KR102843750B1 - 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

Info

Publication number
KR102843750B1
KR102843750B1 KR1020247029993A KR20247029993A KR102843750B1 KR 102843750 B1 KR102843750 B1 KR 102843750B1 KR 1020247029993 A KR1020247029993 A KR 1020247029993A KR 20247029993 A KR20247029993 A KR 20247029993A KR 102843750 B1 KR102843750 B1 KR 102843750B1
Authority
KR
South Korea
Prior art keywords
optionally substituted
mixture
disease
pyrazol
methyl
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.)
Active
Application number
KR1020247029993A
Other languages
English (en)
Korean (ko)
Other versions
KR20240137707A (ko
Inventor
앤서니 에이. 에스트라다
지안웬 에이. 펭
조셉 피. 리시카토스
자카리 케이. 스위니
자비에르 드 비센테 피달고
Original Assignee
데날리 테라퓨틱스 인크.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 데날리 테라퓨틱스 인크. filed Critical 데날리 테라퓨틱스 인크.
Publication of KR20240137707A publication Critical patent/KR20240137707A/ko
Application granted granted Critical
Publication of KR102843750B1 publication Critical patent/KR102843750B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Management, Administration, Business Operations System, And Electronic Commerce (AREA)
KR1020247029993A 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸 Active KR102843750B1 (ko)

Applications Claiming Priority (10)

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

Related Parent Applications (1)

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

Publications (2)

Publication Number Publication Date
KR20240137707A KR20240137707A (ko) 2024-09-20
KR102843750B1 true KR102843750B1 (ko) 2025-08-07

Family

ID=59216078

Family Applications (3)

Application Number Title Priority Date Filing Date
KR1020247029993A Active KR102843750B1 (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
KR1020237022665A Active KR102705724B1 (ko) 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸

Family Applications After (2)

Application Number Title Priority Date Filing Date
KR1020197000749A Active KR102553188B1 (ko) 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸
KR1020237022665A Active KR102705724B1 (ko) 2016-06-16 2017-06-15 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸

Country Status (37)

Country Link
US (7) US20170362206A1 (enExample)
EP (3) EP4635570A2 (enExample)
JP (1) JP7004459B2 (enExample)
KR (3) KR102843750B1 (enExample)
CN (2) CN109311857B (enExample)
AU (3) AU2017286653B2 (enExample)
CA (1) CA3025672A1 (enExample)
CL (1) CL2018003597A1 (enExample)
CO (1) CO2018013585A2 (enExample)
CR (2) CR20220182A (enExample)
CU (1) CU24605B1 (enExample)
CY (1) CY1124789T1 (enExample)
DK (1) DK3998261T3 (enExample)
DO (3) DOP2018000285A (enExample)
EC (1) ECSP18092481A (enExample)
ES (2) ES2900368T3 (enExample)
HR (1) HRP20211923T1 (enExample)
HU (1) HUE056678T2 (enExample)
IL (3) IL299412B2 (enExample)
JO (1) JOP20180113B1 (enExample)
LT (1) LT3472153T (enExample)
MD (1) MD3472153T2 (enExample)
MX (3) MX392230B (enExample)
PE (2) PE20190395A1 (enExample)
PH (1) PH12018502427A1 (enExample)
PL (1) PL3472153T3 (enExample)
PT (1) PT3472153T (enExample)
RS (1) RS62868B1 (enExample)
SA (2) SA521430638B1 (enExample)
SG (2) SG10201912632YA (enExample)
SI (1) SI3472153T1 (enExample)
SM (1) SMT202100699T1 (enExample)
TN (1) TN2018000422A1 (enExample)
TW (1) TWI786049B (enExample)
UA (1) UA126231C2 (enExample)
WO (1) WO2017218843A1 (enExample)
ZA (1) ZA201900229B (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017087905A1 (en) 2015-11-20 2017-05-26 Denali Therapeutics Inc. Compound, compositions, and methods
US11028080B2 (en) 2016-03-11 2021-06-08 Denali Therapeutics Inc. Substituted pyrimidines as LRKK2 inhibitors
CN109311857B (zh) 2016-06-16 2021-11-12 戴纳立制药公司 作为用于治疗神经退化性病症的lrrk2抑制剂的嘧啶-2-基氨基-1h-吡唑
WO2019104086A1 (en) 2017-11-21 2019-05-31 Denali Therapeutics Inc. Polymorphs and solid forms of a pyrimidinylamino-pyrazole compound, and methods of production
AU2018392599A1 (en) * 2017-12-20 2020-07-09 Denali Therapeutics Inc. Process for the preparation of pyrimidinyl-4-aminopyrazole compounds
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
BR112021024194A2 (pt) * 2019-05-31 2022-01-11 Denali Therapeutics Inc Formulação de liberação modificada de um composto de pirimidinilamino-pirazol e métodos de tratamento
EP3769768A1 (en) 2019-07-23 2021-01-27 Consejo Superior de Investigaciones Cientificas (CSIC) Compounds useful for the treatment of parkinson s disease
WO2021086966A1 (en) * 2019-10-29 2021-05-06 Biogen Ma Inc. Spirocyclic o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
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
WO2022074093A1 (en) * 2020-10-07 2022-04-14 Alzprotect Use of n-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1h-benzo[d]imidazol-2-amine sulphate salts and solvates thereof for the treatment of motor neuron diseases and neuromuscular junction disorders
JP7522315B2 (ja) * 2020-10-29 2024-07-24 蘇州亜宝薬物研発有限公司 置換ジアリールアミン化合物及びその医薬組成物、製造方法と用途
JP2024515885A (ja) * 2021-04-30 2024-04-10 デナリ セラピューティクス インコーポレイテッド パーキンソン病を処置及びモニタリングするための方法
TW202330549A (zh) 2021-10-27 2023-08-01 丹麥商H 朗德貝克公司 Lrrk2抑制劑
JP2024546154A (ja) 2021-12-15 2024-12-17 ワン イン ファーマシューティカル カンパニー リミテッド 大環状ピリミジン誘導体、その製造方法、及び、それを活性成分として含む神経変性疾患の予防又は治療のための医薬組成物
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
TW202412777A (zh) 2022-09-15 2024-04-01 丹麥商H 朗德貝克公司 富白胺酸重複激酶2(lrrk2)抑制劑
TW202434570A (zh) 2022-11-03 2024-09-01 美商戴納立製藥公司 嘧啶三唑化合物之固體及共晶體形式
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
JP2025538526A (ja) 2022-11-22 2025-11-28 デナリ セラピューティクス インコーポレイテッド ピリミジンアミノピラゾール化合物を調製するためのプロセス及び中間体
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012062783A1 (en) 2010-11-10 2012-05-18 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as lrrk2 modulators
WO2013164321A1 (en) 2012-05-03 2013-11-07 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as lrrk2 modulators

Family Cites Families (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000038683A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa 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.
EP1841760B1 (en) 2004-12-30 2011-08-10 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
WO2007117995A2 (en) 2006-03-30 2007-10-18 Takeda San Diego, Inc. Kinase inhibitors
CN101473044A (zh) 2006-06-20 2009-07-01 诺瓦提斯公司 阿尔茨海默病进展的生物标记
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
CN101679299A (zh) 2007-04-19 2010-03-24 诺瓦提斯公司 作为代谢型谷氨酸受体-5调节剂的烟酸衍生物
AU2008247592A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
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
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
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
NZ599041A (en) 2009-11-13 2014-05-30 Genosco Kinase inhibitors
GB201008134D0 (en) 2010-05-14 2010-06-30 Medical Res Council Technology Compounds
HUE029196T2 (en) 2010-06-04 2017-02-28 Hoffmann La Roche Aminoprimidine derivatives as LRRK2 modulators
US8637529B2 (en) 2010-06-11 2014-01-28 AbbYie Inc. Pyrazolo[3,4-d]pyrimidine compounds
WO2012058193A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. Leucine-rich repeat kinase enzyme activity
EP2646819A1 (en) 2010-11-30 2013-10-09 Genentech, Inc. Assays and biomarkers for lrrk2
WO2012174338A2 (en) 2011-06-15 2012-12-20 Glaxosmithkline Llc Method of selecting therapeutic indications
BR112014000360A2 (pt) 2011-07-28 2017-02-14 Cellzome Ltd análogos de heterociclil pirimidina como inibidores jak
PE20141228A1 (es) 2011-09-22 2014-10-01 Pfizer Derivados de pirrolopirimidina y purina
CA2852609C (en) 2011-11-29 2020-03-10 F. Hoffmann-La Roche Ag Aminopyrimidine derivatives as lrrk2 modulators
CN106243090A (zh) 2011-11-29 2016-12-21 霍夫曼-拉罗奇有限公司 作为用于治疗帕金森病的激酶lrrk2调节剂的2‑(苯基或吡啶‑3‑基)氨基嘧啶衍生物
WO2013079505A1 (en) 2011-11-29 2013-06-06 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
JP6148248B2 (ja) 2011-11-30 2017-06-14 ジェネンテック, インコーポレイテッド Lrrk2のポジトロン放出断層撮影(pet)イメージングのためのフッ素−18及び炭素−11標識放射性リガンド
WO2013126283A1 (en) 2012-02-20 2013-08-29 E. I. Du Pont De Nemours And Company Fungicidal pyrazoles
AU2013225737B2 (en) 2012-03-01 2018-03-01 Array Biopharma Inc. Serine/threonine kinase inhibitors
EP2844658B1 (en) * 2012-05-03 2019-03-20 Genentech, Inc. Pyrazole aminopyrimidine derivatives as lrrk2 modulators for use in the treatment of parkinson's disease
WO2014116772A2 (en) 2013-01-25 2014-07-31 Bristol-Myers Squibb Company Squaric derivatives for the treatment of hepatitis c
EP3010908A1 (en) 2013-02-20 2016-04-27 E. I. du Pont de Nemours and Company Fungicidal pyrazoles
US9617266B2 (en) 2013-03-05 2017-04-11 Merck Patent Gmbh Imidazopyrimidine derivatives
WO2014150981A1 (en) 2013-03-15 2014-09-25 Elan Pharmaceuticals, Llc Inhibitors of lrrk2 kinase activity
EP3388436B1 (en) 2013-03-15 2020-08-12 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone compounds and methods of treating disorders
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
PT2994465T (pt) 2013-05-10 2018-10-25 Karus Therapeutics Ltd Novos inibidores de histona desacetilase
CA2937431A1 (en) 2014-01-29 2015-08-06 Glaxosmithkline Intellectual Property Development Limited Compounds
CA2940554A1 (en) 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
JP6517319B2 (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
UA120065C2 (uk) 2014-12-05 2019-09-25 Ерей Біофарма Інк. 4,6-ЗАМІЩЕНІ ПІРАЗОЛО[1,5-a]-ПІРАЗИНИ ЯК ІНГІБІТОРИ JAK-КІНАЗИ
EP3271336A1 (en) 2015-03-19 2018-01-24 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
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP6873980B2 (ja) 2015-09-14 2021-05-19 ファイザー・インク LRRK2阻害薬としての新規のイミダゾ[4,5−c]キノリンおよびイミダゾ[4,5−c][1,5]ナフチリジン誘導体
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
WO2017087905A1 (en) 2015-11-20 2017-05-26 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
WO2017106771A1 (en) 2015-12-16 2017-06-22 Southern Research Institute Pyrrolopyrimidine compounds, use as inhibitors of the kinase lrrk2, and methods for preparation thereof
CN118994191A (zh) * 2016-02-05 2024-11-22 戴纳立制药公司 受体相互作用蛋白激酶1的抑制剂
US11028080B2 (en) 2016-03-11 2021-06-08 Denali Therapeutics Inc. Substituted pyrimidines as LRKK2 inhibitors
CN109311857B (zh) 2016-06-16 2021-11-12 戴纳立制药公司 作为用于治疗神经退化性病症的lrrk2抑制剂的嘧啶-2-基氨基-1h-吡唑
WO2018217946A1 (en) 2017-05-24 2018-11-29 Denali Therapeutics Inc. Compounds, compositions and methods

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012062783A1 (en) 2010-11-10 2012-05-18 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as lrrk2 modulators
WO2013164321A1 (en) 2012-05-03 2013-11-07 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as lrrk2 modulators

Also Published As

Publication number Publication date
US20220135546A1 (en) 2022-05-05
JP7004459B2 (ja) 2022-02-10
AU2017286653A1 (en) 2018-12-20
CN109311857B (zh) 2021-11-12
DOP2018000285A (es) 2019-01-15
US11111235B2 (en) 2021-09-07
AU2022202372B2 (en) 2024-04-04
IL299412B2 (en) 2025-05-01
US20210002260A1 (en) 2021-01-07
DOP2022000088A (es) 2022-06-15
US9932325B2 (en) 2018-04-03
EP3472153B1 (en) 2021-09-22
LT3472153T (lt) 2021-12-27
AU2024204621A1 (en) 2024-07-18
KR20190018676A (ko) 2019-02-25
IL299415B1 (en) 2025-05-01
SG11201810579YA (en) 2018-12-28
AU2017286653B2 (en) 2021-11-04
SA521430638B1 (ar) 2023-07-12
KR20240137707A (ko) 2024-09-20
US20180051009A1 (en) 2018-02-22
BR112018075569A2 (pt) 2019-03-19
US10590114B2 (en) 2020-03-17
ECSP18092481A (es) 2018-12-31
PE20190395A1 (es) 2019-03-13
CR20220182A (es) 2022-06-15
EP3472153A1 (en) 2019-04-24
IL299412B1 (en) 2025-01-01
KR20230107407A (ko) 2023-07-14
JP2019521984A (ja) 2019-08-08
ZA201900229B (en) 2022-10-26
JOP20180113A1 (ar) 2019-01-30
DK3998261T3 (da) 2025-08-18
AU2022202372A1 (en) 2022-04-28
KR102553188B1 (ko) 2023-07-11
US11591316B2 (en) 2023-02-28
UA126231C2 (uk) 2022-09-07
IL263484A (en) 2019-01-31
MD3472153T2 (ro) 2022-03-31
EP3998261A1 (en) 2022-05-18
IL299412A (en) 2023-02-01
KR102705724B1 (ko) 2024-09-12
US20170362206A1 (en) 2017-12-21
US20250034119A1 (en) 2025-01-30
PE20240221A1 (es) 2024-02-16
PT3472153T (pt) 2021-12-31
NZ748936A (en) 2024-12-20
TW201835069A (zh) 2018-10-01
MX392230B (es) 2025-03-21
SI3472153T1 (sl) 2022-01-31
US20180208582A1 (en) 2018-07-26
EP4635570A2 (en) 2025-10-22
JOP20180113B1 (ar) 2022-03-14
RS62868B1 (sr) 2022-02-28
CL2018003597A1 (es) 2019-02-15
US20230227436A1 (en) 2023-07-20
EP3998261B1 (en) 2025-05-07
IL263484B2 (en) 2024-02-01
CU24605B1 (es) 2022-06-06
MX2021010304A (es) 2021-10-13
SMT202100699T1 (it) 2022-01-10
CU20180152A7 (es) 2019-09-04
CN114315819A (zh) 2022-04-12
US11834439B2 (en) 2023-12-05
WO2017218843A1 (en) 2017-12-21
SA518400660B1 (ar) 2023-06-04
PL3472153T3 (pl) 2022-02-07
CA3025672A1 (en) 2017-12-21
CY1124789T1 (el) 2022-11-25
CN109311857A (zh) 2019-02-05
DOP2023000077A (es) 2023-05-31
IL263484B1 (en) 2023-10-01
ES2900368T3 (es) 2022-03-16
CO2018013585A2 (es) 2019-01-18
TWI786049B (zh) 2022-12-11
MX2022005610A (es) 2022-06-23
PH12018502427A1 (en) 2019-09-30
CR20180592A (es) 2019-03-05
SG10201912632YA (en) 2020-02-27
MX2018015630A (es) 2019-04-11
ES3036953T3 (en) 2025-09-26
HUE056678T2 (hu) 2022-02-28
HRP20211923T1 (hr) 2022-03-04
TN2018000422A1 (en) 2020-06-15
IL299415A (en) 2023-02-01
IL299415B2 (en) 2025-09-01

Similar Documents

Publication Publication Date Title
KR102843750B1 (ko) 신경퇴행성 장애의 치료에서 사용하기 위한 lrrk2 저해제로서 피리미딘-2-일아미노-1h-피라졸
HK40074923B (en) Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders
HK40074923A (en) Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders
HK40007576B (en) Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders
OA19864A (en) Compounds, compositions, and methods.
BR122021017711B1 (pt) Compostos inibidores de lrrk2, composição farmacêutica que os compreendem, usos dos compostos e processos para preparação dos compostos
EA043797B1 (ru) Пиримидин-2-иламино-1н-пиразолы в качестве ингибиторов lrrk2 для применения при лечении нейродегенеративных заболеваний
BR112018075569B1 (pt) Compostos inibidores de lrrk2, composição farmacêutica que os compreende, uso do composto e processo para preparar os compostos
NZ788753A (en) Pyrimidin-2-ylamino-1H-pyrazols as LRRK2 inhibitors for use in the treatment of neurodegenerative disorders

Legal Events

Date Code Title Description
A107 Divisional application of patent
PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601