Albert Einstein College of Medicine

Industrial Research Limited

Victoria Link Limited

Alber Einslein College of Medicine

Callaghan Innovation Research Limited

Albert Einstein College of Medecine of Yeshiva University

Gary Brian Evans

Peter Charles Tyler

Vern L Schramm

Richard Hubert Furneaux

Keith Clinch

Peter Michael Kelly

Jennifer Mary Mason

Dirk Henning Lenz

Alistair Ian Longshaw

Olga Vladimirovna Zubkova

Shivali Ashwin Gulab

Steven Craig Almo

Gavin Frank Painter

Ashley Jarvis

Kami Kim

Tyler Grove

Anthony David Woolhouse

Richard Fröhlich

Ben William Greatrex

Richard Frohlich

Shivall Ashwah Ashwin Gulab

Antti Marko Haapalainen

Shanzhi Wang

Paul Andrew Benjes

John Adrian Dickison

Anthony Mitchell

Lawrence D Harris

Richard Hurbert Furneaux

Richard Froehlich

Simon Peter Harold Mee

This document discloses a novel class of compounds for inhibiting bacterial growth and treating bacterial infection. The compounds target a key step of the futalosine pathway and therefore are effective for the selective inhibition of certain bacterial species and genera with reduced side effect in comparison with conventional antibiotics.

Compounds and methods for treatment of bacterial infections

Methods of treating infections due to(), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering to the subject an inhibitor ofMTAN (5'-methylthioadenosine nucleosidase) having the structure of formula (I) 

Treatment of helicobacter pylori infections

The invention relates to salt forms of (3R,4S)-1-((4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl)-4-(methyl-thiomethyl)pyrrolidin-3-ol, as well as polymorphic forms of the salts. The invention further relates to processes for preparing the salt forms and to the use of the salt forms in the treatment of diseases and disorders where it is desirable to inhibit 5'-methylthioadenosine phosphorylase (MTAP).

Salt and polymorphic forms of (3R,4S)-L-((4-amino-5H-pyrrolo[3,2,-D]pyrimidin-7-yl)methyl)-4(methylthiomethyl)pyrodin-3-ol(MTDIA)

Salt and polymorphic forms of (3R,4S)-L-((4-amino-5H-pyrrolo[3,2,-d]pyrimidin-7-yl)methyl)-4(methylthiomethyl)pyrodin-3-ol(MTDIA)

The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (1) which are inhibitors of 5'-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5&#x2032;-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.

3-hydroxypyrrolidine inhibitors of 5'-methylthioadenosine phosphorylase and nucleosidase

The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (I) which are inhibitors of 5'-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5&#x2032;-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.

The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5'-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors.

Methods, assays and compounds for treating bacterial infections by inhibiting methylthioinosine phosphorylase

Inhibitors of saporin-L1 are disclosed, as are related compositions and uses thereof, in particular in cancer therapy that employs saporin-L1-linked immunotoxins.

Saporin-L1 inhibitors and uses thereof

The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.

Acyclic amine inhibitors of nucleoside phosphorylases and hydrolases

This invention relates to compounds that are analogues of coformycin, pharmaceutical compositions containing the compounds, and methods of using the compounds for treating protozoan parasite infections, especially malaria.

Analogues of coformycin and their use for treating protozoan parasite infections

The present invention relates to compounds of the general formula (I) which are inhibitors of 5'-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5&#x2032;-methylthioadenosine phosphorylase or 5&#x2032;-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.

Acyclic amine inhibitors of 5-methytioadenosine phosphorylase and nucleosidase

Disclosed are azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors, the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds. 

Azetidine analogues of nucleosidase and phosphorylase inhibitors

A process is disclosed for preparing (3R,4R)-3-hydroxy-4-hydroxymethylpyrrolidine, the compound of formula (I), or (3S,4S)-3-hydroxy-4-hydroxymethylpyrrolidine, the compound of formula (Ia) involving, as a key step, the enzyme-catalysed enantioselective hydrolysis of a racemic 3,4-trans-disubstituted pyrrolidinone compound of formula (II).

Method for preparing 3-hydroxy-4-hydroxymethyl-pyrrolidine compounds

The present invention relates to compounds of the general formula (I) which are inhibitors of purine muclioside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5'-methylthioadenosine phosphorylases (MTAP), 5&#x2032;-methylthioadenosine mucliosidases (MTAN) and/or nucleoside hydrolases (NH). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.

Fused pyrimidines as inhibitors of nucleoside phosphorylases and nucleosidases

Improved transition state analog inhibitors of ricin toxin-A are provided. Methods of using those inhibitors to inhibit ricin toxin-A and to prevent the toxic effects of ricin toxin-A in a mammal are also provided.

Growing community of inventors

Lower Hutt, New Zealand

Gary Brian Evans