Pharmaceutical agents containing methotrexate derivatives

A - Human Necessities – 61 – K

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A61K 31/665 (2006.01) A61K 31/505 (2006.01) A61K 31/519 (2006.01) A61K 31/54 (2006.01) A61K 31/5415 (2006.01) C07D 475/08 (2006.01)

Patent

CA 2216647

Compounds represented by general formula (I) or salts thereof, (wherein R1 represents a member selected from the group consisting of CH2, CH2CH2, CH2O, CH2S and CH2SO; R2 represents hydrogen, lower (C1-4) alkyl or benzyl; R3 represents COOR4, NHCOR5, CONR6R7, PO3H2 or SO3H; and n is an integer of from 1 to 4) which are useful as a remedy for autoimmune diseases such as systemic lupus erythematosus or nephritis such as glomerulonephritis.

La présente invention concerne des composés représentés par la formule générale (I), ou des sels de ces composés, formule dans laquelle R¿1? est un élément choisi dans le groupe constitué par CH¿2?, CH¿2?CH¿2?, CH¿2?O, CH¿2?S et CH¿2?SO; R¿2? est hydrogène, benzyle ou alkyle C¿1-4? inférieur; R¿3? est COOR¿4?, NHCOR¿5?, CONR¿6?R¿7?, PO¿3?H¿2? ou SO¿3?H, et n est un nombre entier de 1 à 4. Ils sont utiles comme remèdes pour les maladies auto-immunes telles que le lupus érythémateux aigu disséminé ou les néphrites telles que la glomérulonéphrite.

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