University College Cardiff Consultants Limited

Katholieke Universiteit Leuven

K.u. Leuven Research & Development

Other

Consejo Superior De Investigaciones Cientificas

Nucana Plc

Nucana Biomed Limited

University College Cork

Technische Universitat Braunschweig

Centre National De La Recherche Scientifique

The United States of America, as Represented by the Secretary, Department of Health and Human Services

Toray Industries, Inc.

Medical Research Council

Université´ D'aix-Marseille

The University of Ferrara

Jan Balzarini

Christopher McGuigan

Magdalena Slusarczyk

Blanka Gonczy

Paola Murziani

Erik De Clercq

Monika Mazik

Marco Migliore

Wim Dehaen

Johan Neyts

Anita Maguire

Alan Ford

Maria Jose Camarasa

Sonsoles Velazquez

Pier Giovanni Baraldi

Masanori Baba

Dominique Schols

Benedikt J Sas

Christopher John Yarnold

David Loakes

Romeo Romagnoli

Johan Van Der Eycken

Johan Van Hemel

Jan Vandenkerckhove

Eric Peys

Daniel M Brown

Jean-Louis Romette

Bart Ruttens

Bruno Canard

Yasuhiro Igarashi

Leonid Margolis

Nuala Maguire

Karine Alvarez

Dolores González Pacanowska

Nicholas D Mullins

Karine Barral

Luis Miguel Ruiz Pérez

Maria José Camarasa Ríus

Sonsoles Velázquez Díaz

Victor Castillo Acosta

Joice Thomas

Sandra Liekens

Eric De Clercq

Kazuo Negishi

Kei Moriyama

Garry Jones

Rudi Pauwels

Andrea Lisco

Christophe Vanpouille

Marco Derudas

Sarah Jane Keane

Christopher Mcguigan

Magdalena Slusarcyzk

Luis Miguel Ruiz PÉREZ

Víctor Castillo Acosta

Dolores GONZÁLEZ Pacanowska

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

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

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.

The present invention relates to a class of novel pradimicins and analogues and derivatives thereof, including the compounds of formula A, I and 111, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof and their use to treat or prevent kinetoplastid infections and their use to manufacture a medicine to treat or prevent kinetoplastid infections, particularly infections withandsuch asand. wherein R, R, R, R, R, R, R, R, Rand Rare as defined in the claimor as described in detail in the description of the invention. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent kinetoplastid infections. The present invention further relates active ingredients, more specifically as medicaments for the treatment of kinetoplastid infections and pathologic conditions such as, but not limited to Trypanosomiasis, such as African trypanosomiasis, sleeping sickness, Chagas disease and leishmaniasis. 

Pradimicin derivatives for the treatment of diseases caused by kinetoplastids

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, and their use in medicine particular as anti-viral agents; wherein:

Phosphonate nucleosides useful in the treatment of viral diseases

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.

A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, wherein the groups are as defined in the claims. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula (I), and the use of compounds of formula (I) in the preparation of a medicament for treating a viral disorder. 

Phosphonucleosides useful in the treatment of viral disorders

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

A compound of formula (I) wherein Ar can be one six-membered or two fused six-membered aromatic rings; Rand Rcan be hydrogen, alkyl, cycloalkyl, halogen, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, or aryl; Q can be O, S or CY, where Y may be H, alkyl or halogen; X can be O, NH, S, N-alkyl, (CHR)where m is 1 to 10, and CY; Z can be O, S, NH, or N-alkyl; U&#x2033; is H and U' can be H or CH; wherein: T can be OH, H, halogen, O-alkyl, O-acyl, O-aryl, CN, NHor N; T&#x2032; and T&#x2033; can be H or halogen; and W can be H or a phosphate group. Compounds show anti-viral activity, for example with respect to varicella zoster virus.

Anti-viral pyrimidine nucleoside analogues

The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R, R, R, A, and X have defined meanings as described in claim. 

Anti-cancer compounds

The invention relates to compounds and methods for treating or preventing a viral infection, by administering a monophosphorylated prodrug of acyclovir or monophosphorylated derivative of an acyclovir prodrug to a subject suffering from or susceptible (to a viral infection, such as HIV infection.

Compounds and methods for the treatment of viral infection

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 mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase. 

A compound of the general formula (III): wherein X is O, S, NH or CH; Y is O, S or NH; Z is O, S or CH; Ris Calkyl, especially Calkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl; at least one of Rand Ris H&#x2014;[R&#x2014;R]&#x2014;R&#x2014;, in which: H&#x2014;[R&#x2014;R]&#x2014; comprises an oligopeptide, Rbeing an amino acid and Rbeing an amino acid selected from proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine, Ris a neutral, non-polar amino acid moiety that is bonded to Rby a peptide bond, and n is 1, 2, 3, 4 or 5; and the other of Rand Ris H&#x2014;[R&#x2014;R]n-R&#x2014; or H; or a pharmaceutically acceptable salt thereof.

Compositions for the treatment or prophylaxis of viral infections

Growing community of inventors

Heverlee, Belgium

Jan Balzarini