CN107108641A - 大环lrrk2激酶抑制剂 - Google Patents
大环lrrk2激酶抑制剂 Download PDFInfo
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- CN107108641A CN107108641A CN201580061216.1A CN201580061216A CN107108641A CN 107108641 A CN107108641 A CN 107108641A CN 201580061216 A CN201580061216 A CN 201580061216A CN 107108641 A CN107108641 A CN 107108641A
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- 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
- 125000001981 tert-butyldimethylsilyl group Chemical group [H]C([H])([H])[Si]([H])(C([H])([H])[H])[*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000006092 tetrahydro-1,1-dioxothienyl group Chemical group 0.000 description 1
- 125000005958 tetrahydrothienyl group Chemical group 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 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
- 125000004588 thienopyridyl group Chemical group S1C(=CC2=C1C=CC=N2)* 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000002053 thietanyl group Chemical group 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
- 238000011200 topical administration Methods 0.000 description 1
- 230000000699 topical effect Effects 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
- 229930195735 unsaturated hydrocarbon Natural products 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 229920003169 water-soluble polymer Polymers 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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14290279 | 2014-09-17 | ||
| EP14290279.0 | 2014-09-17 | ||
| PCT/EP2015/071349 WO2016042089A1 (en) | 2014-09-17 | 2015-09-17 | Macrocyclic lrrk2 kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107108641A true CN107108641A (zh) | 2017-08-29 |
Family
ID=51752058
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580061216.1A Pending CN107108641A (zh) | 2014-09-17 | 2015-09-17 | 大环lrrk2激酶抑制剂 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US10377772B2 (https=) |
| EP (1) | EP3194405B1 (https=) |
| JP (1) | JP2017529365A (https=) |
| KR (1) | KR20170048599A (https=) |
| CN (1) | CN107108641A (https=) |
| AU (1) | AU2015316801B2 (https=) |
| BR (1) | BR112017005299A2 (https=) |
| CA (1) | CA2960777A1 (https=) |
| DK (1) | DK3194405T3 (https=) |
| EA (1) | EA032838B1 (https=) |
| ES (1) | ES2717510T3 (https=) |
| HU (1) | HUE043972T2 (https=) |
| IL (1) | IL251054B (https=) |
| MX (1) | MX2017003470A (https=) |
| PL (1) | PL3194405T4 (https=) |
| SG (1) | SG11201701936WA (https=) |
| TR (1) | TR201904514T4 (https=) |
| TW (1) | TW201625639A (https=) |
| WO (1) | WO2016042089A1 (https=) |
| ZA (1) | ZA201701841B (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Families Citing this family (11)
| 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 |
| UA129879C2 (uk) * | 2020-01-31 | 2025-08-27 | Онкодизайн Пресіжн Медісін (Опм) | Макроциклічні інгібітори rip2-кінази |
| CA3182162A1 (en) | 2020-05-06 | 2021-11-11 | Les Laboratoires Servier | New macrocyclic lrrk2 kinase inhibitors |
| TW202304935A (zh) | 2021-03-18 | 2023-02-01 | 法商施維雅藥廠 | 新穎的巨環lrrk2激酶抑制劑 |
| EP4416133A1 (en) * | 2021-10-11 | 2024-08-21 | Baylor College of Medicine | G-protein-coupled receptor regulators and methods of use thereof |
| 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 |
| AR130483A1 (es) | 2022-09-15 | 2024-12-11 | H Lundbeck As | Inhibidores de la cinasa con repeticiones ricas en leucina 2 (lrrk2) |
| WO2024218296A1 (en) * | 2023-04-20 | 2024-10-24 | H. Lundbeck A/S | Combination treatments comprising administration of leucine-rich repeat kinase 2 (lrrk2) inhibitors |
| TW202442652A (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 |
| WO2024218288A1 (en) * | 2023-04-20 | 2024-10-24 | H. Lundbeck A/S | Leucine-rich repeat kinase 2 (lrrk2) inhibitors |
| WO2024218285A1 (en) * | 2023-04-20 | 2024-10-24 | H. Lundbeck A/S | Leucine-rich repeat kinase 2 (lrrk2) inhibitors |
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| WO2013001310A1 (en) * | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
| CN102971322A (zh) * | 2010-05-20 | 2013-03-13 | 阵列生物制药公司 | 作为trk激酶抑制剂的大环化合物 |
| CN103930427A (zh) * | 2011-09-30 | 2014-07-16 | 昂科迪塞恩股份有限公司 | 大环flt3 激酶抑制剂 |
| CN104023728A (zh) * | 2011-09-30 | 2014-09-03 | 益普生制药股份有限公司 | 大环lrrk2激酶抑制剂 |
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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 |
| SK283569B6 (sk) | 1993-10-01 | 2003-09-11 | Astra Aktiebolag | Spôsob spracovania jemne deleného práškového liečiva, zariadenie na vykonávanie tohto spôsobu a aglomeráty vyrobené týmto spôsobom |
| 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 |
| HU228962B1 (en) | 1996-07-24 | 2013-07-29 | Bristol Myers Squibb Pharma Co | Azolo triazines, pharmaceutical compositions containing them and use of the compounds |
| 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 |
| DE60130924T2 (de) | 2000-12-28 | 2008-07-17 | Ono Pharmaceutical Co. Ltd. | Cyclopentaädüpyrazoloä1,5-aüpyrimidin-verbindung als crf-rezeptor antagonist |
| BR0210391A (pt) * | 2001-06-12 | 2004-06-15 | Elan Pharm Inc | Composto, métodos de tratar um paciente que tenha ou de prevenir um paciente de contrair uma doença ou condição e de preparar um composto, e, uso de um composto |
| WO2006045392A2 (en) | 2004-10-21 | 2006-05-04 | GSF-Forschungszentrum für Umwelt und Gesundheit GmbH | Kaspp (lrrke) 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 |
| NZ568325A (en) | 2005-11-16 | 2011-05-27 | S Bio Pte Ltd | Macrocyclic oxygen linked pyrimidine derivatives |
| WO2009127642A2 (en) | 2008-04-15 | 2009-10-22 | Cellzome Limited | Use of lrrk2 inhibitors for neurodegenerative diseases |
| MX2012003778A (es) | 2009-09-29 | 2012-06-01 | Glaxo Group Ltd | Compuestos novedosos. |
-
2015
- 2015-09-17 TR TR2019/04514T patent/TR201904514T4/tr unknown
- 2015-09-17 US US15/511,879 patent/US10377772B2/en not_active Expired - Fee Related
- 2015-09-17 SG SG11201701936WA patent/SG11201701936WA/en unknown
- 2015-09-17 KR KR1020177010322A patent/KR20170048599A/ko not_active Withdrawn
- 2015-09-17 CN CN201580061216.1A patent/CN107108641A/zh active Pending
- 2015-09-17 PL PL15766801T patent/PL3194405T4/pl unknown
- 2015-09-17 WO PCT/EP2015/071349 patent/WO2016042089A1/en not_active Ceased
- 2015-09-17 JP JP2017515823A patent/JP2017529365A/ja active Pending
- 2015-09-17 CA CA2960777A patent/CA2960777A1/en not_active Abandoned
- 2015-09-17 TW TW104130753A patent/TW201625639A/zh unknown
- 2015-09-17 MX MX2017003470A patent/MX2017003470A/es unknown
- 2015-09-17 EP EP15766801.3A patent/EP3194405B1/en not_active Not-in-force
- 2015-09-17 HU HUE15766801A patent/HUE043972T2/hu unknown
- 2015-09-17 BR BR112017005299A patent/BR112017005299A2/pt not_active IP Right Cessation
- 2015-09-17 EA EA201790626A patent/EA032838B1/ru not_active IP Right Cessation
- 2015-09-17 AU AU2015316801A patent/AU2015316801B2/en not_active Ceased
- 2015-09-17 DK DK15766801.3T patent/DK3194405T3/en active
- 2015-09-17 ES ES15766801T patent/ES2717510T3/es active Active
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2017
- 2017-03-09 IL IL251054A patent/IL251054B/en not_active IP Right Cessation
- 2017-03-15 ZA ZA2017/01841A patent/ZA201701841B/en unknown
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| CN102971322A (zh) * | 2010-05-20 | 2013-03-13 | 阵列生物制药公司 | 作为trk激酶抑制剂的大环化合物 |
| WO2013001310A1 (en) * | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
| CN103930427A (zh) * | 2011-09-30 | 2014-07-16 | 昂科迪塞恩股份有限公司 | 大环flt3 激酶抑制剂 |
| CN104023728A (zh) * | 2011-09-30 | 2014-09-03 | 益普生制药股份有限公司 | 大环lrrk2激酶抑制剂 |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3194405B1 (en) | 2018-12-26 |
| PL3194405T3 (pl) | 2019-07-31 |
| JP2017529365A (ja) | 2017-10-05 |
| ZA201701841B (en) | 2019-08-28 |
| BR112017005299A2 (pt) | 2017-12-12 |
| EP3194405A1 (en) | 2017-07-26 |
| MX2017003470A (es) | 2017-08-07 |
| US20170240565A1 (en) | 2017-08-24 |
| EA032838B1 (ru) | 2019-07-31 |
| AU2015316801A1 (en) | 2017-04-27 |
| SG11201701936WA (en) | 2017-04-27 |
| TW201625639A (zh) | 2016-07-16 |
| AU2015316801B2 (en) | 2019-03-07 |
| DK3194405T3 (en) | 2019-04-15 |
| KR20170048599A (ko) | 2017-05-08 |
| IL251054B (en) | 2019-03-31 |
| US10377772B2 (en) | 2019-08-13 |
| HUE043972T2 (hu) | 2019-09-30 |
| CA2960777A1 (en) | 2016-03-24 |
| PL3194405T4 (pl) | 2019-07-31 |
| TR201904514T4 (tr) | 2019-04-22 |
| EA201790626A1 (ru) | 2017-07-31 |
| ES2717510T3 (es) | 2019-06-21 |
| IL251054A0 (en) | 2017-04-30 |
| WO2016042089A1 (en) | 2016-03-24 |
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