Abstract: 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.
Type:
Grant
Filed:
August 27, 2004
Date of Patent:
March 10, 2009
Assignee:
4 AZA Bioscience NV
Inventors:
Mark Jozef Albert Waer, Piet André Maurits Maria Herdewijn, Wolfgang Eugen Pfleiderer, Arnaud Didier Marie Marchand, Steven Cesar Alfons De Jonghe
Abstract: This invention relates to a group of trisubstituted pyrido(2,3-d)pyrimidine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates 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 derivatives are also useful in preventing or treating cardiovascular disorders, disorders of the central nervous system, TNF-? related disorders and cell proliferative disorders.
Type:
Application
Filed:
February 21, 2006
Publication date:
December 18, 2008
Applicant:
4 AZA BIOSCIENCE NV
Inventors:
Steven Cesar Alfons De Jonghe, Piet Andre Maurits Maria Herdewijn, Ling-Jie Gao
Abstract: 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: R1 C1-7 alkyl or arylalkyl; Z is a group independently defined as R1 or the group NZ together with R1 is an optionally substituted heterocyclic group containing at least one nitrogen atom; R2 is amino or acylamino; R4 is an atom or a group selected from the group consisting of hydrogen; C1-7 alkyl; and C1-7 alkoxy; and R3 is 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, C1-7 alkyl, and C1-7 alkoxy, 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, allergi
Type:
Grant
Filed:
August 29, 2003
Date of Patent:
October 2, 2007
Assignee:
4 Aza Bioscience NV
Inventors:
Mark Jozef Albert Waer, Piet André Maurits Maria Herdewijn, Wolfgang Eugen Pfleiderer
Abstract: 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.
Type:
Grant
Filed:
May 23, 2003
Date of Patent:
September 20, 2005
Assignee:
4 AZA Bioscience NV
Inventors:
Mark Jozef Albert Waer, Piet André Maurits Maria Herdewijn, Wolfgang Eugen Pfleiderer