US4177264A
Expired / Lapsed
US
⏱️ 0.0 years remaining
N-benzyl anthracyclines
Assignee: SRI International Inc
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Filing: 1978-10-02
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Granted: 1979-12-04
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Expires: 1998-10-02
Abstract
Abstract N-Benzyl and N,N-dibenzyl derivatives of the anthracycline compounds adriamycin and daunomycin, said derivatives having anticancer properties and being active against leukemia P-388 in mice, for example. The N,N-dibenzyl derivatives have the unique quality of exhibiting a loss of DNA-binding properties.
Inventors
- 👤 Helen Y. Wu
- 👤 Thomas H. Smith
- 👤 David W. Henry
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 12:30
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/20; C07H15/24; C07H15/252
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
59 words
Compounds having the structure ##STR2## wherein R represents --COCH 3 , --CHOH--CH 3 , --COCH 2 OH and --CHOH--CH 2 OH and wherein X represents --NHCH 2 Ph and N(CH 2 Ph) 2 , and their pharmaceutically acceptable acid addition salts, with the provision that where R is --CHOH--CH 2 OH, X is not N(CH 2 Ph) 2 .
Claim 2
Dependent Claim
59 words
Compounds having the structure ##STR2## wherein R represents --COCH 3 , --CHOH--CH 3 , --COCH 2 OH and --CHOH--CH 2 OH and wherein X represents --NHCH 2 Ph and N(CH 2 Ph) 2 , and their pharmaceutically acceptable acid addition salts, with the provision that where R is --CHOH--CH 2 OH, X is not N(CH 2 Ph) 2 .
Claim 3
Dependent Claim
16 words
The compound of claim 1 which is N-benzyldaunomycin, together with its pharmaceutically acceptable acid addition salts.
Claim 4
Dependent Claim
16 words
The compound of claim 1 which is N-benzyl-13-dihydrodaunomycin, together with its pharmaceutically acceptable acid addition salts.
Claim 5
Dependent Claim
16 words
The compound of claim 1 which is N-benzyladriamycin, together with its pharmaceutically acceptable acid addition salts.
Claim 6
Dependent Claim
16 words
The compound of claim 1 which is N-benzyl-13-dihydroadriamycin, together with its pharmaceutically acceptable acid addition salts.
Claim 7
Dependent Claim
16 words
The compound of claim 1 which is N,N-dibenzyldaunomycin, together with its pharmaceutically acceptable acid addition salts.
Claim 8
Dependent Claim
16 words
The compound of claim 1 which is N,N-dibenzyl-13-dihydrodaunomycin, together with its pharmaceutically acceptable acid addition salts.
Claim 9
Dependent Claim
16 words
The compound of claim 1 which is N,N-dibenzyladriamycin, together with its pharmaceutically acceptable acid addition salts.
Claim 10
Dependent Claim
73 words
A dosage unit of a pharmaceutical composition for treating leukemia L1210 and P388 in mice comprising an amount within the range of from about 0.1 to about 500 mg per dosage unit, therapeutically effective to ameliorate leukemia, of at least one compound selected from the group consisting of N-benzyldaunomycin, N-benzyl-13-dihydrodaunomycin, N-benzyladriamycin, N-benzyl-13-dihydroadriamycin, N,N-dibenzyldaunomycin, N,N-dibenzyl-13-dihydrodaunomycin and N,N-dibenzyladriamycin, and their pharmaceutically acceptable acid addition salts, together with a pharmaceutically acceptable nontoxic carrier or diluent therefor.
Claim 11
Dependent Claim
73 words
A dosage unit of a pharmaceutical composition for treating leukemia L1210 and P388 in mice comprising an amount within the range of from about 0.1 to about 500 mg per dosage unit, therapeutically effective to ameliorate leukemia, of at least one compound selected from the group consisting of N-benzyldaunomycin, N-benzyl-13-dihydrodaunomycin, N-benzyladriamycin, N-benzyl-13-dihydroadriamycin, N,N-dibenzyldaunomycin, N,N-dibenzyl-13-dihydrodaunomycin and N,N-dibenzyladriamycin, and their pharmaceutically acceptable acid addition salts, together with a pharmaceutically acceptable nontoxic carrier or diluent therefor.
Claim 12
Dependent Claim
16 words
A pharmaceutical composition of claim 9 wherein the dosage unit takes the form of a tablet.
Claim 13
Dependent Claim
16 words
A pharmaceutical composition of claim 9 wherein the dosage unit takes the form of a capsule.
Claim 14
Dependent Claim
16 words
A pharmaceutical composition of claim 9 wherein the dosage unit takes the form of a suppository.
Claim 15
Dependent Claim
16 words
A pharmaceutical composition of claim 9 wherein the dosage unit takes the form of a cachet.
Claim 16
Dependent Claim
71 words
A pharmaceutical composition in sterile aqueous form for treating leukemia L1210 and P388 in mice comprising an amount within the range from about 0.1 to about 500 mg, effective to ameliorate leukemia, of at least one compound selected from the group consisting of N-benzyldaunomycin, N-benzyl-13-dihydrodaunomycin, N-benzyladriamycin, N-benzyl-13-dihydroadriamycin, N,N-dibenzyldaunomycin, N,N-dibenzyl-13-dihydrodaunomycin and N,N-dibenzyladriamycin and their pharmaceutically acceptable acid addition salts, together with a pharmaceutically acceptable nontoxic, sterile, inert, aqueous carrier or diluent therefor.
Claim 17
Dependent Claim
71 words
A pharmaceutical composition in sterile aqueous form for treating leukemia L1210 and P388 in mice comprising an amount within the range from about 0.1 to about 500 mg, effective to ameliorate leukemia, of at least one compound selected from the group consisting of N-benzyldaunomycin, N-benzyl-13-dihydrodaunomycin, N-benzyladriamycin, N-benzyl-13-dihydroadriamycin, N,N-dibenzyldaunomycin, N,N-dibenzyl-13-dihydrodaunomycin and N,N-dibenzyladriamycin and their pharmaceutically acceptable acid addition salts, together with a pharmaceutically acceptable nontoxic, sterile, inert, aqueous carrier or diluent therefor.
Claim 18
Dependent Claim
11 words
A pharmaceutical composition according to claim 14 in aqueous solution form.
References Cited (Backward Citations)
US3803124A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-12-03 | 1983-06-04 | 1983-12-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-12-03 | 1987-06-04 | 1987-12-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-12-03 | 1991-06-04 | 1991-12-04 | $7700.00 | Window Closed / Lapsed |