公开(公告)号：US20250011307A1

公开(公告)日：2025-01-09

申请号：US18687609

申请日：2022-08-30

Applicant: Novartis AG

Inventor： Runyan LI ,  Bo LIU ,  Michael MUTZ ,  Lina YUAN ,  Yingcong ZHOU

IPC: C07D405/04 ,  A61K31/343 ,  A61K31/4025 ,  C07D307/81

Abstract: The present invention generally relates to crystalline polymorphic forms of the biaryl YAP/TAZ-TEAD protein-protein interaction inhibitors 4-((2S,4S)-5-Chloro-6-fluoro-2-phenyl-2-((S)-pyrrolidin-2-yl)-2,3-dihydrobenzofuran-4-yl)-5-fluoro-6-(2-hydroxyethoxy)-N-methylnicotinamide and 2-((2S,3S,4S)-5-Chloro-6-fluoro-3-methyl-2-((methylamino)methyl)-2-phenyl-2,3-dihydrobenzofuran-4-yl)-3-fluoro-4-methoxybenzamide and salts thereof, as well as methods of using the forms in the treatment of cancer.

公开(公告)号：US20230357142A9

公开(公告)日：2023-11-09

申请号：US17818889

申请日：2022-08-10

Applicant: Novartis AG

Inventor： Lech CISZEWSKI ,  Marilyn DE LA CRUZ ,  Piotr H. KARPINSKI ,  Michael MUTZ ,  Christian RIEGERT ,  Caspar VOGEL ,  Ricardo SCHNEEBERGER

IPC: C07D205/04 ,  A61K31/397 ,  C07C57/15

CPC classification number: C07D205/04 ,  A61K31/397 ,  C07C57/15

Abstract: This invention relates to a hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethy-l-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.

公开(公告)号：US20180273522A1

公开(公告)日：2018-09-27

申请号：US15762724

申请日：2016-09-20

Applicant: Novartis AG

Inventor： Eric AUBIN ,  Anthony CASAREZ ,  Andreas FISCH ,  Zaixing LI ,  Mika LINDVALL ,  Heinz Ernst MOSER ,  Michael MUTZ ,  Folkert RECK ,  Bernd Ulrich RIEBESEHL ,  Marc SCHOENHENTZ ,  Vijay SETHURAMAN ,  Robert Lowell SIMMONS

IPC: C07D417/14 ,  A61P31/04

CPC classification number: C07D417/14 ,  A61P31/04 ,  C07B2200/13

Abstract: The invention provides new solid forms, salts and polymorphs of 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3-yl)amino)ethylidene)amino)oxy)cyclopropanecarboxylic acid (referred to herein as Compound X), pharmaceutical compositions containing them, and processes for their manufacture and use in therapy.

公开(公告)号：US20220402870A1

公开(公告)日：2022-12-22

申请号：US17818889

申请日：2022-08-10

Applicant: Novartis AG

Inventor： Lech CISZEWSKI ,  Marilyn DE LA CRUZ ,  Piotr H. KARPINSKI ,  Michael MUTZ ,  Christian RIEGERT ,  Caspar VOGEL ,  Ricardo SCHNEEBERGER

IPC: C07D205/04 ,  A61K31/397 ,  C07C57/15

Abstract: This invention relates to a hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethy-l-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.

公开(公告)号：US20210323915A1

公开(公告)日：2021-10-21

申请号：US17095052

申请日：2020-11-11

Applicant: Novartis AG

Inventor： Lech CISZEWSKI ,  Marilyn DE LA CRUZ ,  Piotr H. KARPINSKI ,  Michael MUTZ ,  Christian RIEGERT ,  Caspar VOGEL ,  Ricardo SCHNEEBERGER

IPC: C07D205/04 ,  A61K31/397 ,  C07C57/15

Abstract: This invention relates to a hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.

公开(公告)号：US20230286924A1

公开(公告)日：2023-09-14

申请号：US18040552

申请日：2021-08-04

Applicant: Novartis AG

Inventor： Michael MUTZ ,  Fang WANG ,  Mei XIA

IPC: C07D239/91 ,  A61K9/08 ,  A61K31/517 ,  A61K9/00

CPC classification number: C07D239/91 ,  A61K9/08 ,  A61K31/517 ,  A61K9/0048 ,  C07B2200/13

Abstract: The present disclosure provides polymorphs and formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I). The present disclosure further provides methods for treating ocular surface pain by administering 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I). The present invention also provides 5 methods for treating dry eye disease and ocular hyperemia by administering 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile.

公开(公告)号：US20240239743A1

公开(公告)日：2024-07-18

申请号：US18434514

申请日：2024-02-06

Applicant: Novartis AG

Inventor： Lech CISZEWSKI ,  Marilyn DE LA CRUZ ,  Piotr H. KARPINSKI ,  Michael MUTZ ,  Christian RIEGERT ,  Caspar VOGEL ,  Ricardo SCHNEEBERGER

IPC: C07D205/04 ,  A61K31/397 ,  C07C57/15

CPC classification number: C07D205/04 ,  A61K31/397 ,  C07C57/15

Abstract: This invention relates to a hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.

公开(公告)号：US20220162170A1

公开(公告)日：2022-05-26

申请号：US17430819

申请日：2020-02-13

Applicant: Novartis AG

Inventor： Joseph Paul BULLOCK ,  Chinmay MAHESHWARI ,  Quintus MEDLEY ,  Muneto MOGI ,  Michela MONTECCHI-PALMER ,  Gregory MORANDI ,  Michael MUTZ ,  Kalliopi STASI ,  Christopher Stephen TOWLER

IPC: C07D239/91

Abstract: The present disclosure provides polymorphs and formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I). The present disclosure further provides methods for treating ocular surface pain by administering 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I). The present invention also provides methods for treating dry eye disease and ocular hyperemia by administering 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile.

公开(公告)号：US20180118678A1

公开(公告)日：2018-05-03

申请号：US15799235

申请日：2017-10-31

Applicant: Novartis AG

Inventor： Lech CISZEWSKI ,  Marilyn DE LA CRUZ ,  Piotr H. KARPINSKI ,  Michael MUTZ ,  Christian RIEGERT ,  Caspar VOGEL ,  Ricardo SCHNEEBERGER

IPC: C07D205/04 ,  C07C57/15 ,  A61K31/397

CPC classification number: C07D205/04 ,  A61K31/397 ,  C07C57/15

Abstract: This invention relates to a hemifumarate salt of 1-(4- 1-[(E)-cyclohexyl-3-tritluoromethy 1-benzy loxyimino ]-ethy 1)-2-ethy1-benzy l)-azetidine-3-carboxy lie acid (Compound) to pharmaceutics compositions comprising this salt, to processes for forming this salt and to its use in medical treatment, addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.