AR082880A1 - Derivados de pirazolopiridinona como antagonistas del receptor de lpa - Google Patents

Derivados de pirazolopiridinona como antagonistas del receptor de lpa

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Publication number
AR082880A1
AR082880A1 ARP110103213A ARP110103213A AR082880A1 AR 082880 A1 AR082880 A1 AR 082880A1 AR P110103213 A ARP110103213 A AR P110103213A AR P110103213 A ARP110103213 A AR P110103213A AR 082880 A1 AR082880 A1 AR 082880A1
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Argentina
Prior art keywords
alkyl
heterocyclyl
denotes
cycloalkyl
heteroaryl
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ARP110103213A
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English (en)
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Wolfgang Staehle
Dirk Wienke
Kai Schiemann
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Merck Patent Gmbh
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Publication of AR082880A1 publication Critical patent/AR082880A1/es

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    • 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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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Abstract

La presente solicitud se refiere a derivados de pirazolopiridinona de acuerdo con la formula (1), a un proceso de preparación de ellos, medicamento y composición farmacéutica en base al compuesto. Estos derivados de pirazolopiridinona se pueden usar como antagonistas de receptores de LPA para el tratamiento de diversas enfermedades como tumores benignos o malignos, sarcomas (sarcoma de Ewing o de Kaposi), entre otros.Reivindicación 1: Compuestos de la fórmula (1) en donde R1 denota arilo, heteroarilo, cicloalquilo, heterociclilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterociclilalquilo, que pueden estar opcionalmente sustituidos con uno o varios sustituyentes seleccionados de alquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halógeno, -F, -Cl, -Br, -I, -CN, -CF3, -N3, -NH2, -NHZ1, -NZ2Z3, -NO2, -OH, -OCF3, -SH, -O-SO3H, -OP(O)(OH)2, -CHO, -COOH, -C(O)NH2, -SO3H, -P(O)(OH)2, -CO)-Z4, -C(O)OZ5, C(O)NH-Z6, -C(O)NZ7Z8, -O-Z9, -O(-Z10-O)a-H (a = 1, 2, 3, 4, 5), -O(-Z11-O)b-Z12 (b = 1, 2, 3, 4, 5), -OC(O)-Z13, -OC(O)-O-Z14, -OC(O)-NHZ15, -O-C(O)-NZ16Z17, -OP(O)(OZ18)(OZ19), -OSi(Z20)(Z21)(Z22), -OS(O2)-Z23, -NHC(O)-NH2, -NHC(O)-Z24, -NZ25C(O)-Z26, -NH-C(O)-O-Z27, -NH-C(O)-NH-Z28, -NH-C(O)-NZ29Z30, -NZ31-C(O)-O-Z32, -NZ33-C(O)-NH-Z34, -NZ35-C(O)-NZ36Z37, -NHS(O2)-Z38, -NZ39S(O2)-Z40, -S-Z41, -S(O)-Z42, -S(O2)-Z43, -S(O2)NH-Z44, -S(O2)NZ45Z46, -S(O2)O-Z47, -P(O)(OZ48)(OZ49), -Si(Z50)(Z51)(Z52), -C(NH)-NH2, -C(NZ53)-NH2, -C(NH)-NHZ54, -C(NH)-NZ55Z56, -C(NZ57)-NHZ58, -C(NZ59)-NZ60Z61, -NH-C(O)-NH-O-Z62, -NH-C(O)-NZ63-O-Z64, -NZ65-C(O)-NZ66-O-Z67, -N(-C(O)-NH-O-Z68)2, -N(-C(O)-NZ69-O-Z70)2, -N(-C(O)-NH-O-Z71)(-C(O)-NZ72-O-Z73), -C(S)-Z74, -C(S)-O-Z75, -C(S)-NH-Z76, -C(S)-NZ77Z78, -C(O)-NH-O-Z79, -C(O)-NZ80-O-Z81, -C(S)-NH-O-Z82, -C(S)-NZ83-O-Z84, -C(O)-NH-NH-Z85, -C(O)-NH-NZ86Z87, -C(O)-NZ88-NZ89Z90, -C(S)-NH-NH-Z91, -C(S)-NH-NZ92Z93, -C(S)-NZ94-NZ95Z96, -C(O)-C(O)-O-Z97, -C(O)-C(O)-NH2, -C(O)-C(O)-NHZ98, -C(O)-C(O)-NZ99Z100, -C(S)-C(O)-O-Z101, -C(O)-C(S)-O-Z102, -C(S)-C(S)-O-Z103, -C(S)-C(O)-NH2, -C(S)-C(O)-NHZ104, -C(S)-C(O)-NZ105Z106, -C(S)-C(S)-NH2, -C(S)-C(S)-NHZ107, -C(S)-C(S)-NZ108Z109, -C(O)-C(S)-NH2, -C(O)-C(S)-NHZ110, -C(O)-C(S)-NZ111Z112; en donde Z1, Z2, Z3, Z4, Z5, Z6, Z7, Z8, Z9, Z10, Z11, Z12, Z13, Z14, Z15, Z16, Z17, Z18, Z19, Z20, Z21, Z22, Z23, Z24, Z25, Z26, Z27, Z28, Z29, Z30, Z31, Z32, Z33, Z34, Z35, Z36, Z37, Z38, Z39, Z40, Z41, Z42, Z43, Z44, Z45, Z46, Z47, Z48, Z49, Z50, Z51, Z52, Z53, Z54, Z55, Z56, Z57, Z58, Z59, Z60, Z61, Z62, Z63, Z64, Z65, Z66, Z67, Z68, Z69, Z70, Z71, Z72, Z73, Z74, Z75, Z76, Z77, Z78, Z79, Z80, Z81, Z82, Z83, Z84, Z85, Z86, Z87, Z88, Z89, Z90, Z91, Z92, Z93, Z94, Z95, Z96, Z97, Z98, Z99, Z100, Z101, Z102, Z103, Z104, Z105, Z106, Z107, Z108, Z109, Z110, Z111, Z112 están seleccionados cada uno, de modo independiente entre sí, del grupo que consiste en: “alquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo” y en donde, de modo alternativo, Z7, Z8 y/o Z16, Z17 y/o Z29, Z30 y/o Z36, Z37 y/o Z45, Z46 y/o Z55, Z56 y/o Z60, Z61 y/o Z77, Z78 y/o Z86, Z87 y/o Z89, Z90 y/o Z92, Z93 y/o Z95, Z96 y/o Z99, Z100 y/o Z105, Z106 y/o Z108, Z109 y/o Z111, Z112 respectivamente también pueden formar juntos “heterociclilo”; R2 denota H o alquilo; R3 denota H o alquilo; R4, R5 denotan, de modo independiente entre sí, H, alquilo, OH-alquilo, alcoxi, halógeno, F, Cl, Br, I, CN, NHR, NH2, NR2, S-alquilo o NH-alquil-OH, en donde R denota, de modo independiente entre sí, alquilo, arilo, heteroarilo, cicloalquilo o heterociclilo; o R4 y R5 forman juntos cicloalquilo o heterociclilo; R6 denota H o alquilo; X denota O, NH o N-alquilo; siempre que se excluya el compuesto de fórmula (2) de la fórmula (1); y sus sales, solvatos, tautómeros y estereoisómeros fisiológicamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP110103213A 2010-09-02 2011-09-02 Derivados de pirazolopiridinona como antagonistas del receptor de lpa AR082880A1 (es)

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EP (1) EP2611808B1 (es)
JP (1) JP6039559B2 (es)
CN (1) CN103189378B (es)
AR (1) AR082880A1 (es)
AU (1) AU2011297961B2 (es)
CA (1) CA2809892C (es)
ES (1) ES2530345T3 (es)
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US8859775B2 (en) 2014-10-14
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AU2011297961A1 (en) 2013-04-18
AU2011297961B2 (en) 2015-07-02
US20140350046A1 (en) 2014-11-27
WO2012028243A1 (en) 2012-03-08
US9067938B2 (en) 2015-06-30
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