http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-053826-A1

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filingDate 2006-03-10^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2007-05-23^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-053826-A1
titleOfInvention ORGANIC COMPOUNDS
abstract Compounds of the general formula (1) that possess renin inhibitory properties and can be used as medicines. Claim 1: A compound of the formula (1) in which R 1 is a) saturated heterocyclyl which is optionally substituted one or more times with C 1-8 alkanoyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 alkoxy, C1-6 alkoxy-C1-6 alkoxy, C1-6 alkoxy-C1-6 alkyl, C1-6 alkoxycarbonylamino, C1-6 alkyl, C0-6 alkylcarbonylamino, C1-6 alkylcarbonyloxy, C1-6 alkylenedioxy, optionally N- amino mono or N, N-di-amino C1-6 alkylated, aryl, carbamoyl optionally N-mono or N, N-di-alkylated C1-6, optionally esterified carboxy, cyano, C3-8 cycloalkoxy, C3-8 alkylcyclo C0-6, halogen, C1-6 haloalkoxy, C1-6 haloalkyl, heteroaryl, unsaturated heterocyclyl, partially saturated or saturated, hydroxy, nitro, oxidized or oxo which is attached by means of a C atom; ob) azepanyl-, azetidinyl-, aziridinyl-, dioxanyl-, dioxepanyl-, dioxolanyl-, dithianyl-, dithiolanyl-, furanyl-, oxathianyl-, oxepanlo-, tetrahydropyranyl-, tetrahydrofuranyl-, tetrahydrothiophenyl-, tetrahydrothiopyl-, tetrahydrothiopyl- saturated bicyclic C1-4 alkyl heterocyclyl which is optionally substituted one or more times with C1-8 alkanoyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 alkoxy-C1-6 alkoxy, C1 alkoxy -6-C1-6 alkyl, C1-6 alkoxycarbonylamino, C1-6 alkyl, C0-6 alkylcarbonylamino, C1-6 alkylcarbonyloxy, C1-6 alkylenedioxy, optionally N-mono or N amino, N-di-alkylated C1-6 , aryl, optionally N-mono or N, N-di-alkylated C1-6 carbamoyl, optionally esterified carboxy, cyano, C3-8 cycloalkoxy, C3-8 cycloalkyl-C0-6 alkyl, halogen, C1-6 halo-alkoxy, halo- C 1-6 alkyl, heteroaryl, unsaturated heterocyclyl, partially saturated or saturated, hydroxy, nitro, oxide or oxo; or c) C2-8 alkynyl which is optionally substituted one or more times with C1-8 alkanoyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 alkoxy-C1-6 alkoxy, C1-6 alkoxy -C 1-6 alkyl, C 1-6 alkoxycarbonylamino, C 1-6 alkyl, C 1-6 alkylcarbonylamino, C 1-6 alkylcarbonyloxy, C 1-6 alkylenedioxy, optionally N-mono or N amino, N-di-C 1-6 alkylated, aryl , optionally N-mono or N, N-di-alkylated C1-6 carbamoyl, optionally esterified carboxy, cyano, C3-8 cycloalkoxy, C3-8 cycloalkyl-C0-6 alkyl, halogen, halo C1-6 alkoxy, halo- C1-6 alkyl, heteroaryl, unsaturated heterocyclyl, partially saturated or saturated, hydroxy, nitro or oxo, or R2 is, independently of each other, 1-4 radicals selected from: C1-8 alkanoyl, C1-8 alkanoyl-alkoxy C2-4 carrying the alkanoyl group in a position superior to alpha, C1-8 alkanoylamino-C1-4 alkoxy, N-C1-4 alkanoylamino-C1-4 alkyl, C1-8 alkanoyloxy-C1-4 alkyl, N'- C2-8 alkanoyl piperazin C1-4 alkoxy, N'-alkanoyl piper azina-C2-8-C1-4 alkyl, C1-8 alkanesulfonyl-C1-4 alkoxy, C1-8 alkanesulfonyl-C1-4 alkyl, alkanesulfonylamino C1-8-C1-4 alkoxy, C1-4-sulfonylamino-C1 alkyl -4, C1-8 alkanulfonyl- (hydroxy) C1-4 alkoxy, C2-8 alkenyloxy, C2-8 alkenyloxy-C1-4 alkoxy, C2-8 alkenyloxy-C1-4 alkyl, C1-8 alkoxy, C1- alkoxy 6-C 1-6 alkanoyl, C 1-4 alkoxy-C 2-4 alkenyl, C 1-4 alkoxy-C 2-4 alkoxy, C 1-4 alkoxy-C 1-4 alkoxy, C 1-4 alkoxy-C 1-4 alkoxy-C 1- alkyl 4, C1-4 alkoxy-C1-4 alkyl, C1-4 alkoxycarbonyl-C1-4 alkoxy, C1-4 alkoxycarbonyl C1-4 alkyl, C1-8 alkoxycarbonylamino-C1-4 alkoxy, C1-8 alkoxycarbonylamino-C1 alkyl -4, C1-8 alkyl, C1-4 alkyl, N, N-di-C1-4 alkyl, C1-4 alkylaminoalkoxy, N, N-di-C1-4 alkylamino-C1-4 alkoxy, C1-4 alkylamino C1-4 alkyl, N, N-di-C1-4 alkylamino-C1-4 alkyl, N-mono- or N, N-di-C1-4 alkylcarbamoyl-C1-4 alkoxy, N-mono- or N, N -di-C1-4 alkylcarbamoyl C1-4 alkyl, N'-C1-4 alkylpiperazin C1-4 alkoxy, N'-C1-4 alkylpiperazin-C1-4 alkyl, alkyl C1-4-C1-4alkoxy, C1-4alkyl- (hydroxy) C1-4alkoxy, C1-4alkyl-C1-4alkyl, aminoC1-4alkoxy, amino-C1-4alkyl, carbamoyl-alkoxy C1-4, carbamoyl-C1-8 alkyl, carboxy-C1-4 alkoxy, carboxy-C1-4 alkyl, cyano-C1-4 alkoxy, cyano-C1-4 alkyl, C3-8 cycloalkoxy, C3-8 alkoxycycloalkoxy C1-4, C3-8 cycloalkoxy-C1-4 alkyl, C3-8 cycloalkyl, S, S-dioxothiomorpholino-C1-4 alkoxy, S, S-dioxothiomorpholin-alkyl 14, halogen, halo-C1-4 alkoxy, halo- C1-4 alkyl, halo- (hydroxy) C2-8 alkoxy, hydroxy, hydroxyC2-8 alkoxy, hydroxyC2-8 alkyl, imidazolylthio-C1-4 alkoxy, imidazolylthio-1-4 alkyl, morpholino-C1- alkoxy 4 optionally N-oxidized, morpholin-C 1-4 alkyl, S-oxothiomorpholino-C 1-4 alkoxy, S-oxothiomorpholino-C 1-4 alkyl, piperazino-C 1-4 alkoxy, piperazino-C 1-4 alkyl, piperidino-C 1- alkoxy 4, piperidine-C 1-4 alkyl, pyridyl- or N-oxidopyrididyl-optionally partially hydrogenated C 1-4 alkoxy, pyridyl- or N-oxidopyridyl-optionally partially hydrogenated C 1-4 alkyl, pyridyl optionally N-oxidized C1-4-alkoxy, pyridylthio-C1-4alkyl optionally N-oxidized, pyrimidinylthio-C1-4alkoxy, pyrimidinylthio-C1-4alkyl, pyrrolidino-C1-4alkoxy, pyrrolidine-C1-4alkyl, thiazolinylthio-C1-4 alkoxy, thiazolinylthio-C1-4alkyl, thiazolyl-C1-4alkoxy, thiazolylthio-C1-4alkoxy, thiazolylthio-C1-4alkyl, thiomorpholino-C1-4alkoxy, thiomorpholino-C1-4alkyl, trifluor - C1-8 alkan sulfonyl-C1-4 alkoxy, trifluor-alkane sulfonylamino C1-8-C1-4 alkyl, phenyl or naphthyl which is unsubstituted or mono-, di- or trisubstituted with C1-4 alkoxy, C1-4 alkyl , C1-4 alkylamino, C1-4 di-alkylamino, halogen, hydroxy and / or trifluoromethyl, and phenyl- or naphthyl-C1-4 alkoxy which is unsubstituted or mono-, di- or trisubstituted with C1-4 alkoxy, alkyl C1-4, C1-4 alkylamino, C1-4 d-alkylamino, halogen, hydroxy and / or trifluoromethyl, and its salt, prodrug or compound in which one or more atoms are replaced by their non-radioactive, stable isotopes, especially salt pharmacist only acceptable; except for the compounds in which R1 is optionally substituted N-acetylpiperidin-4-yl or optionally substituted oxopiperidinyl.
priorityDate 2005-03-11^^<http://www.w3.org/2001/XMLSchema#date>
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