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AR119461A1 - Derivados de 4-(imidazo[1,2-a]piridin-3-il)-pirimidina - Google Patents

Derivados de 4-(imidazo[1,2-a]piridin-3-il)-pirimidina

Info

Publication number
AR119461A1
AR119461A1 ARP200102060A ARP200102060A AR119461A1 AR 119461 A1 AR119461 A1 AR 119461A1 AR P200102060 A ARP200102060 A AR P200102060A AR P200102060 A ARP200102060 A AR P200102060A AR 119461 A1 AR119461 A1 AR 119461A1
Authority
AR
Argentina
Prior art keywords
denotes
hal
atoms
unsubstituted
mono
Prior art date
Application number
ARP200102060A
Other languages
English (en)
Inventor
Dorsch Dieter Dr
Blum Andreas Dr
Hans-Peter Buchstaller
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR119461A1 publication Critical patent/AR119461A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicación 1: Compuesto de la fórmula (1) caracterizado porque R¹ denota H, Hal, CF₃, NO₂, A, [C(R³)₂]ₙN(R³)₂, [C(R³)₂]ₙHet¹, OR³, O[C(R³)₂]ₙN(R³)₂, O[C(R³)₂]ₙS(O)ₘR³, O[C(R³)₂]ₙCOOR³, O[C(R³)₂]ₙCOON(R³)₂, O[C(R³)₂]ₙHet¹, O[C(R³)₂]ₙN(R³)Het¹, O[C(R³)₂]ₙPh o O[C(R³)₂]ₙCyc, R² denota H o CH₃, R³ denota H o A, V denota H o Hal, X denota O, o N(R³), Y denota fenileno, piridin-diilo, tiofen-diilo, 1,3-tiazol-diilo o pirazol-diilo, cada uno de los cuales no está sustituido o está mono-, di- o trisustituido por Hal y/o A, Z denota CON(R³)₂, fenilo, Het⁴ o -O-A, Het¹ denota un heterociclo de 4 a 7 miembros monocíclico, aromático, insaturado o saturado que tiene de 1 a 4 átomos de N, O y/o S, que pueden no estar sustituidos o estar mono-, di- o trisustituidos por A, Hal, CN, OR³, [C(R³)₂]ₙN(R³)₂, [C(R³)₂]ₙSO₂R³, Het², oxetanilo, =NR³ y/o =O, y en los que un átomo de N puede estar oxidado, o Het¹ denota un heterociclo de 6 a 10 miembros bicíclico o espirocíclico, aromático, insaturado o saturado que tiene de 1 a 6 átomos de N, O y/o S, que pueden no estar sustituidos o estar mono-, di- o trisustituidos por A, Hal, CN, OR³, [C(R³)₂]ₙN(R³)₂, [C(R³)₂]ₙSO₂R³, Het², oxetanilo, =NR³ y/o =O, y en los que un átomo de N puede estar oxidado, Het² denota un heterociclo de 5 a 6 miembros monocíclico aromático o insaturado que tiene de 1 a 4 átomos de N, O y/o S, que pueden no estar sustituidos o estar sustituidos por A y/o Hal, o Het² denota un heterociclo de 7 a 10 miembros bicíclico aromático o insaturado que tiene de 1 a 4 átomos de N, O y/o S, que pueden no estar sustituidos o estar sustituidos por A y/o Hal, Het³ denota un heterociclo de 4 a 7 miembros monocíclico saturado que tiene de 1 a 4 átomos de N y/u O, que pueden no estar sustituidos o estar sustituidos por A, Hal, OR³ y/o =O, Het⁴ denota un heterociclo de 4 a 7 miembros monocíclico, aromático, insaturado o saturado que tiene de 1 a 4 y/o átomos de O, que pueden no estar sustituidos o estar mono-, di o trisustituidos por A, Hal, OR³, [C(R³)₂]ₙHet³, -N(R³)₂ y/o =O, o Het⁴ denota un heterociclo de 6 a 10 miembros bicíclico, aromático, insaturado o saturado que tiene de 1 a 4 y/o átomos de O, que pueden no estar sustituidos o estar mono-, di o trisustituidos por A, Hal, OR³, [C(R³)₂]ₙHet³ y/o =O, A denota alquilo no ramificado o ramificado con 1 - 10 átomos de C, en el que 1 - 3 grupos no adyacentes CH- y/o CH₂ pueden estar reemplazados por átomos O, o NH y en los que 1 - 7 átomos de H pueden estar reemplazados por R⁵, o denota (CH₂)ₙCyc, Cyc denota alquilo cíclico que tiene 3 - 7 átomos de C, R⁵ denota F, Cl, CN u OH, Ph denota fenilo, que puede no estar sustituido o estar mono-, di- o trisustituido por A, OR³ y/o Hal, Hal denota F, Cl, Br o I, m denota 0, 1 ó 2, n denota 0, 1, 2, 3 ó 4, y/o su sal, tautómero y/o estereoisómero farmacéuticamente aceptable.
ARP200102060A 2019-07-24 2020-07-23 Derivados de 4-(imidazo[1,2-a]piridin-3-il)-pirimidina AR119461A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP19188031 2019-07-24

Publications (1)

Publication Number Publication Date
AR119461A1 true AR119461A1 (es) 2021-12-22

Family

ID=67438678

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP200102060A AR119461A1 (es) 2019-07-24 2020-07-23 Derivados de 4-(imidazo[1,2-a]piridin-3-il)-pirimidina

Country Status (13)

Country Link
US (1) US20220267320A1 (es)
EP (1) EP4003992A1 (es)
JP (2) JP7601852B2 (es)
KR (2) KR102894509B1 (es)
CN (2) CN118955500A (es)
AR (1) AR119461A1 (es)
AU (1) AU2020318710B2 (es)
BR (1) BR112022001158A2 (es)
CA (1) CA3148227A1 (es)
IL (1) IL289953B2 (es)
MX (1) MX2022000794A (es)
TW (1) TWI868186B (es)
WO (1) WO2021013864A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20240124450A1 (en) 2022-09-21 2024-04-18 Pfizer Inc. Novel SIK Inhibitors
WO2024131742A1 (zh) * 2022-12-20 2024-06-27 深圳湾实验室 一种靶向usp1的小分子抑制剂及其应用
WO2025248485A1 (en) 2024-05-31 2025-12-04 Idrx, Inc. Pharmaceutical compositions and methods of use thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
EP2303881A2 (en) 2008-07-14 2011-04-06 Gilead Sciences, Inc. Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases
WO2010132598A1 (en) * 2009-05-13 2010-11-18 Amgen Inc. Heteroaryl compounds as pikk inhibitors
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
WO2015030847A1 (en) 2013-08-30 2015-03-05 Ptc Therapeutics, Inc. Substituted pyrimidine bmi-1 inhibitors

Also Published As

Publication number Publication date
IL289953B2 (en) 2025-03-01
KR102894509B1 (ko) 2025-12-02
IL289953A (en) 2022-03-01
AU2020318710A1 (en) 2022-03-10
JP7601852B2 (ja) 2024-12-17
WO2021013864A1 (en) 2021-01-28
TWI868186B (zh) 2025-01-01
EP4003992A1 (en) 2022-06-01
CN114174293B (zh) 2024-08-06
CN114174293A (zh) 2022-03-11
JP7730407B2 (ja) 2025-08-27
IL289953B1 (en) 2024-11-01
KR20220041133A (ko) 2022-03-31
JP2025060626A (ja) 2025-04-10
BR112022001158A2 (pt) 2022-05-17
MX2022000794A (es) 2022-02-16
AU2020318710B2 (en) 2025-11-20
TW202118762A (zh) 2021-05-16
JP2022542072A (ja) 2022-09-29
US20220267320A1 (en) 2022-08-25
CA3148227A1 (en) 2021-01-28
CN118955500A (zh) 2024-11-15
KR20250174707A (ko) 2025-12-12

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