AR071518A1 - Derivados de arilpirazinona como estimulantes de la secrecion de insulina metodos para obtenerlos y su uso para el tratamiento de diabetes - Google Patents

Derivados de arilpirazinona como estimulantes de la secrecion de insulina metodos para obtenerlos y su uso para el tratamiento de diabetes

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Publication number
AR071518A1
AR071518A1 ARP090101517A ARP090101517A AR071518A1 AR 071518 A1 AR071518 A1 AR 071518A1 AR P090101517 A ARP090101517 A AR P090101517A AR P090101517 A ARP090101517 A AR P090101517A AR 071518 A1 AR071518 A1 AR 071518A1
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AR
Argentina
Prior art keywords
alkyl
aryl
cycloalkyl
hydrogen
groups
Prior art date
Application number
ARP090101517A
Other languages
English (en)
Inventor
Gerard Botton
Samer Elbawab
Micheline Kergoat
Christine Charon
Eric Valeur
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Merck Patent Gmbh
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Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR071518A1 publication Critical patent/AR071518A1/es

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    • CCHEMISTRY; METALLURGY
    • 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
    • C07D241/06Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D241/18Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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

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

Abstract

Derivados de arilpirazinona de la formula en donde: (1) R1 está seleccionado de Z; R2 está seleccionado de hidrogeno, alquilo, cicloalquilo; R3 está seleccionado de hidrogeno, halogeno, alquilo, cicloalquilo; A está seleccionado de arilo, heteroarilo, arilalquilo, en donde los grupos alquilo, arilo y heteroarilo pueden estar opcionalmente sustituidos con uno o varios sustituyentes seleccionados de Y; Z es: alquilo, alquenilo, alquinilo, alcoxialquilo, arilo, arilalquilo, ariloxialquilo, arilalcoxialquilo, ariltioalquilo, arilalquiltioalquilo, heteroarilalquilo, heteroariloxialquilo, heteroarilalcoxialquilo, heteroariltioalquilo, heteroarilalquiltioalquilo, heterocicloalquilo, heterocicloalquilalquilo, heterocicloalquiloxialquilo, heterocicloalquilalcoxialquilo, heterocicloalquiltioalquilo, heterocicloalquilalquiltioalquilo, arilalquenilo, arilalquinilo, cicloalquilo, cicloalquilalquilo, cicloalquiloxialquilo, cicloalquilalcoxialquilo, cicloalquiltioalquilo, cicloalquilalquiltioalquilo, cada uno de estos grupos puede estar opcionalmente sustituido con uno o varios sustituyentes seleccionados de Y; Y es: hidroxi, tio, halogeno, ciano, trifluorometoxi, trifluorometilo, carboxi, carboximetilo, carboxietilo, alquilo, alcoxi, alquilamino, arilo, arilsulfonilalquilo, ariloxi, arilalcoxi, amino, NR5R6, azido, nitro, guanidino, amidino, fosfono, oxo, carbamoílo, alquilsulfonilo, alquilsulfinilo, alquiltio, SF5, dos grupos Y pueden formar un metilendioxi; R5 y R6 están seleccionados, de modo independiente, de hidrogeno, alquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, en donde los grupos alquilo, arilo y heteroarilo pueden estar opcionalmente sustituidos con uno o varios sustituyentes seleccionados de Y, R5 y R6 pueden constituir juntos un heterociclo; R2 y R3 pueden constituir un ciclo que corresponde a la formula general (2) R1 y A se definen como con anterioridad; n = 3, 4, 5; R4 representa uno o varios sustituyentes seleccionados de hidrogeno, alquilo, alcoxi, cicloalquilo, arilo, en donde los grupos alquilo, cicloalquilo y arilo pueden estar opcionalmente sustituidos con uno o varios sustituyentes, seleccionados de hidroxi, halogeno, alquilo, alcoxi, trifluorometoxi, trifluorometilo, alquilsulfonilo, NR7R8; R7 y R8 están seleccionados, de modo independiente, de hidrogeno, alquilo, cicloalquilo; así como sus formas racémicas, tautomeros, enantiomeros, diastereomeros, epímeros y polimorfos y mezclas de ellos y sus sales farmacéuticamente aceptables. Como estimulantes de la secrecion de insulina. También se provee la preparacion y al uso de estos derivados de pirazinona para la prevencion y/o el tratamiento de diabetes y patologías asociadas.
ARP090101517A 2008-04-29 2009-04-29 Derivados de arilpirazinona como estimulantes de la secrecion de insulina metodos para obtenerlos y su uso para el tratamiento de diabetes AR071518A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08008165 2008-04-29

Publications (1)

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AR071518A1 true AR071518A1 (es) 2010-06-23

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Country Status (25)

Country Link
US (2) US8815859B2 (es)
EP (1) EP2268624B1 (es)
JP (1) JP5498482B2 (es)
KR (1) KR101687419B1 (es)
CN (1) CN102015661B (es)
AR (1) AR071518A1 (es)
AU (1) AU2009242720B2 (es)
BR (1) BRPI0910833A2 (es)
CA (1) CA2722813C (es)
CO (1) CO6310997A2 (es)
CY (1) CY1114531T1 (es)
DK (1) DK2268624T3 (es)
EA (1) EA022345B1 (es)
EC (1) ECSP10010642A (es)
ES (1) ES2433210T3 (es)
HR (1) HRP20130992T1 (es)
IL (1) IL208959A (es)
MX (1) MX2010011792A (es)
NZ (1) NZ589555A (es)
PL (1) PL2268624T3 (es)
PT (1) PT2268624E (es)
SI (1) SI2268624T1 (es)
UA (1) UA103191C2 (es)
WO (1) WO2009132739A1 (es)
ZA (1) ZA201008505B (es)

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KR20110061640A (ko) * 2008-09-26 2011-06-09 에프. 호프만-라 로슈 아게 Hcv 치료용 피린 또는 피라진 유도체
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013066838A1 (en) * 2011-10-31 2013-05-10 Glaxosmithkline Llc Compounds and methods
CN104628661A (zh) * 2015-02-05 2015-05-20 北京理工大学 一类喹喔啉酮衍生物作为醛糖还原酶抑制剂的结构、制备方法及用途
CN114907323B (zh) * 2022-05-31 2023-08-15 内蒙古民族大学 喹喔啉酮类化合物及其制备方法和应用

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JPS62198671A (ja) 1986-02-25 1987-09-02 Toyo Jozo Co Ltd 1−置換アルキル1,2−ジヒドロ−2−ピラジノン誘導体
RU2003135424A (ru) * 2001-05-14 2005-05-20 Бристол-Маерс Сквибб Фарма Компани (Us) Замещенные пиразиноны, пиридины и пиримидины в качестве лигандов кортикотропин высвобождающего фактора
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Also Published As

Publication number Publication date
PT2268624E (pt) 2013-11-07
EP2268624B1 (en) 2013-07-31
IL208959A (en) 2015-09-24
US20140329837A1 (en) 2014-11-06
CN102015661A (zh) 2011-04-13
UA103191C2 (ru) 2013-09-25
ES2433210T3 (es) 2013-12-09
EP2268624A1 (en) 2011-01-05
ECSP10010642A (es) 2010-12-30
PL2268624T3 (pl) 2014-01-31
KR20100135313A (ko) 2010-12-24
CA2722813A1 (en) 2009-11-05
EA022345B1 (ru) 2015-12-30
EA201001688A1 (ru) 2011-06-30
CN102015661B (zh) 2014-05-14
US20110046159A1 (en) 2011-02-24
JP5498482B2 (ja) 2014-05-21
AU2009242720B2 (en) 2014-03-27
SI2268624T1 (sl) 2013-12-31
DK2268624T3 (da) 2013-11-04
ZA201008505B (en) 2012-01-25
US9233937B2 (en) 2016-01-12
CO6310997A2 (es) 2011-08-22
CY1114531T1 (el) 2016-10-05
US8815859B2 (en) 2014-08-26
NZ589555A (en) 2012-08-31
KR101687419B1 (ko) 2016-12-19
IL208959A0 (en) 2011-01-31
AU2009242720A1 (en) 2009-11-05
BRPI0910833A2 (pt) 2015-08-11
CA2722813C (en) 2017-03-21
WO2009132739A1 (en) 2009-11-05
JP2011518847A (ja) 2011-06-30
MX2010011792A (es) 2010-11-25
HRP20130992T1 (hr) 2013-11-22

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