JP2021501183A - 二環式のスルホン及びスルホキシド、並びにその使用方法 - Google Patents

二環式のスルホン及びスルホキシド、並びにその使用方法 Download PDF

Info

Publication number
JP2021501183A
JP2021501183A JP2020524177A JP2020524177A JP2021501183A JP 2021501183 A JP2021501183 A JP 2021501183A JP 2020524177 A JP2020524177 A JP 2020524177A JP 2020524177 A JP2020524177 A JP 2020524177A JP 2021501183 A JP2021501183 A JP 2021501183A
Authority
JP
Japan
Prior art keywords
dihydro
pyrrolo
triazole
fluoro
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.)
Pending
Application number
JP2020524177A
Other languages
English (en)
Japanese (ja)
Other versions
JP2021501183A5 (https=
Inventor
パテル,スナヘル
ハミルトン,グレゴリー
スティバラ,クレイグ
チェン,ホイフェン
ダニエルズ,ブレイク
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 JP2021501183A publication Critical patent/JP2021501183A/ja
Publication of JP2021501183A5 publication Critical patent/JP2021501183A5/ja
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16Heterocyclic 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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020524177A 2017-10-31 2018-10-30 二環式のスルホン及びスルホキシド、並びにその使用方法 Pending JP2021501183A (ja)

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
JP2021501183A true JP2021501183A (ja) 2021-01-14
JP2021501183A5 JP2021501183A5 (https=) 2021-12-09

Family

ID=64051580

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2020524177A Pending JP2021501183A (ja) 2017-10-31 2018-10-30 二環式のスルホン及びスルホキシド、並びにその使用方法

Country Status (21)

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

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
US11098058B2 (en) 2017-07-14 2021-08-24 Genentech, Inc. Bicyclic ketone compounds and methods of use thereof
SG11202002877RA (en) 2017-10-31 2020-04-29 Hoffmann La Roche 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
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
WO2023083847A1 (en) 2021-11-11 2023-05-19 Sanofi Isoxazolidines as ripk1 inhibitors and use thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR94123E (fr) * 1965-07-23 1969-07-04 Thomae Gmbh Dr K Procédés pour fabriquer de nouvelles 4,5,6,7-tétrahydro-thiazolo[5,4-c]pyridines.
JPS62258385A (ja) * 1986-04-30 1987-11-10 シエ−リング・アグロケミカルズ・リミテツド 除草剤
WO2017004500A1 (en) * 2015-07-02 2017-01-05 Genentech, Inc. Bicyclic lactams and methods of use thereof
WO2017096301A1 (en) * 2015-12-04 2017-06-08 Denali Therapeutics Inc. Isoxazolidine derived inhibitors of receptor interacting protein kinase 1 (ripk 1)
WO2017136727A2 (en) * 2016-02-05 2017-08-10 Denali Therapeutics Inc. Compounds, compositions and methods

Family Cites Families (46)

* 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
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
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
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
EP1007042A4 (en) 1997-06-13 2001-07-04 Sugen Inc NEW HETEROCYCLIC COMPOUNDS FOR MODULATING THE PROTEIN-TYROSIN-ENZYME-RELATED CELLULAR SIGNAL TRANSDUCTION
WO2001058869A2 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
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
JP4202250B2 (ja) 2001-07-25 2008-12-24 バイオマリン ファーマシューティカル インコーポレイテッド 血液脳関門輸送を調節するための組成物および方法
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
KR101050700B1 (ko) 2002-08-26 2011-07-20 다케다 야쿠힌 고교 가부시키가이샤 칼슘 수용체 조절 화합물 및 이의 용도
CN101284136A (zh) 2002-12-03 2008-10-15 布朗歇特洛克菲勒神经科学研究所 传输物质穿过血脑屏障的人工低密度脂蛋白载体
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
US20050089473A1 (en) 2003-09-10 2005-04-28 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
RU2628616C2 (ru) 2011-11-03 2017-08-21 Ф. Хоффманн-Ля Рош Аг Бициклические соединения пиперазина
EP2852584B1 (en) 2012-05-22 2018-02-28 F. Hoffmann-La Roche AG Substituted dipyridylamines and uses thereof
CA2896187A1 (en) 2013-01-18 2014-07-24 F. Hoffmann-La Roche Ag 3-substituted pyrazoles and use as dlk inhibitors
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)
CA2907912A1 (en) 2013-05-01 2014-11-06 F. Hoffmann-La Roche Ag C-linked heterocycloalkyl substituted pyrimidines and their uses
PH12019502378A1 (en) 2013-05-01 2022-05-11 Hoffmann La Roche Biheteroaryl compounds and uses thereof
WO2015006280A1 (en) 2013-07-10 2015-01-15 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.
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
RU2017109122A (ru) 2014-08-21 2018-09-21 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Способы лечения с использованием гетероциклических амидов в качестве ингибиторов киназы
WO2016142310A1 (en) 2015-03-09 2016-09-15 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
WO2017109724A1 (en) * 2015-12-21 2017-06-29 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
US11180493B2 (en) 2016-11-08 2021-11-23 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
US11098058B2 (en) 2017-07-14 2021-08-24 Genentech, Inc. Bicyclic ketone compounds and methods of use thereof
PE20211246A1 (es) 2017-10-11 2021-07-13 Hoffmann La Roche Compuestos biciclicos para su uso como inhibidores de rip1 quinasa
SG11202002877RA (en) 2017-10-31 2020-04-29 Hoffmann La Roche Bicyclic sulfones and sulfoxides and methods of use thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR94123E (fr) * 1965-07-23 1969-07-04 Thomae Gmbh Dr K Procédés pour fabriquer de nouvelles 4,5,6,7-tétrahydro-thiazolo[5,4-c]pyridines.
JPS62258385A (ja) * 1986-04-30 1987-11-10 シエ−リング・アグロケミカルズ・リミテツド 除草剤
WO2017004500A1 (en) * 2015-07-02 2017-01-05 Genentech, Inc. Bicyclic lactams and methods of use thereof
WO2017096301A1 (en) * 2015-12-04 2017-06-08 Denali Therapeutics Inc. Isoxazolidine derived inhibitors of receptor interacting protein kinase 1 (ripk 1)
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
LIPSON, V. V. ET AL.: "Reactions of 3-amino-1,2,4-triazoles with cinnamic aldehydes", RUSSIAN CHEMICAL BULLETIN, INTERNATIONAL EDITION, vol. 58, no. 7, JPN6022041590, 2009, pages 1 - 4, ISSN: 0005052082 *
REGISTRY[ONLINE], JPN7022004672, ISSN: 0005052084 *
WALY, M. A. ET AL.: "A novel synthesis of imidazo[4,5-d]azepine ring system", POLISH J. CHEM., vol. 70, JPN6022041592, 1996, pages 296 - 301, ISSN: 0005052083 *

Also Published As

Publication number Publication date
EP3704097B1 (en) 2023-10-25
EP3704097C0 (en) 2023-10-25
IL273847A (en) 2020-05-31
CN111278809A (zh) 2020-06-12
EP3704097A1 (en) 2020-09-09
AU2018360270A1 (en) 2020-03-26
US11072617B2 (en) 2021-07-27
AR113811A1 (es) 2020-06-10
SG11202002877RA (en) 2020-04-29
KR20200083515A (ko) 2020-07-08
MA50503A (fr) 2020-09-09
BR112020008446A2 (pt) 2020-12-29
RU2020115915A (ru) 2021-12-01
CA3078688A1 (en) 2019-05-09
US20230002391A1 (en) 2023-01-05
CL2020001062A1 (es) 2020-08-21
MX2020003451A (es) 2020-08-03
RU2020115915A3 (https=) 2022-05-06
PE20211247A1 (es) 2021-07-13
US20190127382A1 (en) 2019-05-02
WO2019086494A1 (en) 2019-05-09
CR20200168A (es) 2020-07-12
US12338241B2 (en) 2025-06-24
CN111278809B (zh) 2024-06-25
TW201922748A (zh) 2019-06-16
CO2020003475A2 (es) 2020-04-24
PH12020550537A1 (en) 2021-03-22

Similar Documents

Publication Publication Date Title
JP7398391B2 (ja) N-[4-オキソ-2,3-ジヒドロ-1,5-ベンズオキサゼピン-3-イル]-5,6-ジヒドロ-4H-ピロロ[1,2-b]ピラゾール-2-カルボキサミド誘導体及び例えば過敏性腸症候群(IBS)を処置するためのRIP1キナーゼ阻害剤としての関連化合物
JP7734163B2 (ja) 二環式ケトン化合物及びその使用方法
US12338241B2 (en) Bicyclic sulfones and sulfoxides and methods of use thereof
JP6890179B2 (ja) 二環式アミド化合物及びその使用方法
JP7362600B2 (ja) Rip1キナーゼ阻害剤として使用するための二環式化合物
US20250282788A1 (en) Bicyclic ketone compounds and methods of use thereof
RU2797922C2 (ru) Бициклические кетоны и способы их применения
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
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)

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211027

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20211027

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220929

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20221004

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20230509