Patent classifications
C07H19/207
Modulators of 5′-nucleotidase, ecto and the use thereof
Compounds that modulate the conversion of AMP to adenosine by 5′-nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5′-nucleotidase, ecto is also provided.
FLUORESCENT SUBSTRATES FOR POLY(ADP-RIBOSYL) HYDROLASES
The post-translational modification (PTM) and signaling molecule poly(ADP-ribose) (PAR) has an impact on diverse biological processes. PTM is regulated by a series of ADP-ribosyl glycohydrolases (PARG enzymes) that cleave polymers and/or liberate monomers from their protein targets. Disclosed herein is a substrate for monitoring PARG activity, TFMU-ADPr, which directly reports on total PAR hydrolase activity via release of a fluorophore; this substrate has excellent reactivity, generality, stability, and usability. A second substrate, TFMU-IDPr, selectively reports on PARG activity only from the enzyme ARH3. Use of these probes in whole-cell lysate experiments has revealed a mechanism by which ARH3 is inhibited by cholera toxin. TFMU-ADPr and TFMU-IDPr are versatile tools for assessing small-molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes.
Herbicidal composition comprising flazasulfuron and an inhibitor of protoporphyrinogen oxidase
Many herbicidal compositions have been developed and are presently used. However, weeds to be controlled are various in types and their emergence extends over a long period. Accordingly, it is desired to develop a herbicidal composition which has a broad herbicidal spectrum, a high activity and a long-lasting effect. The present invention provides a herbicidal composition comprising (A) flazasulfuron or its salt and (B) at least one protoporphyrinogen oxidase inhibitor selected from the group consisting of a phenylpyrazole compound, a triazolinone compound, a N-phenylphthalimide compound, a pyrimidindione compound, an oxadiazole compound, an oxazolidinedione compound, a thiadiazole compound, pyraclonil, profluazol, flufenpyr-ethyl and their salts. According to the present invention, a herbicidal composition which has a broad herbicidal spectrum, a high activity and a long-lasting effect can be provided.
Herbicidal composition comprising flazasulfuron and an inhibitor of protoporphyrinogen oxidase
Many herbicidal compositions have been developed and are presently used. However, weeds to be controlled are various in types and their emergence extends over a long period. Accordingly, it is desired to develop a herbicidal composition which has a broad herbicidal spectrum, a high activity and a long-lasting effect. The present invention provides a herbicidal composition comprising (A) flazasulfuron or its salt and (B) at least one protoporphyrinogen oxidase inhibitor selected from the group consisting of a phenylpyrazole compound, a triazolinone compound, a N-phenylphthalimide compound, a pyrimidindione compound, an oxadiazole compound, an oxazolidinedione compound, a thiadiazole compound, pyraclonil, profluazol, flufenpyr-ethyl and their salts. According to the present invention, a herbicidal composition which has a broad herbicidal spectrum, a high activity and a long-lasting effect can be provided.
Tethering of confactors on graphene-like materials
A family of customizable tethering molecules for tethering cofactors such as, but not necessarily limited to, nicotinamine adenine dinucleotide (NAD+/NADH, NAD(P)+/NAD(P)H) to substrates or structures formed from or including graphene-like materials is described. The tethered cofactor can then be used, for example, as biosensors employed for clinical diagnostic, food industry, medical drug development and environmental and military applications, as well as in reagentless biofuel cells for power generation.
Tethering of confactors on graphene-like materials
A family of customizable tethering molecules for tethering cofactors such as, but not necessarily limited to, nicotinamine adenine dinucleotide (NAD+/NADH, NAD(P)+/NAD(P)H) to substrates or structures formed from or including graphene-like materials is described. The tethered cofactor can then be used, for example, as biosensors employed for clinical diagnostic, food industry, medical drug development and environmental and military applications, as well as in reagentless biofuel cells for power generation.
2' AND/OR 5' AMINO-ACID ESTER PHOSPHORAMIDATE 3'-DEOXY ADENOSINE DERIVATIVES AS ANTI-CANCER COMPOUNDS
The present invention relates to chemical compounds, the compounds for use in a method of treatment, particularly in a method of prophylaxis or treatment for cancer, a process for preparation of the compounds and pharmaceutical compositions comprising the compounds. The compounds may, in particular, be useful in the treatment of leukaemia, lymphoma and/or solid tumours in homo sapiens. The compounds are derivatives of cordycepin (3′-deoxyadenosine).
BETA-D-2'-DEOXY-2'-ALPHA-FLUORO-2'-BETA-C-SUBSTITUTED-2-MODIFIED-N6-SUBSTITUTED PURINE NUCLEOTIDES FOR HCV TREATMENT
A compound of the structure:
##STR00001##
or a pharmaceutically acceptable salt or composition thereof for the treatment of a host infected with or exposed to an HCV virus or other disorders more fully described herein.
BETA-D-2'-DEOXY-2'-ALPHA-FLUORO-2'-BETA-C-SUBSTITUTED-2-MODIFIED-N6-SUBSTITUTED PURINE NUCLEOTIDES FOR HCV TREATMENT
A compound of the structure:
##STR00001##
or a pharmaceutically acceptable salt or composition thereof for the treatment of a host infected with or exposed to an HCV virus or other disorders more fully described herein.
Combination of isoindolinone derivatives with SGI-110
The invention provides a combination comprising: (i) a compound of formula (I.sup.o): ##STR00001## or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims; and (ii) a compound which is SGI-110 ##STR00002## or a tautomer or a solvate or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions containing the combinations and medical uses of the combinations.