Abstract: Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.

Abstract: The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.

Abstract: The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide of the formula: [INSERT CHEMICAL STRUCTURE HERE] Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.

Abstract: Provided herein are cinchonium betaine catalysts and methods of promoting asymmetric imine isomerization reactions using the same.

Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

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

Abstract: In some embodiments, the invention relates to the compounds of Formula (I) and (II) or a pharmaceutically acceptable salt thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, in some embodiments, the present invention relates to the compounds of Formula (I) and (II), pharmaceutical compositions thereof, and the use of the compounds and pharmaceutical compositions in the treatment of a hyperproliferative disorder, an inflammatory disorder, an immune disorder, or an autoimmune disorder.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof wherein Z, Y R3a, R3b, R4a, R4b, G1, G2, G3, G4, L1, m1, m2, m3, m4, n and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract: The present invention relates to sanglifehrin macrocyclic analogues according to Formula (I), particularly for use in treatment of cancer, especially liver cancer.

Abstract: A process for preparing a compound of formula (II): includes reacting a compound of formula (VIII): with a compound of formula (XIV):

Abstract: The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to novel forms of ethyl ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate, pharmaceutical formulations, and therapeutic uses thereof in treating viral infections (e.g., an HIV infection).

Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.

Abstract: This invention provides compounds of the formula (I): wherein Y1, Y2, Z, X1, X2, and W? are defined in the specification. These compounds are useful in the treatment of tyrosine kinases, MAPK signaling pathway kinases and PI3K/AKT/mTor signaling pathway kinases-mediated diseases or conditions, such as neurodegeneration, neuroprotection, cancer, autoimmune as well as other diseases and conditions associated with the modulation of tyrosine kinases selected from FYN, FYN Y531F, FLT3, FLT3-ITD, BRK, ITK, FRK, BTK, BMX, SRC, FGR, YES1, LCK, HCK, RET, CSK, LYN, and ROS1; MAPK pathway kinases selected from ARAF, BRAF, CRAF, ERK1/2, MEK1, MEK2, MEK3, MEK4, MEK5, MEK6, and MEK7; and PI3K/AKT/mTor pathway kinases: selected from mTor, PI3K ?, PI3K ?, PI3K ?, and PI3K ?.

Abstract: The present application provides a method for preparing nintedanib. The method of the present application is carried out by using 4-halo-3-nitro-benzoic acid methyl ester (compound II) and 3-oxo-3-phenylpropionate (compound III) as raw materials, and preparing nintedanib via intermediates of methyl 4-(1-alkoxy-1,3-dioxo-3-phenyl propan-2-yl)-3-nitrobenzoate (compound IV) and methyl 3-benzoyl-2-oxoindoline-6-formate (compound V). The method for preparing nintedanib (I) provided by the present application has the advantages of using easily obtained raw materials, having a simple process, being cost effective and environmentally friendly, and is suitable for industrial-scale production.

Abstract: The present invention relates to an improved process for the preparation of Valacyclovir or pharmaceutically acceptable salts thereof, which comprises reaction of amine-protected Valacyclovir or its salt with deprotecting agent in a continuous flow reactor.

Abstract: The present invention provides mito-honokiol compounds, pharmaceutical compositions thereof, and methods of using the mito-honokiol compounds in the treatment of cancer.

Abstract: The present disclosure provides compounds of Formula I, pharmaceutical salts thereof, and/or solvates of any of the foregoing, which are useful for treating diseases and conditions related to mutant KIT and PDGFR? and present an advantageously non-brain penetrant profile for treating diseases and conditions related to mutant KIT and PDGFR?. The present disclosure also provides methods for treating gastrointestinal stromal tumors and systemic mastocytosis.

Abstract: The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

Abstract: The present disclosure provides inhibitors of Ras protein of Formula (I-A): Also disclosed are methods to modulate the activity of Ras protein and methods of treatment of disorders mediated by Ras protein with compounds of Formula (I-A).