公开(公告)号：US20240217951A1

公开(公告)日：2024-07-04

申请号：US18470521

申请日：2023-09-20

Applicant: AstraZeneca AB

Inventor： Gavin Donal O’MAHONY ,  Olaf PANKNIN ,  Andrey FROLOV ,  Anna TOMBERG ,  Mateusz Piotr PLESNIAK ,  Jens Peter BRANDT ,  Jan Åke LINDBERG ,  Jens Patrik JOHANSSON

IPC: C07D401/14 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/501 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048

CPC classification number: C07D401/14 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/501 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048

Abstract: A compound with the Formula (I):


A-B—C  (I)



wherein A is of the following formula:










where X1 is C—RA1;
B is of formula (B-1) or (B-2)










and C is selected from the group consisting of optionally substituted C6-10 carboaryl, C5-6 heteroaryl and C5-10 heterocyclyl and their use as PCSK9 inhibitors.

公开(公告)号：US20240208997A1

公开(公告)日：2024-06-27

申请号：US18386979

申请日：2023-11-03

Applicant: Boehringer Ingelheim International GmbH

Inventor： Annekatrin Charlotte HEIMANN ,  Alexander DREYER ,  Christian GNAMM ,  Cédrickx GODBOUT ,  Marc Alexander GRUNDL ,  Sandra Ruth HANDSCHUH ,  Christoph HOENKE ,  Joerg Thomas KLEY ,  Christian Andreas KUTTRUFF ,  Jun LI ,  Dirk REINERT ,  Raphael STUBER

IPC: C07D498/22 ,  A61K45/06 ,  C07D491/048

CPC classification number: C07D498/22 ,  A61K45/06 ,  C07D491/048

Abstract: The invention relates to compounds of formula I




wherein R1, R2, R3, A, D, E, G, J, K and L are defined as in claim 1, and prodrugs, deuterated analogues and pharmaceutical acceptable salts thereof, for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), interferonopathies, non-alcoholic steatohepatitis (NASH), interstitial lung disease (ILD) and idiopathic pulmonary fibrosis (IPF).

公开(公告)号：US12006326B2

公开(公告)日：2024-06-11

申请号：US17894412

申请日：2022-08-24

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Adam Szymaniak ,  Kevin McGrath ,  Jianming Yu ,  Tyler Mann ,  Long Nguyen ,  Kaicheng Zhu ,  In Jong Kim ,  Yat Sun Or

IPC: C07D491/052 ,  C07D471/04 ,  C07D491/044 ,  C07D491/048

CPC classification number: C07D491/052 ,  C07D471/04 ,  C07D491/044 ,  C07D491/048

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:




which inhibit Human Respiratory Syncytial Virus (HRSV) or Human Metapneumovirus (HMPV) inhibitors. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HRSV or HMPV infection. The invention also relates to methods of treating an HRSV or HMPV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US12005127B2

公开(公告)日：2024-06-11

申请号：US16962442

申请日：2019-01-16

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： John Patrick Maxwell ,  Katrina Lee Jackson ,  Qing Tang ,  Mark A. Morris ,  Steven M. Ronkin ,  Jinwang Xu ,  Kevin M. Cottrell ,  Paul S. Charifson

IPC: C07D239/74 ,  A61K48/00 ,  C07D239/88 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D491/048

CPC classification number: A61K48/0066 ,  A61K48/0075 ,  C07D239/74 ,  C07D239/88 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D491/048

Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various diseases, conditions, or disorders.

公开(公告)号：US20240174668A1

公开(公告)日：2024-05-30

申请号：US18480925

申请日：2023-10-04

Applicant: Ventus Therapeutics U.S., Inc.

Inventor： Stéphane DORICH ,  Jason BURCH ,  Miguel ST-ONGE ,  Amandine CHEFSON ,  Alexandre CÔTÉ ,  Ramsay BEVERIDGE ,  Stéphane CIBLAT

IPC: C07D471/04 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

Abstract: The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein and having the Formula (I):

公开(公告)号：US11987576B2

公开(公告)日：2024-05-21

申请号：US17480948

申请日：2021-09-21

Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA

Inventor： Todd Ridky ,  Christopher Natale

IPC: A61K8/63 ,  A61G17/04 ,  A61K8/49 ,  A61P17/00 ,  A61P17/06 ,  A61P17/14 ,  A61P17/16 ,  A61P17/18 ,  A61Q19/02 ,  C07D221/16 ,  C07D405/04 ,  C07D491/048

CPC classification number: C07D405/04 ,  A61G17/04 ,  A61K8/49 ,  A61P17/00 ,  A61P17/06 ,  A61P17/14 ,  A61P17/16 ,  A61P17/18 ,  A61Q19/02 ,  C07D221/16 ,  C07D491/048

Abstract: The present invention includes compounds, compositions comprising the same, and methods using the compounds and/or compositions therein, for modulating skin pigmentation in a mammalian subject. In certain embodiments, the compounds of the invention treat or prevent skin disorders or diseases associated with hyperpigmentation in the subject. In other embodiments, the compounds of the invention act as antagonist to the non-canonical sex steroid hormone receptor GPRE1 and do not bind to a canonical nuclear estrogen receptor (ER). In yet other embodiments, the compounds of the invention comprise acts as agonists to the non-canonical sex steroid hormone receptor PAQR7 and do not bind to a canonical nuclear progesterone receptor (PR).

公开(公告)号：US20240158390A1

公开(公告)日：2024-05-16

申请号：US17595468

申请日：2020-05-20

Applicant: Janssen Sciences Ireland Unlimited Company

Inventor： Guillaume Jean Maurice MERCEY ,  David Francis Alain LANCOIS ,  Antoine Benjamin MICHAUT ,  Tony Félicien BOUISSET ,  Jérôme Émile Georges GUILLEMONT ,  Pierre Jean-Marie Bernard RABOISSON

IPC: C07D471/04 ,  A61K45/06 ,  A61P31/14 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D471/04 ,  A61K45/06 ,  A61P31/14 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

Abstract: The invention concerns compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.

公开(公告)号：US20240158381A1

公开(公告)日：2024-05-16

申请号：US18543599

申请日：2023-12-18

Applicant: Libra Therapeutics, Inc.

Inventor： James Guy BREITENBUCHER ,  Maria Pia CATALANI ,  Ali Munaim YOUSIF

IPC: C07D413/04 ,  C07D263/48 ,  C07D413/12 ,  C07D413/14 ,  C07D491/048 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D495/10 ,  C07D498/04

CPC classification number: C07D413/04 ,  C07D263/48 ,  C07D413/12 ,  C07D413/14 ,  C07D491/048 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D495/10 ,  C07D498/04

Abstract: Described herein are oxazole TRPML1 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of TRPML1-mediated disorders or diseases.

公开(公告)号：US11964984B2

公开(公告)日：2024-04-23

申请号：US17231743

申请日：2021-04-15

Applicant: CITY OF HOPE

Inventor： Rama Natarajan ,  Feng Miao ,  Nagarajan Vaidehi ,  Supriyo Bhattacharya

IPC: C07D491/048 ,  A61P3/10 ,  A61P37/06

CPC classification number: C07D491/048 ,  A61P3/10 ,  A61P37/06

Abstract: Disclosed herein, inter alia, are compounds and methods for inhibiting the thioredoxin-thioredoxin-interacting-protein (TXNIP-TRX) complex.

公开(公告)号：US20240130229A1

公开(公告)日：2024-04-18

申请号：US18369543

申请日：2023-09-18

Applicant: Semiconductor Energy Laboratory Co., Ltd.

Inventor： Ryo Narukawa ,  Akira Nagasaka ,  Kunihiko Suzuki ,  Hideko Yoshizumi

IPC: H10K85/60 ,  C07D491/048

CPC classification number: H10K85/6572 ,  C07D491/048 ,  H10K85/626 ,  H10K2101/20

Abstract: A novel high molecular compound is provided. The high molecular compound includes a repeating unit. The repeating unit has a fluorenediyl group, a hole-transport skeleton, and an electron-transport skeleton. The hole-transport skeleton is bonded to the fluorenediyl group through a substituted or unsubstituted first arylene group. The electron-transport skeleton is bonded to the fluorenediyl group through a substituted or unsubstituted second arylene group. In an excited state, intramolecular charge transfer occurs between the hole-transport skeleton and the electron-transport skeleton.