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AR070812A1 - Derivados de 1- bencil-3- hidroximetilindazol y su utilizacion en el tratamiento de enfermedades basadas en la expresion de mcp-1, cx3cr1 y p40 - Google Patents

Derivados de 1- bencil-3- hidroximetilindazol y su utilizacion en el tratamiento de enfermedades basadas en la expresion de mcp-1, cx3cr1 y p40

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Publication number
AR070812A1
AR070812A1 ARP090100802A ARP090100802A AR070812A1 AR 070812 A1 AR070812 A1 AR 070812A1 AR P090100802 A ARP090100802 A AR P090100802A AR P090100802 A ARP090100802 A AR P090100802A AR 070812 A1 AR070812 A1 AR 070812A1
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AR
Argentina
Prior art keywords
group
hydrogen
different
alkyl
forms
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Application number
ARP090100802A
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English (en)
Inventor
Giorgina Mangano
Angelo Guglielmotti
Guido Furlotti
Nicola Cazzolla
Original Assignee
Acraf
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Publication of AR070812A1 publication Critical patent/AR070812A1/es

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    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Pulmonology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
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Abstract

La presente se refiere a derivados de 1-bencil-3-hidroximetilindazol, y a una composicion farmacéutica que los comprende, junto con un vehículo farmacéuticamente aceptable. Además, la presente se refiere a la utilizacion de derivados de 1-bencil-3-hidroximetilindazol para la preparacion de una composicion farmacéutica que es activa en el tratamiento de enfermedades basadas en la expresion de MCP-1, CX3CR1 y p40, y a su utilizacion en un método para tratar o prevenir enfermedades basadas en la expresion de MCP-1, CX3CR1 y p40. Reivindicacion 1: Compuesto de formula (1) en la que: A puede ser un enlace ?, -X1- o -X1-O-X2-, en los que X1 y X2, que pueden ser idénticos o diferentes entre sí, pueden ser un grupo alquilo C1-5, opcionalmente sustituido con uno o más grupos alquilo C1-5 o uno o más grupos alcoxi C1-3, Y es H cuando A es un enlace ?, o Y puede ser H, -OH, o -N(R11)(R12) cuando A es -X1- o -X1-O-X2-, en los que R11 puede ser hidrogeno, un grupo alquilo C1-5, o R11 junto con R12 forma un heterociclo de 4 a 7miembros, R12 puede ser hidrogeno, alquilo C1-5, o R12 junto con R11 forma un heterociclo de 4 a 7miembros, R1 y R2, que pueden ser idénticos o diferentes entre sí, pueden ser hidrogeno, un grupo alquilo C1-5, R3, R4 y R8, que pueden ser idénticos o diferentes entre sí, pueden ser hidrogeno, alquilo C1-5, alcoxi C1-3, un átomo de halogeno, -OH, -N(R')(Rö), -N(R')CORö, -CN, -CONR'Rö, -SO2NR'Rö, -SO2R', nitro y trifluorometilo; con R' y Rö, que pueden ser idénticos o diferentes entre sí, representados por hidrogeno y un alquilo C1-5, R5 puede ser hidrogeno, alquilo C1-5, alcoxi C1-3, un átomo de halogeno, -OH, -N(R')(Rö), -N(R')CORö, nitro y trifluorometilo, o R5 junto con uno de entre R6 y R7 forma un anillo que presenta 5 o 6 átomos de carbono; con R' y Rö, que pueden ser idénticos o diferentes entre sí, representados por H y alquilo C1-5, R6 y R7, que pueden ser idénticos o diferentes entre sí, pueden ser hidrogeno, un grupo alquilo C1-5 o formar conjuntamente un grupo C=O, o uno de entre R6 y R7, junto con R5, forma un anillo que presenta 5 o 6 átomos de carbono, con la condicion de que cuando A sea un enlace ?, e Y, R1, R2, R6, y R7 sean átomos de hidrogeno, si R8 es un átomo de hidrogeno, entonces el grupo enlazado al átomo de nitrogeno en la posicion 1 del anillo de indazol es diferente de un grupo bencilo, un grupo 4-clorobencilo, o un grupo 2,4-diclorobencilo, si R8 es un átomo de fluor en la posicion 5 del anillo de indazol, entonces el grupo enlazado al átomo de nitrogeno en la posicion 1 del anillo de indazol es diferente de un grupo 5-cloro-2-metoxibencilo, y si R8 es un grupo trifluorometilo en la posicion 6 del anillo de indazol, entonces el grupo enlazado al átomo de nitrogeno en la posicion 1 del anillo de indazol es diferente de un grupo 2,4-diclorobencilo.
ARP090100802A 2008-03-07 2009-03-06 Derivados de 1- bencil-3- hidroximetilindazol y su utilizacion en el tratamiento de enfermedades basadas en la expresion de mcp-1, cx3cr1 y p40 AR070812A1 (es)

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AR070812A1 true AR070812A1 (es) 2010-05-05

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US (2) US8461194B2 (es)
EP (1) EP2262778B8 (es)
JP (1) JP5509100B2 (es)
KR (1) KR101640844B1 (es)
CN (1) CN101965337B (es)
AR (1) AR070812A1 (es)
AU (1) AU2009221087B2 (es)
BR (1) BRPI0907974A2 (es)
CA (1) CA2714436C (es)
CY (1) CY1122349T1 (es)
DK (1) DK2262778T5 (es)
EA (1) EA018976B1 (es)
ES (1) ES2753149T3 (es)
GE (1) GEP20135927B (es)
HR (1) HRP20191953T8 (es)
HU (1) HUE047318T2 (es)
IL (1) IL207277A (es)
LT (1) LT2262778T (es)
MX (1) MX2010009625A (es)
PL (1) PL2262778T3 (es)
PT (1) PT2262778T (es)
SG (1) SG188178A1 (es)
SI (1) SI2262778T1 (es)
UA (1) UA103609C2 (es)
WO (1) WO2009109616A2 (es)

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CA2715065C (en) * 2008-03-07 2017-06-27 Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. Novel 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression mcp-1 and cx3cr1
EA018976B1 (ru) * 2008-03-07 2013-12-30 Ацьенде Кимике Рьюните Анджелини Франческо А.К.Р.А.Ф. С.П.А. Производные 1-бензил-3-гидроксиметилиндазола и их применение для лечения заболеваний, основанных на экспрессии мср-1, cx3cr1 и p40
ES2620960T3 (es) * 2009-06-16 2017-06-30 Curna, Inc. Tratamiento de enfermedades relacionadas con un gen de colágeno mediante la inhibición de un transcrito antisentido natural a un gen de colágeno
GEP20135878B (en) * 2009-08-03 2013-07-10 Aziende Chimiche Riunite Angelini Francesco A C R A F S P A It Method of 1-benzyl-3-hydroxymethyl-1h-indazole preparation, derivatives thereof, and required magnesium intermediates
UA108742C2 (uk) 2009-09-23 2015-06-10 Фармацевтична композиція для лікування запальних захворювань, опосередкованих mcp-1

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