Abstract: The present disclosure provides compounds and methods useful in the treatment and suppression of cancer, for example, useful for treating or suppressing cancers characterized by KRAS G12C. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: The present invention aims to find a pharmaceutical preparation which treats or prevents glaucoma or ocular hypertension and is effective for patients with inadequate efficacies of glaucoma or ocular hypertension therapeutic agents. It has been found that omidenepag, an ester thereof, or a salt thereof has an excellent intraocular pressure lowering efficacy on patients with inadequate efficacies of other glaucoma or ocular hypertension therapeutic agents. Therefore, the omidenepag, the ester thereof, or the salt thereof of the present invention is useful as a pharmaceutical preparation which can treat or prevent glaucoma or ocular hypertension even in patients with inadequate efficacies of other glaucoma or ocular hypertension therapeutic agents.

Abstract: Disclosed herein is a compound of Formula (I) for inhibiting both Bcl-2 wild type and mutated Bcl-2, in particular, Bcl-2 G101V and D103Y, and a method of using the compound disclosed herein for treating dysregulated apoptotic diseases.

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):

Abstract: This invention provides rho-associated protein kinase (ROCK) inhibiting compounds for therapeutic applications as described further herein.

Abstract: A compound represented by a formula (I) or a formula (II): (in the formulas (I) and (II), A represents an oxygen atom or a sulfur atom, X1 represents a halogeno group or the like, m represents the number of X1 groups and is any integer of 0 to 5, Z represents a group represented by a formula (Z-1) or a formula (Z-2), a bond marked with a symbol * means a bond with a carbonyl group or a thiocarbonyl group in a pyridinium salt, Y represents a substituted or unsubstituted C2-6 alkenylene group, Q represents a naphthalene ring or a 6- to 10-membered heteroaryl ring, X2 represents a substituted or unsubstituted C1-6 alkyl group or the like, X3 represents a halogeno group or the like, n represents the number of X3 groups and is any integer of 0 to 4, Zq? represents a counter ion, and q represents a valence of the counter ion and is 1 or 2.

Abstract: Disclosed herein are methods and processes of preparing vadadustat and pharmaceutically acceptable salts thereof, and intermediates of formula (I) and their salts useful for the synthesis of vadadustat.

Abstract: The present invention relates to novel antitumor agents and pharmaceutically acceptable salts thereof, processes and intermediates for the manufacture of these novel constrained cyclic frameworks of general formula I and II, and medicaments containing such compounds.

Abstract: The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (1).

Abstract: The present invention relates to compounds of formula (Ib), wherein R1 to R3, M and L are as described herein, and their pharmaceutically acceptable salt, enantiomers and diastereomers thereof, and compositions including the compounds and methods of using the compounds.

Abstract: The present disclosure relates to compounds and compositions for inhibition of Bcr-Abl tyrosine kinases, methods of preparing said compounds and compositions, and their use in the treatment of various cancers, such as chronic myeloid leukemia (CML).

Abstract: A method is disclosed for preparing compounds of Formula 1 by combining compounds of Formulae 2 and 3 and a sulfonyl chloride in a continuous process.

Abstract: The present disclosure describes GLP-1R modulating compounds that are useful for treating GLP-1R-mediated diseases or conditions,

Abstract: This disclosure relates to GLP-1 agonists of Formula (I), including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.

Abstract: The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.

Abstract: The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging.

Abstract: The present invention provides compounds of the formula: for use in the treatment of systemic sclerosis, fibrosis (e.g. pulmonary fibrosis), achondroplasia, thanatophoric dysplasia (e.g. type I), severe achondroplasia with developmental delay and acanthosis nigricans (SADDAN), muenke syndrome or cancer.

Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

Abstract: A five-membered-fused six-membered compound, and a preparation method therefor and a pharmaceutical composition and the use thereof. The five- and six-membered compound is a compound as shown in formula I, II or III. The compound has an inhibitory effect on FLT3 and/or IRAK4.

Abstract: The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein.