C07D491/00

PERIPHERALLY-RESTRICTED DUAL-ACTING KAPPA AND DELTA OPIOID AGONIST FOR ANALGESIA IN PAIN STATES INVOLVING THE INFLAMMATORY RESPONSE
20210161912 · 2021-06-03 ·

The present disclosure teaches the use of a dual-acting opioid agonist for the treatment of pain (e.g., inflammatory pain). The opioid agonist activates both the kappa and delta opioid receptors to provide synergistic reduction in pain. The opioid agonist is peripherally restricted and does not cross the blood-brain barrier.

Compound and composition for detecting phosgene and diethyl chlorophosphate

The present invention relates to a compound for detecting phosgene and DCP (diethyl chlorophosphate) and a composition for detecting phosgene and DCP (diethyl chlorophosphate) comprising the said compound. More precisely, the compound for detecting phosgene and DCP of the present invention can selectively detect phosgene and DCP either in the liquid phase of gas phase by detecting the changes of fluorescence and color development very quickly within a few seconds with nM sensitivity. Therefore, the compound can also be effectively used as an ingredient for the composition and kit for the detection of one or more materials selected from the group consisting of phosgene and DCP.

Tricyclic gyrase inhibitors

Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

Azatriangulenium salts as PET-quenched fluorescent probes

The present invention relates to a new class of substituted aza-triangulenium fluorescent dyes having a hydroxy group attached to an aryl as quenching group. The new substituted aza-triangulenium fluorescent dyes may be attached to a linker, conjugated to carrier molecule such as e.g. a protein, a nucleic acid, a lipid, or a saccharide, or deposited or immobilized on solid support materials. The substituted aza-triangulenium fluorescent dyes are useful for various purposes, including use in sensors for monitoring or determining the concentration of analytes, such as H.sup.+(pH), Na.sup.+, K.sup.+, Ca.sup.2+, O.sub.2, CO.sub.2, H.sub.2O.sub.2, ionic strength, redox potentials, metal ions, and metabolites.

Use of the FL-one hundred eighteen core chemical structure platform to generate FL-one hundred eighteen derivatives for treatment of human disease
10344037 · 2019-07-09 · ·

Described herein, are FL118 core structure platform compounds, matter of compositions, formulation, methods and uses for treating cancer or other human diseases. Chemical modifications of the FL118 structure are employed alone or in combination with other anti-cancer agents to preclude or reverse refractory cancer phenotypes and for unique personalized cancer treatment (personalized medicine or as Obama called precision medicine) through application of a series of structural relevant individual FL118 platform-derived analogs.

Substituted quinolizine derivatives useful as HIV integrase inhibitors

The present invention relates to Substituted Quinolizine Derivatives of Formula (I): ##STR00001##
and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.9 and R.sup.10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.

Benzopyranyl tetracycle compound and pharmaceutical composition having excellent anti-inflammatory effect comprising the same

The present invention relates a novel compound represented by the following Formula 3 or Formula 5, and a pharmaceutical composition having superior anti-inflammatory effect comprising the above. The above compound inhibits the translocation of HMGB1 form nucleus to cytosol, and then has remarkable effect of treating or preventing inflammatory disease, especially sepsis. ##STR00001## ##STR00002##

Compounds for treatment of pain

The aspects of the disclosed embodiments are directed to novel compounds, specifically, quaternary ammonium derivatives of tertiary amine containing opioid drug compounds such as hydrocodone, hydromorphone and oxycodone, formulations containing said. compounds or pharmaceutically acceptable salts thereof, which are capable of providing controlled release of the opioid drug upon administration to a patient in order to treat pain.

Stable amorphous ticagrelor and a process for its preparation

The present invention relates to a stable amorphous ticagrelor and a process for its preparation.

Compounds for the treatment of infectious diseases

The present invention relates to compounds of formula (I), ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.