US4757076A
Expired / Lapsed
US
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Method of inhibiting aromatase
Assignee: Eli Lilly and Co
•
Filing: 1984-06-18
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Granted: 1988-07-12
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Expires: 2004-06-18
Abstract
Abstract This invention provides a method of inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals by administering certain pyridine derivatives.
Inventors
- 👤 Kenneth S. Hirsch
- 👤 Harold M. Taylor
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 22:18
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
152 words
A method of inhibiting aromatase in a mammal which comprises administering to said mammal an aromatase inhibiting amount of a compound of the formula ##STR3## wherein: Q is hydrogen or ##STR4## m and n are independently 0 or 1; R is hydrogen or methyl; R 1 , R 2 , R 3 , and R 4 are independently hydrogen, methyl, C 1 -C 3 alkoxy, halo, nitro, or trifluoromethyl, or when taken together, R 1 and R 2 , and/or R 3 and R 4 are methylenedioxy; and X is hydrogen, hydroxy, methyl, C 1 -C 3 alkoxy, C 1 -C 3 alkylthio, di-(C 1 -C 3 alkyl)amino, or halo, with the proviso that whenever one or both of m or n is 1, the benzene ring to which the respective methylene group is attached must be substituted by at least one substituent other than hydrogen, or a pharmaceutically acceptable salt thereof.
Claim 2
Independent Claim
152 words
A method of inhibiting aromatase in a mammal which comprises administering to said mammal an aromatase inhibiting amount of a compound of the formula ##STR3## wherein: Q is hydrogen or ##STR4## m and n are independently 0 or 1; R is hydrogen or methyl; R 1 , R 2 , R 3 , and R 4 are independently hydrogen, methyl, C 1 -C 3 alkoxy, halo, nitro, or trifluoromethyl, or when taken together, R 1 and R 2 , and/or R 3 and R 4 are methylenedioxy; and X is hydrogen, hydroxy, methyl, C 1 -C 3 alkoxy, C 1 -C 3 alkylthio, di-(C 1 -C 3 alkyl)amino, or halo, with the proviso that whenever one or both of m or n is 1, the benzene ring to which the respective methylene group is attached must be substituted by at least one substituent other than hydrogen, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
21 words
The method according to claim 1 employing a compound wherein one of R 1 and R 2 is fluoro or chloro.
Claim 4
Dependent Claim
26 words
The method according to claim 2 employing a compound wherein Q is substituted phenyl and one of R 3 and R 4 is chloro or fluoro.
Claim 5
Dependent Claim
21 words
The method according to claim 3 employing a compound wherein the chloro or fluoro substituents are in the 4'- and 4"-positions.
Claim 6
Dependent Claim
13 words
The method according to claim 4 employing a compound wherein X is hydrogen.
Claim 7
Dependent Claim
13 words
The method according to claim 4 employing a compound wherein X is hydroxy.
Claim 8
Dependent Claim
18 words
The method according to claim 5 wherein the compound employed is 3-bis(4-chlorophenyl)methylpyridine or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
18 words
The method according to claim 6 wherein the compound employed is α,α-bis(4-chlorophenyl)-3-pyridinemethanol or a pharmaceutically acceptable salt thereof.
Claim 10
Independent Claim
153 words
A method of treating estrogen-dependent diseases in a mammal which comprises administering to said mammal an effective amount of a compound according to the formula ##STR5## wherein: Q is hydrogen or ##STR6## m and n are independently 0 or 1; R is hydrogen or methyl; R 1 , R 2 , R 3 , and R 4 are independently hydrogen, methyl, C 1 -C 3 alkoxy, halo, nitro, or trifluoromethyl, or when taken together, R 1 and R 2 , and/or R 3 and R 4 are methylenedioxy; and X is hydrogen, hydroxy, methyl, C 1 -C 3 alkoxy, C 1 -C 3 alkylthio, di(C 1 -C 3 alkyl)amino, or halo, with the proviso that whenever one or both of m or n is 1, the benzene ring to which the respective methylene group is attached must be substituted by at least one substituent other than hydrogen, or a pharmaceutically acceptable salt thereof.
Claim 11
Independent Claim
153 words
A method of treating estrogen-dependent diseases in a mammal which comprises administering to said mammal an effective amount of a compound according to the formula ##STR5## wherein: Q is hydrogen or ##STR6## m and n are independently 0 or 1; R is hydrogen or methyl; R 1 , R 2 , R 3 , and R 4 are independently hydrogen, methyl, C 1 -C 3 alkoxy, halo, nitro, or trifluoromethyl, or when taken together, R 1 and R 2 , and/or R 3 and R 4 are methylenedioxy; and X is hydrogen, hydroxy, methyl, C 1 -C 3 alkoxy, C 1 -C 3 alkylthio, di(C 1 -C 3 alkyl)amino, or halo, with the proviso that whenever one or both of m or n is 1, the benzene ring to which the respective methylene group is attached must be substituted by at least one substituent other than hydrogen, or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
43 words
The method according to claim 9 employing a compound wherein one of R 1 and R 2 is chloro or fluoro in the 4'-position, Q is substituted phenyl, and one of R 3 and R 4 is fluoro or chloro in the 4"-position.
Claim 13
Dependent Claim
15 words
The method according to claim 10 employing a compound wherein X is hydrogen or hydroxy.
Claim 14
Dependent Claim
18 words
The method according to claim 11 wherein the compound employed is 3-bis(4-chlorophenyl)methylpyridine or a pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim
18 words
The method according to claim 11 wherein the compound employed is α,α-bis(4-chlorophenyl)-3-pyridinemethanol or a pharmaceutically acceptable salt thereof.
Claim 16
Dependent Claim
13 words
The method according to claim 9 wherein the estrogen-dependent disease is breast carcinoma.
Claim 17
Dependent Claim
18 words
The method according to claim 14 wherein the compound employed is 3-bis(4-chlorophenyl)methylpyridine or a pharmaceutically acceptable salt thereof.
Claim 18
Dependent Claim
18 words
The method according to claim 14 wherein the compound employed is α,α-bis(4-chlorophenyl)-3-pyridinemethanol 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 |
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| 3.5 Years (Year 4) | 1991-07-12 | 1992-01-11 | 1992-07-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-07-12 | 1996-01-11 | 1996-07-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-07-12 | 2000-01-11 | 2000-07-12 | $7700.00 | Window Closed / Lapsed |