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

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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
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China
Prior art keywords
dihydro
pyrrolo
fluoro
triazole
phenyl
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CN201880070578.0A
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Chinese (zh)
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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
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F Hoffmann La Roche AG
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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
    • 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

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  • 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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (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)

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

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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
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
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
CN118510775A (zh) 2021-11-11 2024-08-16 建新公司 作为ripk1抑制剂的异噁唑烷及其用途

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 (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
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
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
JP2004502642A (ja) 2000-02-11 2004-01-29 ブリストル−マイヤーズ スクイブ カンパニー カンナビノイドレセプターモジュレーター、それらの製造方法、および呼吸系および非呼吸系疾患の処置のためのカンナビノイドレセプターモジュレーターの使用
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
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
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
PL382706A1 (pl) 2002-08-26 2007-11-26 Takeda Pharmaceutical Company Limited Związek modulujący receptor wapnia i jego zastosowanie
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
ATE410161T1 (de) 2003-05-02 2008-10-15 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
WO2005025511A2 (en) 2003-09-10 2005-03-24 Cedars-Sinai Medical Center Potassium channel mediated delivery of agents through 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
CA2852964A1 (en) 2011-11-03 2013-05-10 F. Hoffmann-La Roche Ag Bicyclic piperazine compounds
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)
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
RU2015147601A (ru) 2013-05-01 2017-06-05 Ф. Хоффманн-Ля Рош Аг С-связанные гетероциклоалкилзамещенные пиримидины и их применения
AU2014287471C1 (en) 2013-07-10 2019-11-28 Vertex Pharmaceuticals Incorporated Fused piperidine amides as modulators of ion channels
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.
CR20160418A (es) 2014-03-26 2016-11-07 Hoffmann La Roche Nuevos compuestos biciclicos de 7 eslabones
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
UY36680A (es) 2015-05-19 2016-12-30 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas como inhibidores de quinasa
US10751444B2 (en) 2015-08-07 2020-08-25 Victor Matthew Phillips Flowable hemostatic gel composition and its methods of use
CN108602809B (zh) * 2015-12-04 2022-09-30 戴纳立制药公司 异噁唑烷衍生的受体相互作用蛋白激酶1(ripk 1)的抑制剂
US10961258B2 (en) * 2015-12-21 2021-03-30 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
AU2017356887B2 (en) 2016-11-08 2022-06-30 Cyclerion Therapeutics, Inc. sGC stimulators
US11071721B2 (en) 2016-12-02 2021-07-27 Genentech, Inc. 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
WO2019072942A1 (en) 2017-10-11 2019-04-18 F. Hoffmann-La Roche Ag BICYCLIC COMPOUNDS FOR USE AS INHIBITORS OF KINASE RIP1
MX2020003451A (es) 2017-10-31 2020-08-03 Hoffmann La Roche Sulfonas y sulfoxidos biciclicos y metodos de uso de los mismos.

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

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

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