JP2018533552A - 二重ｄｙｒｋ１／ｃｌｋ１阻害剤としての新規なピロロ［２，３−ｄ］ピリミジン誘導体 - Google Patents

二重ｄｙｒｋ１／ｃｌｋ１阻害剤としての新規なピロロ［２，３−ｄ］ピリミジン誘導体 Download PDF

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JP2018533552A
JP2018533552A JP2018516488A JP2018516488A JP2018533552A JP 2018533552 A JP2018533552 A JP 2018533552A JP 2018516488 A JP2018516488 A JP 2018516488A JP 2018516488 A JP2018516488 A JP 2018516488A JP 2018533552 A JP2018533552 A JP 2018533552A
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formula
methyl
compound
pyrrolo
group
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JP2018516488A
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Japanese (ja)
Inventor
フィウマナ，アンドレア
フォロッペ，ニコラス
レイ，スチュアート
ウォームズリー，デイビッド
コッチャイ，アンドラーシュ
ビュルブリッジ，ミッシェル・フランク
クルサレギ，フランシスコ・ウンベルト
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Vernalis R&D Ltd
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Vernalis R&D Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • C07D519/00—Heterocyclic 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)
JP2018516488A 2015-09-30 2016-09-30 二重ｄｙｒｋ１／ｃｌｋ１阻害剤としての新規なピロロ［２，３−ｄ］ピリミジン誘導体 Pending JP2018533552A (ja)

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
JP2018533552A true JP2018533552A (ja) 2018-11-15

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JP2018516488A Pending JP2018533552A (ja) 2015-09-30 2016-09-30 二重ｄｙｒｋ１／ｃｌｋ１阻害剤としての新規なピロロ［２，３−ｄ］ピリミジン誘導体

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)

Families Citing this family (17)

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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.
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
CA2878054C (en) * 2012-06-29 2018-09-11 Pfizer Inc. Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors
JP6487921B2 (ja) * 2013-12-17 2019-03-20 ファイザー・インク ＬＲＲＫ２阻害薬としての新規の３，４−二置換−１Ｈ−ピロロ［２，３−ｂ］ピリジンおよび４，５−二置換−７Ｈ−ピロロ［２，３−ｃ］ピリダジン

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
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
EA201890820A1 (ru) 2018-10-31
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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