DK3194405T3 - MACROCYCLIC LRRK2 KINase INHIBITORS - Google Patents
MACROCYCLIC LRRK2 KINase INHIBITORS Download PDFInfo
- Publication number
- DK3194405T3 DK3194405T3 DK15766801.3T DK15766801T DK3194405T3 DK 3194405 T3 DK3194405 T3 DK 3194405T3 DK 15766801 T DK15766801 T DK 15766801T DK 3194405 T3 DK3194405 T3 DK 3194405T3
- Authority
- DK
- Denmark
- Prior art keywords
- alkyl
- halo
- optionally
- 6alkyl
- independently substituted
- Prior art date
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- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- WRIKHQLVHPKCJU-UHFFFAOYSA-N sodium bis(trimethylsilyl)amide Chemical compound C[Si](C)(C)N([Na])[Si](C)(C)C WRIKHQLVHPKCJU-UHFFFAOYSA-N 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 239000012058 sterile packaged powder Substances 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 239000002600 sunflower oil Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- NSILYQWHARROMG-QMMMGPOBSA-N tert-butyl (3s)-3-(hydroxymethyl)piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCN[C@H](CO)C1 NSILYQWHARROMG-QMMMGPOBSA-N 0.000 description 1
- AKQXKEBCONUWCL-QMMMGPOBSA-N tert-butyl (3s)-3-aminopiperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC[C@H](N)C1 AKQXKEBCONUWCL-QMMMGPOBSA-N 0.000 description 1
- PNJXYVJNOCLJLJ-QMMMGPOBSA-N tert-butyl (4r)-4-formyl-2,2-dimethyl-1,3-oxazolidine-3-carboxylate Chemical compound CC(C)(C)OC(=O)N1[C@@H](C=O)COC1(C)C PNJXYVJNOCLJLJ-QMMMGPOBSA-N 0.000 description 1
- VCYKQOGWPICUKV-UHFFFAOYSA-N tert-butyl 2-(2-aminoethyl)pyrrolidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCCC1CCN VCYKQOGWPICUKV-UHFFFAOYSA-N 0.000 description 1
- PWQLFIKTGRINFF-UHFFFAOYSA-N tert-butyl 4-hydroxypiperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC(O)CC1 PWQLFIKTGRINFF-UHFFFAOYSA-N 0.000 description 1
- ACNRTYKOPZDRCO-UHFFFAOYSA-N tert-butyl n-(2-oxoethyl)carbamate Chemical compound CC(C)(C)OC(=O)NCC=O ACNRTYKOPZDRCO-UHFFFAOYSA-N 0.000 description 1
- MHYGQXWCZAYSLJ-UHFFFAOYSA-N tert-butyl-chloro-diphenylsilane Chemical compound C=1C=CC=CC=1[Si](Cl)(C(C)(C)C)C1=CC=CC=C1 MHYGQXWCZAYSLJ-UHFFFAOYSA-N 0.000 description 1
- 125000006092 tetrahydro-1,1-dioxothienyl group Chemical group 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000005307 thiatriazolyl group Chemical group S1N=NN=C1* 0.000 description 1
- 125000004305 thiazinyl group Chemical group S1NC(=CC=C1)* 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000002053 thietanyl group Chemical group 0.000 description 1
- WCNFFKHKJLERFM-UHFFFAOYSA-N thiomorpholinyl sulfone group Chemical group N1(CCSCC1)S(=O)(=O)N1CCSCC1 WCNFFKHKJLERFM-UHFFFAOYSA-N 0.000 description 1
- ZCAGUOCUDGWENZ-UHFFFAOYSA-N thiomorpholinyl sulfoxide group Chemical group N1(CCSCC1)S(=O)N1CCSCC1 ZCAGUOCUDGWENZ-UHFFFAOYSA-N 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000003354 tissue distribution assay Methods 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 238000011830 transgenic mouse model Methods 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- 125000005500 uronium group Chemical group 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 description 1
Classifications
-
- 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
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D487/22—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 four or more hetero rings
-
- 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
- C07D498/22—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 four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14290279 | 2014-09-17 | ||
| PCT/EP2015/071349 WO2016042089A1 (en) | 2014-09-17 | 2015-09-17 | Macrocyclic lrrk2 kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3194405T3 true DK3194405T3 (en) | 2019-04-15 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK15766801.3T DK3194405T3 (en) | 2014-09-17 | 2015-09-17 | MACROCYCLIC LRRK2 KINase INHIBITORS |
Country Status (20)
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111221514B (zh) * | 2020-01-13 | 2023-03-03 | 陕西心像信息科技有限公司 | 基于OsgEarth的三维可视化组件实现方法及系统 |
| CN115698020B (zh) * | 2020-01-31 | 2025-02-25 | 昂科迪塞恩精密医药公司(Opm) | 大环rip2-激酶抑制剂 |
| CN115996932B (zh) | 2020-05-06 | 2025-08-01 | 法国施维雅药厂 | 新的大环lrrk2激酶抑制剂 |
| IL305877A (en) | 2021-03-18 | 2023-11-01 | Servier Lab | Macrocyclic LRRK2 kinase inhibitors |
| WO2023064768A1 (en) * | 2021-10-11 | 2023-04-20 | Baylor College Of Medicine | G-protein-coupled receptor regulators and methods of use thereof |
| EP4422750A1 (en) | 2021-10-27 | 2024-09-04 | H. Lundbeck A/S | Lrrk2 inhibitors |
| WO2023222005A1 (zh) * | 2022-05-18 | 2023-11-23 | 上海翊石医药科技有限公司 | 一种芳杂环类化合物及其中间体、药物组合物和用途 |
| WO2024056775A1 (en) * | 2022-09-15 | 2024-03-21 | H. Lundbeck A/S | Macrocyclic leucine-rich repeat kinase 2 (lrrk2) inhibitors |
| WO2024218296A1 (en) * | 2023-04-20 | 2024-10-24 | H. Lundbeck A/S | Combination treatments comprising administration of leucine-rich repeat kinase 2 (lrrk2) inhibitors |
| AR132488A1 (es) * | 2023-04-20 | 2025-07-02 | H Lundbeck As | Inhibidores de la cinasa con repeticiones ricas en leucina 2 (lrrk2) |
| TW202442235A (zh) * | 2023-04-20 | 2024-11-01 | 丹麥商Ｈ 朗德貝克公司 | 富白胺酸重複激酶2（lrrk2）抑制劑 |
| AR132486A1 (es) * | 2023-04-20 | 2025-07-02 | H Lundbeck As | Inhibidores de la cinasa con repeticiones ricas en leucina 2 (lrrk2) |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
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| IS2334B (is) | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
| CZ289214B6 (cs) | 1993-10-01 | 2001-12-12 | Astra Aktiebolag | Způsob zpracování jemně děleného práąkového léčiva, zařízení k provádění tohoto způsobu a aglomeráty vyrobené tímto způsobem |
| EP0729758A3 (en) | 1995-03-02 | 1997-10-29 | Pfizer | Pyrazolopyrimidines and pyrrolopyrimidines for the treatment of neuronal and other diseases |
| US6043358A (en) | 1995-11-01 | 2000-03-28 | Merck & Co., Inc. | Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases |
| DK0915880T3 (da) | 1996-07-24 | 2008-02-11 | Bristol Myers Squibb Pharma Co | Azolotriaziner og pyrimidiner |
| GB9718913D0 (en) | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
| US6194410B1 (en) | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| US6369087B1 (en) | 1999-08-26 | 2002-04-09 | Robert R. Whittle | Alkoxy substituted benzimidazole compounds, pharmaceutical preparations containing the same, and methods of using the same |
| KR100843281B1 (ko) | 2000-12-28 | 2008-07-09 | 오노 야꾸힝 고교 가부시키가이샤 | 삼환식 복소환 유도체 화합물 및 그 화합물을 유효성분으로 하는 의약 |
| WO2002100399A1 (en) * | 2001-06-12 | 2002-12-19 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| EP2316927B1 (en) | 2004-10-21 | 2014-11-05 | Helmholtz Zentrum München Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH) | Kaspp (lrrk2) gene, its production and use for the detection and treatment of neurodegenerative disorders |
| NO323175B1 (no) | 2004-12-23 | 2007-01-15 | Jan O Aasly | Framgangsmate for a pavise en mutasjon som forarsaker arvelig parkinsonisme |
| FI123725B (fi) | 2005-08-01 | 2013-10-15 | Reijo Viljanen | Menetelmä sahalaitteen terän jännittämiseksi ja ohjaamiseksi sekä ohjaus- ja jännityslaitteet |
| US8143255B2 (en) | 2005-11-16 | 2012-03-27 | S*Bio Pte Ltd. | Heteroalkyl linked pyrimidine derivatives |
| WO2009127642A2 (en) | 2008-04-15 | 2009-10-22 | Cellzome Limited | Use of lrrk2 inhibitors for neurodegenerative diseases |
| BR112012006859A2 (pt) | 2009-09-29 | 2019-09-24 | Glaxo Group Ltd | compostos |
| PT3205654T (pt) * | 2010-05-20 | 2019-04-22 | Array Biopharma Inc | Compostos macrocíclicos como inibidores de cinases trk |
| WO2013001310A1 (en) * | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
| AU2012314035B2 (en) * | 2011-09-30 | 2016-12-15 | Oncodesign S.A. | Macrocyclic LRRK2 kinase inhibitors |
| US9090630B2 (en) * | 2011-09-30 | 2015-07-28 | Oncodesign S.A. | Macrocyclic FLT3 kinase inhibitors |
-
2015
- 2015-09-17 EP EP15766801.3A patent/EP3194405B1/en not_active Not-in-force
- 2015-09-17 DK DK15766801.3T patent/DK3194405T3/en active
- 2015-09-17 PL PL15766801T patent/PL3194405T3/pl unknown
- 2015-09-17 CN CN201580061216.1A patent/CN107108641A/zh active Pending
- 2015-09-17 TW TW104130753A patent/TW201625639A/zh unknown
- 2015-09-17 EA EA201790626A patent/EA032838B1/ru not_active IP Right Cessation
- 2015-09-17 JP JP2017515823A patent/JP2017529365A/ja active Pending
- 2015-09-17 BR BR112017005299A patent/BR112017005299A2/pt not_active IP Right Cessation
- 2015-09-17 KR KR1020177010322A patent/KR20170048599A/ko not_active Withdrawn
- 2015-09-17 HU HUE15766801A patent/HUE043972T2/hu unknown
- 2015-09-17 ES ES15766801T patent/ES2717510T3/es active Active
- 2015-09-17 SG SG11201701936WA patent/SG11201701936WA/en unknown
- 2015-09-17 CA CA2960777A patent/CA2960777A1/en not_active Abandoned
- 2015-09-17 WO PCT/EP2015/071349 patent/WO2016042089A1/en not_active Ceased
- 2015-09-17 MX MX2017003470A patent/MX2017003470A/es unknown
- 2015-09-17 US US15/511,879 patent/US10377772B2/en not_active Expired - Fee Related
- 2015-09-17 TR TR2019/04514T patent/TR201904514T4/tr unknown
- 2015-09-17 AU AU2015316801A patent/AU2015316801B2/en not_active Ceased
-
2017
- 2017-03-09 IL IL251054A patent/IL251054B/en not_active IP Right Cessation
- 2017-03-15 ZA ZA2017/01841A patent/ZA201701841B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20170240565A1 (en) | 2017-08-24 |
| IL251054B (en) | 2019-03-31 |
| KR20170048599A (ko) | 2017-05-08 |
| AU2015316801A1 (en) | 2017-04-27 |
| CA2960777A1 (en) | 2016-03-24 |
| EP3194405B1 (en) | 2018-12-26 |
| TW201625639A (zh) | 2016-07-16 |
| IL251054A0 (en) | 2017-04-30 |
| PL3194405T4 (pl) | 2019-07-31 |
| JP2017529365A (ja) | 2017-10-05 |
| EA032838B1 (ru) | 2019-07-31 |
| US10377772B2 (en) | 2019-08-13 |
| MX2017003470A (es) | 2017-08-07 |
| ES2717510T3 (es) | 2019-06-21 |
| ZA201701841B (en) | 2019-08-28 |
| EA201790626A1 (ru) | 2017-07-31 |
| SG11201701936WA (en) | 2017-04-27 |
| WO2016042089A1 (en) | 2016-03-24 |
| CN107108641A (zh) | 2017-08-29 |
| BR112017005299A2 (pt) | 2017-12-12 |
| PL3194405T3 (pl) | 2019-07-31 |
| TR201904514T4 (tr) | 2019-04-22 |
| AU2015316801B2 (en) | 2019-03-07 |
| EP3194405A1 (en) | 2017-07-26 |
| HUE043972T2 (hu) | 2019-09-30 |
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