Patent classifications
C07F9/650905
PHOSPHINE-BASED COMPOUND AND ORGANIC ELECTROLUMINESCENCE DEVICE INCLUDING THE SAME
A phosphine-based compound and an organic electroluminescence device including the same, the phosphine-based compound being represented by the following Formula 1:
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SULFUR/PHOSPHORUS-CONTAINING ARYL COMPOUND AND APPLICATION THEREOF
Provided are a sulfur/phosphorus-containing aryl compound and an application thereof, and specifically disclosed are a compound represented by formula (V) and a pharmaceutically acceptable salt thereof.
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Heteroaryl compounds as inhibitors of TYK2, composition and application thereof
The present disclosure provides phosphonate-containing heterocycle compounds with TYK2 kinase inhibitory activity, pharmaceutical compositions comprising the same, and applications thereof. The present disclosure provides compounds of Formula (I), as inhibitors of TYK2 kinase. These compounds can be used for preventing and/or treating TYK2 kinase-related diseases and/or conditions.
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PHOSPHINE OXIDE ALKYL AMIDE SUBSTITUTED HETEROARYL COMPOUNDS AS MODULATORS OF IL-12, IL-23, AND/OR IFN ALPHA RESPONSES
Compounds having the following formula I:
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or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFN, by acting on Tyk-2 to cause signal transduction inhibition.
Gold (I)-Phosphine Compounds as Anti-Bacterial Agents
A compound of formula (I) for use in the prevention or treatment of a bacterial infection wherein R.sup.P1 is either methyl, ethyl, isopropyl, cyclohexyl or phenyl; R.sup.P2 is selected from methyl, ethyl, isopropyl, cyclohexyl and phenyl; R.sup.P3 is either ethyl, isopropyl, cyclohexyl, phenyl or pyridyl; A is either S or Se; R.sup.A is selected from wherein each of Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.9 is independently selected from CH or N, wherein at least three of Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.9 are CH; V is selected from O, CHOR.sup.O1, NCO.sub.2R.sup.C2 or NR.sup.N2; one of V, Y.sup.6, Y.sup.7 and Y.sup.8 is selected from CH and N, and the others are CH; X is selected from NH, S or O; R.sup.C1 is selected from OR.sup.O2 or NHR.sup.N1; R.sup.O1 is selected from H and C.sub.1-3 unbranched alkyl; R.sup.O2 is C.sub.1-3 unbranched alkyl; R.sup.N1 is selected from H and C.sub.1-3 unbranched alkyl; R.sup.N2 is C.sub.1-3 unbranched alkyl; R.sup.C2 is either C.sub.1-3 unbranched alkyl or C.sub.3-4 branched alkyl; R.sup.C3 is selected from C.sub.1-3 unbranched alkyl and C.sub.2H.sub.4CO.sub.2H; R.sup.C4 is either H or Me; R.sup.C5 is either H or Me; R.sup.C6 represents one or two optional methyl substituents; and n is an integer from 2 to 8.
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Class of phosphine nitrogen ligand with multiple chiral centers and its synthesis method and application
The present invention discloses a phosphine nitrogen ligand with multiple chiral centers and its synthesis method and application. The ligand has the axial chirality of a biaryl skeleton and the central chirality of a chiral amine. The chiral ligand is synthesized from commercially available raw materials through a simple five-step reaction, and the resulting diastereomer can be separated by simple column chromatography or recrystallization. The chiral phosphine nitrogen ligand synthesized by the present invention can catalyze the asymmetric three-component coupling reaction of terminal alkynes, aldehydes and amines, and realize the efficient preparation of chiral propargyl amines with high optical activity.
Thyroid hormone receptor agonists
Provided herein are novel thyroid hormone receptor (TR) agonists e.g., having Formula I, II, or III. Also provided are methods of preparing the novel TR agonists and method of using the novel TR agonists for treating diseases or disorder modulated by TR agonists, such as NAFLD, NASH, diabetes, hyperlipidemia and/or hypercholesterolemia. ##STR00001##
THYROID HORMONE RECEPTOR AGONISTS
Provided herein are novel thyroid hormone receptor (TR) agonists, e.g., having Formula I, II, or III. Also provided are methods of preparing the novel TR agonists and method of using the novel TR agonists for treating diseases or disorder modulated by TR agonists, such as NAFLD, NASH, diabetes, hyperlipidemia and/or hypercholesterolemia.
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Heteroaryl compounds as inhibitors of TYK2/JAK1, composition and application thereof
The present disclosure provides phosphonate-containing heterocycle compounds with TYK2/JAK1 inhibitory activities, pharmaceutical compositions comprising the same, and applications thereof. The present disclosure provides compounds of Formula (I), as inhibitors of TYK2/JAK1. These compounds can be used for preventing and/or treating TYK2/JAK1 related diseases and/or conditions without significant inhibition of JAK2 activities.
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NOVEL THIOL REDUCTANT, METHOD AND USE THEREOF
The present disclosure relates to a novel thiol reductant having the formula (I), the preparation and the use in the preparation of an antibody with thiol group site-specific modifications with improved homogeneity.