AU2016351813B2 - Dihydroimidazopyrazinone derivatives useful in the treatment of cancer - Google Patents

Dihydroimidazopyrazinone derivatives useful in the treatment of cancer Download PDF

Info

Publication number
AU2016351813B2
AU2016351813B2 AU2016351813A AU2016351813A AU2016351813B2 AU 2016351813 B2 AU2016351813 B2 AU 2016351813B2 AU 2016351813 A AU2016351813 A AU 2016351813A AU 2016351813 A AU2016351813 A AU 2016351813A AU 2016351813 B2 AU2016351813 B2 AU 2016351813B2
Authority
AU
Australia
Prior art keywords
methyl
compound
formula
pharmaceutically
amino
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
AU2016351813A
Other languages
English (en)
Other versions
AU2016351813A1 (en
Inventor
Andrew Hornby Dobson
Mark Andrew Graham
Clifford David Jones
James Francis Mccabe
Steven Swallow
Richard Andrew Ward
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
AstraZeneca AB
Original Assignee
AstraZeneca AB
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 AstraZeneca AB filed Critical AstraZeneca AB
Publication of AU2016351813A1 publication Critical patent/AU2016351813A1/en
Application granted granted Critical
Publication of AU2016351813B2 publication Critical patent/AU2016351813B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2016351813A 2015-11-09 2016-11-08 Dihydroimidazopyrazinone derivatives useful in the treatment of cancer Active AU2016351813B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562252726P 2015-11-09 2015-11-09
US62/252,726 2015-11-09
US201662401351P 2016-09-29 2016-09-29
US62/401,351 2016-09-29
PCT/EP2016/076932 WO2017080979A1 (en) 2015-11-09 2016-11-08 Dihydroimidazopyrazinone derivatives useful in the treatment of cancer

Publications (2)

Publication Number Publication Date
AU2016351813A1 AU2016351813A1 (en) 2018-06-21
AU2016351813B2 true AU2016351813B2 (en) 2019-05-30

Family

ID=57241113

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2016351813A Active AU2016351813B2 (en) 2015-11-09 2016-11-08 Dihydroimidazopyrazinone derivatives useful in the treatment of cancer

Country Status (35)

Country Link
US (2) US9902731B2 (https=)
EP (1) EP3374359B1 (https=)
JP (1) JP6877423B2 (https=)
KR (1) KR20180074788A (https=)
CN (1) CN108349983B (https=)
AU (1) AU2016351813B2 (https=)
BR (1) BR112018008397B1 (https=)
CA (1) CA3003549A1 (https=)
CL (1) CL2018001226A1 (https=)
CO (1) CO2018004857A2 (https=)
CR (1) CR20180316A (https=)
CY (1) CY1123627T1 (https=)
DK (1) DK3374359T3 (https=)
EA (1) EA038028B1 (https=)
ES (1) ES2780650T3 (https=)
HR (1) HRP20200342T1 (https=)
IL (1) IL258953A (https=)
LT (1) LT3374359T (https=)
ME (1) ME03770B (https=)
MX (1) MX376639B (https=)
MY (1) MY197626A (https=)
NI (1) NI201800058A (https=)
PE (1) PE20181288A1 (https=)
PH (1) PH12018500987A1 (https=)
PL (1) PL3374359T3 (https=)
PT (1) PT3374359T (https=)
RS (1) RS60155B1 (https=)
SG (1) SG11201803066VA (https=)
SI (1) SI3374359T1 (https=)
SM (1) SMT202000152T1 (https=)
SV (1) SV2018005687A (https=)
TN (1) TN2018000119A1 (https=)
TW (1) TWI730012B (https=)
WO (1) WO2017080979A1 (https=)
ZA (1) ZA201803742B (https=)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3365334B1 (en) 2015-10-21 2024-07-17 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
RS60155B1 (sr) * 2015-11-09 2020-05-29 Astrazeneca Ab Derivati dihidroimidazopirazinona korisni za upotrebu u tretmanu raka
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
US20210386737A1 (en) * 2018-10-10 2021-12-16 Shenzhen Targetrx, Inc. Dihydroimidazopyrazinone compound, composition including same, and use thereof
BR112021017957A2 (pt) 2019-03-28 2021-11-23 Jiangsu Hengrui Medicine Co Derivado tienoeterocíclico, método de preparação do mesmo e uso médico do mesmo
JP2022534224A (ja) 2019-05-24 2022-07-28 江蘇恒瑞医薬股▲ふん▼有限公司 置換縮合二環式誘導体、その調製方法、および医薬におけるその適用
MX2021014961A (es) 2019-06-06 2022-01-24 Hutchison Medipharma Ltd Compuestos triciclicos y su uso.
AU2020397222B2 (en) * 2019-12-05 2023-07-06 Astrazeneca Ab Process and intermediates for the production of formula (i)
WO2021110169A1 (zh) * 2019-12-06 2021-06-10 南京明德新药研发有限公司 作为erk抑制剂的噻唑并内酰胺类化合物及其应用
WO2022068860A1 (zh) 2020-09-29 2022-04-07 江苏恒瑞医药股份有限公司 一种吡咯并杂环类衍生物的晶型及其制备方法
CN117529321A (zh) * 2021-06-18 2024-02-06 上海德琪医药科技有限公司 Erk抑制剂和kras抑制剂的组合及其用途
WO2022268065A1 (en) * 2021-06-22 2022-12-29 Fochon Biosciences, Ltd. Compounds as erk inhibitors
CN117677398A (zh) 2021-07-27 2024-03-08 东丽株式会社 用于癌的治疗和/或预防的药品
US20250127789A1 (en) 2021-11-04 2025-04-24 Skyhawk Therapeutics, Inc. Compositions useful for modulating splicing
US20250340570A1 (en) 2022-04-27 2025-11-06 Skyhawk Therapeutics, Inc. Compositions useful for modulating splicing
US20250304593A1 (en) 2022-05-12 2025-10-02 Skyhawk Therapeutics, Inc. Compositions useful for modulating splicing
WO2024006971A2 (en) * 2022-07-01 2024-01-04 The Scripps Research Institute Antimalarial compounds

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007042784A2 (en) * 2005-10-14 2007-04-19 Cyclacel Limited Pyrimidin-4-yl-3, 4-dihydr0-2h- pyrrolo [1, 2a] pyrazin-1-one compounds
WO2012085038A1 (en) * 2010-12-22 2012-06-28 Janssen Pharmaceutica Nv 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
WO2016162325A1 (en) * 2015-04-07 2016-10-13 Astrazeneca Ab Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4683195A (en) 1986-01-30 1987-07-28 Cetus Corporation Process for amplifying, detecting, and/or-cloning nucleic acid sequences
US7485640B2 (en) * 2002-11-06 2009-02-03 Merck Sharp & Dohme Limited Imidazopyrazinones as GABA-A receptor anxiolytics
CN101611007A (zh) * 2006-12-20 2009-12-23 先灵公司 新颖的jnk抑制剂
SG11201502728WA (en) * 2011-10-10 2015-05-28 Lundbeck & Co As H Pde9i with imidazo pyrazinone backbone
JP2013166727A (ja) * 2012-02-16 2013-08-29 Dainippon Sumitomo Pharma Co Ltd ジヒドロイミダゾピラジノン誘導体
HUE053994T2 (hu) 2012-03-01 2021-08-30 Array Biopharma Inc Szerin/treonin kináz inhibitorok
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
EP3077401B1 (en) * 2013-12-06 2018-04-18 Genentech, Inc. Serine/threonine kinase inhibitors
KR102379517B1 (ko) 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
JP6642942B2 (ja) * 2013-12-30 2020-02-12 アレイ バイオファーマ、インコーポレイテッド セリン/トレオニンキナーゼ阻害剤
MY188526A (en) 2014-04-09 2021-12-18 Genentech Inc Process for the manufacturing of medicaments
US10412619B2 (en) * 2014-11-14 2019-09-10 Qualcomm Incorporated Buffer status report for eDCS
WO2016192064A1 (en) 2015-06-03 2016-12-08 Js Innopharm (Shanghai) Ltd. Heterocyclic compounds for treating psoriasis
CN107849046B (zh) 2015-06-03 2020-06-12 常州捷凯医药科技有限公司 作为erk抑制剂的杂环化合物
RS60155B1 (sr) * 2015-11-09 2020-05-29 Astrazeneca Ab Derivati dihidroimidazopirazinona korisni za upotrebu u tretmanu raka

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007042784A2 (en) * 2005-10-14 2007-04-19 Cyclacel Limited Pyrimidin-4-yl-3, 4-dihydr0-2h- pyrrolo [1, 2a] pyrazin-1-one compounds
WO2012085038A1 (en) * 2010-12-22 2012-06-28 Janssen Pharmaceutica Nv 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
WO2016162325A1 (en) * 2015-04-07 2016-10-13 Astrazeneca Ab Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JEFFREY T. BAGDANOFF ET AL, "Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, AMSTERDAM, NL, (2015-07-30), vol. 25, no. 18, pages 3788 - 3792 *

Also Published As

Publication number Publication date
JP6877423B2 (ja) 2021-05-26
PH12018500987A1 (en) 2019-01-28
PT3374359T (pt) 2020-03-27
EA038028B1 (ru) 2021-06-24
US20170204100A1 (en) 2017-07-20
ZA201803742B (en) 2020-08-26
BR112018008397A2 (pt) 2018-10-23
HK1256283A1 (en) 2019-09-20
DK3374359T3 (da) 2020-03-30
HRP20200342T1 (hr) 2020-06-12
TWI730012B (zh) 2021-06-11
CL2018001226A1 (es) 2018-10-05
RS60155B1 (sr) 2020-05-29
CN108349983B (zh) 2021-02-26
EP3374359B1 (en) 2020-01-08
EP3374359A1 (en) 2018-09-19
BR112018008397B1 (pt) 2023-12-12
CN108349983A (zh) 2018-07-31
JP2019503337A (ja) 2019-02-07
CR20180316A (es) 2018-10-05
WO2017080979A1 (en) 2017-05-18
ES2780650T3 (es) 2020-08-26
US20180237443A1 (en) 2018-08-23
CO2018004857A2 (es) 2018-07-19
ME03770B (me) 2021-04-20
EA201891063A1 (ru) 2018-12-28
SI3374359T1 (sl) 2020-04-30
TW201728586A (zh) 2017-08-16
SV2018005687A (es) 2018-07-20
CY1123627T1 (el) 2022-03-24
MX376639B (es) 2025-03-07
MY197626A (en) 2023-06-29
PL3374359T3 (pl) 2020-06-29
MX2018005725A (es) 2018-08-14
TN2018000119A1 (en) 2019-10-04
AU2016351813A1 (en) 2018-06-21
SG11201803066VA (en) 2018-05-30
KR20180074788A (ko) 2018-07-03
IL258953A (en) 2018-06-28
US10202391B2 (en) 2019-02-12
PE20181288A1 (es) 2018-08-07
CA3003549A1 (en) 2017-05-18
NI201800058A (es) 2018-10-18
LT3374359T (lt) 2020-03-25
US9902731B2 (en) 2018-02-27
SMT202000152T1 (it) 2020-05-08

Similar Documents

Publication Publication Date Title
AU2016351813B2 (en) Dihydroimidazopyrazinone derivatives useful in the treatment of cancer
WO2017080980A1 (en) Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer
AU2017349797B2 (en) 6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer
EP2948447B1 (en) Chemical compounds
RU2747645C2 (ru) Новые соединения
WO2016162325A1 (en) Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors
HK1256283B (en) Dihydroimidazopyrazinone derivatives useful in the treatment of cancer
KR20180052631A (ko) 비-헤테로아릴 치환된 1,4-벤조디아제핀 및 암의 치료를 위한 이의 용도
HK1214592B (en) Chemical compounds
HK1256593B (en) Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer
HK1256593A1 (en) Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)