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US4416896A
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7-Oxabicyclopheptane substituted amino prostaglandin analogs useful in the treatment of thrombolytic disease
Assignee: ER Squibb and Sons LLC
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Filing: 1982-05-17
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Granted: 1983-11-22
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Expires: 2002-05-17
Abstract
Abstract 7-Oxabicycloheptane substituted amino prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Inventors
- 👤 Masami Nakane
- 👤 David L. Snitman
- 👤 Joyce Reid
- 👤 Martin F. Haslanger
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 10:40
CPC Classifications
C; C07; C07D; C07D493/00; C07D493/02; C07D493/08; A; A61; A61P; A61P11/00; A61P11/08; A61P7/00; A61P7/02
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
129 words
A compound having the structural formula ##STR20## and including all stereoisomers thereof; wherein A is CH═CH or (CH 2 ) 2 ; m is 1 to 8; n is 0 to 5; R is H or lower alkyl; and R 1 is lower alkyl, aryl, aryl-lower alkyl, lower alkoxy, aryl-lower alkoxy or ##STR21## wherein R 2 is lower alkyl, lower alkoxy, aryl, aryl-lower alkyl, aryloxy, aryl-lower alkoxy, lower alkylamino, arylamino or aryl-lower alkylamino, the term "aryl" when defining an R 1 and/or R 2 substituent or when present as part of an R 1 and/or R 2 substituent may be the same or different and is defined as phenyl, naphthyl, phenyl substituted with lower alkyl, halogen or lower alkoxy, or naphthyl substituted with lower alkyl, halogen or lower alkoxy.
Claim 2
Dependent Claim
129 words
A compound having the structural formula ##STR20## and including all stereoisomers thereof; wherein A is CH═CH or (CH 2 ) 2 ; m is 1 to 8; n is 0 to 5; R is H or lower alkyl; and R 1 is lower alkyl, aryl, aryl-lower alkyl, lower alkoxy, aryl-lower alkoxy or ##STR21## wherein R 2 is lower alkyl, lower alkoxy, aryl, aryl-lower alkyl, aryloxy, aryl-lower alkoxy, lower alkylamino, arylamino or aryl-lower alkylamino, the term "aryl" when defining an R 1 and/or R 2 substituent or when present as part of an R 1 and/or R 2 substituent may be the same or different and is defined as phenyl, naphthyl, phenyl substituted with lower alkyl, halogen or lower alkoxy, or naphthyl substituted with lower alkyl, halogen or lower alkoxy.
Claim 3
Dependent Claim
27 words
The compound as defined in claim 1 having the formula ##STR22## wherein R 1 is lower alkyl, lower alkoxy, aryl-lower alkoxy or ##STR23## including all stereoisomers thereof.
Claim 4
Dependent Claim
24 words
The compound as defined in claim 1 having the formula ##STR24## wherein R 1 is lower alkyl or aryl-lower alkyl including all stereoisomers thereof.
Claim 5
Dependent Claim
11 words
The compound as defined in claim 2 wherein A is CH═CH.
Claim 6
Dependent Claim
15 words
The compound as defined in claim 4 wherein R 1 is pentyl, hexyl or heptyl.
Claim 7
Dependent Claim
21 words
The compound as defined in claim 1 having the name [1β,2α(5Z),3β,4β]-7-[3-[(hexylamino)methyl]-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid or the methyl ester thereof or all stereoisomers thereof.
Claim 8
Dependent Claim
21 words
The compound as defined in claim 1 having the name [1β,2α(5Z),3β,4β]-7-(heptylamino)-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid or the methyl ester thereof or all stereoisomers thereof.
Claim 9
Dependent Claim
22 words
The compound as defined in claim 1 having the name [1β,2α(5Z),3α, 4β]-7-[3-[[(phenylmethoxy)amino]methyl]-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid or the methyl ester thereof or all stereoisomers thereof.
Claim 10
Dependent Claim
21 words
The compound as defined in claim 1 having the name [1β,2α(5Z),3β,4β]-7-[3-[[(phenylmethoxy)amino]methyl]-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid or the methyl ester thereof or all stereoisomers thereof.
Claim 11
Dependent Claim
19 words
The compound as defined in claim 1 having the name [1β,2α(5Z),3α,4β]-7-[3-[[2-(propoxycarbonyl)hydrazino]methyl]-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid, its methyl ester or all stereoisomers thereof.
Claim 12
Dependent Claim
36 words
A method of inhibiting platelet aggregation and bronchoconstriction, which comprises administering to the circulatory system of a mammalian host an effective amount of a compound as defined in claim 1 or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
26 words
The method as defined in claim 10 wherein said compound is administered in an amount within the range of from about 1 to about 100 mg/kg.
Claim 14
Dependent Claim
32 words
A composition for inhibiting platelet aggregation and bronchoconstriction comprising an effective amount of a compound as defined in claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier therefor.
Claim 15
Dependent Claim
30 words
A method of inhibiting platelet aggregation which comprises administering to a mammalian host an effective amount of a compound as defined in claim 1 or a pharmaceutically acceptable salt thereof.
Claim 16
Dependent Claim
32 words
A method of inhibiting bronchoconstriction associated with asthma, which comprises administering to a mammalian host an effective amount of a compound as defined in claim 1 or a pharmaceutically acceptable salt thereof.
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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) | 1986-11-21 | 1987-05-23 | 1987-11-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-11-21 | 1991-05-23 | 1991-11-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-11-21 | 1995-05-23 | 1995-11-22 | $7700.00 | Window Closed / Lapsed |