Patent classifications
C07F9/6524
Bisphosphonic acid derivative and application for same
The novel bisphosphonic acid ester derivatives represented by the following formula (1):
YCy(NH).sub.m(CH.sub.2).sub.nC(X)(PO(OR.sup.1)(OR.sup.2)).sub.2(1)
wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.
Bisphosphonic acid derivative and application for same
The novel bisphosphonic acid ester derivatives represented by the following formula (1):
YCy(NH).sub.m(CH.sub.2).sub.nC(X)(PO(OR.sup.1)(OR.sup.2)).sub.2(1)
wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.
Metalloenzyme inhibitor compounds
The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
Metalloenzyme inhibitor compounds
The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
Labeling precursors and radiotracers for nuclear medicine diagnosis and therapy of prostate cancer-induced bone metastases
The invention relates to a labeling precursor for nuclear medicine diagnostics and theranostics that has the structure
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with a first PSMA-specific targeting vector TV1, a second targeting vector TV2 having osteoaffinity, a chelator Chel for complexing a radioisotope, and two or three linkers L1, L2 and L3.
Cyclobutyl (S)-2-[[[(R)-2-(6-aminopurin-9-yl)-1-methyl-ethoxy]methyl-phenoxy-phosphoryl]amino]-propanoates, and production process and application thereof
The present invention relates to chemotherapeutic agents for the treatment of viral and cancerous diseases. Said compounds are prodrugs of the inhibitors of human immunodeficiency virus (HIV) and hepatitis B virus (HBV) of DNA polymerase and are intended for the treatment of human immunodeficiency virus, hepatitis B and co-infections HIV/HCV, HIV/HBV, HIV/HCV/HBV, and HCV/HBV.
Cyclobutyl (S)-2-[[[(R)-2-(6-aminopurin-9-yl)-1-methyl-ethoxy]methyl-phenoxy-phosphoryl]amino]-propanoates, and production process and application thereof
The present invention relates to chemotherapeutic agents for the treatment of viral and cancerous diseases. Said compounds are prodrugs of the inhibitors of human immunodeficiency virus (HIV) and hepatitis B virus (HBV) of DNA polymerase and are intended for the treatment of human immunodeficiency virus, hepatitis B and co-infections HIV/HCV, HIV/HBV, HIV/HCV/HBV, and HCV/HBV.
Chelated PSMA Inhibitors
Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells.
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Chelated PSMA Inhibitors
Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells.
##STR00001##
PHOSPHORAMIDITE ACTIVATOR
The present invention has an object to provide a phosphoramidite activator that improves a solubility of 5-benzylthio-1H-tetrazole in acetonitrile and does not reduce the yield and a purity of a target product.
The present invention relates to a phosphoramidite activator containing (i) at least one compound that is selected from the group consisting of piperidine, pyrrolidine, N-alkylpiperidine, and N-alkylpyrrolidine, (ii) 5-benzylthio-1H-tetrazole, and (iii) acetonitrile; and a method for activating a phosphoramidite and a method for synthesizing a phosphate ester or a thiophosphate ester, both methods using the activator.