C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 233/92 (2006.01) A61K 31/4164 (2006.01) A61P 37/06 (2006.01) C07D 233/84 (2006.01) C07D 233/86 (2006.01) C12Q 1/68 (2006.01)
Patent
CA 2339090
The present invention provides methods for treating autoimmune diseases in mammals and for preventing or treating transplantation rejection in a transplant recipient. These methods utilize specifically- defined methimazole derivatives and tautomeric cyclic thione compounds, as well as pharmaceutical compositions containing those compounds. These compounds and compositions have been found to be at least as effective as methimazole in terms of pharmaceutical activity, while having less of an adverse effect on thyroid function. They are also more soluble in conventional pharmaceutical vehicles than methimazole. An assay for screening the activity of compounds useful against autoimmune diseases (ability to suppress expression of MHC Class I and II molecules) is also taught.
L'invention concerne des procédés relatifs au traitement de maladies auto-immunes chez les mammifères et à la prévention ou au traitement du rejet de greffe chez un receveur. Lesdits procédés consistent à utiliser des dérivés de méthimazole à définition spécifique et des composés à base de thiones cycliques tautomères, ainsi que des compositions renfermant ce type de composé. Les composés et les compositions en question apparaissent comme étant au moins aussi efficaces que la méthimazole en termes d'activité pharmaceutique, mais affectant moins défavorablement la fonction thyroïde. Par ailleurs leur solubilité dans les vecteurs pharmaceutiques classiques est supérieure à celle de la méthimazole. L'invention concerne également une analyse de criblage relative à l'activité des composés utiles contre les maladies auto-immunes (aptitude à inhiber l'expression des molécules du CMH de classe I et II).
Curley Robert W.
Kohn Leonard D.
Rice John M.
Macpherson Leslie & Tyerman Llp
Sentron Medical Inc.
The Government Of The United States Of America
LandOfFree
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