US4871764A
Expired / Lapsed
US
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12-Halogenated forskolin derivatives
Assignee: Aventis Pharmaceuticals Inc
•
Filing: 1986-11-20
•
Granted: 1989-10-03
•
Expires: 2006-11-20
Abstract
Abstract Novel 12-halogenated forskolin derivatives, intermediates and processes for their preparation, and methods for reducing intraocular pressure utilizing the compounds or compositions are disclosed.
Inventors
- 👤 Gregory M. Shutske
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 10:19
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/02; C07D309/08; C07D309/10; C07D407/00; C07D407/02; C07D407/12; A; A61; A61P; A61P27/00; A61P27/02; C07D311/00; C07D311/02; C07D311/78; C07D311/92
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
33 words
A compound of the formula ##STR20## wherein X is F, Cl, Br or I: R is hydrogen or ##STR21## where R 1 is a lower alkyl, or an optical or geometric isomer thereof.
Claim 2
Dependent Claim
33 words
A compound of the formula ##STR20## wherein X is F, Cl, Br or I: R is hydrogen or ##STR21## where R 1 is a lower alkyl, or an optical or geometric isomer thereof.
Claim 3
Dependent Claim
13 words
The compound as defined in claim 1 wherein X is F or I.
Claim 4
Dependent Claim
13 words
The compound as defined in claim 1 wherein X is Cl or Br.
Claim 5
Dependent Claim
11 words
The compound as defined in claim 1 wherein R is hydrogen.
Claim 6
Dependent Claim
10 words
The compound as defined in claim 1 which is 12-chlorodesacetylforskolin.
Claim 7
Dependent Claim
10 words
The compound as defined in claim 1 which is 12-chloroforskolin.
Claim 8
Dependent Claim
10 words
The compound as defined in claim 1 which is 12-bromodesacetylforskolin.
Claim 9
Dependent Claim
10 words
The compound as defined in claim 1 which is 12-bromoforskolin.
Claim 10
Dependent Claim
10 words
The compound as defined in claim 1 which is 12-fluorodesacetylforskolin.
Claim 11
Dependent Claim
10 words
The compound as defined in claim 1 which is 12-fluoroforskolin.
Claim 12
Dependent Claim
55 words
An intraocular pressure reducing composition comprising an inert adjuvant and, as the active ingredient, an amount effective in reducing intraocular pressure of a compound of the formula ##STR22## wherein X is F, Cl, Br or I; R is hydrogen or ##STR23## where R 1 is a lower alkyl, or an optical or geometric isomer thereof.
Claim 13
Dependent Claim
55 words
An intraocular pressure reducing composition comprising an inert adjuvant and, as the active ingredient, an amount effective in reducing intraocular pressure of a compound of the formula ##STR22## wherein X is F, Cl, Br or I; R is hydrogen or ##STR23## where R 1 is a lower alkyl, or an optical or geometric isomer thereof.
Claim 14
Dependent Claim
11 words
The composition as defined in claim 11 wherein R is hydrogen.
Claim 15
Dependent Claim
13 words
The composition as defined in claim 11 wherein said active ingredient is 12-chlorodesacetylforskolin.
Claim 16
Dependent Claim
13 words
The composition as defined in claim 11 wherein said active ingredient is 12-chloroforskolin.
Claim 17
Dependent Claim
13 words
The composition as defined in claim 11 wherein said active ingredient is 12-bromodesacetylforskolin.
Claim 18
Dependent Claim
13 words
The composition as defined in claim 11 wherein said active ingredient is 12-bromodesacetylforskolin.
Claim 19
Dependent Claim
13 words
The composition as defined in claim 11 wherein said active ingredient is 12-fluorodesacetylforskolin.
Claim 20
Dependent Claim
13 words
The composition as defined in claim 11 wherein said active ingredient is 12-fluoroforskolin.
Claim 21
Independent Claim
57 words
A method of reducing intraocular pressure in mammals comprising administering to a mammal requiring intraocular pressure reduction an intraocular pressure reducing effective amount of a compound of the formula ##STR24## wherein X is F, Cl, Br or I; R is hydrogen or ##STR25## where R 1 is a lower alkyl, or an optical or geometric isomer thereof.
Claim 22
Independent Claim
57 words
A method of reducing intraocular pressure in mammals comprising administering to a mammal requiring intraocular pressure reduction an intraocular pressure reducing effective amount of a compound of the formula ##STR24## wherein X is F, Cl, Br or I; R is hydrogen or ##STR25## where R 1 is a lower alkyl, or an optical or geometric isomer thereof.
Claim 23
Dependent Claim
11 words
The method as defined in claim 19 where R is hydrogen.
Claim 24
Dependent Claim
12 words
The method as defined in claim 19 wherein said compound is 12-chlorodesacetylforskolin.
Claim 25
Dependent Claim
12 words
The method as defined in claim 19 wherein said compound is 12-chloroforskolin.
Claim 26
Dependent Claim
12 words
The method as defined in claim 19 wherein said compound is 12-bromodesacetylforskolin.
Claim 27
Dependent Claim
12 words
The method as defined in claim 19 wherein said compound is 12-bromoforskolin.
Claim 28
Dependent Claim
12 words
The method as defined in claim 19 wherein said compound is 12-fluorodesacetylforskolin.
Claim 29
Dependent Claim
12 words
The method as defined in claim 19 wherein said compound is 12-fluoroforskolin.
References Cited (Backward Citations)
US4134986A
Cited
DE3346869A1
Cited
US4517200A
Cited
US4476140A
Cited
US4639446A
Cited
US4639443A
Cited
US4677103A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-10-02 | 1993-04-03 | 1993-10-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-10-02 | 1997-04-03 | 1997-10-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-10-02 | 2001-04-03 | 2001-10-03 | $7700.00 | Window Closed / Lapsed |