Board of Governors for Higher Education, State of Rhode Island and Providence Plantations

Eastern Virginia Medical School

University of Rhode Island

Chapman University

University of California

Board of Governers for Higher Education

State of Rhode Island and Providence Plantations

Keykavous Parang

Gustavo F Doncel

Hitesh Kumar Agarwal

Nguyen Hai Nam

Oleg A Andreev

Yana K Reshetnyak

Sun Yang

Navindra Seeram

David Salehi

Gongqin Sun

Rakesh Tiwari

Khalid Zoghebi

Parvin Mahdipoor

Yue-Hao Wang

Frank L Meyskens, Jr

Yousef Ahamdibeni

Saghar Mozaffari

Hang Ma

Hamidreza Montazeri Aliabadi

Anil Kumar

Guofeng Ye

Soroush Sardari

Richard Chamberlin

Hitesh Kumar Agrawal

Apurinic/apuyrimidinic endonuclease 1/Redox Factor-1 (APE/Ref-1) inhibitors are provided along with methods of using the same. The inhibitor has the structure of Formula I: or a pharmaceutically acceptable salt thereof. n is an integer from 4 to 14, X and X' are each independently H or OH, and Y and Y′ are each independently H or OH.

APE/REF1 inhibitors for the treatment of cancer

Provided herein are drug delivery systems comprising a peptide targeting agent and a pharmaceutical agent for delivery of chemotherapeutic agents. Also provided are methods of treating cancer comprising administration of the drug delivery system disclosed herein.

Targeted peptide-drug conjugates

The present subject matter provides pH triggered peptides, as well as compositions methods, devices, and systems comprising the same. The pH triggered peptides include cyclic and short linear peptides, and may have higher affinity to a membrane lipid bilayer at low pH than at neutral or high pH.

pH-sensitive cyclic peptides

A method is disclosed for synthesizing a compound that includes gallotannins from a part of a maple tree, into new skin whitening compounds. The method includes the step of isolating the gallotannin from the part of the maple tree.

Methods for skin whitening using a gallotannin

The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.

Substituted nucleoside derivatives with antiviral and antimicrobial properties

The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, &#x3b2;-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.

Polymer-bound phosphitylating reagents for the synthesis of organophosphorus compounds

A bisubstrate inhibitor of Src kinases, having a nucleotide or N-heteroaromatic moiety; and a peptide/phosphopeptide, peptidomimetic, or phosphopeptide mimic moiety. The moieties are linked by a rigid or a flexible linker. The nucleotide or N-heteroaromatic moiety is ATP, ATP-mimics, N-heteroaromatics including purine-based derivatives, pyrimidine-based derivatives such as 2,4-diamino-5-substituted pyrimidine derivatives, pyrazole[3,4-d]pyrimidine derivatives, pyrrolo[2,3-d]pyrimidine derivatives, pyrido[2,3-d]pyrimidine derivatives, amino-substituted dihydropyrimido[4,5-d]pyrimidinone derivatives, thieno- and furo-substituted derivatives, quinazoline derivatives, and quinoline derivatives, and several natural products such as aminogenistein. The phosphopeptide mimics comprise phosphonate-based phosphotyrosine mimetics such as phosphonomethylphenylalanine (Pmp) and its analogues, carboxylic acid-based phosphotyrosine mimetics such as malonyltyrosine or phenylalanine analogues and their derivatives such as carboxymethyl phenylalanine, uncharged pTyr mimetics, and conformationally constrained peptides. The phosphopeptide or phosphopeptide mimics inhibits the Src kinases SH2 domain.

Bisubstrate inhibitors of protein tyrosine kinases as therapeutic agents

The present invention is broadly directed to azole derivatives that exhibit antifungal activity and methods for making the same. In one aspect, the invention includes carboxylic acid and phosphate ester derivatives of fluconazole that exhibit antifungal activity. In addition, the invention comprises methods for synthesizing the derivatives and pharmaceutical compositions containing the derivatives.

Azole derivatives and methods for making the same

Growing community of inventors

Irvine, CA, United States of America

Keykavous Parang