Claims
- 1. 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 the group consisting of 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenyl-silyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen or the same meanings as R.sup.1,
- 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.
- 2. 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 hydroxyl selected from the group consisting of 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenyl-siloyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen or the same meanings as R.sup.1,
- R.sup.3 is methyl, ehtyl, propyl or allyl,
- n is an integer of 1 to 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.
- 3. 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 the group consisting of 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenyl-silyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen or the same meanings as R.sup.1,
- 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.
- 4. 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 hydroxy or pharmaceutically acceptable protected hydroxy selected from the consisting of 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenyl-silyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen or the same meanings as R.sup.1,
- 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.
- 5. A method of treatment 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 the group consisting 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenyl-silyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen or the same meanings as R.sup.1,
- 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.
- 6. A method of treating diseases exhibiting delayed type hypersensitivity by external application of an effective amount of a compound of the formula: ##STR21## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from the group consisting 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenyl-silyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen or the same meanings as R.sup.1,
- 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.
- 7. A method of treating lupus erythematosus which comprises the external application of an effective amount of a compound of the formula: ##STR22## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from the group consisting 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenyl-silyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen or the same meanings as R.sup.1,
- 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.
- 8. A method of treating autoimmune diseases by the external application of an effective amount of a compound of the formula: ##STR23## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from the group consisting 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenyl-silyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen or the same meanings as R.sup.1,
- 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.
- 9. A method for treating graft-versus-host diseases by medulla ossium transplantation which comprises administering an effective amount of a compound of the formula: ##STR24## wherein R.sup.1 is hydroxy or pharmaceutically acceptable protected hydroxy selected from the group consisting 1-(lower alkylthio)(lower)alkyloxy, tri(lower)alkylsilyloxy, lower alkyl-diphenyl-silyloxy, pharmaceutically acceptable organic carboxylic acyloxy, pharmaceutically acceptable organic sulfonic acyloxy, and pharmaceutically acceptable organic carbamic acyloxy,
- R.sup.2 is hydrogen or the same meanings as R.sup.1,
- 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.
- 10. The method of any one of claim 1-9 which R.sup.1 is hydroxy, C.sub.1 -C.sub.4 alkanoyloxy which may have carboxy, cyclo (C.sub.5 -C.sub.6)alkyloxy(C.sub.1 -C.sub.4) alkanoyloxy having two (C.sub.1 -C.sub.4) alkyl groups on the cycloalkyl moiety, camphorsulfonyloxy, carboxy (C.sub.1 -C.sub.4)-alkylcarboamoyloxy, tri(C.sub.1 -C.sub.4)alkylsily-(C.sub.1 -C.sub.4) alkoxycarbonyl(C.sub.1 -C.sub.4)alkylcarbamoyloxy, benzoyloxy which may have one or two nitro, benzenesulfonyloxy having halogen, or phenyl(C.sub.1 -C.sub.4)alkanoyloxy having C.sub.1 -C.sub.4 alkoxy and trihalo(C.sub.1 -C.sub.4)alkyl, and
- R.sup.2 is hydrogen, hydroxy or C.sub.1 -C.sub.4 alkanoyloxy.
- 11. The method of claim 10, in which n is an integer of 2.
- 12. The method of claim 11, in which the symbol of a line and dotted line is a single bond.
- 13. The method of claim 12, in which R.sup.1 and R.sup.2 are each hydroxy.
- 14. The method of claim 13, in which the compound is 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone.
Priority Claims (3)
Number |
Date |
Country |
Kind |
8430455 |
Dec 1984 |
GBX |
|
8502869 |
Feb 1985 |
GBX |
|
8508420 |
Apr 1985 |
GBX |
|
Parent Case Info
This is a division of application Ser. No. 07/606,837, filed Oct. 31, 1990, now abandoned; which is a division of application Ser. No. 07/491,205, filed Mar. 9, 1986, now U.S. Pat. No. 4,929,611, which is a continuation in part of application Ser. No. 06/799,855, filed Nov. 20, 1985 now U.S. Pat. No. 4,894,366.
US Referenced Citations (3)
Number |
Name |
Date |
Kind |
4894366 |
Okuhara et al. |
Jan 1990 |
|
4929611 |
Okuhara et al. |
May 1990 |
|
4956352 |
Okuhara et al. |
Sep 1990 |
|
Divisions (2)
|
Number |
Date |
Country |
Parent |
606837 |
Oct 1990 |
|
Parent |
491205 |
Mar 1990 |
|
Continuations (1)
|
Number |
Date |
Country |
Parent |
868749 |
May 1986 |
|
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
799855 |
Nov 1985 |
|