The Hong Kong Polytechnic University

Mcgill University

University of South Florida

Wayne State University

The Royal Institution for the Advancement of Learning / Mcgill University

Other

The Chinese University of Hong Kong

Tak-Hang Chan

Larry Ming-Cheung Chow

Q Ping Dou

David M Smith

Chi-Chiu Wang

Aslamuzzaman Kazi

Wai-Har Lam

Qing Ping Dou

Deborah Joyce Kuhn

Masad Jose Damha

Robert Alexander Donga

Kristin R Landis-Piwowar

Sheng Biao Wan

Kin-Fai Chan

Matthew Hassler

Xun He

Mallikarjuna Reddy Nandyala

Iris Lai King Wong

Kwok-yin Wong

Weishi Miao

Method of treating endometriosis and related indications, comprising the administration of Pro-EGCG, a synthetic and derivative product of epigallocatechin-3-gallate [(&#x2212;)-EGCG]. Use of PRO-EGCG in the manufacture of a medicament for treating endometriosis and related indications. Pro-EGCG for use in the treatment of endometriosis and related indications.

Prodrug of green tea epigallocatechin-3-gallate (pro-EGCG) for use in the treatment of endometriosis

The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II): processes for making these compounds, and the use thereof in the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. The invention also relates to methods of synthesis of oligomers, including but not limited to oligopeptides, oligosaccharides and oligonucleotides, particularly oligoribonucleotides and also oligodeoxyribonucleotides, in solution systems, and ionic tag linkers for use in methods provided herein.

Ionic tags for synthesis of oligoribonucleotides

Method of treating endometriosis and related indications, comprising the administration of Pro-EGCG, a synthetic and derivative product of epigallocatechin-3-gallate [(&#x2212;)-EGCG]. Use of Pro-EGCG in the manufacture of a medicament for treating endometriosis and related indications. Pro-EGCG for use in the treatment of endometriosis and related indications.

The present invention relates to ionic liquids for use in chemical applications and capable of serving the dual function of solvent and liquid support. The ionic liquid lends itself to a method of synthesizing oligomers selected from the group consisting of oligopeptides, oligosaccharides and oligonucleotides, comprising contacting a first monomer unit with an ionic liquid at reaction conditions to provide an ionic liquid bound monomer unit; and contacting the ionic liquid bound monomer unit with at least one further monomer unit at reaction conditions to provide an ionic liquid bound oligomer comprising from 2 to 30 monomer units. The method lends itself to large scale manufacture of oligopeptides, oligosaccharides and oligonucleotides.

Ionic liquid supported synthesis

Filamenting temperature-sensitive mutant Z (FtsZ) protein plays a crucial role in the bacterial cell division machinery and is a validated drug target for antibacterial agents. The present invention relates to FtsZ-interacting compounds that possess a 2,4,6-trisubstituted pyrimidine scaffold. Some of these compounds possess potent anti-staphylococcal properties and potent antibacterial activities against clinically isolated MRSA strains. Compounds have been identified to exhibit low spontaneous frequency of resistance, low toxicity as well as the ability to rescuelarvae infected with lethal dose of the MRSA ATCC 43300 strain. Characterization by saturation transfer difference NMR, light scattering assay and GTPase hydrolysis assay with purifiedFtsZ protein verified the interaction of 2,4,6-trisubstituted pyrimidine with the FtsZ protein, further confirmed by observations of iconic filamentous cell phenotype and mislocalization of the Z-ring formation. Taken together, these pyrimidine derivatives have the potential as effective treatment of staphylococcal infections.

Pyrimidines for treatment of bacterial infections

The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II) processes for making these compounds, and the use thereof in the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. The invention also relates to methods of synthesis of oligomers, including but not limited to oligopeptides, oligosaccharides and oligonucleotides, particularly oligoribonucleotides and also oligodeoxyribonucleotides, in solution systems, and ionic tag linkers for use in methods provided herein.

Prodrug of green tea epigallocatechin-3-gallate (Pro-EGCG) for use in the treatment of endometriosis

The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.

Polyphenol proteasome inhibitors, synthesis, and methods of use

A method of reducing tumor cell growth, the method including administering an effective amount of a compound having the formula: 

(&#x2212;)-Epigallocatechin gallate derivatives for inhibiting proteasome

This invention relates to bis-flavonoid compounds, their synthesis and use for inhibiting multidrug resistance in chemotherapy and protozoan infection, wherein the bis-flavonoids compounds have the formula: 

Flavonoid dimers and their use

(&#x2212;)-epigallocatechin gallate derivatives for inhibiting proteasome

Multidrug resistance (MDR) is a major problem in cancer chemotherapy. The best characterized resistance mechanism is the one mediated by the over-expression of drug efflux transporters, permeability-glycoprotein (P-gp), which pump a variety of anticancer drugs out of the cells, resulting in lowered intracellular drug accumulation. A series of flavonoid dimers are developed in this invention, which are linked together by linker groups of various lengths. These flavonoid dimers are found to be efficient P-gp modulators that increase cytotoxicity of anticancer drugs in vitro and dramatically enhance their intracellular drug accumulation. It is found that the flavonoid dimers of this invention is also useful in reducing drug resistance in treating parasitic diseases.

Flavonoid dimers and methods of making and using such

(&#x2212;)-EGCG, the most abundant catechin, was found to be chemopreventive and anticancer agent. However, (&#x2212;)-EGCG has at least one limitation: it gives poor bioavailability. This invention provides compounds of generally formulae below, wherein R, R, R, R, R, R, R, and Rare each independently selected from the group consisting of &#x2014;H, and Cto Cacyloxyl group; and Ris selected from the group consisting of &#x2014;H, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl, phenyl, benzyl and C-C-cycloalkenyl, whereas each of the last mentioned 7 groups can be substituted with any combination of one to six halogen atoms; at least one of R, R, R, R, R, R, Rand Ris &#x2014;H, which were found to be more potent than their non-protected counterparts, which can be used as proteasome inhibitors to reduce tumor cell growth. 

Growing community of inventors

Hong Kong, China

Tak-Hang Chan