JP7362600B2 - Rip1キナーゼ阻害剤として使用するための二環式化合物 - Google Patents
Rip1キナーゼ阻害剤として使用するための二環式化合物 Download PDFInfo
- Publication number
- JP7362600B2 JP7362600B2 JP2020520532A JP2020520532A JP7362600B2 JP 7362600 B2 JP7362600 B2 JP 7362600B2 JP 2020520532 A JP2020520532 A JP 2020520532A JP 2020520532 A JP2020520532 A JP 2020520532A JP 7362600 B2 JP7362600 B2 JP 7362600B2
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- JP
- Japan
- Prior art keywords
- fluoro
- phenyl
- pyrrolo
- dihydro
- triazole
- 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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Classifications
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762570892P | 2017-10-11 | 2017-10-11 | |
| US62/570,892 | 2017-10-11 | ||
| PCT/EP2018/077656 WO2019072942A1 (en) | 2017-10-11 | 2018-10-10 | BICYCLIC COMPOUNDS FOR USE AS INHIBITORS OF KINASE RIP1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020536915A JP2020536915A (ja) | 2020-12-17 |
| JP2020536915A5 JP2020536915A5 (enExample) | 2021-11-25 |
| JP7362600B2 true JP7362600B2 (ja) | 2023-10-17 |
Family
ID=63840848
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020520532A Active JP7362600B2 (ja) | 2017-10-11 | 2018-10-10 | Rip1キナーゼ阻害剤として使用するための二環式化合物 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US11673892B2 (enExample) |
| EP (1) | EP3694858B1 (enExample) |
| JP (1) | JP7362600B2 (enExample) |
| KR (1) | KR20200070297A (enExample) |
| CN (1) | CN111201229B (enExample) |
| AU (1) | AU2018348930A1 (enExample) |
| BR (1) | BR112020007067A2 (enExample) |
| CA (1) | CA3078653A1 (enExample) |
| CL (1) | CL2020000944A1 (enExample) |
| CO (1) | CO2020004977A2 (enExample) |
| CR (1) | CR20200151A (enExample) |
| IL (1) | IL273443A (enExample) |
| MA (1) | MA50356A (enExample) |
| MX (1) | MX2020003439A (enExample) |
| PE (1) | PE20211246A1 (enExample) |
| PH (1) | PH12020550253A1 (enExample) |
| RU (1) | RU2020114670A (enExample) |
| SG (1) | SG11202003283TA (enExample) |
| WO (1) | WO2019072942A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11071721B2 (en) | 2016-12-02 | 2021-07-27 | Genentech, Inc. | Bicyclic amide compounds and methods of use thereof |
| CN119613408A (zh) * | 2017-07-14 | 2025-03-14 | 豪夫迈·罗氏有限公司 | 二环酮化合物及其使用方法 |
| MX2020003451A (es) | 2017-10-31 | 2020-08-03 | Hoffmann La Roche | Sulfonas y sulfoxidos biciclicos y metodos de uso de los mismos. |
| CN113302193B (zh) * | 2019-01-11 | 2026-05-29 | 豪夫迈·罗氏有限公司 | 双环吡咯并三唑酮化合物及其使用方法 |
| CN114591333B (zh) * | 2020-12-04 | 2023-08-01 | 广州嘉越医药科技有限公司 | 一种吡咯并嘧啶类化合物的制备方法 |
| CA3214802A1 (en) * | 2021-04-02 | 2022-10-06 | Genentech, Inc. | Processes for making bicyclic ketone compounds |
| WO2023039795A1 (zh) * | 2021-09-16 | 2023-03-23 | 维泰瑞隆(北京)生物科技有限公司 | Rip1激酶抑制剂及其用途 |
| WO2025261418A1 (zh) * | 2024-06-19 | 2025-12-26 | 成都赜灵生物医药科技有限公司 | 并芳基类化合物及其用途 |
| WO2026001865A1 (en) * | 2024-06-24 | 2026-01-02 | Sironax Ltd. | Rip1 modulators, preparations, and uses thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JP2012051806A (ja) | 2009-02-26 | 2012-03-15 | Eisai R & D Management Co Ltd | イミダゾリルピラジン誘導体 |
| JP2014518286A (ja) | 2011-07-15 | 2014-07-28 | ヤンセン ファーマシューティカルズ,インコーポレーテッド | γ−セクレターゼ調節剤としての新規な置換インドール誘導体 |
| WO2017004500A1 (en) | 2015-07-02 | 2017-01-05 | Genentech, Inc. | Bicyclic lactams and methods of use thereof |
| WO2017136727A2 (en) | 2016-02-05 | 2017-08-10 | Denali Therapeutics Inc. | Compounds, compositions and methods |
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| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| EP0102324A3 (de) | 1982-07-29 | 1984-11-07 | Ciba-Geigy Ag | Lipide und Tenside in wässriger Phase |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| HUT35524A (en) | 1983-08-02 | 1985-07-29 | Hoechst Ag | Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance |
| US5004697A (en) | 1987-08-17 | 1991-04-02 | Univ. Of Ca | Cationized antibodies for delivery through the blood-brain barrier |
| US5112596A (en) | 1990-04-23 | 1992-05-12 | Alkermes, Inc. | Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability |
| US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
| WO1992004343A1 (fr) * | 1990-09-04 | 1992-03-19 | Yamanouchi Pharmaceutical Co., Ltd. | Nouveau derive de tetrahydrobenzazole |
| AU677216B2 (en) | 1992-07-27 | 1997-04-17 | Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The | Targeting of liposomes to the blood-brain barrier |
| US6080772A (en) | 1995-06-07 | 2000-06-27 | Sugen, Inc. | Thiazole compounds and methods of modulating signal transduction |
| EP1007042A4 (en) | 1997-06-13 | 2001-07-04 | Sugen Inc | NEW HETEROCYCLIC COMPOUNDS FOR MODULATING THE PROTEIN-TYROSIN-ENZYME-RELATED CELLULAR SIGNAL TRANSDUCTION |
| US6514221B2 (en) | 2000-07-27 | 2003-02-04 | Brigham And Women's Hospital, Inc. | Blood-brain barrier opening |
| CA2416527C (en) | 2000-08-10 | 2009-12-22 | Pharmacia Italia S.P.A. | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| AU2001286930A1 (en) | 2000-08-30 | 2002-03-13 | The Board Of Trustees Of The Leland Stanford Junior University | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| US7034036B2 (en) | 2000-10-30 | 2006-04-25 | Pain Therapeutics, Inc. | Inhibitors of ABC drug transporters at the blood-brain barrier |
| DE10121982B4 (de) | 2001-05-05 | 2008-01-24 | Lts Lohmann Therapie-Systeme Ag | Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung |
| SI1397364T1 (sl) | 2001-05-24 | 2007-12-31 | Lilly Co Eli | Novi pirolni derivati kot farmacevtske uäśinkovine |
| CA2450073C (en) | 2001-07-25 | 2017-08-29 | Biomarin Pharmaceutical Inc. | Compositions and methods for modulating blood-brain barrier transport |
| US20030162695A1 (en) | 2002-02-27 | 2003-08-28 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| JP4995423B2 (ja) | 2002-12-03 | 2012-08-08 | ブランシェット・ロックフェラー・ニューロサイエンスィズ・インスティテュート | 物質を血液−脳関門を渡って輸送するための人工低密度リポタンパク質キャリア |
| WO2005025511A2 (en) | 2003-09-10 | 2005-03-24 | Cedars-Sinai Medical Center | Potassium channel mediated delivery of agents through the blood-brain barrier |
| EA017937B1 (ru) | 2007-02-07 | 2013-04-30 | Пфайзер Инк. | ПРОИЗВОДНЫЕ 3-АМИНОПИРРОЛО[3,4-c]ПИРАЗОЛ-5(1H,4H,6H)-КАРБАЛЬДЕГИДА В КАЧЕСТВЕ ИНГИБИТОРОВ РКС |
| WO2011006903A1 (en) | 2009-07-15 | 2011-01-20 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Substituted triazole and imidazole derivatives as gamma secretase modulators |
| JP6267193B2 (ja) | 2012-05-22 | 2018-01-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 置換ジピリジルアミン類及びそれらの使用 |
| MX2015009270A (es) | 2013-01-18 | 2015-10-30 | Hoffmann La Roche | Pirazoles sustituidos en posicion 3 y uso de los mismos como inhibidores de la cinasa cremallera de leucinas dual (dlk). |
| TWI648274B (zh) | 2013-02-15 | 2019-01-21 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺類 (二) |
| RU2015147601A (ru) | 2013-05-01 | 2017-06-05 | Ф. Хоффманн-Ля Рош Аг | С-связанные гетероциклоалкилзамещенные пиримидины и их применения |
| TWI710558B (zh) | 2013-05-01 | 2020-11-21 | 瑞士商赫孚孟拉羅股份公司 | 二雜芳基化合物及其用途 |
| MX2016008110A (es) | 2013-12-20 | 2016-08-19 | Hoffmann La Roche | Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos. |
| RU2017109122A (ru) | 2014-08-21 | 2018-09-21 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Способы лечения с использованием гетероциклических амидов в качестве ингибиторов киназы |
| JP6701225B2 (ja) | 2015-03-09 | 2020-05-27 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 三環式dlk阻害剤及びその使用 |
| KR102613433B1 (ko) | 2017-10-11 | 2023-12-13 | 주식회사 대웅제약 | 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물 |
-
2018
- 2018-10-10 WO PCT/EP2018/077656 patent/WO2019072942A1/en not_active Ceased
- 2018-10-10 AU AU2018348930A patent/AU2018348930A1/en not_active Abandoned
- 2018-10-10 JP JP2020520532A patent/JP7362600B2/ja active Active
- 2018-10-10 CA CA3078653A patent/CA3078653A1/en active Pending
- 2018-10-10 EP EP18785936.8A patent/EP3694858B1/en active Active
- 2018-10-10 PE PE2020000378A patent/PE20211246A1/es unknown
- 2018-10-10 KR KR1020207013188A patent/KR20200070297A/ko not_active Ceased
- 2018-10-10 MA MA050356A patent/MA50356A/fr unknown
- 2018-10-10 CR CR20200151A patent/CR20200151A/es unknown
- 2018-10-10 RU RU2020114670A patent/RU2020114670A/ru unknown
- 2018-10-10 MX MX2020003439A patent/MX2020003439A/es unknown
- 2018-10-10 BR BR112020007067-0A patent/BR112020007067A2/pt not_active Application Discontinuation
- 2018-10-10 CN CN201880066460.0A patent/CN111201229B/zh active Active
- 2018-10-10 SG SG11202003283TA patent/SG11202003283TA/en unknown
-
2020
- 2020-03-19 IL IL273443A patent/IL273443A/en unknown
- 2020-04-08 CL CL2020000944A patent/CL2020000944A1/es unknown
- 2020-04-09 PH PH12020550253A patent/PH12020550253A1/en unknown
- 2020-04-09 US US16/844,952 patent/US11673892B2/en active Active
- 2020-04-23 CO CONC2020/0004977A patent/CO2020004977A2/es unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012051806A (ja) | 2009-02-26 | 2012-03-15 | Eisai R & D Management Co Ltd | イミダゾリルピラジン誘導体 |
| JP2014518286A (ja) | 2011-07-15 | 2014-07-28 | ヤンセン ファーマシューティカルズ,インコーポレーテッド | γ−セクレターゼ調節剤としての新規な置換インドール誘導体 |
| WO2017004500A1 (en) | 2015-07-02 | 2017-01-05 | Genentech, Inc. | Bicyclic lactams and methods of use thereof |
| WO2017136727A2 (en) | 2016-02-05 | 2017-08-10 | Denali Therapeutics Inc. | Compounds, compositions and methods |
Non-Patent Citations (3)
| Title |
|---|
| HARNISCH, F. et al.,Combined intra-intermolecular criss-cross cycloaddition reactions leading to perfluoroalkylated fused tricyclic nitrogen heterocycles,Journal of fluorine chemistry,2014年,Vol.158,pp.38-43 |
| RACKHAM, D. M.,Spectroscopic studies of some imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrimidine derivatives,APPLIED SPECTROSCOPY,1979年,Vol.33, No.6,pp.561-563 |
| REGISTRY[online],2014.2.16-2017.7.28, [Retrieved on 2022.9.22], Retrieved from:STN,CAS登録番号 2104558-36-1, 1545019-33-7, 1553451-22-1, 1556249-42-3, 1547153-77-4 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3694858B1 (en) | 2023-01-11 |
| CL2020000944A1 (es) | 2020-08-21 |
| CR20200151A (es) | 2020-05-23 |
| CN111201229A (zh) | 2020-05-26 |
| CA3078653A1 (en) | 2019-04-18 |
| AU2018348930A1 (en) | 2020-03-26 |
| SG11202003283TA (en) | 2020-05-28 |
| CO2020004977A2 (es) | 2020-05-05 |
| WO2019072942A1 (en) | 2019-04-18 |
| JP2020536915A (ja) | 2020-12-17 |
| US20200283446A1 (en) | 2020-09-10 |
| MA50356A (fr) | 2021-04-21 |
| PE20211246A1 (es) | 2021-07-13 |
| KR20200070297A (ko) | 2020-06-17 |
| PH12020550253A1 (en) | 2021-02-22 |
| EP3694858A1 (en) | 2020-08-19 |
| RU2020114670A (ru) | 2021-11-12 |
| US11673892B2 (en) | 2023-06-13 |
| CN111201229B (zh) | 2024-08-23 |
| BR112020007067A2 (pt) | 2020-10-06 |
| IL273443A (en) | 2020-05-31 |
| MX2020003439A (es) | 2020-07-29 |
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