摘要:
This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.
摘要:
The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders
摘要:
Method of producing compounds of formula (I), wherein R1 is hydrogen or C1-C4-alkyl; R2 is hydrogen, C1-C8-alkyl, C3-C6-cycloalkyl, or a radical -N(R3)R4; or R2 and R6 together are -CH2-CH2-S-; R3 and R4 are hydrogen, C1-C4-alkyl, C3-C6-cycloalkyl or a radical -CH2B; R6 is hydrogen, C1-C8-alkyl, aryl or benzyl; or R3 and R6 together are -CH2-CH2-, -CH2-CH2-CH2-, -CH2-O-CH2-, -CH2-S-CH2- or -CH2-N(R5)-CH2-; X is CH-CN; CH-NO2 or N-NO2; A is an optionally substituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical; and B is optionally substituted phenyl, 3-pyridyl or thiazolyl; characterised in that a compound of formula (II), wherein R2, R6 and X have the same significance as given above in formula (I), is reacted in the presence of a phase transfer catalyst and a base with a compound of formula (III), wherein A and R1 have the same significance as given above in formula (I) and Q is a leaving group.
摘要:
The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.
摘要:
Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington’s disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.
摘要:
Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.
摘要:
Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.
摘要:
Protein conjugated chelated metal radionuclides are provided for use in vivo. Intermediates are provided for preparing the polypeptide compositions efficientiy.