Patent US4605674A successfully refreshed from Google Patents.
US4605674A
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Substituted acetophenones and compositions containing them
Assignee: Hoffmann La Roche Inc
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Filing: 1984-04-24
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Granted: 1986-08-12
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Expires: 2004-04-24
Abstract
Abstract Antivirally active compounds of the formula <IMAGE> I wherein R1 represents hydroxy, acyloxy derived from an aliphatic acid having 2-18 carbon atoms or a heterocyclic carboxylic acid containing nitrogen atom(s), lower alkoxycarbonyloxy, aminoacyloxy or carboxyalkanoyloxy; R2 represents lower alkoxy; R3 represents hydrogen or lower alkoxy; and R4 represents phenyl which may be substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dialkylamino, amino, cyano, hydroxy, halo and alkylenedioxy; or pyridyl, furyl, thienyl or pyrrolyl which may be substituted by lower alkyl, pharmaceutical compositions containing them and a process for the preparation of those compounds of formula I which are novel.
Inventors
- 👤 Morio Fujiu
- 👤 Yasuji Suhara
- 👤 Hideo Ishitsuka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 09:22
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/30; C07D207/32; C07D207/33; C07D207/333; A; A61; A61P; A61P31/00; A61P31/12; C07C; C07C255/00; C07C323/00; C07C45/00; C07C45/61; C07C45/67; C07C45/68; C07C45/72; C07C45/74; C07C49/00; C07C49/76; C07C49/84; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/44; C07D213/46; C07D213/50; C07D213/60; C07D213/78; C07D213/79; C07D213/80; C07D241/00; C07D241/02; C07D241/10; C07D241/14; C07D241/24; C07D307/00; C07D307/02; C07D307/34; C07D307/38; C07D307/40; C07D307/46; C07D317/00; C07D317/08; C07D317/44; C07D317/46; C07D317/48; C07D317/50; C07D317/54; C07D333/00; C07D333/02; C07D333/04; C07D333/06; C07D333/22
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
128 words
A method for treating an animal afflicted with a viral infection, which method comprises administering to such animal a compound of the formula: ##STR6## wherein R 1 represents hydroxy; acyloxy derived from an aliphatic acid having 2-18 carbon atoms or derived from a heterocyclic carboxylic acid containing one or more nitrogen atoms; lower alkoxycarbonyloxy; aminoacyloxy or carboxyalkanoyloxy; R 2 represents lower alkoxy; R 3 represents hydrogen or lower alkoxy; and R 4 represents phenyl which is unsubstituted or substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dialkylamino, amino, cyano, hydroxy, halo and alkylenedioxy; or pyridyl, furyl, thienyl or pyrrolyl any of which is unsubstituted or substituted by lower alkyl, in an amount effective for inhibiting viral infections.
Claim 2
Independent Claim
128 words
A method for treating an animal afflicted with a viral infection, which method comprises administering to such animal a compound of the formula: ##STR6## wherein R 1 represents hydroxy; acyloxy derived from an aliphatic acid having 2-18 carbon atoms or derived from a heterocyclic carboxylic acid containing one or more nitrogen atoms; lower alkoxycarbonyloxy; aminoacyloxy or carboxyalkanoyloxy; R 2 represents lower alkoxy; R 3 represents hydrogen or lower alkoxy; and R 4 represents phenyl which is unsubstituted or substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dialkylamino, amino, cyano, hydroxy, halo and alkylenedioxy; or pyridyl, furyl, thienyl or pyrrolyl any of which is unsubstituted or substituted by lower alkyl, in an amount effective for inhibiting viral infections.
Claim 3
Dependent Claim
20 words
The method for treating an animal afflicted with a viral infection of claim 1 wherein the compound is 4'-ethoxy-2'-hydroxy-4-6'-dimethoxy chalcone.
Claim 4
Dependent Claim
120 words
A pharmaceutical composition comprising: (a) a compound of the formula: ##STR7## wherein R 1 represents hydroxy, acyloxy derived from an aliphatic acid having 2-18 carbon atoms or derived from a heterocyclic carboxylic acid containing one or more nitrogen atoms; lower alkoxycarbonyloxy; aminoacyloxy or carboxyalkanoyloxy; R 2 represents lower alkoxy; R 3 represents lower alkoxy; and R 4 represents phenyl which is unsubstituted or substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dialkylamino, amino, cyano, hydroxy, halo and alkylenedioxy; or pyridyl, furyl, thienyl or pyrrolyl any of which is unsubstituted or substituted by lower alkyl; and (b) a pharmaceutically acceptable carrier material, said composition being formulated in unit dosage form.
Claim 5
Dependent Claim
120 words
A pharmaceutical composition comprising: (a) a compound of the formula: ##STR7## wherein R 1 represents hydroxy, acyloxy derived from an aliphatic acid having 2-18 carbon atoms or derived from a heterocyclic carboxylic acid containing one or more nitrogen atoms; lower alkoxycarbonyloxy; aminoacyloxy or carboxyalkanoyloxy; R 2 represents lower alkoxy; R 3 represents lower alkoxy; and R 4 represents phenyl which is unsubstituted or substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dialkylamino, amino, cyano, hydroxy, halo and alkylenedioxy; or pyridyl, furyl, thienyl or pyrrolyl any of which is unsubstituted or substituted by lower alkyl; and (b) a pharmaceutically acceptable carrier material, said composition being formulated in unit dosage form.
Claim 6
Dependent Claim
16 words
The composition of claim 3, wherein said composition is formulated in a systemic unit dosage form.
Claim 7
Dependent Claim
16 words
The composition of claim 3, wherein said composition is formulated in an oral unit dosage form.
Claim 8
Dependent Claim
27 words
The composition of claim 5 wherein the oral dosage form is selected from the group consisting of tablets, capsules, pills, powders, granules, solutions, suspensions, syrups and elixers.
Claim 9
Dependent Claim
15 words
The composition of claim 4 comprising about 100 to about 2,000 mg of compound I.
Claim 10
Dependent Claim
31 words
The composition of claim 3 wherein R 1' is hydroxy and R 2' and R 3' are each lower alkoxy and R 4' is a phenyl having a lower alkoxy substituent.
Claim 11
Dependent Claim
11 words
The composition of claim 3 wherein the compound is 4'-ethoxy-2'-hydroxy-4-6'-dimethoxy chalcone.
Claim 12
Dependent Claim
15 words
The composition of claim 3, wherein said composition is formulated in topical unit dosage form.
Claim 13
Dependent Claim
27 words
The composition of claim 10, wherein the topical unit dosage form is selected from the group consisting of solutions, emulsions, micronized powders, ointments, gargles, troches and aerosoles.
Claim 14
Dependent Claim
14 words
The composition of claim 10 comprising 0.1 to 100 μg/cm 2 of compound I.
Claim 15
Dependent Claim
31 words
The composition of claim 10 wherein R 1' is hydroxy and R 2' and R 3' are each lower alkoxy and R 4' is a phenyl having a lower alkoxy substituent.
Claim 16
Dependent Claim
11 words
The composition of claim 10 wherein the compound is 4'-ethoxy-2'hydroxy-4-6'-dimethoxy chalcone.
Claim 17
Dependent Claim
18 words
The composition of claim 10 wherein compound I is present in an amount which is effective against viruses.
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) | 1989-08-11 | 1990-02-10 | 1990-08-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-08-11 | 1994-02-10 | 1994-08-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-08-11 | 1998-02-10 | 1998-08-12 | $7700.00 | Window Closed / Lapsed |