Heterocyclic compounds, processes for their preparation and pharmaceutical compositions containing them
First Claim
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1. A compound of Formula (I):
- ##STR9## wherein Q1 is selected from a phenyl group substituted by at least one halo;
optionally substituted naphthyl;
optionally substituted benzyl;
or optionally substituted fluorenyl, said optional substituents being selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, SRa, SORa, SO2 Ra, ORa, NRa Rb, NRa CORb, NRa COORb, COORa or CONRa Rb, where Ra and Rb are as defined below;
the dotted line represents an optional covalent bond;
one of X and Y represents H and the other of X and Y represents hydroxy or C1-6 alkoxy, or X and Y together form a group ═
O or ═
NOR5 where R5 is selected from H and C1-6 alkyl;
R1 and R2 are each independently selected from H;
C1-6 alkyl optionally substituted by hydroxy, cyano, CORc, CO2 Rc, CONRc Rd, or NRc Rd (where Rc and Rd are each independently selected from H, C1-6 alkyl and phenyl (C0-4 alkyl) optionally substituted in the phenyl ring by one or more of C1-6 alkyl, C1-6 alkoxy, halo and trifluoromethyl);
phenyl (C1-4 alkyl) (optionally substituted in the phenyl ring by one or more of C1-6 alkyl, C1-6 alkoxy, halo and trifluoromethyl);
CORc, CO2 Rc, CONRc Rd ;
COC1-6 alkyl NRc Rd ;
CONRc COORd and SO2 Rc ;
where Rc and Rd are as above defined;
R3 is selected from H, C1-6 alkyl and C2-6 alkenyl; and
R4 is 3,5-disubstituted phenylwherein the substituent groups are selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, ORa, SRa, SORa, NRa Rb, NRa CORb, NRa CO2 Rb, CO2 Ra and CONRa Rb, where Ra and Rb are independently selected from H, C1-6 alkyl, phenyl and trifluoromethyl;
or a pharmaceutically acceptable salt thereof.
1 Assignment
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Accused Products
Abstract
Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q1 is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl;
. . is an optional covalent bond;
one of X and Y is H and the other is hydroxy or C1-6 alkoxy, or X and Y are together ═O or ═NOR5 ;
R1 and R2 are H; C1-6 alkyl optionally substituted by hydroxy, cyano, CORc, CO2 Rc, CONRc Rd, or NRc Rd (where Rc and Rd are H, C1-6 alkyl or phenyl(C0-4 alkyl) optionally substituted by C1-6 alkyl, C1-6 alkoxy, halo and trifluoromethyl); phenyl(C1-4 alkyl) (optionally substituted by C1-6 alkyl, C1-6 alkoxy, halo or trifluoromethyl); CORc ; CO2 Rc ; CONRc Rd ; COC1-6 alkylNRc Rd ; CONRc COORd ; or SO2 Rc ;
R3 is H, C1-6 alkyl or C2-6 alkenyl; and
R4 is phenyl optionally substituted by C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, ORa, SRa, SORa, NRa Rb, NRa CORb, NRa CO2 Rb, CO2 Ra or CONRa Rb, where Ra and Rb are H, C1-6 alkyl, phenyl or trifluoromethyl; are tachykinin antagonists.
476 Citations
12 Claims
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1. A compound of Formula (I):
- ##STR9## wherein Q1 is selected from a phenyl group substituted by at least one halo;
optionally substituted naphthyl;
optionally substituted benzyl;
or optionally substituted fluorenyl, said optional substituents being selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, SRa, SORa, SO2 Ra, ORa, NRa Rb, NRa CORb, NRa COORb, COORa or CONRa Rb, where Ra and Rb are as defined below;the dotted line represents an optional covalent bond; one of X and Y represents H and the other of X and Y represents hydroxy or C1-6 alkoxy, or X and Y together form a group ═
O or ═
NOR5 where R5 is selected from H and C1-6 alkyl;R1 and R2 are each independently selected from H;
C1-6 alkyl optionally substituted by hydroxy, cyano, CORc, CO2 Rc, CONRc Rd, or NRc Rd (where Rc and Rd are each independently selected from H, C1-6 alkyl and phenyl (C0-4 alkyl) optionally substituted in the phenyl ring by one or more of C1-6 alkyl, C1-6 alkoxy, halo and trifluoromethyl);
phenyl (C1-4 alkyl) (optionally substituted in the phenyl ring by one or more of C1-6 alkyl, C1-6 alkoxy, halo and trifluoromethyl);
CORc, CO2 Rc, CONRc Rd ;
COC1-6 alkyl NRc Rd ;
CONRc COORd and SO2 Rc ;
where Rc and Rd are as above defined;R3 is selected from H, C1-6 alkyl and C2-6 alkenyl; and R4 is 3,5-disubstituted phenyl wherein the substituent groups are selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, ORa, SRa, SORa, NRa Rb, NRa CORb, NRa CO2 Rb, CO2 Ra and CONRa Rb, where Ra and Rb are independently selected from H, C1-6 alkyl, phenyl and trifluoromethyl;
or a pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
- ##STR9## wherein Q1 is selected from a phenyl group substituted by at least one halo;
Specification
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Current AssigneeZimmer Incorporated (Zimmer Biomet Holdings, Inc.)
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Original AssigneeMerck Sharp & Dohme Limited (Merck & Co., Inc.)
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InventorsLewis, Richard T., Merchant, Kevin J., MacLeod, Angus M.
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Primary Examiner(s)McKane, Joseph K.
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Application NumberUS08/227,943Time in Patent Office753 DaysField of Search564/169, 514/621, 514/419, 514/443, 548/495, 549/49, 549/58US Class Current514/621CPC Class CodesA61P 43/00 Drugs for specific purposes...C07D 209/16 TryptaminesC07D 333/58 Radicals substituted by nit...
