Vion Pharmaceuticals, Inc.

New York University

Nanotherapeutics, Inc.

Aria Neurosciences Inc.

Xu Kevin Lin

Ivan C King

Terrence W Doyle

Yang Xu

John Mao

Michael Belcourt

Bijan Almassian

Qi Qiao

Martin J Sadowski

Zujin Li

Srinivasa Karra

Michael F Belcourt

Compounds are provided according to formula I: where R, R', R, R, R, and Rare as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, Alzheimer's Disease, Down's syndrome, Parkinson's Disease, and others.

Pyridyl-2-methylamino compounds, compositions and uses thereof

The present invention relates to simple, safe, high-yield methods of synthesizing VNP40101M, 1,2-bis(methylsulfonyl)-2-(2-chloroethyl)-2-(methylaminocarbonyl)hydrazine, an anti-neoplasia agent. One particularly preferred method uses methyl chloroformamide in a one-pot reaction at elevated temperatures to provide VNP40101M in high yield.

Process for the synthesis of anti-neoplasia agent VNP40101M

Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. where R is C-Calkyl or haloalkyl;

Phosphate-bearing prodrugs of sulfonyl hydrazines as hypoxia-selective antineoplastic agents

This invention provides a method to determine alkylguanyltransferase activity in a sample, comprising steps of placing the sample in an appropriate condition so that the AGT is functional; contacting the sample with an AGT Detector under conditions permitting the binding of AGT and AGTD to produce a signal; and measuring the signal, thereby determining the AGT activity in said sample. This invention provides different uses of this method.

Alkylguanyltransferase assays

The present invention relates to compounds according to the structure (I):Where R is &#x2014;CHor &#x2014;CHCHCl; R' is C-Calkyl or &#x2014;CHCHCl; Ror Ris OPOH, NO, OCO(Glu-OH), NHCO(Glu-OH), NHRand unassigned groups of R, R, R, Rand Rare, independently H, F, Cl, Br, I, OH, OPOH, OCH, CF, OCF, NO, CN, SOCH, SOCF, COCH, COOCH, SCH, SF, NH, NHR, N(CH), OPOH, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R, R, R, Ror Rare other than H, the other two of unassigned groups of R, R, R, Ror Rare H. Ris H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

Water-soluble SHPs as novel alkylating agents

Modified prodrug forms of AP/AMP

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Branford, CT, United States of America

Xu Kevin Lin