JP2019521984A5 - - Google Patents
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- JP2019521984A5 JP2019521984A5 JP2018565694A JP2018565694A JP2019521984A5 JP 2019521984 A5 JP2019521984 A5 JP 2019521984A5 JP 2018565694 A JP2018565694 A JP 2018565694A JP 2018565694 A JP2018565694 A JP 2018565694A JP 2019521984 A5 JP2019521984 A5 JP 2019521984A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- pharmaceutically acceptable
- alkyl
- acceptable salt
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- -1 triazol-2-yl Chemical group 0.000 claims description 63
- 150000001875 compounds Chemical class 0.000 claims description 62
- 125000000217 alkyl group Chemical group 0.000 claims description 39
- 150000003839 salts Chemical class 0.000 claims description 31
- 125000005843 halogen group Chemical group 0.000 claims description 29
- 239000000203 mixture Substances 0.000 claims description 27
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 23
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- 239000001257 hydrogen Substances 0.000 claims description 21
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 18
- 125000003545 alkoxy group Chemical group 0.000 claims description 17
- 239000000651 prodrug Substances 0.000 claims description 17
- 229940002612 prodrug Drugs 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 16
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 201000011510 cancer Diseases 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 13
- 125000001072 heteroaryl group Chemical group 0.000 claims description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- 125000000623 heterocyclic group Chemical group 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 11
- 150000002431 hydrogen Chemical class 0.000 claims description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims description 9
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims description 9
- 208000027866 inflammatory disease Diseases 0.000 claims description 8
- 230000004770 neurodegeneration Effects 0.000 claims description 8
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 7
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 6
- 208000024827 Alzheimer disease Diseases 0.000 claims description 6
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims description 6
- 206010006187 Breast cancer Diseases 0.000 claims description 6
- 208000026310 Breast neoplasm Diseases 0.000 claims description 6
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 6
- 208000011231 Crohn disease Diseases 0.000 claims description 6
- 206010012289 Dementia Diseases 0.000 claims description 6
- 208000012661 Dyskinesia Diseases 0.000 claims description 6
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 6
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims description 6
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims description 6
- 206010024229 Leprosy Diseases 0.000 claims description 6
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 6
- 208000034578 Multiple myelomas Diseases 0.000 claims description 6
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 6
- 208000018737 Parkinson disease Diseases 0.000 claims description 6
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 6
- 206010060862 Prostate cancer Diseases 0.000 claims description 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 6
- 206010038389 Renal cancer Diseases 0.000 claims description 6
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 6
- 201000005787 hematologic cancer Diseases 0.000 claims description 6
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 6
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 6
- 201000010982 kidney cancer Diseases 0.000 claims description 6
- 201000005202 lung cancer Diseases 0.000 claims description 6
- 208000020816 lung neoplasm Diseases 0.000 claims description 6
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 6
- 125000005338 substituted cycloalkoxy group Chemical group 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 5
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 4
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 4
- 210000003169 central nervous system Anatomy 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 102000009784 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Human genes 0.000 claims description 3
- 108010020246 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Proteins 0.000 claims description 3
- 230000001149 cognitive effect Effects 0.000 claims description 3
- 230000001404 mediated effect Effects 0.000 claims description 3
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims description 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 2
- 125000002252 acyl group Chemical group 0.000 claims description 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 125000001246 bromo group Chemical group Br* 0.000 claims description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 2
- 208000015114 central nervous system disease Diseases 0.000 claims description 2
- 125000006317 cyclopropyl amino group Chemical group 0.000 claims description 2
- 229910052805 deuterium Inorganic materials 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- QKIUAMUSENSFQQ-UHFFFAOYSA-N dimethylazanide Chemical compound C[N-]C QKIUAMUSENSFQQ-UHFFFAOYSA-N 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 230000002757 inflammatory effect Effects 0.000 claims description 2
- 208000028774 intestinal disease Diseases 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000004674 methylcarbonyl group Chemical group CC(=O)* 0.000 claims description 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000004289 pyrazol-3-yl group Chemical group [H]N1N=C(*)C([H])=C1[H] 0.000 claims description 2
- 239000000126 substance Substances 0.000 claims description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 238000010276 construction Methods 0.000 claims 14
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical group CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 3
- 230000008878 coupling Effects 0.000 claims 3
- 238000010168 coupling process Methods 0.000 claims 3
- 238000005859 coupling reaction Methods 0.000 claims 3
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 claims 1
- 208000037902 enteropathy Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 description 2
- 125000000304 alkynyl group Chemical group 0.000 description 2
- UBBRRFLIYRTWNC-UHFFFAOYSA-N CCNc1nc(Nc(c(C2CC2)n2)c[n]2S=O)ncc1C(F)(F)F Chemical compound CCNc1nc(Nc(c(C2CC2)n2)c[n]2S=O)ncc1C(F)(F)F UBBRRFLIYRTWNC-UHFFFAOYSA-N 0.000 description 1
- 0 CCNc1nc(Nc2cc(C(C)(C)[n]3nccn3)n[n]2C(*)(*)*)ncc1Br Chemical compound CCNc1nc(Nc2cc(C(C)(C)[n]3nccn3)n[n]2C(*)(*)*)ncc1Br 0.000 description 1
- VQTCKJUIBCFTNY-UHFFFAOYSA-N CNc1nc(Nc2c[n](C(C3)C3N)nc2C2CC2)ncc1C(F)(F)F Chemical compound CNc1nc(Nc2c[n](C(C3)C3N)nc2C2CC2)ncc1C(F)(F)F VQTCKJUIBCFTNY-UHFFFAOYSA-N 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
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 true JP2019521984A5 (enExample) | 2020-07-30 |
| JP7004459B2 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 (36)
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
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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 |
| WO2026122425A1 (en) * | 2024-12-03 | 2026-06-11 | Neuro3 Therapeutics, Inc. | Substituted phenyl heteroaryl compounds |
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