,  WARIN, Nicolas ,  WILCKEN, Rainer

IPC: A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/437 ,  A61K31/502 ,  A61K31/517 ,  A61K31/538 ,  A61K31/425

Abstract: The present application provides a compound of formula (I) or a stereoisomer thereof, or an atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a stereoisomer thereof, or a pharmaceutically acceptable salt of an atropisomer thereof; method for manufacturing said compound, and its therapeutic uses. The present application further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：WO2021120890A1

公开(公告)日：2021-06-24

申请号：PCT/CN2020/125425

申请日：2020-10-30

Applicant: NOVARTIS AG ,  LIU, Bo

Inventor： COTESTA, Simona ,  GERSPACHER, Marc ,  LEBLANC, Catherine ,  LORTHIOIS, Edwige, Liliane, Jeanne ,  MACHAUER, Rainer ,  MAH, Robert ,  MURA, Christophe ,  RIGOLLIER, Pascal ,  SCHNEIDER, Nadine ,  STUTZ, Stefan ,  VAUPEL, Andrea ,  WARIN, Nicolas ,  WILCKEN, Rainer

IPC: C07D231/02 ,  A61K31/415 ,  A61K31/4155 ,  A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: Provided is a compound of formula (I) or a stereoisomer thereof, or an atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a stereoisomer thereof, or a pharmaceutically acceptable salt of an atropisomer thereof; a method for manufacturing said compound, and its therapeutic uses. Provided are a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：WO2013084138A1

公开(公告)日：2013-06-13

申请号：PCT/IB2012/056927

申请日：2012-12-03

Applicant: NOVARTIS AG

Inventor： BOCK, Mark ,  CHIKKANNA, Dinesh ,  GERSPACHER, Marc ,  KHAIRNAR, Vinayak ,  LAGU, Bharat ,  PANDIT, Chetan

IPC: C07D235/02 ,  C07D235/26 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D491/052 ,  A61K31/4184 ,  A61K31/4188 ,  A61P5/26 ,  A61P35/00

CPC classification number: C07D235/02 ,  C07D235/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D491/052

Abstract: The present invention is directed to compounds of formula (I) wherein R 1 , R 2 , R 3 , and A are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (I) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer.

Abstract translation: 本发明涉及其中R 1，R 2，R 3和A如本文所定义的式（I）化合物。 本发明还提供包含式（I）化合物的药物组合物以及这些化合物如雄激素受体拮抗剂用于治疗由雄激素受体介导的疾病和病症如前列腺癌的药物组合物。