Albert Einstein College of Medicine

Industrial Research Limited

Other

Victoria Link Limited

Tasman Forestry Limited

Alber Einslein College of Medicine

Callaghan Innovation Research Limited

Albert Einstein College of Medecine of Yeshiva University

Richard Hubert Furneaux

Vern L Schramm

Peter Charles Tyler

Gary Brian Evans

Keith Clinch

Peter Michael Kelly

Olga Vladimirovna Zubkova

Shivali Ashwin Gulab

Dirk Henning Lenz

Phillip Martin Rendle

Jennifer Mary Mason

Kami Kim

Ian Sims

Anthony David Woolhouse

Ben William Greatrex

Richard Fröhlich

Antti Marko Haapalainen

Richard Frohlich

Shivall Ashwah Ashwin Gulab

Beverley Janice Nairn

Shanzhi Wang

Simon Peter Harold Mee

Richard Froehlich

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 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

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

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.

Transition state analog inhibitors of ricin A-chain

5h-pyrrolo[3,2-D] pyrimidine inhibitors of nucleoside phosphorylases and nucleosidases

A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH, NHR, H or halogen; D is chosen from OH, NH, NHR, H halogen or SCH; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof,which comprises reacting a compound of the formula (II) with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX),   The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).

Process for preparing inhibitors of nucleoside metabolism

The present invention provides compounds having the formula: wherein A is CH or N; B is chosen from OH, NH, NHR, H or halogen; D is chosen from OH, NH, NHR, H, halogen or SCH; R is an optionally substituted alkyl, aralkyl or aryl group; and X and Y are independently selected from H, OH or halogen except that when one of X and Y is hydroxy or halogen, the other is hydrogen; and Z is OH or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof; and compounds having the formula: wherein A, X, Y, Z and R are defined for compounds of formula (I) where first shown above; E is chosen from COH or a corresponding salt form, COR, CN, CONH, CONHR or CONR; and G is chosen from NH, NHCOR, NHCONHR or NHCSNHR; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof. The present invention also provides the use of the above compounds as pharmaceuticals, pharmaceutical compositions containing the compounds and processes for preparing the compounds.

Inhibitors of nucleoside metabolism

A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH, NHR, H or halogen; D is chosen from OH, NH, NHR, H halogen or SCH; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof,which comprises reacting a compound of the formula (II) with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX), to form a compound of formula (XX)  The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).

The present invention provides a compound of the formula (I): wherein A is selected from N, CH and CR, where R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH, NHR, NRRand SR, where R, Rand Rare each optionally substituted alkyl, aralkyl or aryl groups; B is selected from OH, NH, NHR, H and halogen, where Ris an optionally substituted alkyl, aralkyl or aryl group; D is selected from OH, NH, NHR, H, halogen and SCH, where Ris an optionally substituted alkyl, aralkyl or aryl group; X and Y are independendy selected from H, OH and halogen, with the proviso that when one of X and Y is hydroxy or halogen, the other is hydrogen; Z is OH, or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ and OQ, where Q is an optionally substituted alkyl, aralkyl or aryl group; and W is OH or H, with the proviso that when W is OH, then A is CR where R is as defined above; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof. The invention also provides pharmaceutical compositions comprising compounds of formula (I), methods of preparing compounds of formula (I), and methods of treatment using compounds of formula (I).

5H-pyrrolo[3,2-d]pyrimidine nucleoside metabolism inhibitors

The invention provides a compound of the formula: wherein A is selected from N, CH and CR; R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH, NHR, NRRand SR; R, Rand Rare each optionally substituted alkyl, aralkyl or aryl groups; B is selected from NHand NHR; Ris an optionally substituted alkyl, aralkyl or aryl group; X is selected from H, OH and halogen; Z is selected from H, Q, SQ and OQ; Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer, a pharmaceutically acceptable salt, an ester, or a prodrug thereof; with the proviso that the stereochemistry of the aza-sugar moiety is D-ribo or 2'-deoxy-D-erythro-; pharmaceutical compositions comprising said compound; and methods of treatment using said compound.

Growing community of inventors

Wellington, New Zealand

Richard Hubert Furneaux