Patent classifications
C07F9/65031
IMMUNOMODULATOR
Disclosed is a compound capable of inhibiting interleukin 17A (IL-17A), which is represented by formula (I). An application of the compound or a stereoisomer thereof in the preparation of drugs for inhibiting IL-17A is also provided.
##STR00001##
Substituted bicyclic compounds
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
QUINOLINE cGAS ANTAGONIST COMPOUNDS
The present disclosure provides compounds that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
SUBSTITUTED BICYCLIC COMPOUNDS
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):
##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME
The novel bisphosphonic acid ester derivatives represented by the following formula (1):
Y—Cy—(NH).sub.m—(CH.sub.2).sub.n—C(X)(PO(OR.sup.1)(OR.sup.2)).sub.2 (1)
wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.
Kinase inhibitors
There are provided compounds of formula I, ##STR00001##
wherein R.sup.1 to R.sup.5, X.sup.1, X.sup.2, Ar, L, A, A.sup.1, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
COPPER (I) PYRAZOLATE DIMERS FOR ELECTROLUMINESCENT DEVICES
The invention provides compositions comprising copper(I) pyrazolate dimer compounds for use in OLEDs applications. The inventive compositions can be used to generate visible light colors or a color blend in electronic devices.
##STR00001##
QUINONE METHIDE ANALOG SIGNAL AMPLIFICATION
Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step.
Quinone methide analog signal amplification
Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step.
Phosphorus-containing compound and preparation and use thereof
The present invention provides a phosphorus-containing compound characterized by being a compound represented by the following structure: ##STR00001## the compound is a novel immune cell migration inhibitor. The compound has good hydrophilicity and can be developed into eye drops. The compound has a strong inhibitory ability to immune cell migration and can relieve the symptoms of most dry-eye patients.