JP2014503528A - カゼインキナーゼ１δ（ＣＫ１δ）阻害剤及びタウオパチーなどの神経変性疾患の治療におけるその使用 - Google Patents

カゼインキナーゼ１δ（ＣＫ１δ）阻害剤及びタウオパチーなどの神経変性疾患の治療におけるその使用 Download PDF

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JP2014503528A
JP2014503528A JP2013543881A JP2013543881A JP2014503528A JP 2014503528 A JP2014503528 A JP 2014503528A JP 2013543881 A JP2013543881 A JP 2013543881A JP 2013543881 A JP2013543881 A JP 2013543881A JP 2014503528 A JP2014503528 A JP 2014503528A
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alkyl
aryl
conh
heteroaryl
compound
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JP2014503528A5 (OSRAM
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エム．シェリダン ジョセプフ
アール．ヘアル ジョナトハン
ディー．オー．ハミルトン ウイルリアム
ピケ イアン
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エレクトロプホレトイクス リミテッド
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Priority claimed from GBGB1109162.6A external-priority patent/GB201109162D0/en
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Publication of JP2014503528A publication Critical patent/JP2014503528A/ja
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JP2018521119A (ja) * 2015-06-01 2018-08-02 バンタム、ファーマシューティカル、リミテッド、ライアビリティー、カンパニーＢａｎｔａｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌ， Ｌｌｃ 置換ピラゾールおよびピロール化合物、および翻訳開始の阻害およびこれらに関連する疾患および障害の治療のためにこれらを用いる方法
JP2018525345A (ja) * 2015-07-01 2018-09-06 ノースウェスタン ユニバーシティ 置換キナゾリン化合物及びグルコセレブロシダーゼ活性の調節のためのその使用
JP2018535968A (ja) * 2015-11-02 2018-12-06 ヤンセン ファーマシューティカ エヌ．ベー． ［１，２，４］トリアゾロ［１，５−ａ］ピリミジン−７−イル化合物
JP2019502673A (ja) * 2015-12-07 2019-01-31 ヒノバ ファーマシューティカルズ インコーポレイテッド キノリン系化合物とその調製方法および尿酸トランスポータ阻害剤類薬物としての使用
JP2019529514A (ja) * 2015-10-05 2019-10-17 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 オートファジーフラックス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
JP2019532985A (ja) * 2016-11-02 2019-11-14 ヤンセン ファーマシューティカ エヌ．ベー． ＰＤＥ２阻害剤としての［１，２，４］トリアゾロ［１，５−ａ］ピリミジン誘導体
JP2020519644A (ja) * 2017-05-12 2020-07-02 ボード オブ トラスティーズ オブ ザ サザン イリノイ ユニバーシティ オン ビハーフ オブ サザン イリノイ ユニバーシティ エドワーズビル ３，４，５−三置換−１，２，４−トリアゾールおよび３，４，５−三置換−３−チオ−１，２，４−トリアゾール、ならびにそれらの使用
JP2021507945A (ja) * 2017-12-21 2021-02-25 グリアファーム エスエー 認知症を含む神経障害のための組成物および治療方法
JP2021507944A (ja) * 2017-12-21 2021-02-25 グリアファーム エスエー 運動ニューロン疾患を含む神経障害のための組成物および治療方法
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JP2022529541A (ja) * 2019-04-26 2022-06-22 セルジーン コーポレーション ヘテロ環式化合物ならびに蠕虫感染および疾患におけるその使用
JP2024505708A (ja) * 2021-02-08 2024-02-07 セレヴァンス，インコーポレイテッド 新規化合物
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Families Citing this family (220)

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Publication number Priority date Publication date Assignee Title
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US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
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US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
JP5937102B2 (ja) * 2010-12-14 2016-06-22 エレクトロフォレティクス リミテッド カゼインキナーゼ１デルタ（ｃｋ１デルタ）阻害剤
EP2655374B1 (en) 2010-12-20 2019-10-23 Incyte Holdings Corporation 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
PE20180318A1 (es) 2011-01-10 2018-02-09 Infinity Pharmaceuticals Inc Procedimiento para preparar isoquinolinonas y formas solidas de isoquinolinonas
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
PL3513793T3 (pl) 2011-09-02 2021-09-20 Incyte Holdings Corporation Heterocykloaminy jako inhibitory pi3k
MX360706B (es) 2011-10-07 2018-11-14 Takeda Pharmaceuticals Co Compuestos de 1-arilcarbonil-4-oxi-piperidina utiles para el tratamiento de enfermedades neurodegenerativas.
EA024846B1 (ru) 2011-10-18 2016-10-31 Астеллас Фарма Инк. Бициклическое гетероциклическое соединение
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
PT2785692T (pt) 2011-12-01 2018-01-04 Chemocentryx Inc Anilinas substituídas como antagonistas do ccr(4)
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
ES2984771T3 (es) 2012-06-13 2024-10-31 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
TWI633087B (zh) 2012-06-13 2018-08-21 赫孚孟拉羅股份公司 新穎二氮雜螺環烷及氮雜螺環烷
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
JP6299591B2 (ja) * 2012-07-03 2018-03-28 小野薬品工業株式会社 ソマトスタチン受容体作動活性を有する化合物およびその医薬用途
WO2014009891A1 (en) * 2012-07-11 2014-01-16 Piramal Enterprises Limited Heterocyclic compounds for use in the treatment of cancers
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
WO2014031732A2 (en) 2012-08-22 2014-02-27 Cornell University Methods for inhibiting fascin
KR102046499B1 (ko) * 2012-08-24 2019-11-19 트레벤티스 코포레이션 벤조푸라잔 항아밀로이드 화합물 및 방법
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
HRP20191937T1 (hr) 2012-09-25 2020-01-10 F. Hoffmann - La Roche Ag Derivati heksahidropirolo [3,4-c]pirola i srodni spojevi kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za liječenje npr. bubrežnih bolesti
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
LT2914296T (lt) 2012-11-01 2018-09-25 Infinity Pharmaceuticals, Inc. Vėžio gydymas, panaudojant p13 kinazės izoformos moduliatorius
MY182386A (en) 2012-11-27 2021-01-22 Thomas Helledays Stiftelse For Medicinsk Forskning Pyrimidine-2,4-diamine derivatives for treatment of cancer
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
WO2014103801A1 (ja) 2012-12-28 2014-07-03 株式会社新日本科学 イミダゾピリジン誘導体を有効成分として含むｏｃｔ３活性阻害剤又はｏｃｔ３検出剤
NZ710444A (en) * 2013-02-11 2020-08-28 Univ 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
CA2906194A1 (en) 2013-03-15 2014-09-18 Whitehead Institute For Biomedical Research Benzimidazole derivatives and uses thereof
US9045477B2 (en) * 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
EP2970306A4 (en) 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED 6.5-CONDENSED BICYCLIC HETEROARYL COMPOUNDS
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
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
EP3019874B1 (en) * 2013-07-09 2019-08-21 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.
US10709714B2 (en) 2013-11-22 2020-07-14 Clifton Life Sciences LLC Gastrin antagonists for treatment and prevention of osteoporosis
LT3074400T (lt) 2013-11-26 2018-02-12 F. Hoffmann-La Roche Ag Oktahidro-ciklobuta [1,2-c;3,4-c`]dipirolo dariniai kaip autotaksino inhibitoriai
GB201321738D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic Agents
CA2935944A1 (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
CA2937431A1 (en) 2014-01-29 2015-08-06 Glaxosmithkline Intellectual Property Development Limited Compounds
US9815841B2 (en) 2014-01-29 2017-11-14 Glaxosmithkline Intellectual Property Development Limited Compounds
AU2015217152A1 (en) 2014-02-11 2016-08-11 Mitokinin, Inc. Compositions and methods using the same for treatment of neurodegenerative and mitochondrial disease
PT3105226T (pt) 2014-02-13 2019-11-06 Incyte Corp Ciclopropilaminas como inibidores de lsd1
ME03654B (me) 2014-02-13 2020-07-20 Incyte Corp Ciklopropilamini kao lsd1 inhibitori
TW201613860A (en) 2014-02-13 2016-04-16 Incyte Corp Cyclopropylamines as LSD1 inhibitors
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
CN106232583B (zh) 2014-02-20 2020-04-24 康奈尔大学 用于抑制肌成束蛋白的化合物和方法
LT3110812T (lt) 2014-02-27 2019-07-10 Treventis Corporation Anti-amiloidų junginiai, turintys benzofurazano
PE20161223A1 (es) 2014-03-26 2016-11-12 Hoffmann La Roche Compuestos condensados de [1,4]diazepina como inhibidores de la produccion de autotaxina (atx) y acido lisofosfatidico (lpa)
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)
WO2015157382A1 (en) * 2014-04-11 2015-10-15 Emory University 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
CN105085436B (zh) * 2014-04-19 2019-08-16 广东东阳光药业有限公司 磺酰胺类衍生物及其在药物上的应用
HRP20212035T1 (hr) * 2014-04-23 2022-04-01 Dart Neuroscience Llc Pripravci koji sadrže supstituirane [1,2,4]triazolo[1,5-a]pirimidin-7-il spojeve kao inhibitore pde2
EP3140298A1 (en) 2014-05-07 2017-03-15 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
SG11201609981RA (en) 2014-06-04 2016-12-29 Thomas Helledays Stiftelse För Medicinsk Forskning Mth1 inhibitors for treatment of inflammatory and autoimmune conditions
US10179790B2 (en) 2014-06-04 2019-01-15 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
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
BR112017001221A2 (pt) * 2014-07-31 2017-11-28 Merck Patent Gmbh derivados de indolizina que são aplicáveis a doenças neurodegenerativas
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
KR20170063954A (ko) 2014-10-07 2017-06-08 버텍스 파마슈티칼스 인코포레이티드 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정
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
WO2016104617A1 (ja) 2014-12-25 2016-06-30 小野薬品工業株式会社 キノリン誘導体
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
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
EA038045B1 (ru) 2015-02-20 2021-06-28 Инсайт Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
RS63963B1 (sr) 2015-02-27 2023-03-31 Incyte Holdings Corp Postupak pripreme pi3k inhibitora
CN113350352B (zh) * 2015-03-23 2024-09-10 天莅生物科技私人有限公司 呼吸性疾病的治疗
AU2016243939B2 (en) 2015-04-03 2020-09-03 Incyte Holdings Corporation Heterocyclic compounds as LSD1 inhibitors
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
JP2018514572A (ja) * 2015-04-30 2018-06-07 エムユーエスシー ファウンデーション フォー リサーチ ディベロップメント オキシンドール化合物およびその医薬組成物
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k 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
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
WO2017000277A1 (en) * 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Substituted triazolo bicycliccompounds as pde2 inhibitors
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
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
MX377277B (es) * 2015-09-04 2025-03-07 Hoffmann La Roche Derivados de fenoximetilo.
WO2017047602A1 (ja) 2015-09-18 2017-03-23 科研製薬株式会社 ビアリール誘導体及びそれを含有する医薬
EP3353178B1 (en) 2015-09-24 2021-07-14 F. Hoffmann-La Roche AG Bicyclic compounds as dual atx/ca inhibitors
AU2016328365B2 (en) 2015-09-24 2020-04-23 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
AU2016328535A1 (en) 2015-09-24 2017-11-09 F. Hoffmann-La Roche Ag Bicyclic compounds as ATX inhibitors
CA2991615A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
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
WO2017106367A1 (en) * 2015-12-15 2017-06-22 D.E. Shaw Research, Llc Method of treating neurodegenerative disorders by rescuing alpha-synuclein toxicity
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
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
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
AR109452A1 (es) 2016-04-22 2018-12-12 Incyte Corp Formulación farmacéutica de un inhibidor de lsd1 y método de tratamiento
US10774064B2 (en) 2016-06-02 2020-09-15 Cadent Therapeutics, Inc. Potassium channel modulators
CN114539273A (zh) 2016-06-07 2022-05-27 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
UA125216C2 (uk) 2016-06-24 2022-02-02 Інфініті Фармасьютікалз, Інк. Комбінована терапія
CN109476645A (zh) 2016-07-14 2019-03-15 辉瑞大药厂 作为vanin-1酶抑制剂的新的嘧啶甲酰胺
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
CR20220309A (es) 2016-09-02 2022-09-16 Cyclerion Therapeutics 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
US11970486B2 (en) 2016-10-24 2024-04-30 Janssen Pharmaceutica Nv Compounds and uses thereof
WO2018089967A1 (en) 2016-11-14 2018-05-17 Virginia Commonwealth University Inhibitors of cancer invasion, attachment, and/or metastasis
US20190358238A1 (en) * 2016-11-16 2019-11-28 University Of South Florida ALLOSTERIC ANTAGONISTS OF GPRC6a AND THEIR USE IN MITIGATING PROTEINOPATHIES
JP2020514293A (ja) 2017-01-06 2020-05-21 ユマニティ セラピューティクス，インコーポレーテッド 神経障害を治療する方法
WO2018130537A1 (en) * 2017-01-10 2018-07-19 ETH Zürich Cell-protective compounds and their use
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
CU24560B1 (es) 2017-01-23 2021-12-08 Cadent Therapeutics Inc N-(4,4-difluorociclohexil)-2-(3-metil-1h-pirazol-1-il)-6-morfolinopirimidin-4-amina útil como modulador de canales de potasio
PT3575293T (pt) 2017-01-26 2021-05-25 Ono Pharmaceutical Co Sal de etanossulfonato de n-{5-[(6,7-dimetoxi-4-quinolinil)oxi]-2-piridinil}-2,5-dioxo-1-fenil-1,2,5,6,7,8-hexahidro-3-quinolinocarboxamida
JP7142646B2 (ja) 2017-02-01 2022-09-27 イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティ オブ エルサレム エルティーディー． がんを治療するためのｃｋ１及び／又はｉｒａｋ１インヒビターとしてのｎ１－（４－（５－（シクロプロピルメチル）－１－メチル－１ｈ－ピラゾール－４－イル）ピリジン－２－イル）シクロヘキサン－１，４－ジアミン誘導体及び関連化合物
CN109846879B (zh) * 2017-03-01 2021-06-29 浙江大学 亚胺结构类型雄激素受体拮抗剂及其应用
JP7090099B2 (ja) 2017-03-16 2022-06-23 エフ．ホフマン－ラ ロシュ アーゲー Ａｔｘインヒビターとしての新規二環式化合物
BR112019019017A2 (pt) 2017-03-16 2020-04-14 Hoffmann La Roche compostos heterocíclicos de utilidade como inibidores duplos de atx/ca
US11014927B2 (en) 2017-03-20 2021-05-25 Forma Therapeutics, Inc. Pyrrolopyrrole compositions as pyruvate kinase (PKR) activators
HRP20241239T1 (hr) 2017-03-23 2024-12-06 Jacobio Pharmaceuticals Co., Ltd. Novi heterociklički derivati korisni kao shp2 inhibitori
MX388196B (es) 2017-04-26 2025-03-19 Basilea Pharm Int Ag Procesos para la preparacion de furazanobencimidazoles y formas cristalinas de estos.
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
US20200223837A1 (en) * 2017-06-14 2020-07-16 European Molecular Biology Laboratory Benzofuran amides and heteroaromatic analogues thereof for use in therapy
CA3067695A1 (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
SG11202000143PA (en) 2017-07-10 2020-02-27 Celgene Corp Antiproliferative compounds and methods of use thereof
UY37806A (es) 2017-07-11 2020-01-31 Vertex Pharma Carboxamidas como moduladores de los canales de sodio
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
TWI795440B (zh) 2017-09-15 2023-03-11 美商佛瑪治療公司 作為ＣＢＰ／ｐ３００抑制劑之四氫─咪唑並喹啉化合物
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
AU2018351059B2 (en) 2017-10-19 2022-05-12 Teijin Pharma Limited Benzimidazole derivatives and their uses
CA3083000A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. Compounds and uses thereof
JP7474709B2 (ja) 2018-02-27 2024-04-25 インサイト・コーポレイション Ａ２ａ／ａ２ｂ阻害剤としてのイミダゾピリミジン及びトリアゾロピリミジン
US20210040074A1 (en) * 2018-03-06 2021-02-11 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
EP3768269B1 (en) 2018-03-23 2025-08-20 Janssen Pharmaceutica NV Compounds and uses thereof
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
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
MA52940A (fr) 2018-05-18 2021-04-28 Incyte Corp Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b
AU2019277560B2 (en) 2018-06-01 2025-04-24 Incyte Corporation Dosing regimen for the treatment of PI3K related disorders
GB201810092D0 (en) 2018-06-20 2018-08-08 Ctxt Pty Ltd Compounds
GB201810581D0 (en) 2018-06-28 2018-08-15 Ctxt Pty Ltd Compounds
BR112020026783A2 (pt) 2018-06-29 2021-03-30 Forma Therapeutics, Inc. Inibição da proteína de ligação creb (cbp)
AU2019297361B2 (en) 2018-07-05 2024-06-27 Incyte Corporation Fused pyrazine derivatives as A2A / A2B inhibitors
CN112805000A (zh) * 2018-08-06 2021-05-14 小利兰·斯坦福大学董事会 作为ppargc1a激活剂用于治疗神经退行性疾病的2-芳基苯并咪唑
US11446289B2 (en) 2018-08-29 2022-09-20 Chemocentryx, Inc. Combination therapy using C-C chemokine receptor 4 (CCR4) antagonists and one or more immune checkpoint inhibitors
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
WO2020051206A1 (en) * 2018-09-04 2020-03-12 Brown University Compositions and methods for the modulation of crfbp and the treatment of alcoholism
US20200115389A1 (en) 2018-09-18 2020-04-16 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
US12053458B2 (en) 2018-09-19 2024-08-06 Novo Nordisk Health Care Ag Treating sickle cell disease with a pyruvate kinase R activating compound
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
WO2020063760A1 (en) 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
AU2019366312B2 (en) 2018-10-22 2025-04-24 Novartis Ag Crystalline forms of potassium channel modulators
TWI828783B (zh) * 2018-10-23 2024-01-11 日商第一三共股份有限公司 聯芳基衍生物及其用途
WO2020093097A1 (en) 2018-11-07 2020-05-14 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
KR20210112317A (ko) * 2019-01-04 2021-09-14 벨부르크 랩스, 엘엘씨 치료제로서의 cgas 활성 억제제
US12441703B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020146612A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
MX2021008903A (es) 2019-01-24 2021-11-04 Yumanity Therapeutics Inc Compuestos y usos de los mismos.
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
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
EP3937940A4 (en) 2019-03-15 2022-12-21 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (creb)
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
PL4299135T3 (pl) 2019-06-18 2025-11-12 Pfizer Inc. Pochodne benzizoksazolosulfonamidu
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MX2022001019A (es) 2019-07-31 2022-02-22 Ribon Therapeutics Inc Amidas heterobiciclicas como inhibidoras del cumulo de diferenciacion 38 (cd38).
RU2746423C2 (ru) * 2019-09-02 2021-04-13 Общество с ограниченной ответственностью "Научно-исследовательский институт ХимРар" (ООО "НИИ ХимРар") Ингибитор вируса гепатита В (ВГВ)
EP4031132A4 (en) 2019-09-19 2023-09-13 Forma Therapeutics, Inc. Activating pyruvate kinase r
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
PH12022550892A1 (en) 2019-10-14 2023-05-03 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 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
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
HUE069128T2 (hu) 2019-12-06 2025-02-28 Vertex Pharma Szubsztituált tetrahidrofurán vegyületek mint nátriumcsatornák modulátorai
US12012409B2 (en) 2020-01-15 2024-06-18 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
CN116490503A (zh) * 2020-09-17 2023-07-25 詹森药业有限公司 酪蛋白激酶1δ调节剂
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)
WO2022175747A1 (en) 2021-02-19 2022-08-25 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
MX2023009685A (es) 2021-02-19 2023-10-30 Sudo Biosciences Ltd Inhibidores de tyk2 y sus usos.
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法
AU2022284886A1 (en) 2021-06-04 2023-11-30 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313610A (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
KR20240093606A (ko) * 2021-10-15 2024-06-24 로몬드 테라퓨틱스 인코포레이티드 치환된 1H-피라졸로[4,3-c] 퀴놀린, 이의 제조 방법 및 용도
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
EP4556007A1 (en) * 2022-07-14 2025-05-21 Shanghai Raising Pharmaceutical Co., Ltd. Tpk agonist and method for treating neurodegenerative diseases using same
UY40374A (es) 2022-08-03 2024-02-15 Novartis Ag Inhibidores de inflamasoma nlrp3
WO2024155864A1 (en) * 2023-01-20 2024-07-25 Allianthera (Suzhou) Biopharmaceutical Co., Ltd. Sprk1 inhibitors and methods of use
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002523502A (ja) * 1998-08-28 2002-07-30 サイオス インコーポレイテッド 医薬としてのキナゾリン誘導体
US20040038856A1 (en) * 2002-05-17 2004-02-26 Sarvajit Chakravarty Treatment of fibroproliferative disorders using TGF-beta inhibitors
JP2006527197A (ja) * 2003-06-06 2006-11-30 ザ・トラスティーズ・オブ・ザ・ユニバーシティ・オブ・ペンシルバニア ｐ３８キナーゼ阻害剤組成物及びその使用方法
JP2010531342A (ja) * 2007-06-28 2010-09-24 サノフイ−アベンテイス ６−シクロアミノ−３−（ピリジン−４−イル）イミダゾ［１，２−ｂ］ピリダジン誘導体、これらの調製およびこれらの治療的使用
JP2010533686A (ja) * 2007-07-19 2010-10-28 サノフイ−アベンテイス ６−シクロアミノ−３−（ピリダジン−４−イル）イミダゾ［１，２−ｂ］−ピリダジンおよびこれらの誘導体、これらの調製および治療上の用途

Family Cites Families (36)

* 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
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
WO2002018386A1 (en) * 2000-09-01 2002-03-07 Sanofi-Synthelabo 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 DERIVATI VES
ATE346064T1 (de) * 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
EP1345914A1 (en) * 2000-12-22 2003-09-24 AstraZeneca AB Therapeutic compounds
ES2295441T3 (es) * 2001-12-18 2008-04-16 MERCK & CO., INC. Moduladores de pirazol heteroaril sustituido de receptor 5 metabotropico de glutamato.
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
MXPA04008671A (es) * 2002-03-08 2004-12-06 Lilly Co Eli Derivados de pirrol-2,5-diona y su uso como inhibidores de gsk-3.
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
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
GB0314943D0 (en) 2003-06-25 2003-07-30 Proteome Sciences Plc Screening methods
ATE485824T1 (de) * 2004-04-13 2010-11-15 Icagen Inc Polycyclische pyrimidine als kaliumionenkanal- modulatoren
DE602005017162D1 (de) * 2004-08-19 2009-11-26 Aventis Pharma Inc 3-arylthioindol-2-carbonsäureamidderivate und ihre analoge als hemmer von caseinkinase i
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
MX2009004617A (es) * 2006-11-02 2009-05-22 Hoffmann La Roche 2-imidazoles sustituidos como moduladores de los receptores asociados con trazas de amina.
EP2081892A4 (en) * 2006-11-17 2014-03-05 Donald F Weaver COMPOUNDS AND METHOD FOR THE TREATMENT OF PROTEIN DISAPPEARANCE
ES2446269T3 (es) * 2006-12-19 2014-03-06 The Board Of Trustees Of The University Of Illinois 3-Benzofuranil-4-indolil-maleimidas como potentes inhibidores de GSK-3 para trastornos neurodegenerativos
AU2008266954A1 (en) * 2007-06-20 2008-12-24 Merck Sharp & Dohme Corp. CETP inhibitors derived from benzoxazole arylamides
GB0715939D0 (en) * 2007-08-15 2007-09-26 Vastox Plc Method of treatment of duchenne muscular dystrophy
WO2009073141A2 (en) * 2007-11-28 2009-06-11 Strittmatter Stephen M Nogo receptor binding small molecules to promote axonal growth
AU2008345225A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
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
JP5937102B2 (ja) * 2010-12-14 2016-06-22 エレクトロフォレティクス リミテッド カゼインキナーゼ１デルタ（ｃｋ１デルタ）阻害剤
US8697627B2 (en) 2011-05-09 2014-04-15 Eip Pharma, Llc Compositions and methods for treating alzheimer's disease

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002523502A (ja) * 1998-08-28 2002-07-30 サイオス インコーポレイテッド 医薬としてのキナゾリン誘導体
US20040038856A1 (en) * 2002-05-17 2004-02-26 Sarvajit Chakravarty Treatment of fibroproliferative disorders using TGF-beta inhibitors
JP2006527197A (ja) * 2003-06-06 2006-11-30 ザ・トラスティーズ・オブ・ザ・ユニバーシティ・オブ・ペンシルバニア ｐ３８キナーゼ阻害剤組成物及びその使用方法
JP2010531342A (ja) * 2007-06-28 2010-09-24 サノフイ−アベンテイス ６−シクロアミノ−３−（ピリジン−４−イル）イミダゾ［１，２−ｂ］ピリダジン誘導体、これらの調製およびこれらの治療的使用
JP2010533686A (ja) * 2007-07-19 2010-10-28 サノフイ−アベンテイス ６−シクロアミノ−３−（ピリダジン−４−イル）イミダゾ［１，２−ｂ］−ピリダジンおよびこれらの誘導体、これらの調製および治療上の用途

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, VOL.19, P.2277-2281, JPN6015035504, ISSN: 0003149202 *
J. MED. CHEM., 2005, VOL.48, P.4040-4048, JPN6015035514, ISSN: 0003149203 *
UKRAINICA BIOORGANICA ACTA, 2004, VOL.1(1-2), P.74-79, JPN6015035517, ISSN: 0003149204 *

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017523211A (ja) * 2014-08-04 2017-08-17 ドレクセル ユニバーシティ 新規化合物およびそれを用いてｉｌ−１ｒ媒介性の疾患または障害を処置するかまたは寛解させる方法
JP2018521119A (ja) * 2015-06-01 2018-08-02 バンタム、ファーマシューティカル、リミテッド、ライアビリティー、カンパニーＢａｎｔａｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌ， Ｌｌｃ 置換ピラゾールおよびピロール化合物、および翻訳開始の阻害およびこれらに関連する疾患および障害の治療のためにこれらを用いる方法
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JP2019529514A (ja) * 2015-10-05 2019-10-17 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 オートファジーフラックス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
US10947239B2 (en) 2015-11-02 2021-03-16 Janssen Pharmaceutica Nv [1,2,4]triazolo[1,5-a]pyrimidin-7-yl compound
JP2018535968A (ja) * 2015-11-02 2018-12-06 ヤンセン ファーマシューティカ エヌ．ベー． ［１，２，４］トリアゾロ［１，５−ａ］ピリミジン−７−イル化合物
JP2019502673A (ja) * 2015-12-07 2019-01-31 ヒノバ ファーマシューティカルズ インコーポレイテッド キノリン系化合物とその調製方法および尿酸トランスポータ阻害剤類薬物としての使用
JP7076441B2 (ja) 2016-11-02 2022-05-27 ヤンセン ファーマシューティカ エヌ．ベー． ＰＤＥ２阻害剤としての［１，２，４］トリアゾロ［１，５－ａ］ピリミジン誘導体
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JP7746406B2 (ja) 2021-04-21 2025-09-30 長春金賽薬業有限責任公司 イミダゾール含有縮合環系誘導体、その調製方法及びその医薬上の応用
JP2025528595A (ja) * 2022-10-19 2025-08-28 長春金賽薬業有限責任公司 Ｎｋ３ｒアンタゴニストの結晶形及びその調製方法と用途

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