Abstract: Novel pyrrolo[3,2-c]quinoline compounds, a method of synthesizing these compounds, a pharmaceutical composition comprising these compounds and a suitable carrier, and a method of using the compounds. The pyrrolo[3,2-c]quinoline compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

Abstract: The present disclosure provides metabolites of belumosudil and uses of the metabolites in of treating patients with ROCK2-mediated diseases including cGVHD.

Abstract: The present disclosure provides a compound comprising a modified tetracycline derivative, covalently coupled through a linker to a low-hydrophobicity bioactive molecule useful for treating neurodegenerative diseases, wherein the modified tetracycline derivative is optionally defined by the following formula:

Abstract: Novel pyrrolo[3,2-c]quinoline compounds of the formula I, a method of synthesizing these compounds, a pharmaceutical composition comprising these compounds and a suitable carrier, and a method of using the compounds. The pyrrolo[3,2-c]quinoline compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: Described herein are PARP1 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of cancer.

Abstract: Compounds for treating cancer and, particularly, to compounds that are 5-(3-substituted phenyl)-pyrimido[4,5-d]pyrimidine-2,4,7(1H,3H,8H)-trione analogues and their use as anticancer agents. The compounds have the structure: wherein: R1 is selected from the group consisting of hydrogen, hydroxy, and benzyloxy; R2 is selected from the group consisting of hydrogen, a C1-C6 straight or branched chain alkoxy, and benzyloxy; R3 is selected from the group consisting of hydrogen and a C1-C6 straight or branched chain alkyl; and R4 is selected from the group consisting of hydrogen and a C1-C6 straight or branched chain alkyl.

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.

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: The present invention relates to sulfonylureas and sulfonylthioureas comprising a monocyclic imidazolyl group of formula (I): wherein Q is selected from O or S, R1 is an imidazolyl group, wherein the imidazolyl group is unsubstituted or substituted with one or more monovalent substituents, and R2 is a cyclic group substituted at the ?-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

Abstract: Provided herein are compounds of the general Formula (I) which act as kinase inhibitors, e.g. ROCK, S6K, and/or PKC inhibitors, and are useful in neurite growth and axonal growth.

Abstract: The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2?, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

Abstract: The invention relates to inhibitors of ROCK1 and/or ROCK2 having the formula I: Also provided are methods of inhibiting ROCK1 and/or ROCK2 useful for the treatment of disease.

Abstract: The present invention provides imidazole substituted pyridine N-oxide derivatives, stereoisomers, isotopologues, isotopomers and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.

Abstract: The disclosure describes methods of synthesis of phosphonate ester compounds. The methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity and stability. Also disclosed are morphic forms of phosphonate ester compounds.

Abstract: Described herein are compounds, such as compounds represented by Formula I-R: and pharmaceutically acceptable salts, enantiomers, stereoisomers, and tautomers thereof, that are inhibitors of GCN2 kinase or PERK kinase, and methods of treating diseases, including diseases associated with GCN2 kinase or PERK kinase, with said compounds.

Abstract: Provided is a compound represented by formula M-30: or an N-oxide compound thereof, wherein the variable groups are as defined in the specification. Also provided is an arthropod pest control agent containing a compound represented by formula M-30 and an inert carrier. The compound represented by formula M-30 and arthropod pest control agent exhibit an excellent controlling effect against arthropod pests.

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.