Phenyl derivatives useful as tachykinin antagonists
First Claim
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1. A compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof:
- ##STR13## wherein R1 is imidazoyl nitro, NRa Rb and NRa CORb, where Ra and Rb each independently represent H, C1-6 alkyl or phenyl optionally substituted by C1-6 alkyl, halo or trifluoromethyl;
R2 represents H, C1-6 alkyl or C2-6 alkenyl;
R3 represents C1-3 alkyl substituted by a phenyl group which may itself optionally be substituted by one or more of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, cyano, nitro, trifluoromethyl and trimethylsilyl;
R4 represents H, C1-6 alkyl or C2-6 alkenyl;
each R5 independently represents C1-6 alkyl, C1-6 alkoxy, halo or trifluoromethyl;
Z represents O or S; and
m represents 0, 1, 2 or 3.
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Abstract
Compounds of formula (I), or a salt or prodrug thereof are tachykinin antagonists.
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Citations
8 Claims
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1. A compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof:
- ##STR13## wherein R1 is imidazoyl nitro, NRa Rb and NRa CORb, where Ra and Rb each independently represent H, C1-6 alkyl or phenyl optionally substituted by C1-6 alkyl, halo or trifluoromethyl;
R2 represents H, C1-6 alkyl or C2-6 alkenyl; R3 represents C1-3 alkyl substituted by a phenyl group which may itself optionally be substituted by one or more of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, cyano, nitro, trifluoromethyl and trimethylsilyl; R4 represents H, C1-6 alkyl or C2-6 alkenyl; each R5 independently represents C1-6 alkyl, C1-6 alkoxy, halo or trifluoromethyl; Z represents O or S; and m represents 0, 1, 2 or 3. - View Dependent Claims (2, 3, 4, 5, 7, 8)
- ##STR13## wherein R1 is imidazoyl nitro, NRa Rb and NRa CORb, where Ra and Rb each independently represent H, C1-6 alkyl or phenyl optionally substituted by C1-6 alkyl, halo or trifluoromethyl;
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6. A compound selected from (±
- ) -1- [3,5- (bistrifluoromethylphenyl)methyloxy]-2-N(2-nitroimidazole)-2-phenylethane;
(±
)-2-N(2-aminoimidazole)-1-[3,5-(bistrifluoromethylphenyl)methyloxy]-2-phenylethane;
(±
)-1-[3,5-(bistrifluoromethylphenyl)methyloxy]-2-N(4-nitroimidazole)-2-phenylethane; and
salts and prodrugs thereof.
- ) -1- [3,5- (bistrifluoromethylphenyl)methyloxy]-2-N(2-nitroimidazole)-2-phenylethane;
Specification
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Current AssigneeMerck Sharp & Dohme Limited (Merck & Co., Inc.)
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Original AssigneeMerck Sharp & Dohme Limited (Merck & Co., Inc.)
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InventorsKeown, Linda E., Van Niel, Monique B., Ladduwahetty, Tamara
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Primary Examiner(s)Ramsuer, Robert W.
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Application NumberUS08/481,503Time in Patent Office679 DaysField of Search548/327.5, 548/331.5, 514/392US Class Current514/392CPC Class CodesC07D 207/325 with substituted hydrocarbo...C07D 211/88 attached in positions 2 and...C07D 231/12 with only hydrogen atoms, h...C07D 233/56 with only hydrogen atoms or...C07D 233/88 Nitrogen atoms, e.g. allantoinC07D 233/91 Nitro radicalsC07D 249/08 1,2,4-Triazoles; Hydrogenat...C07D 295/092 with aromatic radicals atta...
