EA201890820A1 - НОВЫЕ ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ДВОЙСТВЕННЫХ ИНГИБИТОРОВ DYRK1/CLK1 - Google Patents

НОВЫЕ ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ДВОЙСТВЕННЫХ ИНГИБИТОРОВ DYRK1/CLK1

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Publication number
EA201890820A1
EA201890820A1 EA201890820A EA201890820A EA201890820A1 EA 201890820 A1 EA201890820 A1 EA 201890820A1 EA 201890820 A EA201890820 A EA 201890820A EA 201890820 A EA201890820 A EA 201890820A EA 201890820 A1 EA201890820 A1 EA 201890820A1
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EA
Eurasian Patent Office
Prior art keywords
dyrk1
clk1
pyrimidine derivatives
dual inhibitors
new pyrrolo
Prior art date
Application number
EA201890820A
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English (en)
Russian (ru)
Inventor
Андреа Фиумана
Николя Фолопп
Стюарт Рэй
Дэвид Уолмсли
Андраш Кочи
Микаэль Франк Бёрбридж
Франсиско Умберто Крузалеги
Original Assignee
Ле Лаборатуар Сервье
Верналис (Р&Д) Лимитед
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.)
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Publication date
Application filed by Ле Лаборатуар Сервье, Верналис (Р&Д) Лимитед filed Critical Ле Лаборатуар Сервье
Publication of EA201890820A1 publication Critical patent/EA201890820A1/ru

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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)
EA201890820A 2015-09-30 2016-09-30 НОВЫЕ ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ДВОЙСТВЕННЫХ ИНГИБИТОРОВ DYRK1/CLK1 EA201890820A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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
EA201890820A1 true EA201890820A1 (ru) 2018-10-31

Family

ID=54979756

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201890820A EA201890820A1 (ru) 2015-09-30 2016-09-30 НОВЫЕ ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ДВОЙСТВЕННЫХ ИНГИБИТОРОВ DYRK1/CLK1

Country Status (26)

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

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Publication number Priority date Publication date Assignee Title
JOP20180094A1 (ar) 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
KR102054910B1 (ko) * 2017-12-19 2019-12-12 한림제약(주) 피롤로[2,3-d]피리미딘 유도체 또는 이의 염 및 이를 포함하는 약학 조성물
CN113164476A (zh) * 2018-09-28 2021-07-23 代表亚利桑那大学的亚利桑那校董会 Dyrk1/clk的小分子抑制剂及其用途
US11071730B2 (en) 2018-10-31 2021-07-27 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
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
WO2020237025A1 (en) 2019-05-23 2020-11-26 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
WO2022117012A1 (zh) * 2020-12-02 2022-06-09 百极弘烨(广东)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
US20240261297A1 (en) * 2021-05-20 2024-08-08 St. John's Cancer Institute Anti-cdk inhibitors for cancer treatment
WO2023064349A1 (en) * 2021-10-12 2023-04-20 Biosplice Therapeutics, Inc. 1h-pyrrolo[2,3-b]pyridines as dyrk1a inhibitors
EP4415816A1 (en) 2021-10-12 2024-08-21 BioSplice Therapeutics, Inc. Pyrrolo[2,1-f][1,2,4]triazines derivatives as inhibitors of dyrk1a
UY39978A (es) * 2021-10-12 2023-04-14 Biosplice Therapeutics Inc 7h-pirrolo[2,3-d]pirimidinas y preparación y usos de las mismas
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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BRPI0610322B8 (pt) 2005-05-20 2021-05-25 Methylgene Inc inibidores de sinalização de receptor de vegf e de receptor de hgf e composição farmacêutica
BRPI0617241A2 (pt) 2005-10-13 2016-11-08 Glaxo Group Ltd composto ou um sal ou solvato do mesmo, composição farmacêutica, método para tratar uma doença ou condição mediada por atividade syk inadequada em um mamífero, e, uso de um composto ou um sal ou solvato farmaceuticamente aceitável do mesmo
ATE531718T1 (de) 2006-03-11 2011-11-15 Vernalis R&D Ltd Als hsp90-inhibitoren verwendete pyrrolopyrimidinderivate
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.
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Also Published As

Publication number Publication date
MX2018003861A (es) 2018-08-16
KR20180054856A (ko) 2018-05-24
HK1255467A1 (zh) 2019-08-16
NI201800042A (es) 2018-06-21
CN108137582A (zh) 2018-06-08
EP3356364A1 (en) 2018-08-08
IL258231A (en) 2018-05-31
US20180273538A1 (en) 2018-09-27
JP2018533552A (ja) 2018-11-15
PH12018500605A1 (en) 2018-09-24
BR112018005851A2 (pt) 2018-10-09
FR3041640A1 (OSRAM) 2017-03-31
SV2018005656A (es) 2018-08-10
AU2016333508A1 (en) 2018-04-12
TN2018000087A1 (en) 2019-07-08
PE20190337A1 (es) 2019-03-07
CA2999937A1 (en) 2017-04-06
CL2018000786A1 (es) 2018-09-28
ECSP18023286A (es) 2018-04-30
DOP2018000082A (es) 2018-10-15
WO2017055533A1 (en) 2017-04-06
CU20180027A7 (es) 2018-07-05
CR20180176A (es) 2018-05-31
FR3041640B1 (fr) 2019-05-17
MA43021A (fr) 2018-08-08
CO2018003466A2 (es) 2018-07-10

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