HK1255467A1 - 作為雙重dyrk1/clk1抑制劑的新的吡咯並[2，3-d]嘧啶衍生物 - Google Patents

作為雙重dyrk1/clk1抑制劑的新的吡咯並[2，3-d]嘧啶衍生物

Info

Publication number: HK1255467A1
Authority: HK; Hong Kong
Prior art keywords: pyrimidine derivatives; new pyrrolo; dyrk1; dual; clk1
Prior art date: 2015-09-30

Application number

HK18114640.5A

Other languages

English (en)

Inventor

Andrea Fiumana

Nicolas Foloppe

Stuart Ray

David Walmsley

András Kotschy

Michaël Frank Burbridge

Francisco Humberto Cruzalegui

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.)

2015-09-30

Filing date

2018-11-15

Publication date

2019-08-16

2018-11-15 Application filed by Servier Lab, Vernalis R&D Ltd filed Critical Servier Lab

2019-08-16 Publication of HK1255467A1 publication Critical patent/HK1255467A1/zh

Classifications

- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Epidemiology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (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)

HK18114640.5A 2015-09-30 2018-11-15 作為雙重dyrk1/clk1抑制劑的新的吡咯並[2，3-d]嘧啶衍生物 HK1255467A1 (zh)

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
HK1255467A1 true HK1255467A1 (zh)	2019-08-16

Family

ID=54979756

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
HK18114640.5A HK1255467A1 (zh)	2015-09-30	2018-11-15	作為雙重dyrk1/clk1抑制劑的新的吡咯並[2，3-d]嘧啶衍生物

Country Status (26)

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

Families Citing this family (15)

* Cited by examiner, † Cited by third party
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
DK3873903T3 (da)	2018-10-31	2024-04-02	Gilead Sciences Inc	Substituerede 6-azabenzimidazolforbindelser som hpk1-hæmmere
CN112969505B (zh)	2018-10-31	2023-11-14	吉利德科学公司	具有hpk1抑制活性的取代的6-氮杂苯并咪唑化合物
US11453681B2 (en)	2019-05-23	2022-09-27	Gilead Sciences, Inc.	Substituted eneoxindoles and uses thereof
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
WO2022245776A1 (en) *	2021-05-20	2022-11-24	Saint John's Cancer Institute	Anti-cdk inhibitors for cancer treatment
EP4415817A1 (en) *	2021-10-12	2024-08-21	BioSplice Therapeutics, Inc.	1h-pyrrolo[2,3-b]pyridines as dyrk1a inhibitors
EP4415818A1 (en) *	2021-10-12	2024-08-21	BioSplice Therapeutics, Inc.	7h-pyrrolo[2,3-d]pyrimidines and preparation as dyrk1a inhibitors
WO2023064366A1 (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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
KR101378716B1 (ko)	2005-05-20	2014-04-10	메틸진 인코포레이티드	Ｖｅｇｆ 수용체 및 ｈｇｆ 수용체 신호전달의 억제제
KR20080063837A (ko)	2005-10-13	2008-07-07	글락소 그룹 리미티드	Ｓｙｋ 억제제로서의 피롤로피리미딘 유도체
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
AU2013282869B2 (en) *	2012-06-29	2015-12-24	Pfizer Inc.	Novel 4-(substituted-amino)-7H-pyrrolo[2,3-d]pyrimidines as LRRK2 inhibitors
CA2933767C (en) *	2013-12-17	2018-11-06	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

2015
- 2015-09-30 FR FR1559259A patent/FR3041640B1/fr not_active Expired - Fee Related
2016
- 2016-09-30 JP JP2018516488A patent/JP2018533552A/ja active Pending
- 2016-09-30 EA EA201890820A patent/EA201890820A1/ru unknown
- 2016-09-30 MX MX2018003861A patent/MX2018003861A/es unknown
- 2016-09-30 KR KR1020187012166A patent/KR20180054856A/ko unknown
- 2016-09-30 CU CUP2018000027A patent/CU20180027A7/xx unknown
- 2016-09-30 EP EP16774684.1A patent/EP3356364A1/en not_active Withdrawn
- 2016-09-30 CN CN201680058179.3A patent/CN108137582A/zh not_active Withdrawn
- 2016-09-30 CA CA2999937A patent/CA2999937A1/en not_active Abandoned
- 2016-09-30 MA MA043021A patent/MA43021A/fr unknown
- 2016-09-30 US US15/763,626 patent/US20180273538A1/en not_active Abandoned
- 2016-09-30 BR BR112018005851A patent/BR112018005851A2/pt not_active Application Discontinuation
- 2016-09-30 WO PCT/EP2016/073403 patent/WO2017055533A1/en active Application Filing
- 2016-09-30 TN TNP/2018/000087A patent/TN2018000087A1/en unknown
- 2016-09-30 PE PE2018000410A patent/PE20190337A1/es unknown
- 2016-09-30 CR CR20180176A patent/CR20180176A/es unknown
- 2016-09-30 AU AU2016333508A patent/AU2016333508A1/en not_active Abandoned
2018
- 2018-03-19 IL IL258231A patent/IL258231A/en unknown
- 2018-03-20 PH PH12018500605A patent/PH12018500605A1/en unknown
- 2018-03-22 SV SV2018005656A patent/SV2018005656A/es unknown
- 2018-03-23 NI NI201800042A patent/NI201800042A/es unknown
- 2018-03-26 DO DO2018000082A patent/DOP2018000082A/es unknown
- 2018-03-26 CL CL2018000786A patent/CL2018000786A1/es unknown
- 2018-03-26 EC ECIEPI201823286A patent/ECSP18023286A/es unknown
- 2018-03-28 CO CONC2018/0003466A patent/CO2018003466A2/es unknown
- 2018-11-15 HK HK18114640.5A patent/HK1255467A1/zh unknown

Also Published As

Publication number	Publication date
FR3041640A1 (zh)	2017-03-31
CL2018000786A1 (es)	2018-09-28
US20180273538A1 (en)	2018-09-27
EP3356364A1 (en)	2018-08-08
JP2018533552A (ja)	2018-11-15
AU2016333508A1 (en)	2018-04-12
SV2018005656A (es)	2018-08-10
CR20180176A (es)	2018-05-31
DOP2018000082A (es)	2018-10-15
ECSP18023286A (es)	2018-04-30
CN108137582A (zh)	2018-06-08
MX2018003861A (es)	2018-08-16
KR20180054856A (ko)	2018-05-24
IL258231A (en)	2018-05-31
PE20190337A1 (es)	2019-03-07
MA43021A (fr)	2018-08-08
TN2018000087A1 (en)	2019-07-08
FR3041640B1 (fr)	2019-05-17
NI201800042A (es)	2018-06-21
CO2018003466A2 (es)	2018-07-10
EA201890820A1 (ru)	2018-10-31
BR112018005851A2 (pt)	2018-10-09
PH12018500605A1 (en)	2018-09-24
CU20180027A7 (es)	2018-07-05
CA2999937A1 (en)	2017-04-06
WO2017055533A1 (en)	2017-04-06

Publication	Publication Date	Title
HK1255467A1 (zh)	2019-08-16	作為雙重dyrk1/clk1抑制劑的新的吡咯並[2，3-d]嘧啶衍生物
HK1258905A1 (zh)	2019-11-22	作為ret激酶抑制劑的取代的吡唑並[1，5-a]吡啶化合物
ZA201904568B (en)	2021-02-24	Benzodiazepine derivatives as rsv inhibitors
HK1252752A1 (zh)	2019-05-31	新型吡唑並嘧啶衍生物
IL254224A0 (en)	2017-10-31	7-substituted 5-alkyl-[4,2,1]triazolo[5,1-a]pyrimidine derivatives as pde2 inhibitors
ZA201505454B (en)	2016-07-27	Pyrrolo [2, 3 -d]pyrimidine derivatives as inhibitors of janus- related kinases (jak)
SI2857404T1 (sl)	2017-11-30	Imidazo(1,2-b)piridazin derivati kot kinazni inhibitorji
EP3231805A4 (en)	2018-06-13	Salt of pyrrolo[2,3-d]pyrimidine compound and novel polymorph of salt
HK1255804A1 (zh)	2019-08-23	作為雙重dyrk1/clk1抑制劑的新的咪唑並[4，5-b]吡啶衍生物
IL242162B (en)	2019-06-30	Pyrrolo [2, 3 –d] pyrimidine derivatives as 2cb receptor agonists
EP2970278A4 (en)	2016-12-07	Pyrrolo [2,3] PYRIDINE KINASE INHIBITORS CDK9-
IL290419B (en)	2022-10-01	Imidazo[a-1,5]pyrazine derivatives as inhibitors of pi3k delta
HK1251232A1 (zh)	2019-01-25	吡咯並[2，3-d]嘧啶化合物或其鹽