US2011144197A1PendingUtilityA1
Alcanoic acid amides substituted by saturated o-heterocycles
Est. expirySep 17, 2025(expired)· nominal 20-yr term from priority
Inventors:Peter HeroldRobert MahVincenzo TschinkeStefan StutzAleksandar StojanovicStjepan JelakovicChristiane Marti
A61P 9/04A61P 9/12A61P 9/00A61P 9/10A61P 27/06A61P 13/12A61K 31/335
45
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Claims
Abstract
Compounds of the general formula (formula I) in which the meanings of the substituents R 1 and R 6 are as indicated in claim 1 , have renin-inhibiting properties and can be used as medicines.
Claims
exact text as granted — not AI-modified1 - 8 . (canceled)
9 . A compound of the formula
or a pharmaceutically useful salt thereof; in which
R 1 is an optionally substituted tetrahydrofuranyl, optionally substituted tetrahydrofuranylmethyl, optionally substituted tetrahydropyranyl or optionally substituted tetrahydropyranylmethyl;
R 2 and R 3 are independently of one another hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, or the two radicals together with the carbon atom to which they are bonded are C 3-8 cycloalkyl;
R 4 and R 5 are independently of one another hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl or the two radicals together with the carbon atom to which they are bonded are C 3-8 cycloalkyl;
R 6 is a group —CH 2 —R 7 , —CH 2 —CO—R 7 , —CH 2 —CH 2 —R 7 , —CH 2 —NR 8 —CO—R 7 , —CH 2 —CO—NR 8 —CH 2 —R 7 , —CH 2 —CH 2 —NR 8 —R 7 , —CH 2 —CO—NR 8 —R 7 or —CO—NR 8 —CH 2 —R 7 ;
R 7 is an optionally substituted cyclic radical; and
R 8 is hydrogen, C 1-6 alkyl or C 1-6 alkanoyl.
10 . A compound of the formula
or a salt thereof, especially a pharmaceutically useful salt thereof; in which
R 1 is an optionally substituted tetrahydrofuranyl, optionally substituted tetrahydrofuranylmethyl, optionally substituted tetrahydropyranyl or optionally substituted tetrahydropyranylmethyl;
R 2 and R 3 are independently of one another hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, or the two radicals together with the carbon atom to which they are bonded are C 3-8 cycloalkyl;
R 4 and R 5 are independently of one another hydrogen, C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl or the two radicals together with the carbon atom to which they are bonded are C 3-8 cycloalkyl;
R 6 is a group —CH 2 —R 7 , —CH 2 —CO—R 7 , —CH 2 —CH 2 —R 7 , —CH 2 —NR 8 —CO—R 7 , —CH 2 —CO—NR 8 —CH 2 —R 7 , —CH 2 —CH 2 —NR 8 —R 7 , —CH 2 —CO—NR 8 —R 7 or —CO—NR 8 —CH 2 —R 7 ;
R 7 is an optionally substituted cyclic radical; and
R 8 is hydrogen, C 1-6 alkyl or C 1-6 alkanoyl.
11 . A compound according to claim 10 of the formula
or a salt thereof; in which
R 1 , R 4 , R 5 and R 6 have the meaning as indicated for the compound of the formula (I) according to claim 10 .
12 . A pharmaceutically useful salt of a compound according to claim 11 .
13 . A method for the prevention, for delaying the progression or for the treatment of high blood pressure, heart failure, glaucoma, myocardial infarction, renal failure or restenoses, which comprises administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically useful salt thereof according to claim 9 , to a patient in need thereof.
14 . A pharmaceutical composition, comprising a compound of the formula (I) or a pharmaceutically useful salt thereof, according to claim 9 , and a pharmaceutically inert excipient.
15 . A pharmaceutical combination in the form of a product or of a kit comprising individual components a) of a compound of the formula (I) or a pharmaceutically useful salt thereof, according to claim 9 , and b) of at least one pharmaceutical form whose active ingredient has a cardiovascular effect.
16 . A compound according to claim 10 , of the formula
or a pharmaceutically useful salt thereof.Cited by (0)
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