HK1214527A1 - 酪蛋白激酶1δ(CK1δ)抑制剂 - Google Patents

酪蛋白激酶1δ(CK1δ)抑制剂 Download PDF

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Publication number
HK1214527A1
HK1214527A1 HK16102571.5A HK16102571A HK1214527A1 HK 1214527 A1 HK1214527 A1 HK 1214527A1 HK 16102571 A HK16102571 A HK 16102571A HK 1214527 A1 HK1214527 A1 HK 1214527A1
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Hong Kong
Prior art keywords
alkyl
aryl
compound
group
heteroaryl
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HK16102571.5A
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English (en)
Chinese (zh)
Inventor
Joseph M. Sheridan
Jonathan R. Heal
William D.O. Hamilton
Ian Pike
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Electrophoretics Limited
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Priority claimed from GBGB1021161.3A external-priority patent/GB201021161D0/en
Priority claimed from GBGB1109162.6A external-priority patent/GB201109162D0/en
Application filed by Electrophoretics Limited filed Critical Electrophoretics Limited
Publication of HK1214527A1 publication Critical patent/HK1214527A1/zh

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Families Citing this family (236)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2635581C (en) 2005-12-28 2017-02-28 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
DK2240451T3 (da) 2008-01-04 2017-11-20 Intellikine Llc Isoquinolinonderivater substitueret med en purin, der er anvendelig som pi3k-inhibitorer
CN102482278B (zh) 2009-06-29 2015-04-22 因塞特公司 作为pi3k抑制剂的嘧啶酮类
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
JP2013523766A (ja) * 2010-03-31 2013-06-17 グラクソ グループ リミテッド キナーゼ阻害剤としてのイミダゾリル‐イミダゾール
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
ES2650744T3 (es) * 2010-12-14 2018-01-22 Electrophoretics Limited Inhibidores de la caseína quinasa 1 delta (CK1delta)
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
DK2663309T3 (en) 2011-01-10 2017-06-19 Infinity Pharmaceuticals Inc METHODS FOR PRODUCING ISOQUINOLINONES AND SOLID FORMS OF ISOQUINOLINONES
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
GB201104267D0 (en) 2011-03-14 2011-04-27 Cancer Rec Tech Ltd Pyrrolopyridineamino derivatives
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
AR087701A1 (es) 2011-08-31 2014-04-09 Japan Tobacco Inc Derivados de pirazol con actividad inhibidora de sglt1
TWI648277B (zh) 2011-09-02 2019-01-21 美商英塞特控股公司 作為pi3k抑制劑之雜環基胺
SG2014010417A (en) 2011-10-07 2014-06-27 Takeda Pharmaceutical 1 - arylcarbonyl - 4 - oxy - piperidine compounds useful for the treatment of neurodegenerative diseases
US9266840B2 (en) 2011-10-18 2016-02-23 Astellas Pharma Inc. Bicyclic heterocyclic compound
AR090037A1 (es) 2011-11-15 2014-10-15 Xention Ltd Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio
PL2785692T3 (pl) 2011-12-01 2018-02-28 Chemocentryx, Inc. Podstawione aniliny jako antagoniści ccr(4)
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
PL2861566T3 (pl) 2012-06-13 2017-06-30 F.Hoffmann-La Roche Ag Nowy diazaspirocykloalkan i azaspirocykloalkan
UA125503C2 (uk) 2012-06-13 2022-04-13 Інсайт Холдинґс Корпорейшн Заміщені трициклічні сполуки як інгібітори fgfr
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
US9630976B2 (en) 2012-07-03 2017-04-25 Ono Pharmaceutical Co., Ltd. Compound having agonistic activity on somatostatin receptor, and use thereof for medical purposes
WO2014009891A1 (en) * 2012-07-11 2014-01-16 Piramal Enterprises Limited Heterocyclic compounds for use in the treatment of cancers
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
DK2888010T3 (da) 2012-08-22 2021-06-28 Univ Cornell Fremgangsmåder til at hæmme fascin
US9328078B2 (en) * 2012-08-24 2016-05-03 Treventis Corporation Benzofurazan anti-amyloid compounds and methods
CN102850341B (zh) * 2012-09-05 2015-02-18 浙江工业大学 一种噻二唑类化合物及其制备与应用
GB201216018D0 (en) 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Pharmacologically active compounds
PL2900669T3 (pl) 2012-09-25 2020-01-31 F. Hoffmann-La Roche Ag Pochodne heksahydropirolo[3,4-C]pirolu i związki pokrewne jako inhibitory autotaksyny (ATX) oraz inhibitory produkcji kwasu lizofosfatydowego (LPA) do leczenia np. chorób nerek
CN103739594A (zh) * 2012-10-17 2014-04-23 南京大学 一类含吡嗪环和三氮唑结构的席夫碱类衍生物及其制法
KR102229478B1 (ko) 2012-11-01 2021-03-18 인피니티 파마슈티칼스, 인코포레이티드 Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료
BR112015011497B1 (pt) 2012-11-27 2023-01-10 Thomas Helledays Stiftelse För Medicinsk Forskning Composto, e, formulação farmacêutica
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US20150329540A1 (en) 2012-12-28 2015-11-19 Shin Nippon Biomedical Laboratories, Ltd. Oct3 activity inhibitor containing imidazopyridine derivative as active component, and oct3 detection agent
CA2900779C (en) * 2013-02-11 2021-10-26 The Regents Of The University Of California Compositions and methods for treating neurodegenerative diseases and cardiomyopathy
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
EP2970306A4 (en) 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED 6.5-CONDENSED BICYCLIC HETEROARYL COMPOUNDS
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
CA2906194A1 (en) 2013-03-15 2014-09-18 Whitehead Institute For Biomedical Research Benzimidazole derivatives and uses thereof
MY181497A (en) 2013-04-19 2020-12-23 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
US9797882B2 (en) 2013-07-09 2017-10-24 The Translational Genomics Research Institute Method of screening for a compound for inhibitory activity of FN14-tweak interaction
WO2015006508A2 (en) 2013-07-09 2015-01-15 The Translational Genomics Research Institute Compositions and methods of screening for compounds that modulate activity at a tweak binding site on a crd of fn14
TWI649308B (zh) 2013-07-24 2019-02-01 小野藥品工業股份有限公司 喹啉衍生物
GB201314452D0 (en) 2013-08-13 2013-09-25 Ostara Biomedical Ltd Embryo implantation
RU2570907C2 (ru) * 2013-10-21 2015-12-20 Автономная Некоммерческая Организация "Научно-Исследовательский Центр Биотехнологии Антибиотиков И Других Биологически Активных Веществ "Биоан" Производные 3-ациламинопиридин-2(1h)-она, применимые как ингибиторы серин-треониновой протеинкиназы gsk3b в качестве лекарственных препаратов для лечения диабета ii типа.
CN106163527A (zh) 2013-11-22 2016-11-23 Cl生物科技有限责任公司 用于治疗和预防骨质疏松症的胃泌素拮抗剂
HUE036117T2 (hu) 2013-11-26 2018-06-28 Hoffmann La Roche Oktahidro-ciklobuta[1,2-C;3,4-C']dipirrol származékok, mint autotaxin inhibitorok
GB201321738D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic Agents
WO2015106025A1 (en) 2014-01-09 2015-07-16 The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone Substituted benzoxazine and related compounds
SG11201605342UA (en) 2014-01-29 2016-08-30 Glaxosmithkline Ip Dev Ltd Compounds
CN105980388B (zh) 2014-01-29 2018-01-16 葛兰素史密斯克莱知识产权发展有限公司 化合物
EP3104706B1 (en) 2014-02-11 2022-03-23 Mitokinin, Inc. Compositions and methods using the same for treatment of neurodegenerative and mitochondrial disease
US9670210B2 (en) 2014-02-13 2017-06-06 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
TWI720451B (zh) 2014-02-13 2021-03-01 美商英塞特控股公司 作為lsd1抑制劑之環丙胺
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
DK3107902T3 (da) 2014-02-20 2021-05-03 Cornell Univ Cornell Center For Technology Enterprise & Commercialization Cctec Forbindelser og fremgangsmåder til at hæmme fascin
RS58976B1 (sr) * 2014-02-27 2019-08-30 Treventis Corp Antiamiloidna jedinjenja koja sadrže benzofuran
EA037928B1 (ru) 2014-03-26 2021-06-08 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
JP6554481B2 (ja) 2014-03-26 2019-07-31 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft オートタキシン(atx)及びリゾホスファチジン酸(lpa)産生の阻害剤としての縮合[1,4]ジアゼピン化合物
US20170029388A1 (en) * 2014-04-11 2017-02-02 Intercontinental Great Brands Llc Treatment of Neurodegenerative Diseases with Asparagine Endopeptidase (AEP) Inhibitors and Compositions Related Thereto
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
WO2015158313A1 (en) * 2014-04-19 2015-10-22 Sunshine Lake Pharma Co., Ltd. Sulfonamide derivatives and pharmaceutical applications thereof
RU2659070C9 (ru) * 2014-04-23 2018-08-24 Дарт Нейросайенс (Кайман) Лтд. ЗАМЕЩЕННЫЕ [1,2,4]ТРИАЗОЛО[1,5-a]ПИРИМИДИН-7-ИЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE2
WO2015170218A1 (en) 2014-05-07 2015-11-12 Pfizer Inc. Tropomyosin-related kinase inhibitors
CN104059060B (zh) * 2014-05-30 2017-08-01 西安交通大学 一种5‑(1h‑吲哚‑3‑亚甲基)‑1,3‑噻唑烷‑4‑酮类衍生物及其合成方法和应用
JP6635949B2 (ja) 2014-06-04 2020-01-29 トーマス・ヘレデイズ・スティフテルス・フォー・メディシンスク・フォルスクニング 炎症性および自己免疫性の病気の処置のためのmth1阻害剤
AU2015268961B9 (en) 2014-06-04 2019-10-10 Thomas Helledays Stiftelse For Medicinsk Forskning MTH1 inhibitors for treatment of cancer
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
ES2927587T3 (es) 2014-07-31 2022-11-08 Merck Patent Gmbh Derivados de indolizina que se pueden aplicar a enfermedades neurodegenerativas
US20170204089A1 (en) 2014-08-04 2017-07-20 Drexel University Novel compounds and methods of treating or ameliorating an il-1r-mediated disease or disorder using same
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
RU2749213C2 (ru) 2014-10-07 2021-06-07 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
GB201419579D0 (en) * 2014-11-03 2014-12-17 Iomet Pharma Ltd Pharmaceutical compound
US10239882B2 (en) 2014-11-05 2019-03-26 Dart Neuroscience (Cayman) Ltd. Substituted 5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-amine compounds as PDE2 inhibitors
ES2749726T3 (es) 2014-12-25 2020-03-23 Ono Pharmaceutical Co Derivado de quinolina
GB201501302D0 (en) 2015-01-27 2015-03-11 Ostara Biomedical Ltd Embryo implantation
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CA3285092A1 (en) 2015-02-27 2025-11-29 Incyte Holdings Corporation Salts of pi3k inhibitor and processes for their preparation
JP6827948B2 (ja) 2015-03-23 2021-02-10 ザ ユニヴァーシティー オブ メルボルン 呼吸器疾患の治療
MX373154B (es) 2015-04-03 2020-04-22 Incyte Holdings Corp Compuestos heterocíclicos como inhibidores de demetilasa 1 específica de lisina (lsd1).
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
ES2898922T3 (es) * 2015-04-30 2022-03-09 Musc Found For Res Dev Compuestos de oxindol y composiciones farmacéuticas de los mismos
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
GB201508276D0 (en) 2015-05-14 2015-06-24 Electrophoretics Ltd A casein kinase 1 delta inhibitor
GB201509134D0 (en) 2015-05-28 2015-07-15 Electrophoretics Ltd Biomolecules involved in Alzheimer's disease
MX2017015456A (es) * 2015-06-01 2018-11-29 Bantam Pharmaceutical Llc Compuestos de pirazol y pirrol sustituidos y metodos para su uso por inhibición de iniciación de traducción y tratamiento de enfermedades y trastornos relacionados con ellos.
WO2016202758A1 (en) 2015-06-18 2016-12-22 Bayer Pharma Aktiengesellschaft Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds
WO2016202756A1 (en) 2015-06-18 2016-12-22 Bayer Pharma Aktiengesellschaft Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds
WO2017004405A1 (en) * 2015-07-01 2017-01-05 Northwestern University Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity
WO2017000277A1 (en) * 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Substituted triazolo bicycliccompounds as pde2 inhibitors
LT3334709T (lt) 2015-08-12 2025-03-10 Incyte Holdings Corporation Lsd1 inhibitoriaus druskos
CN105061462B (zh) * 2015-08-18 2017-05-24 沈阳药科大学 含有酰胺的四氢苯并[4,5]噻吩并[2,3‑d]嘧啶类化合物及其应用
CR20180058A (es) * 2015-09-04 2018-02-26 Hoffmann La Roche Nuevos derivados de fenoximetilo
KR20180052635A (ko) 2015-09-18 2018-05-18 가켄 세이야쿠 가부시키가이샤 바이아릴 유도체 및 이를 포함하는 약제
CN107922412B (zh) 2015-09-24 2021-02-23 豪夫迈·罗氏有限公司 作为atx抑制剂的二环化合物
MX2017015034A (es) 2015-09-24 2018-04-13 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca).
EP3353178B1 (en) 2015-09-24 2021-07-14 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
KR20180054830A (ko) 2015-09-24 2018-05-24 에프. 호프만-라 로슈 아게 오토탁신(atx) 억제제로서의 이환형 화합물
JP6740354B2 (ja) * 2015-10-05 2020-08-12 ザ トラスティーズ オブ コロンビア ユニバーシティー イン ザ シティー オブ ニューヨーク オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法
GB201517523D0 (en) 2015-10-05 2015-11-18 Ostara Biomedical Ltd Methods and compositions for managing reproduction
WO2017063966A1 (en) 2015-10-13 2017-04-20 Bayer Pharma Aktiengesellschaft Substituted 2-(1h-pyrazol-1-yl)-benzothiazole compounds
SG11201803605YA (en) 2015-11-02 2018-05-30 Janssen Pharmaceutica Nv [1,2,4]TRIAZOLO[1,5-a]PYRIMIDIN-7-YL COMPOUND
EP3388420B1 (en) * 2015-12-07 2022-06-22 Hinova Pharmaceuticals Inc. Quinoline compounds, preparation method thereof, and use thereof as urate transporter inhibitor drug
WO2017106367A1 (en) * 2015-12-15 2017-06-22 D.E. Shaw Research, Llc Method of treating neurodegenerative disorders by rescuing alpha-synuclein toxicity
CN107033087B (zh) * 2016-02-04 2020-09-04 西华大学 1h-吲唑-4-胺类化合物及其作为ido抑制剂的用途
WO2017133258A1 (zh) * 2016-02-04 2017-08-10 西华大学 1h-吲唑类衍生物及其作为ido抑制剂的用途
CN107840826B (zh) * 2016-09-19 2021-07-09 西华大学 1h-吲唑类衍生物及其作为ido抑制剂的用途
UA125559C2 (uk) 2016-04-22 2022-04-20 Інсайт Корпорейшн Композиції інгібітора lsd1
AU2017275657B2 (en) 2016-06-02 2021-08-19 Novartis Ag Potassium channel modulators
HUE057838T2 (hu) 2016-06-07 2022-06-28 Jacobio Pharmaceuticals Co Ltd SHP2 inhibitorokként hasznos új heterociklusos származékok
IL263680B2 (en) 2016-06-24 2025-10-01 Infinity Pharmaceuticals Inc PI3K inhibitors for use in combination with a second therapeutic agent for the treatment, management or prevention of cancer
EP3484876A1 (en) 2016-07-14 2019-05-22 Pfizer Inc Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme
WO2018030762A1 (ko) * 2016-08-09 2018-02-15 세종대학교산학협력단 Ampk 억제기능에 기반한 뇌졸중 치료용 약학적 조성물
AU2017311691B2 (en) 2016-08-18 2021-12-02 Vidac Pharma Ltd. Piperazine derivatives, pharmaceutical compositions and methods of use thereof
PE20190607A1 (es) 2016-09-02 2019-04-23 Ironwood Pharmaceuticals Inc Estimuladores de sgc
CN106432235B (zh) * 2016-10-19 2018-02-02 南通大学 靶向CDK和DNA的β‑咔啉衍生物及其制备方法和医药用途
CN117777121A (zh) 2016-10-24 2024-03-29 詹森药业有限公司 化合物及其用途
US10947242B2 (en) * 2016-11-02 2021-03-16 Janssen Pharmaceutica, Nv [1,2,4]triazolo[1,5and#8208;A]pyrimidine compounds as PDE2 inhibitors
CA3038916A1 (en) 2016-11-02 2018-05-11 Janssen Pharmaceutica Nv [1,2,4]triazolo[1,5-a]pyrimidine compounds as pde2 inhibitors
WO2018083101A1 (en) 2016-11-02 2018-05-11 Janssen Pharmaceutica Nv [1,2,4]triazolo[1,5-a]pyrimidine compounds as pde2 inhibitors
US11008325B2 (en) 2016-11-14 2021-05-18 Virginia Commonwealth University Inhibitors of cancer invasion, attachment, and/or metastasis
EP3541378A4 (en) * 2016-11-16 2020-10-07 University of South Florida ALLOSTERIC ANTAGONISTS OF GPRC6A AND THEIR USE IN THE MITIGATION OF PROTEINOPATHIES
EA201991650A1 (ru) 2017-01-06 2020-01-20 Юманити Терапьютикс, Инк. Способы лечения неврологических расстройств
CN116462666B (zh) * 2017-01-10 2025-07-15 瑞士苏黎世联邦理工学院 细胞保护性化合物及其用途
EP3571193B1 (en) 2017-01-23 2021-12-01 Cadent Therapeutics, Inc. Potassium channel modulators
CN106748969B (zh) * 2017-01-23 2019-06-18 南阳师范学院 一种n-(4-苄基哌啶基)-阿魏酰胺化合物、制备方法及其用途
CN106831573B (zh) * 2017-01-23 2019-05-24 南阳师范学院 (n-1,2,3,4-四氢异喹啉基)-阿魏酰胺化合物、制备方法及其应用
MY196680A (en) 2017-01-26 2023-04-29 Ono Pharmaceutical Co Ethanesulfonate salt of n-{5-[(6,7-dimethoxy-4-quinolinyl)oxy]-2- pyridinyl}-2,5-dioxo-1-phenyl-1,2,5,6,7,8-hexahydro-3- quinolinecarboxamide
US11072599B2 (en) 2017-02-01 2021-07-27 Biotheryx, Inc. Pyrazole compounds and uses thereof
CN109730996B (zh) * 2017-03-01 2021-08-24 浙江大学 喹啉结构类型雄激素受体拮抗剂及其应用
EP3596060B1 (en) 2017-03-16 2023-09-20 F. Hoffmann-La Roche AG New bicyclic compounds as atx inhibitors
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
JP6594570B2 (ja) 2017-03-20 2019-10-23 フォーマ セラピューティクス,インコーポレイテッド ピルビン酸キナーゼ(pkr)活性化剤としてのピロロピロール組成物
TWI664175B (zh) 2017-03-23 2019-07-01 大陸商北京加科思新藥研發有限公司 用於作為shp2抑制劑之新穎雜環衍生物
CN110536890B (zh) 2017-04-26 2023-08-15 巴斯利尔药物国际股份公司 制备呋咱并苯并咪唑及其晶型的方法
EP3634406B1 (en) * 2017-05-12 2023-09-06 Board of Trustees of The Southern Illinois University on behalf of Southern Illinois University Edwardsville 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JOP20190282A1 (ar) 2017-06-09 2019-12-05 Novartis Ag مركبات وتركيبات لحث تكوّن الغضاريف
CA3067086A1 (en) * 2017-06-14 2018-12-20 European Molecular Biology Laboratory Benzofuran amides and heteroaromatic analogues thereof for use in therapy
WO2018237145A1 (en) 2017-06-21 2018-12-27 Mitokinin, Inc. Compositions and methods using the same for treatment of neurodegenerative and mitochondrial disease
GB201710851D0 (en) * 2017-07-06 2017-08-23 Galápagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis
PL3651766T3 (pl) 2017-07-10 2025-03-03 Celgene Corporation 4-(4-(4-(((2-(2,6-dioksopiperydyn-3-ylo)-1-oksoizoindolin-4-ylo)oksy)metylo)benzylo)piperazyn-1-ylo)-3-fluorobenzonitryl jako związek przeciwproliferacyjny
CN111065383A (zh) 2017-07-11 2020-04-24 沃泰克斯药物股份有限公司 用作钠通道调节剂的羧酰胺
CN111094264A (zh) * 2017-09-11 2020-05-01 保土谷化学工业株式会社 具有嘧啶环结构的化合物及有机电致发光元件
MA50250A (fr) 2017-09-15 2020-07-22 Forma Therapeutics Inc Compositions de tétrahydroimidazo quinoléine utilisées en tant qu'inhibiteurs de cbp/p300
JP7223998B2 (ja) 2017-10-13 2023-02-17 小野薬品工業株式会社 Axl阻害剤を有効成分として含む固形がん治療剤
KR102697255B1 (ko) 2017-10-19 2024-08-23 데이진 화-마 가부시키가이샤 벤즈이미다졸 유도체 및 이의 용도
WO2019084157A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. COMPOUNDS AND USES THEREOF
EP3728201A1 (en) * 2017-12-21 2020-10-28 Gliapharm SA Compositions and methods of treatment for neurological disorders comprising a dementia
CA3083347A1 (en) * 2017-12-21 2019-06-27 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising motor neuron diseases
CR20230030A (es) 2018-02-27 2023-03-10 Incyte Corp Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b (divisional 2020-0441)
EP3762383B1 (en) * 2018-03-06 2023-12-06 The United States of America, as represented by the Secretary, Department of Health and Human Services Positive allosteric modulators of dopamine 1 receptor and method of use thereof
EP3543231A1 (en) * 2018-03-19 2019-09-25 ETH Zurich Compounds for treating cns- and neurodegenerative diseases
AU2019238326B2 (en) 2018-03-23 2025-03-06 Janssen Pharmaceutica Nv Compounds and uses thereof
PE20210919A1 (es) 2018-05-04 2021-05-19 Incyte Corp Sales de un inhibidor de fgfr
BR112020022392A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation formas sólidas de um inibidor de fgfr e processos para preparação das mesmas
TWI815887B (zh) * 2018-05-15 2023-09-21 美商愛彼特生物製藥股份有限公司 經取代的2,2'-雙嘧啶基化合物、其類似物及其使用方法
MX2020012376A (es) 2018-05-18 2021-03-09 Incyte Corp Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b.
CN120053645A (zh) 2018-06-01 2025-05-30 因赛特公司 治疗pi3k相关病症的给药方案
GB201810092D0 (en) 2018-06-20 2018-08-08 Ctxt Pty Ltd Compounds
GB201810581D0 (en) 2018-06-28 2018-08-15 Ctxt Pty Ltd Compounds
KR20250067962A (ko) 2018-06-29 2025-05-15 포르마 세라퓨틱스 인크. Creb 결합 단백질(cbp)의 저해
MX2021000116A (es) 2018-07-05 2021-03-29 Incyte Corp Derivados de pirazina fusionados como inhibidores de a2a/a2b.
IL280664B2 (en) * 2018-08-06 2023-04-01 Univ Leland Stanford Junior 2-Arylbenzimidazoles as ppargc1a stimulators for the treatment of neurodegenerative diseases
AU2019327430B2 (en) 2018-08-29 2024-10-03 Chemocentryx, Inc. Combination therapy using C-C chemokine receptor 4 (CCR4) antagonists and one or more immune checkpoint inhibitors
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
US11278527B2 (en) 2018-09-04 2022-03-22 Brown University Compositions and methods for the modulation of the corticotropin releasing factor binding protein and the treatment of alcohol use disorder
CA3113234A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
WO2020061255A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Activating pyruvate kinase r
CN112839935A (zh) 2018-09-26 2021-05-25 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
EP3870291A1 (en) 2018-10-22 2021-09-01 Cadent Therapeutics, Inc. Crystalline forms of potassium channel modulators
BR112021007261A2 (pt) * 2018-10-23 2021-08-10 Daiichi Sankyo Company, Limited composto, composição farmacêutica, inibidor de fosfatase alcalina de tecido não específica, métodos para inibir fosfatase alcalina de tecido não específica, para a profilaxia ou tratamento de calcificação ectópica e de uma doença ou condição, e, uso de um composto
EP3877383A4 (en) 2018-11-07 2022-09-21 The University of Melbourne COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF RESPIRATORY DISEASES
CN109503563B (zh) * 2018-12-10 2020-05-12 济南大学 多功能乙酰胆碱酯酶抑制剂及其应用
KR102128509B1 (ko) * 2018-12-19 2020-07-01 한국과학기술연구원 말단 아민기에 아릴 또는 헤테로아릴기가 치환된 신규한 히드라존 유도체 및 이의 용도
EP3906229A4 (en) * 2019-01-04 2022-11-16 Bellbrook Labs, Llc INHIBITORS OF CGAS ACTIVITY AS THERAPEUTIC AGENT
WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
US12440481B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
JP7742775B2 (ja) 2019-01-24 2025-09-22 ヤンセン ファーマシューティカ エヌ.ベー. 化合物及びその使用
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
TW202102494A (zh) 2019-03-15 2021-01-16 美商弗瑪治療公司 抑制環amp-反應元件-結合蛋白(creb)
US11505548B2 (en) * 2019-04-26 2022-11-22 Celgene Corporation Heterocyclic compounds and their use for treatment of helminthic infections and diseases
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
IL288802B2 (en) 2019-06-18 2025-08-01 Pfizer Benzisoxazole sulfonamide derivatives
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
KR20220061958A (ko) 2019-07-31 2022-05-13 리본 테라퓨틱스 인코포레이티드 Cd38의 억제제로서의 헤테로바이사이클릭 아미드
RU2746423C2 (ru) * 2019-09-02 2021-04-13 Общество с ограниченной ответственностью "Научно-исследовательский институт ХимРар" (ООО "НИИ ХимРар") Ингибитор вируса гепатита В (ВГВ)
AU2020350763A1 (en) 2019-09-19 2022-04-07 Novo Nordisk Health Care Ag Pyruvate kinase R (PKR) activating compositions
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
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение
KR102770734B1 (ko) * 2019-11-14 2025-02-21 주식회사 진큐어 Ampk 억제기능과 아연항상성 조절기능에 기반한 다발성 경화증 치료용 약학적 조성물
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
PE20221504A1 (es) 2019-12-04 2022-09-30 Incyte Corp Derivados de un inhibidor de fgfr
LT4069691T (lt) 2019-12-06 2024-12-10 Vertex Pharmaceuticals Incorporated Pakeistieji tetrahidrofuranai kaip natrio kanalų moduliatoriai
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AR122711A1 (es) * 2020-06-25 2022-09-28 Alchemedicine Inc COMPUESTO HETEROCÍCLICO COMO INHIBIDOR DE CASEÍNA QUINASA 1d Y/O QUINASA 5 TIPO RECEPTOR DE ACTIVINA
CA3191164A1 (en) * 2020-08-10 2022-02-17 Dana-Farber Cancer Institute, Inc. Substituted 1,2,4-oxadiazoles as small molecule inhibitors of ubiquitin-specific protease 28
KR20230069169A (ko) * 2020-09-17 2023-05-18 얀센 파마슈티카 엔.브이. 카제인 키나제 1 델타 조절제
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
GB202101734D0 (en) * 2021-02-08 2021-03-24 Cerevance Inc Novel Compounds
CA3207819A1 (en) 2021-02-19 2022-08-25 Anjali Pandey Tyk2 inhibitors and uses thereof
JP2024508794A (ja) 2021-02-19 2024-02-28 スドー バイオサイエンシーズ リミテッド Tyk2阻害剤およびその使用
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
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
KR20230146639A (ko) * 2021-04-21 2023-10-19 장춘 진사이언스 파마슈티컬 씨오., 엘티디. 이미다졸 함유 축합고리계 유도체, 이의 제조방법 및 이의 의약적 용도
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為fgfr抑制劑之三環雜環
JP2024539633A (ja) * 2021-10-15 2024-10-29 ロモンド セラピューティクス,インコーポレイテッド 置換1H-ピラゾロ[4,3-c]キノリン、その調製方法、および使用
CN115466211B (zh) * 2022-06-09 2024-02-23 中国人民解放军空军军医大学 一种n-苯基喹啉-4-胺类化合物及其应用
WO2024012554A1 (zh) * 2022-07-14 2024-01-18 上海日馨医药科技股份有限公司 Tpk激动剂及使用其治疗神经退行性疾病的方法
UY40374A (es) 2022-08-03 2024-02-15 Novartis Ag Inhibidores de inflamasoma nlrp3
TW202428579A (zh) * 2022-10-19 2024-07-16 大陸商長春金賽藥業有限責任公司 Nk3r拮抗劑的晶型及其製備方法和用途
CN120917015A (zh) * 2023-01-20 2025-11-07 元启(苏州)生物制药有限公司 Srpk1抑制剂和使用方法
AR131690A1 (es) * 2023-01-30 2025-04-23 Eurofarma Laboratorios S A COMPUESTOS FENÓLICOS BLOQUEADORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, SUS COMPOSICIONES, SUS USOS, LOS MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y LOS KITS
EP4660182A1 (en) * 2023-01-30 2025-12-10 Eurofarma Laboratórios S.A. Nav1.7- and/or nav1.8-inhibiting aryl pyridine compounds, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits
CN118666857B (zh) * 2024-06-26 2025-02-25 江西农业大学 一种喹啉类化合物及其在农用杀菌剂中的应用
CN119060061B (zh) * 2024-08-26 2025-09-16 浙江师范大学 一类苯并嘧啶硫醚类化合物作为sting蛋白小分子抑制剂的应用

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9506197D0 (en) 1995-03-27 1995-05-17 Hoffmann La Roche Inhibition of tau-tau association.
US5545656A (en) * 1995-04-05 1996-08-13 Pfizer Inc. 2-Oxidole-1-carboxamide pharmaceutical agents for the treatment of alzheimer's disease
US20030219427A1 (en) * 1998-08-18 2003-11-27 Allen Hamish J. TPL-2/COT kinase and methods of use
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6087363A (en) * 1999-07-16 2000-07-11 Harbor Branch Oceanographic Institution, Inc. Use of imidazole and indole compounds as inhibitors of nitric oxide synthase
SI1315731T1 (en) * 2000-09-01 2005-02-28 Sanofi-Aventis 2-pyridinyl-6,7,8,9-tetrahydropyrimido(1,2-a)pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo(1,2-a)pyrimidin-5(1h)one derivatives
ATE346064T1 (de) * 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
WO2002051821A1 (en) * 2000-12-22 2002-07-04 Astrazeneca Ab Therapeutic compounds
DE60223720T2 (de) * 2001-12-18 2008-10-30 Merck & Co., Inc. Heteroaryl-substituierte pyrazol-modulatoren des metabotropen glutamatrezeptors-5
JP2003212859A (ja) * 2002-01-24 2003-07-30 Nippon Nohyaku Co Ltd 置換フェニルヘテロ環類及びこれを有効成分とする除草剤
CA2477984A1 (en) * 2002-03-08 2003-09-18 Pamela Ann Albaugh Pyrrole-2, 5-dione derivatives and their use as gsk-3 inhibitors
FR2836915B1 (fr) * 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
WO2003097615A1 (en) * 2002-05-17 2003-11-27 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-β INHIBITORS
WO2003106439A1 (ja) * 2002-06-12 2003-12-24 株式会社ビーエフ研究所 アミロイド蓄積性疾患の画像診断プローブ化合物、老人斑/びまん性老人斑染色用化合物、ならびにアミロイド蓄積性疾患の治療薬
CL2004000409A1 (es) * 2003-03-03 2005-01-07 Vertex Pharma Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu
US7060698B2 (en) * 2003-05-19 2006-06-13 Hoffmann-La Roche Inc. Benzoxazepinone derivatives
EP1631145A4 (en) * 2003-06-06 2009-12-23 Univ Pennsylvania COMPOSITIONS COMPRISING P38 KINASE INHIBITORS AND METHODS OF USE
GB0314943D0 (en) 2003-06-25 2003-07-30 Proteome Sciences Plc Screening methods
US7560464B2 (en) * 2004-04-13 2009-07-14 Icagen, Inc. Polycyclic pyrimidines as potassium ion channel modulators
KR20070045264A (ko) * 2004-08-19 2007-05-02 아벤티스 파마슈티칼스 인크. 카세인 키나제 Iε 억제제로서의3-아릴티오인돌-2-카복스아미드 유도체 및 이의 유사체
WO2007015866A2 (en) * 2005-07-20 2007-02-08 Kalypsys, Inc. Inhibitors of p38 kinase and methods of treating inflammatory disorders
EP1842541A1 (en) * 2006-03-29 2007-10-10 G.I.M.-Gesellschaft Für Innovative Medizin Gmbh Nfg Ohg Plant components and extracts and uses thereof
TW200813035A (en) * 2006-06-19 2008-03-16 Astrazeneca Ab Novel heteroaryl substituted benzoxazoles
US20090186907A1 (en) * 2006-06-21 2009-07-23 E.I. Dupont De Nemours And Company Pyrazinones As Cellular Proliferation Inhibitors
US7622495B2 (en) * 2006-10-03 2009-11-24 Neurim Pharmaceuticals (1991) Ltd. Substituted aryl-indole compounds and their kynurenine/kynuramine-like metabolites as therapeutic agents
JP5064511B2 (ja) * 2006-11-02 2012-10-31 エフ.ホフマン−ラ ロシュ アーゲー 痕跡アミン関連受容体調節剤としての置換2−イミダゾール
WO2008058402A1 (en) * 2006-11-17 2008-05-22 Queen's University At Kingston Compounds and methods for treating protein folding disorders
WO2008077138A1 (en) * 2006-12-19 2008-06-26 The Board Of Trustees Of The University Of Illinois 3-benzofuranyl-4-indolyl maleimides as potent gsk3 inhibitors for neurogenerative disorders
EP2170058B1 (en) * 2007-06-20 2013-07-03 Merck Sharp & Dohme Corp. Cetp inhibitors derived from benzoxazole arylamides
FR2918061B1 (fr) * 2007-06-28 2010-10-22 Sanofi Aventis Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique.
FR2918986B1 (fr) * 2007-07-19 2009-09-04 Sanofi Aventis Sa Derives de 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]- pyridazine, leur preparation et leur application en therapeutique
GB0715939D0 (en) * 2007-08-15 2007-09-26 Vastox Plc Method of treatment of duchenne muscular dystrophy
US20110065715A1 (en) * 2007-11-28 2011-03-17 Yale University Nogo Receptor Binding Small Molecules to Promote Axonal Growth
JP2011507910A (ja) * 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法
EP2149551A1 (de) 2008-07-30 2010-02-03 Bayer Schering Pharma AG N-(Indol-3-ylalkyl)-(hetero)arylamidderivate als Modulatoren des EP2-Rezeptors
FR2934994B1 (fr) * 2008-08-12 2010-09-17 Sanofi Aventis Derives de 2-alkyl-6cycloamino-3-(pyridin-4-yl)imidaz°1,2-b! pyridazine, leur preparation et leur application en therapeutique
KR101257695B1 (ko) * 2008-12-24 2013-04-24 제일모직주식회사 신규한 유기광전소자용 화합물 및 이를 포함하는 유기광전소자
FR2945289A1 (fr) * 2009-05-11 2010-11-12 Sanofi Aventis Derives de 2-cycloamino-5-(pyridin-4-yl)imidazo°2,1-b! °1,3,4!thiadiazole, leur preparation et leur application en therapeutique
PH12012501480A1 (en) * 2010-01-25 2012-10-22 Chdi Foundation Inc Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
ES2650744T3 (es) * 2010-12-14 2018-01-22 Electrophoretics Limited Inhibidores de la caseína quinasa 1 delta (CK1delta)
ES2773480T3 (es) 2011-05-09 2020-07-13 Eip Pharma Llc Composiciones y métodos para tratar la enfermedad de Alzheimer

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