Other

Isa Pharmaceuticals B.v.

Nederlandse Organisatie Voor Toegepast-natuurwetenschappelijk Onderzoek

Universiteit Leiden

Academisch Ziekenhuis Leiden

Universitätsklinikum Freiburg

Gijsbert Arie Van Der Marel

Jacobus Hubertus Van Boom

Louis Hartog Cohen

Selina Khan

Cornelis Johannes Maria Melief

Ferdinand Antonius Ossendorp

Elsbet Jantine Pieterman

Mark Overhand

Dmitri Viktorovitsj Filippov

Johannes Huebner

Cornelis Johannes Melief

Jeroen Dirk Cornelis Codée

Wouter Frederick Johan Hogendorf

Steven Hendrik Leonard Verhelst

Nicolaas Johannes Meeuwenoord

Adrianus Petrus Valentijn

Dmitri V Filippov

Ferry Ossendorp

Herman Steven Overkleeft

Andrea Kropec-Huebner

Geoffroy P P Gential

Hans Van Den Elst

Nicolette Voskuyl

Andrea Huebner-Kropec

Brigitte Elisa Anna Burm

Wouter Frederik Johan Hogendorf

Adjuvant compounds are described, as well as their conjugates comprising peptide antigens or other immunomodulatory moieties. Also described are methods of modulating immune responses in a subject in need thereof, as well as methods of treating cancer, viral or bacterial infections comprising administering the adjuvant compounds or the conjugates to a subject in need thereof.

Peptide-containing adjuvant compounds having peg spacers

The invention is directed to a compound according to the formula [1] wherein Rand Rare branched or straight groups having up to 17 atoms selected from carbon, nitrogen, oxygen and sulphur, n is 0 to and including 18, Y is sulphur or selene, X is S or O and R is &#x2014;OH or an organic group comprising one or more peptides, one or more nucleic acids, one or more antibodies or combinations thereof. The invention is also directed to process for preparing said compound and the use of said compound as an adjuvant. The invention is also directed to a composition comprising said compound and the use of said composition, for example as a vaccine composition.

Adjuvant compound

The invention is directed to a compound according to the formula [1] wherein Rand Rare branched or straight groups having up to 17 atoms selected from carbon, nitrogen, oxygen and sulphur, n is 0 to and including 18, Y is sulphur or selene, X is S or 0 and R is &#x2014;OH or an organic group comprising one or more peptides, one or more nucleic acids, one or more antibodies or combinations thereof. The invention is also directed to process for preparing said compound and the use of said compound as an adjuvant. The invention is also directed to a composition comprising said compound and the use of said composition, for example as a vaccine composition.

The present invention relates to synthetic lipoteicoic acid (LTA) mimetics which are useful as vaccine components for therapy and/or prophylaxis of bacterial infection.

Synthetic LTA mimetics and use thereof as vaccine component for therapy and/or prophylaxis against gram-positive infections

Novel peptide-like FPP-analogues suitable for inhibiting protein:prenyl transferases, such as protein:geranylgeranyl transferase-1, and other prenyl pyrophosphate-consuming enzymes such as squalene synthase and geranylgeranyl pyrophosphate synthase are disclosed.

Inhibitors of prenylated pyrophosphate consuming enzymes

Protein:prenyl transferase inhibitors

The invention provides a method for inhibiting protein isoprenylation by administration of a polyisoprenyl pyrophosphate analogue. The polyisoprenyl pyrophosphate analogue may have formula 1, ##STR1## wherein: Pren represents a C.sub.10 -C.sub.30 terpenoid group or a derivative thereof; A.sup.1, A.sup.2, A.sup.3 and A.sup.4 independently represent a direct bond or a C.sub.1 -C.sub.4 alkylene or alkenylene group, optionally having substituents selected from methyl, hydroxy, methoxy, mercapto, methylthio, amino, methylamino, dimethylamino, halogen and a group having formula --X.sup.5 --A.sup.5 --P(.dbd.Z.sup.2)Y.sup.2 Y.sup.3 ; A.sup.5 represents a direct bond or a C.sub.1 -C.sub.4 alkylene or alkenylene group; X.sup.1, X.sup.2, X.sup.3, X.sup.4 and X.sup.5 independently represent a direct bond, oxygen, sulphur, imino or methylimino; Y.sup.1, Y.sup.2 and Y.sup.3 independently represent hydroxy, alkoxy, mercapto, alkylthio, amino, mono- or di-alkylamino, alkyl, alkenyl, alkynyl, cycloalkyl, aryl or arylalkyl, whereby one of Y.sup.1, Y.sup.2 and Y.sup.3 may also represent a C.sub.7 -C.sub.30 alkyl or alkenyl group or a group having formula --X.sup.5 --A.sup.5 --P(.dbd.Z.sup.2)Y.sup.2 Y.sup.3 and two of Y.sup.1, Y.sup.2 and Y.sup.3 may together represent an oxygen or sulfur atom or an imino or methylene group; Z.sup.1 and Z.sup.2 independently represent oxygen or sulphur; and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof. The invention further provides a pharmaceutical composition containing such a polyisoprenyl pyrophosphate analogue, which composition is suitable for the treatment of carcinomas such as by the inhibition of the isoprenylation of a member of the ras protein family.

Method for the treatment of diseases related with protein isoprenylation

Growing community of inventors

Leiden, Netherlands

Gijsbert Arie Van Der Marel