AR081994A1 - Derivados de [1,8]naftiridina, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para el tratamiento de enfermedades inducidas por quinasas, en particular diferentes tipos de canceres - Google Patents

Derivados de [1,8]naftiridina, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para el tratamiento de enfermedades inducidas por quinasas, en particular diferentes tipos de canceres

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Publication number
AR081994A1
AR081994A1 ARP110102198A ARP110102198A AR081994A1 AR 081994 A1 AR081994 A1 AR 081994A1 AR P110102198 A ARP110102198 A AR P110102198A AR P110102198 A ARP110102198 A AR P110102198A AR 081994 A1 AR081994 A1 AR 081994A1
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AR
Argentina
Prior art keywords
denotes
cyy
nyy
naphthyridin
atoms
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ARP110102198A
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English (en)
Inventor
Dieter Dorsch
Guenter Hoelzemann
Christiane Amendt
Frank Zenke
Alfred Jonczyk
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Merck Patent Gmbh
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Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR081994A1 publication Critical patent/AR081994A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/4353—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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • 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
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Abstract

Reivindicación 1: Compuestos de la fórmula (1) en donde W1, W2, W3, W4 denota de modo independiente entre sí, N o CR3; W5 denota N o C, con preferencia, denota N o CR3, con mayor preferencia, denota N; Z denota C=C, NR4, C=N, O, S, CH, N=N o N=C, con preferencia, denota C=C, N(R4)CO, NR4, C=N, O, CON(R4), S, CH, N=N o N=C, con mayor preferencia, denota C=C, N(R4)CO, NR4, C=N, O, CON(R4), S, CH o N=N; R1 denota un arilo monocíclico que tiene 5, 6, 7, 8, 9 ó 10 átomos de C o un heteroarilo monocíclico que tiene 5, 6, 7, 8, 9, 10, 11, 12, 13 ó 14 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, cada uno de los cuales puede estar independientemente sustituido con al menos un sustituyente seleccionado del grupo que consiste en Y, Hal, CN, CF3 u OY; R2 denota H, Hal, A, -(CYY)n-OY, -(CYY)n-NYY, -(CYY)n-Het, SY, NO2, CN, COOY, -CO-NYY, -NY-COA, -NY-SO2A, -SO2-NYY, S(O)mA, -CO-Het, -O(CYY)n-OY, -O(CYY)n-NYY, -O(CYY)n-Het, -NH-COOA, -NH-CO-NYY, -NH-COO-(CYY)n-NYY, -NH-COO-(CYY)n-Het, -NH-CO-NH-(CYY)n-NYY, -NH-CO-NH(CYY)n-Het, -OCO-NH-(CYY)n-NYY, -OCO-NH-(CYY)n-Het, CHO, COA, =S, =NY, =O ó un arilo monocíclico que tiene 5, 6, 7, 8, 9 ó 10 átomos de C o un heteroarilo monocíclico que tiene 5, 6, 7, 8, 9, 10, 11, 12, 13 ó 14 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, donde cada uno de arilo monocíclico y heteroarilo monocíclico puede estar sustituido, de modo independiente, con al menos un sustituyente seleccionado del grupo que consiste en Y, Hal, CN, CF3 u OY; R3 denota H, OY, NYY, NY-COY, NY-CO-(CYY)n-OY, NY-COY-NYY, NY-(CYY)n-NYY, O-(CYY)n-NYY u O-(CYY)n-Het; R4 denota H, A, -(CYY)o-Het, -(CYY)o-NYY o -(CYY)o-OY; R5 denota H, A, OY, NYY o Het; Y denota H o A, con preferencia, en caso de -(CYY)n/o-Y denote adicionalmente H, A u OH; A denota alquilo no ramificado o ramificado que tiene 1, 2, 3, 4, 5, 6, 7, 8, 9 ó 10 átomos de C, en donde 1, 2, 3, 4, 5, 6 ó 7 átomos de H pueden estar reemplazados, de modo independiente entre sí, por Hal y/o en donde uno o dos grupos CH2 pueden estar reemplazados, de modo independiente entre sí, con un O, S, SO, SO2, un grupo -CY=CY- y/o un grupo -CºC-; de modo alternativo, A denota cicloalquilo con 3, 4, 5, 6, 7 ó 8 átomos de C; Het denota un heterociclo mono, bi- o tricíclico saturado o insaturado que tiene 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 ó 20 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, que puede estar sustituido con al menos un sustituyente seleccionado del grupo que consiste en Y, Hal, CN, CF3, OY; Hal denota F, Cl, Br o I; m denota 0, 1 ó 2, n denota 0, 1, 2, 3 ó 4; o denota 0, 1, 2, 3 ó 4, con preferencia, si Z es NR4, o adicionalmente denota 2, 3 ó 4; p denota 0, 1, 2 ó 3; q denota 0, 1, 2 ó 3; siempre que se excluyan los siguientes compuestos: (a) 2-(5-cloro-2-fluoro-fenil)-4-isoquinolin-4-il-[1,8]naftiridina, (b) 4-isoquinolin-4-iI-2-(6-metil-piridin-2-il)-[1,8]naftiridina, (c) 4-[2-(2-fluoro-fenil)-[1,8]naftiridin-4-il]-[2,7]naftiridin-1-ilamina, (d) 4-[2-(2,5-difluoro-fenil)-[1,8]naftiridin-4-il]-[2,7]naftiridin-1-ilamina, (e) N-{4-[2-(2-fluoro-fenil)-[1,8]naftiridin-4-il]-[2,7]naftiridin-1-il}-acetamida, (f) 2-(2-fluoro-fenil)-4-[2,7]naftiridin-4-il-[1,8]naftiridina, (g) 5-[2-(2-fluoro-fenil)-[1,8]naftiridin-4-il]-[2,7]naftiridin-1-ilamina, (h) 5-[2-(5-cloro-2-fluoro-fenil)-[1,8]naftiridin-4-il]-[1,7]naftiridina, (i) 4-[2-(5-cloro-2-fluoro-fenil)-[1,8]naftiridin-4-il]-[2,7]naftiridin-1-ilamina, y sus sales, solvatos, estereoisómeros y tautómeros fisiológicamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP110102198A 2010-06-28 2011-06-24 Derivados de [1,8]naftiridina, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para el tratamiento de enfermedades inducidas por quinasas, en particular diferentes tipos de canceres AR081994A1 (es)

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EP10006683 2010-06-28

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AR081994A1 true AR081994A1 (es) 2012-10-31

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US (1) US8791113B2 (es)
EP (1) EP2585461B1 (es)
JP (1) JP5826261B2 (es)
KR (1) KR20130038336A (es)
CN (1) CN102958930B (es)
AR (1) AR081994A1 (es)
AU (1) AU2011273931B2 (es)
BR (1) BR112012033241A2 (es)
CA (1) CA2803665C (es)
CL (1) CL2012003680A1 (es)
CO (1) CO6612243A2 (es)
EA (1) EA201300052A1 (es)
EC (1) ECSP13012408A (es)
ES (1) ES2792799T3 (es)
IL (1) IL223496A (es)
MX (1) MX2012014549A (es)
NZ (1) NZ603456A (es)
PE (1) PE20130376A1 (es)
SG (1) SG186855A1 (es)
WO (1) WO2012000595A1 (es)

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