University College Cardiff Consultants Limited

Nucana Plc

Nucana Biomed Limited

K.u. Leuven Research & Development

Rega Foundation

Other

National Institutes of Health, a Component of the US Dept. of Health & Human Services

Katholieke Universiteit Leuven

Roche Palo Alto LLC

Inhibitex, Inc.

Muscagen Limited

Cardiff Protides Limited

Christopher McGuigan

Jan Balzarini

Magdalena Slusarczyk

Blanka Gonczy

Paola Murziani

Hugh Griffith

Michaela Serpi

Valentina Ferrari

Carmen Jimenez Antunez

Marco Migliore

Erik De Clercq

Fabrizio Pertusati

David Bernard Smith

Susan Mary Daluge

Stanley Dawes Chamberlain

Joseph Armstrong Martin

Christopher John Yarnold

Johan Neyts

Jeff T Hutchins

John Vernachio

Bruce Caterson

Leonid Margolis

Karolina Madela

Kenneth Mills

Claire Bourdin

Antonella Carangio

Clare Louise Curtis

Emily Maguire

Klaus Klumpp

Costantino Congiatu

Edward James

Clare Elizabeth Hughes

Luis Garcia Sevillano

Christophe Vanpouille

Robin Havard Davies

Marco Derudas

Garry Jones

Andrea Lisco

Mohamed Aljarah

Arnaud Gilles

Plinio Perrone

Joachim J Bugert

Arwyn T Jones

Emyr Lloyd-Evans

Ranjith Pathirana

Laura E Farleigh

Arwyn Tomos Jones

Magdalena Slusarcyzk

Laura Elizabeth Farleigh

Joachim Jakob Bugert

The present invention relates to chemical compounds, the compounds for use in a method of treatment, particularly in a method of prophylaxis or treatment for cancer, a process for preparation of the compounds and pharmaceutical compositions comprising the compounds. The compounds may, in particular, be useful in the treatment of leukaemia, lymphoma and/or solid tumours in. The compounds are derivatives of cordycepin (3'-deoxyadenosine).

2' and/or 5′ amino-acid ester phosphoramidate 3′-deoxy adenosine derivatives as anti-cancer compounds

Phosphoramidate derivatives of 5-fluoro-2′-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with-infected cells and/or with cells with a raised level of thymidylate synthase.

Phosphoramidate derivatives of 5-fluoro-2′—deoxyuridine for use in the treatment of cancer

This invention relates to a prodrug of the monophosphate nucleotide of the well-known oncology drug gemcitabine. Specifically, it relates to gemcitabine-[phenyl-benzoxy--alaninyl)]-phosphate when present as a single phosphate diastereoisomer and, in particular, it relates to the (S)-phosphate diastereoisomer which offers a remarkable and unexpected increase in solubility relative to the (R)-diastereoisomer. The (S)-phosphate epimer is also preferentially taken up into cyclodextrin solutions over the (R)-diastereoisomer.

Gemcitabine prodrugs

Phosphoramidate derivatives of 5-fluoro-2'-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with-infected cells and/or with cells with a raised level of thymidylate synthase.

Phosphoramidate derivatives of 5-fluoro-2'-deoxyuridine for use in the treatment of cancer

Disclosed are chemical compounds, the compounds for use in a method of treatment, particularly in a method of prophylaxis or treatment for cancer, a process for preparation of the compounds and pharmaceutical compositions comprising the compounds. The compounds may, in particular, be useful in the treatment of leukaemia, lymphoma and/or solid tumours in. The compounds are derivatives of cordycepin (3'-deoxyadenosine) having a 2&#x2032; and/or 5&#x2032;-amino-acid ester phosphoramidate moiety.

2' and/or 5&#x2032; amino-acid ester phosphoramidate 3&#x2032;-deoxy adenosine derivatives as anti-cancer compounds

Compounds of general formula (I): (Formula I)) wherein R, Q, R, R, R, R, Rand Arare as defined herein are inhibitors of class I histone deacetylases and are of use in the treatment of lysosomal storage disorders, especially Niemann-Pick type C disease, as well as other lysosomal storage disorders, defective autophagy, accumulation of free cholesterol and mycobacterial diseases. 

Phosphorodiamidates and other phosphorus derivatives of fingolimod and related S1P receptor modulators

Provided are phosphoramidate nucleoside compounds of Formula (I), or pharmaceutically acceptable salts or esters or solvates thereof, useful in the treatment of cancer, viral infections and other diseases: Also provided is a process for the synthesis of compounds of Formula (I) where a desired enantiomer, having regard to the asymmetric chiral center of the phosphorus atom P, is provided in an enriched amount. The process comprises admixing a nucleoside with a phosphorochloridate in the presence of a catalyst comprising a metal salt selected from the group consisting of salts of Cu, Fe, La and Yb.

Process for preparing nucleoside prodrugs

Phosphoramidate derivates of 5-fluoro-2'-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.

This invention relates to derivatives of cladribine of Formula (I). The compounds are phosphoramidate derivatives in which the phosphoramidate moiety is situated on the 3'-hydroxyl group of cladribine. The invention also relates to pharmaceutical formulations of the cladribine derivatives and their use in methods of treatment. The compounds are useful in the treatment of cancer. 

Phosphoramidate nucleoside derivatives as anticancer agents

This invention relates to a prodrug of the monophosphate nucleotide of the well-known oncology drug gemcitabine. Specifically, it relates to gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate when present as a single phosphate diastereoisomer and, in particular, it relates to the (S)-phosphate diastereoisomer which offers a remarkable and unexpected increase in solubility relative to the (R)-diastereoisomer. The (S)-phosphate epimer is also preferentially taken up into cyclodextrin solutions over the (R)-diastereoisomer.

2' and/or 5&#x2032; amino-acid ester phosphoramidate 3&#x2032;-deoxy adenosine derivatives as anti- cancer compounds

Phosphoramidate derivatives of nucleotides and their use in the treatment of cancer are described. The base moieties of, for example, each of deoxyuridine, cytarabine, gemcitabine and citidine may be substituted at the 5-position. The phosphoramidate moiety has attached to the P atom an aryl-O moiety and an &#x3b1;-amino acid moiety. The &#x3b1;-amino acid moiety may correspond to or be derived from either a naturally occurring or a non-naturally occurring amino acid.

Phosphoramidate compounds and methods of use

Phosphoramidate derivates of 5-fluoro-2'-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with-infected cells and/or with cells with a raised level of thymidylate synthase.

Phosphoramidate derivatives of 5-fluoro-2'-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with-infected cells and/or with cells with a raised level of thymidylate synthase. 

A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH, Y is O, S or NH, Z is O, S or CH, Ris Calkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of Rand Ris OH, and the other of Rand Ris a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety Ror Rmay be (IV): in which R, R, Rand Rare each independently H or Calkyl. In preferred embodiments, one of Ror Ris valine, leucine, isoleucine or alanine, particularly valine. 

Anti-viral pyrimidine nucleoside derivatives

Growing community of inventors

Cardiff, United Kingdom

Christopher McGuigan