AR036102A1 - Derivados diaminicos. - Google Patents

Derivados diaminicos.

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Publication number
AR036102A1
AR036102A1 ARP020102322A ARP020102322A AR036102A1 AR 036102 A1 AR036102 A1 AR 036102A1 AR P020102322 A ARP020102322 A AR P020102322A AR P020102322 A ARP020102322 A AR P020102322A AR 036102 A1 AR036102 A1 AR 036102A1
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AR
Argentina
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group
substituted
alkyl
saturated
unsaturated
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Daiichi Seiyaku Co
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Publication of AR036102A1 publication Critical patent/AR036102A1/es

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    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Un compuesto representado por la fórmula general (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4 donde: R1 y R2, independientemente el uno del otro, representan un átomo de hidrógeno, un grupo hidroxilo, un grupo alquilo o un grupo alcoxi; Q1 representa un grupo hidrocarburo cíclico de 5 ó 6 miembros saturado o no saturado que puede estar sustituido, un grupo heterocíclico de 5 a 7 miembros saturado o no saturado que puede estar sustituido, un grupo hidrocarburo bicíclico o tricíclico fusionado saturado o no saturado que puede estar sustituido o un grupo heterocíclico bicíclico o tricíclico fusionado saturado o no saturado que puede estar sustituido; Q2 representa un enlace simple, un grupo hidrocarburo cíclico bivalente de 5 ó 6 miembros saturado o no saturado que puede estar sustituido, un grupo heterocíclico bivalente de 5 a 7 miembros saturado o no saturado que puede estar sustituido, un grupo hidrocarburo bicíclico o tricíclico fusionado bivalente saturado o no saturado que puede estar sustituido o un grupo heterocíclico bicíclico o tricíclico fusionado bivalente saturado o no saturado que puede estar sustituido; Q3 representa el grupo de fórmula (2) en el que Q5 significa un grupo alquileno C1-8, un grupo alquenileno C2-8, o un grupo -(CH2)m-CH2-A-CH2-(CH2)n-, en el que m y n, independientemente el uno del otro, son 0 ó un número entero de 1-3 y A significa un átomo de oxígeno, un átomo de nitrógeno, un átomo de azufre, -SO-, -SO2-, -NH-, -O-NH, -NH-NH-, -S-NH-, -SO-NH- ó -SO2-NH-, y R3 y R4 son sustituyentes en átomo(s) de carbono, átomo(s) de nitrógeno o un átomo de azufre de un anillo que comprende Q5 e independientemente el uno del otro, son un átomo de hidrógeno, un grupo hidroxilo, un grupo alquilo, un grupo alquenilo, un grupo alquinilo un átomo de halógeno, un grupo halógenoalquilo, un grupo ciano, un grupo cianoalquilo, un grupo amino, un grupo aminoalquilo, un grupo N-alquilaminoalquilo, un grupo N,N-dialquilaminoalquilo, un grupo acilo, un grupo acilalquilo, un grupo acilamino que puede estar sustituido, un grupo alcoximino, un grupo hidroximino, un grupo acilaminoalquilo, un grupo alcoxi, un grupo alcoxialquilo, un grupo hidroxialquilo, un grupo carboxilo, un grupo carboxialquilo, un grupo alcoxicarbonilo, un grupo alcoxicarbonilalquilo, un grupo alcoxicarbonilalquilamino, un grupo carboxialquilamino, un grupo alcoxicarbonilamino, un grupo alcoxicarbonilaminoalquilo, un grupo carbamoílo, un grupo N-alquilcarbamoílo que puede tener un sustituyente en el grupo alquilo, un grupo N,N-dialquilcarbamoílo que puede tener un sustituyente en los grupos alquilo, un grupo N-alquenilcarbamoílo, N-alquiltiocarbamoílo, N,N-dialquiltiocarbamoílo, N-alqueniltiocarbamoílo, un grupo N-alquenilcarbamoílalquilo, un grupo N-alquenil-N-alquilcarbamoílo, un grupo N-alquenil-N-alquilcarbamoílalquilo, un grupo N-alcoxicarbamoílo, un grupo N-alquil-N-alcoxicarbamaoílo, un grupo N-alcoxicarbamoílalquilo, un grupo N-alquil-N-alcoxicarbamoílalquilo, un grupo carbazoílo que puede estar sustituido por 1 a 3 grupos alquilo, un grupo alquilsulfonilo, un grupo alquilsulfonilalquilo, un grupo carbonilo heterocíclico de 3 a 6 miembros que puede estar sustituido, un grupo carbamoílalquilo, un grupo N-alquilcarbamoílalquilo, que puede tener un sustituyentes en el grupo alquilo, un grupo N,N-dialquilcarbamoílalquilo que puede tener un sustituyente en el (los) grupo(s) alquilo, un grupo carbamoíloxialquilo, un grupo N-alquilcarbamoíloxialquilo, un grupo N,N-dialquilcarbamoíloxialquilo, un grupo carbonilalquilo heterocíclico de 3 a 6 miembros que puede estar sustituido, un grupo carboniloxialquilo heterocíclico de 3 a 6 miembros que puede estar sustituido, un grupo arilo, un grupo aralquilo, un grupo heteroarilo, un grupo heteroarilalquilo, un grupo alquilsulfonilamino, un grupo arilsulfonilamino, un grupo alquilsulfonilaminoalquilo, un grupo arilsulfonilaminoalquilo, un grupo alquilsulfonilaminocarbonilo, un grupo arilsulfonilaminocarbonilo, un grupo alquilsulfonilaminocarbonilalquilo, un grupo arilsulfonilaminocarbonilalquilo, un grupo oxo, un grupo carbamoíloxi, un grupo aralquiloxi, un grupo carboxialquiloxi, un grupo aciloxi, un grupo aciloxialquilo, un grupo arilsulfonilo, un grupo alcoxicarbonilalquilsulfonilo, un grupo carboxialquilsulfonilo, un grupo alcoxicarbonilacilo, un grupo alcoxialquiloxicarbonilo, un grupo hidroxiacilo, un grupo alcoxiacilo, un grupo alcoxitioacilo, un grupo halógenoacilo, un grupo carboxiacilo, un grupo aminoacilo, un grupo aciloxiacilo, un grupo aciloxialquilsulfonilo, un grupo hidroxialquilsulfonilo, un grupo alquiloxialquilsulfonilo, un grupo sulfonilo heterocíclico de 3 a 6 miembros que puede estar sustituido, un grupo N-alquilaminoacilo, un grupo N,N-dialquilaminoacilo, un grupo N,N-dialquilcarbamoílacilo que puede tener un sustituyente en el (los) grupo(s) alquilo, un grupo N,N-dialquilcarbamoílalquilsulfonilo que puede tener un sustituyente en el (los) grupo(s) alquilo o un grupo alquilsulfonilacilo; o R3 y R4 juntos el uno con el otro simbolizan un grupo alquileno C1-5, un grupo alquenileno C2-5, un grupo alquilendioxi C1-5 o un grupo carbonildioxi; Q4 representa un grupo arilo que puede estar sustituido, un grupo arilalquenilo que puede estar sustituido, un grupo arilalquinilo que puede estar sustituido, un grupo heteroarilo que puede estar sustituido, un grupo heteroarilalquenilo que puede estar sustituido, un grupo hidrocarburo bicíclico o tricíclico fusionado saturado o no saturado que puede estar sustituido, o un grupo heterocíclico bicíclico o tricíclico fusionado saturado o no saturado que puede estar sustituido; T0 representa un grupo carbonilo o tiocarbonilo; y T1 representa un grupo carbonilo, un grupo sulfonilo, un grupo -C(=O)-C(=O)-N(R')-, un grupo -C(=S)-C(=O)-N(R')-, un grupo C(=O)-C(=S)-N(R')-, un grupo -C(=S)-C(=S)-NR'-, en los cuales R' significa un átomo de hidrógeno, un grupo hidroxilo, un grupo alquilo o un grupo alcoxi, el grupo -C(=O)-A1-N(R'')-, en el que A1 simboliza un grupo alquileno C1-5 que pueden estar sustituido y R'' significa un átomo de hidrógeno, un grupo hidroxilo, un grupo alquilo o un grupo alcoxi, un grupo -C(=O)-NH-, un grupo -C(=S)-NH-, un grupo -C(=O)-NH-NH-, un grupo -C(=O)-A2-C(=O)-, en el que A2 significa un enlace simple o un grupo alquileno C1-5, un grupo -C(=O)-A3-C(=O)-NH, en el que A3 simboliza un grupo alquileno C1-5, un grupo -C(=O)-C(=NORa)-N(Rb)-, un grupo -C(=S)-C(=NORa)-N(Rb)-, un grupo -C(=NORa)-C(=O)-N(Rb)-, un grupo -C(=NORa)-C(=S)-N(Rb)-, en el que Ra significa un átomo de hidrógeno, un grupo alquilo o un grupo alcanoílo, y Rb simboliza un átomo de hidrógeno, un grupo hidroxilo, un grupo alquilo o un grupo alcoxi, el grupo -C(=O)-N=N-, el grupo -C(=S)-N=N- o un grupo tiocarbonilo; una sal de éste, un solvato de éste o un N-óxido de éste. Un medicamento, un inhibidor del factor X de coagulación sanguínea activado, un anticoagulante, un agente para prevenir y/o tratar trombosis o embolia y una composición medicinal, que comprenden el compuesto de fórmula (1), su sal, solvato o el N-óxido. Uso del compuesto de fórmula (1), su sal, solvato o el N-óxido para la preparación de un medicamento. Intermediarios para su preparación. El compuesto de fórmula (1) es útil como agente para prevenir y/o tratar infarto cerebral, embolia cerebral, infarto de miocardio, angina de pecho, infarto pulmonar, embolia pulmonar, enfermedad de Buerger, trombosis venosa profunda, síndrome de coagulación intravascular diseminada, formación de trombos después del reemplazo de válvula o de junta, formación de trombos y re-oclusión después de la angioplastía, síndrome de reacción inflamatoria sistemática (SIRS), síndrome de enfermedad de órganos múltiples (MODS), formación de trombos durante la circulación extracorporal o coagulación de sangre en la recolección de sangre.
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