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US4166848A Expired / Lapsed US ⏱️ 0.0 years remaining

Anthracycline derivatives, their preparation and use

Assignee: Pfizer Italia SRL
•
Filing: 1977-11-14
•
Granted: 1979-09-04
•
Expires: 1997-11-14
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Abstract

Abstract Disclosed are antitumor compounds of the formula: <IMAGE> I wherein R1 is a C2-C4 alkyl; a C3-C6 cycloalkyl; a C3-C6 cycloalkyl substituted by a halogen, hydroxy, methoxy, amino or dimethylamino group; phenyl or phenyl substituted with nitro, chlorine or methoxy; thiazyl, pyridyl, pyrazyl; or a phenyl-alkyl group of the formula X-Phe-(CH2)n-, in which X is hydrogen, halogen, hydroxyl, amino, or nitro and n is an integer from 1 to 2; R2 is hydrogen, hydroxyl or acyloxy (R-COO-), where R is an alkyl having from 1 to 11 carbon atoms; and R3 is hydrogen or trifluoroacetyl and salts thereof with pharmaceutically acceptable acids. Compounds I are prepared by condensing the aglycones thereof with 2,3,6-trideoxy-3-trifluoroacetamido-4-O-trifluoro-acetyl- alpha -L-lyxopyranosyl chloride according to a conventional technique.

Inventors

  • 👤 Luigi Bernardi
  • 👤 Paolo Masi
  • 👤 Antonino Suarato
  • 👤 Federico Arcamone

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 13:41
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/20; C07H15/24; C07H15/252; A; A61; A61P; A61P35/00

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 108 words
A compound of the formula: ##STR9## wherein R 1 is a C 3 -C 6 cycloalkyl; a C 3 -C 6 cycloalkyl substituted by a halogen, hydroxy, methoxy, amino or dimethylamino group; phenyl or phenyl substituted with nitro, chlorine or methoxy; thiazyl, pyridyl, pyrazyl; or phenyl-alkyl group of the formula X--Phe--(CH 2 ) n --, in which X is hydrogen, halogen, hydroxyl, amino, or nitro, and n is an integer from 1 to 2; R 2 is hydrogen, hydroxyl or acyloxy (R--COO--), where R is an alkyl having from 1 to 11 carbon atoms; and R 3 is hydrogen or trifluoroacetyl and salts thereof with pharmaceutically acceptable acids.
Claim 2
Dependent Claim 108 words
A compound of the formula: ##STR9## wherein R 1 is a C 3 -C 6 cycloalkyl; a C 3 -C 6 cycloalkyl substituted by a halogen, hydroxy, methoxy, amino or dimethylamino group; phenyl or phenyl substituted with nitro, chlorine or methoxy; thiazyl, pyridyl, pyrazyl; or phenyl-alkyl group of the formula X--Phe--(CH 2 ) n --, in which X is hydrogen, halogen, hydroxyl, amino, or nitro, and n is an integer from 1 to 2; R 2 is hydrogen, hydroxyl or acyloxy (R--COO--), where R is an alkyl having from 1 to 11 carbon atoms; and R 3 is hydrogen or trifluoroacetyl and salts thereof with pharmaceutically acceptable acids.
Claim 3
Dependent Claim 9 words
A compound according to claim 1, which is 4-demethoxy-4-benzyloxy-N-trifluoroacetyldaunomycin.
Claim 4
Dependent Claim 10 words
A compound according to claim 1, which is 4-demethoxy-4-benzyloxy-daunomycin hydrochloride.
Claim 5
Dependent Claim 9 words
A compound according to claim 1, which is 4-demethoxy-4-cyclohexyloxy-N-trifluoroacetyldaunomycin.
Claim 6
Dependent Claim 10 words
A compound according to claim 1, which is 4-demethoxy-4-cyclohexyloxydaunomycin hydrochloride.
Claim 7
Dependent Claim 28 words
A pharmaceutical composition for inhibiting the growth of lymphocytic leukemia P 388 comprising a compound according to claim 1 in an amount sufficient to inhibit the growth thereof.
Claim 8
Dependent Claim 34 words
A method of inhibiting the growth of Lymphocytic leukemia P 388 which comprises administering to a host afflicted therewith, a compound according to claim 1, in an amount sufficient to inhibit the growth thereof.
Claim 9
Dependent Claim 12 words
A method according to claim 7, wherein said compound is administered intraperitoneally.

References Cited (Backward Citations)

US4067969A Cited
US4107423A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1982-09-03 1983-03-05 1983-09-04 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1986-09-03 1987-03-05 1987-09-04 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1990-09-03 1991-03-05 1991-09-04 $7700.00 Window Closed / Lapsed

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