Beta-Aminoacid-Derivatives As Factor Xa Inhibitors

A compound of formula I,

• wherein
• R0 is 1) a heterocyclyl selected from acridinyl, azabenzimidazolyl, azaspirodecanyl, azepinyl, azetidinonyl, azetidinyl, aziridinyl, benzimidazolyl, 1,3-benzodioxolyl, benzofuranyl, benzothienyl, benzothiofuranyl, benzothiophenyl, benzoxazolyl, benzothiazolyl, benztriazolyl, benztetrazolyl, benzisoxazolyl, benzisothiazolyl, carbazolyl, 4aH-carbazolyl, carbolinyl, chromanyl, chromenyl, cinnolinyl, decahydrochinolinyl, 4,5-dihydrooxazolinyl, 1,4-diazepanyl, 1,2-diazepinyl, 1,3-diazepinyl, 1,4-diazepinyl, diazirinyl, dioxazolyl, dioxazinyl, 1,3-dioxolanyl, 1,3-dioxolenyl, dioxolyl, 6H-1,5,2-dithiazinyl, dihydrofuro[2,3-b]-tetrahydrofuranyl, furyl, furazanyl, imidazolidinyl, imidazolinyl, imidazolyl, indanyl, 1H-indazolyl, indolinyl, indolizinyl, indolyl, 3H-indolyl, isobenzofuranyl, isochromanyl, isoindazolyl, isoindolinyl, isoindolyl, isoquinolinyl, isothiazolyl, isothiazolidinyl, isothiazolinyl, isoxazolyl, isoxazolinyl, isoxazolidinyl, 2-isoxazolinyl, ketopiperazinyl, morpholinyl, naphthyridinyl, octahydroisoquinolinyl, oxadiazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2-oxa-thiepanyl, 1,2-oxathiolanyl, 1,4-oxazepanyl, 1,4-oxazepinyl, 1,2-oxazinyl, 1,3-oxazinyl, 1,4-oxazinyl, oxaziridinyl, oxazolidinyl, oxazolinyl, oxazolyl, oxiranyl, phenanthridinyl, phenanthrolinyl, phenazinyl, phenothiazinyl, phenoxathiinyl, phenoxazinyl, phenylpyridyl, phthalazinyl, piperazinyl, piperidinyl, pteridinyl, purinyl, pyranyl, pyrazinyl, pyrazolidinyl, pyrazolinyl, pyrazolyl, pyridazinyl, pyridoimidazolyl, pyridonyl, pyridooxazolyl, pyridopyridinyl, pyridopyrimidinyl, pyridothiazolyl, pyridothienyl, pyridyl, pyrimidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolinyl, 1H-pyrrolopyridinyl, 2H-pyrrolyl, pyrrolyl, quinazolinyl, quinolinyl, 4H-quinolizinyl, quinolyl, quinoxalinyl, quinuclidinyl, tetrahydrofuranyl, tetrahydroisoquinolinyl, tetrahydroquinolinyl, 1,4,5,6-tetrahydro-pyridazinyl, tetrahydropyranyl, tetrahydropyridinyl, tetrahydrothiophenyl, tetrazinyl, tetrazolyl, thiadiazinyl, 6H-1,2,5-thiadiazinyl, thiadiazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, thianthrenyl, 1,2-thiazinyl, 1,3-thiazinyl, 1,4-thiazinyl, 1,3-thiazolyl, thiazolyl, thiazolidinyl, thiazolinyl, thienyl, thietanyl, thienothiazolyl, thienooxazolyl, thienoimidazolyl, thietanyl, thiomorpholinyl, thiophenolyl, thiophenyl, thiopyranyl, 1,2,3-triazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl, triazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,5-triazolyl, 1,3,4-triazolyl or xanthenyl,
• wherein the heterocyclyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R8 or
• 2) a 6- to 14-membered aryl selected from phenyl, naphthyl, biphenylyl, 2-biphenylyl, 3-biphenylyl, 4-biphenylyl, anthryl or fluorenyl, wherein the aryl is mono-, di- or trisubstituted independently of one another by R8,
• R8 is halogen, carbamimidoyl, —NO2, —CN, —C(O)—NH2, —OH, —NH2, —O—CF3, —SO2—CH3, —SO2—CF3,
• —O—(C1-C8)-alkyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by halogen, NH2, —OH or methoxy, or —(C1-C8)-alkyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by halogen, NH2, —OH or methoxy,
• provided that R8 is at least one halogen, —C(O)—NH2 or —O—(C1-C8)-alkyl residue,
• Q is a direct bond, —(C0-C2)-alkylene-C(O)—(C0-C2)-alkylene,
• —(C1-C6)-alkylene, —(C0-C3)-alkylene-S(O)2— or —(C0-C2)-alkylene-NR10—C(O)—O—(C0-C2)-alkylene, wherein the alkylene residues are unsubstituted or mono-, di- or trisubstituted independently of one another by halogen, —NH2, —OH or —(C3-C6)-cycloalkylen, wherein cycloalkylen is unsubstituted or mono-, di- or trisubstituted independently of one another by halogen, —NH2 or —OH;
• R1 is a hydrogen atom, —(C1-C3)-alkylene-C(O)—NH—R0,
• —(C1-C3)-alkylene-C(O)—O—R10, —(C1-C3)-perfluoroalkyl, —(C1-C3)-alkylene-S(O)—(C1-C4)-alkyl, —(C1-C3)-alkylene-S(O)2—(C1-C3)-alkyl, —(C1-C3)-alkylene-S(O)2—N(R4′)—R5′, —(C1-C3)-alkylene-O—(C1-C4)-alkyl, —(C0-C3)-alkylene-(C3-C8)-cycloalkyl, —(C1-C4)-alkyl, which is unsubstituted or substituted one to three times by R13,
• a 6- to 14-membered aryl selected from phenyl, naphthyl, biphenylyl, 2-biphenylyl, 3-biphenylyl, 4-biphenylyl, anthryl or fluorenyl, wherein the aryl is mono-, di- or trisubstituted independently of one another by R8, or —(C0-C4)-alkylene-heterocyclyl, wherein the heterocyclyl is as defined for R0, and is unsubstituted or mono-, di- or trisubstituted independently of one another by R14,
• R4′ and R5′ are each independently hydrogen atom or —(C1-C4)-alkyl,
• R2 is a direct bond or —(C1-C4)-alkylene,
• V is 1) a heterocyclyl as defined for R0, wherein said heterocyclyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R14 or
• 2) an aryl as defined for R0, wherein aryl is mono-, di- or trisubstituted independently of one another by R14,
• R1—N—R2—V form a 4- to 10-membered cyclic group selected from azepine, azetidine, azetidinone, dioxazole, dioxazine, 1,4-diazepane, 1,2-diazepine, 1,3-diazepine, 1,4-diazepine, 2,3 dihydroindole, imidazole, imidazoline, imidazolidine, indole, isothiazole, isothiazolidine, isothiazoline, isoxazole, isoxazoline, isoxazolidine, 2-isoxazoline, ketopiperazine, morpholine, 1,4-oxazepane, 1,2-oxa-thiepane, 1,2-oxathiolane, 1,4-oxazepane, 1,2-oxazine, 1,3-oxazine, 1,4-oxazine, oxazole, piperazine, piperidine, pyrazine, pyrazole, pyrazoline, pyrazolidine, pyridine, pyrimidine, pyrrole, pyrrolidine, pyrrolidinone, pyrroline, tetrahydropyridine, tetrazine, tetrazole, thiadiazole, thiazole, thiazolidine, thiazoline, thiomorpholine, 1,2,3-triazine, 1,2,4-triazine, 1,3,5-triazine, 1,2,3-triazole or 1,2,4-triazole,
• wherein the cyclic group is unsubstituted or mono-, di- or trisubstituted independently of one another by R14,
• R14 is halogen, —OH, ═O, —(C1-C8)-alkyl, —(C1-C4)-alkoxy, —NO2, —(C0-C4)-alkyl-C(O)—O—R18, —CN, —(C0-C4)-alkyl-N(R18)-R21, —(C0-C4)-alkyl-O—R18, —(C0-C8)-alkyl-SO2—(C1-C4)-alkyl, —S—R18, —(C0-C8)-alkyl-SO2—(C1-C3)-perfluoroalkyl, —(C0-C8)-alkyl-SO2—N(R18)—R21, —CF3, —C(O)—N(R18)-R21, —NR18—C(O)—NH—(C1-C8)-alkyl, —(C0-C3)-alkyl-(C1-C3)-perfluoroalkyl, —NR18—C(O)—N—[(C1-C8)-alkyl]2, or
• —(C0-C4)-alkylene-heterocyclyl, wherein the heterocyclyl is as defined for R0, and is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• R18 and R21 are each independently hydrogen atom, —(C0-C6)-alkyl-N(R22)—R23, —(C0-C6)-alkyl-O—R22, —(C0-C6)-alkyl-N(R22)—C(O)—N(R22)—R23, —(C0-C6)-alkyl-C(O)—O—R22, —(C1-C6)-alkyl, —(C0-C6)-alkyl-C(O)—N(R22)—R23, —(C0-C6)-alkyl-SO2—R22, —(C1-C3)-perfluoroalkyl, or
• —(C0-C6)-alkyl-heterocyclyl, wherein the heterocyclyl is as defined for R0, and is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• R22 and R23 are each independently hydrogen atom, —(C1-C3)-perfluoroalkyl, —(C3-C6)-cycloalkyl or —(C1-C6)-alkyl,
• G is a direct bond, —(CH2)m—NR10—SO2—NR10—(CH2)n—, —(CH2)m—CH(OH)—(CH2)n—, —(CH2)m—, —(CH2)m—O—(CH2)n—, —(CH2)m—C(O)—NR10—(CH2)n—, —(CH2)—SO2—(CH2)n—, —(CH2)m—NR10—C(O)—NR10—(CH2)n—, —(CH2)m—NR10—C(O)—(CH2)n—, —(CH2)m—C(O)—(CH2)n—, —(CH2)—S—(CH2)n—, —(CH2)m—SO2-NR10—(CH2)n—, —(CH2)m—NR10—SO2—(CH2)n—, —(CH2)m—NR10—, —(CH2)m—O—C(O)—NR10—(CH2)n— or —(CH2)m—NR10—C(O)—O—(CH2)n—,
• n and m are each independently 0, 1, 2, 3, 4, 5 or 6, or
• M is a monocyclic or bicyclic 3-to 15-membered heterocyclyl selected from acridinyl, azaindole, azabenzimidazolyl, azaspirodecanyl, azepanyl, azepinyl, azetidinyl, aziridinyl, azirinyl, benzimidazolyl, benzofuranyl, benzothiofuranyl, benzothiophenyl, benzoxazolyl, benzthiazolyl, benztriazolyl, benztetrazolyl, benzisoxazolyl, benzisothiazolyl, carbazolyl, 4aH-carbazolyl, carbolinyl, chromanyl, chromenyl, cinnolinyl, decahydrochinolinyl, 1,4diazepanyl, 1,2-diazepinyl, 1,3-diazepinyl, 1,4-diazepinyl, diaziridinyl, diazirinyl, dihydropyrimidinonyl, dihydroimidazolonyl, 4,5-dihydrooxazolinyl, dioxazolyl, dioxazinyl, dioxolyl, 1,3-dioxolanyl, 1,3-dioxolenyl, 3,3-dioxo-(1,3,4)oxathiazinyl, 6H-1,5,2-dithiazinyl, dihydrofuro[2,3-b]-tetrahydrofuranyl, furanyl, furazanyl, imidazolidinyl, imidazolidinonyl, imidazolinyl, imidazolyl, 1H-indazolyl, indolinyl, indolizinyl, indolyl, 3H-indolyl, isobenzofuranyl, isochromanyl, isoindazolyl, isoindolinyl, isoindolyl, isoquinolinyl, benzimidazolyl, isothiazolyl, isothiazolidinyl, isothiazolinyl, isoxazolyl, isoxazolinyl, isoxazolidinyl, 2-isoxazolinyl, ketomorpholinyl, ketopiperazinyl, morpholinyl, morpholinonyl, naphthyridinyl, octahydroisoquinolinyl, oxadiazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, [1,3,4]oxathiazinane 3,3-dioxidyl, 1,2-oxa-thiepanyl, 1,2-oxathiolanyl, 1,4-oxazepanyl, 1,4-oxazepinyl, 1,2-oxazinyl, 1,3-oxazinyl, 1,4-oxazinyl, oxazolidinyl, oxazolidinonyl, oxazolinyl, oxazolonyl, oxazolyl, oxetanyl, oxiranyl, oxocanyl, phenanthridinyl, phenanthrolinyl, phenazinyl, phenothiazinyl, phenoxathiinyl, phenoxazinyl, phthalazinyl, piperazinyl, piperazinonyl, piperazin-2-on-yl, piperidinonyl, piperidinyl, pteridinyl, purinyl, pyranyl, pyrazinyl, pyrazinonyl, pyrazin-2-on-yl, pyrazolidinyl, pyrazolinyl, pyrazolyl, pyridazinyl, pyridazinonyl, pyridonyl, pyridooxazolyl, pyridoimidazolyl, pyridothiazolyl, pyridyl, pyrimidinyl, pyrimidinedionyl, pyrimidinonyl, pyrimidine-2,4-dionyl, pyrrolidinyl, pyrrolidinonyl, pyrrolinyl, 2H-pyrrolyl, pyrrolyl, quinazolinyl, quinolinyl, 4H-quinolizinyl, quinoxalinyl, quinuclidinyl, tetrahydrofuranyl, tetrahydroisoquinolinyl, tetrahydroquinolinyl, tetrahydrofuranyl, tetrahydropyranyl, 1,4,5,6,-tetrahydro-pyridazinyl, tetrahydropyridinyl, tetrahydro-pyrimidininyl, tetrahydrothiophenyl, tetrazinyl, tetrazolyl, 6H-1,2,5-thiadiazinyl, thiadiazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, thianthrenyl, 1,2-thiazinyl, 1,3-thiazinyl, 1,4-thiazinyl, 1,3-thiazolyl, thiazolyl, thiazolidinyl, thiazolinyl, thienyl, thietanyl, thienothiazolyl, thienooxazolyl, thienoimidazolyl, thietanyl, thiomorpholinyl, thiomorpholine 1,1-dioxidyl, thiophenolyl, thiophenyl, thiopyranyl, 1,2,3-triazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl, 1,2,3-triazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,5-triazolyl, 1,3,4-triazolyl and xanthenyl, wherein the heterocyclyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R14, provided that M contains or is substituted with at least one oxo-residue,
• R3 or R4 are each independently
• 1) hydrogen atom,
• 2) halogen,
• 3) —(C1-C4)-alkyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 4) —(C1-C3)-perfluoroalkyl,
• 5) phenyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 6) —(C1-C4)-alkylene-O—R19, wherein R19 is
• a) hydrogen atom,
• b) —(C1-C4)-alkyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13, or
• c) phenyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• d) —CF3, or
• e) —CHF2,
• 7) —CN,
• 8) —SOs—R11, wherein s is 1 or 2,
• 9) —SOt—N(R11)—R12, wherein t is 1 or 2,
• 10) —(C0-C4)-alkylene-C(O)—R11,
• 11) —(C0-C4)-alkylene-C(O)—O—R11,
• 12) —(C0-C4)-alkylene-C(O)—N(R11)—R12,
• 13) —(C1-C4)-alkylene-N(R11)—R12,
• 14) —S—R10,
• 15) —(C0-C2)alkylene-C(O)—O—(C2-C4)-alkylene-O—C(O)—(C1-C4)-alkyl,
• 16) —C(O)—O—C(R15, R16)—O—C(O)-R17,
• 17) —(C0-C2)alkylene-C(O)—O—(C2-C4)-alkylene-O—C(O)—O—(C1-C6)-alkyl,
• 18) —C(O)—O—C(R15, R16)—O—C(O)—O—R17,
• 19) —(C1-C4)-alkylene-(C6-C14)-aryl, wherein aryl is mono-, di- or trisubstituted independently of one another by R13,
• 20) —(C1-C4)-alkylene—(C4-C15)-heterocyclyl, wherein heterocyclyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 21) —(C1-C4)-alkylene—(C3-C8)-cycloalkyl, wherein cycloalkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 22) —(C1-C4)-alkylene-het, wherein het is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 23) —(C1-C4)-alkylene-O—CH2—(C1-C3)-perfluoroalkylene-CH2—O—(C0-C4)-alkyl,
• 24) —SOw—N(R11)—R13, wherein w is 1 or 2,
• 25) —(C1-C4)-alkylene-N(R11)—C(O)—R12,
• 26) —(C1-C4)-alkylene-N(R11)—C(O)—O—R12 or
• 27) a residue selected from
• wherein Me is methyl,
• R5 is
• 1) halogen,
• 2) phenyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 3) —(C0-C4)-alkylene-O—R29, wherein R29 is phenyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 4) —NO2,
• 5) —CN,
• 6) —SOs—R11, wherein s is 1 or 2,
• 7) —SOt—N(R11)—R12, wherein t is 1 or 2,
• 8) —C(O)—R11,
• 9) —C(O)—O—R11,
• 10) —C(O)—N(R11)—R12,
• 11) —N(R11)—R12,
• 12) —N(R30)—SO2—R30, wherein R30 is hydrogen atom, —(C1-C4)-alkyl, —(C1-C4)-alkyl-OH, —(C1-C4)-alkyl-O—(C1-C4)-alkyl, or —(C1-C3)-perfluoro-alkyl,
• 13) —C(O)—O—(C2-C4)-alkylene-O—C(O)—(C1-C4)-alkyl,
• 14) —C(O)—O—(C2-C4)-alkylene-O—C(O)—O—(C1-C6)-alkyl,
• 15) —C(O)-O—C(R15, R16)—O—C(O)—R17,
• 16) —C(O)—O—C(R15, R16)—O—C(O)—O—R17,
• 17) —(C1-C4)-alkylene-(C6-C14)-aryl, wherein aryl is mono-, di- or trisubstituted independently of one another by R13,
• 18) —(C1-C4)-alkylene-(C4-C15)-heterocyclyl, wherein heterocyclyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R13
• 19) —(C1-C4)-alkylene-(C3-C8)-cycloalkyl, wherein cycloalkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 20) —(C1-C4)-alkylene-het, wherein het is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 21) —SOw—N(R11)—R13, wherein w is 1 or 2,
• 22) —N(R11)—C(O)—R30,
• 23) —N(R11)—C(O)—O—R30 or
• 24) a residue selected from
• wherein Me is methyl,
• R6 is
• 1) hydrogen atom,
• 2) halogen,
• 3) —(C1-C4)-alkyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 4) —(C1-C3)-perfluoroalkyl,
• 5) phenyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 6) —(C0-C4)-alkylene-O—R19, wherein R19 is
• a) hydrogen atom,
• b) —(C1-C4)-alkyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13, or
• c) phenyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• d) —CF3, or
• e) —CHF2,
• 7) —NO2,
• 8) —CN,
• 9) —SOs—R11, wherein s is 1 or 2,
• 10) —SOt—N(R11)—R12, wherein t is 1 or 2,
• 11) —(C0-C4)-alkylene-C(O)—R11,
• 12) —(C0-C4)-alkylene-C(O)—O—R11,
• 13) —(C0-C4)-alkylene-C(O)—N(R11)—R12,
• 14) —(C0-C4)-alkylene-N(R11)—R12,
• 15) —NR11—SO2—R12,
• 16) —S—R10,
• 17) —(C0-C2)alkylene-C(O)—O—(C2-C4)-alkylene-O—C(O)—(C1-C4)-alkyl,
• 18) —C(O)—O—C(R15, R16)—O—C(O)—R17,
• 19) —(C0-C2)alkylene-C(O)—O—(C2-C4)-alkylene-O—C(O)—O—(C1-C6)-alkyl,
• 20) —C(O)—O—C(R15, R16)—O—C(O)—O—R17,
• 21) —(C1-C4)-alkylene-(C6-C14)-aryl, wherein aryl is mono-, di- or trisubstituted independently of one another by R13,
• 22) —(C1-C4)-alkylene-(C4-C15)-heterocyclyl, wherein heterocyclyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 23) —(C1-C4)-alkylene-(C3-C8)-cycloalkyl, wherein cycloalkyl is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 24) —(C1-C4)-alkylene-het, wherein het is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 25) —(C0-C4)-alkylene-O—CH2—(C1-C3)-perfluoroalkylene-CH2—O—(C0-C4)-alkyl,
• 26) —SOw—N(R11)—R13, wherein w is 1 or 2,
• 27) —(C0-C4)-alkylene-N(R11)—C(O)—R12,
• 28) —(C0-C4)-alkylene-N(R11)—C(O)—O—R12 or
• 29) a residue selected from
• wherein Me is methyl, or
• R3 and R6, R3 and R4, or R4 and R6 together with the carbon atoms to which they are attached form [1,3]-dioxalane or [1,4]-dioxane, each of which is unsubstituted or substituted one, two, three or four times by R13, or R3 and R4, or R5 and R6 together with the carbon atom to which they are attached form a 3-to 8-membered ring selected from azetidine, azocane, azocane-2-one, cyclobutyl, cyloheptyl cyclohexyl, cyclooctane, cyclooctene, cyclopropyl, 1,4-diazepane, 1,2-diazepine, 1,3-diazepine, 1,4-diazepine, [1,4]diazocane, [1,2]diazocan-3-one, [1,3]diazocan-2-one, dioxazine, [1,4]dioxocane, dioxole, ketopiperazine, morpholine, 1,2-oxa-thiepane, 1,4-oxazepane, 1,2-oxazine, 1,3-oxazine, 1,4-oxazine, [1,4]oxazocane, [1,3]oxazocan-2-one, oxetane, oxocane, oxocan-2-one, piperazine, piperidine, pyran, 5,6,7,8-tetrahydro-1H-azocin-2-one, thiomorpholine or tetrahydrofurane, wherein the ring is unsubstituted or mono-, di- or trisubstituted independently of one another by R13, or
• R3 and R5, or R4 and R6 together with the carbon atoms to which they are attached form a 4- to 8-membered ring selected from azetidine, azocane, azocane-2-one, cyclobutyl, cyloheptyl cyclohexyl, cyclooctane, cyclooctene, cyclopropyl, 1,4-diazepane, 1,2-diazepine, 1,3-diazepine, 1,4-diazepine, [1,4]diazocane, [1,2]diazocan-3-one, [1,3]diazocan-2-one, dioxazine, [1,4]dioxocane, dioxole, ketopiperazine, morpholine, 1,2-oxa-thiepane, 1,4-oxazepane, 1,2-oxazine, 1,3-oxazine, 1,4-oxazine, [1,4]oxazocane, [1,3]oxazocan-2-one, oxetane, oxocane, oxocan-2-one, piperazine, piperidine, pyran, 5,6,7,8-tetrahydro-1H-azocin-2-one, thiomorpholine or tetrahydrofurane, wherein the ring is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• R11 and R12 are each independently
• 1) hydrogen atom,
• 2) —(C1-C6)-alkyl, which is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• 3) —(C0-C6)-alkyl-(C3-C8)-cycloalkyl,
• 4) —SOt—R10, wherein t is 1 or 2,
• 5) —(C0-C6)-alkyl-(C6-C14)-aryl, wherein the alkyl and aryl independently from one another are unsubstituted or mono-, di- or trisubstituted by R13,
• 6) —(C1-C3)-perfluoroalkyl,
• 7) —O—R17, or
• 8) —(C0-C6)-alkyl-heterocyclyl, wherein the heterocyclyl is as defined for R0, and the alkyl and heterocyclyl independently from one another are unsubstituted or mono-, di- or trisubstituted by R13, or
• R11 and R12 together with the nitrogen atom to which they are attached form a 4- to 8-membered monocyclic heterocyclic ring which in addition to the nitrogen atom optionally contains one or two identical or different ring heteroatoms selected from oxygen, sulfur or nitrogen, wherein the heterocyclic ring is unsubstituted or mono-, di- or trisubstituted independently of one another by R13,
• R13 is halogen, —NO2, —CN, ═O, —OH, —CF3, —C(O)—O—R10, —C(O)—N(R10)—R20, —N(R10)—R20, —(C3-C8)-cycloalkyl, —(C0-C3)-alkylene-O—R10, —Si—(CH3)3, —N(R10)—S(O)u—R10, wherein u is 1 or 2, —S—R10, —SOr—R10, wherein r is 1 or 2, —S(O)v—N(R10)—R20, wherein v is 1 or 2, —C(O)—R10, —(C1-C8)-alkyl, —(C1-C8)-alkoxy, phenyl, phenyloxy-, —(C1-C3)-perfluoroalkyl, —(C0-C4)-alkyl-C(O)—O—C(R15, R16)—O—C(O)—R17, —O—R15, —NH—C(O)—NH—R10, —O—CF3, —(C0-C4)-alkyl-C(O)—O—C(R15, R16)—O—C(O)—O—R17, —NH—C(O)—O—R10, or a residue selected from
• R10 and R20 are each independently hydrogen, halogen, —(C1-C6)-alkyl, —(C0-C4)-alkyl-OH, —(C0-C4)-alkyl-O—(C1-C4)-akyl or —(C1-C3)-perfluoroalkyl, R15 and R16 are each independently hydrogen, —(C1-C6)-alkyl, or together with the carbon atom to which they are attached form a 3- to 6 membered carbocyclic ring which is unsubstituted or substituted one to three times by R10, and
• R17 is —(C1-C6)-alkyl, —(C1-C6)-alkyl-OH, —(C1-C6)-alkyl-O—(C1-C6)-alkyl, —(C3-C8)-cycloalkyl, —(C1-C6)-alkyl-O—(C1-C8)-alkyl-(C3-C8)-cycloalkyl, —(C1-C6)-alkyl-(C3-C8)-cycloalkyl, wherein the cycloalkyl ring is unsubstituted or substituted one, two or three times by —OH, —O—(C1-C4)-alkyl or R10,
• or a stereoisomeric form thereof, a mixture of the stereoisomeric forms thereof in any ratio, or a physiologically tolerable salt thereof.