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AR096450A1 - Compuestos para la modulación de quinasas, y sus indicaciones - Google Patents

Compuestos para la modulación de quinasas, y sus indicaciones

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Publication number
AR096450A1
AR096450A1 ARP140102152A ARP140102152A AR096450A1 AR 096450 A1 AR096450 A1 AR 096450A1 AR P140102152 A ARP140102152 A AR P140102152A AR P140102152 A ARP140102152 A AR P140102152A AR 096450 A1 AR096450 A1 AR 096450A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
taken together
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ring
Prior art date
Application number
ARP140102152A
Other languages
English (en)
Inventor
Nespi Marika
G Habets Gaston
N Ibrahim Prabha
Zhang Chao
Spevak Wayne
Shi Songyuan
Burton Betsy
Hirth Klaus-Peter
Original Assignee
Plexxikon Inc
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Publication date
Application filed by Plexxikon Inc filed Critical Plexxikon Inc
Publication of AR096450A1 publication Critical patent/AR096450A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/4353—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
    • 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
    • A61K31/4439—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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se describen compuestos activos sobre proteína quinasas y métodos para regular las vías de proteína quinasas, así como también métodos para usar dichos compuestos para tratar enfermedades y condiciones asociadas con una actividad aberrante de las proteínas quinasas. Útiles para tratar neoplasias, ateroesclerosis, leucemia, infección bacteriana y EPOC. Reivindicación 1: Un compuesto caracterizado porque es de la fórmula (1) o una sal farmacéuticamente aceptable, un solvato, un tautómero o un isómero del mismo, donde: Y es -N(R¹)(R²) o -C(R⁸)(R⁹)(R¹⁰); R¹ y R² son en forma independiente entre sí alquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido; o R¹ y R² tomados junto con el átomo de nitrógeno al cual están unidos forman un heterocicloalquilo de 5 ó 6 miembros opcionalmente sustituido que tiene 0 - 1 heteroátomos adicionales como miembros del anillo seleccionados entre O, N o S; R⁸, R⁹ y R¹⁰ son en forma independiente entre sí H, alquilo C₁₋₆ opcionalmente sustituido, haloalquilo C₁₋₆ opcionalmente sustituido, haloalcoxi C₁₋₆ opcionalmente sustituido, cicloalquilo C₃₋₈ opcionalmente sustituido, arilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido; o dos cualesquiera de los grupos R⁸, R⁹ y R¹⁰ tomados junto con el átomo de carbono al cual se encuentran unidos forman un anillo no aromático de entre 3 y 8 miembros opcionalmente sustituido que tiene entre 0 y 2 heteroátomos como miembros del anillo seleccionados entre N, O ó S; en cada caso con la condición de que al menos dos de los grupos R⁸, R⁹ y R¹⁰ no son simultáneamente hidrógeno; R³ es H o alquilo C₁₋₆; R⁴ es halógeno, hidrógeno, alquilo C₁₋₂, haloalquilo C₁₋₂, CN, haloalcoxi C₁₋₂ o alcoxi C₁₋₂; L es una unión, -C(O)-, -C(S)-, -C(O)NH-, -NHC(O)- o -C(=CH₂)- opcionalmente sustituido, donde dos sustituyentes unidos al mismo carbono de metileno en el grupo -C(=CH₂)- opcionalmente se toman juntos para formar un anillo de 5 ó 6 miembros opcionalmente sustituido que tiene 0 - 4 heteroátomos seleccionados entre O, N o S, donde N y S opcionalmente están oxidados; Z es un arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido, con la condición de que Z no es un núcleo de fórmula (2) opcionalmente sustituido cuando R⁴ se une en posición orto con respecto al sustituyente -L-Z en el anillo fenilo, donde la línea ondulada indica el punto de unión al resto de la molécula; y con la condición de que el compuesto no es 4-[[(1S)-1-ciclopropiletil]amino]-5-[3-[[etil(metil)sulfamoil]amino]-2-fluoro-benzoiI]-7H-pirrolo[2,3-d]pirimidina.
ARP140102152A 2013-05-30 2014-05-30 Compuestos para la modulación de quinasas, y sus indicaciones AR096450A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361829190P 2013-05-30 2013-05-30

Publications (1)

Publication Number Publication Date
AR096450A1 true AR096450A1 (es) 2015-12-30

Family

ID=51023140

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140102152A AR096450A1 (es) 2013-05-30 2014-05-30 Compuestos para la modulación de quinasas, y sus indicaciones

Country Status (18)

Country Link
US (2) US9873700B2 (es)
EP (1) EP3004060B1 (es)
JP (1) JP2016520131A (es)
KR (1) KR20160013028A (es)
CN (1) CN105228983A (es)
AR (1) AR096450A1 (es)
AU (1) AU2014274093B2 (es)
BR (1) BR112015028845A2 (es)
CA (1) CA2912568A1 (es)
HK (1) HK1219732A1 (es)
IL (1) IL242587A0 (es)
MX (1) MX2015015966A (es)
PH (1) PH12015502610A1 (es)
RU (1) RU2015149937A (es)
SG (1) SG11201509338QA (es)
TW (1) TW201533028A (es)
UY (1) UY35596A (es)
WO (1) WO2014194127A1 (es)

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