AR075238A1 - Compuestos de piridazinona - Google Patents

Compuestos de piridazinona

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Publication number
AR075238A1
AR075238A1 ARP100100304A ARP100100304A AR075238A1 AR 075238 A1 AR075238 A1 AR 075238A1 AR P100100304 A ARP100100304 A AR P100100304A AR P100100304 A ARP100100304 A AR P100100304A AR 075238 A1 AR075238 A1 AR 075238A1
Authority
AR
Argentina
Prior art keywords
phenyl
pyridazin
trifluoromethyl
pyrazol
substituted
Prior art date
Application number
ARP100100304A
Other languages
English (en)
Inventor
Mitsuyo Kondo
Takahiko Taniguchi
John F Quinn
Jun Kunitomo
Masato Yoshikawa
Makoto Fushimi
Akira Kawada
Original Assignee
Takeda Pharmaceutical
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 Takeda Pharmaceutical filed Critical Takeda Pharmaceutical
Publication of AR075238A1 publication Critical patent/AR075238A1/es

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    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • C07D403/14—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 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

Abstract

La presente provee un compuesto que tiene el efecto de inhibir la PDE, y que es util como un medicamento para prevenir o tratar la esquizofrenia o etc. Reivindicacion 1: Un compuesto de la formula (1) donde R1 representa un sustituyente, R2 representa un átomo de hidrogeno, o un sustituyente, R3 representa un átomo de hidrogeno, o un sustituyentes, el Anillo A representa un anillo aromático que puede estar sustituido, y el Anillo B representa un anillo aromático de 5 miembros que puede estar sustituido; con la condicion de que se excluyan los siguientes compuestos 1-(2-clorofenil)-6-metil-3-{5-tioxo-4-[3-(trifluorometil)fenil]-4,5-dihidro-1H-1,2,4-triazol-3-il}piridazin-4(1H)-ona, 1-(4-clorofenil)-3-[4-(2-fluorofenil)-5-tioxo-4,5-dihidro-1H-1,2,4-triazol-3-il]-6-metilpiridazin-4(1H)-ona, 1-(4-clorofenil)-6-metil-3-{5-tioxo-4-[3-(trifluorometil)fenil]-4,5-dihidro-1H-1,2,4-triazol-3-il}piridazin-4(1H)-ona, 1-(4-clorofenil)-3-[4-(2-fluorofenil)-5-(metilsulfanil)-4H-1,2,4-triazol-3-il]-6-metilpiridazin-4(1H)-ona, 1-(4-clorofenil)-6-metil-3-{5-(metilsulfanil)-4-[3-(trifluorometil)fenil]-4H-1,2,4-triazol-3-il)piridazin-4(1H)-ona, 1-(2-clorofenil)-6-metil-3-{5-(metilsulfanil)-4-[3-(trifluorometil)fenil]-4H-1,2,4-triazol-3-il}piridazin-4-(1H)-ona, 3-(3,5-dimetil-1H-pirazol-1-il)-1-fenilpiridazin-4(1H)-ona, 1-(4-clorofenil)-3-{1-[3-cloro-5-(trifluorometil)piridin-2-il]-1H-pirazol-5-il}piridazin-4(1H)-ona, 3-[1-(2-fluorofenil)-1H-pirazol-5-il]-1-[3-(trifluorometil)fenil]piridazin-4(1H)-ona, 3-[1-(3-clorofenil)-1H-pirazol-5-il]-1-[3-(trifluorometil)fenil]piridazin-4(1H)-ona, 3-[1-(4-metoxifenil)-1H-pirazol-5-il]-1-[3-trifluorometil)fenil]piridazin-4(1H)-ona, 3-(1-fenil-1H-pirazol-5-il)-1-[3-(trifluorometil)fenil]piridazin-4(1H)-ona, 3-[1-(3-nitrofenil)-1H-pirazol-5-il]-1-[3-(trifluorometil)fenil]piridazin-4(1H)-ona, 3-[1-(1,1-dioxidotetrahidrotiofen-3-il)-1H-pirazol-5-il]-1-[3-(trifluorometil)fenil]piridazin-4(1H)-ona, 3-[1-(4-metilfenil)-1H-pirazol-5-il]-1-fenilpiridazin-4(1H)-ona, 3-[1-(4-clorofenil)-1H-pirazol-5-il]-1-fenilpiridazin-4(1H)-ona, 3-(4-etil-5-tioxo-4,5-dihidro-1H-1,2,4-triazol-3-il)-1-(4-metilfenil)piridazin-4(1H)-ona, 1-(4-clorofenil)-3-{1-[3-cloro-5-(trifluorometil)piridin-2-il]-1H-pirazol-3-il}piridazin-4(1H)-ona, 3-[1-(2-fluorofenil)-1H-pirazol-3-il]-1-[3-(trifluorometil)fenil]piridazin-4(1H)-ona, 3-[1-(3-clorofenil)-1H-pirazol-3-il]-1-[3-(trifluorometil)fenil]piridazin-4(1H)-ona, 3-[1-(3-metoxifenil)-1H-pirazol-3-il]-1-[3-(trifluorometil) fenil] piridazin-4(1H)-ona, 3-(1-fenil-1H-pirazol-3-il)-1-[3-(trifluorometil)fenil]piridazin-4(1H)-ona, 3-[1-(3-nitrofenil)-1H-pirazol-3-il]-1-[3-(trifluorometil)fenil]piridazin-4(1H)-ona, 3-[1-(4-metilfenil)-1H-pirazol-3-il]-1-fenilpiridazin-4(1H)-ona, 3-[1-(4-clorofenil)-1H-pirazol-3-il]-1-fenilpiridazin-4(1H)-ona, un compuesto de formula (2) donde el Anillo A' es un anillo de benceno que puede estar sustituido con un sustituyente seleccionado de un átomo de halogeno, y un grupo alquilo, R1' es (i) un grupo etilo, o (ii) un grupo fenilo que puede estar sustituido con uno o más sustituyentes seleccionados de un átomo de fluor, y un grupo trifluorometilo, R3' es un átomo de hidrogeno, o un grupo metilo, y Ra es un átomo de hidrogeno, o un grupo hidrocarbonado acíclico C1-4 que puede estar sustituido, un compuesto de la formula (3) donde el Anillo A'' es un anillo de benceno que puede estar sustituido con halogeno, y R1'' es un grupo acilo; o una sal de los mismos. Reivindicacion 2: El compuesto de acuerdo con la reivindicacion 1, donde R2 representa un átomo de halogeno, un grupo hidroxi, un grupo alquilo C1-10 que pueda estar sustituido, o un grupo alcoxi C1-10 que puede estar sustituido. Reivindicacion 3: El compuesto de acuerdo con la reivindicacion 2, donde R2 representa un grupo alcoxi C1-10 que puede estar sustituido con uno o más sustituyentes seleccionados de un átomo de halogeno, un grupo alcoxi C1-10, y un grupo cicloalquilo C3-7. Reivindicacion 4: El compuesto de acuerdo con la reivindicacion 2, donde R2 representa un grupo alcoxi C1-10. Reivindicacion 5: El compuesto de acuerdo con la reivindicacion 2, donde R1 representa un grupo fenilo que puede estar sustituido con 1 a 5 sustituyentes seleccionados de un átomo de halogeno, un grupo alquilo C1-10 que puede estar sustituido, y un grupo alcoxi C1-10 que puede estar sustituido. Reivindicacion 6: El compuesto de acuerdo con la reivindicacion 2, donde R1 representa un grupo fenilo que puede estar sustituido con 1 a 5 sustituyentes seleccionados de un átomo de halogeno, un grupo alquilo C1-10, y un grupo alcoxi C1-10. Reivindicacion 7: El compuesto de acuerdo con la reivindicacion 2, donde R1 representa un grupo fenilo que puede estar sustituido con 1 a 5 átomos de halogeno. Reivindicacion 8: El compuesto de acuerdo con la reivindicacion 2, donde R3 representa un átomo de H, o un grupo alcoxi C1-10 que puede estar sustituido. Reivindicacion 9: El compuesto de acuerdo con la reivindicacion 2, donde R3 representa un átomo de hidrogeno, o un grupo alcoxi C1-10. Reivindicacion 10: El compuesto de acuerdo con la reivindicacion 2, donde R3 representa un átomo de hidrogeno.
ARP100100304A 2009-02-05 2010-02-04 Compuestos de piridazinona AR075238A1 (es)

Applications Claiming Priority (2)

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US20220709P 2009-02-05 2009-02-05
US21392709P 2009-07-30 2009-07-30

Publications (1)

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AR075238A1 true AR075238A1 (es) 2011-03-16

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US (7) US8354411B2 (es)
EP (2) EP3006031A1 (es)
JP (1) JP5659166B2 (es)
KR (1) KR101730665B1 (es)
CN (1) CN102365020B (es)
AR (1) AR075238A1 (es)
AU (1) AU2010211050B2 (es)
BR (1) BRPI1008498B8 (es)
CA (1) CA2751565C (es)
CO (1) CO6410258A2 (es)
CR (1) CR20110440A (es)
DK (1) DK2393360T3 (es)
DO (1) DOP2011000254A (es)
EA (1) EA020690B1 (es)
EC (1) ECSP11011305A (es)
ES (1) ES2561181T3 (es)
GE (1) GEP20146004B (es)
HK (1) HK1164642A1 (es)
HR (1) HRP20160065T1 (es)
HU (1) HUE027478T2 (es)
IL (1) IL214137A (es)
JO (1) JO3114B1 (es)
MA (1) MA33072B1 (es)
ME (1) ME02337B (es)
MX (1) MX2011008305A (es)
MY (1) MY170610A (es)
NZ (1) NZ594851A (es)
PE (1) PE20110991A1 (es)
PL (1) PL2393360T3 (es)
RS (1) RS54504B1 (es)
SG (1) SG173175A1 (es)
SI (1) SI2393360T1 (es)
SM (1) SMT201600008B (es)
TN (1) TN2011000362A1 (es)
TW (1) TWI457333B (es)
UY (1) UY32417A (es)
WO (1) WO2010090737A1 (es)
ZA (1) ZA201106074B (es)

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