TN2018000087A1 - New pyrrolo[2,3-d]pyrimidine derivatives as dual dyrk1/clk1 inhibitors - Google Patents

New pyrrolo[2,3-d]pyrimidine derivatives as dual dyrk1/clk1 inhibitors

Info

Publication number
TN2018000087A1
TN2018000087A1 TNP/2018/000087A TN2018000087A TN2018000087A1 TN 2018000087 A1 TN2018000087 A1 TN 2018000087A1 TN 2018000087 A TN2018000087 A TN 2018000087A TN 2018000087 A1 TN2018000087 A1 TN 2018000087A1
Authority
TN
Tunisia
Prior art keywords
pyrimidine derivatives
sub
new pyrrolo
dyrk1
dual
Prior art date
Application number
TNP/2018/000087A
Other languages
English (en)
Inventor
Michaël Burbridge
Francisco Cruzalegui
Andrea Fiumana
Nicolas Foloppe
András Kotschy
Stuart Ray
David Walmsley
Original Assignee
Servier Lab
Vernalis R&D Ltd
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 Servier Lab, Vernalis R&D Ltd filed Critical Servier Lab
Publication of TN2018000087A1 publication Critical patent/TN2018000087A1/en

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Classifications

    • 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

Landscapes

  • 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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TNP/2018/000087A 2015-09-30 2016-09-30 New pyrrolo[2,3-d]pyrimidine derivatives as dual dyrk1/clk1 inhibitors TN2018000087A1 (en)

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
TN2018000087A1 true TN2018000087A1 (en) 2019-07-08

Family

ID=54979756

Family Applications (1)

Application Number Title Priority Date Filing Date
TNP/2018/000087A TN2018000087A1 (en) 2015-09-30 2016-09-30 New pyrrolo[2,3-d]pyrimidine derivatives as dual dyrk1/clk1 inhibitors

Country Status (26)

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

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
US12054483B2 (en) 2018-09-28 2024-08-06 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK/CLK and uses thereof
PE20211655A1 (es) 2018-10-31 2021-08-24 Gilead Sciences Inc Compuestos de 6-azabencimidazol sustituidos como inhibidores de hpk1
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
TWI826690B (zh) 2019-05-23 2023-12-21 美商基利科學股份有限公司 經取代之烯吲哚酮化物及其用途
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
WO2022245776A1 (en) * 2021-05-20 2022-11-24 Saint John's Cancer Institute Anti-cdk inhibitors for cancer treatment
CA3234937A1 (en) * 2021-10-12 2023-04-20 Biosplice Therapeutics, Inc. 7h-pyrrolo[2,3-d]pyrimidines and preparation as dyrk1a inhibitors
EP4415817A1 (en) * 2021-10-12 2024-08-21 BioSplice Therapeutics, Inc. 1h-pyrrolo[2,3-b]pyridines as dyrk1a inhibitors
UY39979A (es) 2021-10-12 2023-04-14 Biosplice Therapeutics Inc Pirrolo[2,1-f][1,2,4]triazinas 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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Publication number Priority date Publication date Assignee Title
JP5148499B2 (ja) 2005-05-20 2013-02-20 メチルジーン インコーポレイテッド Vegf受容体およびhgf受容体シグナル伝達の阻害剤
US20080004295A1 (en) 2005-10-13 2008-01-03 Gore Paul M Novel compounds
JP2009533323A (ja) 2006-03-11 2009-09-17 ヴァーナリス アールアンドディー リミテッド Hsp90阻害剤として用いられるピロロピリミジン誘導体
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
MD20140130A2 (ro) * 2012-06-29 2015-04-30 Pfizer Inc. 4-(amino-substituite)-7H-pirolo[2,3-d]pirimidine noi ca inhibitori de LRRK2
WO2015092592A1 (en) * 2013-12-17 2015-06-25 Pfizer Inc. Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors

Also Published As

Publication number Publication date
MA43021A (fr) 2018-08-08
FR3041640B1 (fr) 2019-05-17
EP3356364A1 (en) 2018-08-08
CR20180176A (es) 2018-05-31
BR112018005851A2 (pt) 2018-10-09
CN108137582A (zh) 2018-06-08
HK1255467A1 (zh) 2019-08-16
KR20180054856A (ko) 2018-05-24
CU20180027A7 (es) 2018-07-05
DOP2018000082A (es) 2018-10-15
CA2999937A1 (en) 2017-04-06
MX2018003861A (es) 2018-08-16
NI201800042A (es) 2018-06-21
WO2017055533A1 (en) 2017-04-06
CO2018003466A2 (es) 2018-07-10
FR3041640A1 (enExample) 2017-03-31
PE20190337A1 (es) 2019-03-07
PH12018500605A1 (en) 2018-09-24
SV2018005656A (es) 2018-08-10
IL258231A (en) 2018-05-31
AU2016333508A1 (en) 2018-04-12
ECSP18023286A (es) 2018-04-30
EA201890820A1 (ru) 2018-10-31
US20180273538A1 (en) 2018-09-27
CL2018000786A1 (es) 2018-09-28
JP2018533552A (ja) 2018-11-15

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