AR089944A1 - Derivados de tetrahidro-quinazolinona - Google Patents

Derivados de tetrahidro-quinazolinona

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Publication number
AR089944A1
AR089944A1 ARP130100401A ARP130100401A AR089944A1 AR 089944 A1 AR089944 A1 AR 089944A1 AR P130100401 A ARP130100401 A AR P130100401A AR P130100401 A ARP130100401 A AR P130100401A AR 089944 A1 AR089944 A1 AR 089944A1
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AR
Argentina
Prior art keywords
denotes
cho
hal
mono
noh
Prior art date
Application number
ARP130100401A
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English (en)
Inventor
Dr Buchstaller Hans
Peter-Dra Leuthner Birgitta
Dra Esdar Christina
Original Assignee
Merck Patent Ges Mit Beschränkter Haftung
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47628092&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR089944(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 AR089944A1 publication Critical patent/AR089944A1/es

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    • 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • 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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los compuestos de la fórmula (1), en donde U denota CH₂ o CHR²; V denota CH₂, CHR² o CO; W denota NR¹ o CR³R⁶, o denota NH, si U o V denotan CHR²; R¹ denota Ar, Het, COA, COAr¹, COHet, CO(CH₂)ₙNR⁴R⁵, (CH₂)ₙHet, (CH₂)ₙCONHAr, (CH₂)ₙCONHHet, (CH₂)ₙCONR⁴R⁵, (CH₂)ₙOH, (CH₂)ₙOA o (CH₂)ₙNR⁴R⁵; R² denota A, Ar¹, Hal, CN, COA, COOH, COOA, CONR⁴R⁵, SO₂NR⁴R⁵, (CH₂)ₙOH o (CH₂)ₙNR⁴R⁵; R³ denota H, OH u OA; R⁴, R⁵ denotan cada uno, de modo independiente entre sí, H o A; R⁶ denota A o Ar¹; Ar denota fenilo, que está mono-, di- o trisustituido con Hal, A, O(CH₂)ₚCyc, Alk, (CH₂)ₙOH, (CH₂)ₙOA, (CH₂)ₙCOOH, (CH₂)ₙCOOA, S(O)ₘA, fenoxi, benciloxi. (CH₂)ₙNH₂, (CH₂)ₙNHA, (CH₂)ₙNA₂, (CH₂)ₙCN, NO₂, (CH₂)ₙCONH₂, (CH₂)ₙCONHA, (CH₂)ₙCONA₂, SO₂NH₂, SO₂NHA, SO₂NA₂, NHCONH₂, (CH₂)ₙNHCOA, (CH₂)ₙNHCOAlk, NHCOCH=CH(CH₂)ₚNA₂, CHO, COA, SO₃H, O(CH₂)ₚNH₂, O(CH₂)ₚNHCOOA, O(CH₂)ₚNHA, O(CH₂)ₚNA₂, NHC(CH₂)ₚNH₂. NH(CH₂)ₚNHCOOA, NH(CH₂)ₚNHA, NH(CH₂)ₚNA₂, NHCOHet³, COHet³, (CH₂)ₙHet³, O(CH₂)ₙHet³ y/o O(CH₂)ₙCH(OH)(CH₂); Ar¹ denota fenilo, que no está sustituido o que está mono-, di- o trisustituido con Hal, A, (CH₂)ₙOH, (CH₂)ₙOA, (CH₂)ₙCOOH, (CH₂)ₙCOOA, S(O)ₘA, fenoxi, benciloxi, (CH₂)ₙNH₂. (CH₂)ₙNHA, (CH₂)ₙNA₂, (CH₂)ₙCN, NO₂, (CH₂)ₙCONH₂, (CH₂)ₙCONHA, (CH₂)ₙCONA₂, SO₂NH₂, SO₂NHA, SO₂NA₂, NHCONH₂, (CH₂)ₙNHCOA, CHO, COA y/o SO₃H; Het denota un heterociclo saturado, insaturado o aromático mono- o bicíclico que tiene 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di-, tri- o tetra-sustituido con Hal, A, (CH₂)ₙHet³, OHet³, NH(CH₂)ₙHet³, (CH₂)ₙCOOH, (CH₂)ₙCOOA, fenilo, bencilo, CHO, COA, (CH₂)ₙNH₂, (CH₂)ₙNHA, (CH₂)ₙNA₂, CN, (CH₂)ₙOH, (CH₂)ₙOA, (CH₂)ₚCH(OH)(CH₂)ₚOH, (CH₂)ₚCH(OH)(CH₂)ₚOA, NH(CH₂)ₚNH₂, NHSO₂A, NASO₂A, SO₂A, (CH₂)ₙCONR⁴R⁵, (CH₂)ₙSO₂NR⁴R⁵ y/u =O; Het³ denota un heterociclo saturado, insaturado o aromático mono- o bicíclico que tiene 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di-, tri- o tetra-sustituido con A, Hal, (CH₂)ₙNH₂, (CH₂)ₙNHA, (CH₂)ₙNA₂, (CH₂)ₙOH, (CH₂)ₙOA, COOA, Ar³ y/u =O; A denota alquilo C₁₋₁₀ no ramificado o ramificado, en donde 1 - 7 átomos de H pueden estar reemplazados por F y/o Cl y/o en donde uno o dos grupos CH₂ no adyacentes pueden estar reemplazados por O, NH, S, SO, SO₂ y/o por grupos CH=CH; Cyc denota alquilo cíclico C₃₋₇; Alk denota alquenilo o alquinilo que tiene 2, 3, 4, 5 ó 6 átomos de C; Ar³ denota fenilo, que no está sustituido o que está mono-, di- o trisustituido con Hal y/o A; Hal denota F, Cl Br o I; m denota 0, 1 ó 2; n denota 0, 1, 2, 3 ó 4; p denota 1, 2, 3 ó 4; 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.
ARP130100401A 2012-02-09 2013-02-08 Derivados de tetrahidro-quinazolinona AR089944A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12000841 2012-02-09

Publications (1)

Publication Number Publication Date
AR089944A1 true AR089944A1 (es) 2014-10-01

Family

ID=47628092

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130100401A AR089944A1 (es) 2012-02-09 2013-02-08 Derivados de tetrahidro-quinazolinona

Country Status (31)

Country Link
US (1) US9339503B2 (es)
EP (1) EP2812323B1 (es)
JP (1) JP6116592B2 (es)
KR (1) KR20140121477A (es)
CN (1) CN104093714B (es)
AR (1) AR089944A1 (es)
AU (1) AU2013218357B2 (es)
BR (1) BR112014019357A8 (es)
CA (1) CA2863991C (es)
CL (1) CL2014002097A1 (es)
CO (1) CO7020919A2 (es)
DK (1) DK2812323T3 (es)
EA (1) EA026611B1 (es)
EC (1) ECSP14017586A (es)
ES (1) ES2579980T3 (es)
HR (1) HRP20160735T1 (es)
HU (1) HUE029717T2 (es)
IL (1) IL233984A (es)
MX (1) MX349736B (es)
NZ (1) NZ630170A (es)
PE (1) PE20141823A1 (es)
PH (1) PH12014501581A1 (es)
PL (1) PL2812323T3 (es)
PT (1) PT2812323T (es)
RS (1) RS55377B1 (es)
SG (1) SG11201404654SA (es)
SI (1) SI2812323T1 (es)
TW (1) TWI572593B (es)
UA (1) UA116627C2 (es)
WO (1) WO2013117288A1 (es)
ZA (1) ZA201406579B (es)

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US9611223B2 (en) 2013-09-11 2017-04-04 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
BR112016008994A2 (pt) * 2013-11-07 2017-09-19 Lilly Co Eli Compostos de pirido[2,3-d]pirimidin-4-ona como inibidores de tanquirase
CN106243088B (zh) 2015-06-03 2019-01-04 广东东阳光药业有限公司 取代的哌嗪化合物及其使用方法和用途
KR101777475B1 (ko) * 2015-12-08 2017-09-11 에스티팜 주식회사 신규한 디히드로피라노피리미디논 유도체 및 이들의 용도
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
NZ749946A (en) 2016-06-30 2023-11-24 Yakult Honsha Kk Novel compound or pharmaceutically acceptable salt thereof
CN108727302A (zh) * 2017-10-23 2018-11-02 科迈化工股份有限公司 一种环保型n-叔丁基-2-苯并噻唑次磺酰胺(ns)合成工艺
JP7369968B2 (ja) * 2017-12-27 2023-10-27 公益財団法人がん研究会 抗がん剤
ES2998084T3 (en) 2017-12-27 2025-02-19 Japanese Found For Cancer Res Novel dihydroquinazolinone compound or pharmacologically acceptable salt, and cell growth inhibitor
BR112021002772A2 (pt) 2018-08-16 2021-05-04 F. Hoffmann-La Roche Ag compostos, composições farmacêuticas, método de tratamento de câncer, métodos para regular a atividade de uma proteína, para inibir a proliferação de uma população de células, para tratar um distúrbio, para preparar uma proteína, para inibir metástase de tumor e para tratamento de câncer e usos

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MX349736B (es) 2017-08-10
WO2013117288A8 (en) 2014-07-31
TWI572593B (zh) 2017-03-01
EP2812323B1 (en) 2016-04-06
SI2812323T1 (sl) 2016-08-31
PH12014501581B1 (en) 2014-10-08
WO2013117288A1 (en) 2013-08-15
AU2013218357A1 (en) 2014-09-25
PE20141823A1 (es) 2014-11-29
IL233984A (en) 2017-09-28
ES2579980T3 (es) 2016-08-18
JP2015506965A (ja) 2015-03-05
US20150025071A1 (en) 2015-01-22
US9339503B2 (en) 2016-05-17
BR112014019357A2 (es) 2017-06-20
CA2863991A1 (en) 2013-08-15
DK2812323T3 (en) 2016-05-09
HK1202551A1 (zh) 2015-10-02
CA2863991C (en) 2020-08-11
BR112014019357A8 (pt) 2017-07-11
EP2812323A1 (en) 2014-12-17
CL2014002097A1 (es) 2014-11-07
TW201336828A (zh) 2013-09-16
CN104093714B (zh) 2016-08-24
SG11201404654SA (en) 2014-09-26
HUE029717T2 (en) 2017-03-28
MX2014009491A (es) 2014-08-29
PL2812323T3 (pl) 2016-09-30
RS55377B1 (sr) 2017-03-31
PH12014501581A1 (en) 2014-10-08
AU2013218357B2 (en) 2017-01-05
UA116627C2 (uk) 2018-04-25
ECSP14017586A (es) 2015-09-30
NZ630170A (en) 2016-03-31
CO7020919A2 (es) 2014-08-11
PT2812323T (pt) 2016-07-13
JP6116592B2 (ja) 2017-04-19
CN104093714A (zh) 2014-10-08
EA026611B1 (ru) 2017-04-28
AU2013218357A8 (en) 2015-01-22
KR20140121477A (ko) 2014-10-15
HRP20160735T1 (hr) 2016-07-29
EA201400879A1 (ru) 2015-01-30
ZA201406579B (en) 2015-12-23

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