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AR054529A1 - Derivados de benzazepina como moduladores del receptor de 5-hidroxi-triptamina 6 - Google Patents

Derivados de benzazepina como moduladores del receptor de 5-hidroxi-triptamina 6

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Publication number
AR054529A1
AR054529A1 ARP060102857A ARP060102857A AR054529A1 AR 054529 A1 AR054529 A1 AR 054529A1 AR P060102857 A ARP060102857 A AR P060102857A AR P060102857 A ARP060102857 A AR P060102857A AR 054529 A1 AR054529 A1 AR 054529A1
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AR
Argentina
Prior art keywords
alkyl
haloalkyl
halogen
cor11
so2r11
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ARP060102857A
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Astrazeneca Ab
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Publication of AR054529A1 publication Critical patent/AR054529A1/es

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    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16Benzazepines; Hydrogenated benzazepines
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    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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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    • C07D401/00Heterocyclic 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
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    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Procesos para su preparacion, intermediarios usados en su preparacion, composiciones farmacéuticas que contienen dichos compuestos y al uso de dichos compuestos en la terapia médica. Reivindicacion 1: Un compuesto de formula (1) donde: Q es arilC6- 10alquiloC0-6, heteroarilC5-11alquiloC0-6, cicloalquilC3-7alquiloC0-6, heterocicloalquilC3-7alquiloC0-6 o alquiloC1-10; R1 es H, hidroxilo, halogeno, alquiloC1-10, alqueniloC2-10, alquiniloC2-10, alcoxiC1-10, N(R10) 2, arilC6-10alquiloC0-6, heteroarilC5-6alquiloC0-6, haloalquiloC1-6, haloalquilC1-6O, R8OalquiloC0-6, CN, SR7, R7SO2alquiloC0-6, SO2R7, R7CON(R8)alquiloC0-6, NR8SO2R7, COR7, COOR8, OSO2R8, (R8)2NCOalquiloC0-6, SO2N(R8)2, N(R8)CON(R8)2, NO2, cicloalquiloC3-6, heterocicloalquiloC3-6 u oxo; n es 0, 1, 2, 3, 4, o 5; B es O, N(R6)2, o B es NR6 dentro de un heteroariloC5-11 donde R6 forma un anillo con Q; X es O, CH2, CO, S, SO, SO2 o NR12; R2 es H, hidroxilo, halogeno, alquiloC1-10, alqueniloC2-10, alquiniloC2-10, alcoxiC1-10, N(R10)2, arilC6-10alquiloC0-6, heteroarilC5-6alquiloC0-6, haloalquiloC1-6, haloalquilC1-6O, R7OalquiloC0-6, CN, SR7, SO2R8, SOR7, N(R8)COR7, N(R8) SO2R7, COR7, COOR7, OSO2R7, CON(R8)2 o SO2N(R8)2; R3 es H, alquiloC1-10, alqueniloC2-10, alquiniloC2-10, arilC6-10alquiloC0-6, heteroarilC5-6alquiloC0-6, haloalquiloC1-6 o R7OalquiloC1-6; R4 es H, alquiloC1-5, haloalquiloC1-5, alcoxiC1-5 o haloalcoxiC1-5 y puede estar sustituido con 1 o varios grupos seleccionados independientemente de halogeno, hidroxilo, ciano, alquiloC1-3 y alcoxiC1-3; o R3 y R4 juntos forman un heterocicloalquiloC3-7, el cual puede estar sustituido con 1 o varios grupos seleccionados independientemente de H, halogeno, alquiloC1-6, haloalquiloC1-6, COR11, SO2R11, OR11, ciano, oxo y SO2N(R10)2; R5 es H, alquiloC1-6, alcoxiC1-6, haloalcoxiC1-6 o haloalquiloC1-6; o R4 y R5 juntos forman un heterocicloalquiloC3-7 o un cicloalquiloC3-7, el cual puede estar sustituido con 1 o varios grupos seleccionados independientemente de H, halogeno, alquiloC1-6, haloalquiloC1-6, COR11, SO2R11, OR11, ciano, oxo y SO2N(R10)2; R6 es H, alquiloC1-6, cicloalquilC3-6alquiloC0-6, R7OalquiloC1-6, haloalquiloC1-6, cianoalquiloC1-6, (R10)2NCOalquiloC0-6 o R11SO2alquiloC1-6; R7 es alquiloC1-6, arilC6-10alquiloC0-6, heteroarilC5-6alquiloC0-6, cicloalquilC3-7alquiloC0-6 o haloalquiloC1-6; R8 es H, alquiloC1-6, haloalquiloC1-6, cicloalquilC3-7alquiloC0-6, arilC6-10alquiloC0-6 o heteroarilC5-6alquilC0-6; o R7 y R8 juntos forman un heteroariloC5-6 o un heterocicloalquiloC3-7; donde cualquier arilo y heteroarilo bajo R1, R3, R7 y R8 puede estar sustituido con 1 o varios grupos seleccionados independientemente de H, halogeno, hidroxilo, haloalquiloC1-6, CN, OR10, alquiloC1-6, oxo, SR10, CON(R10)2, N(R10)COR11, SO2R11, SOR11, N(R10)2 y COR11; R9 es H, hidroxilo, halogeno, alquiloC1-6, alcoxiC1-6alquiloC0-3, haloalquiloC1-6, COR11, CON(R10)2, N(R10)COR11, SR10 SOR11, CN o SO2R11; R10 es H, alquiloC1-6 o haloalquiloC1-6; R11 es alquiloC1-6 o haloalquiloC1-6; o R10 y R11 juntos forman un heterocicloalquiloC3-7, el cual puede estar sustituido con uno o varios grupos seleccionados independientemente de H, halogeno, hidroxilo, alquiloC1-3, alcoxiC1-3 y ciano; y R12 es H, alquiloC1-6, haloalquiloC1-6, COR11 o SO2R11; o sus sales, solvatos o sales solvatadas.
ARP060102857A 2005-07-05 2006-07-03 Derivados de benzazepina como moduladores del receptor de 5-hidroxi-triptamina 6 AR054529A1 (es)

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US (1) US20100105657A1 (es)
EP (1) EP1910321A4 (es)
JP (1) JP2009501705A (es)
CN (1) CN101258135A (es)
AR (1) AR054529A1 (es)
WO (1) WO2007004959A1 (es)

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JP5756457B2 (ja) 2009-04-06 2015-07-29 アジオス ファーマシューティカルズ, インコーポレイテッド ピルビン酸キナーゼm2調節剤、治療組成物および関連する使用方法
PL2427441T3 (pl) 2009-05-04 2017-06-30 Agios Pharmaceuticals, Inc. Aktywatory PKM2 do stosowania w leczeniu raka
JP5764555B2 (ja) 2009-06-29 2015-08-19 アジオス ファーマシューティカルズ, インコーポレイテッド 治療組成物および関連する使用方法
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JP5837091B2 (ja) 2010-12-17 2015-12-24 アジオス ファーマシューティカルズ, インコーポレイテッド ピルビン酸キナーゼm2(pkm2)調節剤としての新規n−(4−(アゼチジン−1−カルボニル)フェニル)−(ヘテロ−)アリールスルホンアミド誘導体
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EP1910321A1 (en) 2008-04-16
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US20100105657A1 (en) 2010-04-29
CN101258135A (zh) 2008-09-03
JP2009501705A (ja) 2009-01-22

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