EA201390879A1 - Трициклические ингибиторы pi3k и способы их применения - Google Patents

Трициклические ингибиторы pi3k и способы их применения

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Publication number
EA201390879A1
EA201390879A1 EA201390879A EA201390879A EA201390879A1 EA 201390879 A1 EA201390879 A1 EA 201390879A1 EA 201390879 A EA201390879 A EA 201390879A EA 201390879 A EA201390879 A EA 201390879A EA 201390879 A1 EA201390879 A1 EA 201390879A1
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Eurasian Patent Office
Prior art keywords
formula
compounds
methods
pi3k
tricyclic
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EA201390879A
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English (en)
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EA026134B1 (ru
Inventor
Дженафер Дотсон
Роберт Эндрю Хилд
Тимоти Хеффрон
Грэхэм Элджин Джонс
Сасси Лерш Кринтел
Невиль Джэймс Маклин
Чуди Ндубаку
Алан Г. Оливеро
Лоран Салфати
Лан Ванг
БинКинг Вей
Original Assignee
Ф.Хоффманн-Ля Рош Аг
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Application filed by Ф.Хоффманн-Ля Рош Аг filed Critical Ф.Хоффманн-Ля Рош Аг
Publication of EA201390879A1 publication Critical patent/EA201390879A1/ru
Publication of EA026134B1 publication Critical patent/EA026134B1/ru

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Abstract

Описаны трициклические соединения ингибиторы PI3K формулы I с противораковой активностью, противовоспалительной активностью или иммунорегуляторными свойствами и, более конкретно, с модулирующей или ингибирующей PI3 киназу активностью. Описаны способы применения трициклических ингибиторов-соединений PI3K формулы I для in vitro, in situ и in vivoдиагностики или лечения клеток млекопитающего, организмов или связанных патологических состояний.Соединения формулы I, включая их стереоизомеры, геометрические изомеры, таутомеры и фармацевтически приемлемые соли. Прерывистая линия обозначает возможную двойную связь и по меньшей мере одна прерывистая линия является двойной связью. Заместители являются такими, как описано в описании.
EA201390879A 2010-12-16 2011-12-15 Трициклические ингибиторы pi3k и способы их применения EA026134B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US42369410P 2010-12-16 2010-12-16
PCT/US2011/065101 WO2012082997A1 (en) 2010-12-16 2011-12-15 Tricyclic pi3k inhibitor compounds and methods of use

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EA201390879A1 true EA201390879A1 (ru) 2013-09-30
EA026134B1 EA026134B1 (ru) 2017-03-31

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US (5) US8883799B2 (ru)
EP (3) EP2813506B1 (ru)
JP (1) JP5775171B2 (ru)
KR (2) KR20140099556A (ru)
CN (2) CN105859735B (ru)
AR (2) AR084312A1 (ru)
AU (1) AU2011343712B2 (ru)
BR (1) BR112013014914B8 (ru)
CA (1) CA2820078C (ru)
CL (1) CL2013001093A1 (ru)
CO (1) CO6710942A2 (ru)
CR (1) CR20130247A (ru)
DK (1) DK2651951T3 (ru)
EA (1) EA026134B1 (ru)
EC (1) ECSP13012692A (ru)
ES (1) ES2530545T3 (ru)
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HR (1) HRP20150127T1 (ru)
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Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104583215B (zh) * 2012-08-30 2016-12-07 霍夫曼-拉罗奇有限公司 二噁烯并-和噁嗪-[2,3-d]嘧啶pi3k抑制剂化合物及使用方法
US9676765B2 (en) 2012-11-07 2017-06-13 Karus Therapeutics Limited Histone deacetylase inhibitors and their use in therapy
AR095443A1 (es) * 2013-03-15 2015-10-14 Fundación Centro Nac De Investig Oncológicas Carlos Iii Heterociclos condensados con acción sobre atr
RS57816B1 (sr) 2013-05-10 2018-12-31 Karus Therapeutics Ltd Inhibitori histon deacetilaze
WO2014185367A1 (ja) * 2013-05-13 2014-11-20 第一三共株式会社 モルホリノプリン誘導体の製造方法
CN104557955B (zh) * 2013-10-23 2017-05-03 上海汇伦生命科技有限公司 作为PI3K/mTOR抑制剂的三环类化合物，其制备方法和用途
UY35916A (es) * 2013-12-24 2015-06-30 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Compuestos tricíclicos como agentes antineoplásicos inhibidores del bromodominio
SG11201608303QA (en) 2014-04-04 2016-11-29 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
EP3233852B1 (en) * 2014-12-18 2020-07-15 F. Hoffmann-La Roche AG Tetrahydro-pyrido[3,4-b]indoles as estrogen receptor modulators and uses thereof
JP6038111B2 (ja) * 2014-12-27 2016-12-07 ヤマサ醤油株式会社 多置換７−デアザプリン誘導体合成のための２，６−ジクロロ−８−ヨード−７−デアザプリン
EP3256476B1 (en) * 2015-02-11 2019-01-23 Sunovion Pharmaceuticals Inc. Fused dihydro-4h-pyrazolo[5,1-c][1,4]oxazinyl compounds and analogs for treating cns disorders
CN107406462B (zh) * 2015-03-09 2020-11-10 豪夫迈·罗氏有限公司 三环dlk抑制剂及其用途
TWI689508B (zh) 2015-03-30 2020-04-01 日商第一三共股份有限公司 可作爲ｐｉ３ｋ抑制劑之吡唑衍生物及其用途
WO2017004133A1 (en) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
GB201514751D0 (en) * 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
CA3004534C (en) * 2015-11-23 2023-11-07 Council Of Scientific & Industrial Research Fused pyrimidines as isoform selective phosphoinositide-3-kinase-alpha inhibitors and process for preparation thereof
AU2016369528B2 (en) 2015-12-16 2021-04-22 Genentech, Inc. Process for the preparation of tricyclic PI3K inhibitor compounds and methods for using the same for the treatment of cancer
JP7025350B2 (ja) * 2016-05-24 2022-02-24 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 三環式ヘテロシリック誘導体
WO2018005860A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based antiproliferative agents
CN106008528A (zh) * 2016-07-28 2016-10-12 安徽赛迪生物科技有限公司 一种合成4-氯-5,7-二氢-6h-吡咯并[2,3-d]嘧啶-6-酮的方法
KR20190065246A (ko) 2016-07-29 2019-06-11 선오비온 파마슈티컬스 인코포레이티드 화합물 및 조성물 및 이들의 용도
CN116283877A (zh) 2016-07-29 2023-06-23 赛诺维信制药公司 化合物、组合物及其用途
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201817731A (zh) * 2016-09-29 2018-05-16 日商第一三共股份有限公司 ［２－（１－甲基－１ｈ－吡唑－４－基）－６－（ 啉－４－基）－９ｈ－嘌呤－８－基］［４－（ 啉－４－基）哌啶－１－基］甲酮及其製藥上容許鹽之結晶
WO2018075937A1 (en) 2016-10-21 2018-04-26 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
AU2017368597C1 (en) 2016-12-02 2024-03-28 Daiichi Sankyo Company,Limited Novel endo-β-N-acetylglucosaminidase
WO2019028165A1 (en) 2017-08-02 2019-02-07 Sunovion Pharmaceuticals Inc. ISOCHROMAN COMPOUNDS AND USES THEREOF
AU2019335968B2 (en) 2018-09-07 2024-03-07 Otsuka Pharmaceutical Co., Ltd. Heterocyclic compound
US20210395228A1 (en) 2018-10-02 2021-12-23 Syngenta Participations Ag Pesticidally active benzene- and azine-amide compounds
CN109134480A (zh) * 2018-10-19 2019-01-04 辽宁大学 一种新型4-苯氨基苯并呋喃并[2,3-d]嘧啶类化合物及其应用
KR20210139376A (ko) 2019-03-14 2021-11-22 선오비온 파마슈티컬스 인코포레이티드 이소크로마닐 화합물의 염, 및 이의 결정성 형태, 제조방법, 치료 용도 및 약제학적 조성물
TW202102489A (zh) 2019-03-29 2021-01-16 瑞士商先正達農作物保護公司 殺有害生物活性之二𠯤-醯胺化合物
PE20220171A1 (es) 2019-04-05 2022-01-28 Syngenta Crop Protection Ag Compuestos de diazina-amida activos como pesticidas
JP2022528181A (ja) 2019-04-11 2022-06-08 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺有害生物的に有効なジアジン－アミド化合物
BR112022003375A2 (pt) 2019-08-23 2022-05-17 Syngenta Crop Protection Ag Compostos de pirazina-amida pesticidamente ativos
GB201913921D0 (en) * 2019-09-26 2019-11-13 Sentinel Oncology Ltd Pharmaceutical compounds
CN113004303A (zh) * 2019-12-18 2021-06-22 江苏恒瑞医药股份有限公司 嘧啶并噁嗪类三环衍生物、其制备方法及其在医药上的应用
IL298294A (en) 2020-05-19 2023-01-01 G1 Therapeutics Inc Cyclin-dependent kinase inhibitory compounds for the treatment of medical disorders
EP4352050A1 (en) 2021-06-09 2024-04-17 Syngenta Crop Protection AG Pesticidally active diazine-amide compounds
WO2023072849A1 (en) 2021-10-27 2023-05-04 Syngenta Crop Protection Ag Pesticidally active pyridazinone compounds
WO2023104714A1 (en) 2021-12-10 2023-06-15 Syngenta Crop Protection Ag Pesticidally active pyridazinone compounds
KR20230115493A (ko) 2022-01-27 2023-08-03 인제대학교 산학협력단 특이적 PI3K p110δ 억제제를 유효성분으로 함유하는 스타스민1 관련 질환 예방 또는 치료용 조성물
CN115413669B (zh) * 2022-06-14 2024-03-15 湖南大学 激酶抑制剂及其组合剂在提高植物青枯病抗性中的应用
CN115403593B (zh) * 2022-09-22 2024-02-02 河南师范大学 一种环加成合成手性嘌呤[3,2-c]并噁唑化合物的方法

Family Cites Families (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3016378A (en) 1959-07-01 1962-01-09 Thomae Gmbh Dr K Amino-substituted purine derivatives
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
JPS4872196U (ru) 1971-12-11 1973-09-10
JPS4872196A (ru) * 1971-12-27 1973-09-29
GB1570494A (en) 1975-11-28 1980-07-02 Ici Ltd Thienopyrimidine derivatives and their use as pesticides
US4510144A (en) * 1981-08-26 1985-04-09 Newport Pharmaceuticals International Methods of imparting immunomodulating activity with dihydrothiazolo purine derivatives
JPS60260579A (ja) 1984-01-13 1985-12-23 Yoshitomi Pharmaceut Ind Ltd プリン誘導体
DE3406533A1 (de) 1984-02-23 1985-08-29 Boehringer Mannheim Gmbh, 6800 Mannheim Verwendung von adenosin-derivaten als antiallergica und arzneimittel, die diese enthalten
JPS6216477A (ja) 1985-07-15 1987-01-24 Maruishi Seiyaku Kk 抗ウイルス活性を有する２−（４−ピリジルアミノメチル）−ベンズイミダゾ−ル誘導体
US4740230A (en) 1985-09-13 1988-04-26 Idemitsu Kosan Company Limited Triazine derivatives, and herbicides containing the derivatives as the effective component
US5583024A (en) 1985-12-02 1996-12-10 The Regents Of The University Of California Recombinant expression of Coleoptera luciferase
CA1279648C (en) 1986-07-11 1991-01-29 Haruo Kuriyama 2-(4-pyridylaminometyl)-benzimidazole derivatives having antiviral activity
US4932998A (en) 1986-09-30 1990-06-12 Idemitsu Kosan Company Limited Triazine derivatives, and herbicides comprising the same as the effective ingredient
US5332744A (en) 1989-05-30 1994-07-26 Merck & Co., Inc. Substituted imidazo-fused 6-membered heterocycles as angiotensin II antagonists
US5846824A (en) 1994-02-07 1998-12-08 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
US6274327B1 (en) 1992-04-13 2001-08-14 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
JP3093112B2 (ja) 1994-09-01 2000-10-03 新日本製鐵株式会社 塗覆装鋼製打ち込み部材
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
JPH08336393A (ja) 1995-04-13 1996-12-24 Mitsubishi Chem Corp 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法
US5866702A (en) 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
US6602677B1 (en) 1997-09-19 2003-08-05 Promega Corporation Thermostable luciferases and methods of production
DE19920936A1 (de) 1999-05-07 2000-11-09 Basf Ag Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung
JP3649395B2 (ja) 2000-04-27 2005-05-18 山之内製薬株式会社 縮合ヘテロアリール誘導体
US6608053B2 (en) 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
EP1409125B1 (en) 2001-07-12 2016-04-20 Reaxa Limited Microencapsulated catalyst, methods of preparation and methods of use thereof
EP1427413A2 (en) 2001-09-13 2004-06-16 Synta Pharmaceuticals Corporation 2-aroylimidazole compounds for treating cancer
JP2005512972A (ja) 2001-10-12 2005-05-12 アイアールエム エルエルシー キナーゼ阻害剤足場およびそれらの調製方法
US6949644B2 (en) 2001-10-12 2005-09-27 Irm Llc Methods for the synthesis of substituted purines
US7354932B2 (en) 2001-12-21 2008-04-08 Anormed, Inc. Chemokine receptor binding heterocyclic compounds with enhanced efficacy
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
EP1551410A2 (en) 2002-09-06 2005-07-13 Smithkline Beecham Corporation Novel compounds
CA2502356A1 (en) 2002-10-15 2004-04-29 Synta Pharmaceuticals Corp. Aromatic bicyclic heterocyles to modulate 1l - 12 production
WO2005000404A2 (en) 2003-05-29 2005-01-06 Synta Pharmaceuticals, Corp. Heterocyclic compounds for preventing and treating disorders associated with excessive bone loss
WO2005014558A1 (en) 2003-08-05 2005-02-17 Vertex Pharmaceuticals Incorporated Condensed pyramidine compounds as inhibitors of voltage-gated ion channels
US20060074124A1 (en) 2003-09-12 2006-04-06 Andrew Napper Methods of treating a disorder
WO2005028434A2 (en) 2003-09-18 2005-03-31 Conforma Therapeutics Corporation Novel heterocyclic compounds as hsp90-inhibitors
WO2005039506A2 (en) 2003-10-24 2005-05-06 Exelixis, Inc. P70s6 kinase modulators and method of use
US20050239806A1 (en) 2004-01-13 2005-10-27 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
CA2575560A1 (en) 2004-08-02 2006-02-23 Smithkline Beecham Corporation Chemical compounds
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
US20080269239A1 (en) 2004-11-11 2008-10-30 Argenta Discovery Ltd. Pyrimidine Compounds as Histamine Modulators
KR20130058072A (ko) 2005-10-07 2013-06-03 엑셀리시스, 인코포레이티드 증식성 질환의 치료를 위한 ｍｅｋ 억제제로서의 아제티딘
GB2431156A (en) 2005-10-11 2007-04-18 Piramed Ltd 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase
PT2041139E (pt) 2006-04-26 2012-01-13 Hoffmann La Roche Compostos farmacêuticos
WO2007129161A2 (en) 2006-04-26 2007-11-15 F. Hoffmann-La Roche Ag Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor
WO2007127183A1 (en) 2006-04-26 2007-11-08 Genentech, Inc. Phosphoinositide 3-kinase inhibitor compounds and pharmaceutical compositions containing them
KR20090021155A (ko) 2006-04-26 2009-02-27 에프. 호프만-라 로슈 아게 Ｐｉ3ｋ 억제제로서의 피리미딘 유도체
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
RU2445312C2 (ru) 2006-08-23 2012-03-20 Кудос Фармасьютиклз Лимитед ПРОИЗВОДНЫЕ 2-МЕТИЛМОРФОЛИН ПИРИДО-, ПИРАЗО- И ПИРИМИДО-ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR
MX2009002927A (es) 2006-09-15 2009-03-31 Pfizer Prod Inc Compuestos de pirido (2,3-d)pirimidinona y su uso como inhibidores de la enzima fosfoinositido 3.
WO2008039882A1 (en) 2006-09-30 2008-04-03 Sanofi-Aventis U.S. Llc A combination of niacin and a prostaglandin d2 receptor antagonist
TW200831104A (en) 2006-10-04 2008-08-01 Pharmacopeia Inc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
JP5443988B2 (ja) 2006-10-16 2014-03-19 メディシス・ファーマシューティカル・コーポレーション 治療用のピラゾリルチエノピリジン
AU2007333243B2 (en) 2006-12-07 2013-03-14 F. Hoffmann-La Roche Ag Phosphoinositide 3-kinase inhibitor compounds and methods of use
KR101460816B1 (ko) 2006-12-07 2014-11-12 에프. 호프만-라 로슈 아게 포스포이노시타이드 3-키나제 억제제 화합물 및 그의 사용 방법
US20080233127A1 (en) 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
WO2008116910A1 (en) 2007-03-28 2008-10-02 Neurosearch A/S Purinyl derivatives and their use as potassium channel modulators
KR20100016433A (ko) 2007-04-12 2010-02-12 에프. 호프만-라 로슈 아게 포스파티딜이노시톨-3-키나제의 저해제로서의 피리미딘 유도체
WO2008152394A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
EP2158207B1 (en) 2007-06-12 2011-05-25 F. Hoffmann-La Roche AG Thiazoliopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase
WO2008152387A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Quinazoline derivatives as pi3 kinase inhibitors
JP5492769B2 (ja) * 2007-06-26 2014-05-14 サノフイ 縮環されたベンゾイミダゾール及びアザベンゾイミダゾールの位置選択的金属触媒合成
WO2009034386A1 (en) 2007-09-13 2009-03-19 Astrazeneca Ab Derivatives of adenine and 8-aza-adenine and uses thereof-796
EP2207781B1 (en) 2007-09-24 2012-11-28 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
WO2009045174A1 (en) 2007-10-05 2009-04-09 S*Bio Pte Ltd 2-morpholinylpurines as inhibitors of pi3k
GB0721095D0 (en) 2007-10-26 2007-12-05 Piramed Ltd Pharmaceutical compounds
CA2703138A1 (en) 2007-10-26 2009-04-30 F. Hoffmann-La Roche Ag Purine derivatives useful as pi3 kinase inhibitors
GB0725218D0 (en) 2007-12-24 2008-02-06 Syngenta Ltd Chemical compounds
JP5608099B2 (ja) 2008-01-30 2014-10-15 ジェネンテック， インコーポレイテッド ピラゾロピリミジンｐｉ３ｋ阻害剤化合物および使用方法
WO2009146406A1 (en) 2008-05-30 2009-12-03 Genentech, Inc. Purine pi3k inhibitor compounds and methods of use
ES2398423T3 (es) 2008-06-20 2013-03-19 Astrazeneca Ab Composiciones con y procedimiento para pirido[2,3-D]pirimidinas sustituídas con metilmorfolina
JP2011529920A (ja) 2008-07-31 2011-12-15 ジェネンテック， インコーポレイテッド ピリミジン化合物、組成物及び使用方法
AU2009296931A1 (en) 2008-09-26 2010-04-01 Merck Sharp & Dohme Corp. Oxazolobenzimidazole derivatives
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
GB2465405A (en) * 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
SG171765A1 (en) 2008-11-20 2011-07-28 Genentech Inc Pyrazolopyridine pi3k inhibitor compounds and methods of use
US8158625B2 (en) 2009-05-27 2012-04-17 Genentech, Inc. Bicyclic indole-pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use
MX2011012520A (es) 2009-05-27 2011-12-12 Hoffmann La Roche Compuestos inhibidores de pi3k de pirimidina biciclicos selectivos para p110 delta y metodos de uso de los mismos.
WO2010151601A1 (en) 2009-06-24 2010-12-29 Genentech, Inc. Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use
CA2771594C (en) * 2009-08-20 2018-05-01 Karus Therapeutics Limited Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors
CN102020657A (zh) * 2009-09-11 2011-04-20 上海艾力斯医药科技有限公司 稠合杂芳基衍生物、制备方法及其应用
KR20120081164A (ko) 2009-09-29 2012-07-18 엑스커버리 홀딩 컴퍼니 엘엘씨 Ｐｉ3ｋ(델타) 선택적 억제제
EP2539337A1 (en) 2010-02-22 2013-01-02 F. Hoffmann-La Roche AG Pyrido[3,2-d]pyrimidine pi3k delta inhibitor compounds and methods of use
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
BR112013000867A2 (pt) 2010-07-14 2016-05-17 Hoffmann La Roche composto de purina seletivos para delta p110 de pi3k e métodos de uso.
KR20130116358A (ko) 2011-02-09 2013-10-23 에프. 호프만-라 로슈 아게 Pi3 키나아제 억제제로서 헤테로사이클릭 화합물
JP2014515390A (ja) 2011-06-03 2014-06-30 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｐｉ３ｋ阻害剤化合物を用いた中皮腫の治療法

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