ES2653967T3 - Derivados de pirazol aminopirimidina como moduladores de LRRK2 - Google Patents
Derivados de pirazol aminopirimidina como moduladores de LRRK2 Download PDFInfo
- Publication number
- ES2653967T3 ES2653967T3 ES11782588.5T ES11782588T ES2653967T3 ES 2653967 T3 ES2653967 T3 ES 2653967T3 ES 11782588 T ES11782588 T ES 11782588T ES 2653967 T3 ES2653967 T3 ES 2653967T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- cycloalkyl
- optionally substituted
- halo
- alkoxy
- 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
- C07D403/14—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
- A61K31/506—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
- C07D403/02—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
-
- 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 | |
| US412273P | 2010-11-10 | ||
| US201161546613P | 2011-10-13 | 2011-10-13 | |
| US201161546613P | 2011-10-13 | ||
| PCT/EP2011/069696 WO2012062783A1 (en) | 2010-11-10 | 2011-11-09 | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2653967T3 true ES2653967T3 (es) | 2018-02-09 |
Family
ID=44983512
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11782588.5T Active ES2653967T3 (es) | 2010-11-10 | 2011-11-09 | Derivados de pirazol aminopirimidina como moduladores de LRRK2 |
| ES16180927T Active ES2746134T3 (es) | 2010-11-10 | 2011-11-09 | Derivados de pirazol aminopirimidina como moduladores de LRRK2 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES16180927T Active ES2746134T3 (es) | 2010-11-10 | 2011-11-09 | Derivados de pirazol aminopirimidina como moduladores de LRRK2 |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US8815882B2 (enExample) |
| EP (3) | EP3590933B1 (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) | HUE037844T2 (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) | PT3124483T (enExample) |
| RS (2) | RS59106B1 (enExample) |
| SG (1) | SG189043A1 (enExample) |
| SI (2) | SI3124483T1 (enExample) |
| TW (1) | TW201302733A (enExample) |
| WO (1) | WO2012062783A1 (enExample) |
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012162254A1 (en) | 2011-05-23 | 2012-11-29 | Elan Pharmaceuticals, Inc. | Inhibitors of lrrk2 kinase activity |
| US9145402B2 (en) | 2011-11-29 | 2015-09-29 | Genentech, Inc. | Aminopyrimidine derivatives as LRRK2 modulators |
| US20140228384A1 (en) * | 2011-11-29 | 2014-08-14 | Genentech, Inc. | Assays and biomarkers for lrrk2 |
| AR089182A1 (es) | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| US8791130B2 (en) * | 2011-11-29 | 2014-07-29 | Genentech, Inc. | Aminopyrimidine derivatives as LRRK2 modulators |
| JP6185925B2 (ja) * | 2011-11-29 | 2017-08-23 | ジェネンテック， インコーポレイテッド | Ｌｒｒｋ２モジュレーターとしてのアミノピリミジン誘導体 |
| WO2013079496A1 (en) * | 2011-11-30 | 2013-06-06 | F. Hoffmann-La Roche Ag | Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (pet) imaging for lrrk2 |
| WO2013164323A1 (en) * | 2012-05-03 | 2013-11-07 | F. Hoffmann-La Roche Ag | Pyrazole aminopyrimidine derivatives as lrrk2 modulators for use in the treatment of parkinson's disease |
| CN104271569B (zh) * | 2012-05-03 | 2016-08-24 | 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 |
| EA025186B1 (ru) | 2012-06-29 | 2016-11-30 | Пфайзер Инк. | НОВЫЕ 4-(ЗАМЕЩЕННЫЙ АМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LRRK2 |
| WO2014060381A1 (de) | 2012-10-18 | 2014-04-24 | Bayer Cropscience Ag | Heterocyclische verbindungen als schädlingsbekämpfungsmittel |
| WO2014134772A1 (en) * | 2013-03-04 | 2014-09-12 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
| EP3083618B1 (en) | 2013-12-17 | 2018-02-21 | 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 |
| CA2933927C (en) | 2013-12-17 | 2021-11-16 | 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 |
| SG11201605342UA (en) * | 2014-01-29 | 2016-08-30 | Glaxosmithkline Ip Dev Ltd | Compounds |
| RU2016134751A (ru) | 2014-01-29 | 2018-03-02 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Соединения |
| US9399637B2 (en) * | 2014-03-28 | 2016-07-26 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| EP2927221A1 (en) * | 2014-03-31 | 2015-10-07 | Commonwealth Scientific and Industrial Research Organisation | Diamine compounds for phosphorescent diazaborole metal complexes and electroluminescent devices |
| GB2538476B (en) * | 2014-05-08 | 2019-03-20 | Tosoh F Tech Inc | 5-(Trifluoromethyl)pyrimidine derivatives and method for producing same |
| 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 |
| US10059689B2 (en) | 2014-10-14 | 2018-08-28 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| RU2722149C1 (ru) | 2015-09-14 | 2020-05-27 | Пфайзер Инк. | Новые производные имидазо[4,5-c] хинолинов и имидазо[4,5-c][1,5] нафтиридинов в качестве ингибиторов LRRK2 |
| US11214565B2 (en) | 2015-11-20 | 2022-01-04 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| EP3436443B1 (en) | 2016-03-29 | 2020-03-11 | Merck Patent GmbH | N1-(3,3,3-trifluoro-2-hydroxy-2-methylpropionyl)-piperidine derivatives as inhibitors of pyruvate dehydrogenase kinase |
| CN109071490B (zh) | 2016-04-28 | 2021-04-06 | 默克专利股份公司 | 哌啶基衍生物 |
| PT3472153T (pt) * | 2016-06-16 | 2021-12-31 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazóis como inibidores de lrrk2 para uso no tratamento de distúrbios neurodegenerativos |
| CN106588884B (zh) * | 2016-11-10 | 2019-04-09 | 浙江大学 | 2-多取代芳环-嘧啶类衍生物及制备和医药用途 |
| CN106588885B (zh) * | 2016-11-10 | 2019-03-19 | 浙江大学 | 2-取代芳环-嘧啶类衍生物及制备和应用 |
| SG11201908234WA (en) | 2017-02-24 | 2019-10-30 | Daegu Gyeongbuk Medical Innovation Found | Pharmaceutical composition comprising compound capable of penetrating blood-brain barrier as effective ingredient for preventing or treating brain cancer |
| GB201705263D0 (en) * | 2017-03-31 | 2017-05-17 | Probiodrug Ag | Novel inhibitors |
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| CA3069554A1 (en) * | 2017-07-14 | 2019-01-17 | Glaxosmithkline Intellectual Property Development Limited | Inhibitors of leucine rich repeat kinase 2 |
| WO2019099311A1 (en) | 2017-11-19 | 2019-05-23 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| ES2975319T3 (es) | 2017-11-21 | 2024-07-04 | Denali Therapeutics Inc | Polimorfos y formas sólidas de un compuesto de pirimidinilamino-pirazol y métodos de producción |
| CA3086182A1 (en) * | 2017-12-20 | 2019-06-27 | Denali Therapeutics Inc. | Process for the preparation of pyrimidinyl-4-aminopyrazole compounds |
| WO2019160037A1 (ja) * | 2018-02-14 | 2019-08-22 | 国立大学法人 東京大学 | 酸ハロゲン化物による化合物の製造方法 |
| AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| AR118641A1 (es) * | 2019-04-11 | 2021-10-20 | Denali Therapeutics Inc | Compuestos, composiciones y métodos |
| HRP20231310T1 (hr) * | 2019-05-10 | 2024-02-02 | Deciphera Pharmaceuticals, Llc | Heteroarilaminopirimidin amidni inhibitori autofagije i postupci njihove primjene |
| SG11202112464PA (en) * | 2019-05-31 | 2021-12-30 | Denali Therapeutics Inc | Modified release formulation of a pyrimidinylamino-pyrazole compound, and methods of treatment |
| 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 |
| ES3072710T3 (en) | 2019-06-17 | 2026-07-03 | Deciphera Pharmaceuticals Llc | Aminopyrimidine amide autophagy inhibitors and methods of use thereof |
| TW202116754A (zh) * | 2019-07-11 | 2021-05-01 | 美商Ｅ 斯蓋普生物股份有限公司 | 作為ｌｒｒｋ２抑制劑之吲唑及氮雜吲唑 |
| JP7691991B2 (ja) * | 2020-03-06 | 2025-06-12 | ナショナル・ヘルス・リサーチ・インスティテューツ | ピリミジン化合物及びその薬学的使用 |
| KR102342803B1 (ko) | 2020-03-23 | 2021-12-24 | 환인제약 주식회사 | 신규한 피리미딘 유도체 및 이를 포함하는 신경퇴행성 질환 및 암의 예방 또는 치료용 조성물 |
| CA3172750A1 (en) | 2020-03-23 | 2021-09-30 | Ge Hyeong Lee | Novel pyrimidine derivative, and composition for preventing or treating neurodegenerative diseases and cancer, comprising same |
| AU2021363536A1 (en) | 2020-10-20 | 2023-02-23 | F. Hoffmann-La Roche Ag | Combination therapy of PD-1 axis binding antagonists and LRRK2 inhitibors |
| AU2021371136A1 (en) | 2020-10-29 | 2023-05-11 | Merck Sharp & Dohme Llc | N-linked isoquinoline amides as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof |
| TW202237119A (zh) | 2020-12-10 | 2022-10-01 | 美商住友製藥腫瘤公司 | Ａｌｋ﹘５抑制劑和彼之用途 |
| EP4308115A4 (en) * | 2021-03-17 | 2025-01-22 | Merck Sharp & Dohme LLC | HETEROAROYL AMIDES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF |
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| CN117355304A (zh) * | 2021-03-26 | 2024-01-05 | 住友制药肿瘤公司 | Alk-5抑制剂及其用途 |
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| US20250313575A1 (en) * | 2022-05-20 | 2025-10-09 | Merck Sharp & Dohme Llc | Macrocycles as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof |
| CN120826397A (zh) | 2022-11-03 | 2025-10-21 | 戴纳立制药公司 | 嘧啶三唑化合物的固体及共晶体形式 |
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| CN118546132A (zh) * | 2023-02-27 | 2024-08-27 | 科辉智药(深圳)新药研究中心有限公司 | 亚砜酰亚胺化合物及其作为lrrk2蛋白激酶抑制剂的应用 |
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