US4499102A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Thiazolidine and pyrrolidine compounds and pharmaceutical compositions containing them
Assignee: Santen Pharmaceutical Co Ltd
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Filing: 1981-12-10
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Granted: 1985-02-12
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Expires: 2001-12-10
Abstract
Abstract Thiazolidine and pyrrolidine compounds which have the general formula ##STR1## and salts thereof for preventing or relieving diabetic complications and for reducing blood pressure, the processes for their preparation, and the compositions comprising them and pharmaceutically acceptable excipient(s).
Inventors
- 👤 Masayuki Oya
- 👤 Tadashi Iso
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 18:19
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/02; C07K5/022; C07K5/0222; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07D277/00; C07D277/02; C07D277/04; C07D277/06; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
136 words
A compound of formula (I) ##STR52## wherein R A is selected from the group consisting of (a) phenyl and naphthyl; (b) phenyl substituted by at least one substituent selected from the group consisting of lower alkyl, hydroxy, lower alkoxy, halogenolower alkoxy, acetoxy, halogen, nitro, cyano, carboxy, sulfamoyl and lower alkylsulfinyl; R B is hydroxy or lower alkoxy; R C is hydroxy, lower alkoxy or ##STR53## W is selected from the group consisting of ##STR54## wherein m is 0 or 1; n is from 1 to 12; p, r and t are each 1, 2 or 3; q is 2 or 3; X is O, SO or SO 2 ; and Y is O, S, SO or SO 2 , and salts thereof, said lower alkyl, lower alkanoyl and lower alkoxy having 1 to 6 carbon atoms.
Claim 2
Dependent Claim
136 words
A compound of formula (I) ##STR52## wherein R A is selected from the group consisting of (a) phenyl and naphthyl; (b) phenyl substituted by at least one substituent selected from the group consisting of lower alkyl, hydroxy, lower alkoxy, halogenolower alkoxy, acetoxy, halogen, nitro, cyano, carboxy, sulfamoyl and lower alkylsulfinyl; R B is hydroxy or lower alkoxy; R C is hydroxy, lower alkoxy or ##STR53## W is selected from the group consisting of ##STR54## wherein m is 0 or 1; n is from 1 to 12; p, r and t are each 1, 2 or 3; q is 2 or 3; X is O, SO or SO 2 ; and Y is O, S, SO or SO 2 , and salts thereof, said lower alkyl, lower alkanoyl and lower alkoxy having 1 to 6 carbon atoms.
Claim 3
Dependent Claim
17 words
The compound of claim 1 wherein W is --(CH 2 ) 2 --O--(CH 2 ) 2 --.
Claim 4
Dependent Claim
21 words
The compound of claim 1 wherein R A is selected from phenyl, 4-fluorophenyl, 2-nitrophenyl, 3-nitrophenyl, 4-nitrophenyl, 2-hydroxyphenyl, 3-cyanophenyl 4-cyanophenyl, and 2-hydroxy-5-sulfamoylphenyl.
Claim 5
Dependent Claim
9 words
The compound of claim 1 which is (4R)-3-[8-(ethoxycarbonyl)octanoyl]-2-(3-nitrophenyl)-4-thiazolidinecarboxylic acid.
Claim 6
Dependent Claim
11 words
The compound of claim 1 which is (4R,4'R)-3,3'-(nonanedioyl)bis[2-(3-nitrophenyl)-4-thiazolidinecarboxylic acid methyl ester].
Claim 7
Dependent Claim
9 words
The compound of claim 1 which is (4R)-3-(11-carboxyundecanoyl)-2-(3-cyanophenyl)-4-thiazolidinecarboxylic acid.
Claim 8
Dependent Claim
9 words
The compound of claim 1 which is (4R,4'R)-3,3'-(decanedioyl)bis[2-(3-cyanophenyl)-4-thiazolidinecarboxylic acid].
Claim 9
Dependent Claim
9 words
The compound of claim 1 which is (4R,4'R)-3,3'-(dodecanedioyl)bis[2-(3-cyanophenyl)-4-thiazolidinecarboxylic acid].
Claim 10
Dependent Claim
9 words
The compound of claim 1 which is (4R)-3-(8-carboxyoctanoyl)-2-(3-nitrophenyl)-4-thiazolidinecarboxylic acid.
Claim 11
Dependent Claim
9 words
The compound of claim 1 which is (4R,4'R)-3,3'-(nonanedioyl)bis[2-(3-nitrophenyl)-4-thiazolidinecarboxylic acid].
Claim 12
Dependent Claim
9 words
The compound of claim 1 which is (4R)-3-(7-carboxyheptanoyl)-2-(2-hydroxyphenyl)-4-thiazolidinecarboxylic acid.
Claim 13
Dependent Claim
9 words
The compound of claim 1 which is (4R)-3-(4-carboxybutanoyl)-2-(2-hydroxyphenyl)-4-thiazolidinecarboxylic acid.
Claim 14
Dependent Claim
31 words
The compound of claim 1 wherein W is selected from --CH(CH 3 )--CH 2 --, --(CH 2 ) 1-8 , --(CH 2 ) 10 -- and --(CH 2 ) 12 --.
Claim 15
Dependent Claim
21 words
A composition comprising an amount of the compound of claim 1 sufficient to reduce blood pressure and a pharmaceutically acceptable excipient.
Claim 16
Dependent Claim
24 words
A method of reducing blood pressure in a warm blooded animal which comprises administering the composition of claim 14 to said warm blooded animal.
Claim 17
Dependent Claim
36 words
A composition comprising an amount of the compound of claim 1 sufficient to prevent or relieve diabetes mellitus associated complications consisting of cataracts, neuropathy, nephropathy and retinopathy in a diabetic mammal, and a pharmaceutically acceptable excipient.
Claim 18
Dependent Claim
31 words
A method of preventing or relieving diabetes mellitus associated complications consisting of cataracts and retinopathy in a diabetic mammal which comprises administering the composition of claim 16 to said diabetic mammal.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-02-12 | 1988-08-13 | 1989-02-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-02-12 | 1992-08-13 | 1993-02-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-02-12 | 1996-08-13 | 1997-02-12 | $7700.00 | Window Closed / Lapsed |