CN111278809B - 二环砜类和亚砜类、以及其使用方法 - Google Patents

二环砜类和亚砜类、以及其使用方法 Download PDF

Info

Publication number
CN111278809B
CN111278809B CN201880070578.0A CN201880070578A CN111278809B CN 111278809 B CN111278809 B CN 111278809B CN 201880070578 A CN201880070578 A CN 201880070578A CN 111278809 B CN111278809 B CN 111278809B
Authority
CN
China
Prior art keywords
pyrrolo
dihydro
fluoro
triazole
phenyl
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
CN201880070578.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN111278809A (zh
Inventor
S·帕特尔
G·汉密尔顿
C·斯蒂瓦拉
陈慧芬
B·达涅尔斯
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 CN111278809A publication Critical patent/CN111278809A/zh
Application granted granted Critical
Publication of CN111278809B publication Critical patent/CN111278809B/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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201880070578.0A 2017-10-31 2018-10-30 二环砜类和亚砜类、以及其使用方法 Active CN111278809B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762579392P 2017-10-31 2017-10-31
US62/579,392 2017-10-31
PCT/EP2018/079772 WO2019086494A1 (en) 2017-10-31 2018-10-30 Bicyclic sulfones and sulfoxides and methods of use thereof

Publications (2)

Publication Number Publication Date
CN111278809A CN111278809A (zh) 2020-06-12
CN111278809B true CN111278809B (zh) 2024-06-25

Family

ID=64051580

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880070578.0A Active CN111278809B (zh) 2017-10-31 2018-10-30 二环砜类和亚砜类、以及其使用方法

Country Status (21)

Country Link
US (2) US11072617B2 (enExample)
EP (1) EP3704097B1 (enExample)
JP (1) JP2021501183A (enExample)
KR (1) KR20200083515A (enExample)
CN (1) CN111278809B (enExample)
AR (1) AR113811A1 (enExample)
AU (1) AU2018360270A1 (enExample)
BR (1) BR112020008446A2 (enExample)
CA (1) CA3078688A1 (enExample)
CL (1) CL2020001062A1 (enExample)
CO (1) CO2020003475A2 (enExample)
CR (1) CR20200168A (enExample)
IL (1) IL273847A (enExample)
MA (1) MA50503A (enExample)
MX (1) MX2020003451A (enExample)
PE (1) PE20211247A1 (enExample)
PH (1) PH12020550537A1 (enExample)
RU (1) RU2020115915A (enExample)
SG (1) SG11202002877RA (enExample)
TW (1) TW201922748A (enExample)
WO (1) WO2019086494A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018100070A1 (en) 2016-12-02 2018-06-07 F. Hoffmann-La Roche Ag 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
US11072617B2 (en) 2017-10-31 2021-07-27 Genentech, Inc. Bicyclic sulfones and sulfoxides and methods of use thereof
EP3908586B1 (en) 2019-01-11 2022-12-21 F. Hoffmann-La Roche AG Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof
TW202214617A (zh) 2020-06-02 2022-04-16 法商賽諾菲公司 作為ｒｉｐｋ１抑制劑之異㗁唑啶及其用途
JP2024544533A (ja) 2021-11-11 2024-12-03 ジェンザイム・コーポレーション Ｒｉｐｋ１阻害剤としてのイソオキサゾリジン及びその使用

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 (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1620508A1 (de) * 1965-07-23 1969-09-18 Thomae Gmbh Dr K Verfahren zur Herstellung neuer 4,5,6,7-Tetrahydrothiazolo-[5,4-c]-pyridine
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US3948903A (en) 1972-12-15 1976-04-06 Parke, Davis & Company Substituted N-(1,2-dihydro-2-oxonicotinyl)-cephalexins and -cephaloglycins
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
GB8610530D0 (en) * 1986-04-30 1986-06-04 Fbc Ltd Herbicides
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
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
EP1254115A2 (en) 2000-02-11 2002-11-06 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
WO2002017930A2 (en) 2000-08-30 2002-03-07 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
WO2003009815A2 (en) 2001-07-25 2003-02-06 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
AU2003265585B2 (en) 2002-08-26 2008-07-03 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
KR101111477B1 (ko) 2002-12-03 2012-02-23 블랜체트 록펠러 뉴로사이언시즈 인스티튜트 치료제와 연결된 콜레스테롤을 포함하는 접합체
DE602004016992D1 (de) 2003-05-02 2008-11-20 Elan Pharm Inc 4-bromo-5-(2-chloro-benzoylamino)-1h-pyrazol-3-carbonsäureamid-derivate und verwandte verbindungen als bradykinin b1 rezeptor antagonisten zur behandlung von entzündlichen erkrankungen
EP1663239A4 (en) 2003-09-10 2008-07-23 Cedars Sinai Medical Center KALIUM CHANNEL-MEDIATED FEEDING OF MEDICINES BY THE BLOOD BRAIN BARRIER
EP2083009A1 (de) 2008-01-22 2009-07-29 Grünenthal GmbH Substituierte Tethrahydroimidazopyridin-Verbindungen und deren Verwendung in Arzneimitteln
US8299077B2 (en) 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
CN101824036A (zh) 2009-03-05 2010-09-08 上海恒瑞医药有限公司 四氢咪唑并[1，5-a]吡嗪衍生物的盐,其制备方法及其在医药上的应用
JP5808869B2 (ja) 2011-11-03 2015-11-10 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 二環式ピペラジン化合物
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
CN104918934B (zh) 2013-01-18 2017-12-22 霍夫曼-拉罗奇有限公司 3‑取代的吡唑及其作为dlk抑制剂的用途
TWI648273B (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（三）
EP2991977B1 (en) 2013-05-01 2020-07-22 F.Hoffmann-La Roche Ag C-linked heterocycloalkyl substituted pyrimidines and their uses
EA038235B1 (ru) 2013-05-01 2021-07-28 Ф.Хоффманн-Ля Рош Аг Бигетероарильные соединения и их применения
MX368728B (es) 2013-07-10 2019-10-14 Vertex Pharma Amidas de piperidina fusionadas como moduladores de canales de iones.
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.
WO2015144609A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
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
EP3268373B1 (en) 2015-03-09 2022-04-27 F. Hoffmann-La Roche AG Tricyclic dlk inhibitors and uses thereof
TWI730959B (zh) 2015-05-19 2021-06-21 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
US10751444B2 (en) 2015-08-07 2020-08-25 Victor Matthew Phillips Flowable hemostatic gel composition and its methods of use
US10709692B2 (en) 2015-12-04 2020-07-14 Denali Therapeutics Inc. Isoxazolidine derived inhibitors of receptor interacting protein kinase 1 (RIPK1)
WO2017109724A1 (en) 2015-12-21 2017-06-29 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
EP3538520B1 (en) 2016-11-08 2025-12-31 Tisento Therapeutics Inc. CGS STIMULATORS
WO2018100070A1 (en) 2016-12-02 2018-06-07 F. Hoffmann-La Roche Ag Bicyclic amide compounds and methods of use thereof
US11072607B2 (en) 2016-12-16 2021-07-27 Genentech, Inc. Inhibitors of RIP1 kinase 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
MA50356A (fr) 2017-10-11 2021-04-21 Hoffmann La Roche Composés bicycliques destinés à être utilisés en tant qu'inhibiteurs de la kinase rip1
US11072617B2 (en) 2017-10-31 2021-07-27 Genentech, Inc. Bicyclic sulfones and sulfoxides and methods of use thereof

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
CO2020003475A2 (es) 2020-04-24
RU2020115915A (ru) 2021-12-01
CL2020001062A1 (es) 2020-08-21
EP3704097C0 (en) 2023-10-25
PH12020550537A1 (en) 2021-03-22
IL273847A (en) 2020-05-31
AU2018360270A1 (en) 2020-03-26
US12338241B2 (en) 2025-06-24
MX2020003451A (es) 2020-08-03
EP3704097A1 (en) 2020-09-09
CR20200168A (es) 2020-07-12
JP2021501183A (ja) 2021-01-14
AR113811A1 (es) 2020-06-10
KR20200083515A (ko) 2020-07-08
RU2020115915A3 (enExample) 2022-05-06
US20190127382A1 (en) 2019-05-02
CN111278809A (zh) 2020-06-12
BR112020008446A2 (pt) 2020-12-29
US11072617B2 (en) 2021-07-27
TW201922748A (zh) 2019-06-16
MA50503A (fr) 2020-09-09
EP3704097B1 (en) 2023-10-25
US20230002391A1 (en) 2023-01-05
CA3078688A1 (en) 2019-05-09
WO2019086494A1 (en) 2019-05-09
PE20211247A1 (es) 2021-07-13
SG11202002877RA (en) 2020-04-29

Similar Documents

Publication Publication Date Title
CN111278809B (zh) 二环砜类和亚砜类、以及其使用方法
TW201920115A (zh) 化合物、組合物及方法
WO2019158019A1 (zh) 嘧啶并环化合物及其制备方法和应用
JP2020532506A (ja) 化合物、組成物、及び、方法
CN110914271B (zh) 二环酮化合物及其使用方法
CN111201229B (zh) 用作rip1激酶抑制剂的二环化合物
CN106535891A (zh) 组蛋白脱乙酰酶抑制剂及其组合物和使用方法
CN114206892A (zh) (2-乙酰氨基)硫代-β-D-吡喃半乳糖苷衍生物
US20250282788A1 (en) Bicyclic ketone compounds and methods of use thereof
HK40024493B (zh) 二环碸类和亚碸类、以及其使用方法
HK40024493A (en) Bicyclic sulfones and sulfoxides and methods of use thereof
WO2025237389A1 (zh) 三环wrn抑制剂、其制备方法及其应用
KR20230165238A (ko) 비시클릭 케톤 화합물 제조 공정
HK40062362B (en) Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof
HK40062362A (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
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
HK40029587B (zh) 化合物、组合物及方法

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40024493

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant