KR20180054856A - 이중 dyrk1/clk1 억제제로서의 신규한 피롤로[2,3-d]피리미딘 유도체 - Google Patents

이중 dyrk1/clk1 억제제로서의 신규한 피롤로[2,3-d]피리미딘 유도체 Download PDF

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KR20180054856A
KR20180054856A KR1020187012166A KR20187012166A KR20180054856A KR 20180054856 A KR20180054856 A KR 20180054856A KR 1020187012166 A KR1020187012166 A KR 1020187012166A KR 20187012166 A KR20187012166 A KR 20187012166A KR 20180054856 A KR20180054856 A KR 20180054856A
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methyl
group
formula
compound
pyrrolo
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Korean (ko)
Inventor
안드레아 피우마나
니콜라스 폴로페
스튜어트 레이
데이비드 웜슬리
안드라스 코치
미첼 프랭크 버브리지
프란시스코 험베르토 크루자레귀
Original Assignee
르 라보레또레 쎄르비에르
베르날리스 (알 앤드 디) 리미티드
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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020187012166A 2015-09-30 2016-09-30 이중 dyrk1/clk1 억제제로서의 신규한 피롤로[2,3-d]피리미딘 유도체 Withdrawn KR20180054856A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR15/59259 2015-09-30
FR1559259A FR3041640B1 (fr) 2015-09-30 2015-09-30 NOUVEAUX DERIVES DE PYRROLO[2,3-d]PYRIMIDINE, LEUR PROCEDE DE PREPRATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
PCT/EP2016/073403 WO2017055533A1 (en) 2015-09-30 2016-09-30 New pyrrolo[2,3-d]pyrimidine derivatives as dual dyrk1/clk1 inhibitors

Publications (1)

Publication Number Publication Date
KR20180054856A true KR20180054856A (ko) 2018-05-24

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KR1020187012166A Withdrawn KR20180054856A (ko) 2015-09-30 2016-09-30 이중 dyrk1/clk1 억제제로서의 신규한 피롤로[2,3-d]피리미딘 유도체

Country Status (26)

Country Link
US (1) US20180273538A1 (https=)
EP (1) EP3356364A1 (https=)
JP (1) JP2018533552A (https=)
KR (1) KR20180054856A (https=)
CN (1) CN108137582A (https=)
AU (1) AU2016333508A1 (https=)
BR (1) BR112018005851A2 (https=)
CA (1) CA2999937A1 (https=)
CL (1) CL2018000786A1 (https=)
CO (1) CO2018003466A2 (https=)
CR (1) CR20180176A (https=)
CU (1) CU20180027A7 (https=)
DO (1) DOP2018000082A (https=)
EA (1) EA201890820A1 (https=)
EC (1) ECSP18023286A (https=)
FR (1) FR3041640B1 (https=)
HK (1) HK1255467A1 (https=)
IL (1) IL258231A (https=)
MA (1) MA43021A (https=)
MX (1) MX2018003861A (https=)
NI (1) NI201800042A (https=)
PE (1) PE20190337A1 (https=)
PH (1) PH12018500605A1 (https=)
SV (1) SV2018005656A (https=)
TN (1) TN2018000087A1 (https=)
WO (1) WO2017055533A1 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
KR102054910B1 (ko) * 2017-12-19 2019-12-12 한림제약(주) 피롤로[2,3-d]피리미딘 유도체 또는 이의 염 및 이를 포함하는 약학 조성물
US12528810B2 (en) 2018-03-01 2026-01-20 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK/CLK and uses thereof
CA3118093A1 (en) * 2018-09-28 2020-04-02 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of dyrk1/clk and uses thereof
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
US11203591B2 (en) 2018-10-31 2021-12-21 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
CN110407744A (zh) * 2019-08-13 2019-11-05 上海毕得医药科技有限公司 一种1-(4-氨基吡啶-2-基)乙酮的合成方法
AR120799A1 (es) * 2019-12-20 2022-03-16 Hoffmann La Roche 2-[4-cloro-6-[2-[4-[[4-(hidroximetil)-1-piperidil]metil]fenil]etinil]-1-oxoisoindolin-2-il]-2-(6,7-dihidro-5h-pirrolo[1,2-c]imidazol-1-il)-n-tiazol-2-il-acetamida como inhibidor de egfr
CN116783198B (zh) * 2020-12-02 2025-10-21 广东弘烨医药科技有限公司 螺环jak抑制剂、含其的药物组合物及其应用
WO2022245776A1 (en) * 2021-05-20 2022-11-24 Saint John's Cancer Institute Anti-cdk inhibitors for cancer treatment
PY2289206A (es) * 2021-10-12 2023-11-09 Biosplice Therapeutics Inc 7h-pirrolo[2,3-d] pirimidinas y preparación y usos de las mismas
WO2023064349A1 (en) * 2021-10-12 2023-04-20 Biosplice Therapeutics, Inc. 1h-pyrrolo[2,3-b]pyridines as dyrk1a inhibitors
CA3234831A1 (en) 2021-10-12 2023-04-20 Biosplice Therapeutics, Inc. Pyrrolo[2,1-f][1,2,4]triazines derivatives as inhibitors of dyrk1a
WO2023110843A1 (en) * 2021-12-15 2023-06-22 Almirall, S.A. Heterobicyclic derivatives as itk inhibitors
CN116621843B (zh) * 2022-06-13 2024-05-24 四川大学华西医院 一种dna甲基转移酶1抑制剂及其制备方法和用途
CN115785134B (zh) * 2022-10-28 2023-08-29 浙大城市学院 一种含氮杂环的硼酸化合物及制备方法和应用

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KR101378716B1 (ko) 2005-05-20 2014-04-10 메틸진 인코포레이티드 Vegf 수용체 및 hgf 수용체 신호전달의 억제제
JP2009511528A (ja) 2005-10-13 2009-03-19 グラクソ グループ リミテッド Syk阻害物質としてのピロロピリミジン誘導体群
EA200801968A1 (ru) 2006-03-11 2009-02-27 Вернэлис (Р&Д) Лтд. Пирролопиримидиновые производные, используемые в качестве ингибиторов hsp90
FR2912744B1 (fr) * 2007-02-16 2012-09-07 Centre Nat Rech Scient Composes pyrrolo°2,3-b!pyridine,composes azaindoles utiles dans la synthese de ces composes pyrrolo°2,3-b!pyridine, leurs procedes de fabrication et leurs utilisations.
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
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Publication number Publication date
PH12018500605A1 (en) 2018-09-24
AU2016333508A1 (en) 2018-04-12
EA201890820A1 (ru) 2018-10-31
WO2017055533A1 (en) 2017-04-06
SV2018005656A (es) 2018-08-10
CA2999937A1 (en) 2017-04-06
CL2018000786A1 (es) 2018-09-28
US20180273538A1 (en) 2018-09-27
HK1255467A1 (zh) 2019-08-16
CO2018003466A2 (es) 2018-07-10
DOP2018000082A (es) 2018-10-15
MA43021A (fr) 2018-08-08
FR3041640B1 (fr) 2019-05-17
ECSP18023286A (es) 2018-04-30
FR3041640A1 (https=) 2017-03-31
NI201800042A (es) 2018-06-21
IL258231A (en) 2018-05-31
TN2018000087A1 (en) 2019-07-08
PE20190337A1 (es) 2019-03-07
JP2018533552A (ja) 2018-11-15
EP3356364A1 (en) 2018-08-08
BR112018005851A2 (pt) 2018-10-09
CR20180176A (es) 2018-05-31
MX2018003861A (es) 2018-08-16
CU20180027A7 (es) 2018-07-05
CN108137582A (zh) 2018-06-08

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Patent event date: 20180427

Patent event code: PA01051R01D

Comment text: International Patent Application

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WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid