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US3915958A Expired / Lapsed US ⏱️ 0.0 years remaining

6-Substituted purine nucleotides

Assignee: Viratek Inc
•
Filing: 1972-05-22
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Granted: 1975-10-28
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Expires: 1992-05-22
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Abstract

Abstract A process of synthesizing 6-substituted purine nucleotides is disclosed, as are certain such compounds produced during synthesis which have exhibited the ability to inhibit the enzyme phosphodiesterase, to activate adenosine 3'',5''-cyclic phosphatedependent protein kinase, and, in one instance, antiviral activity and high cytotoxicity for KB and HeLa Carcinomas. As is apparent from the description which follows, such compounds also serve as intermediates in the described synthesis process.

Inventors

  • 👤 Dennis A Shuman
  • 👤 Rich B Meyer

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-31 19:43
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/052; C07H19/16; C07H19/20

Claims Analysis

Total Claims: 22
Claim 1
Independent Claim 13 words
A COMPOUND SELECTED FROM THE GROUP CONSISTING OF A COMPOUND OF THE STRUCTURE:
Claim 2
Dependent Claim 13 words
A COMPOUND SELECTED FROM THE GROUP CONSISTING OF A COMPOUND OF THE STRUCTURE:
Claim 3
Dependent Claim 17 words
The compound of claim 1 in which X is N, Y is C-NH-OR2, and R is OH.
Claim 4
Dependent Claim 10 words
The compound of claim 2 in wHich R2 is H.
Claim 5
Dependent Claim 10 words
The compound of claim 2 in which R2 is CH3.
Claim 6
Dependent Claim 10 words
The compound of claim 2 in which R2 is C2H5.
Claim 7
Dependent Claim 5 words
6-Hydroxylamino-9- Beta -D-ribofuranosylpurine 3'',5''-cyclic phosphate.
Claim 8
Dependent Claim 5 words
6-Hydroxylamino-9- Beta -D-ribofuranosylpurine 3'',5''-cyclic phosphate.
Claim 9
Dependent Claim 5 words
6-Methoxyamino-9- Beta -D-ribofuranosylpurine 3'',5''-cyclic phosphate.
Claim 10
Dependent Claim 5 words
6-Methoxyamino-9- Beta -D-ribofuranosylpurine 3'',5''-cyclic phosphate.
Claim 11
Dependent Claim 5 words
6-Ethoxyamino-9- Beta -D-ribofuranosylpurine 3'',5''-cyclic phosphate.
Claim 12
Dependent Claim 5 words
6-Ethoxyamino-9- Beta -D-ribofuranosylpurine 3'',5''-cyclic phosphate.
Claim 13
Dependent Claim 89 words
A process of synthesizing 6-substituted purine nucleotides comprising alkylating the N1 oxide function of adenosine 3'',5''-cyclic phosphate 1-N-oxide with a compound selected from the group consisting of C1 to C8 alkyl or C7 to C10 aralkyl to provide the corresponding O-alkylated adenosine 3'',5''-cyclic phosphate 1-N-oxide, subjecting said O-alkylated adenosine 3'',5''-cyclic phosphate 1-N-oxide to base catalyzed rearrangement at pH greater than 7 to afford N6-alkoxy adenosine 3'',5''-cyclic phosphate, and reacting said N6 -alkoxy compound with hydrogen sulfide causing it to undergo nucleophillic displacement to yeild the corresponding 6-thione substituted compound.
Claim 14
Dependent Claim 89 words
A process of synthesizing 6-substituted purine nucleotides comprising alkylating the N1 oxide function of adenosine 3'',5''-cyclic phosphate 1-N-oxide with a compound selected from the group consisting of C1 to C8 alkyl or C7 to C10 aralkyl to provide the corresponding O-alkylated adenosine 3'',5''-cyclic phosphate 1-N-oxide, subjecting said O-alkylated adenosine 3'',5''-cyclic phosphate 1-N-oxide to base catalyzed rearrangement at pH greater than 7 to afford N6-alkoxy adenosine 3'',5''-cyclic phosphate, and reacting said N6 -alkoxy compound with hydrogen sulfide causing it to undergo nucleophillic displacement to yeild the corresponding 6-thione substituted compound.
Claim 15
Dependent Claim 51 words
A process of synthesizing 6-substituted purine nucleotides comprising subjecting adenosine 3'',5''-cyclic phosphate-1-N-oxide to base catalyzed rearrangement at pH greater than 7 to afford 6-hydroxylamino-9- Beta -D-ribofuranoxylpurine 3'',5''-cyclic phosphate, and thereafter causing said 6-hydroxylamino derivative to undergo nucleophillic displacement by reacting itt with hydrogen sulfide to yield the corresponding 6-thione substituted compound.
Claim 16
Dependent Claim 51 words
A process of synthesizing 6-substituted purine nucleotides comprising subjecting adenosine 3'',5''-cyclic phosphate-1-N-oxide to base catalyzed rearrangement at pH greater than 7 to afford 6-hydroxylamino-9- Beta -D-ribofuranoxylpurine 3'',5''-cyclic phosphate, and thereafter causing said 6-hydroxylamino derivative to undergo nucleophillic displacement by reacting itt with hydrogen sulfide to yield the corresponding 6-thione substituted compound.
Claim 17
Dependent Claim 30 words
The process of claim 9 in which said 6-thione substituted compound is thereafter alkylated to afford 6-alkylthio-9- Beta -D-ribofuranosylpurine 3'',5''-cyclic phosphate, wherein the alkyl group is from C1 to C6.
Claim 18
Dependent Claim 27 words
The process of claim 9 in which said base catalyzed rearrangement is carried out in a refluxing solution having a pH of between about 7.0 and 9.0.
Claim 19
Dependent Claim 24 words
The process of claim 10 in which said base catalyzed rearrangement is carried out in a solution having a pH of at least 10.
Claim 20
Dependent Claim 38 words
The process of claim 9 in which said nucleophillic displacement is carried out in a closed container in the presence of an aqueous solution of pyridine containing a molar excess of hydrogen sulfide with respect to said pyridine.
Claim 21
Dependent Claim 126 words
A process of synthesizing 6-substituted purine nucleotides comprising alkylating adenosine 3'',5''-cyclic phosphate 1-N-oxide with a compound selected from the group consisting of C1 to C8 alkyl or C7 to C10 aralkyl to provide the corresponding O-alkylated adenosine 3'',5''-cyclic phosphate 1-N-oxide, subjecting said O-alkylated adenosine 3'',5''-cyclic phosphate 1-N-oxide to a refluxing solution having a pH of between about 7.0 and 9.0 at a temperature between 0* and 100*C to cause base catalyzed rearrangement and to afford N6-alkoxy adenosine 3'',5''-cyclic phosphate, and reacting said N6-alkoxy compound in a closed container in the presence of an aqueous solution of pyridine containing a molar excess of hydrogen sulfide with respect to said pyridine to cause said N6 -alkoxy compound to undergo nucleophillic displacement to yield the corresponding 6-thione substituted compound.
Claim 22
Dependent Claim 126 words
A process of synthesizing 6-substituted purine nucleotides comprising alkylating adenosine 3'',5''-cyclic phosphate 1-N-oxide with a compound selected from the group consisting of C1 to C8 alkyl or C7 to C10 aralkyl to provide the corresponding O-alkylated adenosine 3'',5''-cyclic phosphate 1-N-oxide, subjecting said O-alkylated adenosine 3'',5''-cyclic phosphate 1-N-oxide to a refluxing solution having a pH of between about 7.0 and 9.0 at a temperature between 0* and 100*C to cause base catalyzed rearrangement and to afford N6-alkoxy adenosine 3'',5''-cyclic phosphate, and reacting said N6-alkoxy compound in a closed container in the presence of an aqueous solution of pyridine containing a molar excess of hydrogen sulfide with respect to said pyridine to cause said N6 -alkoxy compound to undergo nucleophillic displacement to yield the corresponding 6-thione substituted compound.

References Cited (Backward Citations)

US3317511A Cited
US3712885A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1978-10-27 1979-04-28 1979-10-28 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1982-10-27 1983-04-28 1983-10-28 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1986-10-27 1987-04-28 1987-10-28 $7700.00 Window Closed / Lapsed

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