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Thiophospholipid conjugates of antitumor agents

Assignee: Health Research Inc
•
Filing: 1984-06-21
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Granted: 1986-11-11
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Expires: 2004-06-21
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Abstract

Abstract This invention relates to cytotoxic compounds. More particularly, this invention relates to conjugates of antitumor agents, and thiophospholipids exhibiting enhanced antitumor activity to methods for producing such compounds and to pharmaceutical compositions containing cytotoxically effective amounts of such compounds as a primary effective ingredient.

Inventors

  • 👤 Chung I. Hong
  • 👤 Charles R. West

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-31 14:08
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/10; C07H19/16; C07H19/20

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 96 words
A compound selected from the group of compounds having the formula ##STR4## wherein: R 1 is selected from the group consisting of alkyl and alkenyl containing from about 8 to about 22 carbon atoms; A 1 is S; A 3 , A 4 and A 5 are each 0; and X is fatty acyl containing from about 8 to about 22 carbon atoms; sugar is arabinose, esterified to the phosphate moiety at the 5'-position and covalently bonded to the heterocyclic moiety at the 1'-position to form a nucleoside; heterocyclic is cytosime and physiologically acceptable salts thereof.
Claim 2
Dependent Claim 96 words
A compound selected from the group of compounds having the formula ##STR4## wherein: R 1 is selected from the group consisting of alkyl and alkenyl containing from about 8 to about 22 carbon atoms; A 1 is S; A 3 , A 4 and A 5 are each 0; and X is fatty acyl containing from about 8 to about 22 carbon atoms; sugar is arabinose, esterified to the phosphate moiety at the 5'-position and covalently bonded to the heterocyclic moiety at the 1'-position to form a nucleoside; heterocyclic is cytosime and physiologically acceptable salts thereof.
Claim 3
Dependent Claim 1 words
1-β-D-arabinofuranosylcytosine-5'-diphosphate-rac-1-S-hexadecyl-2-0-palmitoyl-1-thioglycerol.
Claim 4
Dependent Claim 1 words
1-β-D-arabinofuranosylcytosine-5'-diphosphate-rac-1-S-hexadecyl-2-0-palmitoyl-1-thioglycerol.
Claim 5
Dependent Claim 1 words
1-β-D-arabinofuranosylcytosine-5'-diphosphaterac-1-S-octadecyl-2-0-palmitoyl-1-thioglycerol.
Claim 6
Dependent Claim 1 words
1-β-D-arabinofuranosylcytosine-5'-diphosphaterac-1-S-octadecyl-2-0-palmitoyl-1-thioglycerol.
Claim 7
Dependent Claim 31 words
A pharmaceutical composition containing from 1 to about 200 mg of a compound as defined by claim 1 in combination with 1 to about 3000 mg of a pharmaceutically acceptable carrier.

References Cited (Backward Citations)

US3937809A Cited
SU671290A1 Cited
US4291024A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1989-11-10 1990-05-12 1990-11-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1993-11-10 1994-05-12 1994-11-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1997-11-10 1998-05-12 1998-11-11 $7700.00 Window Closed / Lapsed

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