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Details for Patent: 5,952,316

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Details for Patent: 5,952,316

Title: 2-amino-1,3-propanediol compound and immunosuppressant
Abstract:2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients. The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.
Inventor(s): Fujita; Tetsuro (Muko, JP), Sasaki; Shigeo (Kobe, JP), Yoneta; Masahiko (Kobe, JP), Mishina; Tadashi (Iruma, JP), Adachi; Kunitomo (Iruma, JP), Chiba; Kenji (Iruma, JP)
Assignee: Yoshitomi Pharmaceutical Industries, Ltd. (Osaka, JP) Taito Co., Ltd. (Tokyo, JP)
Filing Date:Aug 14, 1997
Application Number:08/911,602
Claims:1. A pharmaceutical composition which comprises an immunosuppressing effective amount of 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride in combination with an immunosuppressant selected from cyclosporin, azathioprine, a steroid and tacrolimus [FK-506].

2. A method for immunosuppression of an immune system of a mammal, which comprises administering to a mammal in need thereof an immunosuppressing effective amount of 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride in combination with an immunosuppressant selected from the group consisting of cyclosporin, azathioprine, a steroid and tacrolimus [FK-506].

3. A method for suppression of rejection in an organ or bone marrow transplantation in a mammal, which comprises administering to a mammal in need thereof a rejection suppressing effective amount of 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride in combination with an immunosuppressant selected from the group consisting of cyclosporin, azathioprine, a steroid and tacrolimus [FK-506].

4. A method for prevention or treatment of autoimmune disease, which comprises administering to a mammal in need thereof a therapeutically effective amount of 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride in combination with an immunosuppressant selected from the group consisting of cyclosporin, azathioprine, a steroid and tacrolimus [FK-506].

5. The method according to claim 4, wherein the autoimmune disease is rheumatoid arthritis.

6. A method for prevention or treatment of psoriasis or atopic dermatitis, which comprises administering to a mammal in need thereof a therapeutically effective amount of 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride in combination with an immunosuppressant selected from the group consisting of cyclosporin, azathioprine, a steroid and tacrolimus [FK-506].

7. A method for prevention or treatment of bronchial asthma or pollinosis, which comprises administering to a mammal in need thereof a therapeutically effective amount of 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride in combination with an immunosuppressant selected from the group consisting of cyclosporin, azathioprine, a steroid and tacrolimus [FK-506].

8. A method for prevention or treatment of Behcet's disease, which comprises administering to a mammal in need thereof a therapeutically effective amount of 2-amino-2-(2-(4-octylphenyl)ethyl)-1,3-propanediol hydrochloride in combination with an immunosuppressant selected from the group consisting of cyclosporin, azathioprine, a steroid and tacrolimus [FK-506].
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