Abstract: The invention provides novel 4-phenyl-coumarin derivatives, processes for their preparation and uses thereof as specific mitochondrial RNA polymerase inhibitors for the treatment of cancer.

Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.

Abstract: A compound which is an arylimidazolyl isoxazole of formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.

Abstract: The present invention relates to a pharmaceutical composition and a lyophilisate of a diazabicyclooctane derivative represented by Compound I, a process for producing the same and methods for using the same.

Abstract: The present invention provides a compound of the following Formula (1) or a pharmaceutically acceptable salt thereof: wherein X is an oxygen atom and the like; Y is —CO—, —SO2— and the like; R1 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkylcarbonyl group and the like; R2 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkoxy group, an optionally-substituted amino group, an optionally-substituted 5- to 12-membered monocyclic or polycyclic saturated heterocyclic group and the like; R3, R4, R5, and R6 are independently a hydrogen atom and the like which exhibits excellent effects in suppressing the proliferation and sphere-forming ability of cancer cells, and can be useful as an antitumor drug or cell growth inhibitor.

Abstract: Provided herein is 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, a mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof, and methods for treating, preventing or managing multiple myeloma using such compounds. Also provided are pharmaceutical compositions comprising the compounds, and methods of use of the compositions.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, Y, A, W, R2, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

Abstract: Provided herein are compounds of formula (I)-(VI): wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.

Abstract: Disclosed in the present invention are a new thiazole compound, particularly a compound represented by formula (I), a pharmaceutical composition thereof and applications thereof in the preparation of drugs for the treatment of diseases related to herpes simplex viruses.

Abstract: Disclosed herein are 5 or 8-substituted imidazo[1,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[1,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8-substituted imidazo[1,5-a]pyridines that can be useful for inhibiting indoleamine 2,3-dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.

Abstract: The present invention is directed to methods for preparing Beraprost and novel synthetic intermediates for Beraprost.

Abstract: The present invention relates to an improved method for producing a diphenylmethane derivative which is effective as a sodium-dependent glucose cotransporter (SGLT) inhibitor, the method being carried out by means of a convergent synthesis method in which each major group is separately synthesized and then coupled. As such, in comparison to a linear synthesis method disclosed in existing documents, the synthesis pathway is compact and yield can be increased, and risk factors inherent in the linear synthesis pathway can be reduced. Furthermore, the crystal form of the compound produced according to the method has superb physicochemical characteristics, and thus can be effectively utilized in fields such as pharmaceutical manufacturing.

Abstract: Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

Abstract: The present invention relates to novel antibacterial compounds (1) as defined below, pharmaceutical compositions containing them and their use as antimicrobials. A compound of formula (1): A-L1-Y-L2-R—B, wherein A is a cyclic group having one of the following formulae (I), (II) and (III), and wherein B is cyclic group having one of the following formulae (IV) to (IX).

Abstract: The present disclosure provides compounds of any one of Formulae (I), (II), and (III). The compounds described herein are inhibitors of histone methyltransferases (e.g., enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2)) and are useful in treating and/or preventing a broad range of diseases (e.g., proliferative diseases). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

Abstract: The present invention provides a compound having the structure:

Abstract: The present invention relates to a novel process for the preparation of Rotigotine of formula (I) and intermediates thereof.

Abstract: The present invention provides a novel crystalline form of Ribociclib succinate, Ribociclib succinate Form APO-I, including Ribociclib succinate, benzyl alcohol and water, compositions thereof, processes for the preparation thereof, and the use of this crystalline form in the treatment of conditions associated with increased CDK4/6 kinase activity, and in particular, cancers, including certain forms of breast cancer.

Abstract: The invention provides certain (phenyl)-(pyrazol)-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one compounds of formula I as D1 positive allosteric modulators (PAMs), and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I, or a pharmaceutically acceptable salt thereof, to treat certain symptoms of Parkinson's disease, schizophrenia, ADHD or Alzheimer's disease.