公开(公告)号：US12012395B2

公开(公告)日：2024-06-18

申请号：US17345909

申请日：2021-06-11

Applicant: Edgewise Therapeutics, Inc.

Inventor： Kevin Hunt ,  Kevin Koch ,  Alan Russell ,  Stephen Schlachter ,  Paul Winship ,  Chris Steele

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-α.

公开(公告)号：US12006307B2

公开(公告)日：2024-06-11

申请号：US17872104

申请日：2022-07-25

Applicant: Achillion Pharmaceuticals, Inc.

Inventor： Jason Allan Wiles ,  Avinash S. Phadke ,  Milind Deshpande ,  Atul Agarwal ,  Dawei Chen ,  Venkat Rao Gadhachanda ,  Akihiro Hashimoto ,  Godwin Pais ,  Qiuping Wang ,  Xiangzhu Wang ,  Joel Charles Barrish ,  William Greenlee ,  Kyle J. Eastman

IPC: C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F9/6558

CPC classification number: C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04 ,  C07F9/65583

Abstract: Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, and Formula IV or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

公开(公告)号：US20240182462A1

公开(公告)日：2024-06-06

申请号：US18526922

申请日：2023-12-01

Applicant: Tenaya Therapeutics, Inc.

Inventor： Snahel PATEL ,  Mohammad A. MANDEGAR ,  Pingyu DING ,  Ulhas BHATT ,  Martin HOLAN ,  John LEE ,  Yihong LI ,  Julio MEDINA ,  Alok NERURKAR ,  Frederick SEIDL ,  David SPERANDIO ,  Tien WIDJAJA

IPC: C07D417/14

CPC classification number: C07D417/14

Abstract: Provided herein are compounds identified as inhibitors of HDAC6 activity having the formula:




or a pharmaceutically acceptable salt thereof, that can be used to treat various diseases and disorders.

公开(公告)号：US11999717B2

公开(公告)日：2024-06-04

申请号：US18061822

申请日：2022-12-05

Applicant: Gilead Sciences, Inc.

Inventor： Brian P. Bestvater ,  Zhimin Du ,  Julie Farand ,  Gregory Notte ,  Barton W. Phillips ,  Doris T. Tang ,  Chandrasekar Venkataramani ,  Peiyuan Wang ,  Kin S. Yang ,  Anna Zagorska

IPC: C07D401/04 ,  A61K31/4439 ,  A61K31/65 ,  A61P11/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

CPC classification number: C07D401/14 ,  C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07B2200/05

Abstract: The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non-alcoholic steatohepatitis (NASH).

公开(公告)号：US20240174637A1

公开(公告)日：2024-05-30

申请号：US18273755

申请日：2022-01-21

Applicant: Grazia PIIZZI ,  Eugene L., Piatnitski CHEKLER ,  Jonathan Barry HUROV ,  Alexandra LANTERMANN ,  Kiley Marie COUTO ,  Hua XU ,  Sourav SARKAR ,  Bruce Allen LEFKER ,  Ralph P. ROBINSON ,  Volodymyr KYSIL ,  Sonata Therapeutics, Inc.

Inventor： Grazia Piizzi ,  Eugene L. Piatnitski Chekler ,  Jonathan Barry Hurov ,  Alexandra Lantermann ,  Kiley Marie Couto ,  Hua Xu ,  Sourav Sarkar ,  Bruce Allen Lefker ,  Ralph P. Robinson ,  Volodymyr Kysil

IPC: C07D401/14 ,  C07D405/14 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D417/14

Abstract: Provided herein are compounds (e.g., compounds of Formulae (A-I), (B-I), (C-I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, isotopically labeled derivatives, solvates, hydrates, polymorphs, co-crystals, and prodrugs thereof, pharmaceutical compositions thereof, and kits comprising the same. The compounds provided herein are degraders of GRK2 proteins and are therefore useful for, e.g., treating and/or preventing diseases (e.g., cancer) in a subject, for inhibiting tumor growth in a subject, for inhibiting the activity of GRK2 and/or degrading a GRK2 protein in vitro or in vivo, etc. In certain embodiments, the compounds provided herein are selective for GRK2. Also provided herein are methods and synthetic intermediates useful in the preparation of compounds described herein.

公开(公告)号：US11993574B2

公开(公告)日：2024-05-28

申请号：US17251295

申请日：2019-06-17

Applicant: REATA PHARMACEUTICALS, INC.

Inventor： Xin Jiang ,  Melean Visnick ,  Christopher F. Bender ,  Gary Bolton ,  Bradley Caprathe ,  Chitase Lee ,  Brian Kornberg ,  Patrick O'Brien ,  Martha R. Hotema

IPC: C07D231/54 ,  C07D235/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

CPC classification number: C07D231/54 ,  C07D235/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: Disclosed herein are compounds of the formula: as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to modulate the activity of IL-17 and RORγ. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or for autoimmune disorders.

公开(公告)号：US11987574B2

公开(公告)日：2024-05-21

申请号：US18352078

申请日：2023-07-13

Applicant: XinThera, Inc.

Inventor： Lynnie Trzoss ,  Qing Dong ,  Stephen W. Kaldor ,  Robert L. Hoffman

IPC: C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

Abstract: Described herein are MK2 inhibitors of Formula (II) and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of autoimmune disorders, chronic inflammatory disorders, acute inflammatory disorders, auto-inflammatory disorders, fibrotic disorders, metabolic disorders, neoplastic disorders, and cardiovascular or cerebrovascular disorders.

公开(公告)号：US11986531B2

公开(公告)日：2024-05-21

申请号：US17387621

申请日：2021-07-28

Applicant: ARVINAS OPERATIONS, INC. ,  YALE UNIVERSITY

Inventor： Andrew P. Crew ,  Keith R. Hornberger ,  Jing Wang ,  Saul Jaime-Figueroa ,  Hanqing Dong ,  Kurt Zimmermann ,  Craig M. Crews

IPC: C07D401/14 ,  A61K31/437 ,  A61K47/55 ,  A61P35/00 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D519/00

CPC classification number: A61K47/55 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D519/00

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20240158369A1

公开(公告)日：2024-05-16

申请号：US18273536

申请日：2022-02-17

Applicant: WIGEN BIOMEDICINE TECHNOLOGY (SHANGHAI) CO., LTD.

Inventor： Yuli XIE ,  Yingming WU ,  Houxing FAN ,  Lihui QIAN

IPC: C07D401/14 ,  A61P35/00 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D401/14 ,  A61P35/00 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention discloses a pyrimidine compound as a Wee-1 inhibitor. Specifically, the present invention relates to a compound of general formula (1), a method for preparing same, and use of the compound of general formula (1) or an isomer, a crystalline form, a pharmaceutically acceptable salt, a hydrate or a solvate thereof as a Wee-1 inhibitor in preparing an anti-tumor medicament.

公开(公告)号：US20240150374A1

公开(公告)日：2024-05-09

申请号：US18507566

申请日：2023-11-13

Applicant: Insilico Medicine IP Limited

Inventor： Xin CHENG ,  Luoheng QIN ,  Feng REN

IPC: C07D498/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D498/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: Described herein are KAT6A inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of a disease or disorder associated with KAT6A.