IL264676B - tlr 7/8 antagonists and their use - Google Patents

tlr 7/8 antagonists and their use

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Publication number
IL264676B
IL264676B IL264676A IL26467619A IL264676B IL 264676 B IL264676 B IL 264676B IL 264676 A IL264676 A IL 264676A IL 26467619 A IL26467619 A IL 26467619A IL 264676 B IL264676 B IL 264676B
Authority
IL
Israel
Prior art keywords
tlr
antagonists
Prior art date
Application number
IL264676A
Other languages
English (en)
Hebrew (he)
Inventor
Nadia Brugger
Xiaoling Chen
Brian A Sherer
Esther Cleary
Original Assignee
Merck Patent Gmbh
Nadia Brugger
Xiaoling Chen
Brian A Sherer
Esther Cleary
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 Merck Patent Gmbh, Nadia Brugger, Xiaoling Chen, Brian A Sherer, Esther Cleary filed Critical Merck Patent Gmbh
Publication of IL264676B publication Critical patent/IL264676B/en

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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201804170RA (en) 2015-12-17 2018-06-28 Merck Patent Gmbh Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
EP3497094B1 (en) 2016-08-08 2023-02-15 Merck Patent GmbH Tlr7/8 antagonists and uses thereof
MA46535A (fr) 2016-10-14 2019-08-21 Prec Biosciences Inc Méganucléases modifiées spécifiques de séquences de reconnaissance dans le génome du virus de l'hépatite b
US11370794B2 (en) * 2016-11-11 2022-06-28 Dynavax Technologies Corporation Toll-like receptor antagonist compounds and methods of use
RU2020123151A (ru) 2017-12-19 2022-01-20 Мерк Патент Гмбх Антагонисты tlr7/8 и их применение
CN111511754B (zh) 2017-12-20 2023-09-12 捷克共和国有机化学与生物化学研究所 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸
EP3728283B1 (en) 2017-12-20 2023-11-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
EP3752505B1 (en) 2018-02-12 2023-01-11 F. Hoffmann-La Roche AG Novel sulfone compounds and derivatives for the treatment and prophylaxis of virus infection
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TW201945388A (zh) 2018-04-12 2019-12-01 美商精密生物科學公司 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶
SG11202011137SA (en) 2018-06-05 2020-12-30 Hoffmann La Roche Tetrahydro-1 h-pyrazino[2,1 -ajisoindolylquinoline compounds for the treatment of autoimmune disease
TW202016105A (zh) 2018-06-12 2020-05-01 瑞士商赫孚孟拉羅股份公司 用於治療自體免疫疾病的新穎雜芳基雜環基化合物
JP7366994B2 (ja) * 2018-07-23 2023-10-23 エフ． ホフマン－ラ ロシュ アーゲー 自己免疫疾患治療用の新規ピペラジン化合物
EP3847169A1 (en) 2018-09-04 2021-07-14 F. Hoffmann-La Roche AG Benzothiazole compounds for the treatment of autoimmune diseases
CN112654620B (zh) 2018-09-06 2023-08-04 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的新型吡唑并吡啶化合物
US11548884B2 (en) 2018-09-06 2023-01-10 Hoffmann-La Roche Inc. Cyclic amidine compounds for the treatment of autoimmune disease
CA3120866A1 (en) * 2018-11-30 2020-06-04 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2021084022A1 (en) 2019-10-31 2021-05-06 F. Hoffmann-La Roche Ag Hydropyrazino[1,2-d][1,4]diazepine compounds for the treatment of autoimmune disease
US12503471B2 (en) 2019-11-19 2025-12-23 Hoffmann-La Roche Inc. Triazatricycle compounds for the treatment of autoimmune disease
CN114728976B (zh) * 2019-11-19 2024-08-16 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的氢-1H-吡咯并[1,2-a]吡嗪化合物
WO2021099406A1 (en) 2019-11-20 2021-05-27 F. Hoffmann-La Roche Ag Spiro(isobenzofuranazetidine) compounds for the treatment of autoimmune disease
CN114761406B (zh) * 2019-12-03 2024-04-19 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的氢吡啶并[1,2-a]吡嗪化合物
DK4069729T3 (da) 2019-12-06 2025-04-07 Prec Biosciences Inc Optimerede, modificerede meganukleaser med specificitet for en genkendelsessekvens i hepatitis b-virusgenomet
EP4216949A4 (en) * 2020-09-28 2024-12-11 Yale University Selective agonists of 5-ht2a receptor and methods of use
EP4323369A1 (en) 2021-04-16 2024-02-21 Gilead Sciences, Inc. Thienopyrrole compounds
JP2024533374A (ja) 2021-09-10 2024-09-12 ギリアード サイエンシーズ， インコーポレイテッド チエノピロール化合物
CN115073369A (zh) * 2022-05-31 2022-09-20 汉瑞药业(荆门)有限公司 一种5-溴喹啉-8-甲醛的制备方法

Family Cites Families (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE812911C (de) 1945-03-12 1951-09-06 Rhone Poulenc Sa Verfahren zur Herstellung von neuen substituierten Derivaten des Piperidins
CH578535A5 (en) 1973-05-11 1976-08-13 Ciba Geigy Ag Quinoline-3-carboxylic acid derivs - with e.g. analgesic, antinociceptive, antiinflammatory and antiallergic props
US4933447A (en) 1987-09-24 1990-06-12 Ss Pharmaceutical Co., Ltd. Quinoline derivatives
FR2798656B1 (fr) 1999-09-17 2004-12-17 Aventis Pharma Sa Derives de la quinolyl propyl piperidine, leur preparation et les compositions qui les contiennent
MXPA04004443A (es) 2001-11-14 2004-08-11 Merck Patent Gmbh Derivados de pirazol.
GB0206033D0 (en) * 2002-03-14 2002-04-24 Pfizer Ltd Compounds useful in therapy
WO2003105850A1 (en) * 2002-06-18 2003-12-24 Abbott Laboratories 2-aminoquinolines as melanin concentrating hormone receptor antagonists
MXPA05001631A (es) 2002-08-12 2005-08-19 Takeda Pharmaceutical Derivado de benceno fusionado y su uso.
CA2505873A1 (en) * 2002-11-12 2004-05-27 Pfizer Products Inc. Quinoline derivatives
GB0227240D0 (en) 2002-11-21 2002-12-31 Glaxo Group Ltd Compounds
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
WO2005087749A1 (ja) 2004-03-15 2005-09-22 Kyowa Hakko Kogyo Co., Ltd. ２−アミノキナゾリン誘導体
US20060211752A1 (en) 2004-03-16 2006-09-21 Kohn Leonard D Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression
RU2006144863A (ru) 2004-05-17 2008-06-27 Акэдиа Фармасьютикалз Инк. (Us) Модуляторы андрогеновых рецепторов и способ лечения заболеваний с их помощью
US20070004679A1 (en) 2004-05-17 2007-01-04 Nathalie Schlienger Androgen receptor modulators and methods of treating disease using the same
EP1772454A4 (en) 2004-07-23 2009-02-25 Mitsubishi Tanabe Pharma Corp NITROGENIC CONDENSED BICYCLIC COMPOUND
GB0510810D0 (en) 2005-05-26 2005-06-29 Novartis Ag Organic compounds
GB0526042D0 (en) 2005-12-21 2006-02-01 Syngenta Participations Ag Chemical compounds
EP1987827A1 (en) 2006-02-20 2008-11-05 Takeda Pharmaceutical Company Limited Novel pharmaceutical
EP1903038A1 (de) 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren
WO2008037681A1 (en) 2006-09-26 2008-04-03 Glaxo Group Limited 5-{2-[4-(2-methyl-5-quinolinyl)-l-piperidinyl] ethyl} quinolinone derivatives as 5ht1a receptor modulators for treating sexual dysfunction, cognition impairement, psychotic disorders, anxiety, depression, etc.
CL2008001002A1 (es) 2007-04-11 2008-10-17 Actelion Pharmaceuticals Ltd Compuestos derivados de oxazolidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para preparar un medicamento para tratar una infeccion bacteriana.
CN101679191B (zh) 2007-06-05 2014-03-12 塞诺菲-安万特股份有限公司 二杂芳基环己烷衍生物、其制备方法、用途及含有它们的药用组合物
WO2009151845A1 (en) 2008-05-12 2009-12-17 Amnestix, Inc. Compounds for rho kinase inhibition and for improving learning and memory
AU2009266806A1 (en) 2008-07-03 2010-01-07 Exelixis Inc. CDK modulators
BRPI0918496A2 (pt) 2008-09-02 2019-09-24 Novartis Ag composto inibidor bicíclico de quinase, uso do mesmo, composição farmacêutica e método para inibir a atividade da quinase pim em uma célula
AU2009321867B2 (en) 2008-12-01 2015-12-10 Merck Patent Gmbh 2,5-Diamino-substituted pyrido[4,3-d]pyrimidines as autotaxin inhibitors against cancer
SG173617A1 (en) 2009-02-11 2011-09-29 Univ California Toll-like receptor modulators and treatment of diseases
US8415333B2 (en) 2009-02-24 2013-04-09 Respiratorious Ab Bronchodilating diazaheteroaryls
US20110015219A1 (en) 2009-07-16 2011-01-20 Mallinckrodt Inc. (+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof
US20120214803A1 (en) 2011-02-18 2012-08-23 Vifor (International) Ag Novel Sulfonaminoquinoline Hepcidin Antagonists
JP2013075834A (ja) 2011-09-29 2013-04-25 Kowa Co Ｔｌｒ９阻害活性を有するピラゾロピリミジン−７−アミン誘導体
WO2013060881A1 (en) 2011-10-27 2013-05-02 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg Pyridopyrimidines and their therapeutic use
WO2014086453A1 (en) 2012-12-07 2014-06-12 Merck Patent Gmbh Azaheterobicyclic compounds
MX355943B (es) 2013-06-26 2018-05-07 Abbvie Inc Carboxamidas primarias como inhibidores de btk.
NZ718190A (en) * 2013-08-23 2017-10-27 Neupharma Inc Substituted quinazolines for inhibiting kinase activity
MY192489A (en) * 2013-10-14 2022-08-23 Eisai R&D Man Co Ltd Selectively substituted quinoline compounds
EP3057948B1 (en) * 2013-10-14 2018-03-14 Eisai R&D Management Co., Ltd. Selectively substituted quinoline derivatives
CN104557913B (zh) 2013-10-28 2017-02-08 上海汇伦生命科技有限公司 吡啶并嘧啶类化合物，其制备方法和用途
CA2933466A1 (en) 2013-12-13 2015-06-18 Takeda Pharmaceutical Company Limited Pyrrolo[3,2-c]pyridine derivatives as tlr inhibitors
EP3083618B1 (en) 2013-12-17 2018-02-21 Pfizer Inc Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors
WO2015120111A2 (en) 2014-02-05 2015-08-13 Stereokem, Inc. (Usa) Expedient synthesis of sitagliptin
CN104945377A (zh) 2014-03-24 2015-09-30 南京明德新药研发股份有限公司 作为smo抑制剂的喹啉衍生物
JP6377245B2 (ja) 2014-03-24 2018-08-22 グアンドン ジョンシェン ファーマシューティカル カンパニー リミテッド Ｓｍｏ阻害剤としてのキノリン誘導体
PL3134402T3 (pl) 2014-04-22 2020-11-02 F.Hoffmann-La Roche Ag Związki 4-amino-imidazochinolinowe
GB201411236D0 (en) 2014-06-25 2014-08-06 Takeda Pharmaceutical Novel compounds
AU2015341913B2 (en) 2014-11-03 2020-07-16 Iomet Pharma Ltd Pharmaceutical compound
UY36390A (es) * 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
JP2017533925A (ja) 2014-11-13 2017-11-16 グラクソスミスクライン バイオロジカルズ ソシエテ アノニム アレルギー性疾患又は他の炎症状態の治療に有用なアデニン誘導体
WO2016087593A1 (en) 2014-12-05 2016-06-09 Syngenta Participations Ag Novel fungicidal quinolinylamidines
MA41169A (fr) 2014-12-17 2017-10-24 Acraf Composés antibactériens à large spectre d'activité
US10167270B2 (en) 2015-07-01 2019-01-01 Northwestern University Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity
WO2017031427A1 (en) 2015-08-19 2017-02-23 3-V Biosciences, Inc. COMPOUNDS AND METHODS FOR INHIBITING mTOR
SG11201804170RA (en) 2015-12-17 2018-06-28 Merck Patent Gmbh Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
US20190119236A1 (en) * 2016-02-23 2019-04-25 Portola Pharmaceuticals, Inc. Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9)
EP3497094B1 (en) 2016-08-08 2023-02-15 Merck Patent GmbH Tlr7/8 antagonists and uses thereof
EP3558984B1 (en) * 2016-12-20 2023-08-02 FMC Corporation Fungicidal oxadiazoles
US11050028B2 (en) * 2017-01-24 2021-06-29 Universal Display Corporation Organic electroluminescent materials and devices
AU2018302026B2 (en) 2017-07-18 2022-04-07 Merck Patent Gmbh TLR7/8 antagonists and uses thereof
RU2020123151A (ru) 2017-12-19 2022-01-20 Мерк Патент Гмбх Антагонисты tlr7/8 и их применение
KR20210040085A (ko) 2018-07-31 2021-04-12 메르크 파텐트 게엠베하 Tlr7/8 안타고니스트 및 이의 용도

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AU2017311047A1 (en) 2019-03-21
KR102635885B1 (ko) 2024-02-14
US20240383876A1 (en) 2024-11-21
WO2018031434A1 (en) 2018-02-15
CN109563075B (zh) 2022-09-30
SG11201900947RA (en) 2019-02-27
BR112019000696A2 (pt) 2019-04-24
EP4198031A1 (en) 2023-06-21
US20210002255A1 (en) 2021-01-07
CN109563075A (zh) 2019-04-02
US10947214B2 (en) 2021-03-16
US20180037570A1 (en) 2018-02-08
JP7125385B2 (ja) 2022-08-24
RU2758686C2 (ru) 2021-11-01
KR20240019867A (ko) 2024-02-14
DK3497094T3 (da) 2023-05-15
CA3033240A1 (en) 2018-02-15
AU2017311047B2 (en) 2021-07-22
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US20210002256A1 (en) 2021-01-07
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US11512069B2 (en) 2022-11-29
MX390698B (es) 2025-03-11
RU2019105719A (ru) 2020-09-11
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RU2019105719A3 (enExample) 2020-10-16

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