MX393395B - Derivado de heteroaril[4,3-c]pirimidina-5-amina, método de preparación del mismo y usos médicos del mismo. - Google Patents
Derivado de heteroaril[4,3-c]pirimidina-5-amina, método de preparación del mismo y usos médicos del mismo.Info
- Publication number
- MX393395B MX393395B MX2019010354A MX2019010354A MX393395B MX 393395 B MX393395 B MX 393395B MX 2019010354 A MX2019010354 A MX 2019010354A MX 2019010354 A MX2019010354 A MX 2019010354A MX 393395 B MX393395 B MX 393395B
- Authority
- MX
- Mexico
- Prior art keywords
- preparation
- amine derivative
- sub
- heteroaryl
- medical uses
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title abstract 4
- FVLAYJRLBLHIPV-UHFFFAOYSA-N pyrimidin-5-amine Chemical class NC1=CN=CN=C1 FVLAYJRLBLHIPV-UHFFFAOYSA-N 0.000 title abstract 3
- 239000003814 drug Substances 0.000 abstract 2
- 230000001668 ameliorated effect Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero 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
- A61K31/495—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
- A61P25/00—Drugs for disorders of the nervous system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un derivado de heteroaril[4,3-c]pirimidin-5-amina, un método de preparación del mismo y usos médicos del mismo. Específicamente, un derivado de heteroaril[4,3-c]pirimidin-5-amina representado por una fórmula general (I), un método de preparación del mismo, una composición farmacéutica que contiene el derivado y usos del mismo como agentes terapéuticos, en particular, un uso como un antagonista del receptor A2a y un uso en la preparación de un medicamento para el tratamiento de afecciones o síntomas que se mejoran al inhibir el receptor A2a ; varios grupos sustituyentes en la fórmula general (I) tienen los significados idénticos a los de la especificación. (ver fórmula)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710156742 | 2017-03-16 | ||
| CN201710982734 | 2017-10-20 | ||
| PCT/CN2018/079086 WO2018166493A1 (zh) | 2017-03-16 | 2018-03-15 | 杂芳基并[4,3-c]嘧啶-5-胺类衍生物、其制备方法及其在医药上的应用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2019010354A MX2019010354A (es) | 2019-10-22 |
| MX393395B true MX393395B (es) | 2025-03-24 |
Family
ID=63523780
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2019010354A MX393395B (es) | 2017-03-16 | 2018-03-15 | Derivado de heteroaril[4,3-c]pirimidina-5-amina, método de preparación del mismo y usos médicos del mismo. |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US11312705B2 (es) |
| EP (1) | EP3575301A4 (es) |
| JP (1) | JP7111733B2 (es) |
| KR (1) | KR20190129851A (es) |
| CN (1) | CN109963854B (es) |
| AU (1) | AU2018233367B2 (es) |
| BR (1) | BR112019017108A2 (es) |
| CA (1) | CA3054976A1 (es) |
| MX (1) | MX393395B (es) |
| RU (1) | RU2764655C2 (es) |
| TW (1) | TWI772386B (es) |
| UA (1) | UA125592C2 (es) |
| WO (1) | WO2018166493A1 (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SMT201900680T1 (it) | 2014-02-13 | 2020-01-14 | Incyte Corp | Ciclopropilammine come inibitori di lsd1 |
| KR102352408B1 (ko) | 2014-02-13 | 2022-01-18 | 인사이트 코포레이션 | Lsd1 저해제로서 사이클로프로필아민 |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| US9695168B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| MX373154B (es) | 2015-04-03 | 2020-04-22 | Incyte Holdings Corp | Compuestos heterocíclicos como inhibidores de demetilasa 1 específica de lisina (lsd1). |
| ES3011209T3 (en) | 2015-08-12 | 2025-04-07 | Incyte Holdings Corp | Salts of an lsd1 inhibitor |
| CN109535161B (zh) * | 2017-09-22 | 2021-09-03 | 江苏恒瑞医药股份有限公司 | 三唑并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| AU2019227607C1 (en) * | 2018-02-27 | 2023-07-20 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors |
| EP3810610A1 (en) | 2018-05-18 | 2021-04-28 | Incyte Corporation | Fused pyrimidine derivatives as a2a / a2b inhibitors |
| JP7490631B2 (ja) | 2018-07-05 | 2024-05-27 | インサイト・コーポレイション | A2a/a2b阻害剤としての縮合ピラジン誘導体 |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| TWI820209B (zh) | 2018-09-12 | 2023-11-01 | 大陸商迪哲(江蘇)醫藥股份有限公司 | 三唑并-嘧啶化合物及其用途 |
| WO2020052648A1 (zh) * | 2018-09-14 | 2020-03-19 | 江苏恒瑞医药股份有限公司 | 一种杂芳基并[4,3-c]嘧啶-5-胺类衍生物的晶型及制备方法 |
| CN110903291B (zh) * | 2018-09-14 | 2021-09-03 | 江苏恒瑞医药股份有限公司 | 一种杂芳基并[4,3-c]嘧啶-5-胺类衍生物的盐、盐的晶型及制备方法 |
| KR102653800B1 (ko) | 2018-11-30 | 2024-04-01 | 머크 샤프 앤드 돔 엘엘씨 | 아데노신 수용체 길항제로서의 9-치환된 아미노 트리아졸로 퀴나졸린 유도체, 제약 조성물 및 그의 용도 |
| WO2020132197A1 (en) | 2018-12-20 | 2020-06-25 | Incyte Corporation | Imidazopyridazine and imidazopyridine compounds as inhibitors of activin receptor-like kinase-2 |
| WO2020128036A1 (en) * | 2018-12-21 | 2020-06-25 | Ryvu Therapeutics S.A. | Modulators of the adenosine a2a receptor |
| JP7625524B2 (ja) | 2019-01-11 | 2025-02-03 | オメロス コーポレーション | がんを処置するための方法および組成物 |
| TWI829857B (zh) * | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| CN111848625B (zh) * | 2019-04-24 | 2022-07-26 | 江苏恒瑞医药股份有限公司 | 一种杂芳基并[4,3-c]嘧啶-5-胺类化合物的制备方法及中间体 |
| WO2021156439A1 (en) | 2020-02-06 | 2021-08-12 | Astrazeneca Ab | Triazole compounds as adenosine receptor antagonists |
| EP4126873A1 (en) * | 2020-03-26 | 2023-02-08 | Heptares Therapeutics Limited | 5-amino-8-(4-pyridyl)-[1,2,4]triazolo[4,3-c]pyrimidin-3-one compounds for use against cancer |
| EP4126871B1 (en) * | 2020-03-26 | 2024-05-08 | Heptares Therapeutics Limited | Triazolone compounds |
| CN115867282B (zh) * | 2020-03-26 | 2025-05-27 | 奈克斯拉制药英国有限公司 | 用于抗癌的5-氨基-8-(4-吡啶基)-[1,2,4]三唑并[4,3-c]嘧啶-3-酮化合物 |
| WO2021191376A1 (en) * | 2020-03-26 | 2021-09-30 | Astrazeneca Ab | Triazolone compounds |
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| DE69820866T2 (de) * | 1997-03-24 | 2004-12-30 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]TRIAZOLO[1,5-c]PYRIMIDIN-DERIVATE |
| US6545000B1 (en) | 1998-09-22 | 2003-04-08 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]triazolo[1,5-c]pyrimidine derivatives |
| US6355653B1 (en) * | 1999-09-06 | 2002-03-12 | Hoffmann-La Roche Inc. | Amino-triazolopyridine derivatives |
| JP2002037787A (ja) * | 2000-05-16 | 2002-02-06 | Kyowa Hakko Kogyo Co Ltd | [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体の製造法 |
| WO2003068776A1 (en) * | 2002-02-15 | 2003-08-21 | Kyowa Hakko Kogyo Co., Ltd. | [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES |
| PT1863818E (pt) * | 2005-03-23 | 2010-04-09 | Hoffmann La Roche | Derivados de acetilenil-pirazolo-pirimidina como antagonistas de mglur2 |
| US7452892B2 (en) * | 2005-06-17 | 2008-11-18 | Bristol-Myers Squibb Company | Triazolopyrimidine cannabinoid receptor 1 antagonists |
| DE102006008880A1 (de) | 2006-02-27 | 2007-09-06 | Merck Patent Gmbh | Aminopyrimidinderivate |
| WO2007116106A1 (es) | 2006-04-12 | 2007-10-18 | Palobiofarma, S.L. | Nuevos compuestos como antagonistas de los receptores a1 de adenosina |
| DE102007061763A1 (de) | 2007-12-20 | 2009-06-25 | Bayer Healthcare Ag | Substituierte azabicyclische Verbindungen und ihre Verwendung |
| AU2009222047A1 (en) * | 2008-03-04 | 2009-09-11 | Schering Corporation | 1,2,4-triazolo[4,3-c]pyrimidin-3-one and pyrazolo [4,3-e] -1,2,4-triazolo [4,3-c] pyrimidin-3-one compounds for use as adenosine A2a receptor antagonists |
| US8796297B2 (en) | 2009-06-30 | 2014-08-05 | Abbvie Inc. | 4-substituted-2-amino-pyrimidine derivatives |
| JO3090B1 (ar) | 2009-12-11 | 2017-03-15 | Janssen Sciences Ireland Uc | 5- امينو-4- هيدروكسي-بنتويل اميدات |
| ES2579949T3 (es) | 2010-02-05 | 2016-08-17 | Heptares Therapeutics Limited | Derivados de 1,2,4-triazin-4-amina |
| RU2012153675A (ru) | 2010-05-12 | 2014-06-20 | Вертекс Фармасьютикалз Инкорпорейтед | Соединения, пригодные в качестве ингибиторов atr киназы |
| UY33452A (es) * | 2010-06-16 | 2012-01-31 | Bayer Schering Pharma Ag | Triazolopiridinas sustituidas |
| WO2011159302A1 (en) | 2010-06-17 | 2011-12-22 | Janssen Pharmaceutica Nv | Arylindenopyrimidines for treating neurodegenerative and movement disorders while minimizing cardiac toxicity |
| GB2483736B (en) | 2010-09-16 | 2012-08-29 | Aragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
| MX2013004733A (es) | 2010-10-29 | 2013-07-02 | Pfizer | Inhibidores de n1/n2-lactama acetil-coa carboxilasa. |
| EA023766B1 (ru) * | 2011-04-21 | 2016-07-29 | Байер Интеллектчуал Проперти Гмбх | Триазолопиридины |
| TW201326170A (zh) * | 2011-12-12 | 2013-07-01 | 拜耳製藥公司 | 經取代之三唑并吡啶 |
| WO2014101120A1 (en) | 2012-12-28 | 2014-07-03 | Merck Sharp & Dohme Corp. | Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties |
| TWI628176B (zh) | 2013-04-04 | 2018-07-01 | 奧利安公司 | 蛋白質激酶抑制劑 |
| WO2015027431A1 (en) | 2013-08-29 | 2015-03-05 | Merck Sharp & Dohme Corp. | 2,2-difluorodioxolo a2a receptor antagonists |
| PE20170303A1 (es) | 2014-06-17 | 2017-04-19 | Chiesi Farm Spa | Derivados de la indolizina como inhibidores de las fosfoinositido-3 quinasas |
| TN2017000204A1 (en) * | 2014-12-23 | 2018-10-19 | Novartis Ag | Triazolopyrimidine compounds and uses thereof |
| CN109535161B (zh) * | 2017-09-22 | 2021-09-03 | 江苏恒瑞医药股份有限公司 | 三唑并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| AU2019227607C1 (en) * | 2018-02-27 | 2023-07-20 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors |
-
2018
- 2018-03-15 EP EP18766881.9A patent/EP3575301A4/en not_active Withdrawn
- 2018-03-15 AU AU2018233367A patent/AU2018233367B2/en not_active Ceased
- 2018-03-15 KR KR1020197025674A patent/KR20190129851A/ko not_active Withdrawn
- 2018-03-15 JP JP2019548401A patent/JP7111733B2/ja active Active
- 2018-03-15 RU RU2019131111A patent/RU2764655C2/ru active
- 2018-03-15 US US16/492,273 patent/US11312705B2/en active Active
- 2018-03-15 CN CN201880004302.2A patent/CN109963854B/zh active Active
- 2018-03-15 UA UAA201910243A patent/UA125592C2/uk unknown
- 2018-03-15 BR BR112019017108A patent/BR112019017108A2/pt not_active Application Discontinuation
- 2018-03-15 MX MX2019010354A patent/MX393395B/es unknown
- 2018-03-15 WO PCT/CN2018/079086 patent/WO2018166493A1/zh not_active Ceased
- 2018-03-15 CA CA3054976A patent/CA3054976A1/en active Pending
- 2018-03-16 TW TW107109077A patent/TWI772386B/zh not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| CN109963854B (zh) | 2022-04-12 |
| RU2019131111A (ru) | 2021-04-16 |
| AU2018233367A1 (en) | 2019-08-29 |
| RU2019131111A3 (es) | 2021-04-16 |
| TW201835083A (zh) | 2018-10-01 |
| RU2764655C2 (ru) | 2022-01-19 |
| UA125592C2 (uk) | 2022-04-27 |
| MX2019010354A (es) | 2019-10-22 |
| JP7111733B2 (ja) | 2022-08-02 |
| EP3575301A4 (en) | 2020-08-05 |
| CA3054976A1 (en) | 2018-09-20 |
| KR20190129851A (ko) | 2019-11-20 |
| JP2020510012A (ja) | 2020-04-02 |
| AU2018233367B2 (en) | 2021-08-12 |
| US20210032224A1 (en) | 2021-02-04 |
| CN109963854A (zh) | 2019-07-02 |
| TWI772386B (zh) | 2022-08-01 |
| WO2018166493A1 (zh) | 2018-09-20 |
| US11312705B2 (en) | 2022-04-26 |
| EP3575301A1 (en) | 2019-12-04 |
| BR112019017108A2 (pt) | 2020-04-07 |
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