JP7004459B2 - 神経変性疾患の治療に用いるｌｒｒｋ２阻害剤としてのピリミジン－２－イルアミノ－１ｈ－ピラゾール - Google Patents
神経変性疾患の治療に用いるｌｒｒｋ２阻害剤としてのピリミジン－２－イルアミノ－１ｈ－ピラゾール Download PDFInfo
- Publication number
- JP7004459B2 JP7004459B2 JP2018565694A JP2018565694A JP7004459B2 JP 7004459 B2 JP7004459 B2 JP 7004459B2 JP 2018565694 A JP2018565694 A JP 2018565694A JP 2018565694 A JP2018565694 A JP 2018565694A JP 7004459 B2 JP7004459 B2 JP 7004459B2
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- compound
- mixture
- disease
- 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
Links
- 0 *c1c(Nc2ncc(*)c(*)n2)[n](*)nc1* Chemical compound *c1c(Nc2ncc(*)c(*)n2)[n](*)nc1* 0.000 description 14
- MDELZHGRFDBKDV-QQSLQFIPSA-N CCNc1nc(N/C(/NC2CC2)=C/C([C@@H](C2)[C@@H]2C#N)=N)ncc1C(F)(F)F Chemical compound CCNc1nc(N/C(/NC2CC2)=C/C([C@@H](C2)[C@@H]2C#N)=N)ncc1C(F)(F)F MDELZHGRFDBKDV-QQSLQFIPSA-N 0.000 description 1
- LXRVHITUSDCRCT-UHFFFAOYSA-N CCNc1nc(Nc2cc(C(C)(CCO3)C3=O)n[n]2C2CC2)ncc1C(F)(F)F Chemical compound CCNc1nc(Nc2cc(C(C)(CCO3)C3=O)n[n]2C2CC2)ncc1C(F)(F)F LXRVHITUSDCRCT-UHFFFAOYSA-N 0.000 description 1
- OJRGUSSBPATGEO-UHFFFAOYSA-N CCNc1nc(Nc2cc(C)n[n]2C2CC2)ncc1C(F)(F)F Chemical compound CCNc1nc(Nc2cc(C)n[n]2C2CC2)ncc1C(F)(F)F OJRGUSSBPATGEO-UHFFFAOYSA-N 0.000 description 1
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
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- 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
- 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
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Immunology (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)
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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019521984A JP2019521984A (ja) | 2019-08-08 |
| JP2019521984A5 JP2019521984A5 (eng) | 2020-07-30 |
| JP7004459B2 true JP7004459B2 (ja) | 2022-02-10 |
Family
ID=59216078
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018565694A Active JP7004459B2 (ja) | 2016-06-16 | 2017-06-15 | 神経変性疾患の治療に用いるｌｒｒｋ２阻害剤としてのピリミジン－２－イルアミノ－１ｈ－ピラゾール |
Country Status (37)
| Country | Link |
|---|---|
| US (7) | US20170362206A1 (eng) |
| EP (3) | EP3472153B1 (eng) |
| JP (1) | JP7004459B2 (eng) |
| KR (3) | KR102705724B1 (eng) |
| CN (2) | CN114315819A (eng) |
| AU (3) | AU2017286653B2 (eng) |
| CA (1) | CA3025672A1 (eng) |
| CL (1) | CL2018003597A1 (eng) |
| CO (1) | CO2018013585A2 (eng) |
| CR (2) | CR20220182A (eng) |
| CU (1) | CU24605B1 (eng) |
| CY (1) | CY1124789T1 (eng) |
| DK (1) | DK3998261T3 (eng) |
| DO (3) | DOP2018000285A (eng) |
| EC (1) | ECSP18092481A (eng) |
| ES (2) | ES3036953T3 (eng) |
| HR (1) | HRP20211923T1 (eng) |
| HU (1) | HUE056678T2 (eng) |
| IL (3) | IL299415B2 (eng) |
| JO (1) | JOP20180113B1 (eng) |
| LT (1) | LT3472153T (eng) |
| MD (1) | MD3472153T2 (eng) |
| MX (3) | MX392230B (eng) |
| PE (2) | PE20240221A1 (eng) |
| PH (1) | PH12018502427A1 (eng) |
| PL (1) | PL3472153T3 (eng) |
| PT (1) | PT3472153T (eng) |
| RS (1) | RS62868B1 (eng) |
| SA (2) | SA518400660B1 (eng) |
| SG (2) | SG11201810579YA (eng) |
| SI (1) | SI3472153T1 (eng) |
| SM (1) | SMT202100699T1 (eng) |
| TN (1) | TN2018000422A1 (eng) |
| TW (1) | TWI786049B (eng) |
| UA (1) | UA126231C2 (eng) |
| WO (1) | WO2017218843A1 (eng) |
| ZA (1) | ZA201900229B (eng) |
Families Citing this family (27)
| 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 |
| CR20220182A (es) | 2016-06-16 | 2022-06-15 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos (divisional 2018-592) |
| CR20200216A (es) | 2017-11-21 | 2021-03-19 | Denali Therapeutics Inc | Polimorfos y formas sòlidas de un compuesto de pirimidinilamino-pirazol y mèdtodos de producciòn |
| 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 |
| TWI859242B (zh) * | 2019-05-31 | 2024-10-21 | 美商戴納立製藥公司 | 嘧啶基胺基-吡唑化合物之修飾釋放調配物及治療方法 |
| EP3769768A1 (en) | 2019-07-23 | 2021-01-27 | Consejo Superior de Investigaciones Cientificas (CSIC) | Compounds useful for the treatment of parkinson s disease |
| AR120324A1 (es) * | 2019-10-29 | 2022-02-09 | Biogen Ma Inc | Inhibidores de o-glucoproteína-2-acetamido-2-deoxi-3-d-glucopiranosidasa espirocíclica |
| US20240254103A9 (en) | 2020-03-23 | 2024-08-01 | Whan In Pharmaceutical Co., Ltd. | 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 |
| IL301633A (en) * | 2020-10-07 | 2023-05-01 | Alzprotect | Use of sulfate salts of N-(3-(4-(3-diisobutylamino)propyl)piperazin-1-yl)propyl-1H-benzo[D]imidazol-2-amine and their sulfates for the treatment of motor neuron diseases and neuromuscular junction diseases |
| MX2023005071A (es) | 2020-10-29 | 2023-05-16 | Merck Sharp & Dohme Llc | Amidas de isoquinolina enlazadas a n como inhibidores de lrrk2, composiciones farmaceuticas y usos de las mismas. |
| CA3197034A1 (en) * | 2020-10-29 | 2022-05-05 | Suzhou Yabao Pharmaceutical R&D Co., Ltd. | Substituted diarylamine compound, pharmaceutical composition thereof, preparation method therefor, and use thereof |
| TW202308635A (zh) * | 2021-04-30 | 2023-03-01 | 美商戴納立製藥公司 | 治療與監測帕金森氏病之方法 |
| TW202330549A (zh) | 2021-10-27 | 2023-08-01 | 丹麥商Ｈ 朗德貝克公司 | Lrrk2抑制劑 |
| MX2024007383A (es) | 2021-12-15 | 2024-08-28 | Whan In Pharmaceutical Co Ltd | Derivado de pirimidina macrocíclica, método para preparar el mismo y composición farmacéutica para prevención o tratamiento de una enfermedad neurodegenerativa que contiene el mismo como ingrediente activo. |
| 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 |
| WO2024097394A1 (en) | 2022-11-03 | 2024-05-10 | 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 |
| TW202434571A (zh) | 2022-11-22 | 2024-09-01 | 美商戴納立製藥公司 | 嘧啶胺基吡唑化合物之製備方法及中間物 |
| 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 |
| CN119968373A (zh) * | 2023-09-07 | 2025-05-09 | 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013545741A (ja) | 2010-11-10 | 2013-12-26 | エフ．ホフマン−ラ ロシュ アーゲー | Ｌｒｒｋ２調節薬としてのピラゾールアミノピリミジン誘導体 |
| JP2015515966A (ja) | 2012-05-03 | 2015-06-04 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｌｒｒｋ２モジュレ−タ−としてのピラゾ−ルアミノピリミジン誘導体 |
Family Cites Families (63)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1140862A4 (en) | 1998-12-23 | 2004-07-28 | Bristol Myers Squibb Pharma Co | THROMBIN OR Xa FACTOR INHIBITORS |
| AU2002339230A1 (en) | 2002-03-08 | 2003-09-22 | 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. |
| JP5208516B2 (ja) | 2004-12-30 | 2013-06-12 | エグゼリクシス， インコーポレイテッド | キナーゼモジュレーターとしてのピリミジン誘導体および使用方法 |
| 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 |
| MX2008016524A (es) | 2006-06-20 | 2009-03-09 | Novartis Ag | Biomarcadores para la progresion de la enfermedad de alzheimer. |
| US7947698B2 (en) | 2007-03-23 | 2011-05-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| EP2146969A1 (en) | 2007-04-19 | 2010-01-27 | Novartis Ag | Nicotinic acid derivatives as modulators of metabotropic glutamate receptor-5 |
| MX2009011810A (es) | 2007-05-02 | 2010-01-14 | Vertex Pharma | Tiazoles y pirazoles utiles como inhibidores de cinasa. |
| AU2008257044A1 (en) | 2007-05-24 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| 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 |
| NZ599041A (en) | 2009-11-13 | 2014-05-30 | Genosco | Kinase inhibitors |
| GB201008134D0 (en) | 2010-05-14 | 2010-06-30 | Medical Res Council Technology | Compounds |
| DK2576541T3 (en) | 2010-06-04 | 2016-05-30 | Hoffmann La Roche | Aminopyrimidine AS LRRK2 MODULATORS |
| US8637529B2 (en) | 2010-06-11 | 2014-01-28 | AbbYie Inc. | Pyrazolo[3,4-d]pyrimidine compounds |
| EP2632260A4 (en) | 2010-10-29 | 2015-06-17 | Merck Sharp & Dohme | LEUCINREICH REPEAT KINASE ENZYME ACTIVITY |
| EP2646819A1 (en) | 2010-11-30 | 2013-10-09 | Genentech, Inc. | Assays and biomarkers for lrrk2 |
| EP2720719A4 (en) | 2011-06-15 | 2015-12-09 | Glaxosmithkline Ip No 2 Ltd | METHOD FOR SELECTION OF THERAPEUTIC INDICATIONS |
| AU2012288892B2 (en) | 2011-07-28 | 2016-04-21 | Cellzome Limited | Heterocyclyl pyrimidine analogues as JAK inhibitors |
| EP2758402B9 (en) | 2011-09-22 | 2016-09-14 | Pfizer Inc | Pyrrolopyrimidine and purine derivatives |
| JP6117816B2 (ja) | 2011-11-29 | 2017-04-19 | 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 |
| 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 |
| ES2592802T3 (es) | 2011-11-29 | 2016-12-01 | F. Hoffmann-La Roche Ag | Derivados de 2-(fenil o pirid-3-il)aminopirimidina como moduladores de la quinasa LRRK2 para el tratamiento de la enfermedad de Parkinson |
| CN104093426B (zh) | 2011-11-30 | 2019-06-28 | 健泰科生物技术公司 | 用于lrrk2的正电子发射体层摄影(pet)成像的氟-18和碳-11标记的放射性配体 |
| WO2013126283A1 (en) | 2012-02-20 | 2013-08-29 | E. I. Du Pont De Nemours And Company | Fungicidal pyrazoles |
| ES2857649T3 (es) | 2012-03-01 | 2021-09-29 | Array Biopharma Inc | Inhibidores de serina/treonina cinasa |
| 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 |
| US9624180B2 (en) | 2013-01-25 | 2017-04-18 | 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 |
| ES2614872T3 (es) | 2013-03-05 | 2017-06-02 | Merck Patent Gmbh | Derivados de 9-(aril o heteroaril)-2-(pirazolilo, pirrolidinilo o ciclopentilo) aminopurina como agentes anticancer |
| JP6553589B2 (ja) | 2013-03-15 | 2019-07-31 | ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド | ピリミド−ジアゼピノン化合物および障害の治療方法 |
| 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 |
| WO2014181137A1 (en) | 2013-05-10 | 2014-11-13 | Karus Therapeutics Ltd | Novel histone deacetylase inhibitors |
| EA029774B1 (ru) | 2014-01-29 | 2018-05-31 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Соединения |
| AU2015222887B2 (en) | 2014-02-28 | 2019-06-27 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-b]indoles and related analogs as BET bromodomain inhibitors |
| WO2015148869A1 (en) | 2014-03-28 | 2015-10-01 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| US10266549B2 (en) | 2014-08-25 | 2019-04-23 | Salk Institute For Biological Studies | ULK1 inhibitors and methods using same |
| 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 |
| DK3227297T3 (da) | 2014-12-05 | 2021-04-06 | Array Biopharma Inc | 4,6-substitueret-pyrazolo[1,5-a]pyraziner som janus kinase-inhibitorer |
| US20180042234A1 (en) | 2015-03-19 | 2018-02-15 | 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 |
| 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 |
| WO2017087282A1 (en) | 2015-11-18 | 2017-05-26 | 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 |
| CN108934162A (zh) | 2015-12-16 | 2018-12-04 | 南方研究所 | 吡咯并嘧啶化合物、作为激酶lrrk2抑制剂的用途及其制备方法 |
| TWI836679B (zh) * | 2016-02-05 | 2024-03-21 | 美商戴納立製藥公司 | 化合物、組合物及方法 |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| CR20220182A (es) * | 2016-06-16 | 2022-06-15 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos (divisional 2018-592) |
| WO2018217946A1 (en) | 2017-05-24 | 2018-11-29 | Denali Therapeutics Inc. | Compounds, compositions and methods |
-
2017
- 2017-06-15 CR CR20220182A patent/CR20220182A/es unknown
- 2017-06-15 SG SG11201810579YA patent/SG11201810579YA/en unknown
- 2017-06-15 HR HRP20211923TT patent/HRP20211923T1/hr unknown
- 2017-06-15 EP EP17733306.9A patent/EP3472153B1/en active Active
- 2017-06-15 IL IL299415A patent/IL299415B2/en unknown
- 2017-06-15 EP EP21198102.2A patent/EP3998261B1/en active Active
- 2017-06-15 CN CN202111282850.1A patent/CN114315819A/zh active Pending
- 2017-06-15 HU HUE17733306A patent/HUE056678T2/hu unknown
- 2017-06-15 UA UAA201812165A patent/UA126231C2/uk unknown
- 2017-06-15 ES ES21198102T patent/ES3036953T3/es active Active
- 2017-06-15 PE PE2023001478A patent/PE20240221A1/es unknown
- 2017-06-15 MX MX2018015630A patent/MX392230B/es unknown
- 2017-06-15 IL IL263484A patent/IL263484B2/en unknown
- 2017-06-15 CN CN201780036925.3A patent/CN109311857B/zh active Active
- 2017-06-15 WO PCT/US2017/037782 patent/WO2017218843A1/en not_active Ceased
- 2017-06-15 EP EP25174508.9A patent/EP4635570A3/en active Pending
- 2017-06-15 RS RS20211513A patent/RS62868B1/sr unknown
- 2017-06-15 MD MDE20190504T patent/MD3472153T2/ro unknown
- 2017-06-15 PL PL17733306T patent/PL3472153T3/pl unknown
- 2017-06-15 TN TNP/2018/000422A patent/TN2018000422A1/en unknown
- 2017-06-15 AU AU2017286653A patent/AU2017286653B2/en active Active
- 2017-06-15 JO JOP/2018/0113A patent/JOP20180113B1/ar active
- 2017-06-15 SI SI201731005T patent/SI3472153T1/sl unknown
- 2017-06-15 DK DK21198102.2T patent/DK3998261T3/da active
- 2017-06-15 CU CU2018000152A patent/CU24605B1/es unknown
- 2017-06-15 PE PE2018003221A patent/PE20190395A1/es unknown
- 2017-06-15 PT PT177333069T patent/PT3472153T/pt unknown
- 2017-06-15 ES ES17733306T patent/ES2900368T3/es active Active
- 2017-06-15 CA CA3025672A patent/CA3025672A1/en active Pending
- 2017-06-15 IL IL299412A patent/IL299412B2/en unknown
- 2017-06-15 KR KR1020237022665A patent/KR102705724B1/ko active Active
- 2017-06-15 KR KR1020197000749A patent/KR102553188B1/ko active Active
- 2017-06-15 LT LTEPPCT/US2017/037782T patent/LT3472153T/lt unknown
- 2017-06-15 CR CR20180592A patent/CR20180592A/es unknown
- 2017-06-15 JP JP2018565694A patent/JP7004459B2/ja active Active
- 2017-06-15 US US15/624,566 patent/US20170362206A1/en not_active Abandoned
- 2017-06-15 SG SG10201912632YA patent/SG10201912632YA/en unknown
- 2017-06-15 KR KR1020247029993A patent/KR102843750B1/ko active Active
- 2017-06-15 SM SM20210699T patent/SMT202100699T1/it unknown
- 2017-06-16 TW TW106120263A patent/TWI786049B/zh active
- 2017-10-25 US US15/793,882 patent/US9932325B2/en active Active
-
2018
- 2018-03-21 US US15/927,920 patent/US10590114B2/en active Active
- 2018-11-19 PH PH12018502427A patent/PH12018502427A1/en unknown
- 2018-12-13 MX MX2022005610A patent/MX2022005610A/es unknown
- 2018-12-13 DO DO2018000285A patent/DOP2018000285A/es unknown
- 2018-12-13 MX MX2021010304A patent/MX2021010304A/es unknown
- 2018-12-13 SA SA518400660A patent/SA518400660B1/ar unknown
- 2018-12-13 SA SA521430638A patent/SA521430638B1/ar unknown
- 2018-12-14 EC ECSENADI201892481A patent/ECSP18092481A/es unknown
- 2018-12-14 CL CL2018003597A patent/CL2018003597A1/es unknown
- 2018-12-14 CO CONC2018/0013585A patent/CO2018013585A2/es unknown
-
2019
- 2019-01-14 ZA ZA2019/00229A patent/ZA201900229B/en unknown
-
2020
- 2020-03-13 US US16/818,745 patent/US11111235B2/en active Active
-
2021
- 2021-08-13 US US17/401,833 patent/US11591316B2/en active Active
- 2021-12-14 CY CY20211101098T patent/CY1124789T1/el unknown
-
2022
- 2022-04-08 AU AU2022202372A patent/AU2022202372B2/en active Active
- 2022-04-25 DO DO2022000088A patent/DOP2022000088A/es unknown
-
2023
- 2023-01-19 US US18/099,082 patent/US11834439B2/en active Active
- 2023-04-17 DO DO2023000077A patent/DOP2023000077A/es unknown
-
2024
- 2024-06-14 US US18/744,133 patent/US20250034119A1/en active Pending
- 2024-07-03 AU AU2024204621A patent/AU2024204621A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013545741A (ja) | 2010-11-10 | 2013-12-26 | エフ．ホフマン−ラ ロシュ アーゲー | Ｌｒｒｋ２調節薬としてのピラゾールアミノピリミジン誘導体 |
| JP2015515966A (ja) | 2012-05-03 | 2015-06-04 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｌｒｒｋ２モジュレ−タ−としてのピラゾ−ルアミノピリミジン誘導体 |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7004459B2 (ja) | 神経変性疾患の治療に用いるｌｒｒｋ２阻害剤としてのピリミジン－２－イルアミノ－１ｈ－ピラゾール | |
| HK40074923A (en) | Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders | |
| HK40074923B (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 | |
| HK1260987A1 (en) | Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders | |
| HK1260987B (zh) | 作为用於治疗神经退化性病症的lrrk2抑制剂的嘧啶-2-基氨基-1h-吡唑 | |
| OA19864A (en) | Compounds, compositions, and methods. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20200615 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20200615 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20210423 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20210428 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20210721 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20210922 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20211022 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20211210 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20211229 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 7004459 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |