AR080803A1 - Derivados de 3,4-dihidro-1h-benzo[b][1,6]naftiridina, composiciones farmaceuticas que los contiene, procedimiento para prepararlos e intermediarios del mismo, y uso de los compuestos en el tratamiento de canceres y enfermedades autoinmunes e inflamatorias. - Google Patents

Derivados de 3,4-dihidro-1h-benzo[b][1,6]naftiridina, composiciones farmaceuticas que los contiene, procedimiento para prepararlos e intermediarios del mismo, y uso de los compuestos en el tratamiento de canceres y enfermedades autoinmunes e inflamatorias.

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Publication number
AR080803A1
AR080803A1 ARP110100979A ARP110100979A AR080803A1 AR 080803 A1 AR080803 A1 AR 080803A1 AR P110100979 A ARP110100979 A AR P110100979A AR P110100979 A ARP110100979 A AR P110100979A AR 080803 A1 AR080803 A1 AR 080803A1
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AR
Argentina
Prior art keywords
nrr
mono
polysubstituted
independently
phenyl
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Application number
ARP110100979A
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English (en)
Inventor
Staehle Wolfgang Dr
Schultz Melanie Dr
Schiemann Kai Dr
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Merck Patent Gmbh
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Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR080803A1 publication Critical patent/AR080803A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
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  • Hematology (AREA)
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Abstract

Reivindicacion 1: Compuestos de la formula (1) en donde D es Ar o Het, Ar es fenilo, indanilo, naftilo o bifenilo no sustituido o mono- o polisustituido, pero en donde se excluye opcional y preferentemente el fenilo no sustituido, Het es un heterociclo saturado, parcialmente insaturado o aromático mono- o bicíclico con 1, 2, 3 o 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono- o polisustituido, X, Y están, de modo independiente entre sí, ausentes, son -CH2-, -(CH2)2-, -C(O)-, -CHOH- o -CH2OC(O)-, en donde solo uno de los radicales X o Y puede estar ausente, R son, de modo independiente entre sí, H, A, Cyc, (CH2)qAr o (CH2)qHet y pueden estar mono- o polisustituidos con R6, en donde en el caso de A y Cyc, la cadena de C o bien el anillo de C también puede estar interrumpido por O, R1 son, de modo independiente entre sí, R, F, CI, Br, I, OH, =O, CN, NO2, NRR, NHC(O)R, NHSO2R, OR, C(O)R, C(O)NRR, CF3, OCF3, SCF3, SO2CH3, SO3R, SO2R, SO2NR, SR, OA, A, fenilo y pueden estar mono- o polisustituidos con R6, R2, R3 son, de modo independiente entre sí, R, en donde R2 y R3 pueden formar juntos también, de modo alternativo, Cyc o Het, que, a su vez, pueden estar mono- o polisustituidos con R6; R4 son, de modo independiente entre sí, R, F, CI, Br, I, OH, =O, CN, NO2, NRR, NHC(O)R, NHSO2R, OR, C(O)R, C(O)NRR, CF3, OCF3, SCF3, SO2CH3, SO3R, SO2R, SO2NR, SR, OA, A, fenilo y pueden estar mono- o polisustituidos con R6; R5 son, de modo independiente entre sí, R, F, CI, Br, I, OH, =O, CN, NO2, NRR, NHC(O)R, NHSO2R, OR, C(O)R, C(O)NRR, CF3, OCF3, SCF3, SO2CH3, SO3R, SO2R, SO2NR, SR, OA, A, fenilo y pueden estar mono- o polisustituidos con R6; R6 son, de modo independiente entre sí, R, F, CI, Br, I, OH, =O, CN, NO2, NRR, NHC(O)R, NHSO2R, OR, C(O)R, C(O)NRR, CF3, OCF3, SCF3, SO2CH3, SO3R, SO2R, SO2NR, SR, OA, A, fenilo y, siempre que sea posible químicamente una sustitucion, pueden estar mono- o polisustituidos con R, F, CI, Br, I, OH, =O, CN, NO2, NRR, NHC(O)R, NHSO2R, OR, C(O)R, C(O)NRR, CF3, OCF3, SCF3, SO2CH3, SO3R, SO2R, SO2NR, SR, OA, A, fenilo, A es alquilo lineal o ramificado con 1, 2, 3, 4, 5, 6, 7 u 8 átomos de C, en donde 1, 2, 3, 4, 5, 6 o 7 átomos de H pueden estar reemplazados por OR, CN, NRR, F y/o CI y/o en donde uno o dos grupos no adyacentes CH2 pueden estar reemplazados por O, NH, S, SO, SO2 y/o por grupos CH=CH, Cyc es alquilo cíclico con 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13 o 14 átomos de C, m es 0, 1, 2, 3, 4 o 5, n es 0, 1, 2 o 3, p es 0, 1, 2, 3 o 4, q es 0, 1 o 2, así como sus sales, solvatos y estereoisomeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP110100979A 2010-03-26 2011-03-23 Derivados de 3,4-dihidro-1h-benzo[b][1,6]naftiridina, composiciones farmaceuticas que los contiene, procedimiento para prepararlos e intermediarios del mismo, y uso de los compuestos en el tratamiento de canceres y enfermedades autoinmunes e inflamatorias. AR080803A1 (es)

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EP10003282 2010-03-26

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AR080803A1 true AR080803A1 (es) 2012-05-09

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ARP110100979A AR080803A1 (es) 2010-03-26 2011-03-23 Derivados de 3,4-dihidro-1h-benzo[b][1,6]naftiridina, composiciones farmaceuticas que los contiene, procedimiento para prepararlos e intermediarios del mismo, y uso de los compuestos en el tratamiento de canceres y enfermedades autoinmunes e inflamatorias.

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US (1) US9029387B2 (es)
EP (1) EP2552914B1 (es)
JP (1) JP5827677B2 (es)
CN (1) CN102822171B (es)
AR (1) AR080803A1 (es)
AU (1) AU2011232058B2 (es)
CA (1) CA2794211A1 (es)
ES (1) ES2562183T3 (es)
WO (1) WO2011116867A1 (es)

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US20130012505A1 (en) 2013-01-10
AU2011232058B2 (en) 2016-09-08
CN102822171A (zh) 2012-12-12
ES2562183T3 (es) 2016-03-02
US9029387B2 (en) 2015-05-12
JP5827677B2 (ja) 2015-12-02
CA2794211A1 (en) 2011-09-29
EP2552914A1 (de) 2013-02-06
CN102822171B (zh) 2015-09-02

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