Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2006-01-24
2006-01-24
McKenzie, Thomas C. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C544S260000
Reexamination Certificate
active
06989386
ABSTRACT:
In one embodiment, the present invention relates to a new class of ammonium salts of Nδ-acyl derivatives of Nα-(4-amino-4-deoxypteroyl)-L-ornithine compounds having a structure according to formula II-IV.Formula II has the structure of:wherein:R2represents up to four groups independently selected at each occurrence of R2from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C1-6alkoxy, chloro, fluoro, hydroxy, and —COOH;R3, R4, and R5are each independently selected from hydrogen and C1-6alkyl; or NR3R4taken combination can form a 5 to 7 member heterocycle having at least one nitrogen ring atom; andx is a real number greater than 0 and less than about 4.The ammonium salts provided by the invention exhibit high inhibitory activity against the growth o methotrexate-resistant cells, and also exhibit superior chemical stability than corresponding acidic Nδ-acyl derivatives of Nδ-acyl derivatives of Nα(4-amino-4-deoxypteroyl)-L-ornithine compounds.
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Bader Henry
Blumbergs Peter
Lin Ming-The
Rosowsky Andre
Ash Stevens, Inc.
Dana-Farber Cancer Institute
Day Jones
McKenzie Thomas C.
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