abstract |
Disclosed are amino phosphate derivative represented by the general formula (la), wherein R3 represents a straight-chain alkyl group having 1 to 3 carbon atoms, X represents an oxygen atom or a sulphur atom, and n denotes 2 or 3, or a pharmaceutically acceptable salt or hydrate thereof. Of particular importance are the compounds (R)-2-amino-5- [2-chloro-4-(3-trifluoromethylphenoxy)phenyl]-2-methylpentyl phosphoric acid monoester, (R)-2-amino-5-[2-chloro-4-(3-trifluoromethylphenylthio)phenyl]-2-methylpentyl phosphoric acid monoester, (R)-2-amino-4-[2-chloro-4-(3-trifluoromethylphenoxy)phenyl]-2-methylbutyl phosphoric acid monoester, (R)-2-amino-4-[2-chloro-4-(3-trifluoromethylphenylthio)phenyl]-2-methylbutyl phosphoric acid monoester, (R)-2-amino-5-[2-chloro-4-(3-trifluoromethylphenylthio)phenyl]-2-propylpentyl phosphoric acid monoester. Further disclosed is an S1P receptor modulator which comprises an amino phosphate derivative as defined above as an active ingredient for treating or preventing rejection of heart transplants, kidney transplants, skin grafts, liver transplants, bone marrow transplants, rheumatoid arthritis, lupus nephritis , systemic lupus erythematosus , Hashimoto's disease, multiple sclerosis, myasthenia gravis, diabetes mellitus, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, or allergic contact dermatitis. |