Amine compound and use thereof for medical purposes

Abstract

A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(═O)(OH) 2 , X is an oxygen atom or a sulfur atom, Y is CH 2 CH 2 or CH═CH, R 1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R 2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R 3 and R 4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.

1 .- 14 . (canceled) 
     
     
         15 . A pharmaceutical composition comprising
 a compound represented by the following formula (I)   
       
         
           
           
               
               
           
         
       
       wherein
 R is a hydrogen atom or P(═O)(OH) 2 , 
 X is an oxygen atom or a sulfur atom, 
 Y is CH 2 CH, or CH═CH, 
 R 1  is trifluoromethyl, difluoromethyl, or cyano, 
 R 2  is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), 
 R 3  and R 4  may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and 
 n is 5-8, 
 
       or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof, and
 a pharmaceutically acceptable carrier, 
 which is used for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of organ or tissue transplantation; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases. 
 
     
     
         16 . The pharmaceutical composition of  claim 15 , wherein the autoimmune disease is rheumatoid arthritis, multiple sclerosis, encephalomyelitis, systemic lupus erythematosus, lupus nephritis, nephrotic syndrome, psoriasis, or Type I diabetes mellitus. 
     
     
         17 . The pharmaceutical composition of  claim 15 , wherein the allergic disease is atopic dermatitis, allergic rhinitis, or asthma.