AR090496A1 - Derivados biciclicos de pirazinona - Google Patents

Derivados biciclicos de pirazinona

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Publication number
AR090496A1
AR090496A1 ARP130100972A ARP130100972A AR090496A1 AR 090496 A1 AR090496 A1 AR 090496A1 AR P130100972 A ARP130100972 A AR P130100972A AR P130100972 A ARP130100972 A AR P130100972A AR 090496 A1 AR090496 A1 AR 090496A1
Authority
AR
Argentina
Prior art keywords
denotes
hal
mono
par2
coa
Prior art date
Application number
ARP130100972A
Other languages
English (en)
Inventor
Moinet Gerard
Dr Wegener Ansgar
Dr Dipl-Chem Dorsch Dieter
Dr Buchstaller Hans-Peter
Original Assignee
Merck Patent Ges Mit Beschränkter Haftung
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48013911&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR090496(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Patent Ges Mit Beschränkter Haftung filed Critical Merck Patent Ges Mit Beschränkter Haftung
Publication of AR090496A1 publication Critical patent/AR090496A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

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

Abstract

Los compuestos de la fórmula (1) en donde R¹ denota H, F, Cl, CN, CH₃, CH₂OH, CH₂CI, CH₂Br, CF₃, CHF₂ o CH₂F; R² denota H o A; R³ denota H, F, Cl, CH₃, CF₃ o CHF₂; X denota CR³ o N; Y denota Ar¹, Carb, Het¹ o Cyc; Ar¹ denota fenilo o naftilo que no está sustituido o que está mono-, di- o trisustituido con Hal, A, [C(R²)₂]ₚOR², [C(R²)₂]ₚN(R²)₂, [C(R²)₂]ₚHet², NO₂, CN, [C(R²)₂]ₚCOOR², [C(R²)₂]ₚCON(R²)₂, NR²COA, NR²SO₂A, [C(R²)₂]ₚSO₂N(R²)₂, S(O)ₙA, COHet³, O[C(R²)₂]ₘN(R²)₂, O[C(R²)₂]ₚAr², O[C(R²)₂]ₚHet², NHCOOA, NHCON(R²)₂, Cyc, CHO y/o COA; Ar² denota fenilo, no está sustituido o que está mono- o disustituido con Hal, A, [C(R²)₂]ₚOR², [C(R²)₂]ₚN(R²)₂, [C(R²)₂]ₚHet³, NO₂, CN, [C(R²)₂]ₚCOOR, [C(R²)₂]ₚN(R²)₂, N(R²)₂COA, NR²SO₂A, [C(R²)₂]ₚSO₂N(R²)₂, S(O)ₙA, COHet³, O[C(R²)₂]ₘN(R²)₂, O[C(R²)₂]ₚHet³, NHCOOA, NHCON(R²)₂, CHO y/o COA; Het¹ denota pirrolidinilo, azetidinilo, tetrahidroimidazolilo, tetrahidrofuranilo, tetrahidropirazolilo, tetrahidropiranilo, piperidinilo, morfolinilo, hexahidropiridazinilo, hexahidropirimidinilo, [1,3]dioxolanilo, piperazinilo, furilo, tienilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, isoxazolilo, oxadiazolilo, tiazolilo, triazolilo, tetrazolilo, piridilo, pirimidilo, piridazinilo, indolilo, isoindolilo, bencimidazolilo, indazolilo, quinolilo, 1,3-benzodioxolilo, benzotiofenilo, benzofuranilo, imidazopiridilo o furo[3,2-b]piridilo, cada uno de los cuales no está sustituido o está mono- o disustituido con Hal, A, [C(R²)₂]ₚOR², [C(R²)₂]ₚN(R²)₂, [C(R²)₂]ₚHet², [C(R²)₂]ₚAr², NO₂, CN, [C(R²)₂]ₚCOOR², [C(R²)₂]ₚCON(R²)₂, NR²COA, NR²SO₂A, [C(R²)₂]ₚSO₂N(R²)₂, S(O)ₙA, COHet³, O[C(R²)₂]ₘN(R²)₂, O[C(R²)₂]ₚAr², O[C(R²)₂]ₚHet², NHCOOA, NHCON(R²)₂, CHO, COA, =S, =NR y/u =O; Carb denota indanilo o tetrahidronaftilo, cada uno de los cuales puede no estar sustituido o puede estar mono-, di-, tri- o tetrasustituido con A; Cyc denota alquilo cíclico con 3, 4, 5, 6 ó 7 átomos de C, que puede no estar sustituido o que puede estar monosustituido con A, OH, Hal, CN o Ar² o Het²; Het² denota pirrolidinilo, azetidinilo, tetrahidroimidazolilo, tetrahidrofuranilo, tetrahidropirazolilo, tetrahidropiranilo, piperidinilo, morfolinilo, hexahidropiridazinilo, hexahidropirimidinilo, [1,3]dioxolanilo, piperazinilo, furilo, tienilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, isoxazolilo, oxadiazolilo, tiazolilo, triazolilo, tetrazolilo, piridilo, pirimidilo, piridazinilo, indolilo, isoindolilo, bencimidazolilo, indazolilo, quinolilo, 1,3-benzodioxolilo, benzotiofenilo, benzofuranilo, imidazopiridilo o furo[3,2-b]piridilo, cada uno de los cuales no está sustituido o está mono- o disustituido con Hal, A, [C(R²)₂]ₚOR², [C(R²)₂]ₚN(R²)₂, [C(R²)₂]ₚHet³, [C(R²)₂]ₚOHet³, [C(R²)₂]ₚAr², NO₂, CN, [C(R²)₂]ₚCOOR², [C(R²)₂]ₚCON(R²)₂, NR²COA, NR²SO₂A, [C(R²)₂]ₚSO₂N(R²)₂, S(O)ₙA, COHet³, O[C(R²)₂]ₘN(R²)₂, O[C(R²)₂]ₚAr², O[C(R²)₂]ₚHet³, NHCOOA, NHCON(R²)₂, CHO, COA, =S, =NR y/u =O; Het³ denota dihidropirrolilo, pirrolidinilo, azetidinilo, oxetanilo, tetrahidroimidazolilo, dihidropirazolilo, tetrahidropirazolilo, tetrahidrofuranilo, dihidropiridilo, tetrahidropiridilo, piperidinilo, morfolinilo, hexahidropiridazinilo, hexahidropirimidinilo, [1,3]dioxolanilo, tetrahidropiranilo o piperazinilo, cada uno de los cuales no está sustituido o está mono- o disustituido con Hal, CN, OR², COOR², CON(R²)₂, S(O)ₙA, S(O)ₙAr, COA, A y/u =O; A denota alquilo no ramificado o ramificado C₁₋₁₀, en donde dos grupos CH y/o CH₂ adyacentes pueden formar un enlace doble y en donde uno o dos grupos CH y/o CH₂ no adyacentes pueden estar reemplazados por átomos de N, O y/o S y en donde 1 - 7 átomos de H pueden estar reemplazados por F o Cl; Hal denota F, Cl, Br o I; n denota 0, 1 ó 2; m denota 1, 2 ó 3; p denota 0, 1, 2, 3 ó 4; con la condición de que, si R¹ es CH₂OH, entonces Ar¹ no sea 2,4-diclorofenilo; y sus solvatos, sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de Tankirasa y se pueden emplear, inter alia, para el tratamiento de enfermedades tales como cáncer, enfermedades cardiovasculares, lesión del sistema nervioso central y diferentes formas de inflamación.
ARP130100972A 2012-03-28 2013-03-26 Derivados biciclicos de pirazinona AR090496A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12002215 2012-03-28

Publications (1)

Publication Number Publication Date
AR090496A1 true AR090496A1 (es) 2014-11-19

Family

ID=48013911

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ARP130100972A AR090496A1 (es) 2012-03-28 2013-03-26 Derivados biciclicos de pirazinona

Country Status (32)

Country Link
US (1) US9120805B2 (es)
EP (1) EP2831077B1 (es)
JP (1) JP6096879B2 (es)
KR (1) KR102070567B1 (es)
CN (1) CN104169284B (es)
AR (1) AR090496A1 (es)
AU (1) AU2013242492B2 (es)
CA (1) CA2868620C (es)
CL (1) CL2014002557A1 (es)
CO (1) CO7111292A2 (es)
DK (1) DK2831077T3 (es)
EA (1) EA027416B1 (es)
EC (1) ECSP14024526A (es)
ES (1) ES2585044T3 (es)
HK (1) HK1203961A1 (es)
HR (1) HRP20160908T1 (es)
HU (1) HUE030067T2 (es)
IL (1) IL234713A (es)
MX (1) MX351149B (es)
MY (1) MY172308A (es)
NZ (1) NZ630489A (es)
PE (1) PE20142186A1 (es)
PH (1) PH12014501829A1 (es)
PL (1) PL2831077T3 (es)
PT (1) PT2831077T (es)
RS (1) RS54997B1 (es)
SG (1) SG11201405750YA (es)
SI (1) SI2831077T1 (es)
TW (1) TWI576346B (es)
UA (1) UA112795C2 (es)
WO (1) WO2013143663A1 (es)
ZA (1) ZA201407828B (es)

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PH12014501829B1 (en) 2014-11-10
CA2868620C (en) 2020-02-25
CN104169284B (zh) 2017-03-29
EA027416B1 (ru) 2017-07-31
HRP20160908T1 (hr) 2016-09-23
MX351149B (es) 2017-10-04
AU2013242492B2 (en) 2016-12-15
SI2831077T1 (sl) 2016-09-30
JP6096879B2 (ja) 2017-03-15
KR20140140099A (ko) 2014-12-08
AU2013242492A1 (en) 2014-11-13
HK1203961A1 (en) 2015-11-06
ZA201407828B (en) 2015-12-23
PE20142186A1 (es) 2014-12-29
MX2014011420A (es) 2014-11-25
CA2868620A1 (en) 2013-10-03
CL2014002557A1 (es) 2014-12-19
SG11201405750YA (en) 2014-10-30
HUE030067T2 (en) 2017-04-28
UA112795C2 (uk) 2016-10-25
EP2831077B1 (en) 2016-04-27
US9120805B2 (en) 2015-09-01
ES2585044T3 (es) 2016-10-03
CO7111292A2 (es) 2014-11-10
ECSP14024526A (es) 2015-09-30
PH12014501829A1 (en) 2014-11-10
IL234713A (en) 2016-09-29
EP2831077A1 (en) 2015-02-04
EA201401062A1 (ru) 2015-04-30
TWI576346B (zh) 2017-04-01
DK2831077T3 (en) 2016-08-15
PL2831077T3 (pl) 2016-10-31
RS54997B1 (sr) 2016-11-30
MY172308A (en) 2019-11-21
KR102070567B1 (ko) 2020-01-29
JP2015511609A (ja) 2015-04-20
TW201343650A (zh) 2013-11-01
CN104169284A (zh) 2014-11-26
PT2831077T (pt) 2016-08-12
US20150057264A1 (en) 2015-02-26
WO2013143663A1 (en) 2013-10-03
NZ630489A (en) 2016-04-29

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