US4127665A
Expired / Lapsed
US
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Thienohydantoin derivatives
Assignee: Pfizer Inc
•
Filing: 1978-01-18
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Granted: 1978-11-28
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Expires: 1998-01-18
Abstract
Abstract Novel spiro-thienohydantoin derivatives useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Preferred compounds include 6,7-dihydro-spiro-[benzo(b)thiophene-4(5H),4'-imidazolidine]-2',5'-dione, 2-chloro-spiro-[cyclopenta(b) thiophene-4,4'-imidazolidine]-2',5'-dione, spiro-[cyclopenta(c)thiophene-4,4'-imidazolidine]-2',5'-dione, 1-chloro-spiro[cyclopenta(c)thiophene-4,4'-imidazolidine]-2',5'-dione and 1,3-dichloro-spiro[cyclopenta(c)thiophene-4,4'-imidazolidine]-2',5'-di one.
Inventors
- 👤 Reinhard Sarges
- 👤 Rodney C. Schnur
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 21:10
CPC Classifications
C; C07; C07D; C07D495/00; C07D495/02; C07D495/10; A; A61; A61P; A61P25/00; A61P25/18; A61P27/00; A61P27/02; A61P27/12; A61P3/00; A61P3/08; C07D333/00; C07D333/02; C07D333/04; C07D333/26; C07D333/28; C07D333/50; C07D333/78
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
109 words
A compound selected from those of the formulae: ##STR3## and the base salts thereof with pharmaceutically acceptable cations, wherein R and R 1 are each selected from hydrogen, alkyl of 1 to 4 carbon atoms, benzyl and monosubstituted benzyl wherein said substituent is selected from hydroxyl, chloro, nitro and amino; X and Y are each selected from hydrogen, alkyl of from 1 to 4 carbon atoms, chloro, bromo, fluoro, phenyl and monosubstituted phenyl wherein said substituent is selected from hydroxyl, alkyl of 1 to 4 carbon atoms, alkoxyl of 1 to 4 carbon atoms, chloro, bromo, fluoro, nitro and amino; and n is an integer from 1 to 3.
Claim 2
Dependent Claim
109 words
A compound selected from those of the formulae: ##STR3## and the base salts thereof with pharmaceutically acceptable cations, wherein R and R 1 are each selected from hydrogen, alkyl of 1 to 4 carbon atoms, benzyl and monosubstituted benzyl wherein said substituent is selected from hydroxyl, chloro, nitro and amino; X and Y are each selected from hydrogen, alkyl of from 1 to 4 carbon atoms, chloro, bromo, fluoro, phenyl and monosubstituted phenyl wherein said substituent is selected from hydroxyl, alkyl of 1 to 4 carbon atoms, alkoxyl of 1 to 4 carbon atoms, chloro, bromo, fluoro, nitro and amino; and n is an integer from 1 to 3.
Claim 3
Dependent Claim
13 words
A compound of claim 1 wherein R and R 1 are each hydrogen.
Claim 4
Dependent Claim
16 words
A compound of claim 1 wherein X and Y are each selected from hydrogen and chloro.
Claim 5
Dependent Claim
9 words
A compound of claim 1 wherein n is 1.
Claim 6
Dependent Claim
9 words
A compound of claim 1 wherein n is 2.
Claim 7
Dependent Claim
7 words
A compound of claim 1, formula I.
Claim 8
Dependent Claim
13 words
A compound of claim 6, wherein R and R 1 are each hydrogen.
Claim 9
Dependent Claim
12 words
A compound of claim 7 wherein X and Y are each hydrogen.
Claim 10
Dependent Claim
9 words
A compound of claim 8 wherein n is 2.
Claim 11
Dependent Claim
13 words
A compound of claim 7 wherein X is hydrogen and Y is chloro.
Claim 12
Dependent Claim
9 words
A compound of claim 10 wherein n is 1.
Claim 13
Dependent Claim
7 words
A compound of claim 1, formula II.
Claim 14
Dependent Claim
13 words
A compound of claim 12 wherein R and R 1 are each hydrogen.
Claim 15
Dependent Claim
12 words
A compound of claim 13, wherein X and Y are each hydrogen.
Claim 16
Dependent Claim
9 words
A compound of claim 14 wherein n is 1.
Claim 17
Dependent Claim
16 words
A compound of claim 13 wherein X and Y are each selected from hydrogen and chloro.
Claim 18
Dependent Claim
16 words
A compound of claim 16 wherein X is chloro, Y is hydrogen and n is 1.
Claim 19
Dependent Claim
16 words
A compound of claim 16 wherein X and Y are each chloro and n is 1.
Claim 20
Dependent Claim
25 words
A method of treating a diabetic host for diabetes-associated complications, which comprises administering to said host an effective amount of a compound of claim 1.
Claim 21
Dependent Claim
23 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.
References Cited (Backward Citations)
DE1135915B
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-11-27 | 1982-05-29 | 1982-11-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-11-27 | 1986-05-29 | 1986-11-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-11-27 | 1990-05-29 | 1990-11-28 | $7700.00 | Window Closed / Lapsed |