Patent US4550115A successfully refreshed from Google Patents.
US4550115A
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US
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Certain piperidino-lower-alkylene esters of 3-methylflavone-8-carboxylates possessing smooth muscle relaxant activity
Assignee: Recordati SA
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Filing: 1982-07-12
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Granted: 1985-10-29
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Expires: 2002-07-12
Abstract
Abstract Novel 3-methylflavone-8-carboxylates having the structural formula (I): ##STR1## wherein Z is N-methylpiperidinyl, tropinyl or quinuclidinyl, or a group having the structural formula (II): ##STR2## in which n is 0 or 1, R is hydrogen or alkyl having from 1 to 4 carbon atoms, or phenyl, R 1 is hydrogen or alkyl having from 1 to 4 carbon atoms, R 2 is hydrogen or hydroxy, and further wherein R, R 1 and R 2 may together form, with the carbon atoms from which they depend, a cycloalkyl ring having from 4 to 6 carbon atoms, and R 3 is hydrogen or alkyl having from 1 to 4 carbon atoms, with the proviso that R, R 1 , R 2 and R 3 cannot at the same time all be hydrogen, and the pharmaceutically acceptable salts thereof, are effective smooth muscle relaxants, calcium blockers, anaesthetics and anti-inflammatories.
Inventors
- 👤 Dante Nardi
- 👤 Alberto Tajana
- 👤 Renzo Pennini
- 👤 Pietro Cazzulani
- 👤 Gabriele Graziani
- 👤 Silvano Casadio
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 09:32
CPC Classifications
C; C07; C07D; C07D311/00; C07D407/00; C07D407/02; C07D407/12; A; A61; A61P; A61P21/00; A61P21/02; A61P23/00; A61P23/02; A61P25/00; A61P25/02; A61P29/00; A61P3/00; A61P3/12; A61P3/14; C07D311/02; C07D311/04; C07D311/22; C07D311/26; C07D311/28; C07D311/30; C07D451/00; C07D451/02; C07D451/04; C07D451/06; C07D451/12; C07D453/00; C07D453/02
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
102 words
A 3-methylflavone-8-carboxylic acid ester having the structural formula (I): ##STR7## wherein Z is N-methylpiperidinyl or a group having the structural formula (II): ##STR8## in which n is 0 or 1 R is hydrogen or alkyl having from 1 to 4 carbon atoms, R 1 is hydrogen or alkyl having from 1 to 4 carbon atoms, R 2 is hydrogen or hydroxy, and R 3 is hydrogen or alkyl having from 1 to 4 carbon atoms, with the proviso that R, R 1 , R 2 and R 3 cannot at the same time all be hydrogen; and the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
102 words
A 3-methylflavone-8-carboxylic acid ester having the structural formula (I): ##STR7## wherein Z is N-methylpiperidinyl or a group having the structural formula (II): ##STR8## in which n is 0 or 1 R is hydrogen or alkyl having from 1 to 4 carbon atoms, R 1 is hydrogen or alkyl having from 1 to 4 carbon atoms, R 2 is hydrogen or hydroxy, and R 3 is hydrogen or alkyl having from 1 to 4 carbon atoms, with the proviso that R, R 1 , R 2 and R 3 cannot at the same time all be hydrogen; and the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
13 words
The carboxylic acid ester as defined by claim 1, wherein Z in N-methylpiperidinyl.
Claim 4
Dependent Claim
16 words
The carboxylic acid ester as defined by claim 1, wherein Z has the structural formula (II).
Claim 5
Dependent Claim
15 words
The carboxylic acid ester as defined by claim 3, in which R 3 is alkyl.
Claim 6
Dependent Claim
15 words
The carboxylic acid ester as defined by claim 3, in which R 2 is hydroxy.
Claim 7
Dependent Claim
21 words
The carboxylic acid ester as defined by claim 3, in which at least one of R and R 1 is alkyl.
Claim 8
Dependent Claim
18 words
The carboxylic acid ester as defined by claim 3, in which both R and R 1 are alkyl.
Claim 9
Dependent Claim
20 words
The carboxylic acid ester as defined by claim 3, in which R, R 1 and R 3 are each alkyl.
Claim 10
Dependent Claim
14 words
The carboxylic acid ester as defined by claim 1, the same being 3-(2-methyl-N-piperidino)-propyl 3-methylflavone-8-carboxylate.
Claim 11
Dependent Claim
14 words
The carboxylic acid ester as defined by claim 1, the same being N-methylpiperidin-3-yl 3-methylflavone-8-carboxylate.
Claim 12
Dependent Claim
14 words
The carboxylic acid ester as defined by claim 1, the same being 1,1-dimethyl-2-(N-piperidino)-ethyl 3-methylflavone-8-carboxylate.
Claim 13
Dependent Claim
14 words
The carboxylic acid ester as defined by claim 1, the same being 2-hydroxy-3-(N-piperidino)-propyl 3-methylflavone-8-carboxylate.
Claim 14
Dependent Claim
14 words
The carboxylic acid ester as defined by claim 1, the same being 1-methyl-3-(N-piperidino)-propyl 3-methylflavone-8-carboxylate.
Claim 15
Dependent Claim
14 words
The carboxylic acid ester as defined by claim 1, the same being 1-methylpiperidin-4-yl 3-methylflavone-8-carboxylate.
Claim 16
Dependent Claim
14 words
The carboxylic acid ester as defined by claim 1, the same being 1-methyl-2-(N-piperidino)-ethyl 3-methylflavone-8-carboxylate.
Claim 17
Dependent Claim
14 words
The carboxylic acid ester as defined by claim 1, the same being 1-phenyl-2-(N-piperidino)-ethyl 3-methylflavone-8-carboxylate.
Claim 18
Dependent Claim
30 words
A composition of matter comprising a smooth muscle relaxant effective amount of the 3-methylflavone-8-carboxylate as defined by claim 1, or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier therefor.
Claim 19
Dependent Claim
41 words
The method for eliciting a smooth muscle relaxant response in a warm-blooded mammal, comprising administering to a warm-blooded mammal in need of such treatment, a therapeutically effective amount of the 3-methylflavone-8-carboxylate as defined by claim 1, or pharmaceutically acceptable salt thereof.
Claim 20
Dependent Claim
38 words
The method for eliciting a smooth muscle relaxant response in a warm-blooded mammal, comprising administering to a warm-blooded mammal in need of such treatment, a therapeutically effective amount of the composition of matter as defined by claim 17.
References Cited (Backward Citations)
US2921070A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-10-28 | 1989-04-29 | 1989-10-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-10-28 | 1993-04-29 | 1993-10-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-10-28 | 1997-04-29 | 1997-10-29 | $7700.00 | Window Closed / Lapsed |