SG11201900947RA - Tlr7/8 antagonists and uses thereof - Google Patents

Tlr7/8 antagonists and uses thereof

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Publication number
SG11201900947RA
SG11201900947RA SG11201900947RA SG11201900947RA SG11201900947RA SG 11201900947R A SG11201900947R A SG 11201900947RA SG 11201900947R A SG11201900947R A SG 11201900947RA SG 11201900947R A SG11201900947R A SG 11201900947RA SG 11201900947R A SG11201900947R A SG 11201900947RA
Authority
SG
Singapore
Prior art keywords
international
massachusetts
pct
tlr7
antagonists
Prior art date
Application number
SG11201900947RA
Other languages
English (en)
Inventor
Brian A Sherer
Xiaoling Chen
Esther Cleary
Nadia Brugger
Original Assignee
Merck Patent Gmbh
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 filed Critical Merck Patent Gmbh
Publication of SG11201900947RA publication Critical patent/SG11201900947RA/en

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    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/53751,4-Oxazines, e.g. morpholine
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US201662371917P 2016-08-08 2016-08-08
PCT/US2017/045671 WO2018031434A1 (en) 2016-08-08 2017-08-07 Tlr7/8 antagonists and uses thereof

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Families Citing this family (22)

* 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
WO2018031434A1 (en) 2016-08-08 2018-02-15 Merck Patent Gmbh Tlr7/8 antagonists and uses thereof
CR20190181A (es) 2016-10-14 2019-08-21 Prec Biosciences Inc Meganucleasas diseñadas específicamente para el reconocimiento de secuencias en el genoma del virus de la hepatitis 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
AU2018392213B2 (en) 2017-12-20 2021-03-04 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein
JP7098748B2 (ja) 2017-12-20 2022-07-11 インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール,ヴイ.ヴイ.アイ. Stingアダプタータンパク質を活性化するホスホン酸結合を有する2’3’環状ジヌクレオチド
JP7328977B2 (ja) 2018-02-12 2023-08-17 エフ. ホフマン-ラ ロシュ アーゲー ウイルス感染の処置および予防のための新規のスルホン化合物および誘導体
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
US11142750B2 (en) 2018-04-12 2021-10-12 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome
US20210371432A1 (en) * 2018-06-05 2021-12-02 Hoffmann-La Roche Inc. Tetrahydro-1H-pyrazino[2,1-a]isoindolylquinoline Compounds for the Treatment of Autoimmune Disease
EP3807270B1 (en) 2018-06-12 2023-09-13 F. Hoffmann-La Roche AG Novel heteroaryl heterocyclyl compounds for the treatment of autoimmune disease
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
WO2020048583A1 (en) 2018-09-04 2020-03-12 F. Hoffmann-La Roche Ag Benzothiazole compounds for the treatment of autoimmune diseases
CN112654618A (zh) 2018-09-06 2021-04-13 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的新型环脒化合物
JP2022509260A (ja) 2018-11-30 2022-01-20 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用
WO2021099284A1 (en) * 2019-11-19 2021-05-27 F. Hoffmann-La Roche Ag Hydro-1h-pyrrolo[1,2-a]pyrazine compounds for the treatment of autoimmune disease
WO2021099285A1 (en) * 2019-11-19 2021-05-27 F. Hoffmann-La Roche Ag Triazatricycle compounds for the treatment of autoimmune disease
JP2023505159A (ja) * 2019-12-03 2023-02-08 エフ.ホフマン-ラ ロシュ アーゲー 自己免疫疾患の処置のためのヒドロピリド[1,2-a]ピラジン化合物
EP4323369A1 (en) 2021-04-16 2024-02-21 Gilead Sciences, Inc. Thienopyrrole compounds
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
JP2005511625A (ja) 2001-11-14 2005-04-28 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフトング 向精神薬としてのピラゾール誘導体
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
CA2495383A1 (en) 2002-08-12 2004-02-26 Takeda Pharmaceutical Company Limited Fused benzene derivative and use
EP1562908A1 (en) 2002-11-12 2005-08-17 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
EP1726584A4 (en) * 2004-03-15 2009-05-13 Kyowa Hakko Kirin Co Ltd 2-AMINOCHINAZOLINDERIVAT
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
US20070004679A1 (en) 2004-05-17 2007-01-04 Nathalie Schlienger Androgen receptor modulators and methods of treating disease using the same
MXPA06013329A (es) 2004-05-17 2007-02-22 Acadia Pharm Inc Moduladores del receptor androgeno, y metodo para tratar enfermedades en el que se utilizan los mismos.
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
US20090042857A1 (en) 2006-02-20 2009-02-12 Masuo Yamaoka 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
US20100004452A1 (en) 2006-09-26 2010-01-07 Barbara Bertani 5-quinolinone derivatives as 5ht1a receptor modulators for treating sexual dysfunction, cognition impairment, 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.
PT2164825E (pt) * 2007-06-05 2014-06-24 Sanofi Sa Derivados de di(hetero)arilciclo-hexano, sua preparação, sua utilização e composições farmacêuticas compreendendo os mesmos
MX2010012104A (es) * 2008-05-12 2011-04-05 Amnestix Inc Compuestos para mejorar el aprendizaje y la memoria.
CA2728559A1 (en) 2008-07-03 2010-01-07 Exelixis Inc. Cdk modulators
EP2342190A1 (en) 2008-09-02 2011-07-13 Novartis AG Bicyclic kinase inhibitors
WO2010063352A1 (en) 2008-12-01 2010-06-10 Merck Patent Gmbh 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer
EP2607365A1 (en) 2009-02-11 2013-06-26 The Regents of The University of California Toll-like receptor modulators and treatment of diseases
EP2401275B1 (en) 2009-02-24 2013-07-24 Respiratorius AB Naphthyridine derivatives having bronchodilating activity
WO2011009015A1 (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
DK3013337T3 (en) 2013-06-26 2019-02-25 Abbvie Inc PRIMARY CARBOXAMIDES AS BTK INHIBITORS
CA2921410C (en) * 2013-08-23 2023-03-28 Neupharma, Inc. Quinazoline derivatives, compositions and their use as kinase inhibitors
WO2015057659A1 (en) * 2013-10-14 2015-04-23 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
BR112016008378B1 (pt) * 2013-10-14 2022-11-08 Eisai R&D Management Co., Ltd Compostos de quinolina seletivamente substituídos ou sal dos mesmos, e composição farmacêutica contendo os ditos compostos
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
US9643967B2 (en) 2013-12-13 2017-05-09 Takeda Pharmaceutical Company Limited Pyrrolo[3,2-c]pyridine derivatives as TLR inhibitors
JP6487921B2 (ja) 2013-12-17 2019-03-20 ファイザー・インク LRRK2阻害薬としての新規の3,4−二置換−1H−ピロロ[2,3−b]ピリジンおよび4,5−二置換−7H−ピロロ[2,3−c]ピリダジン
US9938282B2 (en) 2014-02-05 2018-04-10 Stereokem, Inc. Expedient synthesis of sitagliptin
US9938292B2 (en) 2014-03-24 2018-04-10 Guangdong Zhongsheng Pharmaceutical Co., Ltd Quinoline derivatives as SMO inhibitors
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
ES2804101T3 (es) 2014-04-22 2021-02-03 Hoffmann La Roche Compuestos de 4-amino-imidazoquinolina
GB201411236D0 (en) 2014-06-25 2014-08-06 Takeda Pharmaceutical Novel compounds
CA2965741C (en) 2014-11-03 2022-05-17 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
BE1023340B1 (fr) * 2014-11-13 2017-02-08 Glaxosmithkline Biologicals S.A. Composes
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
EP3317265A4 (en) 2015-07-01 2019-04-17 Northwestern University SUBSTITUTED CHINAZOLIN 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)
WO2018031434A1 (en) 2016-08-08 2018-02-15 Merck Patent Gmbh Tlr7/8 antagonists and uses thereof
WO2018118781A1 (en) * 2016-12-20 2018-06-28 Fmc Corporation Fungicidal oxadiazoles
US11050028B2 (en) * 2017-01-24 2021-06-29 Universal Display Corporation Organic electroluminescent materials and devices
DK3655401T3 (da) 2017-07-18 2023-10-30 Merck Patent Gmbh Tlr7/8-antagonister og anvendelser deraf
RU2020123151A (ru) 2017-12-19 2022-01-20 Мерк Патент Гмбх Антагонисты tlr7/8 и их применение
AU2019313441B2 (en) 2018-07-31 2024-05-23 Merck Patent Gmbh TLR7/8 antagonists and uses thereof

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