EA200600652A1 - Гетероариламины - производные пиримидина и пиридазина в качестве ингибиторов гликогенсинтаза-киназы 3-бета (ингибиторов gsk3) - Google Patents

Гетероариламины - производные пиримидина и пиридазина в качестве ингибиторов гликогенсинтаза-киназы 3-бета (ингибиторов gsk3)

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Publication number
EA200600652A1
EA200600652A1 EA200600652A EA200600652A EA200600652A1 EA 200600652 A1 EA200600652 A1 EA 200600652A1 EA 200600652 A EA200600652 A EA 200600652A EA 200600652 A EA200600652 A EA 200600652A EA 200600652 A1 EA200600652 A1 EA 200600652A1
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Eurasian Patent Office
Prior art keywords
6alkyl
optionally substituted
inhibitors
hydrogen
glycogenesis
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EA200600652A
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English (en)
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EA010859B1 (ru
Inventor
Эдди Жан Эдгар Фрейн
Петер Якобус Йоханнес Антониус Бейнстерс
Марк Виллемс
Вернер Констант Йохан Эмбрехтс
Кристофер Джон Лав
Поль Адриан Ян Жанссен
Паулус Йоаннес Леви
Ян Херес
Марк Рене Де Жонж
Люсьен Мария Хенрикус Койманс
Хендрик Мартен Винкерс
Кун Жанн Альфонс Ван Акен
Гастон Станислас Марселла Дилс
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Янссен Фармацевтика Н.В.
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Publication of EA200600652A1 publication Critical patent/EA200600652A1/ru
Publication of EA010859B1 publication Critical patent/EA010859B1/ru

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Abstract

Данное изобретение относится к соединению формулы (I)его N-оксиду, фармацевтически приемлемой аддитивной соли, четвертичному амину и стереохимически изомерной форме, где кольцо А является 6-членным замещенным гетероциклилом - производным пиримидинила или пиридазинила; Rобозначает водород; арил; формил; C-алкилкарбонил; необязательно замещенный Cалкил; Cалкилоксикарбонил; необязательно замещенный СалкилоксиСалкилкарбонил; Х обозначает прямую связь или линкерный атом или линкерную группу; Z обозначает прямую связь или линкерный атом или линкерную группу; Rобозначает водород, Cалкил, Салкенил, Салкинил, карбоцикл или гетероцикл, каждая из указанных групп может быть необязательно замещенной; Rобозначает водород; гидрокси; галоген; необязательно замещенный Cалкил или Cалкенил или Салкинил; Cалкилокси; Cалкилтио; Cалкилоксикарбонил; Cалкилкарбонилокси; карбоксил; циано; нитро; амино; моно- или ди(Cалкил)амино; полигалогенСалкил; полигалогенСалкилокси; полигалогенСалкилтио; R; R-Cалкил; R-O-; R-S-; R-C(=О)-; R-S(=О)-; R-S(=О)-; R-S(=O)-NH-; R-S(=O)-NH-; R-C(=O)-; -NHC(=O)H; -C(=O)NHNH; R-C(=O)-NH-; R-C(=O)-NH-; -C(=NH)R; -C(=NH)R; Rобозначает необязательно замещенный гетероцикл, при условии, что -X-Rи/или Rявляется другим, чем водород; их применению, содержащим их фармацевтическим композициям и способам их получения.
EA200600652A 2001-11-01 2002-10-29 Гетероариламины - производные пиримидина и пиридазина в качестве ингибиторов гликогенсинтаза-киназы 3-бета (ингибиторов gsk3) EA010859B1 (ru)

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EA010859B1 EA010859B1 (ru) 2008-12-30

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EA200400617A EA007298B1 (ru) 2001-11-01 2002-10-29 Гетероариламины в качестве ингибиторов гликогенсинтаза-киназы 3-бета (ингибиторов gsk3)

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US (1) US7514445B2 (ru)
EP (1) EP1448556A1 (ru)
JP (1) JP2005507423A (ru)
KR (1) KR20040048920A (ru)
CN (1) CN100491371C (ru)
AU (1) AU2002363176B2 (ru)
BR (1) BR0213792A (ru)
CA (1) CA2463822A1 (ru)
EA (2) EA010859B1 (ru)
HU (1) HUP0402106A3 (ru)
IL (1) IL161662A0 (ru)
MX (1) MXPA04004178A (ru)
NO (1) NO20041911L (ru)
NZ (1) NZ531853A (ru)
PL (1) PL369259A1 (ru)
WO (1) WO2003037891A1 (ru)

Families Citing this family (152)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003076434A1 (en) 2002-03-09 2003-09-18 Astrazeneca Ab 4- imidazolyl substuited pyrimidine derivatives with cdk inhibitiory activity
GB0205690D0 (en) 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
GB0205693D0 (en) 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
CN1717396A (zh) * 2002-11-28 2006-01-04 舍林股份公司 Chk－、Pdk－和Akt－抑制嘧啶,其制备及作为药物的用途
BRPI0406809A (pt) * 2003-01-17 2005-12-27 Warner Lambert Co Heterociclos substituìdos de 2-aminopiridina como inibidores da proliferação celular
GB0311274D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
GB0311276D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
EP1727806A1 (en) * 2004-01-16 2006-12-06 Novartis AG 2,4-diaminopyrimidines and their use for inducing cardiomyogenesis
TW200528101A (en) 2004-02-03 2005-09-01 Astrazeneca Ab Chemical compounds
JP2007531753A (ja) 2004-03-31 2007-11-08 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 非イミダゾール系複素環式化合物
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
WO2005113494A2 (en) 2004-05-07 2005-12-01 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
US7879853B2 (en) 2004-06-28 2011-02-01 Bayer Schering Pharma Ag 4,6-disubstituted pyrimidines and their use as protein kinase inhibitors
GB0416699D0 (en) 2004-07-27 2004-09-01 Prometic Biosciences Ltd Prion protein ligands and methods of use
GB0428082D0 (en) 2004-12-22 2005-01-26 Welcome Trust The Ltd Therapeutic compounds
WO2006117212A2 (en) 2005-05-04 2006-11-09 Develogen Aktiengesellschaft Use of gsk-3 inhibitors for preventing and treating pancreatic autoimmune disorders
CA2609716C (en) 2005-05-26 2014-10-14 Tibotec Pharmaceuticals Ltd. Process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)amino]benzonitrile
JP5614930B2 (ja) * 2005-06-10 2014-10-29 プロメティック バイオサイエンシズ，リミテッド タンパク質結合性リガンドとしてのトリアジン
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
CN101321531A (zh) * 2005-10-03 2008-12-10 阿斯利康(瑞典)有限公司 嘧啶衍生物在制备用于预防和/或治疗阿尔茨海默病的药物中的用途
AR058073A1 (es) * 2005-10-03 2008-01-23 Astrazeneca Ab Derivados de imidazol 5-il-pirimidina, procesos de obtencion, composiciones farmaceuticas y usos
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
WO2007104035A1 (en) * 2006-03-08 2007-09-13 Braincells, Inc. Modulation of neurogenesis by nootropic agents
US20100216734A1 (en) * 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
MX2008014320A (es) 2006-05-09 2009-03-25 Braincells Inc Neurogenesis mediada por el receptor de 5-hidroxitriptamina.
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
AU2007256931B2 (en) 2006-05-30 2013-01-24 Janssen Pharmaceutica N.V. Substituted pyridyl amide compounds as modulators of the histamine H3 receptor
JP5306190B2 (ja) 2006-06-15 2013-10-02 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ２−アニリノ−４−アミノアルキレンアミノピリミジン
US20070293494A1 (en) * 2006-06-15 2007-12-20 Djung Jane F 2-Anilino-4-(Heterocyclic) Amino-Pyrimidines
MX2009002496A (es) * 2006-09-08 2009-07-10 Braincells Inc Combinaciones que contienen un derivado de 4-acilaminopiridina.
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
JP2010518014A (ja) * 2007-01-31 2010-05-27 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用な２−アミノピリジン誘導体
RU2009143753A (ru) * 2007-04-27 2011-06-10 Астразенека Аб (Se) Производные n'-(фенил)-n-(морфолин-4-ил-пиридин-2-ил)-пиримидин-2, 4-идиамина в качестве ингибиторов ернв4 киназы для лечения пролиферативных состояний
JP2010526856A (ja) * 2007-05-16 2010-08-05 バイエル・クロツプサイエンス・エス・アー 殺菌剤フェニル−ピリミジニル−アミノ誘導体
EP2152079A4 (en) * 2007-06-04 2011-03-09 Avila Therapeutics Inc HETEROCYCLIC COMPOUNDS AND USES THEREOF
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
US7989465B2 (en) * 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
CA2920996A1 (en) * 2007-10-19 2009-04-23 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
MX2010005033A (es) 2007-11-06 2010-05-27 Du Pont Aminas heterociclicas fungicidas.
KR101546712B1 (ko) 2007-11-20 2015-08-24 얀센 파마슈티카 엔.브이. 히스타민 ｈ3 수용체의 조절제로서 사이클로알킬옥시- 및 헤테로사이클로알킬옥시피리딘 화합물
ES2535083T3 (es) * 2007-12-20 2015-05-05 Astrazeneca Ab Compuestos de carbamoilo como inhibidores 190 de DGAT1
NZ613219A (en) 2008-01-04 2014-11-28 Intellikine Llc Heterocyclic containing entities, compositions and methods
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
JPWO2009107391A1 (ja) * 2008-02-27 2011-06-30 武田薬品工業株式会社 ６員芳香環含有化合物
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
SI2300013T1 (en) 2008-05-21 2018-03-30 Adriad Pharmacaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
JP5658662B2 (ja) * 2008-06-12 2015-01-28 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ ヒスタミンｈ４受容体のジアミノピリジン、ピリミジン、及びピリダジンモジュレーター
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
ES2711249T3 (es) 2008-06-27 2019-04-30 Celgene Car Llc Compuestos de heteroarilo y usos de los mismos
CA2730603C (en) 2008-07-16 2019-09-24 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
NZ590784A (en) 2008-07-23 2012-12-21 Vertex Pharma Pyrazolopyridine kinase inhibitors
WO2010011768A1 (en) 2008-07-23 2010-01-28 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
US8569337B2 (en) 2008-07-23 2013-10-29 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
MX2011001319A (es) * 2008-08-06 2011-04-05 Vertex Pharma Inhibidores de aminopiridina cinasa.
WO2010036380A1 (en) 2008-09-26 2010-04-01 Intellikine, Inc. Heterocyclic kinase inhibitors
CN102264228A (zh) 2008-10-22 2011-11-30 默沙东公司 用于抗糖尿病药的新的环状苯并咪唑衍生物
US8329914B2 (en) 2008-10-31 2012-12-11 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
US8178529B2 (en) 2009-04-15 2012-05-15 Astrazeneca Ab Imidazole substituted pyrimidines
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
JP5627675B2 (ja) 2009-05-06 2014-11-19 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ピラゾロピリジン
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
KR20120099215A (ko) * 2009-09-22 2012-09-07 뉴로내슨트, 아이엔씨. 다운 증후군을 치료하기 위한 방법 및 약학적 조성물
AU2011209651A1 (en) 2010-01-27 2012-08-09 Vertex Pharmaceuticals Incorporated Pyrazolopyrimidine kinase inhibitors
AU2011209649A1 (en) 2010-01-27 2012-08-09 Vertex Pharmaceuticals Incorporated Pyrazolopyrazine kinase inhibitors
CA2787315A1 (en) 2010-01-27 2011-08-04 Vertex Pharmaceuticals Incorporated Pyrazolopyridine kinase inhibitors
WO2011106273A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
BR112012029647A2 (pt) 2010-05-21 2016-08-02 Chemilia Ab novos derivados de pirimidinas
ES2593256T3 (es) 2010-05-21 2016-12-07 Infinity Pharmaceuticals, Inc. Compuestos químicos, composiciones y métodos para las modulaciones de cinasas
KR20130099040A (ko) 2010-08-10 2013-09-05 셀진 아빌로믹스 리서치, 인코포레이티드 Ｂｔｋ 억제제의 베실레이트 염
US20130156720A1 (en) 2010-08-27 2013-06-20 Ironwood Pharmaceuticals, Inc. Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
NZ609957A (en) 2010-11-01 2015-08-28 Celgene Avilomics Res Inc Heterocyclic compounds and uses thereof
ES2635713T3 (es) 2010-11-01 2017-10-04 Celgene Car Llc Compuestos de heteroarilo y usos de los mismos
WO2012060847A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
JP5957003B2 (ja) 2010-11-10 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド 変異体選択的ｅｇｆｒ阻害剤およびその使用
CA2817577A1 (en) 2010-11-10 2012-05-18 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
UA115767C2 (uk) 2011-01-10 2017-12-26 Інфініті Фармасьютікалз, Інк. Способи отримання ізохінолінонів і тверді форми ізохінолінонів
CA2826649C (en) 2011-02-25 2016-07-26 Merck Sharp & Dohme Corp. Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
RU2013147417A (ru) 2011-03-24 2015-04-27 Кемилиа Аб Новые производные пиримидина
EA201391626A1 (ru) 2011-05-04 2014-03-31 Ариад Фармасьютикалз, Инк. Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака
US8969363B2 (en) 2011-07-19 2015-03-03 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9056877B2 (en) 2011-07-19 2015-06-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PE20141371A1 (es) 2011-08-29 2014-10-13 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos
JP2014532658A (ja) 2011-10-28 2014-12-08 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ブルトン型チロシンキナーゼ疾患または障害を治療する方法
ES2880109T3 (es) 2012-03-15 2021-11-23 Celgene Car Llc Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico
SG10201700799WA (en) 2012-03-15 2017-02-27 Celgene Avilomics Res Inc Salts of an epidermal growth factor receptor kinase inhibitor
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
ME03300B (me) 2012-06-13 2019-07-20 Incyte Holdings Corp Supsтituisana triciklična jedinjenja као inhibiтori 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
US20140045746A1 (en) 2012-08-02 2014-02-13 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
EP2935226A4 (en) 2012-12-21 2016-11-02 Celgene Avilomics Res Inc HETEROARYL COMPOUNDS AND USES THEREOF
WO2014124230A2 (en) 2013-02-08 2014-08-14 Celgene Avilomics Research, Inc. Erk inhibitors and uses thereof
BR112015019836A2 (pt) 2013-02-22 2017-07-18 Merck Sharp & Dohme composto, composição farmacêutica, e, uso de um composto
PT2970890T (pt) 2013-03-14 2020-04-24 Massachusetts Inst Technology Composições e métodos para expansão e cultura de células estaminais epiteliais
US9650375B2 (en) 2013-03-14 2017-05-16 Merck Sharp & Dohme Corp. Indole derivatives useful as anti-diabetic agents
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
ES2657451T3 (es) 2013-04-19 2018-03-05 Incyte Holdings Corporation Heterocíclicos bicíclicos como inhibidores del FGFR
CN113388007A (zh) 2013-06-05 2021-09-14 博士医疗爱尔兰有限公司 鸟苷酸环化酶c的超纯激动剂、制备和使用所述激动剂的方法
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
EA201690713A1 (ru) 2013-10-04 2016-08-31 Инфинити Фармасьютикалз, Инк. Гетероциклические соединения и их применения
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
DK3119397T3 (da) 2014-03-19 2022-03-28 Infinity Pharmaceuticals Inc Heterocykliske forbindelser til anvendelse i behandling af PI3K-gamma-medierede lidelser
CA2945263A1 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
EP3179858B1 (en) 2014-08-13 2019-05-15 Celgene Car Llc Forms and compositions of an erk inhibitor
JP6773645B2 (ja) 2014-09-03 2020-10-21 ザ ブリガム アンド ウィミンズ ホスピタル，インコーポレイテッド 聴覚障害の治療のための内耳毛細胞を生成するための組成物、システムおよび方法
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
ES2751669T3 (es) 2015-02-20 2020-04-01 Incyte Corp Heterociclos bicíclicos como inhibidores FGFR
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
US10336734B2 (en) 2015-08-02 2019-07-02 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibitors of ACK1/TNK2 tyrosine kinase
AU2016322552B2 (en) 2015-09-14 2021-03-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
AU2017205194A1 (en) 2016-01-08 2018-07-19 Massachusetts Institute Of Technology Production of differentiated enteroendocrine cells and insulin producing cells
US10213511B2 (en) 2016-03-02 2019-02-26 Frequency Therapeutics, Inc. Thermoreversible compositions for administration of therapeutic agents
US11260130B2 (en) 2016-03-02 2022-03-01 Frequency Therapeutics, Inc. Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV
US10201540B2 (en) 2016-03-02 2019-02-12 Frequency Therapeutics, Inc. Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
EP3465212A4 (en) * 2016-05-23 2020-01-08 California Institute of Technology REGULAR FLORAL REGULATION FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
KR20190033526A (ko) 2016-06-24 2019-03-29 인피니티 파마슈티칼스, 인코포레이티드 병용 요법
US11072602B2 (en) 2016-12-06 2021-07-27 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
EP3558298A4 (en) 2016-12-20 2020-08-05 Merck Sharp & Dohme Corp. ANTIDIABETIC SPIROCHROMAN COMPOUNDS
BR112019013388A2 (pt) 2016-12-30 2020-03-03 Frequency Therapeutics, Inc. Compostos de 1h-pirrol-2,5-diona e métodos de uso dos mesmos para induzir a autorrenovação de células de suporte tronco/progenitoras
US11331313B2 (en) 2017-05-22 2022-05-17 Whitehead Institute For Biomedical Research KCC2 expression enhancing compounds 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
WO2019040750A1 (en) * 2017-08-25 2019-02-28 The Board Of Trustees Of The University Of Illinois MULTIVALENT LIGAND FOR MYOTONIC DYSTROPHY
CR20200590A (es) 2018-05-04 2021-04-26 Incyte Corp Formas sólidas de un inhibidor de fgfr y procesos para prepararlas
JP2021523118A (ja) 2018-05-04 2021-09-02 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｆｇｆｒ阻害剤の塩
CN110484555B (zh) * 2018-05-10 2021-03-23 中国农业科学院作物科学研究所 具有多籽粒簇生性状的转基因水稻的构建方法
WO2020037323A1 (en) 2018-08-17 2020-02-20 Frequency Therapeutics, Inc. Compositions and methods for generating hair cells by upregulating jag-1
WO2020037326A1 (en) 2018-08-17 2020-02-20 Frequency Therapeutics, Inc. Compositions and methods for generating hair cells by downregulating foxo
US20220133740A1 (en) 2019-02-08 2022-05-05 Frequency Therapeutics, Inc. Valproic acid compounds and wnt agonists for treating ear disorders
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
IL291901A (en) 2019-10-14 2022-06-01 Incyte Corp Bicyclyl heterocycles as fgr suppressors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP2023505257A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤の誘導体
JP2023505258A (ja) 2019-12-04 2023-02-08 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
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0164204A1 (en) 1984-05-12 1985-12-11 FISONS plc Novel pharmaceutically useful pyrimidines
SG47583A1 (en) 1986-01-13 1998-04-17 American Cyanamid Co 4,5,6-Substituted-n- (substituted-phenyl) -2- pyrimidinamines
US4966622A (en) 1988-04-12 1990-10-30 Ciba-Geigy Corporation N-phenyl-N-pyrimidin-2-ylureas
GB9012592D0 (en) 1990-06-06 1990-07-25 Smithkline Beecham Intercredit Compounds
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
US5516775A (en) 1992-08-31 1996-05-14 Ciba-Geigy Corporation Further use of pyrimidine derivatives
JP3588116B2 (ja) * 1993-10-01 2004-11-10 ノバルティス アクチェンゲゼルシャフト 薬理活性のピリミジンアミン誘導体およびその製造方法
KR100330553B1 (ko) 1993-10-01 2002-11-27 노파르티스 아게 약물학적활성피리딘유도체및그의제조방법
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
WO1997041854A1 (en) 1996-05-07 1997-11-13 The Trustees Of The University Of Pennsylvania Inhibitors of glycogen synthase kinase-3 and methods for identifying and using the same
NO311614B1 (no) 1996-10-01 2001-12-17 Janssen Pharmaceutica Nv Substituerte diamino-1,3,5-triazinderivater
GB9622363D0 (en) 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
GB9705361D0 (en) * 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
SK287996B6 (sk) 1998-03-27 2012-09-03 Janssen Pharmaceutica N. V. Pyrimide compound, pharmaceutical composition the compound is comprised, method for preparation thereof, combination and product containing the composition and use of the pyrimide compound
ATE274510T1 (de) 1998-06-19 2004-09-15 Chiron Corp Glycogen synthase kinase 3 inhibitoren
HU230394B1 (hu) 1998-11-10 2016-04-28 Janssen Pharmaceutica N.V. HIV-vírus szaporodását gátló pirimidin-származékok
IL144910A0 (en) 1999-04-15 2002-06-30 Bristol Myers Squibb Co Cyclic compounds and pharmaceutical compositions containing the same
CA2269364A1 (en) * 1999-04-19 2000-10-19 Vasogen Ireland Limited Treatment of inflammatory and allergic disorders
BR0013551A (pt) 1999-08-13 2003-06-17 Vertex Pharma Inibidores de cinases n-terminal cjun (jnk) e outras cinases de proteìnas
GB9924862D0 (en) * 1999-10-20 1999-12-22 Celltech Therapeutics Ltd Chemical compounds
CA2396693A1 (en) * 1999-12-28 2001-07-05 Stephen T. Wrobleski Cytokine, especially tnf-alpha, inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
CA2400447C (en) * 2000-02-17 2008-04-22 Amgen Inc. Kinase inhibitors
CN100355751C (zh) * 2000-03-29 2007-12-19 西克拉塞尔有限公司 2－取代的4－杂芳基－嘧啶、其组合物及其用途

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