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AR043832A1 - Compuestos de carbonilo y proceso de preparacion de los mismos - Google Patents

Compuestos de carbonilo y proceso de preparacion de los mismos

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Publication number
AR043832A1
AR043832A1 ARP040101114A ARP040101114A AR043832A1 AR 043832 A1 AR043832 A1 AR 043832A1 AR P040101114 A ARP040101114 A AR P040101114A AR P040101114 A ARP040101114 A AR P040101114A AR 043832 A1 AR043832 A1 AR 043832A1
Authority
AR
Argentina
Prior art keywords
atoms
hal
coor3
het
monosubstituted
Prior art date
Application number
ARP040101114A
Other languages
English (en)
Inventor
Tsaklakidis Christos Dr
Dipl Chem Dorsch Dieter Dr
Mederski Werner Dr
Cezanne Bertram Dr
Gleitz Johannes Dr
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33135449&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR043832(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from DE10315377A external-priority patent/DE10315377A1/de
Priority claimed from DE2003129295 external-priority patent/DE10329295A1/de
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR043832A1 publication Critical patent/AR043832A1/es

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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D413/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D207/2632-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
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    • C07D211/72Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Los compuestos de la fórmula (1) en donde R1 y R2 son cada uno, de modo independiente entre si, H, =O, Hal, A, etinilo, OR3, N(R3)2, NO2, CN, N3, COOR3, CON(R3)2, -[C(R4)2]n-Ar, -[C(R4)2]n-Het, -[C(R4)2]n-cicloalquilo, -OCOR3, -OCON(R3)2, NR3COA o NR3SO2A; R1 y R2 son juntos, de modo alternativo, un anillo carbocíclico o heterocíclico de 3 a 7 miembros unido de forma bicíclica o espirocíclica que tiene de 0 a 3 átomos de N, O y/o S, R3 es H, A. H-C:::C-CH2-, -CH3-C:::C-CH2-, -CH2-CH(OH)-CH2OH, -CH2-CH(OH)-CH2NH2, -CH2-CH(OH)-CH2Het´, -[C(R4)2]n-Ar´, -[C(R4)2]n-Het´, -[C(R4)2]n-cicloalquilo, -[C(R4)2]n-COOA o, -[C(R4)2]n-N(R4)2; R4 es H o A; W es N, CR3 o un átomo de C hibridado en sp2; E es, junto con W un anillo carbocíclico o heterocíclico saturado de 3 a 7 miembros que tiene de 0 a 3 átomos de N, de 0 a 2 átomos de O y/o de 0 a 2 átomos de S; el cual puede contener un doble enlace, D es un anillo carbocíclico o heterocíclico monocíclico o bicíclico aromático que tiene de 0 a 4 átomos de N, O y/o S que está insustituido o monosustituido o polisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3 o CON(R3)2; G es -[C(R4)2]n-, -[C(R4)2]n-NR3-, -[C(R4)2]n-O-, -[C(R4)2]n-S- o [C(R4)=C(R4)]n-, X es -[C(R4)2]n-CONR3-[C(R4)2]n-, -[C(R4)2]n-NR3CO[C(R4)2]n-, -[C(R4)2]n-NR3[C(R4)2]n-, -[C(R4)2]n-O [C(R4)2]n-,-[C(R4)2]n CO [C(R4)2]n-, o [C(R4)2]nCOO [C(R4)2]n-, Y es alquileno, cicloalquileno, Het-diilo o Ar-diilo, T es un anillo carbocíclico o heterocíclico monocíclico o bicíclico, saturado o insaturado que tiene de 0 a 4 átomos de N, O y/o S que está monosustituido o disustituido con =O, =S, =NR3, =N-CN, =N-NO2, =NOR3, =NCOR3, =NCOOR3 o =NOCOR3 y además puede estar monosustituido, disustituido o trisustituido con R3, Hal, A, -[C(R4)2]n-Ar, -[C(R4)2]n-Het, -[C(R4)2]n-cicloalquilo, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2NR3 y/o S(O)nA; A es alquilo lineal o ramificado que tiene 1-10 átomos de C, en el cual uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH- y/o además, 1-7 átomos de H pueden estar reemplazados por F; Ar es fenilo, naftilo o bifenilo, cada uno de los cuales está insustituido o monosustituido, disustituido o trisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)nA; -[C(R4)2]n-COOR3 u -O[C(R4)2]o-COOR3, Ar´ es fenilo, naftilo o bifenilo, cada uno de los cuales está insustituido o monosustituido, disustituido o trisustituido con Hal, A, OR4, N(R4)2, NO2, CN, COOR4, CON(R4)2, NR4COA, NR4CON(R4)2, NR4SO2A, COR4, SO2N(R4)2, S(O)nA; -[C(R4)2]n-COOR4 u -O[C(R4)2]o-COOR4; Het es un anillo heterocíclico monocíclico o bicíclico, saturado, insaturado o aromático que tiene de 1 a 4 átomos de N, O y/o S que puede estar insustituido o monosustituido, disustituido o trisustituido con Hal, A, -[C(R4)2]n-Ar, -[C(R4)2]n-Het´, -[C(R4)2]n-cicloalquilo, OR3, N(R3)2, NR3CON(R3)2, NO2, CN, -[C(R4)2]n-COOR3, -[C(R4)2]n-CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3, S(O)mA y/u O del carbonilo; Het´ es un anillo heterocíclico monocíclico o bicíclico, saturado, insaturado o aromático que tiene de 1 a 4 átomos de N, O y/o S que puede estar insustituido o monosustituido o disustituido con el O del carbonilo, =S., =N(R4)2, Hal, A, OR4, N(R4)2, NO2, CN, COOR4, CON(R4)2, NR4COA, NR4CON(R4)2, NR4SO2A, COR4, SO2NR4 y/o S(O)nA, Hal es F, Cl, Br o I, n es 0, 1 o 2; o es 1, 2 o 3; y sus derivados, solvatos, sales y estereoisómeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores del factor de coagulación Xa y pueden emplearse para la profilaxis y/o la terapia de enfermedades tromboembólicas y para el tratamiento de tumores.
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