AR065767A1 - Derivados de fenilquinazolinas,composiciones farmaceuticas que los contienen,metodo de preparacion de los mismos y usos para el tratamiento del cancer. - Google Patents

Derivados de fenilquinazolinas,composiciones farmaceuticas que los contienen,metodo de preparacion de los mismos y usos para el tratamiento del cancer.

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Publication number
AR065767A1
AR065767A1 ARP080101080A ARP080101080A AR065767A1 AR 065767 A1 AR065767 A1 AR 065767A1 AR P080101080 A ARP080101080 A AR P080101080A AR P080101080 A ARP080101080 A AR P080101080A AR 065767 A1 AR065767 A1 AR 065767A1
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AR
Argentina
Prior art keywords
alkyl
optionally substituted
substituted
hydrogen
heterocycloalkyl
Prior art date
Application number
ARP080101080A
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English (en)
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Exelixis Inc
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Publication date
Application filed by Exelixis Inc filed Critical Exelixis Inc
Publication of AR065767A1 publication Critical patent/AR065767A1/es

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    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicacion 1 Un compuesto de la Formula 1 o un isomero individual del mismo, donde el compuesto está optativamente en forma de sal aceptable para uso farmacéutico, hidrato, solvato o una combinacion de los mismos, donde R1 es alquilo,cicloalquilo, fenilo, o heteroarilo donde el cicloalquilo, fenilo y heteroarilo están optativamente sustituidos con 1, 2 o 3 R6; R2 y R3 junto con el pirimidinilo al cual están unidos forman un quinazolinilo optativamente sustituido en lasposiciones 5, 6, 7 y 8 con uno o dos grupos seleccionados independientemente de alquilo, alcoxi, halo, hidroxi, heterocicloalquilalquiloxi, heterocicloalquilo y heterocicloalquilo sustituido con alquilo; o R2 y R3 junto con el pirimidinilo al cualestán unidos forman un pirido[3,2-d]pirimidinilo, pirido[4,3-d]pirimidinilo, pirido[3,4-d]pirimidinilo, o pirido[2,3-d]pirimidinilo, cada uno de los cuales está optativamente sustituido en un átomo de carbono, en las posiciones 5, 6, 7 y 8, con unoo dos grupos seleccionados independientemente entre alquilo, alcoxi, halo, hidroxi, heterocicloalquilalquiloxi, heterocicloalquilo y heterocicloalquilo sustituido con alquilo; o R2 y R3 junto con el pirimidinilo al cual están unidos forman un 6,7-dihidro-5H-ciclopenta[d]pirimidinilo, 5,6,7,8-tetrahidroquinazolinilo, o 6,7,8,9-tetrahidro- 5H-ciclohepta[d]pirimidinilo; o R2 y R3 junto con el pirimidinilo al cual están unidos forman un 5,6,7,8-tetrahidropirido[3,2-d]pirimidinilo, 5,6,7,8-tetrahidropirido[4 ,3-d]pirimidinilo, 5,6,7,8-tetrahidropirido[3 ,4-d]pirimidinilo, o 5,6,7,8-tetrahidropirido[2,3-d]pirimidinilo, cada uno de los cuales está optativamente sustituido en las posiciones 5, 6, 7 y 8 con uno o dos grupos seleccionadosindependientemente entre alquilo, alcoxicarbonilo, benciloxicarbonilo y fenilalquilo optativamente sustituido; cada R6, en caso de estar presente R6, es independientemente seleccionado entre alquilo, alcoxi, amino, alquilamino, dialquilamino, halo,haloalquilo, haloalcoxi, halofenilo, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, hidroxialquilo, alcoxicarbonilo, aminoalquilo, alquilaminoalquilo, dialquilaminoalquilo, aminoalquilamino, alquilaminoalquilamino,dialquilaminoalquilamino, alquiloxialquilamino, heterocicloalquilo y heterocicloalquilalquilo; donde el heterocicloalquilo, solo o como parte del heterocicloalquilalquilo, está optativamente sustituido con alquilo o alcoxicarbonilo; R40 es hidrogenoo alquilo; R50 es seleccionado entre el grupo de formulas 2; n1 es 0, 1,o 2; cada R5, en caso de estar presente R5, es independientemente alquilo, hidroxi, alcoxi, amino, alquilamino, dialquilamino, halo, nitro, heterocicloalquilo,heterocicloalquilamino, o heterocicloalquilalquiloxi; donde cada heterocicloalquilo, solo o como parte de otro grupo presente en R5, está independientemente optativamente sustituido con alquilo o alcoxicarbonilo; R4a es hidrogeno o alquilo; R4 esheteroarilo sustituido con un R8 y está sustituido además con 1 o 2 R8a; R4 es fenilo sustituido con un R29 y está sustituido además con 1 o 2 R9a; R4 es cicloalquilo optativamente sustituido con uno o dos grupos seleccionados independientementeentre alquilo, hidroxi, alcoxi, amino, alquilamino y dialquilamino; o R4 es heterocicloalquilo optativamente sustituido con alquilo o alcoxicarbonilo; R17 es cicloalquilo, heterocicloalquilo (optativamente sustituido con uno o dos gruposseleccionados entre alquilo y alcoxicarbonilo), fenilalquilamino, fenilalquilo, o fenilo; donde cada fenilo, solo o como parte de un grupo presente en R17, está sustituido con 1, 2 o 3 R9a; R18 es hidrogeno, halo, o alquilo; R18a es hidrogeno oalquilo; R18b es heteroarilo sustituido con 1, 2 o 3 R8a, o R18b es fenilo sustituido con 1, 2 o 3 R9a; R19 es fenilo sustituido con 1, 2 o 3 R9a, o R19 es heteroarilo sustituido con 1, 2 o 3 R8a; R20 es hidrogeno, alquilo, alquilcarbonilo,alquilsulfonilo, o alcoxicarbonilo; R20 es hidrogeno o alquilo; R20b es heteroarilo sustituido con 1, 2 o 3 R8a, o R20b es fenilo sustituido con 1, 2 o 3 R9a; R21 es fenilo sustituido con 1, 2 o 3 R9a, o R21 es heteroarilo sustituido con 1, 2 o 3R8a, o R21 es heterocicloalquilo optativamente sustituido con alquilo o alcoxicarbonilo; R22 es fenilo sustituido con 1, 2 o 3 R9a, o R22 es heteroarilo sustituido con 1, 2 o 3 R8a; cada R8 es independientemente alquilo, cicloalquilo,fenílalquiloxialquilo, o R9b; cada R8 es independientemente hidrogeno, halo, o R8; cada R9 es independientemente hidrogeno, R9b, o R9c; R29 es R9b o R9c siempre que R29 sea R9b cuando R1 es fenilo no sustituido y cuando R1 es fenilo sustituido con1, 2 o 3 R6 seleccionado independientemente entre alquilo, halo, alcoxi, hidroxialquilo, aminoalquilo y alcoxicarbonilo; cada R9b, cuando R9b está presente, es independientemente amino, alquilamino, dialquilamino, heterocicloalquilo optativamentesustituido, heterocicloalquilalquiloxi optativamente sustituido, aminoalquiloxi, alquilaminoalquiloxi, dialquilaminoalquiloxi, heteroarilo optativamente sustituido, ciano, -C(O)R14, CR14a(=NR14b), -C(=NR24)R24a, -S(O)2NR13R13a, -NR23C(O)R23a -C(O)NR12R12a, o alquilo sustituido con uno o dos R11; cada R9C, cuando R9C está presente, es independientemente alquilo, haloalquilo, hidroxialquilo, halo, hidroxi, alcoxi, ciano, nitro, o fenilcarbonilo; cada R11 es independientemente seleccionadoentre hidroxi, -NR15R15a, heteroarilo optativamente sustituido, heterocicloalquilo optativamente sustituido y cicloalquilo optativamente sustituido; R12 es hidrogeno o alquilo y R12a es hidrogeno, hidroxi, alcoxi, alquilo, aminoalquilo,alquilaminoalquilo, dialquilaminoalquilo, hidroxialquilo, heterocicloalquilo optativamente sustituido, heterocicloalquilalquilo optativamente sustituido, o heteroarilo optativamente sustituido; o R12 y R12a junto con el nitrogeno al cual estánunidos forman un heterocicloalquilo optativamente sustituido con 1, 2 o 3 grupos seleccionados independientemente entre alquilo, hidroxialquilo, haloalquilo, alquilcarbonilo, alcoxicarbonilo, cicloalquilo optativamente sustituido, cicloalquilalquilooptativamente sustituido, heteroarilo optativamente sustituido, heteroarilalquilo optativamente sustituido, fenilo optativamente sustituido y fenilalquilo optativamente sustituido; R13 es hidrogeno o alquilo; R13a es alquilo, aminoalquilo,alquilaminoalquilo, o dialquilaminoalquilo; cada R14 es independientemente hidrogeno, alquilo, hidroxi, alcoxi, heteroarilalquilo optativamente sustituido, o heterocicloalquilalquilo optativamente sustituido; cada R14a es hidrogeno o alquilo; R14bes alcoxi, amino, alquilamino, dialquilamino, o heterocicloalquilo optativamente sustituido; R15 es hidrogeno, alquilo, alcoxialquilo, hidroxialquilo, o haloalquilo; R15a es hidrogeno, alquilo, alcoxialquilo, haloalquilo, hidroxialquilo,carboxialquilo, aminocarbonilalquilo, alquilaminocarbonilalquilo, dialquilaminocarbonilalquilo, cicloalquilo optativamente sustituido, o fenilalquilo optativamente sustituido; R23 es hidrogeno o alquilo; R23a es hidrogeno, alquilo, aminoalquilo,alquilaminoalquilo, dialquilaminoalquilo, o heterocicloalquilalquilo optativamente sustituido; R24 es hidrogeno o alquilo, hidroxi, o alcoxi; y R24a es hidroxi, alcoxi, amino, alquilamino, o dialquilamino.
ARP080101080A 2007-03-14 2008-03-14 Derivados de fenilquinazolinas,composiciones farmaceuticas que los contienen,metodo de preparacion de los mismos y usos para el tratamiento del cancer. AR065767A1 (es)

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US91816007P 2007-03-14 2007-03-14
US96261707P 2007-07-30 2007-07-30

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Country Status (18)

Country Link
US (3) US8222263B2 (es)
EP (2) EP2527330A1 (es)
JP (1) JP5577104B2 (es)
KR (1) KR20090130051A (es)
CN (1) CN101679308B (es)
AR (1) AR065767A1 (es)
AU (1) AU2008224941C1 (es)
BR (1) BRPI0808772A2 (es)
CA (1) CA2680796A1 (es)
CO (1) CO6231031A2 (es)
EA (1) EA018441B1 (es)
GE (1) GEP20135925B (es)
IL (1) IL200603A (es)
MX (1) MX2009009786A (es)
NZ (2) NZ598251A (es)
SG (1) SG179418A1 (es)
TW (1) TWI430798B (es)
WO (1) WO2008112913A1 (es)

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