CN103534254B - 作为抗肿瘤剂的三环和四环吡唑并[3,4-b]吡啶化合物 - Google Patents

作为抗肿瘤剂的三环和四环吡唑并[3,4-b]吡啶化合物 Download PDF

Info

Publication number
CN103534254B
CN103534254B CN201280023479.XA CN201280023479A CN103534254B CN 103534254 B CN103534254 B CN 103534254B CN 201280023479 A CN201280023479 A CN 201280023479A CN 103534254 B CN103534254 B CN 103534254B
Authority
CN
China
Prior art keywords
group
alkyl
aromatic
compound
formula
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.)
Expired - Fee Related
Application number
CN201280023479.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN103534254A (zh
Inventor
R·拉博
K·贝叶古拉
E·B·卡伦
P·施密特
N·拉耶
P·迈耶
E·富尼耶
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.)
Pierre Fabre Medicament SA
Original Assignee
Pierre Fabre Medicament SA
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 Pierre Fabre Medicament SA filed Critical Pierre Fabre Medicament SA
Publication of CN103534254A publication Critical patent/CN103534254A/zh
Application granted granted Critical
Publication of CN103534254B publication Critical patent/CN103534254B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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
    • C07D491/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/12—Heterocyclic 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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
    • C07D493/14—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280023479.XA 2011-04-12 2012-04-12 作为抗肿瘤剂的三环和四环吡唑并[3,4-b]吡啶化合物 Expired - Fee Related CN103534254B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR1153200A FR2974088A1 (fr) 2011-04-12 2011-04-12 Composes pyrazolo[3,4-b]pyridines tri- et tetracycliques comme agent anticancereux
FR1153200 2011-04-12
PCT/EP2012/056637 WO2012140114A1 (en) 2011-04-12 2012-04-12 Tri- and tetracyclic pyrazolo[3,4-b]pyridine compounds as antineoplastic agent

Publications (2)

Publication Number Publication Date
CN103534254A CN103534254A (zh) 2014-01-22
CN103534254B true CN103534254B (zh) 2015-11-25

Family

ID=44512344

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280023479.XA Expired - Fee Related CN103534254B (zh) 2011-04-12 2012-04-12 作为抗肿瘤剂的三环和四环吡唑并[3,4-b]吡啶化合物

Country Status (15)

Country Link
US (1) US9085575B2 (enExample)
EP (1) EP2697222A1 (enExample)
JP (1) JP5972964B2 (enExample)
KR (1) KR20140023341A (enExample)
CN (1) CN103534254B (enExample)
AR (1) AR085987A1 (enExample)
AU (1) AU2012241891B2 (enExample)
BR (1) BR112013026355A2 (enExample)
CA (1) CA2832704A1 (enExample)
FR (1) FR2974088A1 (enExample)
MX (1) MX2013011854A (enExample)
RU (1) RU2013148922A (enExample)
TW (1) TWI560187B (enExample)
WO (1) WO2012140114A1 (enExample)
ZA (1) ZA201307783B (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
PH12019502809B1 (en) 2012-06-13 2024-04-24 Incyte Holdings Corp Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
MY181497A (en) 2013-04-19 2020-12-23 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
US10053477B2 (en) 2014-07-04 2018-08-21 Qilu Pharmaceutical Co., Ltd. Spirocyclic aryl phosphorus oxide and aryl phosphorus sulfide
CN104447736B (zh) * 2014-10-14 2016-06-08 雅安职业技术学院 一种veranamine的合成方法
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9974784B2 (en) * 2015-01-21 2018-05-22 The Texas A&M University System Inhibitors of activin-like receptor kinases
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JP7568512B2 (ja) 2018-05-04 2024-10-16 インサイト・コーポレイション Ｆｇｆｒ阻害剤の塩
CN112867716B (zh) 2018-05-04 2024-09-13 因赛特公司 Fgfr抑制剂的固体形式和其制备方法
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11607416B2 (en) 2019-10-14 2023-03-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
US11897891B2 (en) 2019-12-04 2024-02-13 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US20230303570A1 (en) * 2020-08-07 2023-09-28 Abm Therapeutics Corporation Kinase inhibitors and uses thereof
CA3215903A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
JP2024522188A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101525497A (zh) * 2008-03-06 2009-09-09 中国科学院理化技术研究所 吡唑啉吡啶并苯并香豆素荧光染料衍生物及其合成方法和用途

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2004259012C1 (en) * 2003-07-23 2012-08-02 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
CA2619049A1 (en) * 2005-08-16 2007-02-22 Irm, Llc Compounds and compositions as protein kinase inhibitors
US20100113415A1 (en) * 2008-05-29 2010-05-06 Rajapakse Hemaka A Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101525497A (zh) * 2008-03-06 2009-09-09 中国科学院理化技术研究所 吡唑啉吡啶并苯并香豆素荧光染料衍生物及其合成方法和用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"Monastrol analogs: A synthesis of pyrazolopyridine, benzopyranopyrazolopyri-dine, and oxygen-bridged azolopyrimidine derivatives and their biological screening";Jan Svetlilc et al;《Bioorganic & Medicinal Chemistry Letters》;20100526;第20卷(第14期);第4074页图2 *

Also Published As

Publication number Publication date
CA2832704A1 (en) 2012-10-18
US9085575B2 (en) 2015-07-21
KR20140023341A (ko) 2014-02-26
JP5972964B2 (ja) 2016-08-17
HK1190397A1 (zh) 2014-07-04
AR085987A1 (es) 2013-11-13
CN103534254A (zh) 2014-01-22
RU2013148922A (ru) 2015-05-20
US20140031362A1 (en) 2014-01-30
TW201247665A (en) 2012-12-01
AU2012241891B2 (en) 2016-06-16
TWI560187B (en) 2016-12-01
JP2014510774A (ja) 2014-05-01
EP2697222A1 (en) 2014-02-19
AU2012241891A1 (en) 2013-10-31
FR2974088A1 (fr) 2012-10-19
BR112013026355A2 (pt) 2016-12-27
WO2012140114A1 (en) 2012-10-18
ZA201307783B (en) 2015-01-28
MX2013011854A (es) 2013-11-01

Similar Documents

Publication Publication Date Title
CN103534254B (zh) 作为抗肿瘤剂的三环和四环吡唑并[3,4-b]吡啶化合物
CN114163457B (zh) 嘧啶并五元氮杂环化合物及其用途
AU747920B2 (en) Bicyclic pyridine and pyrimidine derivatives as neuropeptide Y receptor antagonists
JP4287649B2 (ja) Ｈｉｖインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類
TWI576346B (zh) 雙環吡嗪酮衍生物
ES2775217T3 (es) Inhibidores de bromodominio
CN103958479B (zh) 吡唑并喹啉酮衍生物、其制备和其治疗用途
JP6457623B2 (ja) ２，４−二置換７Ｈ−ピロロ［２，３−ｄ］ピリミジン誘導体、その製造方法および医薬における使用
JP5350277B2 (ja) Ｐｉ３ｋ阻害剤としてのピロロピリミジン誘導体及びその用途
KR20170069199A (ko) 섬유 아세포 성장 인자 수용체 키나아제 억제제인 인다졸계 화합물 및 이의 제조와 응용
TW201927792A (zh) 作為溴結構域蛋白質抑制劑的化合物和組合物
JP2004517860A (ja) Ｈｉｖインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類
JP2010533674A (ja) Ｍｋ２阻害剤として有用なヘテロ環式化合物
CN115028648B (zh) 三并环化合物及其药物组合物和应用
JP2003516989A (ja) Ｇａｂａ受容体リガンドとしてのピラゾロ−ピリジン誘導体
TWI336253B (en) Diazaindole-dicarbonyl-piperazinyl antiviral agents
CN103313970A (zh) 新型二环式化合物或其盐
CN114605390A (zh) 具有cdk激酶抑制活性的化合物、其药物组合物和用途
US20210032239A1 (en) Compounds and pharmaceutical compositions for modulating sgk activity, and methods thereof
CN106146493A (zh) 吡唑并[3,4-b]吡啶类和吲唑类化合物的制备方法和用途
CN115677730B (zh) 8-氧-3-氮杂二环[3.2.1]辛烷类化合物或其盐及其制备方法和用途
EP1556381B1 (en) Pyrazole amides for treating hiv infections
CN116836184A (zh) Wee1激酶抑制剂的制备及其应用
HK1190397B (en) Tri- and tetracyclic pyrazolo[3,4-b]pyridine compounds as antineoplastic agent
JP2021011492A (ja) ４Ｈ−ピリド［１，２−ａ］ピリミジン−４−オン化合物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1190397

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1190397

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20151125

Termination date: 20170412