Amino alcohol derivative and immunosuppresive agent having same as an active ingredient
AssigneeKyorin Pharmaceutical Co., Ltd.
InventorsYasushi Kohno, Kiyoshi Fujii, Tatsuhiro Saito, Kazuhiko Kuriyama, Tokutarou Yasue
Life of this patent
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Abstract
An amino alcohol derivative useful as an excellent immunosuppressive agent is provided. As a result of intensive research to create a highly safe compound which has an excellent immunosuppressive activity, it was discovered that an amino alcohol derivative represented by the general formula (1), has excellent immunosuppressive activity.
Claims16
An amino alcohol derivative represented by the general formula (1a),
- wherein R3represents a methyl group, X represents an oxygen atom or a sulfur atom, and n denotes 2 or 3, or a pharmaceutically acceptable salt thereof.
An amino alcohol derivative represented by the general formula (1),
- wherein R1 represents a trifluoromethyl group, R2 represents a chlorine atom, R3 represents a methyl group, X represents an oxygen atom or a sulfur atom, and n denotes 2 or 3, or a pharmaceutically acceptable salt thereof, being obtainable by a step of allowing a compound represented by the general formula (2),
- wherein R1 represents a trifluoromethyl group, R2 represents a chlorine atom, A represents a halogen atom, X represents an oxygen atom or a sulfur atom, and n denotes 2 or 3, and a compound represented by the general formula (10),
- wherein R3 represents a methyl group and R4 represents an alkyl group having 1 to 6 carbon atoms to react in the presence of a base, and a step of subjecting the resultant product to acidolysis, then further protecting a nitrogen atom with a t-butoxycarbonyl group, reducing, and deprotecting the nitrogen atom.
(−)-2-Amino-5-[2-chloro-4-(3-trifluoromethylphenylthio)phenyl]-2-methylpentan-1-ol, or a pharmaceutically acceptable salt thereof.
A method for treating a rejection in organ transplantation or bone marrow transplantation in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of an amino alcohol derivative represented by the general formula (1a),
- wherein R3 represents a methyl group, X represents an oxygen atom or a sulfur atom, and n denotes 2 or 3, or a pharmaceutically acceptable salt thereof, as an active ingredient.
Dependencies are inferred from the claim text.