发明名称 AMINOPHOSPHORIC ACID ESTER DERIVATIVE AND S1P RECEPTOR MODULATOR CONTAINING THE SAME AS ACTIVE INGREDIENT
摘要 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.
申请公布号 NZ574011(A) 申请公布日期 2011.10.28
申请号 NZ20070574011 申请日期 2007.08.07
申请人 KYORIN PHARMACEUTICAL CO., LTD. 发明人 KOHNO, YASUSHI;FUJII, KIYOSHI;SAITO, TATSUHIRO
分类号 A61K31/661;A61P1/04;A61P1/16;A61P3/10;A61P7/02;A61P9/04;A61P9/10;A61P11/00;A61P11/02;A61P11/06;A61P13/12;A61P17/00;A61P17/02;A61P21/04;A61P25/00;A61P27/14;A61P29/00;A61P31/04;A61P35/00;A61P37/02;A61P37/06;A61P37/08;A61P43/00;C07F9/09 主分类号 A61K31/661
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