AR042342A1 - Derivados de pirazina que presentan efecto inhibidor selectivo sobre gsk3, proceso de preparacion y formulaciones farmaceuticas que los contienen - Google Patents

Derivados de pirazina que presentan efecto inhibidor selectivo sobre gsk3, proceso de preparacion y formulaciones farmaceuticas que los contienen

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Publication number
AR042342A1
AR042342A1 ARP030104527A ARP030104527A AR042342A1 AR 042342 A1 AR042342 A1 AR 042342A1 AR P030104527 A ARP030104527 A AR P030104527A AR P030104527 A ARP030104527 A AR P030104527A AR 042342 A1 AR042342 A1 AR 042342A1
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Argentina
Prior art keywords
amino
phenyl
sulfonyl
hydrochloride
methylpiperazin
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ARP030104527A
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English (en)
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Astrazeneca Ab
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Publication of AR042342A1 publication Critical patent/AR042342A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/073Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61P17/00Drugs for dermatological disorders
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/16Anti-Parkinson drugs
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/24Antidepressants
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
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    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56Nitrogen atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic 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
    • C07D241/14Heterocyclic 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
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26Sulfur atoms
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    • 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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    • 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
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    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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

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  • Engineering & Computer Science (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Biomedical Technology (AREA)
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  • Diabetes (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente se refiere a derivados de pirazina que presentan efecto inhibidor selectivo sobre GSK3, a un proceso para su preparación y al uso de dichos compuestos activos en terapia, de modo de proporcionar compuestos que presentan efecto inhibidor selectivo sobre la GSK3. Reivindicación 1:Un compuesto, el cual es 3-Amino-N-(3-nitrofenil)-6-[4-(pirrolidin-1-ilsulfonil)fenil]pirazin-2-carboxamida; 3-Amino-6-[4-(pirrolidin-1-ilsulfonil)fenil]-N-1H-tetrazol-5-ilpirazin-2-carboxamida; N-[3-(Acetilamino)fenil]-3-amino-6-[4-[(4-metil-1-piperazinil)sulfonil]fenil]-2-pirazincarboxamida; 3-Amino-N-[3-(aminosulfonil)fenil]-6-[4-[(4-metil-1-piperazinil)sulfonil]fenil]-2-pirazincarboxamida; en forma de base libre o de una sal, solvato o solvato de una sal del mismo aceptables desde el punto de vista farmacéutico; Clorhidrato de 3-amino-6-[4-({[(1R)-2-metoxi-1-metiletil]amino}sulfonil)fenil]-N-piridin-3-ilpirazin-2-carboxamida; clorhidrato de 3-amino-6-[4-({[(1S)-2-metoxi-1-metiletil]amino}sulfonil)fenil]-N-piridin-3-ilpirazin-2-carboxamida; clorhidrato de 3-amino-6-(4-{[(2-etoxietil)amino]sulfonil}fenil)-N-piridin-3-ilpirazin-2-carboxamida; clorhidrato de 3-amino-N-(2-metoxifenil)-6-{4-[(4-metilpiperazin-1-il)sulfonil]fenil}pirazin-2-carboxamida; clorhidrato de 3-amino-N-(4-metoxifenil)-6-{4-[(4-metilpiperazin-1-il)sulfonil]fenil}pirazin-2-carboxamida; clorhidrato de 3-amino-N-[2-(aminocarbonil)fenil]-6-{4-[(4-metilpiperazin-1-il)sulfonil]fenil}pirazin-2-carboxamida; clorhidrato de 3-amino-N-[3-(aminocarbonil)fenil]-6-{4-[(4-metilpiperazin-1-il)sulfonil]fenil}pirazin-2-carboxamida; clorhidrato de 3-amino-N-(3-cianofenil)-6-{4-[(4-metilpiperazin-1-il)sulfonil]fenil}pirazin-2-carboxamida; clorhidrato de 3-amino-N-(2-bromofenil)-6-{4-[(4-metilpiperazin-1-il)sulfonil]fenil}pirazin-2-carboxamida; clorhidrato de 3-amino-N-(3-bromofenil)-6-{4-[(4-metilpiperazin-1-il)sulfonil]fenil}pirazin-2-carboxamida; clorhidrato de 3-amino-6-{4-[(4-metilpiperazin-1-il)sulfonil]fenil}-N-1H-pirazol-3-ilpirazin-2carboxamida; clorhidrato de 3-amino-N-[4-(aminocarbonil)-1H-pirazol-3-il]-6-{4-[(4-metilpiperazin-1-il)-sulfonil]fenil}pirazin-2-carboxamida; clorhidrato de 3-amino-N-1H-imidazol-2-il-6-{4-[(4-metilpiperazin-1-il)-sulfonil]fenil}pirazin-2-carboxamida; clorhidrato de 3-amino-6-[3-fluor-4-[2-(4-morfolinil)etoxi]fenil]-N-3-piridinil-2-pirazincarboxamida; clorhidrato de 3-amino-6-[4-[[(1-etil-3-piperidinil)amino]sulfonil]fenil]-N-3-piridinil-2-pirazincarboxamida; clorhidrato de 3-amino-6-[4-[[bis(2-metoxietil)amino]sulfonil]fenil]-N-3-piridinil-2-pirazincarboxamida; clorhidrato de 3-amino-6-[4-[[(3-metilbutil)amino]sulfonil]fenil]-N-3-piridinil-2-pirazincarboxamida; clorhidrato de 3-amino-6-[4-[[[(1S)-2-metoxi-1-metiletil]amino]carbonil]fenil]-N-3-piridinil-2-pirazincarboxamida; clorhidrato de 3-amino-N-3-piridinil-6-[4-[[[2-(1pirrolidinil)etil]amino]carbonil]fenil]-2-pirazincarboxamida; clorhidrato de 3-amino-N-(3-metoxifenil)-6-[4-[(4-metil-1-piperazinil)sulfonil]fenil]-2-pirazincarboxamida; clorhidrato de N-(3-acetilfenil)-3-amino-6-[4-[(4-metil-1-piperazinil)sulfonil]fenil]-2-pirazincarboxamida; clorhidrato de 3-amino-6-[4-[(4-metil-1-piperazinil)sulfonil]fenil]-N-[3-(trifluormetil)fenil]-2-pirazincarboxamida; o en forma de una base libre o de una sal, solvato o solvato de una sal del mismo alternativas, aceptables desde el punto de vista farmacéutico.
ARP030104527A 2002-12-17 2003-12-09 Derivados de pirazina que presentan efecto inhibidor selectivo sobre gsk3, proceso de preparacion y formulaciones farmaceuticas que los contienen AR042342A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE0203752A SE0203752D0 (sv) 2002-12-17 2002-12-17 New compounds

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AR042342A1 true AR042342A1 (es) 2005-06-15

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US (2) US7595319B2 (es)
EP (1) EP1575939A1 (es)
JP (1) JP2006516124A (es)
AR (1) AR042342A1 (es)
AU (1) AU2003287136A1 (es)
SE (1) SE0203752D0 (es)
TW (1) TW200510375A (es)
WO (1) WO2004055006A1 (es)

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