AR062295A1 - Compuesto de 1h-quinolin-4-ona, procedimientos para su preparacion y composicion farmaceutica - Google Patents

Compuesto de 1h-quinolin-4-ona, procedimientos para su preparacion y composicion farmaceutica

Info

Publication number
AR062295A1
AR062295A1 ARP070103514A ARP070103514A AR062295A1 AR 062295 A1 AR062295 A1 AR 062295A1 AR P070103514 A ARP070103514 A AR P070103514A AR P070103514 A ARP070103514 A AR P070103514A AR 062295 A1 AR062295 A1 AR 062295A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
hydrogen
isoolaryl
oalkyl
Prior art date
Application number
ARP070103514A
Other languages
English (en)
Inventor
Jose Luis Falco
Albert Palomer
Antonio Guglietta
Original Assignee
Ferrer Int
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ferrer Int filed Critical Ferrer Int
Publication of AR062295A1 publication Critical patent/AR062295A1/es

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Classifications

    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/06—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/18—Halogen atoms or nitro radicals
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/06—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 linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

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

Abstract

Los compuestos de formula 1 son utiles en el tratamiento o prevencion de enfermedades asociadas a la modulacion de los receptores GABAA, ansiedad, epilepsia, trastornos del sueno que incluyen insomnio e inducir sedacion-hipnosis, anestesia, sueno y relajacion muscular. La invencion también se refiere al procedimiento de síntesis para la preparacion de dichos compuestos y a una composicion farmacéutica en base al compuesto. Reivindicacion 1: Un compuesto de 1H-quinolin-4-ona caracterizado porque es de formula (1): donde R1 y R2 se seleccionan independientemente del grupo que consiste en hidrogeno, alquilo(C1-6), Oalquilo(C1-6), halogeno y fenilo; R3 y R4 se seleccionan independientemente del grupo que consiste en hidrogeno y fenilo opcionalmente sustituido con alquilo(C1-6), halogeno y Oalquilo(C1-6); R5 se selecciona del grupo que consiste en NR6R7, N(R8)NH2, OH, OR9, y un anillo heteroarilo seleccionado del grupo que consiste en piridilo, furilo, tienilo, oxazolilo, isoxazolilo, imidazolilo, pirrolilo, pirazolilo, pirimidinilo y pirazinilo, donde cada anillo heteroarilo contiene uno o dos sustituyentes alquilo(C1-6) opcionales; R6 y R7 se seleccionan independientemente del grupo que consiste en hidrogeno; alquilo(C1-6); alquenilo(C2-6); cicloalquilo(C3-6)alquiloC1-6); hidroxialquilo(C1-6); heteroarilo seleccionado del grupo que consiste en piridilo, pirimidilo, pirazinilo, tiazolilo, benzotiazolilo, oxazolilo, benzoxazolilo, isoxazolilo, benzisoxazolilo, pirazolilo, furilo, benzotienilo, tiadiazolilo, pirrolilo, imidazolilo, bencimidazolilo, indolilo, quinolilo e isoquinolilo, donde cada heteroarilo contiene uno o dos cuctituyentes opcionales independientemente del grupo que consiste en alquilo(C1-6), Oalquilo(C1-6), haloalquilo(C1-6), cicloalquilo(C3-6), NO2 y COalquilo(C1-6); tienilalquilo(C1-6), furilalquilo(C1-6), piridilalquilo(C1-6); y ariloseleccionado del grupo que consiste en fenilo e indanilo, donde cada arilo contiene uno o dos sustituyentes opcionales seleccionados del grupo que consiste en alquilo(C1-6), haloalquilo(C1-6), halogeno, Ndialquilo(C1-6), NHalquilo(C1-6), Oalquilo(C1-6), NO2, CN, OH, NH2, COOH, COalquilo(C1-6), COOalquilo(C1-6), CONHalquilo(C1-6), CONdialquilo(C1-6) y COfenilo; o R6 y R7 pueden formar, junto con el átomo de nitrogeno al cual están unidos, un heterociclo seleccionado entre pirrolidina, 3-pirrolina, 1,2,3,6-tetrahidropiridina, piperidina, morfolina, tiomorfolina y piperazina, donde cada heterociclo contiene uno, dos, tres o cuatro sustituyentes opcionales seleccionados del grupo que consiste en OH, alquilo(C1-6) y COalquilo(C1-6); R8 se selecciona del grupo que consiste en hidrogeno y alquilo(C1-6); y R9 es alquilo(C1-6); con la condicion de que R3 y R4 no pueden ser simultaneamente hidrogeno; y las sales farmacéuticamente aceptables e hidratos de los mismos.
ARP070103514A 2006-08-10 2007-08-09 Compuesto de 1h-quinolin-4-ona, procedimientos para su preparacion y composicion farmaceutica AR062295A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP06118720A EP1886996A1 (en) 2006-08-10 2006-08-10 1H-Quinolin-4-one compounds, with affinity for the GABA receptor, processes, uses and compositions

Publications (1)

Publication Number Publication Date
AR062295A1 true AR062295A1 (es) 2008-10-29

Family

ID=37651083

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070103514A AR062295A1 (es) 2006-08-10 2007-08-09 Compuesto de 1h-quinolin-4-ona, procedimientos para su preparacion y composicion farmaceutica

Country Status (13)

Country Link
US (1) US20100168099A1 (es)
EP (1) EP1886996A1 (es)
CN (1) CN101522630A (es)
AR (1) AR062295A1 (es)
AT (1) ATE512138T1 (es)
BR (1) BRPI0715817A2 (es)
CL (1) CL2007002324A1 (es)
DK (1) DK2064185T3 (es)
PT (1) PT2064185E (es)
RU (1) RU2009108361A (es)
SI (1) SI2064185T1 (es)
TW (1) TW200833665A (es)
UY (1) UY30529A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI366565B (en) 2007-06-06 2012-06-21 Otsuka Pharma Co Ltd Quinolone compound and pharmaceutical composition
TWI492943B (zh) * 2008-12-05 2015-07-21 大塚製藥股份有限公司 喹啉酮化合物及藥學組成物（二）
JP5769504B2 (ja) * 2010-06-04 2015-08-26 大塚製薬株式会社 医薬
CN104093310A (zh) 2012-02-03 2014-10-08 泰华制药工业有限公司 拉喹莫德用于治疗一线抗TNFα疗法失败的克罗恩氏病患者的用途
TW201400117A (zh) 2012-06-05 2014-01-01 Teva Pharma 使用拉喹莫德治療眼發炎疾病
TW201410244A (zh) 2012-08-13 2014-03-16 Teva Pharma 用於治療ｇａｂａ媒介之疾病之拉喹莫德（ｌａｑｕｉｎｉｍｏｄ）

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2728900B1 (fr) * 1994-12-29 1997-01-31 Synthelabo Derives de 3-phenylisoquinolein-1(2h)-one, leur preparation et leur application en therapeutique
GB9621757D0 (en) * 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
FR2813791B1 (fr) * 2000-09-14 2004-03-12 Lafon Labor Utilisation de 2- et 4-quinolones pour inhiber la neo-proliferation intimale
ES2319176T3 (es) * 2002-05-14 2009-05-05 The Regents Of The University Of California Acidos quinolona-carboxilicos sustituidos, sus derivados, sitio de accion y uso de los mismos.

Also Published As

Publication number Publication date
EP1886996A1 (en) 2008-02-13
TW200833665A (en) 2008-08-16
ATE512138T1 (de) 2011-06-15
SI2064185T1 (sl) 2011-10-28
CL2007002324A1 (es) 2008-01-18
RU2009108361A (ru) 2010-09-20
PT2064185E (pt) 2011-09-12
UY30529A1 (es) 2008-02-29
CN101522630A (zh) 2009-09-02
BRPI0715817A2 (pt) 2014-12-23
DK2064185T3 (da) 2011-09-19
US20100168099A1 (en) 2010-07-01

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