CA3017869C - Pyrazole aminopyrimidine derivatives as lrrk2 modulators - Google Patents
Pyrazole aminopyrimidine derivatives as lrrk2 modulators Download PDFInfo
- Publication number
- CA3017869C CA3017869C CA3017869A CA3017869A CA3017869C CA 3017869 C CA3017869 C CA 3017869C CA 3017869 A CA3017869 A CA 3017869A CA 3017869 A CA3017869 A CA 3017869A CA 3017869 C CA3017869 C CA 3017869C
- Authority
- CA
- Canada
- Prior art keywords
- methyl
- pyrazol
- trifluoromethyl
- diamine
- pyrimidine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- 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
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41227310P | 2010-11-10 | 2010-11-10 | |
| US61/412,273 | 2010-11-10 | ||
| US201161546613P | 2011-10-13 | 2011-10-13 | |
| US61/546,613 | 2011-10-13 | ||
| CA2812669A CA2812669C (en) | 2010-11-10 | 2011-11-09 | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2812669A Division CA2812669C (en) | 2010-11-10 | 2011-11-09 | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA3017869A1 CA3017869A1 (en) | 2012-05-18 |
| CA3017869C true CA3017869C (en) | 2021-07-27 |
Family
ID=44983512
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2812669A Active CA2812669C (en) | 2010-11-10 | 2011-11-09 | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
| CA3017869A Active CA3017869C (en) | 2010-11-10 | 2011-11-09 | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2812669A Active CA2812669C (en) | 2010-11-10 | 2011-11-09 | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US8815882B2 (enExample) |
| EP (3) | EP3124483B1 (enExample) |
| JP (3) | JP5986094B2 (enExample) |
| KR (1) | KR101566091B1 (enExample) |
| CN (1) | CN103313978B (enExample) |
| AR (1) | AR083813A1 (enExample) |
| AU (1) | AU2011328139A1 (enExample) |
| BR (1) | BR112013011600B1 (enExample) |
| CA (2) | CA2812669C (enExample) |
| CY (1) | CY1120073T1 (enExample) |
| DK (2) | DK3124483T3 (enExample) |
| EC (1) | ECSP13012611A (enExample) |
| ES (2) | ES2653967T3 (enExample) |
| HR (2) | HRP20172006T1 (enExample) |
| HU (2) | HUE046617T2 (enExample) |
| IL (1) | IL225234A0 (enExample) |
| LT (2) | LT2638031T (enExample) |
| MA (1) | MA34644B1 (enExample) |
| MX (1) | MX2013005199A (enExample) |
| NO (1) | NO2638031T3 (enExample) |
| PH (1) | PH12013500880A1 (enExample) |
| PL (2) | PL3124483T3 (enExample) |
| PT (2) | PT2638031T (enExample) |
| RS (2) | RS56583B1 (enExample) |
| SG (1) | SG189043A1 (enExample) |
| SI (2) | SI3124483T1 (enExample) |
| TW (1) | TW201302733A (enExample) |
| WO (1) | WO2012062783A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| RU2017140639A (ru) | 2011-05-23 | 2019-02-12 | Элан Фармасьютикалз, Инк. | Ингибиторы активности киназы lrrk2 |
| EP2785711B1 (en) * | 2011-11-29 | 2016-08-03 | F.Hoffmann-La Roche Ag | 2-(phenyl or pyrid-3-yl)aminopyrimidine derivatives as kinase lrrk2 modulators for the treatment of parkinson's disease |
| AR089182A1 (es) | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| WO2013079493A1 (en) | 2011-11-29 | 2013-06-06 | F. Hoffmann-La Roche Ag | Aminopyrimidine derivatives as lrrk2 modulators |
| MX348606B (es) * | 2011-11-29 | 2017-06-21 | Genentech Inc | Derivados de aminopirimidina como moduladores de proteina cinasa 2 de repeticion rica en leucina (lrrk2). |
| US20140228384A1 (en) * | 2011-11-29 | 2014-08-14 | Genentech, Inc. | Assays and biomarkers for lrrk2 |
| RU2650641C2 (ru) | 2011-11-30 | 2018-04-16 | Дженентек, Инк. | Фтор-18 и углерод-11 меченые радиолиганды для томографии с позитронной эмиссией (рет), визуализирующей lrrk2 |
| CN106220615A (zh) * | 2012-05-03 | 2016-12-14 | 霍夫曼-拉罗奇有限公司 | 作为lrrk2调节剂的吡唑氨基嘧啶衍生物 |
| BR112014027117B1 (pt) * | 2012-05-03 | 2022-09-06 | Genentech, Inc | Derivados de pirazol aminopirimidina como moduladores de lrrk2, seus usos, e composição |
| EP3255049A1 (en) | 2012-06-29 | 2017-12-13 | Pfizer Inc | Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors |
| WO2014060381A1 (de) | 2012-10-18 | 2014-04-24 | Bayer Cropscience Ag | Heterocyclische verbindungen als schädlingsbekämpfungsmittel |
| WO2017156493A1 (en) | 2016-03-11 | 2017-09-14 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
| WO2014134772A1 (en) * | 2013-03-04 | 2014-09-12 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| 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 |
| EP3083591B1 (en) | 2013-12-17 | 2018-01-03 | Merck Patent GmbH | N1-(3,3,3-trifluoro-2-hydroxo-2-methylpropionyl)-piperidine derivatives as inhibitors of pyruvate dehydrogenase kinase |
| RU2016129380A (ru) | 2013-12-20 | 2018-01-25 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Замещенные диаминопиримидильные соединения, их композиции и способы лечения с их участием |
| WO2015113451A1 (en) | 2014-01-29 | 2015-08-06 | Glaxosmithkline Intellectual Property Development Limited | Compounds |
| UA118369C2 (uk) * | 2014-01-29 | 2019-01-10 | Глаксосмітклайн Інтеллектьюел Проперті Девелопмент Лімітед | Сполуки, що інгібують активність lrrk2 кінази |
| US9403801B2 (en) * | 2014-03-28 | 2016-08-02 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| US9859504B2 (en) * | 2014-03-31 | 2018-01-02 | Commonwealth Scientific And Industrial Research Organisation | Diamine compounds for phosphorescent diazaborole metal complexes and electroluminescent devices |
| WO2015170600A1 (ja) * | 2014-05-08 | 2015-11-12 | 東ソー・エフテック株式会社 | ５－（トリフルオロメチル）ピリミジン誘導体及びその製造方法 |
| WO2015176010A1 (en) | 2014-05-15 | 2015-11-19 | The United States Of America, As Represented By The Secretary, Departmentof Health & Human Services | Treatment or prevention of an intestinal disease or disorder |
| JP6262079B2 (ja) * | 2014-06-02 | 2018-01-17 | 東ソー・ファインケム株式会社 | ４−（２，２，２−トリフルオロエトキシ）−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法 |
| JP6431294B2 (ja) * | 2014-06-16 | 2018-11-28 | 東ソー・ファインケム株式会社 | ５−（トリフルオロメチル）ピリミジン誘導体及びその製造法 |
| WO2016060963A1 (en) | 2014-10-14 | 2016-04-21 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| KR102161364B1 (ko) | 2015-09-14 | 2020-09-29 | 화이자 인코포레이티드 | LRRK2 억제제로서 이미다조[4,5-c]퀴놀린 및 이미다조[4,5-c][1,5]나프티리딘 유도체 |
| WO2017087905A1 (en) * | 2015-11-20 | 2017-05-26 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| AU2017242225B2 (en) | 2016-03-29 | 2021-02-18 | Merck Patent Gmbh | N1-(3,3,3-trifluoro-2-hydroxy-2-methylpropionyl)-piperidine derivatives as inhibitors of pyruvate dehydrogenase kinase |
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| US20200157081A1 (en) * | 2017-05-24 | 2020-05-21 | Denali Therapeutics Inc. | Compounds, compositions and methods |
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| KR20220015437A (ko) * | 2019-05-31 | 2022-02-08 | 데날리 테라퓨틱스 인크. | 피리미디닐아미노-피라졸 화합물의 변형 방출 제제, 및 치료 방법 |
| CN110627810B (zh) * | 2019-06-05 | 2024-05-10 | 中国医学科学院药用植物研究所 | 一种三氟甲基吡唑衍生物的制备方法 |
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| BR112022018477A2 (pt) | 2020-03-23 | 2022-11-01 | Whan In Pharmaceutical Co Ltd | Composto derivado de pirimidina, composição compreendendo o mesmo, e seus usos na prevenção ou tratamento de doenças neurodegenerativas e câncer |
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| EP4525875A1 (en) * | 2022-05-20 | 2025-03-26 | Merck Sharp & Dohme LLC | Macrocycles as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof |
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| KR20250102043A (ko) | 2022-11-22 | 2025-07-04 | 데날리 테라퓨틱스 인크. | 피리미딘 아미노피라졸 화합물의 제조 방법 및 중간체 |
| CN115819405A (zh) * | 2022-12-20 | 2023-03-21 | 沪渝人工智能研究院 | 嘧啶氨基吡唑衍生物及其作为富亮氨酸重复激酶2抑制剂的应用 |
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