Abstract: The invention relates to compounds of formula I inhibiting Rho Kinase that are tyrosine analogues derivatives, processes of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

Abstract: The present invention provides compounds useful as inhibitors of Ca2+/calmodulin-dependent protein kinase (CaMKII), compositions thereof, and methods of using the same.

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: Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as cancer and tumors, as well as viral infections such as HIV.

Abstract: Provided is a therapeutic agent for Lewy body disease comprising (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one represented by formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, and an application of the compound or slat in preparation of drugs for treating diseases related to an A2A receptor.

Abstract: The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

Abstract: The present invention is related to crystalline salts of N-(3-(5-((1-ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide, a RAF kinase Inhibitor, useful in the treatment of cancer and other diseases.

Abstract: Compounds of formula I are provided: wherein X is NH, or CH2, Y is a single bond, or —CHR5—, R1 is H, C1-C4 alkyl, or C1-C4 hydroxyalkyl, R2 and R2? are each independently H, C1-C4 alkyl, or C1-C4 hydroxyalkyl, each R3 is independently H, halo, —CF3, C1-C4 alkyl, or C1-C4 alkoxy, C3 perhaloalkyl, each R4 is independently H, halo, or C1-C4 alkyl, R5 is C1-C4 alkoxy, r is integer from 0 to 3; and p is integer from 0 to 3.

Abstract: It relates to a process for the preparation of lifitegrast (I) by: a) reacting benzofuran-6-carboxylic acid (II) with a non-chlorinated carboxyl activating agent; b) reacting the activated compound of formula (II) obtained in step a) with compound (III) or a salt thereof to give lifitegrast or a salt thereof; and c) optionally isolating the obtained lifitegrast. It also relates to a process for the purification of lifitegrast (I) by i) reacting lifitegrast (I) with dicyclohexylamine to give the dicyclohexylamine salt of lifitegrast (Ia); ii) isolating the compound of formula (Ia) from the reaction medium; iii) converting the dicyclohexylamine salt into lifitegrast by the treatment with an acid; and iv) isolating the compound of formula (I) from the reaction medium. It also relates to dicyclohexylamine salt of lifitegrast and to a process for its preparation.

Abstract: This disclosure is directed, at least in part, to AMPK activators useful for the treatment of conditions or disorders associated with AMPK. In some embodiments, the condition or disorder is associated with the gut-brain axis. In some embodiments, condition or disorder is associated with systemic infection and inflammation from having a leaky gut barrier. In some embodiments, the AMPK activators are gut-restricted compounds. In some embodiments, the AMPK activators are agonists or partial agonists.

Abstract: The invention provides a method for stimulating an immune response in an animal with a compound of formula: or a pharmaceutically acceptable salt thereof, wherein R1-R3, Ra, and Rb have any of the values defined herein.

Abstract: The present invention provides a compound having excellent histone acetyl transferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: wherein ring Q1, ring Q2, R1, R2, R3 and R4 respectively have the same meanings as defined in the specification.

Abstract: This invention is directed to novel carbocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention.

Abstract: The present disclosure relates to novel compounds, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions.

Abstract: Provided is a crystal of a novel pyrido[3, 4-d]pyrimidine derivative having excellent CDK 4/6 inhibitory activity. A crystal of a compound represented by formula (I). In the formula, R1 represents a hydrogen atom or a C1-3 alkyl group; R2 represents a hydrogen atom or an oxo group; L represents a single bond or a C1-3 alkylene group; and X represents CH or N.

Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R5, A and q have the meanings given in the claims and specification, their use as inhibitors of CDK8/19, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, L and A are as defined in the description and claims, or pharmaceutically acceptable salts thereof having mTOR kinase inhibitor activity. The invention also relates to pharmaceutical compositions including a compound of formula (I) or a pharmaceutically acceptable salt thereof, and to the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in therapy, including in the treatment of a disease or condition for which an mTOR kinase inhibitor activity is indicated, and in particular the treatment of idiopathic pulmonary fibrosis.

Abstract: 1,8-naphthyridinone compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.

Abstract: The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.