KR102553188B1 - 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸 - Google Patents

신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸 Download PDF

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KR102553188B1
KR102553188B1 KR1020197000749A KR20197000749A KR102553188B1 KR 102553188 B1 KR102553188 B1 KR 102553188B1 KR 1020197000749 A KR1020197000749 A KR 1020197000749A KR 20197000749 A KR20197000749 A KR 20197000749A KR 102553188 B1 KR102553188 B1 KR 102553188B1
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앤서니 에이. 에스트라다
지안웬 에이. 펭
조셉 피. 리시카토스
자카리 케이. 스위니
자비에르 드 비센테 피달고
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데날리 테라퓨틱스 인크.
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KR1020197000749A 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸 Active KR102553188B1 (ko)

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KR1020237022665A KR102705724B1 (ko) 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201662350876P 2016-06-16 2016-06-16
US62/350,876 2016-06-16
US201662417151P 2016-11-03 2016-11-03
US62/417,151 2016-11-03
US201762476581P 2017-03-24 2017-03-24
US62/476,581 2017-03-24
US201762510711P 2017-05-24 2017-05-24
US62/510,711 2017-05-24
PCT/US2017/037782 WO2017218843A1 (en) 2016-06-16 2017-06-15 Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders

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KR1020237022665A Division KR102705724B1 (ko) 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸

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KR102553188B1 true KR102553188B1 (ko) 2023-07-11

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KR1020237022665A Active KR102705724B1 (ko) 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸
KR1020197000749A Active KR102553188B1 (ko) 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸
KR1020247029993A Active KR102843750B1 (ko) 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸

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Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017156493A1 (en) 2016-03-11 2017-09-14 Denali Therapeutics Inc. Compounds, compositions, and methods
US11214565B2 (en) 2015-11-20 2022-01-04 Denali Therapeutics Inc. Compound, compositions, and methods
AU2017286653B2 (en) 2016-06-16 2021-11-04 Denali Therapeutics Inc. Pyrimidin-2-ylamino-1H-pyrazols as LRRK2 inhibitors for use in the treatment of neurodegenerative disorders
SG11202004733WA (en) 2017-11-21 2020-06-29 Denali Therapeutics Inc Polymorphs and solid forms of a pyrimidinylamino-pyrazole compound, and methods of production
KR20200100757A (ko) 2017-12-20 2020-08-26 데날리 테라퓨틱스 인크. 피리미디닐-4-아미노피라졸 화합물의 제조를 위한 공정
KR20190131981A (ko) * 2018-05-18 2019-11-27 재단법인 대구경북첨단의료산업진흥재단 외상성 뇌손상 또는 뇌졸중의 예방 또는 치료용 약학적 조성물
AR118641A1 (es) * 2019-04-11 2021-10-20 Denali Therapeutics Inc Compuestos, composiciones y métodos
MX2021014705A (es) * 2019-05-31 2022-04-06 Denali Therapeutics Inc Formulacion de liberacion modificada de un compuesto de pirimidinilamino-pirazol y metodos de tratamiento.
EP3769768A1 (en) 2019-07-23 2021-01-27 Consejo Superior de Investigaciones Cientificas (CSIC) Compounds useful for the treatment of parkinson s disease
EP4051682A1 (en) * 2019-10-29 2022-09-07 Biogen MA Inc. Spirocyclic o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
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
KR102342803B1 (ko) 2020-03-23 2021-12-24 환인제약 주식회사 신규한 피리미딘 유도체 및 이를 포함하는 신경퇴행성 질환 및 암의 예방 또는 치료용 조성물
DK4225306T3 (da) * 2020-10-07 2025-03-24 Alzprotect Anvendelse af n-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1h-benzo[d]imidazol-2-aminsulfatsalte og solvater heraf til behandling af motorneuronsygdomme og neuromuskulære forbindelseslidelser
CN114426542B (zh) * 2020-10-29 2023-06-30 苏州亚宝药物研发有限公司 取代的二芳基胺化合物及其药物组合物、制备方法和用途
US20240207266A1 (en) * 2021-04-30 2024-06-27 Denali Therapeutics Inc. Methods for treating and monitoring parkinson's disease
AR127470A1 (es) 2021-10-27 2024-01-31 H Lundbeck As Inhibidores de lrrk2
CA3250447A1 (en) 2021-12-15 2025-07-09 Whan In Pharmaceutical Co., Ltd. MACROCYCLIC PYRIMIDINE DERIVATIVE, ITS PREPARATION PROCESS, AND PHARMACEUTICAL COMPOSITION INTENDED FOR THE PREVENTION OR TREATMENT OF A NEURODEGENERATIVE DISEASE AND CONTAINING THIS DERIVATIVE AS AN ACTIVE INGREDIENT
CN117624185B (zh) * 2022-08-23 2025-12-05 长春金赛药业有限责任公司 Lrrk2抑制剂化合物、药物组合物及其制备方法和应用
US11958865B1 (en) 2022-09-15 2024-04-16 H. Lundbeck A/S Leucine-rich repeat kinase 2 (LRRK2) inhibitors
AU2023371948A1 (en) 2022-11-03 2025-05-15 Denali Therapeutics Inc. Solid and co-crystal forms of a pyrimidine triazole compound
CN115894456A (zh) * 2022-11-13 2023-04-04 药康众拓(江苏)医药科技有限公司 一种氘代吡唑氨基嘧啶类化合物、药物组合物和用途
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
WO2025051214A1 (zh) * 2023-09-07 2025-03-13 上海翊石医药科技有限公司 一种芳杂环类化合物及其制备方法
CN118878521B (zh) * 2024-09-26 2025-02-14 苏州美诺医药科技有限公司 一种lrrk2抑制剂的制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013164321A1 (en) 2012-05-03 2013-11-07 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as lrrk2 modulators

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1058549A4 (en) 1998-12-23 2003-11-12 Bristol Myers Squibb Pharma Co FACTOR Xa OR THROMBIN INHIBITORS
WO2003076658A2 (en) 2002-03-08 2003-09-18 Decode Genetics Ehf. A susceptibility gene for late-onset idiopathic parkinson's disease
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
US7371759B2 (en) * 2003-09-25 2008-05-13 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
AR049418A1 (es) 2004-02-27 2006-08-02 Bayer Pharmaceuticals Corp Derivados de heteroarilaminopirazol y composiciones farmaceuticas para el tratamiento de la diabetes.
US8211929B2 (en) 2004-12-30 2012-07-03 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
EP1746096A1 (en) 2005-07-15 2007-01-24 4Sc Ag 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
US20090247554A1 (en) 2006-03-30 2009-10-01 Takeda San Diego, Inc. Kinase inhibitors
BRPI0713738A2 (pt) 2006-06-20 2014-06-24 Novartis Ag Biomarcadores para a progressão de doença alzheimer
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
AR068072A1 (es) 2007-04-19 2009-11-04 Novartis Ag Derivados de bencimidazoles, composiciones farmaceuticas y usos
CN101679378A (zh) 2007-05-02 2010-03-24 沃泰克斯药物股份有限公司 用作激酶抑制剂的噻唑和吡唑
CN101687852A (zh) 2007-05-24 2010-03-31 沃泰克斯药物股份有限公司 可用作激酶抑制剂的噻唑类和吡唑类化合物
AU2008296479A1 (en) 2007-08-28 2009-03-12 Dana Farber Cancer Institute Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis
WO2009127642A2 (en) 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
AR075713A1 (es) 2009-03-03 2011-04-20 Du Pont Pirazoles fungicidas
WO2010111406A2 (en) 2009-03-24 2010-09-30 Myriad Pharmaceuticals, Inc. Compounds and therapeutic uses thereof
TW201111385A (en) 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
CA2780892C (en) 2009-11-13 2017-02-14 Genosco Kinase inhibitors
GB201008134D0 (en) 2010-05-14 2010-06-30 Medical Res Council Technology Compounds
AU2011260323A1 (en) 2010-06-04 2012-11-15 F. Hoffmann-La Roche Ag Aminopyrimidine derivatives as LRRK2 modulators
WO2011156698A2 (en) 2010-06-11 2011-12-15 Abbott Laboratories NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
US9233977B2 (en) 2010-10-29 2016-01-12 Merck Sharp & Dohme Corp. Leucine-rich repeat kinase enzyme activity
DK2638031T3 (en) 2010-11-10 2017-12-11 Genentech Inc PYRAZOLAMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
JP2014504362A (ja) 2010-11-30 2014-02-20 ジェネンテック， インコーポレイテッド Ｌｒｒｋ２のためのアッセイ及びバイオマーカー
EP2720719A4 (en) 2011-06-15 2015-12-09 Glaxosmithkline Ip No 2 Ltd METHOD FOR SELECTION OF THERAPEUTIC INDICATIONS
CN103781780B (zh) 2011-07-28 2015-11-25 赛尔佐姆有限公司 作为jak抑制剂的杂环基嘧啶类似物
PH12014500638A1 (en) 2011-09-22 2017-08-09 Pfizer Pyrrolopyrimidine and purine derivatives
WO2013079493A1 (en) 2011-11-29 2013-06-06 F. Hoffmann-La Roche Ag Aminopyrimidine derivatives as lrrk2 modulators
CA2850594C (en) 2011-11-29 2020-03-10 F. Hoffmann-La Roche Ag Aminopyrimidine derivatives as lrrk2 modulators
AR089182A1 (es) 2011-11-29 2014-08-06 Hoffmann La Roche Derivados de aminopirimidina como moduladores de lrrk2
HRP20161396T1 (hr) 2011-11-29 2016-12-02 F. Hoffmann - La Roche Ag Derivati 2-(fenil ili pirid-3-il)aminopirimidina kao modulatori lrrk2-kinaze za liječenje parkinsonove bolesti
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
WO2013126283A1 (en) 2012-02-20 2013-08-29 E. I. Du Pont De Nemours And Company Fungicidal pyrazoles
SI2820009T1 (en) 2012-03-01 2018-05-31 Array Biopharma, Inc. Serine / Threonine kinase inhibitors
BR112014027117B1 (pt) * 2012-05-03 2022-09-06 Genentech, Inc Derivados de pirazol aminopirimidina como moduladores de lrrk2, seus usos, e composição
WO2017156493A1 (en) 2016-03-11 2017-09-14 Denali Therapeutics Inc. Compounds, compositions, and methods
US9624180B2 (en) 2013-01-25 2017-04-18 Bristol-Myers Squibb Company Squaric derivatives for the treatment of hepatitis C
WO2014130241A1 (en) 2013-02-20 2014-08-28 E. I. Du Pont De Nemours And Company Fungicidal pyrazoles
CA2903901A1 (en) 2013-03-05 2014-09-12 Merck Patent Gmbh 9-(aryl or heteroaryl)-2-(pyrazolyl, pyrrolidinyl or cyclopentyl)aminopurine derivatives as anticancer agents
EP3388436B1 (en) 2013-03-15 2020-08-12 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone compounds and methods of treating disorders
US20160024071A1 (en) 2013-03-15 2016-01-28 Elan Pharmaceuticals, Llc Inhibitors of lrrk2 kinase activity
TW201533043A (zh) * 2013-04-18 2015-09-01 Lundbeck & Co As H 作爲ｌｒｒｋ２抑制劑的芳基吡咯并吡啶衍生化合物
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
DK2994465T3 (en) 2013-05-10 2018-10-08 Karus Therapeutics Ltd HISTONDEACETYLASE INHIBITORS UNKNOWN
SG11201605342UA (en) 2014-01-29 2016-08-30 Glaxosmithkline Ip Dev Ltd Compounds
US9580430B2 (en) 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
JP6517318B2 (ja) 2014-03-28 2019-05-22 キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーＣａｌｉｔｏｒ Ｓｃｉｅｎｃｅｓ， Ｌｌｃ 置換されたヘテロアリール化合物および使用方法
JP6684780B2 (ja) 2014-08-25 2020-04-22 ソーク インスティテュート フォー バイオロジカル スタディーズ 新規ｕｌｋ１阻害剤およびそれを使用する方法
CN105461694B (zh) 2014-09-27 2019-05-24 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
WO2016090285A1 (en) 2014-12-05 2016-06-09 Array Biopharma Inc. 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS
WO2016149311A1 (en) 2015-03-19 2016-09-22 E I Du Pont De Nemours And Company Fungicidal pyrazoles
JP2018135268A (ja) 2015-06-05 2018-08-30 大日本住友製薬株式会社 新規ヘテロアリールアミノ−３−ピラゾール誘導体およびその薬理学上許容される塩
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
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
EP3377629B1 (en) 2015-11-18 2023-07-05 Rosalind Franklin University of Medicine and Science Antisense compounds targeting leucine-rich repeat kinase 2 (lrrk2) for the treatment of parkinsons disease
US11214565B2 (en) 2015-11-20 2022-01-04 Denali Therapeutics Inc. Compound, compositions, and methods
TW201720828A (zh) 2015-11-23 2017-06-16 赫孚孟拉羅股份公司 治療性化合物及組合物以及其使用方法
WO2017100703A1 (en) 2015-12-10 2017-06-15 Colin Combs Ems analogues of lyn/src-tyrosine kinase inhibitors
US10023579B2 (en) 2015-12-16 2018-07-17 Southern Research Institute Pyrrolopyrimidine compounds, use as inhibitors of the kinase LRRK2, and methods for preparation thereof
TWI781920B (zh) * 2016-02-05 2022-11-01 美商戴納立製藥公司 化合物、組合物及方法
AU2017286653B2 (en) 2016-06-16 2021-11-04 Denali Therapeutics Inc. Pyrimidin-2-ylamino-1H-pyrazols as LRRK2 inhibitors for use in the treatment of neurodegenerative disorders
US20200157081A1 (en) 2017-05-24 2020-05-21 Denali Therapeutics Inc. Compounds, compositions and methods

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013164321A1 (en) 2012-05-03 2013-11-07 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as lrrk2 modulators

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Journal of Medicinal Chemistry, vol. 57. no. 3, pp. 921-936 (2014)

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