The present invention relates to novel purines of general formula A ##STR00001##
processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.

Heterocyclic compounds of formula I shown below and pharmaceutical compositions containing one of such compounds: Also disclosed is a method of treating a condition modulated by the colony-stimulating factor-1 receptor with one of the heterocyclic compounds.

##STR00001##

This disclosure relates to cannabinoid derivatives having the structure of formula (I), pharmaceutical compositions comprising them, and methods of using the cannabinoid derivatives in the treatment or prevention of a disease associated with a cannabinoid receptor, including receptors selected from CB1, CB2, 5HT1A, 5HT2A, GPR18, GPR55, GPR119, TRPV1, TRPV2, PPARγ or a μ-opioid receptor.

This disclosure relates to cannabinoid derivatives having the structure of formula (I), pharmaceutical compositions comprising them, and methods of using the cannabinoid derivatives in the treatment or prevention of a disease associated with a cannabinoid receptor, including receptors selected from CB1, CB2, 5HT1A, 5HT2A, GPR18, GPR55, GPR119, TRPV1, TRPV2, PPARγ or a μ-opioid receptor.

Purine-derived covalent probes (e.g., halo or di-halo-substituted purine based covalent probes) and related ligands are described. The compounds can be used to identify reactive nucleophilic amino acid residues, such as reactive cysteine residues, in proteins and to modify the activity of proteins with reactive nucleophilic amino acid residues (e.g., reactive cysteine residues) via the formation of protein adducts comprising the ligands Modified proteins prepared from the probes and ligands are also described.

Purine-derived covalent probes (e.g., halo or di-halo-substituted purine based covalent probes) and related ligands are described. The compounds can be used to identify reactive nucleophilic amino acid residues, such as reactive cysteine residues, in proteins and to modify the activity of proteins with reactive nucleophilic amino acid residues (e.g., reactive cysteine residues) via the formation of protein adducts comprising the ligands Modified proteins prepared from the probes and ligands are also described.

The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.

The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.

The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.

The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.