Abstract: There is provided herein compounds of formula (I) and pharmaceutically-acceptable salts and/or detectably-labelled derivatives thereof, wherein R1 to R3, X, Y, n and m have meanings as provided in the description, together with formulations and products comprising the same. There is also provided the use of such compounds, formulations and products in the treatment of cancers characterised by increased MYC activity.

Abstract: The present disclosure encompasses solid state forms of Belumosudil, in embodiments crystalline polymorphs of Belumosudil or salts thereof, processes for preparation thereof, and pharmaceutical compositions thereof.

Abstract: Methods for treating bladder cancer and solid tumors are disclosed. The methods include administering to a patient a compound of formula 1 Pharmaceutical compositions of compound 1 are also disclosed.

Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Abstract: Generally, the present invention provides novel quinolone and 5H-1,5,7,11b-tetraaza-benzo[c]fluoren-6-one compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.

Abstract: Disclosed herein are compounds of Formula I: or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising such compounds, and methods of treating disease by administering or contacting a subject with one or more of the above compounds.

Abstract: The present invention provides PI3K protein kinase modulators of Formula (I) wherein R, n, R1, R2, L1, Cy1 and Cy2 are as defined herein, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

Abstract: Disclosed are a pyrimidine small-molecule compound and an application thereof. The pyrimidine small-molecule compound has efficient inhibitory activity towards PDGFR? and PDGFR? kinases, but has relatively weak inhibitory activity towards other kinases. Therefore, the compound has very high selectivity and is capable of being used as a potential drug for resisting tumors or relieving ophthalmic diseases such as wet age-related macular degeneration or uveitis.

Abstract: Disclosed are heteroaromatic carboxamides of formula (I), wherein R, R1, A1, A2, L1, and L2 are as defined herein, and pharmaceutically acceptable salts thereof. Also disclosed are methods of using the compounds of formula (I) for treatment of diseases, which can be influenced by inhibition of plasma kallikrein.

Abstract: Disclosed is a use of a small-molecule AURKB inhibitor for treatment of non-small cell lung cancer.

Abstract: The present invention provides a composition comprising a compound of formula (I) or a physiologically acceptable salt thereof, in which the compound of formula (I) or a physiologically acceptable salt thereof has a HPLC purity of ?90%; wherein R1, R2, X and n are as defined herein. The present invention further provides use of the composition according to the present invention for preparing and/or purifying a composition comprising a salt of the compound of formula (I), and a method for treating a disease caused by a coronavirus which comprises administering the composition of the present invention to a subject. The composition of the present invention comprises the compound of formula (I) with high purity, and has good fluidity and anti-caking property; moreover, the claimed composition comprising the compound of formula (I)) with high purity is more suitable for preparing a composition comprising a salt of the compound of formula (I) with higher purity.

Abstract: The present disclosure relates to methods of making LRRK2-inhibiting, pyrimidinyl-4-aminopyrazole compounds and intermediates of formulae I and IV: The compounds are useful as LRRK2 inhibitors in the treatment of LRRK2 mediated diseases, and as intermediates for their manufacture.

Abstract: The present disclosure is directed to a cleavable agent for enhanced magnetic resonance generally corresponding to the formula Y-L-R, wherein Y represents a catalyst-binding moiety having at least one isotopically labeled heteroatom, L represents a cleavable bond, and R represents a hyperpolarized payload having at least one isotopically labeled carbon. Also disclosed herein is a method of cleaving the cleavable agent for enhanced magnetic resonance.

Abstract: A compound having one of the following structures of Formula (IV) or (V): or a stereoisomer, salt, or tautomer thereof, wherein R1, R2, R3, R4, R5 R6, R7, R8, R10, R11a R11b, R12a R12b, X, Y, and Z are as defined herein. Pharmaceutical composition comprising the compounds, and their use in methods of treating diseases are also described.

Abstract: The present invention relates to a pyrimidine derivative, a method for preparing same and use thereof in medicine. In particular, the present invention relates to a pyrimidine derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as a FGFR4 kinase inhibitor, definitions of each substituent in the general formula (I) being the same as those defined in the description.

Abstract: Provided are compounds of Formula (I): including compounds of Formulas (II), (III) and (IV), wherein X, R1, R2, R3 and n are as defined herein, and pharmaceutically acceptable salts thereof, and methods for their use and production. These compounds can be useful, e.g., in the treatment of disorders responsive to the inhibition of apoptosis signal-regulating kinase 1 (ASK1).

Abstract: The application relates to a compound having Formula I: which modulates the activity of HER2 and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof plays a role.

Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salts thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: Figure I and Figure II where the definitions of the variables are provided herein.

Abstract: The pyrrolo[3,4-b]quinoline compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis. These compounds have the following structure, with all variables being as defined herein.

Abstract: Described herein are azetidine and pyrrolidine PARP1 inhibitors and pharmaceutical compositions comprising said inhibitors.