Method for immunosuppression
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsMasakuni Okuhara, Hirokazu Tanaka, Toshio Goto, Tohru Kino, Hiroshi Hatanaka
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Abstract
This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases, infectious diseases, and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to a use thereof.
Claims5
A method for treating resistance to transplantation which comprises administering an effective amount of a compound of the formula:
- ##STR16## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenylsilyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen, hydroxy or lower alkanoyloxy,
- R.sup.3 is methyl, ethyl, propyl or allyl,
- n is an integer of 1 or 2, and
- the symbol of a line and dotted line is a single bond or a double bond,
- or pharmaceutically acceptable basic salt thereof to a subject in need of said treatment.
A method for treating autoimmune disease which comprises administering an effective amount of a compound of the formula:
- ##STR17## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenylsilyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen, hydroxy or lower alkanoyloxy,
- R.sup.3 is methyl, ethyl, propyl or allyl,
- n is an integer of 1 or 2, and
- the symbol of a line and dotted line is a single bond or a double bond,
- or pharmaceutically acceptable basic salt thereof to a subject in need of said treatment.
A method for treating infectious diseases which comprises administering an effective amount of a compound of the formula:
- ##STR18## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenylsilyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen, hydroxy or lower alkanoyloxy,
- R.sup.3 is methyl, ethyl, propyl or allyl,
- n is an integer of 1 or 2, and
- the symbol of a line and dotted line is a single bond or a double bond,
- provided that when R.sup.1 and R.sup.2 are each hydroxy, n is an integer of 2 and the symbol of a line and dotted line is a single bond, then R.sup.3 is methyl, propyl or allyl, or pharmaceutically acceptable basic salt thereof to a subject in need of said treatment.
A method for treatment of diseases beneficially treated by external administration of compounds having immunosuppressive activity in a patient in need of such treatment, which comprises externally administering to such patient a compound of the formula:
- ##STR19## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenylsilyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen, hydroxy or lower alkanoyloxy,
- R.sup.3 is methyl, ethyl, propyl or allyl,
- n is an integer of 1 or 2, and
- the symbol of a line and dotted line is a single bond or a double bond,
- or pharmaceutically acceptable basic salt thereof.
A method for treatment of diseases beneficially treated by administration of compounds having immunosuppressive activity in a patient in need of such treatment, which comprises administering to such patient a compound of the formula:
- ##STR20## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenylsilyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen, hydroxy or lower alkanoyloxy,
- R.sup.3 is methyl, ethyl, propyl or allyl,
- n is an integer of 1 or 2, and
- the symbol of a line and dotted line is a single bond or a double bond,
- or pharmaceutically acceptable basic salt thereof.
Dependencies are inferred from the claim text.