US4152451A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Benzocycloheptapyrans, compositions, and method of treatment
Assignee: Eli Lilly and Co
•
Filing: 1978-03-09
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Granted: 1979-05-01
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Expires: 1998-03-09
Abstract
Abstract {PG,1 Octahydro and hexahydrobenzo{8 b{9 cyclohepta{8 d{9 pyrans having the general formula {r1 {tc,1 {rb {rd,588bbdd003 {a,1 {sd,5 {sb,27 Z{A,2 {500 {A,3 {500 {A,4 {500 {A,5 {500 {A,6 {500 {A,3 {M,1 {A,4 {RD,885 {A,2 {BA,C {SD,5 {SB,20 R{HU 3{A,2 {BN,8 {SD,15 {SB,4 R{HU 3{A,2 {500 {MR,1 {BN,55 {RD,335588BBDD00/246 {500 {A,2 {500 {A,2 {BN,0 {US,5 {SB,4 OR{HU 1{A,3 {500 {A,4 {500 {A,4 {BA,4 {SD,5 {S,5 R{HU 2{A,5 {500 {A,6 {500 {A,6 {BN,B {SD,5 {SB,28 O{RE {PS {PS wherein R{HU 1 {L is hydrogen or alkanoyl, R{HU 2 {L is alkyl or alkenyl, R{HU 3 {L is hydrogen or alkyl, and Z is a two carbon alkylene chain which is substituted or unsubstituted and saturated or unsaturated are provided. Pharmaceutical compositions containing such benzocycloheptapyrans, and a method of treating hypertension are disclosed.
Inventors
- 👤 Robert A. Archer
- 👤 Moses W. McMillan
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-10 02:27
CPC Classifications
C; C07; C07D; C07D311/00; C07D311/02; C07D311/94; A; A61; A61P; A61P25/00; A61P25/22; A61P25/24; A61P27/00; A61P27/02; A61P27/06; A61P29/00
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
97 words
A pharmaceutical formulation useful for treating hypertension which comprises a hypotensively effective amount of a compound of the formula ##STR16## wherein: R 1 is hydrogen or C 1 -C 4 alkanoyl; R 2 is C 5 -C 10 alkyl or C 5 -C 10 alkenyl; R 3 is hydrogen or methyl; and Z is selected from the group consisting of ##STR17## wherein: R 4 is hydrogen or C 1 -C 4 alkoxycarbonyl; R 5 is hydrogen or C 1 -C 4 alkyl; and R 6 is hydrogen or hydroxy, in combination with a pharmaceutically acceptable carrier therefor.
Claim 2
Dependent Claim
97 words
A pharmaceutical formulation useful for treating hypertension which comprises a hypotensively effective amount of a compound of the formula ##STR16## wherein: R 1 is hydrogen or C 1 -C 4 alkanoyl; R 2 is C 5 -C 10 alkyl or C 5 -C 10 alkenyl; R 3 is hydrogen or methyl; and Z is selected from the group consisting of ##STR17## wherein: R 4 is hydrogen or C 1 -C 4 alkoxycarbonyl; R 5 is hydrogen or C 1 -C 4 alkyl; and R 6 is hydrogen or hydroxy, in combination with a pharmaceutically acceptable carrier therefor.
Claim 3
Dependent Claim
58 words
The formulation according to claim 1 wherein in the formula defining the active ingredient, R 1 is hydrogen, R 2 is C 5 -C 10 alkyl, R 3 is methyl, and Z is selected from the group consisting of ##STR18## wherein: R 5 is hydrogen or C 1 -C 4 alkyl; and R 6 is hydrogen or hydroxy.
Claim 4
Dependent Claim
13 words
The formulation according to claim 2 wherein R 5 is hydrogen or methyl.
Claim 5
Dependent Claim
17 words
The formulation according to claim 3 wherein the active ingredient is a mixture of (±)-6a,11a-trans-1-hydroxy-3-(1,1-dimethylheptyl)-6,6,9-trimethyl-6,6a,7,10,11,11a-hexahydrobenzo[b]cyclohepta[d]pyran and (±)-6a,11a-trans-1-hydroxy-3-(1,1-dimethylheptyl)-6,6,9-trimethyl-6,6a,7,8,11,11a-hexahydrobenzo[b]cyclohepta[d]pyran.
Claim 6
Independent Claim
106 words
A method of treating hypertension comprising administering to a subject suffering from hypertension and in need of treatment or to a subject suspected of developing hypertension a hypotensively effective dose of a compound of the formula ##STR19## wherein: R 1 is hydrogen or C 1 -C 4 alkanoyl; R 2 is C 5 -C 10 alkyl or C 5 -C 10 alkenyl; R 3 is hydrogen or methyl; and Z is selected from the group consisting of ##STR20## wherein: R 4 is hydrogen or C 1 -C 4 alkoxycarbonyl; R 5 is hydrogen or C 1 -C 4 alkyl; and R 6 is hydrogen or hydroxy.
Claim 7
Independent Claim
106 words
A method of treating hypertension comprising administering to a subject suffering from hypertension and in need of treatment or to a subject suspected of developing hypertension a hypotensively effective dose of a compound of the formula ##STR19## wherein: R 1 is hydrogen or C 1 -C 4 alkanoyl; R 2 is C 5 -C 10 alkyl or C 5 -C 10 alkenyl; R 3 is hydrogen or methyl; and Z is selected from the group consisting of ##STR20## wherein: R 4 is hydrogen or C 1 -C 4 alkoxycarbonyl; R 5 is hydrogen or C 1 -C 4 alkyl; and R 6 is hydrogen or hydroxy.
Claim 8
Dependent Claim
51 words
The method according to claim 5 wherein in the compound administered, R 1 is hydrogen, R 2 is alkyl, R 3 is methyl, and Z is selected from the group consisting of ##STR21## wherein: R 5 is hydrogen or C 1 -C 4 alkyl; and R 6 is hydrogen or hydroxy.
Claim 9
Dependent Claim
11 words
The method according to claim 6 wherein R 5 is hydrogen.
Claim 10
Dependent Claim
15 words
The method according to claim 6 wherein R 5 is C 1 -C 4 alkyl.
Claim 11
Dependent Claim
11 words
The method according to claim 8 wherein R 5 is methyl.
Claim 12
Dependent Claim
14 words
The method according to claim 9 wherein in the compound administered, Z is ##STR22##
Claim 13
Dependent Claim
20 words
The method according to claim 10 wherein the compound administered is selected from the group consisting of (±)-6a,11a-trans-1-hydroxy-3-(1,1-dimethylheptyl)-6,6,9-trimethyl-6,6a,7,10,11,11a-hexahydrobenzo[b]cyclohepta[d]pyran and (±)-6a,11a-trans-1-hydroxy-3-(1,1-dimethylheptyl)-6,6,9-trimethyl-6,6a,7,8,11,11a-hexahydrobenzo[b]cyclohepta[d]pyran.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-04-30 | 1982-10-30 | 1983-05-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-04-30 | 1986-10-30 | 1987-05-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-04-30 | 1990-10-30 | 1991-05-01 | $7700.00 | Window Closed / Lapsed |