CN108349983B - 治疗癌症有用的二氢咪唑并吡嗪酮衍生物 - Google Patents

治疗癌症有用的二氢咪唑并吡嗪酮衍生物 Download PDF

Info

Publication number
CN108349983B
CN108349983B CN201680064567.2A CN201680064567A CN108349983B CN 108349983 B CN108349983 B CN 108349983B CN 201680064567 A CN201680064567 A CN 201680064567A CN 108349983 B CN108349983 B CN 108349983B
Authority
CN
China
Prior art keywords
methyl
pyrimidin
dihydroimidazo
amino
pyrazol
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
CN201680064567.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN108349983A (zh
Inventor
R.A.沃德
C.D.琼斯
S.斯瓦罗
M.A.格雷厄姆
A.H.多布森
J.F.麦凯布
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 CN108349983A publication Critical patent/CN108349983A/zh
Application granted granted Critical
Publication of CN108349983B publication Critical patent/CN108349983B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
CN201680064567.2A 2015-11-09 2016-11-08 治疗癌症有用的二氢咪唑并吡嗪酮衍生物 Active CN108349983B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562252726P 2015-11-09 2015-11-09
US62/252726 2015-11-09
US201662401351P 2016-09-29 2016-09-29
US62/401351 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
CN108349983A CN108349983A (zh) 2018-07-31
CN108349983B true CN108349983B (zh) 2021-02-26

Family

ID=57241113

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680064567.2A Active CN108349983B (zh) 2015-11-09 2016-11-08 治疗癌症有用的二氢咪唑并吡嗪酮衍生物

Country Status (35)

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

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3365334T3 (pl) 2015-10-21 2024-11-25 Otsuka Pharmaceutical Co., Ltd. Związki benzolaktamu jako inhibitory kinazy białkowej
PE20181288A1 (es) * 2015-11-09 2018-08-07 Astrazeneca Ab Derivados de dihidroimidazopirazinona usados en el tratamiento del cancer
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
JP7352981B2 (ja) * 2018-10-10 2023-09-29 深▲チェン▼市塔吉瑞生物医薬有限公司 ジヒドロイミダゾピラジノン化合物、該化合物を含む組成物およびその使用
TW202102511A (zh) 2019-03-28 2021-01-16 大陸商江蘇恆瑞醫藥股份有限公司 噻吩并雜環類衍生物、其製備方法及其在醫藥上的應用
CN113825757B (zh) 2019-05-24 2023-10-20 江苏恒瑞医药股份有限公司 取代的稠合双环类衍生物、其制备方法及其在医药上的应用
CA3140475A1 (en) 2019-06-06 2020-12-10 Wei-Guo Su Tricyclic compounds and their use
CA3157504A1 (en) * 2019-12-05 2021-06-10 Astrazeneca Ab Process and intermediates for the production of formula (i)
AU2020398022B2 (en) * 2019-12-06 2023-04-27 D3 Bio (Wuxi) Co., Ltd. Thiazololactam compound as ERK inhibitor and use thereof
EP4223758A4 (en) 2020-09-29 2024-04-03 Jiangsu Hengrui Pharmaceuticals Co., Ltd. CRYSTALLINE FORM OF A PYRROLO-HETEROCYCLIC DERIVATIVE AND PREPARATION METHOD THEREFOR
AR126166A1 (es) * 2021-06-18 2023-09-27 Antengene Discovery Ltd Combinación de un inhibidor de erk y un inhibidor de kras y usos de estos
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
WO2023081857A1 (en) 2021-11-04 2023-05-11 Skyhawk Therapeutics, Inc. Condensed pyridazine amine derivatives treating sca3
WO2023212237A1 (en) 2022-04-27 2023-11-02 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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101326188A (zh) * 2005-10-14 2008-12-17 西克拉塞尔有限公司 嘧啶-4-基-3,4-二氢-2h-吡咯并[1,2a]吡嗪-1-酮化合物
CN101611007A (zh) * 2006-12-20 2009-12-23 先灵公司 新颖的jnk抑制剂
CN103403007A (zh) * 2010-12-22 2013-11-20 詹森药业有限公司 用作β-分泌酶(BACE)抑制剂的5,6-二氢-咪唑并[1,2-a]吡嗪-8-基胺衍生物
CN104703987A (zh) * 2011-10-10 2015-06-10 H.隆德贝克有限公司 具有咪唑并吡嗪酮骨架的pde9抑制剂

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4683195A (en) 1986-01-30 1987-07-28 Cetus Corporation Process for amplifying, detecting, and/or-cloning nucleic acid sequences
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US7485640B2 (en) * 2002-11-06 2009-02-03 Merck Sharp & Dohme Limited Imidazopyrazinones as GABA-A receptor anxiolytics
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
SI2820009T1 (en) 2012-03-01 2018-05-31 Array Biopharma, Inc. Serine / Threonine kinase inhibitors
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
JP6449293B2 (ja) * 2013-12-06 2019-01-09 ジェネンテック, 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
KR102379517B1 (ko) 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
KR102396710B1 (ko) 2013-12-30 2022-05-10 어레이 바이오파마 인크. 세린/트레오닌 키나제 저해제
AR099989A1 (es) 2014-04-09 2016-08-31 Genentech Inc Proceso de preparación de (s)-1-(1-(4-cloro-3-fluorofenil)-2-hidroxietil)-4-(2-((1-metil-1h-pirazol-5-il)amino)pirimidin-4-il)-2(1h)-ona y sus sales
US10412619B2 (en) * 2014-11-14 2019-09-10 Qualcomm Incorporated Buffer status report for eDCS
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
EP3303335B1 (en) 2015-06-03 2021-07-28 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
PE20181288A1 (es) * 2015-11-09 2018-08-07 Astrazeneca Ab Derivados de dihidroimidazopirazinona usados en el tratamiento del cancer

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101326188A (zh) * 2005-10-14 2008-12-17 西克拉塞尔有限公司 嘧啶-4-基-3,4-二氢-2h-吡咯并[1,2a]吡嗪-1-酮化合物
CN101611007A (zh) * 2006-12-20 2009-12-23 先灵公司 新颖的jnk抑制剂
CN103403007A (zh) * 2010-12-22 2013-11-20 詹森药业有限公司 用作β-分泌酶(BACE)抑制剂的5,6-二氢-咪唑并[1,2-a]吡嗪-8-基胺衍生物
CN104703987A (zh) * 2011-10-10 2015-06-10 H.隆德贝克有限公司 具有咪唑并吡嗪酮骨架的pde9抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase;Jeffrey T.Bagdanoff 等;《Bioorganic & Medicinal Chemistry Letters》;20150730;第25卷;第3788-3792页 *

Also Published As

Publication number Publication date
EA038028B1 (ru) 2021-06-24
MY197626A (en) 2023-06-29
HRP20200342T1 (hr) 2020-06-12
AU2016351813A1 (en) 2018-06-21
PT3374359T (pt) 2020-03-27
CR20180316A (es) 2018-10-05
US9902731B2 (en) 2018-02-27
EA201891063A1 (ru) 2018-12-28
BR112018008397B1 (pt) 2023-12-12
CO2018004857A2 (es) 2018-07-19
SMT202000152T1 (it) 2020-05-08
LT3374359T (lt) 2020-03-25
JP2019503337A (ja) 2019-02-07
ZA201803742B (en) 2020-08-26
PE20181288A1 (es) 2018-08-07
AU2016351813B2 (en) 2019-05-30
US20170204100A1 (en) 2017-07-20
SV2018005687A (es) 2018-07-20
MX376639B (es) 2025-03-07
KR20180074788A (ko) 2018-07-03
CY1123627T1 (el) 2022-03-24
NI201800058A (es) 2018-10-18
TW201728586A (zh) 2017-08-16
RS60155B1 (sr) 2020-05-29
EP3374359B1 (en) 2020-01-08
MX2018005725A (es) 2018-08-14
DK3374359T3 (da) 2020-03-30
IL258953A (en) 2018-06-28
US10202391B2 (en) 2019-02-12
EP3374359A1 (en) 2018-09-19
CL2018001226A1 (es) 2018-10-05
PL3374359T3 (pl) 2020-06-29
CN108349983A (zh) 2018-07-31
PH12018500987A1 (en) 2019-01-28
SI3374359T1 (sl) 2020-04-30
BR112018008397A2 (pt) 2018-10-23
ES2780650T3 (es) 2020-08-26
TN2018000119A1 (en) 2019-10-04
ME03770B (me) 2021-04-20
SG11201803066VA (en) 2018-05-30
WO2017080979A1 (en) 2017-05-18
HK1256283A1 (en) 2019-09-20
JP6877423B2 (ja) 2021-05-26
CA3003549A1 (en) 2017-05-18
US20180237443A1 (en) 2018-08-23
TWI730012B (zh) 2021-06-11

Similar Documents

Publication Publication Date Title
CN108349983B (zh) 治疗癌症有用的二氢咪唑并吡嗪酮衍生物
CN106459010B (zh) 用作fgfr激酶调节剂的喹喔啉衍生物
EP2948447B1 (en) Chemical compounds
WO2017080980A1 (en) Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer
JP6898919B2 (ja) 新規化合物
CN108137546B (zh) 双杂芳基取代的1,4-苯并二氮杂卓化合物及其用于治疗癌症的用途
HK1256283B (en) Dihydroimidazopyrazinone derivatives useful in the treatment of cancer
HK1214592B (en) Chemical compounds
HK1256593A1 (en) Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer
HK1256593B (en) Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer
HK1254965B (zh) 新化合物

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant