4 Aza Bioscience Nv

Katholieke Universiteit Leuven, Ku Leuven R&d

K.u. Leuven Research & Development

Mark Jozef Albert Waer

Wolfgang Pfleiderer

Piet André Maurits Maria Herdewijn

Piet Herdewijn

Bart Vanderhoydonck

Steven De Jonghe

Jean Herman

Ling-Jie Gao

Mi-Yeon Jang

Yuan Lin

Thierry Andre Michel Louat

Steven Cesar Alfons De Jonghe

Arnaud Didier Marie Marchand

Piet André´ M M Herdewijn

Jean Ferdinand Herman

Thierry André Michel Louat

The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R, R, R, R, R, R, R, R, R, R, and Rare as defined in the claim. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections. 

Thiazolopyrimidine modulators as immunosuppressive agents

This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydro-derivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.

Immunosuppressive effects of pteridine derivatives

This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, having the formula: wherein X represents an oxygen atom or a group with the formula NZ and wherein: RCalkyl or arylalkyl; Z is a group independently defined as Ror the group NZ together with Ris an optionally substituted heterocyclic group containing at least one nitrogen atom; Ris amino or acylamino; Ris an atom or a group selected from the group consisting of hydrogen; Calkyl; and Calkoxy; and Ris an atom or a group selected from the group consisting of aryl optionally substituted with one or more substituents selected from the group consisting of halogen, Calkyl, and Calkoxy, their pharmaceutically acceptable salts, and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and being useful in the treatment in transplant rejection, certain inflammatory diseases, cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.

The invention relates to a novel use of 8-substituted xanthine derivatives for the manufacture of a medicament for the treatment of auto-immuno disorders.

Immunosuppressive effects of 8-substituted xanthine derivatives

Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, being represented by the general formula (I).are useful as biologically active ingredients in preparing pharmaceutical compositions especially for the treatment or prevention of a CNS disorder, a cell proliferative disorder, a viral infection, an immune or auto-immune disorder or a transplant rejection. Combinations of the pteridine derivatives of the invention with an immunosuppressant or immunomodulator drug, an antineoplastic drug or an antiviral agent, providing potential synergistic effects, are also disclosed.

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Heverlee, Belgium

Mark Jozef Albert Waer