US4482709A
Expired / Lapsed
US
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Inclusion compounds of cyclodextrin with sulfur-containing compounds
Assignee: SANTEN PAHARMACEUTICAL Co Ltd
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Filing: 1982-02-24
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Granted: 1984-11-13
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Expires: 2002-02-24
Abstract
Abstract This invention relates to inclusion compounds of cyclodextrin with the compounds of the general formula [I] and salts thereof, which show pharmacological effects (for example antihypertensive effect), ##STR1## wherein A is straight or branched lower alkylene; R 1 is hydrogen or lower alkyl; R 2 is hydrogen, lower alkyl, phenyl, phenyl-lower alkyl, hydroxyphenyl-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, guanidino-lower alkyl, imidazolyl-lower alkyl, indolyl-lower alkyl, mercapto-lower alkyl or lower alkylthio-lower alkyl; R 1 or R 2 may join to complete pyrrolidine ring or thiazolidine ring, and each ring may be substituted by phenyl or pyridyl, and phenyl may be resubstituted by hydroxy, lower alkoxy, halogen, nitro or sulfamoyl; R 3 is hydrogen or ##STR2## said lower alkyl and lower alkoxy having 1 to 6 carbon atoms.
Inventors
- 👤 Jun-ichi Iwao
- 👤 Tadashi Iso
- 👤 Masayuki Oya
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 12:36
CPC Classifications
C; C07; C07C; C07C319/00; C07C319/14; C07C319/20; A; A61; A61K; A61K47/00; A61K47/50; A61K47/69; A61K47/6949; A61K47/6951; B; B82; B82Y; B82Y5/00; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07D277/00; C07D277/02; C07D277/04; C07D277/06; C08; C08B; C08B37/00; C08B37/0006; C08B37/0009; C08B37/0012; C08B37/0015
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
130 words
An inclusion complex of cyclodextrin with a compound of formula [I] and pharmaceutically acceptable salts thereof, ##STR5## wherein A is straight or branched lower alkylene; R 1 is hydrogen or lower alkyl; R 2 is selected from the group consisting of hydrogen, lower alkyl, phenyl, phenyl-lower alkyl, hydroxyphenyl-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, guanidino-lower alkyl, imidazolyl-lower alkyl, indolyl-lower alkyl, mercapto-lower alkyl and lower alkylthio-lower alkyl; wherein R 1 and R 2 may join to complete a pyrrolidine ring or a thiazolidine ring, and each of said rings may be substituted by a substituent selected from the group consisting of phenyl, phenyl substituted with hydroxy, lower alkoxy, halogen, nitro and sulfamoyl, and pyridyl; R 3 is hydrogen or ##STR6## said lower alkyl and lower alkoxy having 1 to 6 carbon atoms.
Claim 2
Dependent Claim
130 words
An inclusion complex of cyclodextrin with a compound of formula [I] and pharmaceutically acceptable salts thereof, ##STR5## wherein A is straight or branched lower alkylene; R 1 is hydrogen or lower alkyl; R 2 is selected from the group consisting of hydrogen, lower alkyl, phenyl, phenyl-lower alkyl, hydroxyphenyl-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, guanidino-lower alkyl, imidazolyl-lower alkyl, indolyl-lower alkyl, mercapto-lower alkyl and lower alkylthio-lower alkyl; wherein R 1 and R 2 may join to complete a pyrrolidine ring or a thiazolidine ring, and each of said rings may be substituted by a substituent selected from the group consisting of phenyl, phenyl substituted with hydroxy, lower alkoxy, halogen, nitro and sulfamoyl, and pyridyl; R 3 is hydrogen or ##STR6## said lower alkyl and lower alkoxy having 1 to 6 carbon atoms.
Claim 3
Dependent Claim
11 words
The inclusion complex of claim 1, wherein R 3 is hydrogen.
Claim 4
Dependent Claim
11 words
The inclusion complex of claim 1, wherein R 3 is ##STR7##
Claim 5
Dependent Claim
34 words
The inclusion complex of claim 1, wherein A is selected from the group consisting of --CH 2 CH 2 --, --CH 2 CH(CH 3 )--, --C(CH 3 ) 2 -- and --CH(CH 3 )--.
Claim 6
Dependent Claim
15 words
The inclusion complex of claim 1, wherein the compound of formula [I] is (2R,4R)-2-(2-hydroxyphenyl)-3-(3mercaptopropanoyl)-4-thiazolidinecarboxylic acid.
Claim 7
Dependent Claim
15 words
The inclusion complex of claim 1, wherein the compound of formula [I] is (2S)-1-[(2S)-3-mercapto-2-methylpropanoyl]-2-pyrrolidinecarboxylic acid.
Claim 8
Dependent Claim
15 words
The inclusion complex of claim 1, wherein the compound of formula [I] is (4R,4'R)-3,3'-[3,3'-dithiobis(propanoyl)]bis-[2-(2-hydroxyphenyl)-4-thiazolidinecarboxylic acid].
Claim 9
Dependent Claim
14 words
The inclusion complex of claim 1, wherein the compound of formula [I] is N-(2-mercapto-2-methylpropanoyl)-L-cysteine.
Claim 10
Dependent Claim
14 words
The inclusion complex of claim 1, wherein the compound of formula [I] is N-(2-mercaptopropanoyl)glycine.
Claim 11
Dependent Claim
35 words
The inclusion complex of claim 2, wherein A is is selected from the group consisting of --CH 2 CH 2 --, --CH 2 CH(CH 3 )--, --C(CH 3 ) 2 -- and --CH(CH 3 ).
Claim 12
Dependent Claim
35 words
The inclusion complex of claim 2, wherein A is is selected from the group consisting of --CH 2 CH 2 --, --CH 2 CH(CH 3 )--, --C(CH 3 ) 2 -- and --CH(CH 3 ).
Claim 13
Dependent Claim
11 words
The inclusion complex of claim 1, wherein said cyclodextrin is beta-cyclodextrin.
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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) | 1987-11-13 | 1988-05-14 | 1988-11-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-11-13 | 1992-05-14 | 1992-11-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-11-13 | 1996-05-14 | 1996-11-13 | $7700.00 | Window Closed / Lapsed |