US4461912A
Expired / Lapsed
US
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Phenylacetic acid derivatives, their preparation and compositions containing them
Assignee: Sankyo Co Ltd
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Filing: 1982-12-06
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Granted: 1984-07-24
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Expires: 2002-12-06
Abstract
Abstract Phenylacetic derivatives of formula (I): ##STR1## (wherein R represents a hydrogen atom or a C 1 -C 3 alkyl group and n represents an integer from 1 to 3) and salts and esters thereof have analgesic, antipyretic and anti-inflammatory activity and may be prepared by reducing the corresponding acid or ester having an oxo group at the 2-position of the cycloalkylidene ring system and, if necessary, salifying the resulting product.
Inventors
- 👤 Atsusuke Terada
- 👤 Shunji Naruto
- 👤 Eiichi Misaka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 05:13
CPC Classifications
C; C07; C07C; C07C59/00; C07C59/40; C07C59/42; C07C59/54; A; A61; A61P; A61P29/00
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
35 words
Compounds of formula (I): ##STR4## (wherein R represents a hydrogen atom or a C 1 -C 3 alkyl group and n represents an integer from 1 to 3) and pharmaceutically acceptable salts and esters thereof.
Claim 2
Dependent Claim
35 words
Compounds of formula (I): ##STR4## (wherein R represents a hydrogen atom or a C 1 -C 3 alkyl group and n represents an integer from 1 to 3) and pharmaceutically acceptable salts and esters thereof.
Claim 3
Dependent Claim
12 words
Compounds as claimed in claim 1, wherein R represents a hydrogen atom.
Claim 4
Dependent Claim
12 words
Compounds as claimed in claim 1, wherein R represents a methyl group.
Claim 5
Dependent Claim
12 words
Compounds as claimed in claim 1, wherein n is 1 or 2.
Claim 6
Dependent Claim
59 words
Compounds as claimed in claim 1, which are the esters of said compounds of formula (I), wherein the ester moiety is selected from the group consisting of C 1 -C 6 alkyl groups; aralkyl groups; substituted aralkyl groups having at least one substituent selected from the group consisting of lower alkyl, lower alkoxy, halogen, and trifluoromethyl; and pyridylmethyl groups.
Claim 7
Dependent Claim
21 words
Compounds as claimed in claim 1, which are the C 1 -C 4 alkyl esters of said compounds of formula (I).
Claim 8
Dependent Claim
28 words
Compounds as claimed in claim 1, which are the alkali metal, alkaline earth metal, aluminium, ammonium, organic base or amino acid salts of said compounds of formula (I).
Claim 9
Dependent Claim
71 words
A process for preparing a compound of formula (I): ##STR5## (wherein R represents a hydrogen atom or a C 1 -C 3 alkyl group and n represents an integer from 1 to 3) and esters and salts of said compound of formula (I), which comprises reducing a compound of formula (II): ##STR6## (wherein R and n are as defined above) or an ester thereof and, if necessary, salifying the resulting product.
Claim 10
Dependent Claim
71 words
A process for preparing a compound of formula (I): ##STR5## (wherein R represents a hydrogen atom or a C 1 -C 3 alkyl group and n represents an integer from 1 to 3) and esters and salts of said compound of formula (I), which comprises reducing a compound of formula (II): ##STR6## (wherein R and n are as defined above) or an ester thereof and, if necessary, salifying the resulting product.
Claim 11
Dependent Claim
20 words
A process as claimed in claim 8, wherein the reduction is effected with an alkali metal borohydride as reducing agent.
Claim 12
Dependent Claim
24 words
A process as claimed in claim 9, wherein said alkali metal borohydride is selected from the group consisting of sodium borohydride and sodium cyanoborohydride.
Claim 13
Dependent Claim
41 words
A process as claimed in claim 8, wherein R represents a hydrogen atom or a methyl group and n is 1 or 2 and there is employed said compound of formula (II) or a C 1 -C 4 alkyl ester thereof.
Claim 14
Dependent Claim
62 words
A pharmaceutical composition for analgesic, antipyretic or anti-inflammatory use, comprising an effective amount of an active ingredient selected from compounds of formula (I): ##STR7## (wherein R represents a hydrogen atom or a C 1 -C 3 alkyl group and n represents an integer from 1 to 3), their pharmaceutically acceptable salts and esters, in admixture with a pharmaceutically acceptable carrier or diluent.
Claim 15
Dependent Claim
62 words
A pharmaceutical composition for analgesic, antipyretic or anti-inflammatory use, comprising an effective amount of an active ingredient selected from compounds of formula (I): ##STR7## (wherein R represents a hydrogen atom or a C 1 -C 3 alkyl group and n represents an integer from 1 to 3), their pharmaceutically acceptable salts and esters, in admixture with a pharmaceutically acceptable carrier or diluent.
Claim 16
Dependent Claim
14 words
A composition as claimed in claim 12, formulated for oral, rectal or topical application.
Claim 17
Dependent Claim
23 words
A composition as claimed in claim 12, wherein said active ingredient is selected from the group consisting of 2-[4-(2-hydroxycyclohexylidenemethyl)phenyl]propionic acid and 2-[4-(2-hydroxycyclopentylidenemethyl)phenyl]propionic acid.
Claim 18
Dependent Claim
17 words
Compounds as claimed in claim 1, selected from the group consisting of 2-[4-(2-hydroxycyclohexylidenemethyl)phenyl]propionic acid and 2-[4-(2-hydroxycyclopentylidenemethyl)phenyl]propionic acid.
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) | 1987-07-24 | 1988-01-23 | 1988-07-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-07-24 | 1992-01-23 | 1992-07-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-07-24 | 1996-01-23 | 1996-07-24 | $7700.00 | Window Closed / Lapsed |