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US4055652A Expired / Lapsed US ⏱️ 0.0 years remaining

1-[β(R-thio)phenethyl]imidazoles and derivatives thereof

Assignee: Syntex USA LLC
•
Filing: 1976-03-08
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Granted: 1977-10-25
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Expires: 1996-03-08
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Abstract

Abstract Novel 1-[ beta -(R-thio)phenethyl]-imidazoles and the corresponding 1-[ beta -(R-sulfinyl)phenethyl]imidazoles and 1-[ beta -(R-sulfonyl)phenethyl]imidazoles wherein R is alkyl, alkenyl, aralkenyl, substituted aralkenyl, alkynyl, cycloalkyl, cycloalkyl alkyl, aralkyl, substituted aralkyl, aryl or substituted aryl; and the antimicrobial acid addition salts thereof, are useful as antifungal, anti-bacterial and anti-protozoal agents.

Inventors

  • 👤 Keith A. M. Walker

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 12:19
CPC Classifications
A; A01; A01N; A01N43/00; A01N43/48; A01N43/50; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/415; C; C07; C07D; C07D233/00; C07D233/04; C07D233/20; C07D233/22; C07D233/54; C07D233/56; C07D233/60; C07D233/66; C07D233/68; C07D233/91; C07D233/92

Claims Analysis

Total Claims: 49
Claim 1
Independent Claim 268 words
A compound of the formula: ##STR10##and the antimicrobial acid addition salts thereof, wherein: R is alkyl, alkenyl, aralkenyl, substituted aralkenyl, alkynyl, cycloalkyl, cycloalkyl alkyl, aralkyl, substituted aralkyl, aryl or substituted aryl, said substituted aralkenyl and substituted aralkyl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano and said substituted aryl containing at least one substituent selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, amino alkanoylamino and cyano; R 1 is hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, cyano, thiocyano or the group ##STR11##in which R 2 is alkyl, cycloalkyl, aralkyl, substituted aralkyl, aryl or substituted aryl, and substituted aralkyl and said substituted aryl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano; and wherein with reference to the above, alkyl has 1 to 20 carbon atoms, cycloalkyl has 5 to 8 carbon atoms, cycloalkyl has 6 to 11 carbon atoms, alkenyl and alkynyl have 2 to 12 carbon atoms, aryl has 6 to 10 carbon atoms, aralkyl has 7 to 14 carbon atoms, aralkenyl has 8 to 14 carbon atoms, lower alkyl and lower alkoxy have 1 to 6 carbon atoms and alkanoylamino has 2 to 12 carbon atoms; m, n and p are independently selected from the integers zero, 1 and 2; provided that the value of m cannot be greater than the value of n except when R 1 is the group ##STR12##and R 2 is aryl or substituted aryl.
Claim 2
Dependent Claim 268 words
A compound of the formula: ##STR10##and the antimicrobial acid addition salts thereof, wherein: R is alkyl, alkenyl, aralkenyl, substituted aralkenyl, alkynyl, cycloalkyl, cycloalkyl alkyl, aralkyl, substituted aralkyl, aryl or substituted aryl, said substituted aralkenyl and substituted aralkyl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano and said substituted aryl containing at least one substituent selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, amino alkanoylamino and cyano; R 1 is hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, cyano, thiocyano or the group ##STR11##in which R 2 is alkyl, cycloalkyl, aralkyl, substituted aralkyl, aryl or substituted aryl, and substituted aralkyl and said substituted aryl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano; and wherein with reference to the above, alkyl has 1 to 20 carbon atoms, cycloalkyl has 5 to 8 carbon atoms, cycloalkyl has 6 to 11 carbon atoms, alkenyl and alkynyl have 2 to 12 carbon atoms, aryl has 6 to 10 carbon atoms, aralkyl has 7 to 14 carbon atoms, aralkenyl has 8 to 14 carbon atoms, lower alkyl and lower alkoxy have 1 to 6 carbon atoms and alkanoylamino has 2 to 12 carbon atoms; m, n and p are independently selected from the integers zero, 1 and 2; provided that the value of m cannot be greater than the value of n except when R 1 is the group ##STR12##and R 2 is aryl or substituted aryl.
Claim 3
Dependent Claim 15 words
The compound of claim 1 which is 1-[2,4-dichloro-β-(4'-chlorobenzylsulfinyl)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 4
Dependent Claim 15 words
The compound of claim 1 which is 1-[2,4-dichloro-β-(n-heptylsulfinyl)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 5
Dependent Claim 15 words
The compound of claim 1 which is 1-[2,4-dichloro-β-(2',4'-dichlorobenzylsulfinyl)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 6
Dependent Claim 15 words
The compound of claim 1 which is 1-[2,4-dichloro-β-(3',4'-dichlorophenylsulfinyl)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 7
Dependent Claim 9 words
A compound of claim 1 wherein m is zero.
Claim 8
Dependent Claim 34 words
A compound of claim 6 wherein R 1 is halo and R is alkyl, alkenyl, aralkenyl, halo substituted aralkenyl, aralkyl, halo or lower alkoxy substituted aralkyl, aryl or halo or lower alkoxy substituted aryl.
Claim 9
Dependent Claim 35 words
A compound of claim 7 wherein R is alkyl containing 1 to 12 carbon atoms, 2-alkenyl, 3-phenyl-2-alkenyl, halo substituted 3-phenyl-2alkenyl, benzyl, halo or lower alkoxy substituted benzyl, phenyl or halo or lower alkoxy substituted phenyl.
Claim 10
Dependent Claim 12 words
A compound of claim 8 wherein [R 1 ] p is 2,4-dihalo.
Claim 11
Dependent Claim 15 words
The compound of claim 9 which is 1-[2,4-dichloro-β-(2-octenylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 12
Dependent Claim 15 words
The compound of claim 9 which is 1-[2,4-dichloro-β-(3-phenyl-2-propenylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 13
Dependent Claim 16 words
The compound of claim 9 which is 1-{2,4-dichloro-β-[3-(4'-chlorophenyl)-2- propenylthio]phenethyl}imidazole and the antimicrobial acid addition salts thereof.
Claim 14
Dependent Claim 15 words
The compound of claim 9 which is 1-{2,4-dichloro-β-[3-(4'-fluorophenyl)-2-propenylthio]phenethyl}imidazole and the antimicrobial acid addition salts thereof.
Claim 15
Dependent Claim 26 words
A compound of claim 9 wherein R is alkyl containing 4 to 10 carbon atoms, halo or methoxy substituted benzyl, or halo or methoxy substituted phenyl.
Claim 16
Dependent Claim 14 words
The compound of claim 14 which 1-[2,4-dibromo-β-(n-pentylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 17
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-dibromo-β-(n-hexylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 18
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-dibromo-β-(n-heptylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 19
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-dibromo-β-(4'-chlorobenzylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 20
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-dibromo-β-(3',4'-dichlorophenylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 21
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-dichloro-β-(4'-fluorobenzylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 22
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-dichloro-β-(4'-methoxybenzylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 23
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-dichloro-β-(4'-methoxyphenylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 24
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-difluoro-β-(n-heptylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 25
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-difluoro-β-(n-octylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 26
Dependent Claim 15 words
The compound of claim 14 which is 1-[2,4-difluoro-β-(n-nonylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 27
Dependent Claim 32 words
A compound of claim 14 wherein [R 1 ] p is 2,4-dichloro and R is a straight chain alkyl containing 4 to 10 carbon atoms, chloro substituted benzyl or chloro substituted phenyl.
Claim 28
Dependent Claim 15 words
The compound of claim 26 which is 1-[2,4-dichloro-β-(n-butylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 29
Dependent Claim 15 words
The compound of claim 26 which is 1-[2,4-dichloro-β-(n-octylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 30
Dependent Claim 15 words
The compound of claim 26 which is 1-[2,4-dichloro-β-(n-nonylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 31
Dependent Claim 15 words
The compound of claim 26 which is 1-[2,4-dichloro-β-(3',4',5'-trichlorophenylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 32
Dependent Claim 27 words
A compound of claim 26 wherein R is a straight chain alkyl containing 5 to 7 carbon atoms, 4-chloro-, 2,4-dichloro- or 3,4-dichlorobenzyl, or 4-chloro-, 2,4-dichloro- or 3,4-dichlorophenyl.
Claim 33
Dependent Claim 15 words
The compound of claim 31 which is 1-[2,4-dichloro-β-(n-pentylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 34
Dependent Claim 15 words
The compound of claim 31 which is 1-[2,4-dichloro-β-(n-hexylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 35
Dependent Claim 15 words
The compound of claim 31 which is 1-[2,4-dichloro-β-(n-heptylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 36
Dependent Claim 15 words
The compound of claim 31 which is 1-[2,4-dichloro-β-(4'-chlorobenzylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 37
Dependent Claim 15 words
The compound of claim 31 which is 1-[2,4-dichloro-β-(2',40'-dichlorobenzylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 38
Dependent Claim 15 words
The compound of claim 31 which is 1-[2,4-dichloro-β-(3',4'-dichlorobenzylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 39
Dependent Claim 15 words
The compound of claim 31 which is 1-[2,4-dichloro-β-(4'-chlorophenylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 40
Dependent Claim 15 words
The compound of claim 31 which is 1-[2,4-dichloro-β-(2',4'-dichlorophenylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 41
Dependent Claim 15 words
The compound of claim 31 which is 1-[2,4-dichloro-β-(3',4'-dichlorophenylthio)phenethyl]imidazole and the antimicrobial acid addition salts thereof.
Claim 42
Dependent Claim 293 words
A composition useful for inhibiting the growth of fungi, bacteria or protozoa which comprises an effective amount of a compound of the formula: ##STR13##or an antimicrobial acid addition salt thereof, wherein: R is alkyl, alkenyl, aralkenyl, substituted aralkenyl, alkynyl, cycloalkyl, cycloalkyl alkyl, aralkyl, substituted aralkyl, aryl and substituted aryl, said substituted aralkenyl and substituted aralkyl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano and said substituted aryl containing at least one substituent selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, amino, alkanoylamino and cyano; R 1 is hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, cyano, thiocyano and the group ##STR14##in which R 2 is alkyl, cycloalkyl, aralkyl, substituted aralkyl, aryl and substituted aryl, said substituted aralkyl and said substituted aryl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano; and wherein with reference to the above, alkyl has 1 to 20 carbon atoms, cycloalkyl has 5 to 8 carbon atoms, cycloalkyl alkyl has 6 to 11 carbon atoms, alkenyl and alkynyl have 2 to 12 carbon atoms, aryl has 6 to 10 carbon atoms, aralkyl has 7 to 14 carbon atoms, aralkenyl has 8 to 14 carbon atoms, lower alkyl and lower alkoxy have 1 to 6 carbon atoms and alkanoylamino has 2 to 12 carbon atoms; m, n and p are independently selected from the integers zero, 1 and 2; provided that the value of m cannot be greater than the value of n except when R 1 is the group ##STR15##and R 2 is aryl or substituted aryl; in admixture with a suitable carrier.
Claim 43
Dependent Claim 293 words
A composition useful for inhibiting the growth of fungi, bacteria or protozoa which comprises an effective amount of a compound of the formula: ##STR13##or an antimicrobial acid addition salt thereof, wherein: R is alkyl, alkenyl, aralkenyl, substituted aralkenyl, alkynyl, cycloalkyl, cycloalkyl alkyl, aralkyl, substituted aralkyl, aryl and substituted aryl, said substituted aralkenyl and substituted aralkyl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano and said substituted aryl containing at least one substituent selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, amino, alkanoylamino and cyano; R 1 is hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, cyano, thiocyano and the group ##STR14##in which R 2 is alkyl, cycloalkyl, aralkyl, substituted aralkyl, aryl and substituted aryl, said substituted aralkyl and said substituted aryl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano; and wherein with reference to the above, alkyl has 1 to 20 carbon atoms, cycloalkyl has 5 to 8 carbon atoms, cycloalkyl alkyl has 6 to 11 carbon atoms, alkenyl and alkynyl have 2 to 12 carbon atoms, aryl has 6 to 10 carbon atoms, aralkyl has 7 to 14 carbon atoms, aralkenyl has 8 to 14 carbon atoms, lower alkyl and lower alkoxy have 1 to 6 carbon atoms and alkanoylamino has 2 to 12 carbon atoms; m, n and p are independently selected from the integers zero, 1 and 2; provided that the value of m cannot be greater than the value of n except when R 1 is the group ##STR15##and R 2 is aryl or substituted aryl; in admixture with a suitable carrier.
Claim 44
Dependent Claim 17 words
A composition of claim 41 for pharmaceutical use wherein the carrier is a pharmaceutically acceptable, non-toxic carrier.
Claim 45
Dependent Claim 29 words
A composition of claim 42 for topical administration wherein the compound of Formula (I) is present in an amount ranging between 0.1 and 10.0 weight percent of the composition.
Claim 46
Independent Claim 302 words
A method of inhibiting the growth of fungi, bacteria or protozoa which comprises applying to a host object containing, or subject to attack by fungi, bacteria or protozoa, an effective amount of a compound of the formula ##STR16##or an antimicrobial acid addition salt thereof or a composition containing same as an active ingredient, wherein: R is alkyl, alkenyl, aralkenyl, substituted aralkenyl, alkynyl cycloalkyl, cycloalkyl alkyl, aralkyl, substituted aralkyl, aryl or substituted aryl, said substituted aralkenyl and substituted aralkyl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano and said substituted aryl containing at least one substituent selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, amino alkanoylamino and cyano; R 1 is hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, cyano, thiocyano or the group ##STR17##in which R 2 is alkyl, cycloalkyl, aralkyl, substituted aralkyl, aryl or substituted aryl, said substituted aralkyl and said substituted aryl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano; and wherein with reference to the above, alkyl has 1 to 20 carbon atoms, cycloalkyl has 5 to 8 carbon atoms, cycloalkyl alkyl has 6 to 11 carbon atoms, alkenyl and alkynyl have 2 to 12 carbon atoms, aralkyl has 7 to 14 carbon atoms, aralkenyl has 8 to 14 carbon atoms, lower alkyl and alkoxy have 1 to 6 carbon atoms and alkanoylamino has 2 to 12 carbon atoms; m, n and p are independently selected from the integers zero, 1 and 2; provided that the value of m cannot be greater than the value of n except when R 1 is the group ##STR18##and R 2 is aryl or substituted aryl.
Claim 47
Independent Claim 302 words
A method of inhibiting the growth of fungi, bacteria or protozoa which comprises applying to a host object containing, or subject to attack by fungi, bacteria or protozoa, an effective amount of a compound of the formula ##STR16##or an antimicrobial acid addition salt thereof or a composition containing same as an active ingredient, wherein: R is alkyl, alkenyl, aralkenyl, substituted aralkenyl, alkynyl cycloalkyl, cycloalkyl alkyl, aralkyl, substituted aralkyl, aryl or substituted aryl, said substituted aralkenyl and substituted aralkyl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano and said substituted aryl containing at least one substituent selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, amino alkanoylamino and cyano; R 1 is hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro, cyano, thiocyano or the group ##STR17##in which R 2 is alkyl, cycloalkyl, aralkyl, substituted aralkyl, aryl or substituted aryl, said substituted aralkyl and said substituted aryl containing at least one substituent on the aryl moiety selected from the group consisting of halo, lower alkyl, lower alkoxy, trifluoromethyl, nitro and cyano; and wherein with reference to the above, alkyl has 1 to 20 carbon atoms, cycloalkyl has 5 to 8 carbon atoms, cycloalkyl alkyl has 6 to 11 carbon atoms, alkenyl and alkynyl have 2 to 12 carbon atoms, aralkyl has 7 to 14 carbon atoms, aralkenyl has 8 to 14 carbon atoms, lower alkyl and alkoxy have 1 to 6 carbon atoms and alkanoylamino has 2 to 12 carbon atoms; m, n and p are independently selected from the integers zero, 1 and 2; provided that the value of m cannot be greater than the value of n except when R 1 is the group ##STR18##and R 2 is aryl or substituted aryl.
Claim 48
Dependent Claim 14 words
The method of claim 44 wherein the compound of Formula (I) is administered topically.
Claim 49
Dependent Claim 16 words
The method of claim 44 wherein the compound of Formula (I) is administered orally or parenterally.

References Cited (Backward Citations)

US3717655A Cited
US3658813A Cited
US3796704A Cited
US3682951A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-10-24 1981-04-25 1981-10-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-10-24 1985-04-25 1985-10-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-10-24 1989-04-25 1989-10-25 $7700.00 Window Closed / Lapsed

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