AR080765A1 - Derivado de piridina y pirazina para el tratamiento de fibrosis quistica (cf) - Google Patents

Derivado de piridina y pirazina para el tratamiento de fibrosis quistica (cf)

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Publication number
AR080765A1
AR080765A1 ARP110100866A ARP110100866A AR080765A1 AR 080765 A1 AR080765 A1 AR 080765A1 AR P110100866 A ARP110100866 A AR P110100866A AR P110100866 A ARP110100866 A AR P110100866A AR 080765 A1 AR080765 A1 AR 080765A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
heterocyclic group
aryl
halogen atoms
Prior art date
Application number
ARP110100866A
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English (en)
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Novartis Ag
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44647718&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR080765(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR080765A1 publication Critical patent/AR080765A1/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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  • Pyridine Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Los cuales restablecen o mejoran la funcion del regulador de conductancia transmembrana de fibrosis quística (CFTR) mutante y/o de tipo silvestre, para el tratamiento de fibrosis quística, dipielesia ciliar primaria, bronquitis cronica, enfermedad pulmonar obstructiva cronica, asma, infecciones del tracto respiratorio, carcinoma pulmonar, xerostomia y queratoconjuntivitis sire, o estrenimiento (síndrome de intestino irritable (IBS), enfermedad de intestino irritable (IBD), inducido por opioide). También se abarcan composiciones farmacéuticas que comprenden tales derivados. Reivindicacion 1: Un compuesto de la formula (1) o sales farmacéuticamente aceptables del mismo, en donde: A es N o CR4a; R1 es H; alquilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno; alquenilo C2-8; alquinilo C2-8; cicloalquilo C3-10; cicloalquenilo C5-10; -alquilo C1-4-cicloalquilo C3-8; alcoxilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno; halogeno; SO2NR8R9; SO2R10; S-alquilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno; S-arilo C6-14; CN; NR11R12; C(O)NR13R14; NR13SO2R15; NR13C(O)R15; CO2R15; -(alquilo C0-4)-arilo C6-14; o -(alquilo C0-4)-grupo heterocíclico de 3 a 14 miembros, en donde el grupo heterocíclico contiene cuando menos un heteroátomo seleccionado a partir de N, O y S; en donde los grupos cicloalquilo, cicloalquenilo, arilo, y heterociclilo están cada uno opcionalmente sustituidos por uno o más sustituyentes Z; R2 es halo-alquilo C1-4; R3 y R4a son cada uno independientemente H o alquilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno; R4 es H, o alquilo C1-8 opcionalmente sustituido con uno o más átomos de halogeno; R5 es (CH2)m-NR17R18, -(CH2)m-OR'; alcoxilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno; -(alquilo C0-4)-CO2R15; -(alquilo C0-4)-arilo C6-14 o -grupo heterocíclico de 3 a 14 miembros, en donde el grupo heterocíclico contiene cuando menos un heteroátomo seleccionado a partir de N, O y S; en donde el -(alquilo C0-4)-arilo C6-14, y -(alquilo C0-4)-grupo heterocíclico de 3 a 14 miembros, están cada uno opcionalmente sustituidos por uno o más sustituyentes Z; R6 es alquilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno; cicloalquilo C3-10; -alquilo C1-4-cicloalquilo C3-8; alcoxilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno; OH; CN; halogeno; -(alquilo C0-4)-arilo C6-14; o -(alquilo C0-4)-grupo heterocíclico de 3 a 14 miembros, en donde el grupo heterocíclico contiene cuando menos un heteroátomo seleccionado a partir de N, O y S; en donde el cicloalquilo, cicloalquenilo, -(alquilo C0-4)-arilo C6-14, y -(alquilo C0-4)-grupo heterocíclico de 3 a 14 miembros, están cada uno opcionalmente sustituidos por uno o más sustituyentes Z; o R6 es H, y R5 es -(CH2)m-NR17R18, -(CH2)m-OR', alcoxilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno; -(alquilo C0-4)-arilo C6-14; -(alquilo C0-4)-grupo heterocíclico de 3 a 14 miembros, en donde el grupo heterocíclico contiene cuando menos un heteroátomo seleccionado a partir de N, O y S; o -(alquilo C0-4)-CO2R15, en donde los grupos -(alquilo C0-4)-arilo C6-14, y -(alquilo C0-4)-grupo heterocíclico de 3 a 14 miembros están cada uno opcionalmente sustituidos por uno o más sustituyentes Z; o R4 y R6 junto con los átomos de carbono con los que están unidos, forman un sistema de anillo carbocíclico de 3 a 8 miembros; o R4 y R5 forman juntos un grupo oxo (C=O), y R6 es alquilo C1-4 opcionalmente sustituido por uno o más átomos de halogeno; alcoxilo C1-4 opcionalmente sustituido por uno o más átomos de halogeno; -(alquilo C0-4)-arilo C6-14; o -(alquilo C0-4)-grupo heterocíclico de 3 a 14 miembros, en donde el grupo heterocíclico contiene cuando menos un heteroátomo seleccionado a partir de N, O, y S, en donde los grupos arilo y heterociclilo están cada uno opcionalmente sustituidos por uno o más sustituyentes Z; o R5 y R6 junto con los átomos de carbono con los que están enlazados, forman un sistema de anillo heterocíclico de 5 a 8 miembros que contiene uno o más heteroátomos seleccionados a partir de N, O, y S, en donde el sistema de anillo está opcionalmente sustituido por uno o más sustituyentes Z; o R4 y R5 y R6 junto con los átomos de carbono con los que están unidos, forman un sistema de anillo heterocíclico de 5 a 8 miembros que contiene uno o más heteroátomos seleccionados a partir de N, O, y S, en donde el sistema de anillo está opcionalmente sustituido por uno o más sustituyentes Z; R' es H, o alquilo C1-8 opcionalmente sustituido con uno o más átomos de halogeno; m es 0, 1, 2 o 3; R8, R11, R13 y R17 son cada uno independientemente H, alquilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno, cicloalquilo C3-10 o -(alquilo C1-4)-cicloalquilo C3-8; R9, R10, R12, R14, R15, R16 y R18 son cada uno independientemente H; alquilo C1-8 opcionalmente sustituido por uno o más átomos de halogeno; alquenilo C2-8; alquinilo C2-8; cicloalquilo C3-10; cicloalquenilo C5-10; -alquilo C1-4-cicloalquilo C3-8; -(alquilo C0-4)-arilo C6-14; o -(alquilo C0-4)-grupo heterocíclico de 3 a 14 miembros, en donde el grupo heterocíclico contiene cuando menos un heteroátomo seleccionado a partir de N, O, y S, en donde los grupos cicloalquilo, cicloalquenilo, arilo, y heterociclilo están cada uno opcionalmente sustituidos por uno o más sustituyentes Z; o R8 y R9, R11 y R12, R13 y R14, y R17 y R18, junto con el átomo de nitrogeno con el que están unidos, pueden formar un grupo heterocíclico de 4 a 14 miembros opcionalmente sustituido por uno o más sustituyentes Z; Z es independientemente OH, arilo, O-arilo, bencilo, O-bencilo, alquilo C1-6 opcionalmente sustituido por uno o más grupos OH o grupos NH2, alquilo C1-6 opcionalmente sustituido por uno o más átomos de halogeno, alcoxilo C1-6 opcionalmente sustituido por uno o más grupos OH, o alcoxilo C1-4, NR18(SO2)R21, (SO2)NR19R21, (SO2)R21, NR18C(O)R21, C(O)NR19R21, NR18C(O)NR19R21, NR18C(O)OR19, NR19R21, C(O)OR19, C(O)R19, SR19, OR19, oxo, CN, NO2, halogeno, o un grupo heterocíclico de 3 a 14 miembros, en donde el grupo heterocíclico contiene cuando menos un heteroátomo seleccionado a partir de N, O y S; R19 y R21 son cada uno independientemente H; alquilo C1-8; cicloalquilo C3-8; alcoxilo C1-4-alquilo C1-4; (alquilo C0-4)-arilo opcionalmente sustituido por uno o más grupos seleccionados a partir de alquilo C1-6, alcoxilo C1-6, y halogeno; (alquilo C0-4)-grupo heterocíclico de 3 a 14 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos seleccionados a partir de N, O, y S, opcionalmente sustituido por uno o más grupos seleccionados a partir de halogeno, oxo, alquilo C1-6, y C(O)-alquilo C1-6; (alquilo C0-4)-O-arilo opcionalmente sustituido por uno o más grupos seleccionados a partir de alquilo C1-6, alcoxilo C1-6, y halogeno; y (alquilo C0-4)-O-grupo heterocíclico de 3 a 14 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos seleccionados a partir de N, O, y S, opcionalmente sustituido por uno o más grupos seleccionados a partir de halogeno. alquilo C1-6, o C(O)-alquilo C1-6; en donde los grupos alquilo están opcionalmente sustituidos por uno o más átomos de halogeno, alcoxilo C1-4, C(O)NH2, C(O)NH-alquilo C1-6 o C(O)N(alquilo C1-6)2; o R19 y R21 junto con el átomo de nitrogeno con el que están unidos, forman un grupo heterocíclico de 5 a 10 miembros, incluyendo el grupo heterocíclico uno o más heteroátomos adicionales seleccionados a partir de N, O, y S, estando el grupo heterocíclico opcionalmente sustituido por uno o más sustituyentes seleccionados a partir de OH; halogeno; arilo; grupo heterocíclico de 5 a 10 miembros que incluye uno o más heteroátomos seleccionados a partir de N, O y S; S(O)2-arilo; S(O)2-alquilo C1-6; alquilo C1-6 opcionalmente sustituido por uno o más átomos de halogeno; alcoxilo C1-6 opcionalmente sustituido por uno o más grupos OH, o alcoxilo C1-4; y C(O)O-alquilo C1-6, en donde los grupos sustituyentes de arilo y heterocíclico están ellos mismos opcionalmente sustituidos por alquilo C1-6, halo-alquilo C1-6, o alcoxilo C1-6.
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