AR077505A1 - Compuestos de piridina y sus usos - Google Patents

Compuestos de piridina y sus usos

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Publication number
AR077505A1
AR077505A1 ARP100102732A ARP100102732A AR077505A1 AR 077505 A1 AR077505 A1 AR 077505A1 AR P100102732 A ARP100102732 A AR P100102732A AR P100102732 A ARP100102732 A AR P100102732A AR 077505 A1 AR077505 A1 AR 077505A1
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AR
Argentina
Prior art keywords
carbon atoms
alkyl
optionally substituted
halo
group
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ARP100102732A
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English (en)
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Novartis Ag
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Publication of AR077505A1 publication Critical patent/AR077505A1/es

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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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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
    • C07D213/72—Nitrogen atoms
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D241/20—Nitrogen atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Reproductive Health (AREA)

Abstract

También se proporciona un método para el tratamiento de una enfermedad o condicion mediada por CDK9. Composiciones farmacéuticas. Reivindicacion 1: Un compuesto de la formula (1): o una sal farmacéuticamente aceptable del mismo, en donde: A1 es N o CR6; A2 es N, N(O) o CR7; A3 es N o CR8; A4 se selecciona a partir de un enlace, SO2, NR9, u O; L se selecciona a partir de un enlace, alquilo de 1 a 4 átomos de carbono opcionalmente sustituido, cicloalquilo de 3 a 6 átomos de carbono, hetero-cicloalquilo de 3 a 6 átomos de carbono, o alquenilo de 2 a 4 átomos de carbono; R1 es X-R16; X es un enlace, o alquilo de 1 a 4 átomos de carbono, y R16 se selecciona a partir del grupo que consiste en alquilo de 1 a 6 átomos de carbono, alquilo ramificado de 3 a 6 átomos de carbono, cicloalquilo de 3 a 8 átomos de carbono, hetero-cicloalquilo, cicloalquilo parcialmente insaturado de 3 a 8 átomos de carbono, arilo, y heteroarilo; en donde R16 está sustituido con uno a tres grupos independientemente seleccionados a partir de halogeno, hidrogeno, alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, alquilo ramificado de 3 a 6 átomos de carbono, halo-alquilo ramificado de 3 a 6 átomos de carbono, OH, alcoxilo de 1 a 6 átomos de carbono, R22-OR12, S(O)0-2R12, R22-S(O)0-2R12, S(O)2NR13R14, R22-S(O)2NR13R14, C(O)OR12, R22-C(O)OR12, C(O)R19, R22-C(O)R19, O-C1-3 alquilo, OC1-3 halo-alquilo, OC(O)R19, R22-OC(O)R19, C(O)NR13R14, R22-C(O)NR13R14, NR15S(O)2R12, R22-NR15S(O)2R12, NR17R18, R22-NR17R18, NR15C(O)R19, R22-NR15C(O)R19, NR15C(O)OCH2Ph, R22-NR15C(O)OCH2Ph, NR15C(O)OR12, R22-NR15C(O)OR12, NR15C(O)NR13R14, y R22-NR15C(O)NR13R14; R17 y R18 se seleccionan cada uno independientemente a partir del grupo que consiste en hidrogeno, hidroxilo, alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, alquilo ramificado de 3 a 6 átomos de carbono, cicloalquilo de 3 a 6 átomos de carbono, R22-OR12, R22-S(O)0-2R12, R22-S(O)2NR13R14, R22-C(O)OR12, R22-C(O)R19, R22OC(O)R19, R22C(O)NR13R14, R22-NR15S(O)2R12, R22-NR23R24, R22-NR15C(O)R19, R22-NR15C(O)OCH2Ph, R22-NR15C(O)OR12, R22-NR15C(O)NR13R14, cicloalquilo, hetero-cicloalquilo y heteroarilo; de una manera alternativa, R17 y R18, junto con el átomo de nitrogeno con el que están unidos, se pueden tomar juntos para formar un anillo heterocíclico de cuatro a seis miembros, en donde los átomos de carbono de este anillo están opcionalmente sustituidos con R20, y los átomos de nitrogeno de este anillo están opcionalmente sustituidos con R21; R19 se selecciona a partir de alquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, hetero-cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, y heteroarilo opcionalmente sustituido; R20 se selecciona a partir del grupo que consiste en alquilo de 1 a 6 átomos de carbono, o halo-alquilo de 1 a 6 átomos de carbono; R21 se selecciona a partir del grupo que consiste en alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono; C(O)R12, C(O)OR12, S(O)2R12; R22 se selecciona a partir del grupo que consiste en alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, alquilo ramificado de 3 a 6 átomos de carbono, halo-alquilo ramificado de 3 a 6 átomos de carbono; R23 y R24 se seleccionan cada uno independientemente a partir del grupo que consiste en hidrogeno, alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, alquilo ramificado de 3 a 6 átomos de carbono, halo-alquilo ramificado de 3 a 6 átomos de carbono; R2 se selecciona a partir del grupo que consiste en alquilo de 1 a 6 átomos de carbono opcionalmente sustituido, alquilo ramificado de 3 a 6 átomos de carbono opcionalmente sustituido, cicloalquilo de 3 a 8 átomos de carbono opcionalmente sustituido, hetero-cicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, y heteroarilo opcionalmente sustituido; R4, R5, y R6 se seleccionan cada uno independientemente a partir del grupo que consiste en hidrogeno, hidroxilo, ciano, halogeno, alquilo de 1 a 4 átomos de carbono, halo-alquilo de 1 a 4 átomos de carbono, alquenilo de 2 a 4 átomos de carbono, alquinilo de 2 a 4 átomos de carbono, amino, NR10R11, y alcoxilo; R3, R7 y R8 se seleccionan cada uno independientemente a partir del grupo que consiste en hidrogeno, hidroxilo, ciano, halogeno, alquilo, halo-alquilo, alquenilo, alquinilo, alcoxilo, NR10R11, C(O)R12, C(O)OR12, C(O)NR13R14, S(O)0-2R12', S(O)0-2NR13R14, y cicloalquilo de 3 a 4 átomos de carbono opcionalmente sustituido; R9 se selecciona a partir del grupo que consiste en hidrogeno, alquilo de 1 a 4 átomos de carbono, alcoxilo, C(O)R12, C(O)OR15, C(O)NR13R14, S(O)0-2R12', S(O)0-2NR13R14, cicloalquilo de 3 a 4 átomos de carbono opcionalmente sustituido, y hetero-cicloalquilo opcionalmente sustituido; R10 y R11 se seleccionan cada uno independientemente a partir del grupo que consiste en hidrogeno, hidroxilo, alquilo, alcoxilo, C(O)R12, C(O)OR12, C(O)NR13R14, S(O)0-2R12, y S(O)0-2NR13R14; de una manera alternativa, R10 y R11, junto con el átomo de nitrogeno con el que están unidos, se pueden tomar juntos para formar un anillo heterocíclico heteroaromático o no aromático de cuatro a seis miembros opcionalmente sustituido; R12 y R15 se seleccionan cada uno individualmente a partir del grupo que consiste en hidrogeno, alquilo, alquilo ramificado, halo-alquilo, halo-alquilo ramificado, (CH2)0-3-cicloalquilo, (CH2)0-3-hetero-cicloalquilo, (CH2)0-3-arilo, y heteroarilo; R13 y R14 se seleccionan cada uno independientemente a partir del grupo que consiste en hidrogeno, hidroxilo, alquilo, alquilo ramificado, halo-alquilo, halo-alquilo ramificado, alcoxilo, cicloalquilo o hetero-cicloalquilo; y de una manera alternativa, R13 y R14, junto con el átomo de nitrogeno con el que están unidos, se pueden tomar juntos para formar un anillo heterocíclico heteroaromático o no aromático de cuatro a seis miembros opcionalmente sustituido.
ARP100102732A 2009-07-30 2010-07-28 Compuestos de piridina y sus usos AR077505A1 (es)

Applications Claiming Priority (2)

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