Patent classifications
C07K5/02
Crystalline forms of s-acetyl glutathione, their preparations and uses in pharmaceutical and nutraceutical formulations
Disclosed are two novel crystalline forms of S-acetyl glutathione (SAG) called Form A and Form B, obtained by crystallization of SAG from mixtures of water-acetone, water-ethanol or water acetone under controlled conditions. Forms A and B can be advantageously used as ingredients of pharmaceutical or nutraceutical formulations.
METHOD OF MAKING PRODRUGS AND TARGETED THERAPEUTIC COMPOUNDS
Provided is a method for making the compound of Formula 1. Various compounds utilized in that method are also provided, as are methods of making those compounds. Also provided is a compound having the formula XO—CO—(CH.sub.2).sub.nNH.sub.2, where n is an integer greater than 2. A method of making that compound is additionally provided. Further provided is a method of making a prodrug of a bioactive compound.
Solid state forms of ivosidenib
Solid state forms of Ivosidenib, processes for preparation thereof, pharmaceutical compositions thereof, and uses thereof are disclosed.
ANTIBODY-DRUG CONJUGATE OF AN ANTI-GLYPICAN-3 ANTIBODY AND A TUBULYSIN ANALOG, PREPARATION AND USES
An antibody-drug conjugate having a structure represented by formula (I)
##STR00001##
wherein m is 1, 2, 3, or 4 and Ab is an anti-glypican-3 antibody having heavy and light chain CDRs as disclosed herein.
PEPTIDOMIMETIC PROTEASOME INHIBITORS
The compounds of the present invention are represented by the following compounds having Formula (I) and Formula (I′):
##STR00001##
where the substituents R, R.sup.1, R.sup.3, R.sup.4, R, W, X, Y, Z, k, and m are as defined herein and
##STR00002##
where the substituents R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y, Z, and m are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.
PEPTIDOMIMETIC PROTEASOME INHIBITORS
The compounds of the present invention are represented by the following compounds having Formula (I) and Formula (I′):
##STR00001##
where the substituents R, R.sup.1, R.sup.3, R.sup.4, R, W, X, Y, Z, k, and m are as defined herein and
##STR00002##
where the substituents R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y, Z, and m are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.
Functional lipid constructs
The invention relates to methods for effecting qualitative and quantitative changes in the functional moieties expressed at the surface of cells and multi-cellular structures, and functional lipid constructs for use in such methods. In particular, the invention relates to functional lipid constructs and their use in diagnostic and therapeutic applications, including serodiagnosis, where the functional moiety is a carbohydrate, peptide, chemically reactive group, conjugator or fluorophore.
Functional lipid constructs
The invention relates to methods for effecting qualitative and quantitative changes in the functional moieties expressed at the surface of cells and multi-cellular structures, and functional lipid constructs for use in such methods. In particular, the invention relates to functional lipid constructs and their use in diagnostic and therapeutic applications, including serodiagnosis, where the functional moiety is a carbohydrate, peptide, chemically reactive group, conjugator or fluorophore.
Gamma amino acid building blocks
The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained α-substituted-γ-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected γ-amino acid residues, which are essential for systematic conformational studies of γ-peptide foldamers. New methods are also provided to prepare other γ-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as α/γ-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.
Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology use.