CO4410337A1 - CONDENSED DERIVATIVES OF AZEPINA, MEDICINES CONTAINING THESE COMPOUNDS AND PROCEDURE FOR THEIR PREPARATION - Google Patents

CONDENSED DERIVATIVES OF AZEPINA, MEDICINES CONTAINING THESE COMPOUNDS AND PROCEDURE FOR THEIR PREPARATION

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Publication number
CO4410337A1
CO4410337A1 CO95035030A CO95035030A CO4410337A1 CO 4410337 A1 CO4410337 A1 CO 4410337A1 CO 95035030 A CO95035030 A CO 95035030A CO 95035030 A CO95035030 A CO 95035030A CO 4410337 A1 CO4410337 A1 CO 4410337A1
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Colombia
Prior art keywords
group
carbon
case
atoms
alkyl
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CO95035030A
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Spanish (es)
Inventor
Frank Himmelsbach
Helmut Pieper
Austel Volkhard
Gunter Linz
Brian Guth
Johannes Weisenberger
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Thomae Gmbh Dr K
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Publication of CO4410337A1 publication Critical patent/CO4410337A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

1. DERIVADOS DE AZEPINA CONDENSADOS DE LA FORMULA GENERAL (I) FIGURA 1 EN LA QUE R1 REPRESENTA UN ATOMO DE HIDROGENO, UN GRUPO ALQUILO CON 1 A 6 ATOMOS DE CARBONO, UN GRUPO CICLOALQUILO DE 3 A 7 ATOMOS DE CARBONO, UN GRUPO ALQUENILO O ALQUINILO QUE TIENE EN CADA CASO DE 3 A 8 ATOMOS DE CARBONO, UN GRUPO ALQUILO, QUE ESTA SUSTITUIDO CON UN GRUPO HIDROXI, ALCOXI, AMINO, ALQUILAMINO, DIALQUILAMI- NO, CARBOXI, ALCOXICARBONILO, AMINOCARBONILO, AL- QUILAMINOCARBONILO, DIALQUILAMINOCARBONILO, ARILO O HETEROARILO, O CON UN GRUPO CICLOALQUILO QUE TIENE DE 3 A 7 ATOMOS DE CARBONO, UN GRUPO AMIDINO, UN GRUPO CARBONILO, QUE ESTA SUSTITUIDO CON UN ATOMO DE HIDROGENO, CON UN GRUPO ALQUILO, TRIFLUO- ROMETILO, ALCOXI, ARILALCOXI, ALILOXI O R10 -CO-0- (R11CR12)-O, REPRESENTADO R10 UN GRUPO ALQUILO CON 1 A 8 ATOMOS DE CARBONO, UN GRUPO CICLOALQUILO CON 5 A 7 ATOMOS DE CARBONO, UN GRUPO ARILO O ARILALQUILO, R11 UN ATOMO DE HIDROGENO, UN GRUPO ALQUILO, UN GRUPO CICLOALQUILO CON 5 A 7 ATOMOS DE CARBONO O UN GRUPO ARILO, Y R12 UN ATOMO DE HIDROGENO O UN GRUPO ALQUILO, R2 HASTA R9, QUE PUEDEN SER IGUALES O DIFERENTES, REPRESENTAN ATOMOS DE HIDROGENO, GRUPOS ALQUILO, ARILO O ARIALQUILO, O R2 Y R4 EN COMUN Y/O R6 Y R8 EN COMUN REPRESENTAN EN CADA CASO OTRO ENLACE DE CARBONO CON CARBONO, A y B, QUE PUEDEN SER IGUALES O DIFERENTES, REPRE- SENTAN EN CADA CASO UN GRUPO -CR13=CR14-, -O-, -S-, -N=, =CR15- o -NR16, REPRESENTADO R13 Y R14, QUE PUEDEN SER IGUALES O DIFERENTES, A- TOMOS DE HIDROGENO, FLUOR, CLORO O BROMO, O GRUPOS ALQUILO, HIDROXI, ALCOXI, TRIFLUOROMETILO, ALQUIL- SULFENILO, ALQUILSULFINILO, ALQUILSULFONILO, NI- TRO, AMINO, ALQUILAMINO, DIALQUILAMINO O ALQUIL- CARBONILAMINO, R1 UN ATOMO DE HIDROGENO, UN GRUPO ALQUILO, HIDRO- XI O ALCOXI, Y R16 UN ATOMO DE HIDROGENO, UN GRUPO ALQUILO CON 1 A 6 ATOMOS DE CARBONO O UN GRUPO ARILALQUILO, X1 REPRESENTA UN GRUPO >C= o >N-, X2 y X5, QUE PUEDEN SER IGUALES O DIFERENTES, RE- PRESENTAN EN CADA CASO UN GRUPO -CR17=, -O-, -S-, -N=, -NR18-, -CO- o -(R17CR18)-, REPRESENTANDO R17 UN ATOMO DE HIDROGENO O UN GRUPO ALQUILO, Y R18 UN ATOMO DE HIDROGENO, O UN GRUPO ALQUILO CON 1 A 6 ATOMOS DE CARBONO O UN GRUPO ARILALQUILO, UNO DE LOS RADICALES X3 o X4 REPRESENTA UN GRUPO y3-y2-y1-C< o y3-y2-y1-NCH- ESTA REEMPLA- ZADA POR UN ATOMO DE NITROGENO, PUDIENDO ADEMAS DE ELLO, EN LOS ANILLOS DE 5 A 7 MIEMBROS PRECEDENTE- MENTE MENCIONADOS, EN CADA CASO UN GRUPO METILENO CONTIGUO A UN ATOMO DE NITROGENO ESTAR REEMPLAZADO POR UN GRUPO CARBONILO, O, CUANDO y2 REPRESENTA UN GRUPO AMINO CICLICO, TAMBIEN UN GRUPO CARBONILALQUILENO QUE TIENE EN TOTAL DE 2 A 6 ATOMOS DE CARBONO, ESTANDO UNIDO EL GRUPO CARBONILO EN CADA CASO AL ATOMO DE NITROGENO DEL GRUPO AMINO CICLICO DEL GRUPO y2, y2 REPRESENTA UN ENLACE, UN GRUPO ALQUILENO CON 1 A 6 ATOMOS DE CARBONO, QUE PUEDE ESTAR SUSTITUIDO CON UNO O DOS GRUPOS ALQUILO QUE TIENEN EN CADA CASO DE 1 A 8 ATOMOS DE CARBONO, CON UN GRUPO ALQUENILO O ALQUINILO QUE TIENE EN CADA CASO DE 2 A 4 ATOMOS DE CARBONO, CON UN GRUPO HIDROXI, AMINO, ARILO O HETEROARILO, CON UN GRUPO ALCOXI O ALQUILAMINO QUE TIENE EN CADA CASO DE 1 A 8 ATOMOS DE CARBONO, CON UN DIALQUILA- MINO QUE TIENE EN TOTAL DE 2 A 10 ATOMOS DE CARBO- NO, CON UN GRUPO HNR21- o N-(ALQUIL)-NR21, REPRE- SENTANDO R21 UN GRUPO ALQUILCARBONILO O ALQUILSULFONILO QUE TIENE EN CADA CASO DE 1 A 8 ATOMOS DE CARBONO EN LA PARTE DE ALQUILO, UN GRUPO ALQUILOXICARBONILO QUE TIENE EN TOTAL DE 2 A 5 ATOMOS DE CARBONO, UN GRUPO CICLOALQUILCARBONILO O CICLOALQUILSULFONILO QUE TIENE EN CADA CASO DE 5 A 7 ATOMOS DE CARBONO EN LA PARTE DE CICLOALQUILO, UN GRUPO ARILALQUIL- CARBONILO, ARILALQUILSULFONILO, ARILALCOXICARBONI- LO, ARILCARBONILO O ARILSULFONILO, UN GRUPO ALQUENILENO CON 2 A 6 ATOMOS DE CARBONO, UN GRUPO ARILENO, UN GRUPO PIRIDINILENO, PIRIMIDINILENO, PIRAZINILE- NO O PIRIDAZINILENO, EVENTUALMENTE SUSTITUIDOS CON UNO O DOS GRUPOS ALQUILO, UN GRUPO CICLOALQUILENO CON 5 A 7 ATOMOS DE CARBO- NO, EVENTUALMENTE SUSTITUIDO CON UNO O DOS GRUPOS ALQUILO, EN EL CUAL UNA UNIDAD >CH- ESTA REEMPLA- ZADA POR UN ATOMO DE NITROGENO, QUE ESTA UNIDO CON UN ATOMO DE CARBONO DEL RADICAL y1, UN GRUPO CICLOALQUILENO CON 4 A 7 ATOMOS DE CARBO- NO EN LA PARTE DE CICLOALQUILENO, EVENTUALMENTE SUSTITUIDO CON UNO O DOS GRUPOS ALQUILO QUE TIE- NEN EN CADA CASO DE 1 A 8 ATOMOS DE CARBONO, CON UN GRUPO ALQUENILO O ALQUINILO QUE TIENE EN CADA CASO DE 2 A 4 ATOMOS DE CARBONO, CON UN GRUPO HI- DROXI, AMINO, ARILO O HETEROARILO, CON UN GRUPO ALCOXI O ALQUILAMINO QUE TIENE EN CADA CASO 1 A 8 ATOMOS DE CARBONO, CON UN GRUPO DIALQUILAMINO QUE TIENE EN TOTAL DE 2 A 10 ATOMS DE CARBONO, CON UN GRUPO HNR21 o N-(ALQUIL)-NR21, ESTANDO DEFINIDO R22 IGUAL QUE PRECEDENTEMENTE, O TAMBIEN UN GRUPO ALQUILENO UNIDO CON EL RADICAL y1 A TRAVES DEL RADICAL W, EN EL CUAL W, REPRESEN- TA UN ATOMO DE OXIGENO O DE AZUFRE, UN GRUPO SUL- FINILO, SULFONILO, -NR19, -NR20-CO o -CO-NR20, ES- TANDO DEFINIDOS R19 Y R20 COMO INICIALMENTE Y PU- DIENDO EL GRUPO ALQUILENO ESTAR SUSTITUIDO ADICIO- NALMENTE CON UNO O DOS GRUPOS ALQUILO QUE TIENEN EN CADA CASO DE 1 A 8 ATOMOS DE CARBONO, CON UN GRUPO ALQUENILO O ALQUINILO QUE TIENE DE 2 A 4 A- TOMOS DE CARBONO HIDROXI, AMINO, ARILO O HETEROA- RILO, CON UN GRUPO ALCOXI O ALQUILAMINO QUE TIENEN EN CADA CASO DE 1 A 8 ATOMOS DE CARBONO, CON UN GRUPO DIALQUILAMINO QUE TIENE EN TOTAL DE 2 A 10 ATOMOS DE CARBON, CON UN GRUPO -HNR21 o N-(ALQUIL) -NR21, ESTANDO SEPARADO EL HETEROATOMO DEL SUSTI- TUYENTE ADICIONAL POR AL MENOS 2 ATOMOS DE CARBONO DE UN HETEROATOMO DEL RADICAL W Y ESTANDO DEFINIDO R21 COMO PRECEDENTEMENTE, Y y3 REPRESENTA UN GRUPO CARBONILO, QUE ESTA SUSTI- TUIDO CON UN GRUPO HIDROXI, CON UN GRUPO ALCOXI QUE TIENE DE 1 A 8 ATOMOS DE CARBONO, CON UN GRUPO ARILALCOXI O CON UN GRUPO R22O, REPRESENTANDO R22 UN GRUPO CICLOALQUILO O CICLOALQUILALQUILO QUE TIENEN EN CADA CASO DE 3 A 8 ATOMOS DE CARBONO EN LA PARTE DE CICLOALQUILO, EN LOS CUALES EN CADA CASO EL GRUPO CICLOALQUILO ESTA SUSTITUIDO CON UN GRUPO ALQUILO, ALCOXI O DIALQUILAMINO, CON UN GRU- PO ALQUILOXI QUE TIENE DE 1 HASTA 3 GRUPOS METILO, Y ADICIONALMENTE UN GRUPO METILENO EN UNA PARTE DE CICLOALQUILO DE 4 A 8 ESLABONES PUEDE ESTAR REEM- PLAZADA POR UN ATOMO DE OXIGENO O POR UN GRUPO AL- QUILIMINO, O REPRESENTA UN GRUPO BENZOCICLOALQUILO CON 9 A 12 ATOMOS DE CARBONO O UN GRUPO ARILO, UN GRUPO SULFO, FOSFONO, O-ALQUILFOSFONO, 0,0´-DI- ALQUILFOSFONO, TETRAZOL-5-ILO o R23CO-O-CHR24-O-CO -, REPRESENTANDO R23 UN GRUPO ALQUILO O ALCOXI QUE TIENE EN CADA CASO DE 1 A 8 ATOMOS DE CARBONO, UN GRUPO CICLOAL- QUILO O CICLOALCOXI QUE TIENE EN CADA CASO DE 5 A 7 ATOMOS DE CARBONO EN LA PARTE DE CICLOALQUILO, O UN GRUPO ARILO, ARILOXI, ARILALQUILO o ARILALCOXI, Y R24 UN ATOMO DE HIDROGENO O UN GRUPO ALQUILO, Y EL OTRO DE LOS RADICALES X3 o X4 REPRESENTA UN GRUPO -CR17=, -O-, -S-, -N=, -NR18-, -CO- o (R17CR 18)-, ESTANDO DEFINIDOS R17 y R18 COMO INICIALMEN- TE, CON LA CONDICION DE QUE EL ATOMO QUE SE EN- CUENTRA EN EL ANILLO DE POR LO MENOS UNO DE LOS RADICALES X1 HASTA X5 HA DE SER UN ATOMO DE CARBO- NO, COMO MAXIMO UNO DE LOS RADICALES X1 HASTA X5 RE- PRESENTA UN GRUPO -O-, -S- o -NR18-, Y EN EL CASO DE QUE A o B REPRESENTE UN GRUPO -CR13= CR14, -X1-X2-X3- o -X1-X5-X4- NO HA DE REPRESENTAR NINGUN GRUPO >N-CO-N(y1-y2-y3), Y LA DISTANCIA MAS CORTA ENTRE EL RADICAL y3 Y EL ATOMO DE NITROGENO DE LA PARTE DE AZEPINA HA DE A- SCENDER POR LO MENOS A 11 ENLACES, HABIENDOSE DE ENTENDER, SIEMPRE Y CUANDO NO SE HU- BIERA MENCIONADO OTRA COSA DISTINTA, ENTRE LAS PARTES DE ARILO MENCIONADAS CON OCASION DE LA DE- FINICION DE LOS RADICALES PRECEDENTES, UN GRUPO FENILO, QUE EN CADA CASO PUEDE ESTAR MONOSUSTITUI- DO CON R25, mono-, DI o TRI-SUSTITUIDO CON R26, O MONOSUSTITUIDO CON R25 Y ADICIONALMENTE MONO- O DI-SUSTITUIDO CON R26, PUDIENDO SER LOS SUSTITU- YENTES IGUALES O DIFERENTES, Y REPRESENTANDO R25 UN GRUPO CIANO, CARBOXI, AMINOCARBONILO, AL- QUILAMINOCARBONILO, DIALQUILAMINOCARBONILO, ALCO- XICARBONILO, ALQUILCARBONILO, ALQUILSULFENILO, AL- QUILSULFINILO, ALQUILSULFONILO, ALQUILSULFONILOXI, PERFLUOROALQUILO, PERFLUOROALCOXI, NITRO, AMINO, ALQUILAMINO, DIALQUILAMINO, ALQUICARBONILAMINO, FENILALQUILCARBONILO, FENILCARBONILAMINO, ALQUIL- SULFONILAMINO, FENILSULFONILAMINO, N-ALQUIL- ALQUILCARBONILAMINO, N-ALQUIL-FENILALQUILCARBONI- LAMINO, N-ALQUIL-FENILCARBONILAMINO, N-ALQUIL-AL- QUILSULFONILAMINO, N-ALQUIL-FENILALQUILSULFOLAMI- NO, N-ALQUIL-FENILSULFONILAMINO, AMINOSULFONILO, ALQUILAMINOSULFONILO o DIALQUILAMINO-SULFONILO, Y REPRESENTANDO R26 UN GRUPO ALQUILO, HIDROXI, O ALCOXI, O UN ATO- MO DE FLUOR, CLORO, BROMO O YODO, PUDIENDO DOS RA- DICALES R26, SIEMPRE Y CUANDO QUE ESTOS SE ENCUEN- TREN UNIDOS A ATOMOS DE CARBONO CONTIGUOS, TAMBIEN REPRESENTAR UN GRUPO ALQUILENO CON 3 A 6 ATOMOS DE CARBONO, UN GRUPO 1,3-BUTADIEN-1,4-DILENO O UN GRUPO METILENDIOXI, ENTRE LAS PARTES DE ARILENO MENCIONADAS CON OCA- SION DE LA DEFINICION DE LOS RADICALES PRECEDEN- TES, UN GRUPO FENILENO, QUE EN CADA CASO PUEDE ES- TAR MONOSUSTITUIDO CON R25, MONO- O DI-SUSTITUIDO CON R26 O MONOSUSTITUIDO CON R25 Y ADICIONALMENTE MONOSUSTITUIDO CON R26, PUDIENDO LOS SUSTITUYENTES SER IGUALES O DIFERENTES, Y ESTANDO DEFINIDOS COMO PRECEDENTEMENTE SE MENCIONA, ENTRE LAS PARTES DE HETEROARILO MENCIONADAS CON OCASION DE LA DEFINI- CION DE LOS RADICALES PRECEDENTES, UN ANILLO HETE- ROAROMATICO DE 5 ESLABONES, QUE CONTIENE UN ATOMO DE OXIGENO, AZUFRE O NITROGENO, UN ATOMO DE NITRO- GENO Y UN ATOMO DE OXIGENO, AZUFRE O NITROGENO, O DOS ATOMOS DE NITROGENO Y UN ATOMO DE OXIGENO, A- ZUFRE O NITROGENO, O UN ANILLO HETEROAROMATICO DE 6 ESLABONES, QUE CONTIENE 1, 2 o 3 ATOMOS DE NI- TROGENO Y EN QUE ADICIONALMENTE UNO O DOS GRUPOS -CH=N PUEDEN ESTAR REEMPLAZADOS EN CADA CASO POR UN GRUPO -CO-NR20, ESTANDO DEFINIDO R20 COMO PRE- CEDENTEMENTE SE MENCIONA, Y PUDIENDO ADICIONALMEN- TE LOS ANILLOS HETEROAROMATICOS PRECEDENTEMENTE MENCIONADOS ESTAR SUSTITUIDOS CON UNO O DOS GRUPOS ALQUILO, O EN EL ENTRAMADO DE CARBONOS TAMBIEN CON UN ATOMO DE FLUOR, CLORO, BRO1. CONDENSATED AZEPINE DERIVATIVES OF THE GENERAL FORMULA (I) FIGURE 1 IN WHICH R1 REPRESENTS AN ATOM OF HYDROGEN, A RENTAL GROUP WITH 1 TO 6 ATOMS OF CARBON, A CYCLOALKYL GROUP OF 3 TO 7 ATOMS OF CARBON, AN ALKYL GROUP OR ALKYNYL WHICH HAS IN EACH CASE 3 TO 8 CARBON ATOMS, AN ALKYL GROUP, WHICH IS SUBSTITUTED WITH A HYDROXY, ALCOXI, AMINO, ALKYLAMINO, NOX, CARBOXY, ALCOXICARBONYL, AMINOXYARIN, O HETEROARILO, OR WITH A CYCLOALKYL GROUP WHICH HAS 3 TO 7 CARBON ATOMS, AN AMIDINE GROUP, A CARBONYL GROUP, WHICH IS REPLACED WITH A HYDROGEN ATOM, WITH AN ALKYL GROUP, ALCOI, ALCOX, ALCOX R10 -CO-0- (R11CR12) -O, REPRESENTED R10 A RENT GROUP WITH 1 TO 8 ATOMS OF CARBON, A CYCLOALKYL GROUP WITH 5 TO 7 ATOMS OF CARBON, A GROUP ARYL OR ARYALKYL, R11 A HYDROGEN ATOM, RENT, A CYCLOALKYL GROUP WITH 5 TO 7 ATOMS OF CARBON OU N ARILO GROUP, AND R12 A HYDROGEN ATOM OR A RENT GROUP, R2 UP TO R9, WHICH MAY BE THE SAME OR DIFFERENT, REPRESENT HYDROGEN ATOMS, ALKYL, ARYL OR ARIALKYL GROUP, OR R2 AND R4 IN COMMON AND / OR IN COMMON THEY REPRESENT IN EACH CASE ANOTHER LINK OF CARBON TO CARBON, A AND B, WHICH MAY BE THE SAME OR DIFFERENT, REPRESENT IN EACH CASE A GROUP -CR13 = CR14-, -O-, -S-, -N =, = CR15- or -NR16, REPRESENTED R13 AND R14, WHICH MAY BE THE SAME OR DIFFERENT, A- WE TAKE OF HYDROGEN, FLUORINE, CHLORINE OR BROMO, OR GROUPS ALKYL, HYDROXY, ALCOXY, ALIFYL, SULPHYL, SULPHYL - TRO, AMINO, ALQUILAMINO, DIALQUILAMINO OR ALQUIL- CARBONILAMINO, R1 AN ATOM OF HYDROGEN, A GROUP ALKYL, HYDROXI OR ALCOXI, AND R16 AN ATOM OF HYDROGEN, A RENT A 1 TO 6O ATOMO , X1 REPRESENTS A GROUP> C = o> N-, X2 and X5, WHICH MAY BE THE SAME OR DIFFERENT, REPRESENT IN EACH CASE A GROUP -CR17 =, -O-, -S-, -N =, -NR18 -, -CO- or - (R17CR18) -, R17 REPRESENTING A HYDROGEN ATOM OR A RENT GROUP, AND R18 A HYDROGEN ATOM, OR A RENT GROUP WITH 1 TO 6 CARBON ATOMS OR AN ARYALKYL GROUP, ONE OF THE X3 OR X4 RADICALS GROUP y3-y2-y1-C <o y3-y2-y1-NCH- IS REPLACED BY AN ATOM OF NITROGEN, IN ADDITION TO IT, IN THE RINGS OF 5 TO 7 PRECEDENT MEMBERS- IN EACH CASE A GRUPO METTILENO CONTIGUO A ATOMO DE NITROGENO TO BE REPLACED BY A CARBONILO GROUP, OR, WHEN y2 REPRESENTS A CYCLE AMINO GROUP, ALSO A TOTAL OF 2 TO 6 CARBON-CARBON-CARBON-CARBON ATOMOS, NITROGEN ATOM OF THE AMINO CYCLE GROUP OF GROUP y2, y2 REPRESENTS A LINK, AN ALKYLENE GROUP WITH 1 TO 6 ATOMS OF CARBON, WHICH MAY BE REPLACED WITH ONE OR TWO RENT GROUPS THAT HAVE IN EACH CASE 1 TO 8 ATOMS OF WITH AN ALKYLL OR ALKYNIL GROUP THAT HAS IN EACH CASE OF 2 TO 4 CARBON ATOMS, WITH A HYDROXY, AMINO, ARYL OR HETEROARYL GROUP, WITH AN ALCOXI OR ALKYLAMINE GROUP THAT HAS IN EACH CASE 1 TO 8 CARBON ATOMS, WITH A DIALKYL- MINUS THAT HAS TOTAL 2 TO 10 CARBON ATOMS, WITH A GROUP HNR21- or N- (ALKYL) -NR21, REPRE- LAYING R21 AN ALKYL CARBONYL OR ALKYL SULPHONYL GROUP THAT HAS IN EACH CASE 1 TO 8 CARBON ATOMS IN THE PART OF ALKYL, A 2-ALKYLOXICARBENE TILE WHICH ATOMOS DE CARBONO, A GROUP CICLOALQUILCARBONILO OR CICLOALQUILSULFONILO THAT HAS IN EACH CASE 5 TO 7 ATOMOS DE CARBONO IN THE PART OF CICLOALQUILO, A GROUP ARILALILIL-CARBONILO, ARILALQUILSULFONILO ATOMOS DE CARBONO, A GROUP ARILENO, A GROUP PIRIDINILENO, PIRIMIDINILENO, PIRAZINILE- NO OR PIRIDAZINILENO, EVENTUALLY SUBSTITUTED WITH ONE OR TWO GROUPS ALQUILO, SOME ONE WITH SOME 5 TO 7 OURS, WITH A 5-TO-7-YEAR ASSUMPTION, 5-TO-7 , IN WHICH A UNIT> CH- IS REPLACED BY A NITROGEN ATOM, WHICH IS UNITED WITH A RADICAL CARBON ATOM AND 1, A CYCLOALKYLENE GROUP WITH 4 TO 7 CARBON ATOMS, EVENTUALLY SUBSTITUTED WITH ONE OR TWO RENT GROUPS THAT HAVE IN EACH CASE FROM 1 TO 8 CARBON ATOMS, WITH AN ALKENYL OR ALKYNIL GROUP THAT HAS IN EACH CASE FROM 2 TO 4 CARBON ATOMS, WITH A HYDROXY, AMINO, ARYL GROUP OR HETEROARILO, WITH A GROUP ALCOXI OR ALKYLAMINE THAT HAS IN EACH CASE 1 TO 8 ATOMS OF CARBON, WITH A GROUP DIALKYLAMINE THAT HAS A TOTAL OF 2 TO 10 ATOMS OF CARBON, WITH A GROUP HNR21 or N- (ALKYL) -NR21, R22 BEING DEFINED AS PREVIOUSLY, OR ALSO A RENTAL GROUP UNITED WITH THE RADICAL AND 1 THROUGH THE RADICAL W, IN WHICH W, REPRESENTS AN ATOME OF OXYGEN OR SULFUR, A GROUP SULFIN, SULPHONYL, -NR19 -NR20-CO or -CO-NR20, BEING DEFINED R19 AND R20 AS INITIALLY AND MAY- THE ALKYLENE GROUP BE REPLACED ADIC IO- NALLY WITH ONE OR TWO ALKYL GROUPS THAT HAVE IN EACH CASE 1 TO 8 ATOMS OF CARBON, WITH A GROUP OF ALKYNILE OR ALKYNYL WHICH HAS 2 TO 4 A- WE TAKE CARBON HYDROXY, AMINO, ARYL OR HETEROARILE, WITH A GROUP ALCOXI OR ALKYLAMINE THAT HAVE IN EACH CASE 1 TO 8 ATOMS OF CARBON, WITH A DIALKYLAMINE GROUP THAT HAS IN TOTAL 2 TO 10 ATOMS OF CARBON, WITH A GROUP -HNR21 or N- (ALKYL) -NR21, BEING SEPARATED THE ADDITIONAL SUBSTITUTE HETEROATOMO FOR AT LEAST 2 CARBON ATOMS OF A RADICAL WY HETEROATOM BEING DEFINED R21 AS PREVIOUSLY, AND y3 REPRESENTS A CARBONYL GROUP, WHICH IS SUSTAINED WITH A HYDROXI GROUP, WITH ONE GROUP TO IT 1 TO 8 CARBON ATOMS, WITH AN ARILALCOXI GROUP OR WITH A R22O GROUP, R22 REPRESENTING A CYCLOALKYL OR CYCLOALKYLALKYL GROUP WHICH HAVE IN EACH CASE 3 TO 8 CARBON ATOMS IN THE PART OF CICLOALQUILO, IN THE CASE OF CICLOALQUILO IN THE CASE CICLOALQUILO IS REPLACED WITH A GROUP ALQUILO, ALCOXI OR DI ALKYLAMINE, WITH A GROUP OF ALKYLOXI THAT HAS FROM 1 TO 3 METHYL GROUPS, AND ADDITIONALLY A METHYLENE GROUP IN A PART OF CYCLOALKYL OF 4 TO 8 LINKS MAY BE REPLACED BY AN OXYGEN ATOM, OR BY A GROUP. OR REPRESENTS A BENZOCICLOALKYL GROUP WITH 9 TO 12 CARBON ATOMS OR AN ARYL GROUP, A SULFO GROUP, PHOSPHONE, O-ALKYLPHOSPHONE, 0,0´-DI-ALKYL PHOSPHONE, TETRAZOL-5-ILO or R23CO-O-CHR24 CO -, R23 REPRESENTING AN ALKYL OR ALCOXY GROUP THAT HAS IN EACH CASE 1 TO 8 ATOMS OF CARBON, A CICLOAL- QUILO OR CICLOALCOXY GROUP THAT HAS IN EACH CASE 5 TO 7 ATOMS OF CARBON IN THE PART OF CYCLOALKYL, OR GRUPO ARILO, ARILOXI, ARILALQUILO o ARILALCOXI, AND R24 ONE HYDROGEN ATOM OR ONE ALKYL GROUP, AND THE OTHER OF THE RADICALS X3 or X4 REPRESENTS A GROUP -CR17 =, -O-, -S =, -NR18 -, -CO- or (R17CR 18) -, R17 and R18 BEING DEFINED AS INITIAL, WITH THE CONDITION THAT THE ATOM THAT IS IN THE RING OF AT LEAST ONE OF THE RADICALE S X1 UP TO X5 MUST BE AN ATOM OF CARBON, AT LEAST ONE OF THE RADICALS X1 UP TO X5 REPRESENTS A GROUP -O-, -S- or -NR18-, AND IN THE CASE THAT A OR B REPRESENTS A GROUP -CR13 = CR14, -X1-X2-X3- or -X1-X5-X4- MUST NOT REPRESENT ANY GROUP> N-CO-N (y1-y2-y3), AND THE SHORTEST DISTANCE BETWEEN THE RADICAL y3 AND THE NITROGEN ATOM OF THE PART OF AZEPINA MUST ACCESS AT LEAST 11 LINKS, HAVING BEEN UNDERSTANDING, ALWAYS AND WHEN NOTHING OTHER THAN MENTIONED, WERE MENTIONED DEFINITION OF THE PREVIOUS RADICALS, A PHENYLUS GROUP, WHICH IN EACH CASE MAY BE MONOSUSTITUTED WITH R25, mono-, DI or TRI-SUBSTITUTED WITH R26, OR MONOSUSTITUTED WITH R25 AND ADDITIONALLY MONO- OR DI-SUBSTITUTED WITH R26, THE SUBSTITUTION folken MAY BE DIFFERENT OR THE SAME, AND REPRESENTING A GROUP R25 cyano, carboxy, aminocarbonyl, AL- QUILAMINOCARBONILO, dialkylaminocarbonyl, alco XICARBONILO, alkylcarbonyl, alkylsulfenyl, AL- QUILSU LFINILO, alkylsulfonyl, alkylsulfonyloxy, perfluoroalkyl, perfluoroalkoxy, nitro, amino, alkylamino, dialkylamino, ALQUICARBONILAMINO, phenylalkylcarbonyl, phenylcarbonylamino, alkyl- sulfonylamino, phenylsulfonylamino, N-alkyl- alkylcarbonylamino, N-alkyl-FENILALQUILCARBONI- LAMINO, N-alkyl-phenylcarbonylamino, N-ALQUIL-AL- QUILSULFONILAMINO, N-ALQUIL-FENILALQUILSULFOLAMI- NO, N-ALQUIL-FENILSULFONILAMINO, AMINOSULFONILO, OR DIALQUILAMINO-SULFONILO, AND REPRESENTING AROUXYRON CHLORINE, BROMINE OR IODINE, BEING ABLE TWO ROADS R26, ALWAYS AND WHEN THESE ARE FOUND TOGETHER OF CONTAINED CARBON, ALSO REPRESENT A RENTING GROUP WITH 3 TO 6 CARBON ATOMS, A GROUP 1.3-B 1,4-DILENE OR A METHYLENDIOXI GROUP, AMONG THE PARTS OF ARYLENE MENTIONED WITH OCCASION OF THE DEFINITION OF THE PREVIOUS RADICALS, A PHENYLENE GROUP, WHICH IN EACH CASE MAY BE MONOSUSTITUTED WITH R25, M ONO- OR DI-SUBSTITUTED WITH R26 OR SINGLE-SUBSTITUTED WITH R25 AND ADDITIONALLY SINGLE-SUBSTITUTED WITH R26, THE SUBSTITUTES MAY BE THE SAME OR DIFFERENT, AND ARE DEFINED AS PRECEDENTLY MENTIONED BY THE RADIO-LISTED PARTIES WITH OCASI PRECEDENTS, A 5-HETE ROAROMATIC RING, CONTAINING AN OXYGEN, SULFUR OR NITROGEN ATOM, A NITROGEN ATOM AND AN OXYGEN OR NITROGEN ATOM, OR TWO NITROGEN AND NITROGEN ATOMES. - SULFUR OR NITROGEN, OR A HETEROAROMATIC RING OF 6 LINKS, CONTAINING 1, 2 or 3 ATOMS OF NITROGEN AND IN WHICH ADDITIONALLY ONE OR TWO GROUPS -CH = N MAY BE REPLACED IN EACH CASE BY A GROUP -CO-NR20 , R20 BEING DEFINED AS PREVIOUSLY MENTIONED, AND BEING ADDITIONALLY ABLE FOR THE PRECEDENTLY MENTIONED HETEROAROMATIC RINGS TO BE REPLACED WITH ONE OR TWO RENT GROUPS, OR IN THE CARBON INLET, WITH A FLUID ATOMOR OR

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