http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-060945-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_12a9e9ce63eb0bbf3658453fb50a6d9b |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-435 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| filingDate | 2007-05-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_070c548f2509c9ab0f98e4cc6c1313d5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ff9d614067e2b34a0a0ac0ebf55a78a0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_523f4a07260a50d472dc1c0670d75cf9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_64c382bbd23338942d7703bf7ff885be http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_49b65f0b283407d8c9ce49db5554257d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c9f2b43b9904d60c6060d563a54cfafb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5cc1c1f495068d5d04f326d1e2de71bc |
| publicationDate | 2008-07-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-060945-A1 |
| titleOfInvention | PROLINAMIDES REPLACED AND ITS USE AS MEDICATIONS |
| abstract | Claim 1: Compounds of the general formula (1) in which D represents a system of substituted bicyclic rings of the formula (2) or (3) where K1 is a bond, or a group -CH2-, -CHR7a-, - CR7bR7c- or -C (O) -, and where R7a / R7b / R7c in each case independently from each other, an F atom, a hydroxy group, C1-5-oxy alkyl, amino, C1-5 alkyl- amino, di- (C1-5 alkyl) -amino, C3-5 cycloalkenyl, C1-5 alkylcarbonylamino, a C1-5 alkyl group, which may be substituted with 1-3 F atoms, a hydroxy group C1-5 alkyl, C1-5 alkyl-C1-5 alkyl, amino C1-5 alkyl, C1-5 alkyl-C1-5 alkyl, di- (C1-5 alkyl) -amino-C1- alkyl 5, C4-7 cycloalkyl-imino-C1-5 alkyl, carboxy-C0-5 alkyl, C1-5 alkyl-oxycarbonll-C0-5 alkyl, aminocarbonyl-C0-5 alkyl, C1-5 alkyl-aminocarbonyl-C0- alkyl 5, di- (C1-5 alkyl) -aminocarbonyl-C0-5 alkyl or a C4-7 -iminocarbonyl-C0-5 alkyl group, where not at the same time the two radicals R7b / R7c may be attached to the ring carbon atom through a heteroatom, except that -C (R7bR7c) - corresponds to a group -CF2, or R7a is a phenyl group substituted with fluorine, chlorine, bromine, methyl, methoxy, amino or nitro or monocyclic heteroaryl, or two radicals R7b / R7c together with the carbon atom of the ring can form a saturated carbocycle of 3, 4, 5, 6 or 7 members or a cyclopentene, cyclohexene, oxetane, azetidine, tiethane, tetrahydrofuran, pyrrolidine ring, tetrahydrothiophene, tetrahydropyran, piperidine, pentamethylene sulfide, hexamethyleneimine, 1,3-dioxolane, 1,4-dioxane, hexahydropyridazine, piperazine, thiomorpholine, morpholine, 2-imidazolidinone, 2-oxazolidinone, tetrahydro-2 (1H) 3] oxazinan-2-one, where their methylene groups may be substituted with 1-2 C1-3 or CF3 alkyl groups, and / or their methylene groups, insofar as they are not bound to a heteroatom, may be substituted with 1-2 fluorine atoms, and / or in which a -CH2 group, next to an atom or of N, it can be replaced by a -CO group, and / or its imino groups can be substituted in each case with a C1-3 alkyl or C1-3 alkylcarbonyl group, and / or in which the sulfur atom it can be oxidized in a sulfoxide or sulfone group, K2 and K3, in each case independently of each other, mean a group -CH2, -CHR8a, -CR8bR8c or a group -C (O), where R8a / R8b / R8c, in each case, independently of one another, a C1-5 alkyl group, which may be substituted with 1-3 fluorine atoms, a C1-5 hydroxyalkyl group, C1-5 alkyl-C1-5 alkyl-alkyl, amino- C1-5 alkyl, C1-5 alkyl-C1-5 alkyl, di- (C1-5 alkyl) -amino-C1-5 alkyl, C4-7 cycloalkylene-C1-5 alkyl, carboxy-C0 alkyl- 5, C1-5 alkyl-oxycarbonyl-C0-5 alkyl, aminocarbonyl-C0-5 alkyl, C1-5 alkyl-C0-5 alkylcarbonyl, di (C1-5 alkyl) -aminocarbonyl-C0-5 alkyl or a group C4-7 cycloalkylene-iminocarbonyl-C0-5 alkyl, or two R8b / R8c radicals, together with the ring carbon atom, can form a saturated carbocycle of 3, 4, 5, 6 or 7 members, or a ring of cyclopentene, cyclohexene, oxetane, azetidine, tiethane, tetrahydrofuran, pyrrolidine, tetrahydrothiophene, tetrahydropyran, piperidine, pentamethylene sulfide, hexamethyleneimino, hexahydropyrrozine, tetrahydropyrrozine 2 (1H) -pyrimidinone, [1,3] oxazinan-2-one, where their methylene groups may be substituted with 1-2 C1-3 or CF3 alkyl groups, and / or their methylene groups, to the extent that they are not bound to a heteroatom, they can be substituted with 1-2 fluorine atoms, and / or in which a -CH2 group, together with a nitrogen atom, can be replaced by a -CO group, and / or its groups imino may be substituted in each case with a C1-3 alkyl or C1-3 alkylcarbonyl group, and / or in which the sulfur atom may be oxidized in a sulfoxide or sulfone group, with the proviso that a heteroatom incorporated by R8b or R8c cannot be separated by only one carbon atom of X in the formula ( 1), and a maximum of four radicals selected from R7a, R7b, R7c, R8a, R8b and R8c may be present in total, and X is an oxygen or sulfur atom, a group CF2, sulfen, sulfone group NR1, in wherein R1 is a hydrogen atom or a hydroxy group, C1-3-oxy alkyl, amino, C1-3-alkyl, di- (C1-3 alkyl) -amino, a C1-5 alkyl group, C2-alkenyl 5-CH2, C2-5-CH2- alkynyl, C3-6 cycloalkyl, C4-6 cycloalkenyl, oxetan-3-yl, tetrahydrofuran-3-yl, benzyl, C1-5 alkylcarbonyl, trifluoromethylcarbonyl, C3-6 cycloalkyl carbonyl, C1-5 alkyl sulfonyl, C3-6 cycloalkyl sulfonyl, aminocarbonyl, C1-5 alkylcarbonyl, di- (C1-5 alkyl) -aminocarbonyl, C1-5-oxycarbonyl alkyl, C4-7-iminocarbonyl cycloalkylene, wherein the methylene and methyl groups found in the groups mentioned above may be additionally substituted with a C1-3 alkyl, carboxy, C1-5 alkoxycarbonyl group, or with a hydroxy group, C1-5-oxy alkyl, amino, C1-5-alkyl, d C1-5-alkyl or C4-7-imino cycloalkylene, provided that the methylene or methyl groups are not directly linked to a heteroatom of the group O, N or S, and / or one to three hydrogen atoms may be replaced by atoms fluorine, provided that the methylene or methyl groups are not directly linked to a heteroatom of the group O, N or S, and in which A1 means N or CR10; A2 means N or CR11; A3 means N or CR12, where R10, R11 and R12, in each case independently of one another, a hydrogen, fluorine, chlorine, bromine or iodine atom, or a C1-5 alkyl group, CF3, C2-5 alkenyl, C2-5 alkynyl, cyano, carboxy, C1-5-oxycarbonyl alkyl, hydroxy, C1-3-oxy alkyl, CF3O, CHF2O, CH2FO, amino, C1-5-amino alkyl, di- (C1-5 alkyl) -amino or C4-7 -imino cycloalkylene; and -LEGJ- is a -CCCC or -CC = CC group, which may be substituted with R4 and R5, and R3 means a hydrogen atom or a C1-3 alkyl group, and R4 is a hydrogen atom or an alkyl group C1-6, C2-6 alkenyl or linear or branched C2-6 alkynyl, wherein the hydrogen atoms of the methylene and / or methyl fragments of the C1-6 alkyl, C2-6 alkenyl or C2-6 straight chain alkynyl group or branched may be replaced, optionally in whole or in part, with fluoro atoms, and / or wherein the hydrogen atoms of the methylene and / or methyl fragments of the C1-6 alkyl, C2-6 alkenyl or alkynyl group Linear or branched C2-6 may optionally be substituted, independently of one another, with one to two substituents selected from a C3-5 cycloalkyl group, a nitrile, hydroxy or C1-5-oxy alkyl group, wherein the hydrogen atoms of the C1-5-oxy alkyl group, they may be replaced wholly or partially by fluorine atoms, a g rupo allyloxy, propargiloxy, benzyloxy, C1-5 alkylcarbonyloxy, C1-5 alkylcarboxyloxy, carboxy C1-5 alkyl oxy, C1-5 alkyl oxycarbonylalkyl C1-5 oxi, mercapto, C1-5 alkyl -sulfanyl, C1-5 alkyl sulfinyl, C1-5 alkyl sulfonyl, carboxy, C1-5 alkyl oxycarbonyl, aminocarbonyl, C1-5 alkyl aminocarbonyl, di- (C1-5 alkyl) aminocarbonyl, C4-7 cycloalkylene -iminocarbonyl, aminosulfonyl, C1-5 alkyl-aminosulfonyl, di- (C1-5 alkyl) -aminosulfonyl, C4-7 -iminosulfonyl cycloalkyl, amino, C1-5-alkyl, di- (C1-5 alkyl) -amino, C1-5 alkylcarbonylamino, C1-5 alkyl sulfonylamino, N- (C1-5 alkyl sulfonyl) -C1-5 alkyl, C3-6 cycloalkylcarbonylamino, or a morpholinyl, thiomorpholinyl, pyrrolidinyl, piperidinyl group, piperazinyl, tetrahydrofuranyl, tetrahydropyranyl, wherein the carbocycles and heterocycles mentioned above in the ring may be substituted in each case with 1-4 C1-3 alkyl or C1-3 alkylcarbonyl groups or with 1-2 oxo groups, and / or where the hydrogen atoms of the sp2-hybridized carbon atoms of the linear or branched C2-6 alkenyl group may be eventually totally or partially replaced by fluorine atoms, or a nitrile, carboxy, aminocarbonyl, C1-5-aminocarbonyl, C3 cycloalkyl group -6-aminocarbonyl, di- (C1-5 alkyl) -aminocarbonyl, C1-5 alkyl-oxycarbonyl or a C4-7-iminocarbonyl cycloalkylene group, where eventually a methylene group may be replaced by an oxygen, sulfur or nitrogen atom substituted with C0-3 alkyl, or a phenyl, mono- or bicyclic heteroaryl, phenyl-C1-5 alkyl or C1-5 heteroarylalkyl- or bicyclic group, which may be substituted in the part of the phenyl or heteroaryl optionally one to three times with the same or different substituents selected from the group consisting of fluorine, chlorine, bromine and iodine atoms, and C1-5 alkyl, trifluoromethyl, amino, C1-5-alkyl, di- (C1-5 alkyl) -amino, hydroxy groups , C1-5-oxy alkyl, mono-, di- or trifluo romethoxy, carboxy and C1-5-oxycarbonyl alkyl, and when -LEGJ- is a -CCCC group, R4 can also represent E or G, also a fluorine atom or a hydroxy, methoxy, C3-5-oxy alkenyl, alkynyl group C3-5-oxy, C2-5-oxy alkyl, C3-6-oxycycloalkyl, C1-5-alkylcarbonyloxy, di (C1-5-alkyl) aminocarbonyloxy or C4-7-iminocarbonyloxy, phenyl-C0-3- alkyl oxy, heteroaryl-C0-3-oxy alkyl, amino, C1-5-alkyl, di- (C1-5-alkyl) -amino, C4-7-imino cycloalkylene, C1-3-amino acyl, (C1-3 acyl ) C1-3-amino alkyl, C1-5 alkyl-oxycarbonylamino, C1-5 alkylcarbonylamino, di (C1-5 alkyl) aminocarbonylamino or C4-7-cycloalkylene iminocarbonylamino, wherein the methyl or methylene groups existing in the alkyl radicals or cycloalkyl previously mentioned may be substituted, independently of each other, with a substituent selected from the group morpholinyl, thiomorpholinyl, pyrrolidinyl, piperidinyl, piperazinyl, tetrahydrofuranyl, tetrahydropyranyl, di methylaminocarbonyl, C1-5 alkylcarboxylic, carboxy, methyl, hydroxyl, methoxy or amino, and the phenyl or heteroaryl radicals mentioned above may optionally be substituted one to three times with the same or different substituents selected from the co group |
| priorityDate | 2006-05-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 110.