Patent classifications
C07D473/18
HYPOXANTHINE COMPOUNDS
The present invention aims to provide a novel compound which has prolyl hydroxylases (PHDs) inhibitory effect and which is useful for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. The present invention relates to hypoxanthine compound or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof have prolyl hydroxylase inhibitory effect and are useful as agents for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. In an embodiment, the present invention relates to a method for treating an inflammatory bowel disease, comprising administering a necessary amount of a pharmaceutical composition containing hypoxanthine compound or a pharmaceutically acceptable salt thereof, and pharmaceutical additive to a patient.
Substituted purines as TLR7 agonists
The present invention relates to TLR7 agonists according to Formula I and their use in the treatment of diseases such as cancer and infectious disease. ##STR00001##
Substituted purines as TLR7 agonists
The present invention relates to TLR7 agonists according to Formula I and their use in the treatment of diseases such as cancer and infectious disease. ##STR00001##
PEPTIDE NUCLEIC ACID (PNA) MONOMERS WITH AN ORTHOGONALLY PROTECTED ESTER MOIETY
This application pertains to orthogonally protected esters of peptide nucleic acid (PNA) monomers, which ester groups can be removed under conditions that permit typical backbone and side chain acid- and base-labile protecting groups to remain substantially intact thereby permitting the high yield of PNA monomer carboxylic acids that are suitable for use in PNA oligomer synthesis. Exemplary ester groups include, but are not limited to, 2,2,2-trichloroethyl (TCE), 2,2,2-tribromoethyl (TBE), 2-bromoethyl (2-BE) and 2-iodoethyl groups (2-IE). This invention also pertains to novel methods for the synthesis of Backbone Ester compounds and related Backbone Ester Acid Salts.
PEPTIDE NUCLEIC ACID (PNA) MONOMERS WITH AN ORTHOGONALLY PROTECTED ESTER MOIETY
This application pertains to orthogonally protected esters of peptide nucleic acid (PNA) monomers, which ester groups can be removed under conditions that permit typical backbone and side chain acid- and base-labile protecting groups to remain substantially intact thereby permitting the high yield of PNA monomer carboxylic acids that are suitable for use in PNA oligomer synthesis. Exemplary ester groups include, but are not limited to, 2,2,2-trichloroethyl (TCE), 2,2,2-tribromoethyl (TBE), 2-bromoethyl (2-BE) and 2-iodoethyl groups (2-IE). This invention also pertains to novel methods for the synthesis of Backbone Ester compounds and related Backbone Ester Acid Salts.
Synthetic co-crystals of anhydrous guanine and process for preparing the same
This invention is directed to synthetic co-crystals of anhydrous guanine and at least one additional material, wherein the co-crystals have a high refraction index and therefore, provide products with pearlescence or whiteness with high coverage. The invention is further directed to a process for the preparation of anhydrous guanine and of the co-crystals.
Synthetic co-crystals of anhydrous guanine and process for preparing the same
This invention is directed to synthetic co-crystals of anhydrous guanine and at least one additional material, wherein the co-crystals have a high refraction index and therefore, provide products with pearlescence or whiteness with high coverage. The invention is further directed to a process for the preparation of anhydrous guanine and of the co-crystals.
Purine nucleotide derivatives
The present invention provides a compound having the structure: ##STR00001##
Purine nucleotide derivatives
The present invention provides a compound having the structure: ##STR00001##
CANCER TREATMENT WITH (2,2-BISHYDROXYMETHYL) METHYLENECYCLOPROPANE NUCLEOTIDES
The invention provides a compound of formula (I)
##STR00001## wherein B is a nucleobase; U is O or S; R.sup.x is OC(O)R.sup.y, OC(O)CH(R.sup.y)NH.sub.2, OCH.sub.2OC(O)R.sup.y; R.sup.y is optionally substituted alkyl or alkenyl or the side chain of a natural or unnatural amino acid R.sup.1 is H, or optionally substituted phenyl, benzyl, naphthyl, pyridyl or indolyl, or R.sup.x and R.sup.1 together define a bond thus forming a cyclic phosphate; R.sup.2 and R.sup.2 together define the side chain of a natural or unnatural amino acid; R.sup.3 is optionally substituted alkyl, cycloalkyl, phenyl or benzyl; and pharmaceutically acceptable salts and compositions thereof which are useful in the treatment of cancer, especially leukemias.