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AR070519A1 - Derivados de piridina como inhibidores de alk-5 y alk-4 - Google Patents

Derivados de piridina como inhibidores de alk-5 y alk-4

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Publication number
AR070519A1
AR070519A1 ARP090100052A ARP090100052A AR070519A1 AR 070519 A1 AR070519 A1 AR 070519A1 AR P090100052 A ARP090100052 A AR P090100052A AR P090100052 A ARP090100052 A AR P090100052A AR 070519 A1 AR070519 A1 AR 070519A1
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AR
Argentina
Prior art keywords
carbon atoms
alkyl
halo
optionally substituted
hydroxy
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ARP090100052A
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English (en)
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Novartis Ag
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Publication of AR070519A1 publication Critical patent/AR070519A1/es

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract

Estos compuestos son utiles para el tratamiento de trastornos inflamatorios u obstructivos de las vías respiratorias, hipertension pulmonar, fibrosis pulmonar, fibrosis hepática, enfermedades musculares y trastornos esqueléticos sistémicos. También se describen composiciones farmacéuticas que contienen los compuestos y procesos para prepararlos. Reivindicacion 1: Un compuesto de formula (1) en forma libre, de sal o de solvato, en donde T1 es un grupo heterocíclico de 4 a 14 miembros o un grupo cicloalquenilo de 4 a 15 átomos de carbono, cada uno, opcionalmente, sustituido con uno, dos o tres sustituyentes que se seleccionan cada uno independientemente de R1, O-R1, cicloalquilo de 3 a 5 átomos de carbono, alquiltio de 1 a 8 átomos de carbono, halo, halo-alquilo de 1 a 8 átomos de carbono, amino, alquilamino de 1 a 8 átomos de carbono, di(alquil de 1 a 8 átomos de carbono)amino, ciano, oxo, hidroxi, carboxi y nitro; T2 es un grupo heterocíclico de 4 a 14 miembros opcionalmente sustituido con uno, dos o tres sustituyentes que se seleccionan cada uno independientemente de R1, R2, R5, O-R1, alcoxicarbonilo de 1 a 8 átomos de carbono, alquiltio de 1 a 8 átomos de carbono, halo, halo-alquilo de 1 a 8 átomos de carbono, amino, alquilamino de 1 a 8 átomos de carbono, di(alquil de 1 a 8 átomos de carbono)amino, ciano, oxo, hidroxi, carboxi y nitro; X se selecciona de CRc, N, O y S, con la condicion de que cuando X sea O o S, Ra esté ausente; Ra y Rb cada uno, independientemente, se selecciona de hidrogeno; OH; NHR10; alquilo de 1 a 8 átomos de carbono opcionalmente sustituido en las posiciones uno, dos o tres, con cicloalquilo de 3 a 10 átomos de carbono opcionalmente sustituido en las posiciones uno o dos, con hidroxi, amino, alquilo de 1 a 8 átomos de carbono, alcoxi de 1 a 8 átomos de carbono, halo, ciano, oxo, carboxi o nitro; y arilo de 6 a 15 átomos de carbono opcionalmente sustituido en las posiciones uno, dos o tres, con halo hidroxi, amino, ciano, oxo, carboxi, nitro o R5; o Ra y Rb junto con X, forman un grupo cíclico de 3, 4, 5 o 6 miembros, opcionalmente sustituido con OH, halo, NR6R7 o R1; Rc se selecciona de H, OH, alquilo de 1 a 8 átomos de carbono y NHR10; R1 es un radical alquilo de 1 a 8 átomos de carbono, alquenilo de 2 a 8 átomos de carbono, cicloalquilo de 3 a 8 átomos de carbono o alquinilo de 2 a 8 átomos de carbono, cada uno opcionalmente sustituido con uno, dos o tres sustituyentes que se seleccionan cada uno independientemente de hidroxi, ciano, amino, halo, R5, -C(=O)-R5, alquilamino de 1 a 8 átomos de carbono, di(alquil de 1 a 8 átomos de carbono)amino, alcanoilamino de 1 a 8 átomos de carbono, alcoxi de 1 a 8 átomos de carbono, -C(=O)NR6R7, -NH(C=O)-alquilo de 1 a 8 átomos de carbono y -SO2NR6R7; R2 es un radical arilo de 6 a 15 átomos de carbono o cicloalquenilo de 4 a 15 átomos de carbono, cada uno opcionalmente sustituido con uno, dos o tres sustituyentes que se seleccionan cada uno independientemente de halo, hidroxi, R1, R5, alquiltio de 1 a 8 átomos de carbono, ciano, C(=O)H, nitro, -O-arilo de 6 a 15 átomos de carbono, halo-alquilo de 1 a 8 átomos de carbono, -NR6R7, -alquil(de 1 a 8 átomos de carbono)-NR6R7, -alquil(de 1 a 8 átomos de carbono)-R5, -O-R1, opcionalmente sustituido con NR6R7, -O-R5, -C(=O)-R5, -C(=O)NR6R7, -C(=O)O-R1, -OC(=O)-R1, -SO2NH2, -SO2-R1, -NH-SO2-alquilo de 1 a 8 átomos de carbono, -C(=O)-NH-R1, -C(=O)-NH-R5, -SO2-arilo de 6 a 15 átomos de carbono, -SO2R5 y -SO2NR6R7; R4 es hidroxi, alcoxi de 1 a 8 átomos de carbono, alquiltio de 1 a 8 átomos de carbono, halo, halo-alquilo de 1 a 8 átomos de carbono, ciano, carboxi, nitro, -N(H)-C(=NH)-NH2, -N(H)-SO2-R2, -R2, -C(=O)R2, -C(=O)-R5, -O-R2, -O-R5, -N(H)-R5, -N(H)-R2, -NR6R7, -C(=O)-R1, -C(=O)-NH2, -SO2R5, -C(=O)-O-R1, -C(=O)-O-R2, -C(=O)O-R5, -SO2-R2 o -C(=O)-N(H)-alquil(de 1 a 8 átomos de carbono)-C(=O)-N(H)-R2; o R4 es un grupo heterocíclico de 4 a 14 miembros, estando dicho grupo sustituido opcionalmente con uno, dos o tres sustituyentes que se seleccionan cada uno independientemente de hidroxi, halo, oxo, ciano, -NR6R7, carboxi, nitro, -N(H)R1, -N(H)-SO2-alquilo de 1 a 8 átomos de carbono, -N(H)-C(=O)-alquil(de 1 a 4 átomos de carbono)-R2, -C(=O)-NH2, -C(=O)-NR6R7, -C(=O)-N(H)-alquil(de 1 a 8 átomos de carbono)-R6, -C(=O)-R2, -C(=O)-R5, alcoxi de 1 a 8 átomos de carbono, alquiltio de 1 a 8 átomos de carbono, cicloalquilo de 3 a 10 átomos de carbono, -C(=O)-R1, halo-alquilo de 1 a 8 átomos de carbono, -R2, -alquil(de 1 a 8 átomos de carbono)R2, -R5, -SO2-alquilo de 1 a 8 átomos de carbono, -SO2-R2, -SO2-R5, -SO2NR6R7 y alquilo de 1 a 8 átomos de carbono opcionalmente sustituido con hidroxi; o R4 es arilo de 6 a 15 átomos de carbono opcionalmente sustituido con uno, dos o tres sustituyentes que se seleccionan cada uno independientemente de hidroxi, alcoxi de 1 a 8 átomos de carbono, -O-arilo de 6 a 15 átomos de carbono y alquilo de 1 a 8 átomos de carbono opcionalmente sustituido con hidroxi; o R4 es cicloalquilo de 3 a 10 átomos de carbono sustituido con uno, dos o tres sustituyentes que se seleccionan cada uno independientemente de hidroxi, -NR6R7, halo, ciano, carboxi, nitro y alquilo de 1 a 8átomos de carbono; R5 es un grupo heterocíclico de 4 a 14 miembros opcionalmente sustituido con uno, dos o tres sustituyentes que se seleccionan cada uno independientemente de oxo, halo, -NR6R7, ciano, hidroxi, carboxi, nitro, -R1, alcoxi de 1 a 8 átomos de carbono, alquiltio de 1 a 8 átomos de carbono, halo-alquilo de 1 a 8 átomos de carbono, -C(=O)-NH2, -SO2-NH2, un grupo éter que contiene 2 a 8 átomos de carbono, y uno, dos o tres átomos enlazados con oxígeno, y un grupo heterocíclico de 4 a 10 miembros que contiene uno o más heteroátomos que se seleccionan independientemente de N, O y S, opcionalmente sustituido con uno o más grupos alquilo de 1 a 6 átomos de carbono; R6 y R7 cada uno independientemente, es hidrogeno, -R1, arilo de 6 a 15 átomos de carbono, -alquil(de 1 a 8 átomos de carbono)-arilo de 6 a 15 átomos de carbono, R5 o -alquil(de 1 a 8 átomos de carbono)-R5; o R6 y R7 junto con el átomo de nitrogeno al que están unidos, forman un anillo heterocíclico de 4 a 10 miembros que contiene opcionalmente uno o más heteroátomos adicionales, que se seleccionan independientemente de N, O y S, en donde el anillo heterocíclico está opcionalmente sustituido con uno o más grupos alquilo de 1 a 6 átomos de carbono; R8 y R9, cada uno independientemente es H, halo, OH, R1, O-R1 o CN; y R10 es H, R1, R2, R5, -SO2-R1, -C(=O)-alquil(de 1 a 4 átomos de carbono)-R2, -C(=O)-NR6R7, -C(=O)-R2, -C(=O)-R5, -C(=O)-R1, -alquil(de 1 a 8 átomos de carbono)-R2, -SO2-R1, -SO2-R2, -SO2-R5 o -SO2NR6R7.
ARP090100052A 2008-01-11 2009-01-08 Derivados de piridina como inhibidores de alk-5 y alk-4 AR070519A1 (es)

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BR112015009751A2 (pt) 2012-10-31 2017-07-11 Bayer Cropscience Ag novos compostos heterocíclicos como pesticidas
JP2017502092A (ja) 2014-01-14 2017-01-19 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． ヘテロアリール及びその使用
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US20090215776A1 (en) 2009-08-27
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