CN111201229B - 用作rip1激酶抑制剂的二环化合物 - Google Patents

用作rip1激酶抑制剂的二环化合物 Download PDF

Info

Publication number
CN111201229B
CN111201229B CN201880066460.0A CN201880066460A CN111201229B CN 111201229 B CN111201229 B CN 111201229B CN 201880066460 A CN201880066460 A CN 201880066460A CN 111201229 B CN111201229 B CN 111201229B
Authority
CN
China
Prior art keywords
fluoro
pyrrolo
dihydro
phenyl
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.)
Active
Application number
CN201880066460.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN111201229A (zh
Inventor
陈慧芬
G·汉密尔顿
S·帕特尔
赵桂玲
B·达涅尔斯
C·斯蒂瓦拉
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CN111201229A publication Critical patent/CN111201229A/zh
Application granted granted Critical
Publication of CN111201229B publication Critical patent/CN111201229B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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)
CN201880066460.0A 2017-10-11 2018-10-10 用作rip1激酶抑制剂的二环化合物 Active CN111201229B (zh)

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 (2)

Publication Number Publication Date
CN111201229A CN111201229A (zh) 2020-05-26
CN111201229B true CN111201229B (zh) 2024-08-23

Family

ID=63840848

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880066460.0A Active CN111201229B (zh) 2017-10-11 2018-10-10 用作rip1激酶抑制剂的二环化合物

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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201831478A (zh) 2016-12-02 2018-09-01 瑞士商赫孚孟拉羅股份公司 雙環醯胺化合物及其使用方法
KR102664604B1 (ko) * 2017-07-14 2024-05-14 에프. 호프만-라 로슈 아게 이환형 케톤 화합물 및 이의 사용 방법
AU2018360270A1 (en) 2017-10-31 2020-03-26 F. Hoffmann-La Roche Ag Bicyclic sulfones and sulfoxides and methods of use thereof
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
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (35)

* 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
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
AU8071698A (en) 1997-06-13 1998-12-30 Sugen, Inc. Novel heteroaryl compounds for the modulation of protein tyrosine enzyme relatedcellular signal transduction
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
MXPA03001169A (es) 2000-08-10 2003-06-30 Pharmacia Italia Spa Biciclo-pirazoles activos como inhibidores de quinasa, proceso para su preparacion y composiciones farmaceuticas que comprenden los mismos.
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
ES2289116T3 (es) 2001-05-24 2008-02-01 Eli Lilly And Company Nuevos derivados de pirrol como agentes farmaceuticos.
US20030129186A1 (en) 2001-07-25 2003-07-10 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
CA2791165C (en) 2002-12-03 2015-02-24 Blanchette Rockefeller Neurosciences Institute A conjugate comprising cholesterol linked to tetracycline
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
EP2118112B1 (en) 2007-02-07 2015-07-08 Pfizer Inc. 3-amino-pyrrolo[3,4-c] pyrazole- 5 (1h, 4h, 6h) carbaldehyde derivatives as pkc inhibitors
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
ES2519565T3 (es) 2009-07-15 2014-11-07 Janssen Pharmaceuticals Inc. Derivados de triazol e imidazol sustituidos como moduladores de gamma secretasa
MX2014000626A (es) 2011-07-15 2014-04-30 Janssen Pharmaceuticals Inc Nuevos derivados de indol sustituidos como moduladores de gamma secretasa.
MX2014013407A (es) 2012-05-22 2014-11-26 Hoffmann La Roche Dipiridilaminas sustituidas y uso de las mismas.
BR112015016395A2 (pt) 2013-01-18 2017-07-11 Hoffmann La Roche pirazóis 3-substituídos e uso como inibidores de dlk
TWI638815B (zh) 2013-02-15 2018-10-21 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（一）
KR20160002850A (ko) 2013-05-01 2016-01-08 에프. 호프만-라 로슈 아게 C-연결된 헤테로사이클로알킬 치환된 피리미딘 및 이의 용도
MA42164B1 (fr) 2013-05-01 2019-12-31 Hoffmann La Roche Composes biheteroaryle et leurs utilisations
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
RU2020114670A (ru) 2021-11-12
CA3078653A1 (en) 2019-04-18
PH12020550253A1 (en) 2021-02-22
WO2019072942A1 (en) 2019-04-18
EP3694858B1 (en) 2023-01-11
MA50356A (fr) 2021-04-21
KR20200070297A (ko) 2020-06-17
PE20211246A1 (es) 2021-07-13
MX2020003439A (es) 2020-07-29
US20200283446A1 (en) 2020-09-10
CN111201229A (zh) 2020-05-26
CL2020000944A1 (es) 2020-08-21
IL273443A (en) 2020-05-31
CO2020004977A2 (es) 2020-05-05
JP7362600B2 (ja) 2023-10-17
US11673892B2 (en) 2023-06-13
BR112020007067A2 (pt) 2020-10-06
CR20200151A (es) 2020-05-23
EP3694858A1 (en) 2020-08-19
JP2020536915A (ja) 2020-12-17
SG11202003283TA (en) 2020-05-28
AU2018348930A1 (en) 2020-03-26

Similar Documents

Publication Publication Date Title
CN111201229B (zh) 用作rip1激酶抑制剂的二环化合物
US11634436B2 (en) Pyridine lactam compounds and methods of use thereof
TW201821424A (zh) 雙環吡啶酮內醯胺及其使用方法
CN110023313B (zh) 二环酰胺化合物及其使用方法
TWI805595B (zh) 二環酮化合物及其使用方法
CN111278809B (zh) 二环砜类和亚砜类、以及其使用方法
US20250282788A1 (en) Bicyclic ketone compounds and methods of use thereof
HK40020605B (zh) 用作rip1激酶抑制剂的二环化合物
HK40020605A (en) Bicyclic compounds for use as rip1 kinase inhibitors
HK40036919B (zh) 作为rip1激酶抑制剂用於治疗例如肠易激综合征(ibs)的化合物
HK40062362A (en) Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof
HK40062362B (en) Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof
HK40036919A (en) Compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs)
HK40017913B (zh) 二环酮化合物及其使用方法
HK40011755B (en) Inhibitors of rip1 kinase and methods of use thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40020605

Country of ref document: HK

SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant