Patent classifications
A61P37/02
Substituted pyrimidine derivatives useful in the treatment of autoimmune diseases
The present invention describes compounds of formula (I) ##STR00001##
Wherein:
R.sup.1 is selected from H and CH.sub.3
R.sup.2 is selected from H, C.sub.4H.sub.9 alkyl, C.sub.6H.sub.13 alkyl and C.sub.3H.sub.6-phenyl, said phenyl optionally substituted by OH or OCH.sub.3, (1R,2S,5S)-5-methylcyclopent-3-ene-1,2-diol
X is O or S
Y is C, N or S. These compounds have been identified as novel compounds useful in the treatment of multiple sclerosis and other autoimmune diseases.
Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
The present disclosure relates to compounds that are Syk inhibitors or pharmaceutically acceptable salts or co-crystals thereof, and pharmaceutical compositions thereof, and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, a Syk inhibitor is a crystalline monomesylate salt of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo-[1,2-a]pyrazin-8-amine of formula 2: ##STR00001##
Substrates, peptide arrays, and methods
Disclosed herein are formulations, substrates, and arrays. Also disclosed herein are methods for manufacturing and using the formulations, substrates, and arrays. Also disclosed are methods for identifying peptide sequences useful for diagnosis and treatment of disorders, and methods for using the peptide sequences for diagnosis and treatment of disorders, e.g., celiac disorder. In certain embodiments, substrates and arrays comprise a porous layer for synthesis and attachment of polymers or biomolecules.
Modified polynucleotides for the production of cytoplasmic and cytoskeletal proteins
The invention relates to compositions including polynucleotides encoding polypeptides which have been chemically modified by replacing the uridines with 1-methyl-pseudouridine to improve one or more of the stability and/or clearance in tissues, receptor uptake and/or kinetics, cellular access by the compositions, engagement with translational machinery, mRNA half-life, translation efficiency, immune evasion, protein production capacity, secretion efficiency, accessibility to circulation, protein half-life and/or modulation of a cell's status, function, and/or activity.
Therapeutic methods using erythrocytes
The present disclosure relates to methods for modulating the level of proteins in a subject or in target cells by priming red blood cells with various agents or conditions that modulate the levels of proteins associated with red blood cells and administering the primed red blood cells to a subject. The disclosed methods represent a novel use of red blood cells primed to express a number of proteins, as cell therapies for numerous diseases or disorders.
Multi-drug-loading-site, high drug-loading capacity ligand-drug conjugate
The present invention provides a multi-drug-loading site and high drug-loading capacity ligand-drug conjugate. The ligand-drug conjugate has a structure of general formula (I). The ligand-drug conjugate has the characteristics of high loading capacity, high drug efficacy, low toxicity, and low risks. The ligand-drug conjugate can be used particularly to connect to a low toxicity chemical molecule, thereby extending a therapeutic window. Furthermore, the present invention provides an antibody-drug conjugate molecule. The antibody-drug conjugate molecule has the characteristics of multiple drug-loading ability and high drug-loading capacity, such that the antibody-drug conjugate can carry a large amount of a low toxicity chemical molecule and achieve a therapeutic effect without depending on antibody targeting or high toxicity chemicals.
TM-{R.sup.2-PEG1-[R.sup.1-PEG2-(R.sup.3-A′-D).sub.n].sub.m}.sub.l (I
Bifidobacterium bacteria and composition including novel bifidobacterium bacteria
Provide are beneficial bacteria that can be beneficially applied across a wide range of age groups and a composition containing the same. Bifidobacterium longum subspecies longum NITE BP-02568 and/or Bifidobacterium longum subspecies longum NITE BP-02569; and Bifidobacterium longum subspecies longum, having utilization ability for 2′-fucosyllactose are also provided. More preferably, bacteria having utilization ability for carbohydrates arabinoxylan, arabinan, and pectic galactan; and a composition containing the bacteria are also provided. More preferably, a composition containing 2′-fucosyllactose are also provided. More preferably, a composition containing at least one carbohydrate selected from the group consisting of arabinoxylan, arabinan, pectic galactan, and oligosaccharides derived therefrom or containing at least a carbohydrate derived from a gramineous plant or a carbohydrate derived from a solanaceous plant are also provided.
Peptide-nanoparticle conjugates
Described herein is a nanoparticle system including a multivalent nanoparticle core having a plurality of β-hairpin peptides conjugated thereto. Also included are pharmaceutical compositions and methods of making the nanoparticle system. Further included are immunotherapy methods including administering the nanoparticle system to a subject in need thereof, such as a human cancer patient.
Peptide-nanoparticle conjugates
Described herein is a nanoparticle system including a multivalent nanoparticle core having a plurality of β-hairpin peptides conjugated thereto. Also included are pharmaceutical compositions and methods of making the nanoparticle system. Further included are immunotherapy methods including administering the nanoparticle system to a subject in need thereof, such as a human cancer patient.
NITROGEN-CONTAINING SPIRO CYCLIC COMPOUNDS AND PHARMACEUTICAL USES THEREOF
A compound of the following general formula [I]:
##STR00001##
wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.