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/CLK1Info
- 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
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- dyrk1
- clk1
- pyrimidine derivatives
- dual inhibitors
- new pyrrolo
- Prior art date
Links
- 102100040862 Dual specificity protein kinase CLK1 Human genes 0.000 title 1
- 102100028554 Dual specificity tyrosine-phosphorylation-regulated kinase 1A Human genes 0.000 title 1
- 101000749294 Homo sapiens Dual specificity protein kinase CLK1 Proteins 0.000 title 1
- 101000838016 Homo sapiens Dual specificity tyrosine-phosphorylation-regulated kinase 1A Proteins 0.000 title 1
- 230000009977 dual effect Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000004943 pyrrolo[2,3-d]pyrimidines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
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)
- 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)
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) |
Families Citing this family (17)
| 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 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
-
2015
- 2015-09-30 FR FR1559259A patent/FR3041640B1/fr not_active Expired - Fee Related
-
2016
- 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 EA EA201890820A patent/EA201890820A1/ru unknown
- 2016-09-30 AU AU2016333508A patent/AU2016333508A1/en not_active Abandoned
- 2016-09-30 CR CR20180176A patent/CR20180176A/es unknown
- 2016-09-30 WO PCT/EP2016/073403 patent/WO2017055533A1/en not_active Ceased
- 2016-09-30 JP JP2018516488A patent/JP2018533552A/ja active Pending
- 2016-09-30 CA CA2999937A patent/CA2999937A1/en not_active Abandoned
- 2016-09-30 CU CUP2018000027A patent/CU20180027A7/xx unknown
- 2016-09-30 MA MA043021A patent/MA43021A/fr unknown
- 2016-09-30 PE PE2018000410A patent/PE20190337A1/es unknown
- 2016-09-30 EP EP16774684.1A patent/EP3356364A1/en not_active Withdrawn
- 2016-09-30 KR KR1020187012166A patent/KR20180054856A/ko not_active Withdrawn
- 2016-09-30 MX MX2018003861A patent/MX2018003861A/es unknown
- 2016-09-30 HK HK18114640.5A patent/HK1255467A1/zh unknown
- 2016-09-30 TN TNP/2018/000087A patent/TN2018000087A1/en unknown
- 2016-09-30 CN CN201680058179.3A patent/CN108137582A/zh not_active Withdrawn
-
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 EC ECIEPI201823286A patent/ECSP18023286A/es unknown
- 2018-03-26 CL CL2018000786A patent/CL2018000786A1/es unknown
- 2018-03-26 DO DO2018000082A patent/DOP2018000082A/es unknown
- 2018-03-28 CO CONC2018/0003466A patent/CO2018003466A2/es unknown
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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