Patent classifications
C07D403/12
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
PFKFB3 INHIBITORS AND THEIR USES
- Petr Olegovich FEDICHEV ,
- Kevin GREENMAN ,
- Chang CHIH-TSUNG ,
- Maksim Nikolaevich KHOLIN ,
- Evgeny Gennadievich GETMANTSEV ,
- Tatiana Vladimirovna ZHIDKOVA ,
- Alexandr Viktorovich KADUSHKIN ,
- Timofey Vladimirovich PYRKOV ,
- Dmitry Veniaminovich SHISHOV ,
- Juan Pedro BOLANOS-HERNANDEZ ,
- Kristina Aleksandrovna ZAKURDAEVA ,
- Olga Andreevna BURMISTROVA
This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.
NOVEL ADAMANTANE DERIVATIVES AS INHIBITORS OF FOCAL ADHESION KINASE
The present invention provides novel adamantane derivatives as inhibitors of a focal adhesion kinase, pharmaceutically acceptable salts thereof, stereoisomers thereof, hydrates or solvates thereof, and a pharmaceutical composition comprising same.
NOVEL PHENOL COMPOUND OR SALT THEREOF
The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof:
##STR00001##
wherein R.sub.1, R.sub.2, R.sub.5, L.sub.1, L.sub.2, L.sub.3, A, X, and m are as described in the specification.
NOVEL PHENOL COMPOUND OR SALT THEREOF
The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof:
##STR00001##
wherein R.sub.1, R.sub.2, R.sub.5, L.sub.1, L.sub.2, L.sub.3, A, X, and m are as described in the specification.
TASPASE1 INHIBITORS AND USES THEREOF
Disclosed herein, inter alia, are compounds and methods for inhibiting Taspase1 and the treatment of cancer.
TASPASE1 INHIBITORS AND USES THEREOF
Disclosed herein, inter alia, are compounds and methods for inhibiting Taspase1 and the treatment of cancer.
DEUCRAVACITINIB CRYSTAL FORM, PREPARATION METHOD THEREFOR AND USE THEREOF
Disclosed are a crystal form of a compound (I) and a preparation method therefor, a pharmaceutical composition containing the crystal form, and the use of the crystal form in the preparation of a TYK2 inhibitor drug and a drug for treating psoriasis, systemic lupus erythematosus, and Crohn’s disease. The crystal form of compound I has one or more improved properties compared with the prior art and is of great value to the future optimization and development of the drug.
##STR00001##
DEUCRAVACITINIB CRYSTAL FORM, PREPARATION METHOD THEREFOR AND USE THEREOF
Disclosed are a crystal form of a compound (I) and a preparation method therefor, a pharmaceutical composition containing the crystal form, and the use of the crystal form in the preparation of a TYK2 inhibitor drug and a drug for treating psoriasis, systemic lupus erythematosus, and Crohn’s disease. The crystal form of compound I has one or more improved properties compared with the prior art and is of great value to the future optimization and development of the drug.
##STR00001##