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AR077033A1 - Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas - Google Patents

Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas

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Publication number
AR077033A1
AR077033A1 ARP100102023A ARP100102023A AR077033A1 AR 077033 A1 AR077033 A1 AR 077033A1 AR P100102023 A ARP100102023 A AR P100102023A AR P100102023 A ARP100102023 A AR P100102023A AR 077033 A1 AR077033 A1 AR 077033A1
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AR
Argentina
Prior art keywords
alkyl
halogen
optionally substituted
link
independently
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ARP100102023A
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English (en)
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Hoffmann La Roche
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Publication of AR077033A1 publication Critical patent/AR077033A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Una composicion farmacéutica que incluye un compuesto de la formula 1 y métodos para el uso del mismo. Reivindicacion 1: Un compuesto de la formula (1): los estereoisomeros o las sales farmacéuticamente aceptables del mismo, en la que: A es CR3 o N; B y D son con independencia CR15 o N, dichos B y D no pueden ser N al mismo tiempo; R1 es con independencia H, halogeno, alquilo C1-3, cicloalquilo C3-4, -CF3, -OR6, -SR6, -OCF3, -CN, -NO2, -NR6SO2R7, -NR6C(O)R7 o -NR6R7, en la que dos R1 no pueden ser H al mismo tiempo y dichos alquilo y cicloalquilo están opcionalmente sustituidos por halogeno, OR6, -NR6R7 o fenilo; R2 y R3 son con independencia H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halogeno, -(alquilo C0-3)CN, -(alquilo C0-3)OR8, -(alquilo C0-3)SR8, -(alquilo C0-3)NR8R9, -(alquilo C0-3)CF3, -O(alquilo C0-3)CF3, -(alquilo C0-3)NO2, -(alquilo C0-3)C(O)R8, -(alquilo C0-3)C(O)OR8, -(alquilo C0-3)C(O)NR8R9, -(alquilo C0-3)NR8C(O)R9, -(alquilo C0-3)S(O)1-2R8, -(alquilo C0-3)NR8S-(O)1-2R9, -(alquilo C0-3)S-(O)1-2NR8R9, -(alquilo C0-3)(cicloalquilo C3-6), -(alquilo C0-3) (heterociclilo de 3-6 eslabones), -(alquilo C0-3)-(heteroarilo de 5-6 eslabones) o -(alquilo C0-3)fenilo, en la que y R3 están opcionalmente sustituidos con independencia por R10; R4 es H, -NH2, -NH-, -OH, -SH, -NR6C(O)-, -NR6C(O)O-, -NR6C(O)NR7-, -NR6S(O)1-2- o -NR6S(O)1-2NR7-. R5 está ausente, es alquilo C1-6, cicloalquilo C3-6, fenilo, heterociclilo de 3-7 eslabones o heteroarilo de 5-6 eslabones, dicho R5 está opcionalmente sustituido por R10; R6 y R7 son en cada caso con independencia H o alquilo C1-3, opcionalmente sustituido por halogeno, oxo o -NR11R12; o R6 y R7 junto con el átomo al que están unidos forman con independencia un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo, -NR11R12 o alquilo C1-3; R8 y R9 son en cada caso con independencia H, alquilo C1-3, cicloalquilo C3-6, fenilo, heterociclilo de 3-6 eslabones o heteroarilo de 5-6 eslabones, opcionalmente sustituido por R10; o R8 y R9 junto con el átomo al que están unidos forman con independencia un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo, -NR11R12 o alquilo C1-3; R10 es con independencia H, oxo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halogeno, -(alquilo C0-3)CN, -(alquilo C0-3)OR11, -(alquilo C0-3)SR11, -(alquilo C0-3)NR11R12, -(alquilo C0-3)CF3, -(alquilo C0-3)NO2, -(alquilo C0-3)C(O)R11, -(alquilo C0-3)C(O)ORH, -(alquilo C0-3)-C(O)NR11R12, -(alquilo C0-3)NR11C(O)R12, -(alquilo C0-3)-S(O)1-2R11, -(alquilo C0-3)NR11S(O)1-2R12, -(alquilo C0-3)-S(O)1-2NR11R12, -(alquilo C0-3) (ciclo-alquilo C3-6) , -(alquilo C0-3)(heterociclilo de 3-6 eslabones), -(alquilo C0-3)C(O)-(heterociclilo de 3-6 eslabones), -(alquilo C0-3) (heteroarilo de 5-6 eslabones) o -(alquilo C0-3)fenilo, dicho R10 está opcionalmente sustituido con independencia por halogeno, alquilo C1-3, oxo, -CF3, -(alquilo C0-3)OR13, -(alquilo C0-3)NR13R14, -(alquilo C0-3)C(O)R13 o -(alquilo C0-3)S(O)1-2R13; R11 y R12 son con independencia H, alquilo C1-6, -(alquilo C0-3) (cicloalquilo C3-6) , -(alquilo C0-3) -(heterociclilo de 3-6 eslabones), -(alquilo C0-3) (heteroarilo de 5-6 eslabones) o -(alquilo C0-3)fenilo, opcionalmente sustituido por halogeno, oxo, -OR13, -SR13, -NR13R14, alquilo C1-3, -(alquilo C0-3) (cicloalquilo C3-6), -(alquilo C0-3)-fenilo, -(alquilo C0-3) (heterociclilo de 3-6 eslabones) o -(alquilo C0-3)(heteroarilo de 5-6 eslabones); o R11 y R12 junto con el átomo al que están unidos forman un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo, -NR13R14 o alquilo C1-3; R13 y R14 son con independencia H, alquilo C1-6, OH u OCH3, opcionalmente sustituido por halogeno, -NH2, -N(CH3)2, fenilo u oxo, dicho fenilo está opcionalmente sustituido por halogeno, alquilo C1-6, CF3, -NRaRb u ORa; o R13 y R14 junto al átomo al que están unidos forman un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo, -NH2, -N(CH3)2 o alquilo C1-3; R15 es con independencia H, halogeno, alquilo C1-3, alquenilo C1-3, alquinilo C1-3, cicloalquilo C3-4, -CF3, -ORa, -SRa, -CN, -NO2, -NRaSO2Rb, -NRaC(O)Rb o -NRaRb; Ra y Rb son con independencia H o alquilo C1-6 opcionalmente sustituido por halogeno u oxo; o Ra y Rb junto al átomo al que están unidos forman un heterociclilo de 3-6 eslabones, opcionalmente sustituido por halogeno, oxo o alquilo C1-3; con las condiciones siguientes: si R4 es -OH, R5 está ausente, y uno de B y D es N y el otro es CH, entonces la porcion de la formula 1 que tiene la estructura: (2), es diferente de (3) si la porcion de la formula 1 que tiene la estructura: (4) es (5), entonces la porcion de la formula 1 que tiene la estructura: (2) es diferente de las siguientes: (6); si la porcion de la formula 1 que tiene la estructura: (4) es (7), entonces la porcion de la formula 1 que tiene la estructura: (2) es diferente de las siguientes: (8), si A es CR3, B y D son CH, o B es CH y D es N, un R1 es -CH3 y el otro R1 es H, R2 es H, R4 es H o Cl; R5 está ausente; R3 es diferente de la estructura: (9); si A es CR3, B y D son CH, un R1 es F y el otro R1 es H, R2 es H, R4 es H o Cl; R5 está ausente; R3 es diferente de 3-cloro-piridin-2-ilo; si A es CR3, B es N; D es CH, un R1 es -CH3 y el otro R1 es H; R2 y son H; R5 está ausente; R4 es diferente de OH; y si A es CR3, B es CH, D es N, R1 es Cl, R2 y R3 son H, R4 es -NH-, R5 es diferente de la estructura: (10), en las que la línea ondulada representa el punto de union a la formula 1.
ARP100102023A 2009-06-11 2010-06-09 Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas AR077033A1 (es)

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US18632209P 2009-06-11 2009-06-11

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Country Link
US (1) US8486950B2 (es)
EP (1) EP2440529A1 (es)
JP (1) JP5763057B2 (es)
KR (1) KR101530117B1 (es)
CN (1) CN102459187B (es)
AR (1) AR077033A1 (es)
AU (1) AU2010258597B2 (es)
BR (1) BRPI1011129A2 (es)
CA (1) CA2764728A1 (es)
IL (1) IL216511A0 (es)
MX (1) MX2011012840A (es)
SG (1) SG176781A1 (es)
TW (1) TW201103904A (es)
WO (1) WO2010142752A1 (es)

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IL216511A0 (en) 2012-02-29
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AU2010258597A1 (en) 2011-12-15
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