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Spiro-oxazolidindiones

Assignee: Pfizer Inc
•
Filing: 1978-08-21
•
Granted: 1980-04-29
•
Expires: 1998-08-21
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Abstract

Abstract Novel spiro-oxazolidindiones useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed.

Inventors

  • 👤 Rodney C. Schnur

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-26 15:22
CPC Classifications
C; C07; C07D; C07D335/00; C07D335/04; C07D335/06; A; A61; A61P; A61P25/00; A61P25/02; A61P25/22; A61P27/00; A61P27/02; A61P27/12; A61P3/00; A61P3/08; A61P3/10; C07D311/00; C07D311/02; C07D311/04; C07D311/22; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/18; C07F7/1804

Claims Analysis

Total Claims: 24
Claim 1
Independent Claim 139 words
A compound of the formula ##STR11## and the pharmaceutically acceptable salts thereof, wherein X is selected from the group consisting of oxygen and sulfur; n is one or two; R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, benzyl and monosubstituted benzyl, wherein said substituent is selected from the group consisting of chloro, bromo, fluoro, hydroxy, alkyl of 1 to 3 carbon atoms and alkoxy of 1 to 3 carbon atoms; and R 1 , R 2 and R 3 are each selected from the group consisting of hydrogen, chloro, bromo, fluoro, alkyl of 1 to 3 carbon atoms, phenyl and monosubstituted phenyl, wherein said substituent is selected from the group consisting of chloro, bromo, fluoro, hydroxy, alkyl of 1 to 3 carbon atoms and alkoxy of 1 to 3 carbon atoms.
Claim 2
Dependent Claim 139 words
A compound of the formula ##STR11## and the pharmaceutically acceptable salts thereof, wherein X is selected from the group consisting of oxygen and sulfur; n is one or two; R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, benzyl and monosubstituted benzyl, wherein said substituent is selected from the group consisting of chloro, bromo, fluoro, hydroxy, alkyl of 1 to 3 carbon atoms and alkoxy of 1 to 3 carbon atoms; and R 1 , R 2 and R 3 are each selected from the group consisting of hydrogen, chloro, bromo, fluoro, alkyl of 1 to 3 carbon atoms, phenyl and monosubstituted phenyl, wherein said substituent is selected from the group consisting of chloro, bromo, fluoro, hydroxy, alkyl of 1 to 3 carbon atoms and alkoxy of 1 to 3 carbon atoms.
Claim 3
Dependent Claim 9 words
A compound of claim 1 wherein X is oxygen.
Claim 4
Dependent Claim 9 words
A compound of claim 2 wherein n is one.
Claim 5
Dependent Claim 9 words
A compound of claim 3 wherein R is hydrogen.
Claim 6
Dependent Claim 27 words
A compound of claim 3 wherein R 1 , R 2 and R 3 are each selected from the group consisting of hydrogen, chloro, bromo and fluoro.
Claim 7
Dependent Claim 19 words
A compound of claim 4 wherein R 1 is chloro and R 2 and R 3 are each hydrogen.
Claim 8
Dependent Claim 19 words
A compound of claim 4 wherein R 1 is fluoro and R 2 and R 3 are each hydrogen.
Claim 9
Dependent Claim 19 words
A compound of claim 4 wherein R 1 is bromo and R 2 and R 3 are each hydrogen.
Claim 10
Dependent Claim 17 words
A compound of claim 4 wherein R 1 , R 2 and R 3 are each hydrogen.
Claim 11
Dependent Claim 19 words
A compound of claim 4 wherein R 1 is chloro, R 2 is hydrogen and R 3 is methyl.
Claim 12
Dependent Claim 19 words
A compound of claim 4 wherein R 1 is chloro, R 2 is hydrogen and R 3 is chloro.
Claim 13
Dependent Claim 9 words
A compound of claim 6 having negative optical rotation.
Claim 14
Dependent Claim 9 words
A compound of claim 1 wherein X is sulfur.
Claim 15
Dependent Claim 9 words
A compound of claim 13 wherein n is one.
Claim 16
Dependent Claim 9 words
A compound of claim 14 wherein R is hydrogen.
Claim 17
Dependent Claim 27 words
A compound of claim 14 wherein R 1 , R 2 and R 3 are each selected from the group consisting of hydrogen, chloro, bromo and fluoro.
Claim 18
Dependent Claim 17 words
A compound of claim 15 wherein R 1 , R 2 and R 3 are each hydrogen.
Claim 19
Dependent Claim 19 words
A compound of claim 15 wherein R 1 is fluoro and R 2 and R 3 are each hydrogen.
Claim 20
Dependent Claim 19 words
A compound of claim 15 wherein R 1 is chloro and R 2 and R 3 are each hydrogen.
Claim 21
Dependent Claim 24 words
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of claim 1 in an amount effective for the treatment of diabetes-associated complications.
Claim 22
Dependent Claim 30 words
A pharmaceutical composition according to claim 20 wherein X is oxygen, n is one, R is hydrogen, R 1 is chloro and R 2 and R 3 are each hydrogen.
Claim 23
Dependent Claim 25 words
A method for treating a diabetic host for diabetes-associated complications, which comprises administering to said host an effective amount of a compound of claim 1.
Claim 24
Dependent Claim 29 words
A method according to claim 22 wherein X is oxygen, n is one, R is hydrogen, R 1 is chloro and R 2 and R 3 are each hydrogen.

References Cited (Backward Citations)

US3532744A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1983-04-29 1983-10-29 1984-04-29 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1987-04-29 1987-10-29 1988-04-29 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1991-04-29 1991-10-29 1992-04-29 $7700.00 Window Closed / Lapsed

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