KR102351270B1 - Akt 억제제인 디히드로피라졸로아제핀계 화합물 - Google Patents

Akt 억제제인 디히드로피라졸로아제핀계 화합물 Download PDF

Info

Publication number
KR102351270B1
KR102351270B1 KR1020197001396A KR20197001396A KR102351270B1 KR 102351270 B1 KR102351270 B1 KR 102351270B1 KR 1020197001396 A KR1020197001396 A KR 1020197001396A KR 20197001396 A KR20197001396 A KR 20197001396A KR 102351270 B1 KR102351270 B1 KR 102351270B1
Authority
KR
South Korea
Prior art keywords
group
thieno
lcms
esi
dihydro
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
KR1020197001396A
Other languages
English (en)
Korean (ko)
Other versions
KR20190017996A (ko
Inventor
룬 루
지보 장
강 리
리홍 후
찰스 제트. 딩
슈후이 첸
Original Assignee
하얼빈 젠바오 파마슈티컬 컴퍼니, 리미티드
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 하얼빈 젠바오 파마슈티컬 컴퍼니, 리미티드 filed Critical 하얼빈 젠바오 파마슈티컬 컴퍼니, 리미티드
Publication of KR20190017996A publication Critical patent/KR20190017996A/ko
Application granted granted Critical
Publication of KR102351270B1 publication Critical patent/KR102351270B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14Ortho-condensed systems
    • C07D491/147Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020197001396A 2016-06-16 2017-06-13 Akt 억제제인 디히드로피라졸로아제핀계 화합물 Active KR102351270B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201610428049 2016-06-16
CN201610428049.6 2016-06-16
CN201610674021.0 2016-08-15
CN201610674021 2016-08-15
PCT/CN2017/088030 WO2017215588A1 (zh) 2016-06-16 2017-06-13 作为Akt抑制剂的二氢吡唑氮杂卓类化合物

Publications (2)

Publication Number Publication Date
KR20190017996A KR20190017996A (ko) 2019-02-20
KR102351270B1 true KR102351270B1 (ko) 2022-01-14

Family

ID=60663995

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020197001396A Active KR102351270B1 (ko) 2016-06-16 2017-06-13 Akt 억제제인 디히드로피라졸로아제핀계 화합물

Country Status (6)

Country Link
US (1) US10654868B2 (enExample)
EP (1) EP3473628B1 (enExample)
JP (1) JP6900406B2 (enExample)
KR (1) KR102351270B1 (enExample)
CN (1) CN109311908B (enExample)
WO (1) WO2017215588A1 (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019114741A1 (zh) * 2017-12-13 2019-06-20 南京明德新药研发股份有限公司 作为Akt抑制剂的盐型及其晶型
WO2022121788A1 (zh) * 2020-12-07 2022-06-16 南京正大天晴制药有限公司 一种吡唑并氮杂卓类akt抑制剂

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003076429A2 (en) 2002-03-12 2003-09-18 F. Hoffmann-La Roche Ag Azepane derivatives and their use as atk1 inhibitors
WO2008065054A1 (en) 2006-11-28 2008-06-05 Nerviano Medical Sciences S.R.L. Tricyclic indoles and (4,5-dihydro) indoles
WO2009089305A1 (en) 2008-01-07 2009-07-16 Synta Pharmaceuticals Corp. Compounds for inflammation and immune-related uses

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101094833A (zh) * 2004-07-12 2007-12-26 伊邓药品公司 四肽类似物
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
DE602008003055D1 (de) * 2007-05-31 2010-12-02 Nerviano Medical Sciences Srl Zyklokondensierte Azaindole, die als Kinase-Hemmer wirken
WO2009158371A1 (en) 2008-06-26 2009-12-30 Smithklike Beecham Corporation Inhibitors of akt activity
EP2640369A1 (en) 2010-11-17 2013-09-25 F.Hoffmann-La Roche Ag Methods of treating tumors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003076429A2 (en) 2002-03-12 2003-09-18 F. Hoffmann-La Roche Ag Azepane derivatives and their use as atk1 inhibitors
WO2008065054A1 (en) 2006-11-28 2008-06-05 Nerviano Medical Sciences S.R.L. Tricyclic indoles and (4,5-dihydro) indoles
WO2009089305A1 (en) 2008-01-07 2009-07-16 Synta Pharmaceuticals Corp. Compounds for inflammation and immune-related uses

Also Published As

Publication number Publication date
CN109311908B (zh) 2021-05-07
US10654868B2 (en) 2020-05-19
CN109311908A (zh) 2019-02-05
KR20190017996A (ko) 2019-02-20
JP6900406B2 (ja) 2021-07-07
JP2019518052A (ja) 2019-06-27
WO2017215588A1 (zh) 2017-12-21
EP3473628A4 (en) 2019-05-01
US20190233434A1 (en) 2019-08-01
EP3473628B1 (en) 2019-12-11
EP3473628A1 (en) 2019-04-24

Similar Documents

Publication Publication Date Title
EP3293177B1 (en) Tyrosine kinase inhibitor and pharmaceutical composition comprising same
JP6600365B2 (ja) Jak阻害剤
EP3333157B1 (en) Vinyl compounds as fgfr and vegfr inhibitors
JP6494622B2 (ja) カゼインキナーゼ1d/e阻害剤としての置換された4,5,6,7−テトラヒドロピラゾロ[1,5−a]ピラジン誘導体
ES2671354T3 (es) Inhibidores de ADN-PK
EP4079734B1 (en) Triazolopyridazine derivative, preparation method therefor, pharmaceutical composition thereof, and use thereof
AU2013251804A1 (en) DNA-PK inhibitors
JP2020516606A (ja) A2A受容体阻害剤としての[1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体
CN115697993A (zh) 作为axl抑制剂的嘧啶类化合物
JP2018531218A6 (ja) Fgfr及びvegfr阻害剤であるビニル化合物
KR102495840B1 (ko) PI3K 억제제로 사용되는 피리디노[1,2-a]피리미돈 유사체
EP4567038A1 (en) Novel prmt5 inhibitor and use thereof
WO2020186220A1 (en) Compounds as inhibitors of macrophage migration inhibitory factor
CN112292374A (zh) 一种新型磷酸肌醇3-激酶抑制剂及其制备方法和用途
KR102351270B1 (ko) Akt 억제제인 디히드로피라졸로아제핀계 화합물
CN112979654A (zh) 杂芳基稠环化合物、其制备方法及应用
CN112209934B (zh) 含有氮杂螺庚烷的btk抑制剂
TWI690529B (zh) 羥基嘌呤類化合物及其應用
CN113880842A (zh) 取代的炔基杂环化合物
HK40007681B (en) Lsd1 inhibitor and preparation method and application thereof

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20190115

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PN2301 Change of applicant

Patent event date: 20191002

Comment text: Notification of Change of Applicant

Patent event code: PN23011R01D

A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20200401

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20210608

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20211215

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20220111

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20220112

End annual number: 3

Start annual number: 1

PG1601 Publication of registration