公开(公告)号：US20220033407A1

公开(公告)日：2022-02-03

申请号：US17414672

申请日：2019-12-13

Applicant: NOVARTIS AG

Inventor： Mihai D. Azimioara ,  Bei Chen ,  Robert Epple ,  Declan Hardy ,  Ayako Honda ,  Philip Lam ,  Hasnain Ahmed Malik ,  Fabio Meier ,  Truc Ngoc Nguyen ,  Barun Okram ,  Sejal Patel ,  Rodrigo Rodriguez ,  Duncan Shaw ,  Yiping Shen ,  Baogen WU

IPC: C07D487/10 ,  C07D401/04 ,  C07D213/74 ,  C07D413/04 ,  C07D491/107 ,  A61K45/06

Abstract: The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.

公开(公告)号：US11192877B2

公开(公告)日：2021-12-07

申请号：US16504375

申请日：2019-07-08

Applicant: Novartis AG

Inventor： Claire Adcock ,  Simone Bonazzi ,  Artiom Cernijenko ,  Philip Lam ,  Kathryn Taylor Linkens ,  Hasnain Ahmed Malik ,  Noel Marie-France Thomsen ,  Michael Scott Visser

IPC: C07D401/04 ,  C07D407/14

Abstract: The present disclosure provides a compound of Formula (I′): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Rx, X1, X2, and R1 are as defined herein, and methods of making and using same.

公开(公告)号：US20200002281A1

公开(公告)日：2020-01-02

申请号：US16566083

申请日：2019-09-10

Applicant: Novartis AG

Inventor： Mihai Azimioara ,  Bei Chen ,  Robert Epple ,  Ayako Honda ,  Philip Lam ,  Hasnain Ahmed Malik ,  Casey Jacob Nelson Mathison ,  Truc Ngoc Nguyen ,  Victor Ivanovich Nikulin ,  Sejal Patel ,  Dean Paul Phillips ,  Rodrigo A. Rodriguez ,  Baogen Wu ,  Xuefeng Zhu

IPC: C07D213/76 ,  C07D401/14 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  C07D405/14 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D493/08

Abstract: The invention relates to heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.

公开(公告)号：US10450273B2

公开(公告)日：2019-10-22

申请号：US15688089

申请日：2017-08-28

Applicant: Novartis AG

Inventor： Mihai Azimioara ,  Bei Chen ,  Robert Epple ,  Ayako Honda ,  Philip Lam ,  Hasnain Ahmed Malik ,  Casey Jacob Nelson Mathison ,  Truc Ngoc Nguyen ,  Victor Ivanovich Nikulin ,  Sejal Patel ,  Dean Paul Phillips ,  Rodrigo A. Rodriguez ,  Baogen Wu ,  Xuefeng Zhu

IPC: C07D213/76 ,  C07D401/14 ,  A61K31/444 ,  C07D401/12 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  C07D405/14 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D493/08

Abstract: The invention relates to heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.

公开(公告)号：US11066369B2

公开(公告)日：2021-07-20

申请号：US16566083

申请日：2019-09-10

Applicant: Novartis AG

Inventor： Mihai Azimioara ,  Bei Chen ,  Robert Epple ,  Ayako Honda ,  Philip Lam ,  Hasnain Ahmed Malik ,  Casey Jacob Nelson Mathison ,  True Ngoc Nguyen ,  Victor Ivanovich Nikulin ,  Sejal Patel ,  Dean Paul Phillips ,  Rodrigo A. Rodriguez ,  Baogen Wu ,  Xuefeng Zhu

IPC: C07D401/02 ,  C07D213/76 ,  C07D401/14 ,  A61K31/444 ,  C07D401/12 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  C07D405/14 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D493/08

Abstract: The invention relates to heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.

公开(公告)号：US11566022B2

公开(公告)日：2023-01-31

申请号：US17124127

申请日：2020-12-16

Applicant: NOVARTIS AG

Inventor： Simone Bonazzi ,  Artiom Cernijenko ,  Jennifer Stroka Cobb ,  Natalie Dales ,  John Ryan Kerrigan ,  Philip Lam ,  Hasnain Ahmed Malik ,  Gary O'Brien ,  Andrew W. Patterson ,  Noel Marie-France Thomsen ,  Pamela Ting

IPC: C07D413/14 ,  C07D401/14 ,  A61K45/06 ,  C07D417/14 ,  C07D471/04

Abstract: The present disclosure relates to compounds of formula (I′) and pharmaceutical compositions and their use in reducing Widely Interspaced Zinc Finger Motifs (WIZ) expression levels, or inducing fetal hemoglobin (HbF) expression, and in the treatment of inherited blood disorders, including hemoglobinopathies, sickle cell disease and beta-thalassemia.