Amino-alkyl-isothioureas and processes for their preparation

C - Chemistry – Metallurgy – 07 – D

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C07D 295/14 (2006.01) C07C 335/32 (2006.01) C07D 233/42 (2006.01) C07D 295/088 (2006.01)

Patent

CA 1086758

ABSTRACT OF THE DISCLOSURE Novel compounds are provided herein which are pharmaceutically acceptable salts of an isothiourea derivative of Formula I: Image Formula I wherein n is 2, 3 or 4; R1 and R2, which may be the same or sifferent, are lower alkyl, or R1 and R2 may, together with the nitrogen atom shown, form a pyrrolidine, piperidine, morpholine, 4-lower alkyl piperazine or hexahydro-1H-azepine ring; and wherein R3 and R4, which be the same or different, are lower alkyl, or together may form a -(CH2)x- group, where x is 2, 3 or 4, These compounds may be prepared by certain reactions of dialkylamino derivatives. These compounds have immunosuppressant activity, i.e., they delay the onset and/or decrease immunosuppressant activity. In other words, they delay the onset and/or decrease the magnitude of immunological reactions. They can be used to reduce or delay immunological reactions which cause graft rejection in warm-blooded animals by administration of these compounds. The compounds are also useful in suppressing delayed hypersensitive reactions, e.g., contact sensitivity to metal ions, and in suppressing autoimmune diseases, e.g., rheumatoid arthritis and psorinsis.

278412

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