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AR057993A1 - Compuestos derivados de pirazol 1,2 - Google Patents

Compuestos derivados de pirazol 1,2

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Publication number
AR057993A1
AR057993A1 ARP060105410A ARP060105410A AR057993A1 AR 057993 A1 AR057993 A1 AR 057993A1 AR P060105410 A ARP060105410 A AR P060105410A AR P060105410 A ARP060105410 A AR P060105410A AR 057993 A1 AR057993 A1 AR 057993A1
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AR
Argentina
Prior art keywords
alkyl
group
membered heterocyclic
amino
heterocyclic group
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ARP060105410A
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English (en)
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Novartis Ag
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Publication of AR057993A1 publication Critical patent/AR057993A1/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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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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Abstract

Se describen compuestos de pirazol 1,2, una composicion farmacéutica en base al compuesto y un método de preparacion. Son utiles para el tratamiento de enfermedades inflamatorias. Reivindicacion 1: Un compuesto de formula (1), en forma libre o de sal, en donde: A se selecciona independientemente de CH y por lo menos un nitrogeno; D se selecciona independientemente de CR3 y nitrogeno; R1 y R2 son independientemente H, halogeno o alquilo C1-8, o R1 y R2 junto con el átomo de carbono al cual están unidos, forman un grupo carbocíclico C3-15; R3 se selecciona de alquilo C1-8, halogeno, ciano, hidroxilo, amino, aminoalquilo, amino(di)alquilo, un grupo carbocíclico C3-15, haloalquilo C1-8, alcoxi C1-8-alquilo C1-8, e hidroxialquilo C1-8; R4 se selecciona de halogeno, alquilo C1-8, haloalquilo C1-8, un grupo carbocíclico C3-15, un grupo carbocíclico aromático C6-15, nitro, ciano, alquilsulfonilo C1-8, alquilsulfinilo C1-8, alcoxicarbonilo C1-8, alcoxicarbonilo C1-8, alcoxi C1-8, haloalcoxi C1-8, carboxi, carboxialquilo C1-8, amino, alquilamino C1-8, di(alquilo C1-8)amino, SO2NH2, (alquilamino C1-8)sulfonilo, di(alquilo C1-8)aminosulfonilo, aminocarbonilo, alquilaminocarbonilo C1-8,di(alquil C1-8)aminocarbonilo y un grupo heterocíclico de 4 a 10 miembros; R5 se selecciona del grupo de formulas (2); R5a y R5b son independientemente seleccionados de H, un grupo heterocíclico de 4 a 14 miembros, un grupo carbocíclico C6-15 aromático, un grupo carbocíclico C3-15, y alquilo C1-8 opcionalmente sustituido por un grupo heterocíclico de 4 a 14 miembros o un grupo carbocíclico C3-15, en donde por lo menos uno de R5a o R5b es alquilo C1-8 sustituido por un grupo heterocíclico de 4 a 14 miembros o un grupo carbocíclico C3-15, o R5a y R5b junto con el átomo de nitrogeno al cual están unidos forman un grupo heterocíclico de 4 a 14 miembros, R5c, R5d y R5e se seleccionan independientemente de H, y alquilo C1-8 opcionalmente sustituido por un grupo heterocíclico de 4 a 14 miembros, un grupo carbocíclico aromático C6-15, un grupo carbocíclico C3-15, o R5c junto con R5d y R5e junto con los átomos de nitrogeno a los cuales están unidos y el carbonilo, forman un grupo heterocíclico de 5 a 14 miembros; R5f es H, alquilo C1-8 opcionalmente sustituido por un grupo heterocíclico de 4 a 14 miembros o un grupo carbocíclico C3-15; R5g se selecciona de H, y alquilo C1-8 opcionalmente sustituido por un grupo heterocíclico de 4 a 14 miembros o un grupo carbocíclico C3-15; R5f y R5g junto con el grupo NSO2 al cual están unidos, forman un grupo heterocíclico de 5 a 14 miembros; R5h y R5i se seleccionan independientemente de H. y alquilo C1-8 opcionalmente sustituido por un grupo heterocíclico de 4 a 14 miembros o un grupo carbocíclico C3-15, o R5h y R5i junto con el grupo NCO al cual están unidos, forman un heterociclo de 5 a 14 miembros; R5j y R5k se seleccionan independientemente de H, y alquilo C1-8 opcionalmente sustituido por un grupo heterocíclico de 4 a 14 miembros o un grupo carbocíclico C3-15 o R5j y R5k junto con el átomo de nitrogeno al cual están unidos, forman un grupo heterocíclico de 4 a 14 miembros; R5l, R5m y R5q se seleccionan independientemente de H, y alquilo C1-8 opcionalmente sustituido por un grupo heterocíclico de 4 a 14 miembros o un grupo carbocíclico C3-15, o R5I junto con R5m o R5q junto con los átomos de nitrogeno de la aminosulfonamida a la cual están unidos, forman un grupo heterocíclico de 5 a 14 miembros; la parte cíclica B de los radicales del grupo (2) se selecciona de un grupo heterocíclico de 4 a 14 miembros, un grupo carbocíclico aromático C6-15 y un grupo carbocíclico C3-15; R6 es H o alquilo C1-8; W es un grupo carbocíclico aromático C6-15 o un grupo heterocíclico de 4 a 14 miembros; X es -SO2-, -CH2-, -CON(Y)-, -(V1)-T-(V)-, un grupo heterocíclico de 5 a 14 miembros o un enlace; Y es alquilo C1-8 opcionalmente sustituido por alquilo C1-8, halogeno, oxo, hidroxilo, amino, amino-alquilo C1-8, o amino(di-alquilo C1-8); V1 es alquilo C1-7 opcionalmente sustituido por alquilo C1-8, halogeno, oxo, hidroxilo, amino, amino, amino-alquilo C1-8, amino(di-alquilo C1-8); V es alquilo C1-7 opcionalmente sustituido por alquilo C1-8, halogeno, oxo, hidroxilo, amino, amino-alquilo C1-8, amino(di-alquilo C1-8); T es oxígeno o NR7; R7 es H o alquilo C1-8; en donde cada grupo carbocíclico C3-15, grupo carbocíclico aromático C6-15 y cada grupo heterocíclico de 4 a 14 miembros, a menos que se especifique otra cosa, está independiente y opcionalmente sustituido por uno o más grupos seleccionados de halogeno, oxo, hidroxi, ciano, amino, nitro, carboxi, alquilo C1-8, halo-alquilo C1-8, alcoxi C1-8, alquilcarbonilo C1-8, alquilsulfonilo C1-8, -SO2NH2, (alquilamino C1-8)-sulfonilo, di(alquilo C1-8)aminosulfonilo, aminocarbonilo, alquilaminocarbonilo C1-8 y di(alquilo C1-8)aminocarbonilo, un grupo carbocíclico C3-15, un grupo carbocíclico aromático de 6 a 15 miembros, un grupo heterocíclico de 4 a 14 miembros, cianoalquilo C1-8, hidroxi-alquilo C1-8, haloalquilo C1-8, amino-alquilo C1-8, amino(hidroxi)alquilo C1-8 y alcoxi C1-8 opcionalmente sustituido por aminocarbonilo; m y n son cada uno, independientemente, un entero de 0-3; y p es un entero de 0-4.
ARP060105410A 2005-12-09 2006-12-07 Compuestos derivados de pirazol 1,2 AR057993A1 (es)

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EP (1) EP1963322B1 (es)
JP (1) JP4870166B2 (es)
KR (1) KR101020341B1 (es)
CN (1) CN101326183B (es)
AR (1) AR057993A1 (es)
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MY144903A (en) 2004-06-17 2011-11-30 Novartis Ag Pyrrolopyridine derivatives and their use as crth2 antagonists
KR101411820B1 (ko) 2006-08-07 2014-06-24 액테리온 파마슈티칼 리미티드 (3-아미노-1,2,3,4-테트라하이드로-9ｈ-카르바졸-9-일)-아세트산 유도체
WO2009061730A2 (en) * 2007-11-05 2009-05-14 Array Biopharma Inc. 4-heteroaryl-substituted phenoxyphenylacetic acid
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