EA200971143A1 - Бензамидные mglur5 позитивные аллостерические модуляторы и способы их получения и применения - Google Patents

Бензамидные mglur5 позитивные аллостерические модуляторы и способы их получения и применения

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Publication number
EA200971143A1
EA200971143A1 EA200971143A EA200971143A EA200971143A1 EA 200971143 A1 EA200971143 A1 EA 200971143A1 EA 200971143 A EA200971143 A EA 200971143A EA 200971143 A EA200971143 A EA 200971143A EA 200971143 A1 EA200971143 A1 EA 200971143A1
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EA
Eurasian Patent Office
Prior art keywords
methods
compounds
positive allosteric
allosteric modulators
benzamide
Prior art date
Application number
EA200971143A
Other languages
English (en)
Russian (ru)
Inventor
П. Джеффри Конн
Крейг У. Линдсли
Чарльз Дэвид Уивер
Элис Л. Родригес
Коллин М. Нисвендер
Кэрри К. Джоунс
Ричард Уилльямс
Original Assignee
Вандербилт Юниверсити
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Publication date
Application filed by Вандербилт Юниверсити filed Critical Вандербилт Юниверсити
Publication of EA200971143A1 publication Critical patent/EA200971143A1/ru

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    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010513283A (ja) 2006-12-15 2010-04-30 アボット・ラボラトリーズ 新規なオキサジアゾール化合物
US8853392B2 (en) 2007-06-03 2014-10-07 Vanderbilt University Benzamide mGluR5 positive allosteric modulators and methods of making and using same
US8034806B2 (en) 2007-11-02 2011-10-11 Vanderbilt University Bicyclic mGluR5 positive allosteric modulators and methods of making and using same
GB0811643D0 (en) 2008-06-25 2008-07-30 Cancer Rec Tech Ltd New therapeutic agents
TW201028421A (en) * 2009-01-15 2010-08-01 Abbott Lab Novel benzenesulfonamides as calcium channel blockers
US8389536B2 (en) 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
US8586581B2 (en) 2009-12-17 2013-11-19 Hoffmann-La Roche Inc Ethynyl compounds useful for treatment of CNS disorders
NZ600605A (en) 2009-12-18 2013-08-30 Janssen Pharmaceutica Nv Bicyclic thiazoles as allosteric modulators of mglur5 receptors
CA2784830C (en) 2009-12-18 2018-03-27 Sunovion Pharmaceuticals Inc. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
US9174953B2 (en) 2009-12-18 2015-11-03 Janssen Pharmaceutica Nv Bicyclic thiazoles as allosteric modulators of mGluR5 receptors
EA021568B1 (ru) 2009-12-23 2015-07-30 Такеда Фармасьютикал Компани Лимитед Конденсированные гетероароматические пирролидиноны как ингибиторы syk
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
CN103037693A (zh) * 2010-05-24 2013-04-10 范德比尔特大学 作为mglur5正向变构调节剂的取代的6-甲基烟酰胺
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
US8772300B2 (en) 2011-04-19 2014-07-08 Hoffmann-La Roche Inc. Phenyl or pyridinyl-ethynyl derivatives
SG194120A1 (en) 2011-04-26 2013-11-29 Hoffmann La Roche Ethynyl derivatives as positive allosteric modulators of the mglur5
PH12013501928A1 (en) 2011-04-26 2013-11-25 Hoffmann La Roche Pyrazolidin-3-one derivatives
JP6026525B2 (ja) 2011-06-22 2016-11-16 武田薬品工業株式会社 置換6−アザ−イソインドリン−1−オン誘導体
US20130123254A1 (en) 2011-09-30 2013-05-16 Barbara Biemans Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification
UA110862C2 (uk) 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
UA110995C2 (uk) 2011-10-07 2016-03-10 Ф. Хоффманн-Ля Рош Аг Етинільні похідні як модулятори метаботропного глутаматного рецептора
EP3312160B1 (en) * 2011-12-21 2020-03-18 Novira Therapeutics Inc. Hepatitis b antiviral agents
PT3495367T (pt) 2012-06-13 2020-11-12 Incyte Holdings Corp Compostos tricíclicos substituídos como inibidores de fgfr
MY167810A (en) 2012-07-17 2018-09-26 Hoffmann La Roche Arylethynyl derivatives
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
UA113223C2 (xx) * 2012-08-13 2016-12-26 Арилетинілпіримідини
CN104684911B (zh) 2012-09-27 2017-05-10 霍夫曼-拉罗奇有限公司 芳基乙炔基衍生物
EA025667B1 (ru) * 2012-10-18 2017-01-30 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ЭТИНИЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРА mGluR5
JP5989253B2 (ja) * 2012-10-18 2016-09-07 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft mGluR5受容体活性のモジュレータとしてのエチニル誘導体
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
MY183953A (en) * 2013-09-25 2021-03-17 Hoffmann La Roche Ethynyl derivatives
TWI649310B (zh) * 2014-01-10 2019-02-01 赫孚孟拉羅股份公司 乙炔基衍生物
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
TWI713497B (zh) 2015-02-26 2020-12-21 南韓商愛思開生物製藥股份有限公司 咪唑并嘧啶及咪唑并三衍生物及包含該衍生物之醫藥組成物
CN106146391A (zh) * 2015-04-15 2016-11-23 中国科学院上海药物研究所 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途
UA120309C2 (uk) 2015-06-03 2019-11-11 Ф. Хоффманн-Ля Рош Аг Етинільні похідні
EP3319968A1 (en) 2015-07-06 2018-05-16 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
EP3939973A1 (en) 2015-07-06 2022-01-19 Alkermes, Inc. Hetero-halo inhibitors of histone deacetylase
SI3322701T1 (sl) 2015-07-15 2019-08-30 F. Hoffmann-La Roche Ag Derivati etinila kot modulatorji metabotropnega receptorja za glutamat
GB201517216D0 (en) 2015-09-29 2015-11-11 Cancer Res Technology Ltd And Astex Therapeutics Ltd Pharmaceutical compounds
GB201517217D0 (en) 2015-09-29 2015-11-11 Astex Therapeutics Ltd And Cancer Res Technology Ltd Pharmaceutical compounds
ES2826389T3 (es) 2016-07-18 2021-05-18 Hoffmann La Roche Derivados de etinilo
RS62959B1 (sr) 2017-01-11 2022-03-31 Alkermes Inc Biciklični inhibitori histon-deacetilaze
GB201704966D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
GB201704965D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
SG11202000970WA (en) 2017-08-07 2020-02-27 Rodin Therapeutics Inc Bicyclic inhibitors of histone deacetylase
IL312465A (en) 2018-05-04 2024-06-01 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
JP7568512B2 (ja) 2018-05-04 2024-10-16 インサイト・コーポレイション Fgfr阻害剤の塩
DE102019200805A1 (de) * 2019-01-23 2020-07-23 Henkel Ag & Co. Kgaa Neue fluoreszierende Materialien auf Basis von Phthalimiden
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
JP2023505257A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Fgfr阻害剤の誘導体
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
CR20230057A (es) 2020-07-02 2023-08-15 Incyte Corp Compuestos tríciclicos de urea como inhibidores de jak2 v617f
JP2023536137A (ja) * 2020-07-29 2023-08-23 ヴィヴォゾン・インコーポレイテッド mGluR5及び5-HT2A受容体の二重調節剤及びその使用
WO2022040002A1 (en) 2020-08-17 2022-02-24 Aligos Therapeutics, Inc. Methods and compositions for targeting pd-l1
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
US11958861B2 (en) 2021-02-25 2024-04-16 Incyte Corporation Spirocyclic lactams as JAK2 V617F inhibitors
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含fgfr抑制劑及nectin-4靶向劑之組合療法
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Fgfr阻害剤としての三環式ヘテロ環
CN116514790A (zh) * 2022-01-24 2023-08-01 华东师范大学 一类靶向于stat3的三联芳香杂环哌嗪类小分子有机化合物及其应用
AU2023213484A1 (en) * 2022-01-27 2024-07-25 Vivozon,Inc. Pharmaceutical composition for preventing or treating mental disorder
US12084430B2 (en) 2022-03-17 2024-09-10 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW544448B (en) * 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
GB9823871D0 (en) * 1998-10-30 1998-12-23 Pharmacia & Upjohn Spa 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents
CA2452159A1 (en) * 2001-07-23 2003-02-06 Galileo Laboratories, Inc. Cytoprotective compounds, pharmaceutical and cosmetic formulations, and methods
AU2003249983A1 (en) * 2002-07-18 2004-02-09 Actelion Pharmaceuticals Ltd Piperidines useful for the treatment of central nervous system disorders
WO2004087048A2 (en) * 2003-03-26 2004-10-14 Merck & Co. Inc. Benzamide modulators of metabotropic glutamate receptors
AR046276A1 (es) * 2003-10-07 2005-11-30 Renovis Inc Derivados de amida como ligandos de canales ionicos y composiciones farmaceuticas y metodos que los utilizan.
GB0324159D0 (en) * 2003-10-15 2003-11-19 Glaxo Group Ltd Novel compounds
GB0325956D0 (en) * 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
CN1950372A (zh) * 2004-05-10 2007-04-18 万有制药株式会社 咪唑并吡啶化合物
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
JP2008531690A (ja) * 2005-02-28 2008-08-14 レノビス, インコーポレイテッド イオンチャネルリガンドとしてのアミド誘導体並びにそれを使用する医薬組成物及び方法

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