C07D239/00

URIDINE MONOPHOSPHATE AND TRIPHOSPHATE DERIVATIVES, COMPOSITIONS AND METHODS OF USE
20180085386 · 2018-03-29 ·

This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to compounds, such as agonists, of P.sub.2Y.sub.6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.

Triazolopyrimidinone or triazolopyridinone derivatives, and use thereof

The present invention relates to a novel triazolopyrimidinone or triazolopyridinone derivative, a tautomer thereof, a stereoisomer thereof and their mixture, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating a tankyrase-related disease, which contains the same as an active ingredient.

Bicyclic-fused heteroaryl or aryl compounds

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, ##STR00001##
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

METHOD OF FIXATING CARBON DIOXIDE TO SUBSTITUTED OXAZOLIDINONES

A method of fixating carbon dioxide (CO.sub.2) to form a substituted oxazolidinone is described. The method includes mixing a metal-organic framework (MOF), at least one epoxide, and at least one aromatic amine to form a mixture. The method further includes contacting the mixture with a gas stream containing CO.sub.2 to react the CO.sub.2 in the gas stream with the epoxide and the aromatic amine to form a substituted oxazolidinone. The MOF is a MIL-68(In)-X MOF. X is of formula (I):

##STR00001##

where at least one of R.sup.1 to R.sup.4 is an amine-containing group, and R.sup.1 to R.sup.4 are independently an amine-containing group or a hydrogen.

METHOD OF FIXATING CARBON DIOXIDE TO SUBSTITUTED OXAZOLIDINONES

A method of fixating carbon dioxide (CO.sub.2) to form a substituted oxazolidinone is described. The method includes mixing a metal-organic framework (MOF), at least one epoxide, and at least one aromatic amine to form a mixture. The method further includes contacting the mixture with a gas stream containing CO.sub.2 to react the CO.sub.2 in the gas stream with the epoxide and the aromatic amine to form a substituted oxazolidinone. The MOF is a MIL-68(In)-X MOF. X is of formula (I):

##STR00001##

where at least one of R.sup.1 to R.sup.4 is an amine-containing group, and R.sup.1 to R.sup.4 are independently an amine-containing group or a hydrogen.

Triazolo-pyrazinyl derivatives useful as soluble guanylate cyclase activators

A compound of Formula I ##STR00001##
or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.

POLYCARBONATE-POLYESTER COMPOSITION AND ARTICLE
20170190904 · 2017-07-06 ·

A composition includes specific amounts of a polyester with 1,4 cyclohexanedimethylene terephthalate repeat units, a halogen-free aromatic polycarbonate, a brominated aromatic polycarbonate, and an unsubstituted or substituted C.sub.2 C.sub.18 hydrocarbyl sulfonate salt. The composition exhibits an improved balance of flame retardancy and transparency relative to a corresponding composition without the sulfonate salt. The composition can be used to fabricate articles that benefit from its transparency and flame retardancy

Thienopyrimidine derivatives, a process for their preparation and pharmaceutical compositions containing them

Compounds of formula (I): ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.12, X, A and n are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives

The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists

Embodiments of the invention include substituted indole compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition.