EA201400245A1 - Ингибиторы dyrk1 и их применение - Google Patents
Ингибиторы dyrk1 и их применениеInfo
- Publication number
- EA201400245A1 EA201400245A1 EA201400245A EA201400245A EA201400245A1 EA 201400245 A1 EA201400245 A1 EA 201400245A1 EA 201400245 A EA201400245 A EA 201400245A EA 201400245 A EA201400245 A EA 201400245A EA 201400245 A1 EA201400245 A1 EA 201400245A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- inhibitors
- dyrk1
- application
- alleviating
- treating
- Prior art date
Links
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—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
- A61K31/535—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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C219/02—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
- C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Изобретение касается новых соединений тиазоло[5,4-f]хиназолинов и способов, применимых для облегчения, лечения или контролирования синдрома Дауна или ранней стадии болезни Альцгеймера либо для облегчения, лечения или контролирования раковых заболеваний, в особенности солидных опухолей. Более конкретно, изобретение касается ингибиторов DYRK1A и/или DYRK1B и способов получения таких соединений.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11178190 | 2011-08-19 | ||
PCT/EP2012/066151 WO2013026806A1 (en) | 2011-08-19 | 2012-08-17 | Dyrk1 inhibitors and uses thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201400245A1 true EA201400245A1 (ru) | 2014-07-30 |
EA026377B1 EA026377B1 (ru) | 2017-04-28 |
Family
ID=46704656
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201400245A EA026377B1 (ru) | 2011-08-19 | 2012-08-17 | Ингибиторы dyrk1 и их применение |
Country Status (16)
Country | Link |
---|---|
US (1) | US9446044B2 (ru) |
EP (1) | EP2744797B1 (ru) |
JP (1) | JP6017559B2 (ru) |
KR (1) | KR102006749B1 (ru) |
CN (1) | CN103797002B (ru) |
AU (1) | AU2012298510B2 (ru) |
BR (1) | BR112014003774B1 (ru) |
CA (1) | CA2848896C (ru) |
DK (1) | DK2744797T3 (ru) |
EA (1) | EA026377B1 (ru) |
ES (1) | ES2551268T3 (ru) |
HK (1) | HK1198827A1 (ru) |
IL (1) | IL230917A (ru) |
PL (1) | PL2744797T3 (ru) |
PT (1) | PT2744797E (ru) |
WO (1) | WO2013026806A1 (ru) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20150292032A1 (en) * | 2012-10-10 | 2015-10-15 | Felicitex Therapeutics, Inc. | Treatment of cancer by targeting quiescent cancer cells |
FR3002044A1 (fr) * | 2013-02-08 | 2014-08-15 | Centre Nat Rech Scient | Marqueur dyrk1a pour la maladie d'alzheimer |
CA2854542A1 (en) | 2013-06-18 | 2014-12-18 | 4Sc Discovery Gmbh | Method of inhibiting dyrk1b |
JP2015107945A (ja) * | 2013-12-05 | 2015-06-11 | 国立大学法人京都大学 | 神経新生に関する化合物及び医薬組成物 |
WO2017040993A1 (en) * | 2015-09-03 | 2017-03-09 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of dyrk1a and uses thereof |
CN109313197A (zh) * | 2016-04-15 | 2019-02-05 | 费利克斯疗法公司 | 使用静止细胞靶向和有丝分裂抑制剂的用于治疗肿瘤的组合 |
KR20230020565A (ko) | 2016-04-15 | 2023-02-10 | 펠리시텍스 쎄라퓨틱스, 인코포레이티드 | 정지 세포 표적화 및 egfr 억제제를 이용하는 신생물 치료를 위한 조합 |
JP7134973B2 (ja) * | 2016-12-23 | 2022-09-12 | フェリシテックス・セラピューティクス,インコーポレイテッド | Dyrk1aおよび/またはdyrk1bキナーゼの阻害剤としてのキノリンの誘導体 |
US11547712B2 (en) | 2017-11-20 | 2023-01-10 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
US11788064B2 (en) | 2018-01-05 | 2023-10-17 | Icahn School Of Medicine At Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
CA3093340A1 (en) | 2018-03-20 | 2019-09-26 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
US20220041590A1 (en) * | 2018-09-28 | 2022-02-10 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of dyrk/clk and uses thereof |
WO2020142486A1 (en) * | 2018-12-31 | 2020-07-09 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
WO2021153665A1 (ja) * | 2020-01-30 | 2021-08-05 | カルナバイオサイエンス株式会社 | 新規アルキン誘導体 |
AU2021343770A1 (en) | 2020-09-18 | 2023-05-18 | Carna Biosciences, Inc. | Amine derivative |
WO2022059778A1 (ja) * | 2020-09-18 | 2022-03-24 | カルナバイオサイエンス株式会社 | 環状ウレア誘導体 |
WO2023008472A1 (ja) * | 2021-07-28 | 2023-02-02 | カルナバイオサイエンス株式会社 | 新規ベンゾチアゾール誘導体 |
WO2023008470A1 (ja) * | 2021-07-28 | 2023-02-02 | 住友ファーマ株式会社 | 縮環アミン誘導体 |
WO2023140846A1 (en) * | 2022-01-20 | 2023-07-27 | Felicitex Therapeutics, Inc. | Combination cancer therapy with dyrk1 inhibitors and inhibitors of the ras-raf-mek-erk (mapk) pathway |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL112249A (en) * | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
IL112248A0 (en) * | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
GB0705566D0 (en) | 2007-03-23 | 2007-05-02 | Univ Dundee | Method of treating learning impairment in down's syndrome subjects |
FR2943057B1 (fr) * | 2009-03-12 | 2011-06-03 | Centre Nat Rech Scient | DERIVES DE 10-AMINO-1,2,3,4-TETRAHYDROPYRIDO°2,1-a!ISOINDOL-6(10bH)- ONES, LEUR PROCEDE DE PREPARATION ET LEURS UTILISATIONS THERAPEUTIQUES |
WO2011041655A1 (en) * | 2009-10-01 | 2011-04-07 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Quinazolin-4-amine derivatives; and methods of use |
-
2012
- 2012-08-17 WO PCT/EP2012/066151 patent/WO2013026806A1/en active Application Filing
- 2012-08-17 PT PT127484707T patent/PT2744797E/pt unknown
- 2012-08-17 PL PL12748470T patent/PL2744797T3/pl unknown
- 2012-08-17 BR BR112014003774-4A patent/BR112014003774B1/pt active IP Right Grant
- 2012-08-17 ES ES12748470.7T patent/ES2551268T3/es active Active
- 2012-08-17 JP JP2014525468A patent/JP6017559B2/ja active Active
- 2012-08-17 KR KR1020147007325A patent/KR102006749B1/ko active IP Right Grant
- 2012-08-17 EA EA201400245A patent/EA026377B1/ru not_active IP Right Cessation
- 2012-08-17 AU AU2012298510A patent/AU2012298510B2/en active Active
- 2012-08-17 CN CN201280040405.7A patent/CN103797002B/zh active Active
- 2012-08-17 EP EP12748470.7A patent/EP2744797B1/en active Active
- 2012-08-17 DK DK12748470.7T patent/DK2744797T3/en active
- 2012-08-17 CA CA2848896A patent/CA2848896C/en active Active
- 2012-08-17 US US14/238,925 patent/US9446044B2/en active Active
-
2014
- 2014-02-11 IL IL230917A patent/IL230917A/en active IP Right Grant
- 2014-12-05 HK HK14112274.6A patent/HK1198827A1/xx unknown
Also Published As
Publication number | Publication date |
---|---|
BR112014003774B1 (pt) | 2021-12-14 |
AU2012298510A1 (en) | 2014-04-10 |
EA026377B1 (ru) | 2017-04-28 |
HK1198827A1 (en) | 2015-06-12 |
CA2848896A1 (en) | 2013-02-28 |
WO2013026806A1 (en) | 2013-02-28 |
DK2744797T3 (en) | 2015-10-19 |
BR112014003774A2 (pt) | 2017-03-07 |
IL230917A0 (en) | 2014-03-31 |
PT2744797E (pt) | 2015-11-16 |
US20140275064A1 (en) | 2014-09-18 |
EP2744797B1 (en) | 2015-09-09 |
CA2848896C (en) | 2019-10-29 |
AU2012298510B2 (en) | 2016-10-27 |
IL230917A (en) | 2017-02-28 |
EP2744797A1 (en) | 2014-06-25 |
KR102006749B1 (ko) | 2019-08-02 |
KR20140057614A (ko) | 2014-05-13 |
JP2014525928A (ja) | 2014-10-02 |
PL2744797T3 (pl) | 2016-01-29 |
ES2551268T3 (es) | 2015-11-17 |
CN103797002B (zh) | 2017-02-22 |
US9446044B2 (en) | 2016-09-20 |
JP6017559B2 (ja) | 2016-11-02 |
CN103797002A (zh) | 2014-05-14 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
EA201400245A1 (ru) | Ингибиторы dyrk1 и их применение | |
AU2018236800B2 (en) | DNA-PK inhibitors | |
EP4257591A3 (en) | Inhibitors of lysine specific demethylase-1 | |
EA201200473A1 (ru) | Замещенные (гетероарилметил)тиогидантоины | |
EA201692166A1 (ru) | Гетероциклические ингибиторы глютаминазы | |
EA201291143A1 (ru) | Пиразолилхиназолиновые ингибиторы киназы | |
EA201101650A1 (ru) | Новые производные пиримидина и их применение в лечении злокачественных новообразований и последующих заболеваний | |
PH12016500722A1 (en) | Bromodomain inhibitors | |
EA201500362A1 (ru) | Ингибиторы rho-киназы | |
EA201490891A1 (ru) | Пиридопиразины, обладающие противораковой активностью через ингибирование fgfr киназ | |
NZ700928A (en) | Dna-pk inhibitors | |
SA515360657B1 (ar) | مثبطات ديميثيلاز هيستون | |
EA201390711A1 (ru) | Гидроксиамидные соединения пиримидина в качестве ингибиторов деацетилаз белков и способы их применения | |
EA201892339A3 (ru) | Несиалированный выделенный полипептид, способ получения указанного полипептида и фармацевтическая композиция для лечения воспалительного заболевания | |
EA201591753A1 (ru) | 3-пиримидин-4-илоксазолидин-2-оны в качестве ингибиторов мутантного idh | |
EA201491391A1 (ru) | Терапевтически активные соединения и способы их применения | |
TN2014000128A1 (en) | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh | |
WO2012118812A3 (en) | Substituted 6,5-fused bicyclic heteroaryl compounds | |
AU2016219704A1 (en) | Anti-Notch1 antibodies | |
EA201500298A1 (ru) | Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы | |
EA201490423A1 (ru) | СПОСОБЫ И КОМПОЗИЦИИ, ОТНОСЯЩИЕСЯ К p62, ДЛЯ ЛЕЧЕНИЯ И ПРОФИЛАКТИКИ РАКА | |
UA112795C2 (uk) | Біциклічні піразинонові похідні | |
EA201590183A1 (ru) | Производные азаиндола, выступающие в качестве ингибиторов pi3k | |
WO2013040227A3 (en) | Therapeutic compounds | |
EA202091923A1 (ru) | Замещенные трициклические соединения как ингибиторы fgfr |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KG TJ TM |