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 (https=) | 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 (37)
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| MD3472153T2 (ro) | 2016-06-16 | 2022-03-31 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1H-pirazoli în calitate de inhibitori L RRK2 pentru utilizare în tratamentul tulburărilor neurodegenerative |
| MA51222A (fr) | 2017-11-21 | 2020-10-07 | Denali Therapeutics Inc | Polymorphes et formes solides d'un composé de pyrimidinylamino-pyrazole, et procédés de production |
| MX2020006641A (es) * | 2017-12-20 | 2021-01-08 | Denali Therapeutics Inc | Proceso para la preparacion de compuestos de pirimidinil-4-aminopi razol. |
| 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 |
| US12565504B2 (en) * | 2019-10-29 | 2026-03-03 | Biogen Ma Inc. | Spirocyclic O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors |
| BR112022018477A2 (pt) | 2020-03-23 | 2022-11-01 | Whan In Pharmaceutical Co Ltd | Composto derivado de pirimidina, composição compreendendo o mesmo, e seus usos na prevenção ou tratamento de doenças neurodegenerativas e câncer |
| KR102342803B1 (ko) | 2020-03-23 | 2021-12-24 | 환인제약 주식회사 | 신규한 피리미딘 유도체 및 이를 포함하는 신경퇴행성 질환 및 암의 예방 또는 치료용 조성물 |
| US20230364076A1 (en) * | 2020-10-07 | 2023-11-16 | 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 |
| EP4236950A4 (en) | 2020-10-29 | 2024-10-23 | Merck Sharp & Dohme LLC | N-LINKED ISOQUINOLINE AMIDES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF |
| CN114426542B (zh) * | 2020-10-29 | 2023-06-30 | 苏州亚宝药物研发有限公司 | 取代的二芳基胺化合物及其药物组合物、制备方法和用途 |
| US20240207266A1 (en) * | 2021-04-30 | 2024-06-27 | Denali Therapeutics Inc. | Methods for treating and monitoring parkinson's disease |
| JP2024541934A (ja) | 2021-10-27 | 2024-11-13 | ハー・ルンドベック・アクチエゼルスカベット | Ｌｒｒｋ２阻害剤 |
| CA3250447A1 (en) | 2021-12-15 | 2025-07-09 | Whan In Pharmaceutical Co., Ltd. | MACROCYCLIC PYRIMIDINE DERIVATIVE, ITS PREPARATION PROCESS, AND PHARMACEUTICAL COMPOSITION INTENDED FOR THE PREVENTION OR TREATMENT OF A NEURODEGENERATIVE DISEASE AND CONTAINING THIS DERIVATIVE AS AN ACTIVE INGREDIENT |
| CN117624185B (zh) * | 2022-08-23 | 2025-12-05 | 长春金赛药业有限责任公司 | Lrrk2抑制剂化合物、药物组合物及其制备方法和应用 |
| AR130483A1 (es) | 2022-09-15 | 2024-12-11 | H Lundbeck As | Inhibidores de la cinasa con repeticiones ricas en leucina 2 (lrrk2) |
| JP2026504627A (ja) | 2022-11-03 | 2026-02-06 | デナリ セラピューティクス インコーポレイテッド | ピリミジントリアゾール化合物の固体及び共結晶形態 |
| 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 |
| AU2023385721A1 (en) | 2022-11-22 | 2025-05-22 | 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 |
| WO2026002197A1 (zh) * | 2024-06-28 | 2026-01-02 | 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 |
Family Cites Families (65)
| 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 |
| AU2002339230A1 (en) | 2002-03-08 | 2003-09-22 | Decode Genetics Ehf. | A susceptibility gene for late-onset idiopathic parkinson's disease |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| US7202257B2 (en) | 2003-12-24 | 2007-04-10 | 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. |
| AU2005322855B2 (en) | 2004-12-30 | 2012-09-20 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| EP1746096A1 (en) | 2005-07-15 | 2007-01-24 | 4Sc Ag | 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer |
| US20090247554A1 (en) | 2006-03-30 | 2009-10-01 | Takeda San Diego, Inc. | Kinase inhibitors |
| US20100035251A1 (en) | 2006-06-20 | 2010-02-11 | Yunsheng He | BioMarkers for the Progression of Alzheimer's Disease |
| US7947698B2 (en) | 2007-03-23 | 2011-05-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| MX2009011208A (es) | 2007-04-19 | 2009-10-30 | Novartis Ag | Derivados de acido nicotinico como moduladores del receptor de glutamato metabotropico-5. |
| AU2008247592A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| MX2009012719A (es) | 2007-05-24 | 2010-02-04 | Vertex Pharma | Tiazoles y pirazoles utiles como inhibidores de cinasa. |
| 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 |
| MX2012005332A (es) | 2009-11-13 | 2012-10-15 | Oscotec Inc | Inhibidores de cinasa. |
| GB201008134D0 (en) | 2010-05-14 | 2010-06-30 | Medical Res Council Technology | Compounds |
| PT2576541T (pt) | 2010-06-04 | 2016-07-08 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| US8637529B2 (en) | 2010-06-11 | 2014-01-28 | AbbYie Inc. | Pyrazolo[3,4-d]pyrimidine compounds |
| US9233977B2 (en) | 2010-10-29 | 2016-01-12 | Merck Sharp & Dohme Corp. | Leucine-rich repeat kinase enzyme activity |
| HRP20172006T1 (hr) * | 2010-11-10 | 2018-02-09 | Genentech, Inc. | Derivati pirazol-aminopiridina kao lrrk2-modulatori |
| CN103348243A (zh) | 2010-11-30 | 2013-10-09 | 基因泰克公司 | Lrrk2的分析方法和生物标记物 |
| US20140170157A1 (en) | 2011-06-15 | 2014-06-19 | Glaxosmithkline Intellectual Property (No.2) Limited | Method of selecting therapeutic indications |
| CN103781780B (zh) | 2011-07-28 | 2015-11-25 | 赛尔佐姆有限公司 | 作为jak抑制剂的杂环基嘧啶类似物 |
| KR20140059246A (ko) | 2011-09-22 | 2014-05-15 | 화이자 인코포레이티드 | 피롤로피리미딘 및 퓨린 유도체 |
| BR112014009717B1 (pt) | 2011-11-29 | 2022-06-14 | Genentech, Inc | Derivados de 2-(fenil ou pirid-3-il)aminopirimidina, seus usos, e composição farmacêutica |
| CN103958498B (zh) | 2011-11-29 | 2016-09-07 | 霍夫曼-拉罗奇有限公司 | 作为lrrk2调节剂的氨基嘧啶衍生物 |
| AR089182A1 (es) | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| CN103958482B (zh) | 2011-11-29 | 2017-06-09 | 健泰科生物技术公司 | 作为lrrk2调节剂的氨基嘧啶衍生物 |
| EP2785381B1 (en) | 2011-11-30 | 2016-05-18 | F.Hoffmann-La Roche Ag | Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (pet) imaging for lrrk2 |
| WO2013126283A1 (en) | 2012-02-20 | 2013-08-29 | E. I. Du Pont De Nemours And Company | Fungicidal pyrazoles |
| HUE053994T2 (hu) | 2012-03-01 | 2021-08-30 | Array Biopharma Inc | Szerin/treonin kináz inhibitorok |
| CN106279202A (zh) * | 2012-05-03 | 2017-01-04 | 霍夫曼-拉罗奇有限公司 | 作为lrrk2调节剂用于治疗帕金森病的吡唑氨基嘧啶衍生物 |
| RU2637947C2 (ru) * | 2012-05-03 | 2017-12-08 | Дженентек, Инк. | Производные пиразоламинопиримидина в качестве модуляторов обогащенной лейциновыми повторами киназы 2 |
| EP2948434B1 (en) | 2013-01-25 | 2017-03-01 | 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 |
| AU2014224976B2 (en) | 2013-03-05 | 2017-09-28 | Merck Patent Gmbh | 9-(aryl or heteroaryl)-2-(pyrazolyl, pyrrolidinyl or cyclopentyl)aminopurine derivatives as anticancer agents |
| EP2968995B1 (en) | 2013-03-15 | 2018-05-09 | Elan Pharmaceuticals LLC | Inhibitors of lrrk2 kinase activity |
| WO2014145909A2 (en) | 2013-03-15 | 2014-09-18 | 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 |
| NZ714283A (en) | 2013-05-10 | 2020-04-24 | Karus Therapeutics Ltd | Novel histone deacetylase inhibitors |
| KR20160106622A (ko) | 2014-01-29 | 2016-09-12 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | 화합물 |
| US9580430B2 (en) | 2014-02-28 | 2017-02-28 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors |
| MX2016012574A (es) | 2014-03-28 | 2017-09-26 | Calitor Sciences Llc | Compuestos heteroarilo sustituidos y metodos de uso. |
| DK3185868T3 (da) | 2014-08-25 | 2022-05-23 | Salk Inst For Biological Studi | Hidtil ukendte ULK1-inhibitorer og fremgangsmåder til anvendelse af samme |
| 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 |
| HUE054371T2 (hu) | 2014-12-05 | 2021-09-28 | Array Biopharma Inc | 4,6-szubsztituált pirazolo[l,5-A]pirazinok mint janus kináz inhibitorok |
| CA2978066A1 (en) | 2015-03-19 | 2016-09-22 | E I Du Pont De Nemours And Company | Fungicidal pyrazoles |
| JP2018135268A (ja) | 2015-06-05 | 2018-08-30 | 大日本住友製薬株式会社 | 新規ヘテロアリールアミノ−３−ピラゾール誘導体およびその薬理学上許容される塩 |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| KR102161364B1 (ko) | 2015-09-14 | 2020-09-29 | 화이자 인코포레이티드 | LRRK2 억제제로서 이미다조[4,5-c]퀴놀린 및 이미다조[4,5-c][1,5]나프티리딘 유도체 |
| US9840710B2 (en) | 2015-11-18 | 2017-12-12 | Rosalind Franklin University Of Medicine And Science | Antisense compounds targeting leucine-rich repeat kinase 2 (LRRK2) for the treatment of parkinsons disease |
| US11214565B2 (en) | 2015-11-20 | 2022-01-04 | Denali Therapeutics Inc. | Compound, compositions, and methods |
| TW201720828A (zh) | 2015-11-23 | 2017-06-16 | 赫孚孟拉羅股份公司 | 治療性化合物及組合物以及其使用方法 |
| WO2017100703A1 (en) | 2015-12-10 | 2017-06-15 | Colin Combs | Ems analogues of lyn/src-tyrosine kinase inhibitors |
| JP2018537502A (ja) | 2015-12-16 | 2018-12-20 | サウザーン リサーチ インスチチュート | ピロロピリミジン化合物、キナーゼｌｒｒｋ２阻害剤としての使用、及びその調製方法 |
| MA44007A (fr) * | 2016-02-05 | 2018-12-19 | Denali Therapeutics Inc | Inhibiteurs du récepteur interagissant avec protéine kinase 1 |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| MD3472153T2 (ro) * | 2016-06-16 | 2022-03-31 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1H-pirazoli în calitate de inhibitori L RRK2 pentru utilizare în tratamentul tulburărilor neurodegenerative |
| WO2018217946A1 (en) | 2017-05-24 | 2018-11-29 | Denali Therapeutics Inc. | Compounds, compositions and methods |
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