ES2637167T3 - Compuestos de tetrahidro-pirido-piridina y tetrahidro-pirido-pirimidina y su uso como moduladores de los receptores de C5a - Google Patents

Compuestos de tetrahidro-pirido-piridina y tetrahidro-pirido-pirimidina y su uso como moduladores de los receptores de C5a Download PDF

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ES2637167T3
ES2637167T3 ES12743023T ES12743023T ES2637167T3 ES 2637167 T3 ES2637167 T3 ES 2637167T3 ES 12743023 T ES12743023 T ES 12743023T ES 12743023 T ES12743023 T ES 12743023T ES 2637167 T3 ES2637167 T3 ES 2637167T3
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carbon atoms
alkyl
alkoxy
hydrogen
atoms
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Christine GELIN
Alec FLYER
Christopher Michael Adams
Veronique DARSIGNY
Timothy Brian Hurley
Rajeshri Ganesh KARKI
Nan JI
Toshio Kawanami
Erik Meredith
Michael H. Serrano-Wu
Chang Rao
Catherine SOLOVAY
George Tien-San Lee
Christopher Towler
Denis Har
Lichun Shen
Bin Hu
Xinglong Jiang
Christina CAPPACI-DANIEL
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Abstract

Un compuesto de la fórmula (I), o una sal del mismo: en donde: X es N o CH; Z1 es N o CR1c; Z2 es N o CR1d, en donde al menos uno de Z1 y Z2 no es N; R1a se selecciona a partir del grupo que consiste en hidrógeno, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, halo-alcoxilo de 1 a 6 átomos de carbono, ciano o halógeno; R1b se selecciona a partir del grupo que consiste en hidrógeno, amino, hidroxilo, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, y mono- y di-alquilo de 1 a 4 átomos de carbono-amino; R1c es hidrógeno, halógeno, o alquilo de 1 a 6 átomos de carbono; R1d se selecciona a partir del grupo que consiste en hidrógeno, halógeno, alquilo de 1 a 6 átomos de carbono, y alcoxilo de 1 a 6 átomos de carbono; R1e se selecciona a partir de hidrógeno, halógeno, ciano, alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono y halo-alcoxilo de 1 a 6 átomos de carbono, sulfona, cicloalquilo de 3 a 7 átomos de carbono; o R1a y R1b tomados en combinación, forman un anillo heterocíclico saturado o insaturado de 5 miembros que tiene uno o dos heteroátomos del anillo seleccionados a partir de N, O o S, cuyo anillo heterocíclico está sustituido con 0, 1 o 2 sustituyentes de alquilo de 1 a 6 átomos de carbono o de halógeno seleccionados independientemente; en donde al menos uno de R1a y R1e no es hidrógeno; R2 se selecciona a partir del grupo que consiste en hidrógeno, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, tioalquilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 7 átomos de carbono, cicloalquilo de 3 a 7 átomos de carbono-alquilo de 1 a 4 átomos de carbono y (CH2)pNR2aR2b, en donde cada grupo alquilo y alcoxilo está sustituido con 0 o 2 sustituyentes seleccionados a partir del grupo que consiste en hidroxilo, halógeno, y alcoxilo de 1 a 4 átomos de carbono, amino, mono- y di-alquilo de 1 a 4 átomos de carbono-amino; p es 0 o 1; R2a es hidrógeno, alquilo de 1 a 6 átomos de carbono, o hidroxi-alquilo de 1 a 6 átomos de carbono; R2b es hidrógeno, alquilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 7 átomos de carbono, o cicloalquilo de 3 a 7 átomos de carbono-alquilo de 1 a 4 átomos de carbono, en donde cada alquilo está insustituido o sustituido con hidroxilo, alcoxilo de 1 a 4 átomos de carbono, alcoxilo de 1 a 4 átomos de carbono-carbonilo, o heterociclo en donde el heterociclo es un anillo de cinco o seis miembros saturado, insaturado o aromático que tiene 1 o 2 heteroátomos del anillo seleccionados a partir de N, O o S, y que está insustituido o sustituido con 1 o 2 sustituyentes de alquilo de 1 a 4 átomos de carbono independientemente seleccionados; o NR2aR2b tomados en combinación, forman un sistema de anillo heterocíclico saturado de 4 a 8 miembros que tiene 1 o 2 anillos y 0 o 1 heteroátomo adicional del anillo seleccionado a partir de N, O o S, en donde el sistema de anillo heterocíclico saturado está insustituido o sustituido con 1 a 4 sustituyentes seleccionados independientemente a partir del grupo que consiste en alquilo de 1 a 4 átomos de carbono, hidroxilo, alcoxilo de 1 a 4 átomos de carbono, alcoxilo de 1 a 4 átomos de carbono-alquilo de 1 a 4 átomos de carbono, hidroxi-alquilo de 1 a 4 átomos de carbono, halógeno, amino, mono- y di-alquilo de 1 a 4 átomos de carbono-amino, alcoxilo de 1 a 4 átomos de carbonocarbonilo, alcanoílo de 1 a 4 átomos de carbono, S(O)2alquilo de 1 a 4 átomos de carbono, CH2C(O)(alcoxilo de 1 a 4 átomos de carbono), y CH2C(O)NH2; R3 se selecciona a partir del grupo que consiste en fenilo sustituido, heteroarilo sustituido, y fenil-alquilo de 1 a 3 átomos de carbono, en donde el heteroarilo se selecciona a partir de piridilo, pirazolilo, imidazolilo, tetrazolilo, oxazolilo, e isoxazolilo, y en donde cada grupo fenilo o heteroarilo está sustituido con 1, 2 o 3 sustituyentes, los cuales se seleccionan independientemente a partir del grupo que consiste en alquilo de 1 a 4 átomos de carbono, alcoxilo de 1 a 4 átomos de carbono, halógeno, ciano, halo-alquilo de 1 a 4 átomos de carbono, halo-alcoxilo de 1 a 4 átomos de carbono, hidroxi-alquilo de 1 a 4 átomos de carbono, alcoxilo de 1 a 4 átomos de carbono-alquilo de 1 a 4 átomos de carbono, cicloalquilo de 3 a 6 átomos de carbono, y oxaciclo saturado que tiene 4, 5, o 6 átomos del anillo y un átomo de oxígeno del anillo, cuyo oxaciclo está insustituido o sustituido con 1 o 2 sustituyentes de alquilo de 1 a 4 átomos de carbono independientemente seleccionados, y en donde cada fenilo o heteroarilo comprende al menos un sustituyente no de hidrógeno orto para el punto de unión con el resto del compuesto de la fórmula (I); R4 es hidrógeno o alquilo de 1 a 4 átomos de carbono; R5 es hidrógeno; o R4 y R5 tomados en combinación son oxo; y R6 es hidrógeno en cada presentación, o CR62, tomados en combinación, forman un carbonilo divalente.
ES12743023T 2011-07-22 2012-07-20 Compuestos de tetrahidro-pirido-piridina y tetrahidro-pirido-pirimidina y su uso como moduladores de los receptores de C5a Active ES2637167T3 (es)

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US201161510643P 2011-07-22 2011-07-22
US201161539732P 2011-09-27 2011-09-27
PCT/US2012/047617 WO2013016197A1 (en) 2011-07-22 2012-07-20 Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as c5a receptor modulators

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EP (1) EP2734521B1 (es)
JP (1) JP6040237B2 (es)
KR (1) KR20140096020A (es)
CN (1) CN103814027B (es)
AP (1) AP2014007398A0 (es)
AR (1) AR087288A1 (es)
AU (1) AU2012287183B2 (es)
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