US4080458A
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Thiaprostaglandins
Assignee: Merck Patent GmbH
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Filing: 1975-05-09
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Granted: 1978-03-21
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Expires: 1995-05-09
Abstract
Abstract 13-Thiaprostanoic acid derivatives of the formula ##STR1## wherein A is --CO-- or --CHOH--, B is --CH 2 --CH 2 -- or --CH=CH--, R 1 is H or alkyl of 1 to 4 carbon atoms, m is a whole number from 0 to 5, n is a whole number from 0 to 3 or, when B is --CH=CH--, additionally 4, 5, 6, 7, 8 or 9, R 2 is alkoxy of 1 to 4 carbon atoms, phenoxy, pyridyl, thienyl, naphthyl, phenyl substituted by F, Cl, Br, OH, OCH 3 or OF 3 or phenoxy substituted by F, Cl, Br, OH, OCH 3 , CH 3 or CF 3 or, when B is --CH=CH--, additionally hydrogen, phenyl or tolyl, R 3 is H, methyl or ethyl, possess pharmacological activity, including blood pressure lowering activity.
Inventors
- 👤 Hans-Eckart Radunz
- 👤 Josef Kramer
- 👤 Manfred Baumgarth
- 👤 Dieter Orth
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 08:01
CPC Classifications
C; C07; C07C; C07C405/00; C07C405/0008; C07C405/0033; A; A61; A61P; A61P43/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
106 words
A compound of the formula ##STR6## wherein A is --CO-- or --CHOH--, B is --CH═CH--, R 1 is H or alkyl of 1 to 4 carbon atoms, m is a whole number from 0 to 5, n is a whole number from 1 to 9, R 2 is hydrogen, alkoxy of 1 to 4 carbon atoms, phenyl, tolyl, phenoxy, pyridyl, thienyl, naphthyl, phenyl substituted by F, Cl, Br, OH, OCH 3 or CF 3 , or phenoxy substituted by F, Cl, Br, OH, OCH 3 , CH 3 or CF 3 , and R 3 is H, methyl or ethyl, and the physiologically acceptable salts thereof.
Claim 2
Dependent Claim
106 words
A compound of the formula ##STR6## wherein A is --CO-- or --CHOH--, B is --CH═CH--, R 1 is H or alkyl of 1 to 4 carbon atoms, m is a whole number from 0 to 5, n is a whole number from 1 to 9, R 2 is hydrogen, alkoxy of 1 to 4 carbon atoms, phenyl, tolyl, phenoxy, pyridyl, thienyl, naphthyl, phenyl substituted by F, Cl, Br, OH, OCH 3 or CF 3 , or phenoxy substituted by F, Cl, Br, OH, OCH 3 , CH 3 or CF 3 , and R 3 is H, methyl or ethyl, and the physiologically acceptable salts thereof.
Claim 3
Dependent Claim
30 words
A compound of claim 1 wherein R 2 is phenyl, phenoxy or phenyl or phenoxy substituted by F, Cl, Br, OH, OCH 3 , CH 3 or CF 3 .
Claim 4
Dependent Claim
22 words
A compound of claim 1 wherein R 2 is phenyl substituted by F, Cl, Br, OH, OCH 3 or CF 3 .
Claim 5
Dependent Claim
25 words
A compound of claim 1 wherein R 2 is phenoxy substituted by F, Cl, Br, OH, OCH 3 , CH 3 or CF 3 .
Claim 6
Dependent Claim
10 words
A compound of claim 1 wherein R 1 is H.
Claim 7
Dependent Claim
9 words
A compound of claim 1 wherein A is --CO--.
Claim 8
Dependent Claim
9 words
A compound of claim 1 wherin A is --CHOH--.
Claim 9
Dependent Claim
39 words
A compound of claim 1 wherein R 1 is H, methyl or ethyl; R 3 is H; C n H 2n --R 2 is pentyl, hexyl, heptyl, 1-methylpentyl or 1,1-dimethylpentyl; and C m H 2m+1 is H or methyl.
Claim 10
Dependent Claim
7 words
A compound of claim 1, 9,11,15-trihydroxy-15-methyl-13-thia-5-prostenoic acid.
Claim 11
Dependent Claim
7 words
A compound of claim 1, 9,11,15-trihydroxy-16-p-fluorophenoxy-17,18,19,20-tetranor-13-thia-5-prostenoic acid.
Claim 12
Dependent Claim
7 words
A compound of claim 1, 9,11,15-trihydroxy-16-m-chlorophenoxy-17,18,19,20-tetranor-13-thia-5-prostenoic acid.
Claim 13
Dependent Claim
7 words
A compound of claim 1, 9,11-dihydroxy-16-p-fluorophenoxy-15-methoxy-17,18,19,20-tetranor-13-thia-5-prostenoic acid.
Claim 14
Dependent Claim
22 words
A pharmaceutical composition comprising a blood pressure lowering amount of a compound of claim 1 in admixture with a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
US3932487A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1981-03-20 | 1981-09-19 | 1982-03-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-03-20 | 1985-09-19 | 1986-03-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-03-20 | 1989-09-19 | 1990-03-21 | $7700.00 | Window Closed / Lapsed |