CA2818903C - 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor - Google Patents

5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor Download PDF

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CA2818903C
CA2818903C CA2818903A CA2818903A CA2818903C CA 2818903 C CA2818903 C CA 2818903C CA 2818903 A CA2818903 A CA 2818903A CA 2818903 A CA2818903 A CA 2818903A CA 2818903 C CA2818903 C CA 2818903C
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alkyl
compound
aryl
disease
tau
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French (fr)
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CA2818903A1 (en
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Joseph M. Sheridan
Jonathan R. Heal
William D.O. Hamilton
Ian Pike
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Proteome Sciences PLC
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Electrophoretics Ltd
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Priority claimed from GBGB1109162.6A external-priority patent/GB201109162D0/en
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
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CA2818903A 2010-12-14 2011-12-14 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor Active CA2818903C (en)

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Families Citing this family (243)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007079139A2 (en) 2005-12-28 2007-07-12 Vertex Pharmaceuticals, Inc. Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
MX2010007419A (es) 2008-01-04 2010-11-12 Intellikine Inc Ciertas entidades quimicas, composiciones y metodos.
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
KR101763656B1 (ko) 2009-06-29 2017-08-01 인사이트 홀딩스 코포레이션 Ｐｉ3ｋ 저해물질로서의 피리미디논
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
US20130018039A1 (en) * 2010-03-31 2013-01-17 Bodmer Vera Q Imidazolyl-imidazoles as kinase inhibitors
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
WO2012080729A2 (en) * 2010-12-14 2012-06-21 Electrophoretics Limited CASEIN KINASE 1δ (CK1δ) INHIBITORS
EP3660016A1 (en) 2010-12-20 2020-06-03 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
ES2637113T3 (es) 2011-01-10 2017-10-10 Infinity Pharmaceuticals, Inc. Procedimientos para preparar isoquinolinonas y formas sólidas 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
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte 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
PT3513793T (pt) 2011-09-02 2021-05-10 Incyte Holdings Corp Heterociclilaminas como inibidores de pi3k
AP2014007606A0 (en) 2011-10-07 2014-05-31 Takeda Pharmaceutical 1-Arylcarbonyl-4-oxy-piperidine compounds useful for the treatment of neurodegenerative diseases
KR101987514B1 (ko) 2011-10-18 2019-06-10 아스텔라스세이야쿠 가부시키가이샤 이환식 헤테로환 화합물
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
BR112014013138B1 (pt) 2011-12-01 2022-06-28 Chemocentryx, Inc Compostos de anilinas substituídas como antagonistas de ccr(4) e composição farmacêutica compreendendo os mesmos
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
CN104364239B (zh) 2012-06-13 2017-08-25 霍夫曼-拉罗奇有限公司 二氮杂螺环烷烃和氮杂螺环烷烃
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
WO2014007228A1 (ja) 2012-07-03 2014-01-09 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
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
ES2877570T3 (es) 2012-08-22 2021-11-17 Univ Cornell Métodos para inhibir fascina
MX365851B (es) * 2012-08-24 2019-06-17 Treventis Corp Compuestos de benzofurazano anti-amiloides y metodos.
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
MX368615B (es) 2012-09-25 2019-10-09 Hoffmann La Roche Derivados bicíclicos como inhibidores de la autotaxina (atx) que son inhibidores de la producción de ácido lisofosfatídico (lpa) y el uso de los mismos.
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
AU2013337717B2 (en) 2012-11-01 2018-10-25 Infinity Pharmaceuticals, Inc. Treatment of cancers using PI3 kinase isoform modulators
EP2925744B1 (en) 2012-11-27 2020-12-30 Thomas Helledays Stiftelse För 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
WO2014124458A1 (en) * 2013-02-11 2014-08-14 The Regents Of The University Of California Compositions and methods for treating neurodegenerative diseases
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
US9776996B2 (en) 2013-03-15 2017-10-03 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
HK1220325A1 (zh) 2013-03-15 2017-05-05 Whitehead Institute For Biomedical Research 苯并咪唑衍生物及其用途
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
US9238034B2 (en) * 2013-07-09 2016-01-19 The Translational Genomics Research Institute FN14 antagonists and therapeutic uses thereof
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
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.
WO2015077572A1 (en) 2013-11-22 2015-05-28 CL BioSciences LLC Gastrin antagonists (eg yf476, netazepide) for treatment and prevention of osteoporosis
DK3074400T3 (en) 2013-11-26 2018-01-15 Hoffmann La Roche Octahydro-cyclobuta [1,2-c; 3,4-c '] dipyrrole derivatives as autotaxin inhibitors
GB201321738D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic Agents
US10087151B2 (en) 2014-01-09 2018-10-02 The J. David Gladstone Institutes, A Testimentary Trust Established Under The Will Of J. David Gladstone Substituted benzoxazine and related compounds
MA39219B1 (fr) 2014-01-29 2018-11-30 Glaxosmithkline Ip Dev Ltd Nouveaux composés inhibiteurs de la kinase lrrk2 utilisés pour le traitement du parkinson, de l’alzheimer et de la sclérose latérale amyotrophique
RU2016134751A (ru) 2014-01-29 2018-03-02 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Соединения
ES2919024T3 (es) 2014-02-11 2022-07-21 Mitokinin Inc Composiciones y procedimientos que utilizan las mismas para el tratamiento de enfermedades neurodegenerativas y mitocondriales
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3105218B1 (en) 2014-02-13 2019-09-25 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
JP6602779B2 (ja) 2014-02-13 2019-11-06 インサイト・コーポレイション Ｌｓｄ１阻害剤としてのシクロプロピルアミン類
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9573946B2 (en) 2014-02-20 2017-02-21 Novita Pharmaceuticals, Inc. Compounds and methods for inhibiting fascin
RS58976B1 (sr) 2014-02-27 2019-08-30 Treventis Corp Antiamiloidna jedinjenja koja sadrže benzofuran
CA2937616A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
EP3129361A4 (en) * 2014-04-11 2017-11-15 Emory University Treatment of neurodegenerative diseases with asparagine endopeptidase (aep) inhibitors and compositions related thereto
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
US9840482B2 (en) * 2014-04-19 2017-12-12 Sunshine Lake Pharma Co., Ltd. Sulfonamide derivatives and pharmaceutical applications thereof
HUE057317T2 (hu) * 2014-04-23 2022-04-28 Dart Neuroscience Llc Helyettesített [1,2,4]triazolo[1,5-A]pirimidin-7-IL vegyületeket tartalmazó készítmények mint PDE2 inhibítorok
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
US10064869B2 (en) 2014-06-04 2018-09-04 Thomas Helledays Stiftelse For Medicinsk Forskning MTH1 inhibitors for treatment of inflammatory and autoimmune conditions
WO2015187088A1 (en) 2014-06-04 2015-12-10 Thomas Helledays Stiftelse För 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
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
MX2017001103A (es) * 2014-07-31 2017-04-27 Merck Patent Gmbh Derivados de indolizina que son aplicables a enfermedades neurodegenerativas.
EP3189070A4 (en) 2014-08-04 2018-06-27 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
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
TWI568737B (zh) 2014-11-05 2017-02-01 達特神經科學（開曼）有限責任公司 作為ｐｄｅ２抑制劑之經取代的５－甲基－［１，２，４］三唑并［１，５－ａ］嘧啶－２－胺化合物
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
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
SG10201907576SA (en) 2015-02-27 2019-09-27 Incyte Corp Salts of pi3k inhibitor and processes for their preparation
WO2016149756A1 (en) 2015-03-23 2016-09-29 The University Of Melbourne Treatment of respiratory diseases
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
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
WO2017000277A1 (en) 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Substituted triazolo bicycliccompounds as pde2 inhibitors
CN108290855A (zh) * 2015-07-01 2018-07-17 西北大学 被取代的喹唑啉化合物及其调节葡糖脑苷脂酶活性的用途
MY189367A (en) 2015-08-12 2022-02-08 Incyte Corp Salts of an lsd1 inhibitor
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
CA2992889A1 (en) * 2015-09-04 2017-03-09 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
SG11201801856XA (en) 2015-09-18 2018-04-27 Kaken Pharmaceutical Co Ltd Biaryl derivative and medicine containing same
JP6876685B2 (ja) 2015-09-24 2021-05-26 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ａｔｘ阻害剤としての二環式化合物
AU2016328436B2 (en) 2015-09-24 2020-05-14 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
BR112017026682A2 (pt) 2015-09-24 2018-08-14 Hoffmann La Roche novos compostos bicíclicos como inibidores de dupla ação de atx/ca
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
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
ES2765738T3 (es) * 2015-11-02 2020-06-10 Janssen Pharmaceutica Nv Compuesto de [1,2,4]triazolo[1,5-a]pirimidin-7-ilo
WO2017097182A1 (zh) * 2015-12-07 2017-06-15 成都海创药业有限公司 喹啉类化合物及其制备方法和作为尿酸盐转运体抑制剂类药物的用途
US20200375996A1 (en) * 2015-12-15 2020-12-03 D.E. Shaw Research, Llc Method of treating neurodegenerative disorders by rescuing alpha-synuclein toxicity
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
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
TWI833686B (zh) 2016-04-22 2024-03-01 美商英塞特公司 Lsd1 抑制劑之調配物
CA3026149A1 (en) 2016-06-02 2017-12-07 Cadent Therapeutics, Inc. Potassium channel modulators
MX388576B (es) 2016-06-07 2025-03-20 Jacobio Pharmaceuticals Co Ltd Derivados heterociclicos novedosos utiles como inhibidores de shp2.
SG11201811237WA (en) 2016-06-24 2019-01-30 Infinity Pharmaceuticals Inc Combination therapies
WO2018011681A1 (en) 2016-07-14 2018-01-18 Pfizer Inc. Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme
ES2901059T3 (es) * 2016-08-09 2022-03-21 Zincure Corp Composición farmacéutica para el tratamiento de apoplejía basado en la inhibición de AMPK
US11084807B2 (en) 2016-08-18 2021-08-10 Vidac Pharama Ltd. Piperazine derivatives, pharmaceutical compositions and methods of use thereof
SI3507291T1 (sl) 2016-09-02 2021-11-30 Cyclerion Therapeutics, Inc. Kondenzirani biciklični SGS stimulatorji
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
JP2019533022A (ja) 2016-10-24 2019-11-14 ユマニティ セラピューティクス，インコーポレーテッド 化合物及びその使用
MX385576B (es) * 2016-11-02 2025-03-18 Janssen Pharmaceutica Nv Derivados de [1,2,4]triazol[1,5-a]pirimidina como inhibidores de pde2
CA3038916A1 (en) 2016-11-02 2018-05-11 Janssen Pharmaceutica Nv [1,2,4]triazolo[1,5-a]pyrimidine compounds as pde2 inhibitors
AU2017353313C1 (en) * 2016-11-02 2022-06-09 Janssen Pharmaceutica Nv (1,2,4)triazolo(1,5-a)pyrimidine compounds as PDE2 inhibitors
EP3538101B1 (en) 2016-11-14 2024-06-19 Virginia Commonwealth University Inhibitors of cancer and/or metastasis
WO2018094106A2 (en) 2016-11-16 2018-05-24 University Of South Florida ALLOSTERIC ANTAGONISTS OF GPRC6a AND THEIR USE IN MITIGATING PROTEINOPATHIES
EP3566055B1 (en) 2017-01-06 2025-03-12 Janssen Pharmaceutica NV Scd inhibitor for the treatment of neurological disorders
AU2018208458B2 (en) * 2017-01-10 2020-07-16 ETH Zürich Cell-protective compounds and their use
SI3571193T1 (sl) 2017-01-23 2022-04-29 Cadent Therapeutics, Inc. Modulatorji kalijevega kanalčka
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
TWI779007B (zh) 2017-01-26 2022-10-01 日商小野藥品工業股份有限公司 喹啉衍生物的乙磺酸鹽
MX394556B (es) * 2017-02-01 2025-03-24 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Derivados de n1-(4-(5-(ciclopropilmetil)-1-metil-1h-pirazol-4-il) piridin-2-il) ciclohexano-1,4-diamina y compuestos relacionados como inhibidores de ck1 y/o irak1 para tratar cáncer.
CN109700798A (zh) * 2017-03-01 2019-05-03 浙江大学 苯并吡喃黄酮结构类型雄激素受体拮抗剂及其应用
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
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
LT3483164T (lt) 2017-03-20 2020-05-11 Forma Therapeutics, Inc. Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai
EA202190196A1 (ru) 2017-03-23 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
MX388196B (es) 2017-04-26 2025-03-19 Basilea Pharm Int Ag Procesos para la preparacion de furazanobencimidazoles y formas cristalinas de estos.
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
UY37759A (es) 2017-06-09 2019-01-31 Novartis Ag Compuestos y composiciones para inducir condrogénesis
US20200223837A1 (en) * 2017-06-14 2020-07-16 European Molecular Biology Laboratory Benzofuran amides and heteroaromatic analogues thereof for use in therapy
AU2018290225A1 (en) 2017-06-21 2020-01-23 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
EP4467143B1 (en) 2017-07-10 2026-03-11 Celgene Corporation Method for preparing 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-l-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-l-yl)-3-fluorobenzonitrile
AU2018300150A1 (en) 2017-07-11 2020-01-30 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
JP7159173B2 (ja) * 2017-09-11 2022-10-24 保土谷化学工業株式会社 ピリミジン環構造を有する化合物および有機エレクトロルミネッセンス素子
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
US11826363B2 (en) 2017-10-13 2023-11-28 Ono Pharmaceutical Co., Ltd. Therapeutic agent for solid cancers, which comprises Axl inhibitor as active ingredient
HUE070649T2 (hu) 2017-10-19 2025-06-28 Teijin Pharma Ltd Benzimidazol-származékok és felhasználásuk
CA3083000A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. Compounds and uses thereof
US20200339591A1 (en) * 2017-12-21 2020-10-29 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising a dementia
SG11202004971YA (en) * 2017-12-21 2020-06-29 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising motor neuron diseases
TWI877770B (zh) 2018-02-27 2025-03-21 美商英塞特公司 作為a2a / a2b抑制劑之咪唑并嘧啶及三唑并嘧啶
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
WO2019183587A1 (en) 2018-03-23 2019-09-26 Yumanity Therapeutics, Inc. Compounds and uses thereof
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
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
EP3810610A1 (en) 2018-05-18 2021-04-28 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
SG11202011680YA (en) 2018-06-01 2020-12-30 Incyte Corp 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
US10870648B2 (en) 2018-06-29 2020-12-22 Forma Therapeutics, Inc. Inhibiting CREB binding protein (CBP)
WO2020010197A1 (en) 2018-07-05 2020-01-09 Incyte Corporation Fused pyrazine derivatives as a2a / a2b inhibitors
KR20210068399A (ko) * 2018-08-06 2021-06-09 더 보드 오브 트러스티스 오브 더 리랜드 스탠포드 주니어 유니버시티 신경퇴행성 질병의 치료를 위한 피피에이알지씨1알파 활성제로서 2-아릴벤즈이미다졸
KR102817790B1 (ko) 2018-08-29 2025-06-05 케모센트릭스, 인크. C-c 케모카인 수용체 4(ccr4) 길항제 및 하나 이상의 면역 체크포인트 억제제를 사용한 병용 요법
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
CA3111848A1 (en) * 2018-09-09 2020-03-12 Qanatpharma Ag Use of casein kinase 1 inhibitors for treating vascular diseases
CR20210175A (es) 2018-09-18 2021-06-01 Nikang Therapeutics Inc Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2)
EP3853206B1 (en) 2018-09-19 2024-04-10 Novo Nordisk Health Care AG Treating sickle cell disease with a pyruvate kinase r activating compound
EP3852791B1 (en) 2018-09-19 2024-07-03 Novo Nordisk Health Care AG Activating pyruvate kinase r
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
CA3116339A1 (en) 2018-10-22 2020-04-30 Cadent Therapeutics, Inc. Crystalline forms of potassium channel modulators
KR102880470B1 (ko) * 2018-10-23 2025-11-03 다이이찌 산쿄 가부시키가이샤 바이아릴 유도체
JP7614646B2 (ja) 2018-11-07 2025-01-16 ティアンリ バイオテック プロプライエタリ リミテッド 呼吸器疾患の処置のための化合物及び組成物
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
CA3125626A1 (en) * 2019-01-04 2020-07-09 Bellbrook Labs, Llc Inhibitors of cgas activity as therapeutic agents
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
WO2020154571A1 (en) 2019-01-24 2020-07-30 Yumanity Therapeutics, Inc. Compounds and uses thereof
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
WO2020190791A1 (en) 2019-03-15 2020-09-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (creb)
CN114072395A (zh) * 2019-04-26 2022-02-18 新基公司 杂环化合物及其治疗蠕虫感染和疾病的用途
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
DK4299135T3 (da) 2019-06-18 2025-09-08 Pfizer Benzisoxazol-sulfonamid-derivater
US11591329B2 (en) 2019-07-09 2023-02-28 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)
HRP20251148T1 (hr) 2019-09-19 2025-11-21 Novo Nordisk Health Care Ag Pripravci koji aktiviraju piruvat-kinazu r (pkr)
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation 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
EP4066832A4 (en) 2019-11-14 2024-01-03 Zincure Corp. Pharmaceutical composition for treating multiple sclerosis on basis of ampk inhibitory function and zinc homeostasis control function
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Ｆｇｆｒ阻害剤の誘導体
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
BR112022010924A2 (pt) 2019-12-06 2022-09-06 Vertex Pharma Tetra-hidrofuranos substituídos como moduladores de canais de sódio
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
AU2021325872A1 (en) * 2020-08-10 2023-03-16 Dana-Farber Cancer Institute, Inc. Substituted 1,2,4-oxadiazoles as small molecule inhibitors of ubiquitin-specific protease 28
MX2023003170A (es) * 2020-09-17 2023-03-27 Janssen Pharmaceutica Nv Moduladores de la caseina cinasa 1 delta.
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
AU2022222470A1 (en) 2021-02-19 2023-09-21 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
CA3208361A1 (en) 2021-02-19 2022-08-25 Anjali Pandey Tyk2 inhibitors and uses thereof
EP4294806A1 (en) 2021-02-19 2023-12-27 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CN121851016A (zh) * 2021-04-21 2026-04-14 长春金赛药业有限责任公司 含咪唑稠环类衍生物、其制备方法及其在医药上的应用
SMT202500481T1 (it) 2021-06-04 2026-01-12 Vertex Pharma N-(idrossialchil(etero)aril)tetraidrofuran carbossammidi come modulatori di canali del sodio
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4416146A4 (en) * 2021-10-15 2025-11-05 Lomond Therapeutics Inc 1H-PYRAZOLO[4,3-C]QUINOLINE SUBSTITUTES, THEIR PREPARATION PROCESSES AND THEIR USE
WO2023205463A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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
JP2025525514A (ja) * 2022-07-14 2025-08-05 シャンハイ、レイジング、ファーマシューティカル、カンパニー、リミテッド Ｔｐｋアゴニスト及びそれを用いた神経変性疾患の治療方法
US12600722B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
US12600723B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
UY40374A (es) 2022-08-03 2024-02-15 Novartis Ag Inhibidores de inflamasoma nlrp3
CN119855819B (zh) * 2022-10-19 2025-10-28 长春金赛药业有限责任公司 一种nk3r拮抗剂的晶型及其制备方法和应用
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
PY2404641A (es) * 2023-01-30 2024-10-03 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 SUS 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
IT202400002560A1 (it) * 2024-02-07 2025-08-07 Univ Pisa Inibitori della proteina rock per uso nel trattamento della fibrosi polmonare
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
WO2026062521A2 (en) 2024-09-18 2026-03-26 Institute Of Molecular And Clinical Ophthalmology Basel (Iob) Methods and compounds for promoting survival of photoreceptors

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
AR030587A1 (es) * 2000-09-01 2003-08-27 Sanofi Aventis Derivados de 2-piridinil-6,7,8,9-tetrahidropirimido[1,2-a]pirimidin-4-ona y 7-piridinil-2,3-dihidroimidazo[1,2-a]pirimidin-5(1h)-ona
WO2002022605A1 (en) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
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
ES2289274T3 (es) * 2002-03-08 2008-02-01 Eli Lilly And Company 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
AU2003229305A1 (en) * 2002-05-17 2003-12-02 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-Beta 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
CA2535980A1 (en) * 2003-06-06 2005-01-06 The Trustees Of The University Of Pennsylvania P38 kinase inhibitor compositions and methods of use
GB0314943D0 (en) 2003-06-25 2003-07-30 Proteome Sciences Plc Screening methods
CA2561895A1 (en) * 2004-04-13 2005-10-27 Icagen, Inc. Polycyclic pyrimidines as potassium ion channel modulators
ATE445396T1 (de) * 2004-08-19 2009-10-15 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
JP2009541321A (ja) * 2006-06-21 2009-11-26 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー 細胞増殖阻害剤としてのピラジノン
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
CA2668454A1 (en) * 2006-11-02 2008-05-08 F. Hoffmann-La Roche Ag Substituted 2-imidazoles
CA2668744C (en) * 2006-11-17 2015-09-15 Queen's University At Kingston Compounds and methods for treating protein folding disorders
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
WO2008156715A1 (en) * 2007-06-20 2008-12-24 Merck & Co., Inc. 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
WO2009073141A2 (en) * 2007-11-28 2009-06-11 Strittmatter Stephen M Nogo receptor binding small molecules to promote axonal growth
WO2009086303A2 (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
CA2787365A1 (en) * 2010-01-25 2011-07-28 Chdi Foundation, Inc. Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
WO2012080729A2 (en) * 2010-12-14 2012-06-21 Electrophoretics Limited CASEIN KINASE 1δ (CK1δ) INHIBITORS
DK3081568T3 (da) 2011-05-09 2020-02-24 Eip Pharma Llc Sammensætninger og fremgangsmåder til behandling af alzheimers sygdom

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