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US5466700A
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Anesthetic use of N-phenyl-N-(4-piperidinyl)amides
Assignee: Mylan Teoranta
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Filing: 1993-08-30
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Granted: 1995-11-14
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Expires: 2013-08-30
Abstract
Abstract The use of particular opioids to induce and maintain anesthesia and conscious sedation is disclosed. The opioids used in the method of the present invention relate to the anesthetic action of the N-phenyl-N-(4-piperidinyl)amides as disclosed in U.S. Pat. No. 5,019,583 to Feldman, et al.
Inventors
- 👤 Randal L. Batenhorst
- 👤 Anthony W. Fox
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 07:04
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61K31/4468
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
164 words
A method for providing anesthesia in a mammal comprising administering to such mammal a compound having the Formula (I): ##STR2## wherein X is a member selected from the group consisting of alkoxycarbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxycarbonyl-lower alkyl, and (C 1-2 )alkoxy-(C 1-2 )alkoxycarbonyl-lower alkyl; Ar is a member selected from the group consisting of phenyl and mono-,di- and tri-substituted phenyl, wherein each substituent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl; R is a member selected from the group consisting of lower alkyl and lower alkoxy-lower alkyl; R 1 is a member selected from the group consisting of hydrogen and lower alkoxycarbonyl; and R 2 is a member selected from the group consisting of hydrogen and methyl; and the optically active and cis-trans isomers thereof and the acid addition salts thereof; said compound being administered to said mammal in an amount in excess of an amount effective for analgesia in order to induce or maintain anesthesia.
Claim 2
Independent Claim
164 words
A method for providing anesthesia in a mammal comprising administering to such mammal a compound having the Formula (I): ##STR2## wherein X is a member selected from the group consisting of alkoxycarbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxycarbonyl-lower alkyl, and (C 1-2 )alkoxy-(C 1-2 )alkoxycarbonyl-lower alkyl; Ar is a member selected from the group consisting of phenyl and mono-,di- and tri-substituted phenyl, wherein each substituent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl; R is a member selected from the group consisting of lower alkyl and lower alkoxy-lower alkyl; R 1 is a member selected from the group consisting of hydrogen and lower alkoxycarbonyl; and R 2 is a member selected from the group consisting of hydrogen and methyl; and the optically active and cis-trans isomers thereof and the acid addition salts thereof; said compound being administered to said mammal in an amount in excess of an amount effective for analgesia in order to induce or maintain anesthesia.
Claim 3
Dependent Claim
11 words
The method of claim 1, wherein said compound is administered parenterally.
Claim 4
Dependent Claim
11 words
The method of claim 1, wherein said compound is administered sublingually.
Claim 5
Dependent Claim
11 words
The method of claim 1, wherein said compound is administered transdermally.
Claim 6
Dependent Claim
12 words
The method of claim 1, wherein said compound is administered i.v. bolus.
Claim 7
Dependent Claim
19 words
The method of claim 5, wherein said compound is administered in an amount of about 8 to 20 g/kg.
Claim 8
Dependent Claim
19 words
The method of claim 6, wherein said compound is administered in an amount of about 0.1 to 3.0 g/kg/min.
Claim 9
Dependent Claim
13 words
The method of claim 1, wherein said compound is administered by continuous infusion.
Claim 10
Dependent Claim
10 words
The method of claim 1 wherein X is alkoxycarbonyl-lower alkyl.
Claim 11
Dependent Claim
11 words
The method of claim 1 wherein X is lower alkylcarbonyloxy-lower alkyl.
Claim 12
Dependent Claim
10 words
The method of claim 1 wherein X is alkenyloxycarbonyl-lower alkyl.
Claim 13
Dependent Claim
10 words
The method of claim 1 wherein X is alkoxycarbonyl-lower alkyl.
Claim 14
Dependent Claim
11 words
The method of claim 1 wherein Ar is phenyl or 2-fluorophenyl.
Claim 15
Dependent Claim
9 words
The method of claim 1 wherein R is ethyl.
Claim 16
Dependent Claim
10 words
The method of claim 1 wherein R 1 is methoxycarbonyl.
Claim 17
Dependent Claim
37 words
The method of claim 1 wherein said compound is selected from the group consisting of 5-[4-methoxycarbonyl-4-[(1-oxopropyl)phenylamino]-1-piperidine]pentanoic acid, methyl ester; 2-[4-methoxycarbonyl-4-[(1-oxopropyl)phenylamino]-1-piperidine]ethyl acetate; 3-[4-(1-oxopropyl)-2-fluorophenylamino]-1-piperidine]-propanoic acid, methyl ester; or 3-[4-methoxycarbonyl-4-[(oxopropyl)phenylamino]-1-piperidine]propanoic acid, vinyl ester and pharmaceutically acceptable acid addition salts thereof.
Claim 18
Dependent Claim
22 words
The method of claim 1 wherein said compound is 3-[4-methoxycarbony-4-[(1-oxopropyl)-phenylamino]-1-piperidine] propanoic acid, alkyl ester, and the pharmaceutically acceptable acid addition salts thereof.
Claim 19
Dependent Claim
11 words
The method of claim 1, wherein said mammal is a human.
Claim 20
Dependent Claim
28 words
The method of claim 18, wherein said compound of Formula (I) is administered in an amount at least 4 times in excess of its ED 50 for analgesia.
Claim 21
Dependent Claim
22 words
The method of claim 18, wherein said compound is administered in conjunction with a hypnotic in an effective amount to induce unconsciousness.
Claim 22
Dependent Claim
23 words
The method of claim 18, wherein said compound is administered in conjunction with a CNS depressant in an effective amount to induce unconsciousness.
Claim 23
Dependent Claim
21 words
The method of claim 18, wherein said compound is administered in an amount in excess of its ED 50 for analgesia.
Claim 24
Dependent Claim
34 words
The method of claim 22, wherein said compound is administered in conjunction with a hypnotic, an anxiolytic, or an inhaled agent being delivered in an amount less than 50% of its ED 50 .
Claim 25
Dependent Claim
17 words
The method of claim 23, wherein said compound is administered in an effective amount to maintain anesthesia.
Claim 26
Dependent Claim
47 words
The method of claim 23, wherein said compound is administered alone or in conjunction with a hypnotic, an anxiolytic or an inhaled anesthetic agent in an amount such that upon discontinuing administration of said compound, said mammal recovers from anesthesia or sedation in less than 15 minutes.
Claim 27
Dependent Claim
40 words
The method of claim 25, wherein said hypnotic, anxiolytic and/or inhaled agent is administered in an amount such that upon discontinuing administration of said compound of Formula (I), said mammal recovers from anesthesia or sedation in less than 15 minutes.
Claim 28
Independent Claim
166 words
A method for providing conscious sedation in a mammal comprising administering to such mammal a compound having the Formula (I): ##STR3## wherein X is a member selected from the group consisting of alkoxycarbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxycarbonyl-lower alkyl, and (C 1-2 )alkoxy-(C 1-2 )alkoxycarbonyl-lower alkyl; Ar is a member selected from the group consisting of phenyl and mono-,di- and tri-substituted phenyl, wherein each substituent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl; R is a member selected from the group consisting of lower alkyl and lower alkoxy-lower alkyl; R 1 is a member selected from the group consisting of hydrogen and lower alkoxycarbonyl; and R 2 is a member selected from the group consisting of hydrogen and methyl; and the optically active and cis-trans isomers thereof and the acid addition salts thereof; said compound being administered to said mammal in an amount in excess of an amount effective for analgesia in order to induce or maintain conscious sedation.
Claim 29
Independent Claim
166 words
A method for providing conscious sedation in a mammal comprising administering to such mammal a compound having the Formula (I): ##STR3## wherein X is a member selected from the group consisting of alkoxycarbonyl-lower alkyl, lower alkyl-carbonyloxy-lower alkyl, alkenyloxycarbonyl-lower alkyl, and (C 1-2 )alkoxy-(C 1-2 )alkoxycarbonyl-lower alkyl; Ar is a member selected from the group consisting of phenyl and mono-,di- and tri-substituted phenyl, wherein each substituent is independently selected from the group consisting of halo, lower alkyl, lower alkoxy and trifluoromethyl; R is a member selected from the group consisting of lower alkyl and lower alkoxy-lower alkyl; R 1 is a member selected from the group consisting of hydrogen and lower alkoxycarbonyl; and R 2 is a member selected from the group consisting of hydrogen and methyl; and the optically active and cis-trans isomers thereof and the acid addition salts thereof; said compound being administered to said mammal in an amount in excess of an amount effective for analgesia in order to induce or maintain conscious sedation.
References Cited (Backward Citations)
US5019583A
Cited
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