RU2703273C2 - Тиазолопиримидиноны в качестве модуляторов активности рецепторов nmda - Google Patents
Тиазолопиримидиноны в качестве модуляторов активности рецепторов nmda Download PDFInfo
- Publication number
- RU2703273C2 RU2703273C2 RU2016115487A RU2016115487A RU2703273C2 RU 2703273 C2 RU2703273 C2 RU 2703273C2 RU 2016115487 A RU2016115487 A RU 2016115487A RU 2016115487 A RU2016115487 A RU 2016115487A RU 2703273 C2 RU2703273 C2 RU 2703273C2
- Authority
- RU
- Russia
- Prior art keywords
- methyl
- thiazolo
- pyrimidin
- trifluoromethyl
- oxo
- Prior art date
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Classifications
-
- 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
- C07D513/12—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 three hetero rings
- C07D513/14—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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring 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
- A61K31/495—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
-
- 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
- C07D513/10—Spiro-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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Psychology (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Rheumatology (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013085031 | 2013-10-11 | ||
| CNPCT/CN2013/085031 | 2013-10-11 | ||
| CNPCT/CN2014/085959 | 2014-09-05 | ||
| CN2014085959 | 2014-09-05 | ||
| PCT/EP2014/071522 WO2015052226A1 (en) | 2013-10-11 | 2014-10-08 | Thiazolopyrimidinones as modulators of nmda receptor activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2016115487A RU2016115487A (ru) | 2017-11-16 |
| RU2016115487A3 RU2016115487A3 (enExample) | 2018-06-21 |
| RU2703273C2 true RU2703273C2 (ru) | 2019-10-16 |
Family
ID=51688060
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016115487A RU2703273C2 (ru) | 2013-10-11 | 2014-10-08 | Тиазолопиримидиноны в качестве модуляторов активности рецепторов nmda |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US9988400B2 (enExample) |
| EP (2) | EP3055315B1 (enExample) |
| JP (2) | JP6419800B2 (enExample) |
| KR (1) | KR102361108B1 (enExample) |
| CN (2) | CN105612162B (enExample) |
| BR (1) | BR112016007563B1 (enExample) |
| CA (1) | CA2926830C (enExample) |
| DK (1) | DK3055315T3 (enExample) |
| ES (1) | ES2690355T3 (enExample) |
| HR (1) | HRP20181596T1 (enExample) |
| HU (1) | HUE040651T2 (enExample) |
| LT (1) | LT3055315T (enExample) |
| MX (1) | MX2016004540A (enExample) |
| PL (1) | PL3055315T3 (enExample) |
| PT (1) | PT3055315T (enExample) |
| RS (1) | RS58047B1 (enExample) |
| RU (1) | RU2703273C2 (enExample) |
| SI (1) | SI3055315T1 (enExample) |
| WO (1) | WO2015052226A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2866010C1 (ru) * | 2025-12-23 | 2026-07-13 | Федеральное государственное бюджетное учреждение "Российский научный центр радиологии и хирургических технологий имени академика А.М. Гранова" Министерства здравоохранения Российской Федерации | 3-(Азидометил)-7-метил-5H-тиазоло[3,2-a]пиримидин-5-он, обладающий цитотоксическим действием |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20180316A1 (es) | 2015-04-15 | 2018-02-09 | Hoffmann La Roche | Compuestos piridopirimidinona y su uso como moduladores del receptor de nmda |
| WO2017100599A1 (en) | 2015-12-09 | 2017-06-15 | Luc Therapeutics | Thienopyrimidinone nmda receptor modulators and uses thereof |
| ES2821010T3 (es) | 2015-12-09 | 2021-04-23 | Cadent Therapeutics Inc | Moduladores heteroaromáticos del receptor NMDA y usos de los mismos |
| WO2017109709A2 (en) | 2015-12-22 | 2017-06-29 | Novartis Ag | A high-throughput assay method for identifying allosteric nmda receptor modulators |
| AU2017382339B2 (en) * | 2016-12-22 | 2024-02-15 | Novartis Ag | NMDA receptor modulators and uses thereof |
| PT3830092T (pt) | 2018-08-03 | 2023-07-25 | Novartis Ag | Moduladores do recetor nmda heteroaromáticos e suas utilizações |
| CN111840296B (zh) * | 2020-07-22 | 2021-05-04 | 华中农业大学 | 一种5H-噻唑并[3,2-a]嘧啶-5-酮类化合物在制备单胺氧化酶抑制剂中的用途 |
| CN112094267B (zh) * | 2020-08-14 | 2025-06-06 | 贵州省中国科学院天然产物化学重点实验室(贵州医科大学天然产物化学重点实验室) | 1-苯基-吡咯并异喹啉-3-酮类化合物及其制备方法和应用 |
| EP4032896A1 (en) * | 2021-01-20 | 2022-07-27 | Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) | Thiazolopyrimidones as inhibitors of ddr1/2 and therapeutic uses thereof |
| CN112724157B (zh) * | 2021-01-23 | 2022-04-19 | 中国科学院新疆理化技术研究所 | 二氢噁唑并[5,4-d]吡咯并[1,2-a]嘧啶-9(5H)-酮类衍生物及用途 |
| US20250073242A1 (en) * | 2021-07-30 | 2025-03-06 | The Regents Of The University Of California | Slc26a3 inhibitors and use thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2197493C2 (ru) * | 1997-07-18 | 2003-01-27 | Ф.Хоффманн-Ля Рош Аг | Производные 5h-тиазол[3,2-а]пиримидина, промежуточные продукты и лекарственное средство |
| WO2004074270A2 (en) * | 2003-02-21 | 2004-09-02 | Pfizer Inc. | Inhibitors of hepatitis c virus rna-dependent rna polymerase, and compositions and treatments using the same |
| US20070155779A1 (en) * | 2006-01-05 | 2007-07-05 | Pfizer Inc | Bicyclic heteroaryl compounds as pde10 inhibitors |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3888983A (en) * | 1970-08-14 | 1975-06-10 | Seperic | Derivatives of thiazolino-pyrimidin-6-ones, in inducing analgesia |
| US5902815A (en) * | 1996-09-03 | 1999-05-11 | Washington University | Use of 5HT-2A serotonin agonists to prevent adverse effects of NMDA receptor hypofunction |
| WO2007006175A1 (en) | 2005-07-11 | 2007-01-18 | Zte Corporation | Method for implementing channel shared ring protection supported easy failure prevention |
| KR101811549B1 (ko) | 2013-06-19 | 2017-12-26 | 에프. 호프만-라 로슈 아게 | 인돌린-2-온 또는 피롤로-피리딘/피리미딘-2-온 유도체 |
| PE20180316A1 (es) | 2015-04-15 | 2018-02-09 | Hoffmann La Roche | Compuestos piridopirimidinona y su uso como moduladores del receptor de nmda |
-
2014
- 2014-10-08 PT PT14781878T patent/PT3055315T/pt unknown
- 2014-10-08 RS RS20181185A patent/RS58047B1/sr unknown
- 2014-10-08 ES ES14781878T patent/ES2690355T3/es active Active
- 2014-10-08 DK DK14781878.5T patent/DK3055315T3/en active
- 2014-10-08 BR BR112016007563-3A patent/BR112016007563B1/pt active IP Right Grant
- 2014-10-08 RU RU2016115487A patent/RU2703273C2/ru active
- 2014-10-08 KR KR1020167012236A patent/KR102361108B1/ko active Active
- 2014-10-08 CA CA2926830A patent/CA2926830C/en active Active
- 2014-10-08 SI SI201430905T patent/SI3055315T1/sl unknown
- 2014-10-08 HU HUE14781878A patent/HUE040651T2/hu unknown
- 2014-10-08 MX MX2016004540A patent/MX2016004540A/es active IP Right Grant
- 2014-10-08 WO PCT/EP2014/071522 patent/WO2015052226A1/en not_active Ceased
- 2014-10-08 HR HRP20181596TT patent/HRP20181596T1/hr unknown
- 2014-10-08 PL PL14781878T patent/PL3055315T3/pl unknown
- 2014-10-08 EP EP14781878.5A patent/EP3055315B1/en active Active
- 2014-10-08 CN CN201480055668.4A patent/CN105612162B/zh active Active
- 2014-10-08 JP JP2016521943A patent/JP6419800B2/ja active Active
- 2014-10-08 LT LTEP14781878.5T patent/LT3055315T/lt unknown
- 2014-10-08 CN CN201810852075.0A patent/CN108929336A/zh active Pending
- 2014-10-08 EP EP18177888.7A patent/EP3415519A1/en not_active Withdrawn
-
2016
- 2016-04-08 US US15/094,687 patent/US9988400B2/en active Active
-
2018
- 2018-04-25 US US15/962,333 patent/US10647731B2/en active Active
- 2018-10-10 JP JP2018191536A patent/JP2019023217A/ja active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2197493C2 (ru) * | 1997-07-18 | 2003-01-27 | Ф.Хоффманн-Ля Рош Аг | Производные 5h-тиазол[3,2-а]пиримидина, промежуточные продукты и лекарственное средство |
| WO2004074270A2 (en) * | 2003-02-21 | 2004-09-02 | Pfizer Inc. | Inhibitors of hepatitis c virus rna-dependent rna polymerase, and compositions and treatments using the same |
| US20070155779A1 (en) * | 2006-01-05 | 2007-07-05 | Pfizer Inc | Bicyclic heteroaryl compounds as pde10 inhibitors |
Non-Patent Citations (1)
| Title |
|---|
| Guo Chuangxing et al, Discovery of 2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as novel PKM2 activators, Bioorganic & Medicinal Chemistry Letters, 23, 11, стр.: 3358 - 3363, 2013. * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2866010C1 (ru) * | 2025-12-23 | 2026-07-13 | Федеральное государственное бюджетное учреждение "Российский научный центр радиологии и хирургических технологий имени академика А.М. Гранова" Министерства здравоохранения Российской Федерации | 3-(Азидометил)-7-метил-5H-тиазоло[3,2-a]пиримидин-5-он, обладающий цитотоксическим действием |
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