US4287205A
Expired / Lapsed
US
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Hypotensive and analgesic compounds and compositions and methods for using same
Assignee: National Foundation for Cancer Research
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Filing: 1979-11-13
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Granted: 1981-09-01
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Expires: 1999-11-13
Abstract
Abstract Novel cyclic acetals of the general formulae: ##STR1## wherein R 1 is ##STR2## wherein R 2 is hydrogen, alkyl, aryl or R 1 , wherein R 3 through R 10 are hydrogen, alkyl or aryl, wherein R 5 and R 6 together may form ═O, wherein X is hydrogen, alkyl, cycloalkyl, aryl, hydroxyaryl or arylakyl, or wherein R 8 is ##STR3## are described. Said compounds are prepared by mixing approximately equimolar amounts of the appropriate aldehyde or ketone, and enediol compound, and allowing same to react in aqueous solution under a nitrogen atmosphere. Compositions containing these novel compounds exhibit hypotensive and analgesic properties and are useful in the treatment of hypertension and pain in animals and humans.
Inventors
- 👤 Albert Szent-Gyorgyi
- 👤 Gabor B. Fodor
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:28
CPC Classifications
C; C07; C07D; C07D493/00; C07D493/02; C07D493/04; C07D317/00; C07D317/08; C07D317/10; C07D317/12; C07D317/14; C07D317/18; C07D317/20; C07D317/26
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
136 words
A compound of the formula ##STR17## wherein R 1 is selected from the group consisting of ##STR18## wherein R 2 is selected from the group consisting of hydrogen, alkyl, aryl and R 1 , wherein R 3 and R 4 are selected from the group consisting of hydrogen, alkyl, and aryl, or wherein R 3 and R 4 together form ##STR19## wherein R 5 , R 6 , R 7 , and R 8 are selected from the group consisting of hydrogen, alkyl, and aryl, wherein R 5 and R 6 together may form ═O, wherein R 8 may be ##STR20## and wherein R 9 and R 10 are selected from the group consisting of hydrogen, alkyl and aryl, and wherein X is selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, hydroxyaryl and arylalkyl.
Claim 2
Dependent Claim
136 words
A compound of the formula ##STR17## wherein R 1 is selected from the group consisting of ##STR18## wherein R 2 is selected from the group consisting of hydrogen, alkyl, aryl and R 1 , wherein R 3 and R 4 are selected from the group consisting of hydrogen, alkyl, and aryl, or wherein R 3 and R 4 together form ##STR19## wherein R 5 , R 6 , R 7 , and R 8 are selected from the group consisting of hydrogen, alkyl, and aryl, wherein R 5 and R 6 together may form ═O, wherein R 8 may be ##STR20## and wherein R 9 and R 10 are selected from the group consisting of hydrogen, alkyl and aryl, and wherein X is selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, hydroxyaryl and arylalkyl.
Claim 3
Dependent Claim
37 words
A compound of claim 1, wherein R 3 and R 4 together form ##STR21## wherein R 5 , R 6 , R 7 and R 8 are selected from the group consisting of hydrogen, alkyl and aryl.
Claim 4
Dependent Claim
37 words
A compound of claim 2, wherein R 5 and R 6 together form ═O, wherein R 8 is ##STR22## and wherein R 9 and R 10 are selected from the group consisting of hydrogen, alkyl and aryl.
Claim 5
Dependent Claim
15 words
The compound of claim 1, wherein R 1 is ##STR23## and R 2 is hydrogen.
Claim 6
Dependent Claim
15 words
The compound of claim 2, wherein R 1 is ##STR24## and R 2 is hydrogen.
Claim 7
Dependent Claim
21 words
The compound of claim 3, wherein R 1 is ##STR25## and R 2 , R 9 and R 10 are hydrogen.
Claim 8
Dependent Claim
10 words
The compound of claim 1, wherein R 1 is ##STR26##
Claim 9
Dependent Claim
10 words
The compound of claim 2, wherein R 1 is ##STR27##
Claim 10
Dependent Claim
10 words
The compound of claim 3, wherein R 1 is ##STR28##
Claim 11
Dependent Claim
21 words
An analgesic composition comprising an effective amount of a compound of claim 1 for treating pain and a pharmaceutical carrier therefor.
Claim 12
Dependent Claim
21 words
A hypotensive composition comprising an effective amount of a compound of claim 1 for treating hypertension and a pharmaceutical carrier therefor.
Claim 13
Dependent Claim
35 words
An analgesic composition comprising an effective amount of a compound of claim 1 for treating pain dissolved in about 10 to 10,000 weight percent, based on the weight of said compound, of 0.9 percent saline.
Claim 14
Dependent Claim
35 words
An hypotensive composition comprising an effective amount of a compound of claim 1 for treating hypertension dissolved in about 10 to 10,000 weight percent, based on the weight of said compound, of 0.9 percent saline.
Claim 15
Dependent Claim
18 words
A method for treating pain in humans and animals comprising intravenous injection of the composition of claim 12.
Claim 16
Dependent Claim
18 words
A method for treating hypertension in humans and animals comprising intravenous injection of the composition of claim 13.
Claim 17
Dependent Claim
18 words
A method for treating pain in humans and animals comprising intraperitoneal injection of the composition of claim 12.
Claim 18
Dependent Claim
18 words
A method for treating hypertension in humans and animals comprising intraperitoneal injection of the composition of claim 13.
References Cited (Backward Citations)
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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) | 1984-08-31 | 1985-03-02 | 1985-09-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-08-31 | 1989-03-02 | 1989-09-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-08-31 | 1993-03-02 | 1993-09-01 | $7700.00 | Window Closed / Lapsed |