CU24605B1 - Pirimidin-2-il amino-1h-pirazoles útiles como inhibidores de lrrk2 - Google Patents
Pirimidin-2-il amino-1h-pirazoles útiles como inhibidores de lrrk2Info
- Publication number
- CU24605B1 CU24605B1 CU2018000152A CU20180152A CU24605B1 CU 24605 B1 CU24605 B1 CU 24605B1 CU 2018000152 A CU2018000152 A CU 2018000152A CU 20180152 A CU20180152 A CU 20180152A CU 24605 B1 CU24605 B1 CU 24605B1
- Authority
- CU
- Cuba
- Prior art keywords
- pyrimidin
- amino
- lrrk2 inhibitors
- useful
- inhibitors
- Prior art date
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- 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
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- 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
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- 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
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- 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
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- 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
- A61P25/28—Drugs 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
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- C07—ORGANIC CHEMISTRY
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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
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- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/14—Heterocyclic 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
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- 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
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/12—Heterocyclic 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
- C07D491/20—Spiro-condensed systems
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic 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
- C07D498/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Oncology (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)
- Medicinal Preparation (AREA)
- Management, Administration, Business Operations System, And Electronic Commerce (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
<p>La presente divulgación se refiere en general a los inhibidores de LRRK2 de fórmula Ia:</p> <p>ESPACIO PARA LA FÓRMULA</p> <p>o uno de sus análogos deuterados, tautómeros, estereoisómeros farmacéuticamente aceptables, o mezcla de sus estereoisómeros, en donde dichos inhibidores son útiles en el tratamiento de una enfermedad neurodegenerativa, cáncer o una enfermedad inflamatoria.</p>
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662350876P | 2016-06-16 | 2016-06-16 | |
| US201662417151P | 2016-11-03 | 2016-11-03 | |
| US201762476581P | 2017-03-24 | 2017-03-24 | |
| US201762510711P | 2017-05-24 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CU20180152A7 CU20180152A7 (es) | 2019-09-04 |
| CU24605B1 true CU24605B1 (es) | 2022-06-06 |
Family
ID=59216078
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CU2018000152A CU24605B1 (es) | 2016-06-16 | 2017-06-15 | Pirimidin-2-il amino-1h-pirazoles útiles como inhibidores de lrrk2 |
Country Status (36)
| Country | Link |
|---|---|
| US (7) | US20170362206A1 (es) |
| EP (3) | EP3472153B1 (es) |
| JP (1) | JP7004459B2 (es) |
| KR (3) | KR102843750B1 (es) |
| CN (2) | CN109311857B (es) |
| AU (3) | AU2017286653B2 (es) |
| CL (1) | CL2018003597A1 (es) |
| CO (1) | CO2018013585A2 (es) |
| CR (2) | CR20220182A (es) |
| CU (1) | CU24605B1 (es) |
| CY (1) | CY1124789T1 (es) |
| DK (1) | DK3998261T3 (es) |
| DO (3) | DOP2018000285A (es) |
| EC (1) | ECSP18092481A (es) |
| ES (2) | ES3036953T3 (es) |
| HR (1) | HRP20211923T1 (es) |
| HU (1) | HUE056678T2 (es) |
| IL (3) | IL299412B2 (es) |
| JO (1) | JOP20180113B1 (es) |
| LT (1) | LT3472153T (es) |
| MD (1) | MD3472153T2 (es) |
| MX (3) | MX392230B (es) |
| PE (2) | PE20240221A1 (es) |
| PH (1) | PH12018502427A1 (es) |
| PL (1) | PL3472153T3 (es) |
| PT (1) | PT3472153T (es) |
| RS (1) | RS62868B1 (es) |
| SA (2) | SA521430638B1 (es) |
| SG (2) | SG10201912632YA (es) |
| SI (1) | SI3472153T1 (es) |
| SM (1) | SMT202100699T1 (es) |
| TN (1) | TN2018000422A1 (es) |
| TW (1) | TWI786049B (es) |
| UA (1) | UA126231C2 (es) |
| WO (1) | WO2017218843A1 (es) |
| ZA (1) | ZA201900229B (es) |
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| 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 |
| 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 |
| 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 |
| 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 |
| SG11202112464PA (en) * | 2019-05-31 | 2021-12-30 | Denali Therapeutics Inc | Modified release formulation of a pyrimidinylamino-pyrazole compound, and methods of treatment |
| EP3769768A1 (en) | 2019-07-23 | 2021-01-27 | Consejo Superior de Investigaciones Cientificas (CSIC) | Compounds useful for the treatment of parkinson s disease |
| TW202130643A (zh) * | 2019-10-29 | 2021-08-16 | 美商百健Ｍａ公司 | 螺環o-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃糖苷酶抑制劑 |
| 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 |
| KR102342803B1 (ko) | 2020-03-23 | 2021-12-24 | 환인제약 주식회사 | 신규한 피리미딘 유도체 및 이를 포함하는 신경퇴행성 질환 및 암의 예방 또는 치료용 조성물 |
| JP7500875B2 (ja) * | 2020-10-07 | 2024-06-17 | アルツプロテクト | 運動ニューロン疾患及び神経筋接合部障害の処置のためのｎ－（３－（４－（３－（ジイソブチルアミノ）プロピル）ピペラジン－１－イル）プロピル）－１ｈ－ベンゾ［ｄ］イミダゾール－２－アミン硫酸塩及びそれらの溶媒和物の使用 |
| AU2021371697B2 (en) * | 2020-10-29 | 2024-10-24 | Suzhou Yabao Pharmaceutical R&D Co., Ltd. | Substituted diarylamine compound, pharmaceutical composition thereof, preparation method therefor, and use thereof |
| AU2021371136A1 (en) | 2020-10-29 | 2023-05-11 | Merck Sharp & Dohme Llc | N-linked isoquinoline amides as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof |
| 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 |
| WO2023073013A1 (en) | 2021-10-27 | 2023-05-04 | H. Lundbeck A/S | Lrrk2 inhibitors |
| 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 |
| US11958865B1 (en) | 2022-09-15 | 2024-04-16 | H. Lundbeck A/S | Leucine-rich repeat kinase 2 (LRRK2) inhibitors |
| 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 |
| 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 |
| WO2024112746A1 (en) | 2022-11-22 | 2024-05-30 | Denali Therapeutics Inc. | Processes and intermediates for the preparation of a pyrimidine aminopyrazole compound |
| 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 |
| CN121226329A (zh) * | 2024-06-28 | 2025-12-30 | 成都康弘药业集团股份有限公司 | 一种治疗或预防lrrk2介导的疾病的化合物 |
| 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 |
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