AR063946A1 - Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. - Google Patents

Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.

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Publication number
AR063946A1
AR063946A1 ARP070103990A ARP070103990A AR063946A1 AR 063946 A1 AR063946 A1 AR 063946A1 AR P070103990 A ARP070103990 A AR P070103990A AR P070103990 A ARP070103990 A AR P070103990A AR 063946 A1 AR063946 A1 AR 063946A1
Authority
AR
Argentina
Prior art keywords
phenyl
pyrimidin
optionally substituted
carboxamide
alkyl
Prior art date
Application number
ARP070103990A
Other languages
English (en)
Original Assignee
Cgi Pharmaceuticals Inc
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
Application filed by Cgi Pharmaceuticals Inc filed Critical Cgi Pharmaceuticals Inc
Publication of AR063946A1 publication Critical patent/AR063946A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Composiciones farmacéuticas que comprenden al menos una entidad química de formula 1, junto con al menos un vehículo aceptable para uso farmacéutico seleccionado entre vehículos, coadyuvantes y excipientes. Uso de estos compuestos para tratar pacientes que sufren de ciertas enfermedades que responden a la inhibicion de la actividad de Btk y/o la actividad de las células B. Reivindicacion 1: Un compuesto seleccionado entre los compuestos de formula 1, y sales aceptables para uso farmacéutico, quelatos, complejos no covalentes, prodrogas y mezclas de los mismos, en donde Z1 es CR y Z2 es N o Z1 es N y Z2 es CR; A se selecciona entre fenileno opcionalmente sustituido, piridilideno opcionalmente sustituido, 2-oxo-1,2- dihidropiridinilo opcionalmente sustituido, grupo de formulas (2) en donde * indica el punto de union al grupo -L-G y la union partida indica el punto de union al grupo amino; X1 se selecciona entre N y CR7; X2 se selecciona entre N y CR7; y X3 se selecciona entre N y CR7; y en donde no más que uno de X1, X2, y X3 es N, y R7 se selecciona entre hidrogeno, hidroxi, ciano, halo, alquilo inferior opcionalmente sustituido, y alcoxi inferior opcionalmente sustituido; L se selecciona entre alquileno C0-4 opcionalmente sustituido, -O-alquileno C0-4 opcionalmente sustituido, -(alquileno C0-4)(SO)-, -(alquileno C0-4)(SO2)-; y -(alquileno C0-4)(C=O)-; G se selecciona entre hidrogeno, halo, hidroxi, alcoxi, nitro, alquilo opcionalmente sustituido, amino opcionalmente sustituido, carbamimidoilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, y heteroarilo opcionalmente sustituido; R y R1 se seleccionan en forma independiente entre hidrogeno y alquilo inferior opcionalmente sustituido; W se selecciona entre fenileno opcionalmente sustituido y piridilideno opcionalmente sustituido; Q se selecciona entre -C(R10)(R11)-N(R12), -N(R12)- C(R10)(R11), -N(R13)-C(=O)-, -C(=O)N(R13)-, y -N(R14)-C(=O)N(R15)-en donde R10 y R11 se seleccionan en forma independiente entre hidrogeno, alquilo C1-6, y haloalquilo C1-6; y R12, R13, R14, y R15 se seleccionan en forma independiente entre hidrogeno, alquilo C1-6, haloalquilo C1-6, fenilo, fenilo sustituido seleccionado entre fenilo mono-, di-, y trisustituido en donde los sustituyentes se seleccionan en forma independiente entre hidroxi, nitro, ciano, amino, halo, alquilo C1-6, alcoxi C1-6, alquiloxi C1-6-alcoxi C1-6, perfluoroalquilo C1-6, perfluoroalcoxi C1-6, mono-(C1-6 alquil)amino, di(C1-6 alquil)amino, y amino(C1-6 alquilo), heteroarilo, y heteroarilo sustituido seleccionado entre mono-, di-, y triheteroarilo sustituido en donde los sustituyentes se seleccionan en forma independiente entre hidroxi, nitro, ciano, amino, halo, alquilo C1-6, alcoxi C1-6, alquiloxi C1-6-alcoxi C1-6, perfluoroalquilo C1-6, perfluoroalcoxi C1-6, mono-(C1-6 alquil)amino, di(C1- 6 alquil)amino, y amino(C1-6 alquil); y R2 se selecciona entre arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido, con la condicion de que, el compuesto de formula 1 no se selecciona entre N-(4-(2-(4-(4-acetilpiperazina-1- carbonil)fenilamino)pirimidin-4-il)fenil)benzamida; 1-(4-(2-(4-(4-acetilpiperazina-1-carbonil)fenilamino)pirimidin-4-iI)fenil)-3- fenilurea; N-(3-(2-(3,4,5-trimetoxifenilamino)pirimidin-4-iI)fenil)piridin-3-carboxamida; N-(3-(2-(3,4,5- trimetoxifenilamino)pirimidin-4-il)fenil)-5-metilisoxazol-3-carboxamida; N-(3-(2-(3-sulfamoilfenilamino)pirimidin-4-il)fenil)furan-2-carboxamida; N-(3-(2-(3-metoxifenilamino)pirimidin-4-il)fenil)-N-metilfuran-2-carboxamida; N-(3-(2-(3- metoxifenilamino)pirimidin-4-il)fenil)furan-2-carboxamida; N-(3-(2-(3-hidroxifenilamino)pirimidin-4-il)fenil)furan-2-carboxamida; N-(3-(2-(3-aminofenilamino)pirimidin-4-il)fenil)picolinamida; N-(3-(2-(3-aminofenilamino)pirimidin-4-il)fenil)tiofen-2- carboxamida; N-(3-(2-(3-aminofenilamino)pirimidin-4-il)fenil)furan-2-carboxamida; N-(5-(2-(3-aminofenilamino)pirimidin-4-il)-2-metoxifenil)tiofen-2-carboxamida; N-(4-(2-(3-aminofenilamino)pirimidin-4-il)fenil)tiofen-2-carboxamida; N-(4-(2-(3- aminofenilamino)pirimidin-4-il)fenil)furan-2-carboxamida; N-(4-(2-(3-hidroxifenilamino)pirimidin-4-il)fenil)tiofen-2-carboxamida; N-(3-(2-(3-sulfamoilfenilamino)piridin-4-il)fenil)furan-2-carboxamida; N-(3-(2-(3-metoxifenilamino)piridin-4-il)fenil)- N-metilfuran-2-carboxamida; N-(3-(2-(3-metoxifenilamino)piridin-4-il)fenil)furan-2-carboxamida; N-(3-(2-(3-hidroxifenilamino)piridin-4-il)fenil)furan-2-carboxamida; N-(3-(2-(3-aminofenilamino)piridin-4-il)fenil)picolinamida; N-(3-(2-(3- aminofenilamino)piridin-4-il)fenil)tiofen-2-carboxamida; N-fenil-4-(2-(fenilamino)pirimidin-4-iI)benzamida; 4-(5-metil-2-(fenilamino)pirimidin-4-il)-N-fenilbenzamida; N-(4-(2-(3-hidroxifenilamino)pirimidin-4-il)fenil)-2-fenoxiacetamida; y 2-fenoxi-N- (4-(2-(3-sulfamoilfenilamino)pirimidin-4-il)fenil)acetamida.
ARP070103990A 2006-09-11 2007-09-10 Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. AR063946A1 (es)

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US84383606P 2006-09-11 2006-09-11

Publications (1)

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AR063946A1 true AR063946A1 (es) 2009-03-04

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ID=38884547

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ARP070103990A AR063946A1 (es) 2006-09-11 2007-09-10 Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.

Country Status (18)

Country Link
US (1) US20080125417A1 (es)
EP (1) EP2069314A1 (es)
JP (1) JP2010502749A (es)
KR (1) KR20090061655A (es)
CN (1) CN101605766A (es)
AR (1) AR063946A1 (es)
AU (1) AU2007296550A1 (es)
BR (1) BRPI0716888A2 (es)
CA (1) CA2661938A1 (es)
CL (1) CL2007002641A1 (es)
IL (1) IL197231A0 (es)
MX (1) MX2009002648A (es)
NO (1) NO20091423L (es)
PE (1) PE20081059A1 (es)
RU (1) RU2009113691A (es)
TW (1) TW200829577A (es)
WO (1) WO2008033834A1 (es)
ZA (1) ZA200901593B (es)

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EP2069314A1 (en) 2009-06-17
TW200829577A (en) 2008-07-16
PE20081059A1 (es) 2008-10-22
CL2007002641A1 (es) 2008-06-20
MX2009002648A (es) 2009-03-26
NO20091423L (no) 2009-06-10
ZA200901593B (en) 2010-03-31
CN101605766A (zh) 2009-12-16
KR20090061655A (ko) 2009-06-16
BRPI0716888A2 (pt) 2013-10-22
WO2008033834A1 (en) 2008-03-20
AU2007296550A1 (en) 2008-03-20
JP2010502749A (ja) 2010-01-28
CA2661938A1 (en) 2008-03-20
US20080125417A1 (en) 2008-05-29
RU2009113691A (ru) 2010-10-20
IL197231A0 (en) 2009-12-24

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