1,2-dihydro-2-oxopyridines
First Claim
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1. A 1,2-dihydro-2-oxopyridine compound of formula I ##STR10## wherein R is the radical ##STR11## R1 is H, Hal, A, OA or NO2 ;
- R2 is COOH, COOA, CN, NO2, NH2, NHCOR7, NHSO2 R7 or tetrazol-5-yl;
R3 is CH2 NR10 R11, or tetrazol-5-yl;
R4 is H or A;
R5, R6 and R10 are in each case independently H, A, alkenyl having 2-6 C atoms, alkynyl having 2-6 C atoms, Ar or Ar-alkyl having 1-6 C atoms in the alkyl moiety;
R7 is A or A monosubstituted or polysubstituted by F;
R11 is H, A, A monosubstituted or polysubstituted by F, Ar, Ar-alkyl having 1-6 C atoms in the alkyl moiety, CO-A, CO-Ar, CO-alkyl-Ar having 1-6 C atoms in the alkyl moiety, COOA, COOAr, COO--alkyl--Ar having 1-6 C atoms in the alkyl moiety, CONR12 R13, SO2 R7 or SO2 Ar,NR10 R11 can also be pyrrolidino, piperidino, morpholino, succinimido or phthalimido;
R12 and R13 are in each case independently H, A, cycloalkyl having 3-8 C atoms, alkenyl having 2-6 C atoms, alkynyl having 2-6 C atoms, or Ar;
X is absent or is --CO--, --O--, --NH--CO--, --CO--NH--, --CH2 --O-- or --O--CH2 --;
A is alkyl having 1-6 C atoms;
Ar is phenyl which is unsubstituted or monosubstituted by A, OA, CF3, Hal or NO2 ; and
Hal is F, Cl, Br or I;
ora physiologically acceptable salt.
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Abstract
New 1,2-dihydro-2-oxopyridines of formula I ##STR1## in which R is the radical ##STR2## and R1 to R6 and X are as defined herein,
and their salts, have antagonistic properties towards angiotensin II and can be used for the treatment of hypertension, aldosteronism and cardiac insufficiency.
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Citations
25 Claims
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1. A 1,2-dihydro-2-oxopyridine compound of formula I ##STR10## wherein R is the radical ##STR11## R1 is H, Hal, A, OA or NO2 ;
- R2 is COOH, COOA, CN, NO2, NH2, NHCOR7, NHSO2 R7 or tetrazol-5-yl;
R3 is CH2 NR10 R11, or tetrazol-5-yl; R4 is H or A; R5, R6 and R10 are in each case independently H, A, alkenyl having 2-6 C atoms, alkynyl having 2-6 C atoms, Ar or Ar-alkyl having 1-6 C atoms in the alkyl moiety; R7 is A or A monosubstituted or polysubstituted by F; R11 is H, A, A monosubstituted or polysubstituted by F, Ar, Ar-alkyl having 1-6 C atoms in the alkyl moiety, CO-A, CO-Ar, CO-alkyl-Ar having 1-6 C atoms in the alkyl moiety, COOA, COOAr, COO--alkyl--Ar having 1-6 C atoms in the alkyl moiety, CONR12 R13, SO2 R7 or SO2 Ar, NR10 R11 can also be pyrrolidino, piperidino, morpholino, succinimido or phthalimido; R12 and R13 are in each case independently H, A, cycloalkyl having 3-8 C atoms, alkenyl having 2-6 C atoms, alkynyl having 2-6 C atoms, or Ar; X is absent or is --CO--, --O--, --NH--CO--, --CO--NH--, --CH2 --O-- or --O--CH2 --; A is alkyl having 1-6 C atoms; Ar is phenyl which is unsubstituted or monosubstituted by A, OA, CF3, Hal or NO2 ; and Hal is F, Cl, Br or I;
ora physiologically acceptable salt. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25)
- R2 is COOH, COOA, CN, NO2, NH2, NHCOR7, NHSO2 R7 or tetrazol-5-yl;
Specification
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Current AssigneeMerck Patent GmbH (Merck & Co., Inc.)
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Original AssigneeMerck Patent GmbH (Merck & Co., Inc.)
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InventorsBeier, Norbert, Mederski, Werner, Schelling, Pierre, Lues, Ingeborg, Minck, Klaus-Otto
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Primary Examiner(s)Fan, Jane T.
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Application NumberUS08/050,800Time in Patent Office460 DaysField of Search546/276, 514/340US Class Current514/340CPC Class CodesC07D 213/64 attached in position 2 or 6C07D 213/80 in position 3C07D 213/82 in position 3C07D 213/85 in position 3C07D 401/10 linked by a carbon chain co...C07D 401/12 linked by a chain containin...C07D 401/14 containing three or more he...
