AR072198A1 - Derivados de isoquinolinona como antagonistas de nk3 y composiciones farmaceuticas que los contienen - Google Patents

Derivados de isoquinolinona como antagonistas de nk3 y composiciones farmaceuticas que los contienen

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Publication number
AR072198A1
AR072198A1 ARP090102238A ARP090102238A AR072198A1 AR 072198 A1 AR072198 A1 AR 072198A1 AR P090102238 A ARP090102238 A AR P090102238A AR P090102238 A ARP090102238 A AR P090102238A AR 072198 A1 AR072198 A1 AR 072198A1
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AR
Argentina
Prior art keywords
alkyl
alkynyl
alkenyl
haloalkyl
halogen
Prior art date
Application number
ARP090102238A
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English (en)
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Lundbeck & Co As H
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Publication date
Application filed by Lundbeck & Co As H filed Critical Lundbeck & Co As H
Publication of AR072198A1 publication Critical patent/AR072198A1/es

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    • 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
    • C07D401/04—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
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    • A61P25/22—Anxiolytics
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se proporcionan derivados de isoquinolona de la formula general 1. Los compuestos son antagonistas de NK3 y son utiles para el tratamiento por ejemplo de la psicosis y la esquizofrenia. Reivindicacion 1: Un compuesto de acuerdo con la formula 1 en donde A representa N, CH o CR1; cada R1 independientemente representa hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -C(O)-alquilo C1-6, -C(O)-alquenilo C2-6, -C(O)-alquinilo C2-6, -C(O)-O-alquilo C1-6, -C(O)-O-alquenilo C2-6, -C(O)-O-alquinilo C2-6 o fenilo, en donde dicho fenilo, alquilo C1-6, alquenilo C2-6 o alquinilo C2-6 est  opcionalmente sustituido con uno o m s sustituyentes seleccionados de halogeno, hidroxilo, haloalquilo C1-6, nitro, alcoxi C1-6, y NR2R3; X representa hidrogeno, alquilo C1-6 o -CraRb-X', en donde X' representa un resto monoc¡clico saturado que tiene 5-6  tomos en el anillo uno de los cuales es N y en donde uno o dos  tomos del anillo adicionales pueden ser un hetero tomo seleccionado de N, O y S, dicho anillo monoc¡clico puede estar sustituido con uno o m s sustituyentes W, en donde W se selecciona de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, o (=O); Ra y Rb representan cada uno individualmente hidrogeno, -CH3 o halogeno; Y representa un resto heteroarom tico que tiene 5-6  tomos en el anillo, en donde 1-4 de dichos  tomos del anillo se seleccionan de N, O y S, dicho resto heteroarom tico puede opcionalmente estar benzofusionado, y dicho resto heteroarom tico puede estar sustituido con uno o m s sustituyentes Z, en donde Z se selecciona de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, ciano, halogeno, hidroxi, alcoxi C1-6, haloalquilo C1-6, y NR2R3 en donde cada uno de R2 y R3 independientemente representan hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, hidroxialquilo C1-6, o haloalquilo C1-6; cada uno de R4-R8 y R9-R12 independientemente representan hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halogeno, NR2R3, hidroxi, ciano, nitro, alcoxi C1-6, haloalquilo C1-6 o hidroxialquilo C1-6; y sales farmaceuticamente aceptables del mismo.
ARP090102238A 2008-06-23 2009-06-19 Derivados de isoquinolinona como antagonistas de nk3 y composiciones farmaceuticas que los contienen AR072198A1 (es)

Applications Claiming Priority (1)

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DKPA200800859 2008-06-23

Publications (1)

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AR072198A1 true AR072198A1 (es) 2010-08-11

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US (1) US8415356B2 (es)
EP (1) EP2313391B1 (es)
JP (1) JP2011525517A (es)
KR (1) KR20110026429A (es)
CN (1) CN102123998A (es)
AR (1) AR072198A1 (es)
AU (1) AU2009264365A1 (es)
BR (1) BRPI0914182A2 (es)
CA (1) CA2728283A1 (es)
CO (1) CO6280532A2 (es)
EA (1) EA201170074A1 (es)
ES (1) ES2401059T3 (es)
IL (1) IL209663A0 (es)
MX (1) MX2010013868A (es)
NZ (1) NZ590154A (es)
TW (1) TW201000458A (es)
WO (1) WO2009156339A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008131779A1 (en) 2007-04-26 2008-11-06 H. Lundbeck A/S Isoquinolinone derivatives as nk3 antagonists
US8242134B2 (en) 2008-09-15 2012-08-14 H. Lundbeck A/S Isoquinolinone derivatives as NK3 antagonists
WO2010045948A1 (en) 2008-10-20 2010-04-29 H. Lundbeck A/S Isoquinolinone derivatives as nk3 antagonists
TW201143768A (en) 2009-12-15 2011-12-16 Lundbeck & Co As H Pyridone derivatives as NK3 antagonists
TW201144311A (en) * 2010-03-12 2011-12-16 Lundbeck & Co As H Azaisoquionolinone derivatives as NK3 antagonists
US20110224247A1 (en) * 2010-03-12 2011-09-15 H. Lundbeck A/S Azaisoquinolinone derivatives as nk3 antagonists
WO2012035078A1 (en) * 2010-09-16 2012-03-22 Novartis Ag 17α-HYDROXYLASE/C17,20-LYASE INHIBITORS
CN108484591B (zh) * 2018-05-28 2019-07-02 西安培华学院 用于治疗阿尔茨海默症的化合物及其应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3664492B2 (ja) 1994-05-27 2005-06-29 スミスクライン・ビーチャム・ファーマシューティチ・ソシエタ・ペル・アチオニ タチキニン ｎｋ▲下３▼ 受容体アンタゴニストとしてのキノリン誘導体
GB0318727D0 (en) * 2003-08-08 2003-09-10 Smithkline Beecham Corp Novel compounds
MXPA06001738A (es) 2003-08-15 2006-05-12 Lundbeck & Co As H Derivados de ciclopropilo como antagonistas del receptor nk3.
GB0425077D0 (en) 2004-11-12 2004-12-15 Smithkline Beecham Corp Novel compounds
GB0425076D0 (en) 2004-11-12 2004-12-15 Smithkline Beecham Corp Novel compounds
US20080200500A1 (en) 2005-06-03 2008-08-21 Astrazeneca Ab Quinoline Derivatives as Nk3 Antagonists
WO2008131779A1 (en) 2007-04-26 2008-11-06 H. Lundbeck A/S Isoquinolinone derivatives as nk3 antagonists
US8173639B2 (en) 2007-04-26 2012-05-08 H. Lundbeck A/S Isoquinolinone derivatives as NK3 antagonists
BRPI0917245B8 (pt) 2008-09-15 2021-05-25 H Lundbeck As compostos derivados de isoquinolinona e sua composição farmacêutica
WO2010045948A1 (en) 2008-10-20 2010-04-29 H. Lundbeck A/S Isoquinolinone derivatives as nk3 antagonists

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Publication number Publication date
NZ590154A (en) 2012-05-25
WO2009156339A1 (en) 2009-12-30
CN102123998A (zh) 2011-07-13
MX2010013868A (es) 2011-02-24
US20110130407A1 (en) 2011-06-02
EP2313391A1 (en) 2011-04-27
KR20110026429A (ko) 2011-03-15
US8415356B2 (en) 2013-04-09
BRPI0914182A2 (pt) 2019-09-24
JP2011525517A (ja) 2011-09-22
CO6280532A2 (es) 2011-05-20
CA2728283A1 (en) 2009-12-30
IL209663A0 (en) 2011-02-28
EA201170074A1 (ru) 2011-10-31
EP2313391B1 (en) 2012-12-26
ES2401059T3 (es) 2013-04-16
AU2009264365A1 (en) 2009-12-30
TW201000458A (en) 2010-01-01

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