BR112018005851A2 - derivados de pirrolo[2,3-d]pirimidina como inibidores de dyrk1 / clk1 duais - Google Patents
derivados de pirrolo[2,3-d]pirimidina como inibidores de dyrk1 / clk1 duaisInfo
- Publication number
- BR112018005851A2 BR112018005851A2 BR112018005851A BR112018005851A BR112018005851A2 BR 112018005851 A2 BR112018005851 A2 BR 112018005851A2 BR 112018005851 A BR112018005851 A BR 112018005851A BR 112018005851 A BR112018005851 A BR 112018005851A BR 112018005851 A2 BR112018005851 A2 BR 112018005851A2
- Authority
- BR
- Brazil
- Prior art keywords
- pyrrolo
- pyrimidine derivatives
- dyrk1
- dual
- clk1
- Prior art date
Links
- 101100003180 Colletotrichum lindemuthianum ATG1 gene Proteins 0.000 title 1
- 101100444294 Dictyostelium discoideum dyrk1 gene 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
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 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 |
|---|---|
| BR112018005851A2 true BR112018005851A2 (pt) | 2018-10-09 |
Family
ID=54979756
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112018005851A BR112018005851A2 (pt) | 2015-09-30 | 2016-09-30 | derivados de pirrolo[2,3-d]pirimidina como inibidores de dyrk1 / clk1 duais |
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 (17)
| 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 |
| 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 |
| US11071730B2 (en) | 2018-10-31 | 2021-07-27 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds |
| PL3873903T3 (pl) | 2018-10-31 | 2024-05-20 | Gilead Sciences, Inc. | Podstawione związki 6-azabenzimidazolu jako inhibitory hpk1 |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| EP3972695A1 (en) | 2019-05-23 | 2022-03-30 | 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 |
| WO2022245776A1 (en) * | 2021-05-20 | 2022-11-24 | Saint John's Cancer Institute | Anti-cdk inhibitors for cancer treatment |
| EP4415816A1 (en) | 2021-10-12 | 2024-08-21 | BioSplice Therapeutics, Inc. | Pyrrolo[2,1-f][1,2,4]triazines derivatives as inhibitors of dyrk1a |
| EP4415818A1 (en) * | 2021-10-12 | 2024-08-21 | 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 |
| 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 |
|---|---|---|---|---|
| EP1957498B1 (en) | 2005-05-20 | 2017-02-15 | MethylGene Inc. | Inhibitors of vegf receptor and hgf receptor signaling |
| EA200800664A1 (ru) | 2005-10-13 | 2009-02-27 | Глаксо Груп Лимитед | Производные пирролопиримидина в качестве ингибиторов syk |
| EA200801968A1 (ru) | 2006-03-11 | 2009-02-27 | Вернэлис (Р&Д) Лтд. | Пирролопиримидиновые производные, используемые в качестве ингибиторов hsp90 |
| 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 |
| EP2867236B1 (en) * | 2012-06-29 | 2017-06-14 | Pfizer Inc | Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors |
| 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 |
-
2015
- 2015-09-30 FR FR1559259A patent/FR3041640B1/fr not_active Expired - Fee Related
-
2016
- 2016-09-30 CR CR20180176A patent/CR20180176A/es unknown
- 2016-09-30 CU CUP2018000027A patent/CU20180027A7/xx unknown
- 2016-09-30 MA MA043021A patent/MA43021A/fr unknown
- 2016-09-30 EP EP16774684.1A patent/EP3356364A1/en not_active Withdrawn
- 2016-09-30 AU AU2016333508A patent/AU2016333508A1/en not_active Abandoned
- 2016-09-30 US US15/763,626 patent/US20180273538A1/en not_active Abandoned
- 2016-09-30 CN CN201680058179.3A patent/CN108137582A/zh not_active Withdrawn
- 2016-09-30 TN TNP/2018/000087A patent/TN2018000087A1/en unknown
- 2016-09-30 EA EA201890820A patent/EA201890820A1/ru unknown
- 2016-09-30 CA CA2999937A patent/CA2999937A1/en not_active Abandoned
- 2016-09-30 PE PE2018000410A patent/PE20190337A1/es unknown
- 2016-09-30 KR KR1020187012166A patent/KR20180054856A/ko not_active Withdrawn
- 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 MX MX2018003861A patent/MX2018003861A/es unknown
- 2016-09-30 BR BR112018005851A patent/BR112018005851A2/pt not_active Application Discontinuation
- 2016-09-30 HK HK18114640.5A patent/HK1255467A1/zh unknown
-
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 CL CL2018000786A patent/CL2018000786A1/es unknown
- 2018-03-26 DO DO2018000082A patent/DOP2018000082A/es unknown
- 2018-03-26 EC ECIEPI201823286A patent/ECSP18023286A/es unknown
- 2018-03-28 CO CONC2018/0003466A patent/CO2018003466A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CO2018003466A2 (es) | 2018-07-10 |
| PE20190337A1 (es) | 2019-03-07 |
| CN108137582A (zh) | 2018-06-08 |
| MA43021A (fr) | 2018-08-08 |
| PH12018500605A1 (en) | 2018-09-24 |
| KR20180054856A (ko) | 2018-05-24 |
| CA2999937A1 (en) | 2017-04-06 |
| HK1255467A1 (zh) | 2019-08-16 |
| WO2017055533A1 (en) | 2017-04-06 |
| CU20180027A7 (es) | 2018-07-05 |
| EA201890820A1 (ru) | 2018-10-31 |
| FR3041640B1 (fr) | 2019-05-17 |
| TN2018000087A1 (en) | 2019-07-08 |
| SV2018005656A (es) | 2018-08-10 |
| DOP2018000082A (es) | 2018-10-15 |
| AU2016333508A1 (en) | 2018-04-12 |
| CR20180176A (es) | 2018-05-31 |
| NI201800042A (es) | 2018-06-21 |
| US20180273538A1 (en) | 2018-09-27 |
| IL258231A (en) | 2018-05-31 |
| CL2018000786A1 (es) | 2018-09-28 |
| FR3041640A1 (enExample) | 2017-03-31 |
| EP3356364A1 (en) | 2018-08-08 |
| ECSP18023286A (es) | 2018-04-30 |
| MX2018003861A (es) | 2018-08-16 |
| JP2018533552A (ja) | 2018-11-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
| B11Y | Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette] |