US4929611A
Expired / Lapsed
US
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Method for immunosuppression
Assignee: Astellas Pharma Inc
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Filing: 1986-05-30
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Granted: 1990-05-29
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Expires: 2006-05-30
Abstract
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.
Inventors
- 👤 Masakuni Okuhara
- 👤 Hirokazu Tanaka
- 👤 Toshio Goto
- 👤 Tohru Kino
- 👤 Hiroshi Hatanaka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 00:30
CPC Classifications
C; C07; C07H; C07H17/00; C07D; C07D498/00; C07D498/12; C07D498/18; A; A61; A61P; A61P31/00; A61P31/04; A61P37/00; A61P37/02; A61P37/06; C07H19/00; C07H19/01; C12; C12N; C12N1/00; C12N1/20; C12N1/205; C12P; C12P17/00; C12P17/18; C12P17/188; C12P19/00; C12P19/44; C12R; C12R2001/00; C12R2001/01; C12R2001/465; C12R2001/55; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55; Y10; Y10S; Y10S435/00; Y10S435/8215; Y10S435/822; Y10S435/886; Y10S435/898
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
108 words
A method for treating resistance to transplantation which comprises administering an effective amount of a compound of the formula: ##STR16## wherein R 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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.
Claim 2
Independent Claim
108 words
A method for treating resistance to transplantation which comprises administering an effective amount of a compound of the formula: ##STR16## wherein R 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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.
Claim 3
Independent Claim
107 words
A method for treating autoimmune disease which comprises administering an effective amount of a compound of the formula: ##STR17## wherein R 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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.
Claim 4
Independent Claim
107 words
A method for treating autoimmune disease which comprises administering an effective amount of a compound of the formula: ##STR17## wherein R 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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.
Claim 5
Independent Claim
145 words
A method for treating infectious diseases which comprises administering an effective amount of a compound of the formula: ##STR18## wherein R 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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 1 and R 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 3 is methyl, propyl or allyl, or pharmaceutically acceptable basic salt thereof to a subject in need of said treatment.
Claim 6
Independent Claim
145 words
A method for treating infectious diseases which comprises administering an effective amount of a compound of the formula: ##STR18## wherein R 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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 1 and R 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 3 is methyl, propyl or allyl, or pharmaceutically acceptable basic salt thereof to a subject in need of said treatment.
Claim 7
Independent Claim
117 words
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 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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.
Claim 8
Independent Claim
117 words
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 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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.
Claim 9
Independent Claim
115 words
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 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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.
Claim 10
Independent Claim
115 words
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 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 2 is hydrogen, hydroxy or lower alkanoyloxy, R 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.
References Cited (Backward Citations)
US3244592A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-05-28 | 1993-11-27 | 1994-05-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-05-28 | 1997-11-27 | 1998-05-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-05-28 | 2001-11-27 | 2002-05-29 | $7700.00 | Window Closed / Lapsed |