公开(公告)号：US12083101B2

公开(公告)日：2024-09-10

申请号：US17201268

申请日：2021-03-15

Applicant: Novartis AG

Inventor： Vincent Bordas ,  Cara Brocklehurst ,  Patrick Chene ,  Pascal Furet ,  Vito Guagnano ,  Patricia Imbach-Weese ,  Joerg Kallen ,  Mickael Le Douget ,  Edwige Liliane Jeanne Lorthiois ,  Joseph McKenna ,  Bahaa Salem ,  Tobias Schmelzle ,  Holger Sellner ,  Nicolas Soldermann ,  Markus Voegtle ,  Markus Wartmann

IPC: A61K31/4155 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/404 ,  A61K31/41 ,  A61K31/426 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/506 ,  A61P35/00 ,  C07D307/81 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D413/04 ,  C07D417/04 ,  C07D491/04

CPC classification number: A61K31/4155 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/41 ,  A61K31/426 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/506 ,  A61P35/00 ,  C07D307/81 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D417/04

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof;






a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：US09051279B2

公开(公告)日：2015-06-09

申请号：US13778910

申请日：2013-02-27

Applicant: Novartis AG

Inventor： Joerg Berghausen ,  Nicole Buschmann ,  Pascal Furet ,  Francois Gessier ,  Joanna Hergovich Lisztwan ,  Philipp Holzer ,  Edgar Jacoby ,  Joerg Kallen ,  Keiichi Masuya ,  Carole Pissot Soldermann ,  Haixia Ren ,  Stefan Stutz

IPC: C07D239/82 ,  A01N43/54 ,  A61K31/517 ,  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

CPC classification number: 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

Abstract: The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) wherein Z is CH2 or N—R4 and X, R1, R2, R4, R6, R7 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.

Abstract translation: 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。

公开(公告)号：US20150111927A1

公开(公告)日：2015-04-23

申请号：US14387653

申请日：2013-03-27

Applicant: NOVARTIS AG

Inventor： Pascal Furet ,  Christine Fritsch ,  Sauveur-Michel Maira

IPC: A61K31/4439 ,  C12Q1/68

CPC classification number: A61K31/4439 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/156

Abstract: The present invention relates to selective cancer treatment regimes based on assaying for the presence or absence of a glutamine or a nucleic acid that encodes glutamine at position 859 of the catalytic p110α subunit of PI3K; methods for producing a transmittable form of information for predicting the responsiveness of patient to (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide), or a pharmaceutically acceptable salt thereof; and a kit thereof.

Abstract translation: 本发明涉及基于测定PI3K的催化性p110α亚基的位置859处谷氨酰胺或编码谷氨酰胺的核酸的存在或不存在的选择性癌症治疗方案; 用于产生用于预测患者对（S） - 吡咯烷-1,2-二羧酸2-酰胺1 - （{4-甲基-5- [2-（2,2,2-三氟乙基） 三氟-1,1-二甲基 - 乙基） - 吡啶-4-基] - 噻唑-2-基} - 酰胺）或其药学上可接受的盐; 及其套件。

公开(公告)号：US20140350010A1

公开(公告)日：2014-11-27

申请号：US14361068

申请日：2012-11-28

Applicant: NOVARTIS AG

Inventor： Pascal Furet ,  Vito Guagnano ,  Philipp Holzer ,  Robert Mah ,  Keiichi Masuya ,  Achim Schlapbach ,  Stefan Stutz ,  Andrea Vaupel

IPC: C07D487/04 ,  A61K31/4178 ,  A61K31/4162 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/41 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/41 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377

Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.

Abstract translation: 本发明涉及本文所述的式（I）化合物，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM4的活性介导的疾病或疾病的化合物的用途和用途，以及组合 包括这样的化合物。

公开(公告)号：US08865894B2

公开(公告)日：2014-10-21

申请号：US13773947

申请日：2013-02-22

Applicant: Novartis AG

Inventor： Giorgio Caravatti ,  Robin Alec Fairhurst ,  Pascal Furet ,  Frédéric Stauffer ,  Frank Hans Seiler ,  Clive McCarthy ,  Heinrich Rueeger

IPC: C07D401/14 ,  A01N43/54 ,  C07D403/04 ,  C07D413/14 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D498/04 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08815926B2

公开(公告)日：2014-08-26

申请号：US13748790

申请日：2013-01-24

Applicant: Novartis AG

Inventor： Pascal Furet ,  Vito Guagnano ,  Philipp Holzer ,  Joerg Kallen ,  Lv Liao ,  Robert Mah ,  Liang Mao ,  Keiichi Masuya ,  Achim Schlapbach ,  Stefan Stutz ,  Andrea Vaupel

IPC: A61K31/4188 ,  C07D235/02 ,  C07D487/04 ,  A61K45/06 ,  A61K31/541 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/501

CPC classification number: C07D487/04 ,  A61K31/4188 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06

Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.

Abstract translation: 本发明涉及式（I）化合物：如本文所述，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM4的活性介导的疾病或疾病的这些化合物的用途和方法，以及 包含这些化合物的组合。

公开(公告)号：US08815901B2

公开(公告)日：2014-08-26

申请号：US13962542

申请日：2013-08-08

Applicant: Novartis AG

Inventor： Pascal Furet ,  Diana Graus Porta ,  Vito Guagnano

IPC: A61K31/47 ,  C07D215/16

CPC classification number: A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  C07D215/06 ,  C07D215/48 ,  C07D241/42 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14

Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; 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，其中取代基如说明书中所定义，游离形式或其药学上可接受的盐，溶剂合物，酯，N-氧化物的形式; 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：US08759517B2

公开(公告)日：2014-06-24

申请号：US13624320

申请日：2012-09-21

Applicant: Novartis AG

Inventor： Guido Bold ,  Pascal Furet ,  Vito Guagnano

IPC: C07D239/48

CPC classification number: C07D239/48 ,  C07D401/12

Abstract: 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.

Abstract translation: 本发明涉及式IA的杂芳基芳基脲，其中基团和符号具有本文定义的含义，这些化合物在治疗蛋白激酶依赖性疾病中的用途; 涉及包含所述杂芳基芳基脲的药物制剂，以及制备这些新化合物的方法和包括使用这种杂芳基芳基脲的治疗方法。

公开(公告)号：US20130030171A1

公开(公告)日：2013-01-31

申请号：US13624320

申请日：2012-09-21

Applicant: Novartis AG

Inventor： Guido Bold ,  Pascal Furet ,  Vito Guagnano

IPC: C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D413/12 ,  C07D239/48

CPC classification number: C07D239/48 ,  C07D401/12

Abstract: 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.

Abstract translation: 本发明涉及式IA的杂芳基芳基脲，其中基团和符号具有本文定义的含义，这些化合物在治疗蛋白激酶依赖性疾病中的用途; 涉及包含所述杂芳基芳基脲的药物制剂，以及制备这些新化合物的方法和包括使用这种杂芳基芳基脲的治疗方法。

公开(公告)号：US09539260B2

公开(公告)日：2017-01-10

申请号：US13721805

申请日：2012-12-20

Applicant: Novartis AG

Inventor： Giorgio Caravatti ,  Sylvie Chamoin ,  Pascal Furet ,  Klemens Hogenauer ,  Konstanze Hurth ,  Karen Kammertoens ,  Ian Lewis ,  Henrik Moebitz ,  Alexander Baxter Smith ,  Nicolas Soldermann ,  Romain Wolf ,  Frederic Zecri

IPC: C07D498/04 ,  A61K31/538 ,  A61K31/5383 ,  C07D413/14 ,  C12Q1/25 ,  C12N9/12 ,  C12Q1/68

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

Abstract: 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.

Abstract translation: 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。 这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。