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 PDF

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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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fluoro
phenyl
pyrrolo
dihydro
triazole
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JP2020536915A5 (https=
JP2020536915A (ja
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チェン，ホイフェン
ハミルトン，グレゴリー
パテル，スナヘル
ジャオ，グォイリン
ダニエルズ，ブレイク
スティバラ，クレイグ
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F Hoffmann La Roche AG
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    • 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

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  • 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)
JP2020520532A 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 Active JP7362600B2 (ja)

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

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JP2020536915A JP2020536915A (ja) 2020-12-17
JP2020536915A5 JP2020536915A5 (https=) 2021-11-25
JP7362600B2 true JP7362600B2 (ja) 2023-10-17

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US (1) US11673892B2 (https=)
EP (1) EP3694858B1 (https=)
JP (1) JP7362600B2 (https=)
KR (1) KR20200070297A (https=)
CN (1) CN111201229B (https=)
AU (1) AU2018348930A1 (https=)
BR (1) BR112020007067A2 (https=)
CA (1) CA3078653A1 (https=)
CL (1) CL2020000944A1 (https=)
CO (1) CO2020004977A2 (https=)
CR (1) CR20200151A (https=)
IL (1) IL273443A (https=)
MA (1) MA50356A (https=)
MX (1) MX2020003439A (https=)
PE (1) PE20211246A1 (https=)
PH (1) PH12020550253A1 (https=)
RU (1) RU2020114670A (https=)
SG (1) SG11202003283TA (https=)
WO (1) WO2019072942A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
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
BR112020000771A2 (pt) 2017-07-14 2020-07-14 F. Hoffmann-La Roche Ag compostos de cetona bicíclica e métodos de uso dos mesmos
AR113811A1 (es) 2017-10-31 2020-06-10 Hoffmann La Roche Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos
CN113302193A (zh) 2019-01-11 2021-08-24 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
IL307250A (en) * 2021-04-02 2023-11-01 Hoffmann La Roche Processes for preparing 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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
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
AU8405691A (en) * 1990-09-04 1992-03-30 Yamanouchi Pharmaceutical Co., Ltd. Novel tetrahydrobenzazole derivative
ATE191853T1 (de) 1992-07-27 2000-05-15 Us Health Zielgerichte liposome zur blut-hirne schranke
US6080772A (en) 1995-06-07 2000-06-27 Sugen, Inc. Thiazole compounds and methods of modulating signal transduction
CA2293400A1 (en) 1997-06-13 1998-12-17 Gerald Mcmahon Novel heteroaryl compounds for the modulation of protein tyrosine enzyme related cellular signal transduction
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
DK1320531T3 (da) 2000-08-10 2011-01-03 Pfizer Italia Srl Bicyclo-pyrazoler, der er aktive som kinase inhibitorer, fremgangsmåde til fremstilling deraf og farmaceutiske sammensætninger, der indeholder disse
US20020065259A1 (en) 2000-08-30 2002-05-30 Schatzberg Alan F. 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
SK287857B6 (sk) 2001-05-24 2012-01-04 Eli Lilly And Company Novel pyrrole derivatives as pharmaceutical agents
AU2002322720B2 (en) 2001-07-25 2008-11-13 Raptor 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
JP2007505142A (ja) 2003-09-10 2007-03-08 セダーズ−シナイ メディカル センター 血液脳関門を通過する薬剤のカリウムチャネル媒介性送達
CA2677572C (en) 2007-02-07 2012-12-18 Pfizer Inc. 3-amino-pyrrolo[3,4-c]pyrazole-5(1h,4h,6h) carbaldehyde derivatives as pkc inhibitors
ES2519565T3 (es) 2009-07-15 2014-11-07 Janssen Pharmaceuticals Inc. Derivados de triazol e imidazol sustituidos como moduladores de gamma secretasa
CN104271566B (zh) 2012-05-22 2017-05-31 霍夫曼-拉罗奇有限公司 取代的联吡啶胺及其用途
JP6199991B2 (ja) 2013-01-18 2017-09-20 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ３置換ピラゾール及びｄｌｋ阻害剤としての使用
TWI637951B (zh) 2013-02-15 2018-10-11 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
JP6523251B2 (ja) 2013-05-01 2019-05-29 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｃ−結合ヘテロシクロアルキル置換ピリミジン類及びそれらの用途
AR096151A1 (es) 2013-05-01 2015-12-09 Hoffmann La Roche Compuestos de biheteroarilo y usos de los mismos
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.
CN106573006A (zh) 2014-08-21 2017-04-19 葛兰素史密斯克莱知识产权发展有限公司 作为药物的rip1激酶抑制剂杂环酰胺
CN107406462B (zh) 2015-03-09 2020-11-10 豪夫迈·罗氏有限公司 三环dlk抑制剂及其用途
KR102613433B1 (ko) 2017-10-11 2023-12-13 주식회사 대웅제약 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물

Patent Citations (4)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

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WO2019072942A1 (en) 2019-04-18
MA50356A (fr) 2021-04-21
MX2020003439A (es) 2020-07-29
SG11202003283TA (en) 2020-05-28
IL273443A (en) 2020-05-31
PH12020550253A1 (en) 2021-02-22
CL2020000944A1 (es) 2020-08-21
EP3694858B1 (en) 2023-01-11
US20200283446A1 (en) 2020-09-10
KR20200070297A (ko) 2020-06-17
JP2020536915A (ja) 2020-12-17
CN111201229B (zh) 2024-08-23
RU2020114670A (ru) 2021-11-12
PE20211246A1 (es) 2021-07-13
CA3078653A1 (en) 2019-04-18
CN111201229A (zh) 2020-05-26
BR112020007067A2 (pt) 2020-10-06
CO2020004977A2 (es) 2020-05-05
EP3694858A1 (en) 2020-08-19
US11673892B2 (en) 2023-06-13
CR20200151A (es) 2020-05-23
AU2018348930A1 (en) 2020-03-26

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