CN101511840A - 磷酸肌醇3-激酶抑制剂化合物及其使用方法 - Google Patents

磷酸肌醇3-激酶抑制剂化合物及其使用方法 Download PDF

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Publication number
CN101511840A
CN101511840A CNA2007800241241A CN200780024124A CN101511840A CN 101511840 A CN101511840 A CN 101511840A CN A2007800241241 A CNA2007800241241 A CN A2007800241241A CN 200780024124 A CN200780024124 A CN 200780024124A CN 101511840 A CN101511840 A CN 101511840A
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bases
pyrimidine
indazole
morpholinoes
thieno
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Pending
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CNA2007800241241A
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Chinese (zh)
Inventor
G·凯斯坦多
R·戈德史密斯
J·冈茨纳
T·赫夫伦
K·梅尔斯基
S·马蒂厄
A·奥利夫罗
D·P·萨瑟林
V·徐
王淑梅
C·维斯曼
朱炳炎
J·多森
A·雷尔克斯
S·舒特尔沃思
S·奥克森富德
T·汉科克斯
T·贝利斯
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F Hoffmann La Roche AG
Genentech Inc
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F Hoffmann La Roche AG
Genentech Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38561741&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN101511840(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by F Hoffmann La Roche AG, Genentech Inc filed Critical F Hoffmann La Roche AG
Publication of CN101511840A publication Critical patent/CN101511840A/zh
Pending legal-status Critical Current

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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D495/04—Ortho-condensed systems

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CNA2007800241241A 2006-04-26 2007-04-24 磷酸肌醇3-激酶抑制剂化合物及其使用方法 Pending CN101511840A (zh)

Applications Claiming Priority (2)

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US79504706P 2006-04-26 2006-04-26
US60/795,047 2006-04-26

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US (2) US7846929B2 (enExample)
EP (1) EP2046799B1 (enExample)
JP (1) JP5291616B2 (enExample)
KR (1) KR101402474B1 (enExample)
CN (1) CN101511840A (enExample)
AR (1) AR060632A1 (enExample)
AU (1) AU2007243466B2 (enExample)
BR (1) BRPI0710908A2 (enExample)
CA (1) CA2650295C (enExample)
CL (1) CL2007001166A1 (enExample)
IL (1) IL194761A0 (enExample)
MX (1) MX2008013583A (enExample)
NO (1) NO20084927L (enExample)
RU (1) RU2437888C2 (enExample)
TW (1) TW200801012A (enExample)
WO (1) WO2007127183A1 (enExample)
ZA (1) ZA200810023B (enExample)

Cited By (15)

* Cited by examiner, † Cited by third party
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CN102498115A (zh) * 2009-08-20 2012-06-13 卡鲁斯治疗有限公司 作为磷酸肌醇3-激酶抑制剂的三环杂环化合物
CN102625708A (zh) * 2009-09-09 2012-08-01 阿维拉制药公司 Pi3激酶抑制剂及其用途
CN102643272A (zh) * 2011-12-30 2012-08-22 沈阳药科大学 新的噻吩并[3,2-d]嘧啶类化合物
CN102781923A (zh) * 2010-01-26 2012-11-14 贝林格尔.英格海姆国际有限公司 5-炔基-嘧啶化合物
CN103957902A (zh) * 2011-10-13 2014-07-30 基因泰克公司 药理学诱导的胃酸过少的治疗
CN105461736A (zh) * 2011-04-01 2016-04-06 柯瑞斯公司 具有锌结合位的磷脂酰肌醇3-激酶抑制剂
CN107098846A (zh) * 2016-02-26 2017-08-29 中国医学科学院药物研究所 N-酰基磺酰胺类FBPase抑制剂、其制备方法、药物组合物及用途
CN109796465A (zh) * 2017-11-16 2019-05-24 华中科技大学同济医学院附属协和医院 靶向pet显像化合物、包含该化合物的显象剂及其制备方法和用途
CN111032662A (zh) * 2017-06-21 2020-04-17 尚医治疗有限责任公司 与ras超家族相互作用的用于治疗癌症、炎性疾病、ras蛋白病和纤维化疾病的化合物
CN114539293A (zh) * 2022-02-24 2022-05-27 佛山市晨康生物科技有限公司 一种噻吩并嘧啶类化合物或其药学上可接受的盐及其制备方法和应用
WO2022184152A1 (zh) * 2021-03-03 2022-09-09 劲方医药科技(上海)有限公司 稠环取代的六元杂环化合物及其制法和用途
WO2022268025A1 (zh) * 2021-06-22 2022-12-29 成都苑东生物制药股份有限公司 Atr抑制剂及其用途
CN115991716A (zh) * 2021-10-19 2023-04-21 中国药科大学 嘧啶并环类化合物及其衍生物、制备方法、药物组合物和应用
WO2023227139A1 (zh) * 2022-05-25 2023-11-30 沈阳药科大学 稠合嘧啶类衍生物及其应用
TWI854426B (zh) * 2022-01-04 2024-09-01 大陸商勁方醫藥科技(上海)有限公司 稠環取代的六員雜環化合物及其製法和用途

Families Citing this family (106)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998010381A1 (en) * 1996-09-04 1998-03-12 Intertrust Technologies Corp. Trusted infrastructure support systems, methods and techniques for secure electronic commerce, electronic transactions, commerce process control and automation, distributed computing, and rights management
MX2008013584A (es) * 2006-04-26 2009-03-23 Genentech Inc Compuestos farmaceuticos.
KR101402474B1 (ko) 2006-04-26 2014-06-19 제넨테크, 인크. 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물
AR064155A1 (es) 2006-12-07 2009-03-18 Piramed Ltd Compuestos de inhibidores de fosfoinositido-3 quinasa y metodos de uso
ES2571028T3 (es) * 2006-12-07 2016-05-23 Genentech Inc Compuestos inhibidores de fosfoinositida 3-cinasa y métodos de uso
KR101472607B1 (ko) * 2007-02-20 2014-12-15 노파르티스 아게 지질 키나제 및 ｍＴＯＲ의 이중 억제제로서의 이미다조퀴놀린
CN101679456B (zh) * 2007-06-12 2012-09-05 霍夫曼-拉罗奇有限公司 噻唑并嘧啶类和它们作为磷脂酰肌醇3-激酶的抑制剂的应用
EP2205242B1 (en) * 2007-09-12 2015-04-15 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
CA2704711C (en) 2007-09-24 2016-07-05 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
JP5348725B2 (ja) 2007-10-25 2013-11-20 ジェネンテック， インコーポレイテッド チエノピリミジン化合物の製造方法
GB0721095D0 (en) * 2007-10-26 2007-12-05 Piramed Ltd Pharmaceutical compounds
EP2215090B1 (en) * 2007-10-26 2015-03-04 F. Hoffmann-La Roche AG Purine derivatives useful as pi3 kinase inhibitors
CN102088995B (zh) 2008-05-14 2016-01-20 维多利亚农业服务控股公司 血管生成素和血管生成素激动剂用于治疗疾病和障碍的用途
EP2279188B1 (en) * 2008-05-30 2015-01-28 Genentech, Inc. Purine pi3k inhibitor compounds and methods of use
KR20110046514A (ko) * 2008-07-31 2011-05-04 제넨테크, 인크. 피리미딘 화합물, 조성물 및 사용 방법
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
AU2009304596A1 (en) 2008-10-17 2010-04-22 Akaal Pharma Pty Ltd S1P receptors modulators
CA2740484C (en) * 2008-10-17 2021-09-21 Akaal Pharma Pty Ltd S1p receptors modulators and their use thereof
CA2743015A1 (en) 2008-11-11 2010-05-20 Xcovery Holding Company Llc Pi3k/mtor kinase inhibitors
EP2356117B1 (en) * 2008-11-20 2012-09-26 Genentech, Inc. Pyrazolopyridine pi3k inhibitor compounds and methods of use
CA2749012C (en) * 2009-01-08 2017-01-31 Merck Patent Gmbh Polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof
CA2749228C (en) * 2009-01-08 2016-05-17 Curis, Inc. Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
CN102369011A (zh) 2009-03-12 2012-03-07 健泰科生物技术公司 用于治疗造血恶性肿瘤的磷酸肌醇3-激酶抑制剂化合物与化学治疗剂的组合
ES2543216T3 (es) * 2009-03-13 2015-08-17 Katholieke Universiteit Leuven, K.U. Leuven R&D Moduladores de tiazolopirimidina como agentes inmunosupresores
SG172951A1 (en) 2009-03-24 2011-08-29 Sumitomo Chemical Co Method for manufacturing a boronic acid ester compound
BRPI1013600A2 (pt) 2009-03-27 2019-09-24 Pathway Therapeutics Inc "sulfonamidas de pirimidinila e benzintoazol de 1,3,5-triazinila e seu uso em terapia de câncer"
CA2772371A1 (en) * 2009-05-27 2010-12-02 F. Hoffmann-La Roche Ag Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
BRPI1009022A2 (pt) 2009-05-27 2016-03-08 Hoffmann La Roche "composto, composição farmacêutica, processo para produzir uma composição farmacêutica, uso de um composto, método para tratamento de uma doença ou transtorno e kit"
SG176959A1 (en) * 2009-06-24 2012-01-30 Genentech Inc Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use
CA2987503C (en) 2009-07-07 2019-02-26 Mei Pharma, Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
EP2461813A4 (en) * 2009-08-05 2014-02-19 Univ Wake Forest Health Sciences COMPOSITIONS AND METHODS FOR APOPTOSIS-TREATMENT IN PROSTATE MAINTENANCE CELLS
US9085560B2 (en) 2009-08-17 2015-07-21 Intellikine, Inc. Heterocyclic compounds and uses thereof
US20130012709A1 (en) * 2009-09-10 2013-01-10 Centre National De La Recherche Scientifique NOVEL INHIBITORS OF STEAROYL-CoA-DESATURASE-1 AND THEIR USES
PE20140918A1 (es) 2009-09-28 2014-08-06 Hoffmann La Roche Compuestos de benzoxepina inhibidores de la pi3k
WO2011049625A1 (en) 2009-10-20 2011-04-28 Mansour Samadpour Method for aflatoxin screening of products
PT2496567T (pt) 2009-11-05 2017-11-15 Rhizen Pharmaceuticals S A Novos moduladores de quinase benzopiran
US8288381B2 (en) * 2009-11-12 2012-10-16 Genentech, Inc. N-9 substituted purine compounds, compositions and methods of use
ES2567168T3 (es) * 2009-11-12 2016-04-20 F. Hoffmann-La Roche Ag Compuestos purina y pirazolopirimidina N7-sustituidos, composiciones y métodos de utilización
MX2012009059A (es) 2010-02-22 2012-09-07 Hoffmann La Roche Compuestos inhibidores de fosfoinositida 3-cinasa delta (pi3k) pirido [3,2-d]pirimidina y metodos de uso.
UY33304A (es) * 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
RU2013104038A (ru) 2010-07-14 2014-08-20 Ф. Хоффманн-Ля Рош Аг СЕЛЕКТИВНЫЕ В ОТНОШЕНИИ PI3K p110 ДЕЛЬТА ПУРИНОВЫЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
KR20140099556A (ko) * 2010-12-16 2014-08-12 에프. 호프만-라 로슈 아게 트라이사이클릭 pi3k 억제제 화합물 및 이의 사용 방법
US20140206678A1 (en) * 2011-01-27 2014-07-24 Kadmon Corporation, Llc Inhibitors of mtor kinase as anti -viral agent
CA2825028A1 (en) 2011-02-09 2012-08-16 F. Hoffman-La Roche Ag Heterocyclic compounds as pi3 kinase inhibitors
RU2013143747A (ru) 2011-03-21 2015-04-27 Ф. Хоффманн-Ля Рош Аг Соединения бензоксазепина, селективные в отношении pi3k p110 дельта и способы их применения
BR112013024907A2 (pt) 2011-03-28 2016-12-20 Mei Pharma Inc composto, composição farmacêutica, método para o tratamento, prevenção ou atenuação de um ou mais sintomas de um distúrbio, doença ou condição mediada por pi3k em um sujeito, método para modular a atividade enzimática de pi3k
KR101992311B1 (ko) 2011-05-04 2019-09-27 리젠 파마슈티컬스 소시에떼 아노님 단백질 키나아제의 조절제로서 신규한 화합물
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
KR101255939B1 (ko) * 2011-05-31 2013-04-23 동화약품주식회사 4-(1ｈ-인다졸-6-일아미노)-ｎ-아이소프로필-2-(메틸티오)피리미딘-5-카르복스아미드 화합물 또는 이의 약학적으로 허용가능한 염을 포함하는 당뇨병 예방 또는 치료용 조성물
US9682141B2 (en) 2011-11-11 2017-06-20 Intellikine Llc Combination of kinase inhibitors and uses thereof
GB201204125D0 (en) 2012-03-08 2012-04-25 Karus Therapeutics Ltd Compounds
FR2988722B1 (fr) 2012-04-03 2014-05-09 Sanofi Sa Nouveaux derives de thienopyrimidines, leurs procedes de preparation et leurs utilisations therapeutiques
CN103467482B (zh) 2012-04-10 2017-05-10 上海璎黎药业有限公司 稠合嘧啶类化合物，其制备方法，中间体，组合物和应用
WO2016144958A1 (en) 2015-03-08 2016-09-15 Case Western Reserve University Inhibitors of short-chain dehydrogenase activity for treating fibrosis
EP3295940A1 (en) 2012-04-16 2018-03-21 Case Western Reserve University Compositions and methods of modulating 15-pgdh activity
US9801863B2 (en) 2012-04-16 2017-10-31 Case Western Reserve University Inhibitors of short-chain dehydrogenase activity for modulating hematopoietic stem cells and hematopoiesis
PT2848254T (pt) * 2012-05-07 2016-10-05 Kissei Pharmaceutical Derivado de pirazol e utilização do mesmo para propósitos médicos
AU2013204740C1 (en) 2012-05-10 2015-10-01 Agriculture Victoria Services Pty Ltd Methods of treating cancer using angiogenin or an angiogenin agonist
BR112014028881A2 (pt) 2012-05-23 2017-06-27 Hoffmann La Roche populações de células, banco de células, métodos de obtenção de uma população de células, métodos de identificação de um fator, métodos de seleção, métodos de fornecimento de terapia, populações de hepatócitos e método de obtenção de células
EP2858666B1 (en) 2012-06-08 2019-09-04 F.Hoffmann-La Roche Ag Mutant selectivity and combinations of a phosphoinositide 3 kinase inhibitor compound and chemotherapeutic agents for the treatment of cancer
KR101988079B1 (ko) 2012-07-04 2019-06-11 리젠 파마슈티컬스 소시에떼 아노님 선택적 pi3k 델타 억제제
JP6022691B2 (ja) * 2012-08-30 2016-11-09 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ジオキシノ−及びオキサジン−［２，３−ｄ］ピリミジンｐｉ３ｋ阻害剤化合物及び使用方法
WO2014068070A1 (en) 2012-10-31 2014-05-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for preventing antiphospholipid syndrome (aps)
MX364295B (es) 2012-11-07 2019-04-22 Karus Therapeutics Ltd Inhibidores de histona desacetilasa novedosos y su uso en terapia.
AU2014250836C1 (en) * 2013-04-12 2019-01-17 Asana Biosciences, Llc Quinazolines and azaquinazolines as dual inhibitors of RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways
PL2994465T3 (pl) 2013-05-10 2019-01-31 Karus Therapeutics Limited Nowe inhibitory deacetylazy histonowej
DE102013008118A1 (de) * 2013-05-11 2014-11-13 Merck Patent Gmbh Arylchinazoline
WO2014203129A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Combinations of benzopyran compounds, compositions and uses thereof
CN104513254B (zh) 2013-09-30 2019-07-26 上海璎黎药业有限公司 稠合嘧啶类化合物、中间体、其制备方法、组合物和应用
CA2927730A1 (en) 2013-10-15 2015-05-07 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase activity
AU2014336775B2 (en) 2013-10-16 2018-04-05 Shanghai Yingli Pharmaceutical Co., Ltd Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
KR20160118345A (ko) 2014-02-06 2016-10-11 애브비 인코포레이티드 6-헤테로아릴옥시- 및 6-아릴옥시-퀴놀린-2-카복사미드 및 이의 용도
GB201402431D0 (en) 2014-02-12 2014-03-26 Karus Therapeutics Ltd Compounds
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
WO2016154075A1 (en) * 2015-03-20 2016-09-29 Vertex Pharmaceuticals Incorporated Bicyclic heteroaryl compounds useful as inhibitors of the par-2 signaling pathway
AR104068A1 (es) 2015-03-26 2017-06-21 Hoffmann La Roche Combinaciones de un compuesto inhibidor de fosfoinosítido 3-cinasa y un compuesto inhibidor de cdk4/6 para el tratamiento del cáncer
HUE045192T2 (hu) * 2015-03-30 2019-12-30 Daiichi Sankyo Co Ltd 6-morfolinil-2-pirazolil-9H-purin származékok és felhasználásuk PI3K inhibitorokként
US20180118756A1 (en) * 2015-04-14 2018-05-03 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase activity
AU2016287189A1 (en) 2015-06-29 2017-10-12 F. Hoffmann-La Roche Ag Methods of treatment with taselisib
GB201514754D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
GB201514758D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Formulation
GB201514751D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds
GB201514760D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Compounds and method of use
US10221191B2 (en) 2015-12-22 2019-03-05 SHY Therapeutics LLC Compounds for the treatment of cancer and inflammatory disease
EP3454852A4 (en) 2016-05-11 2020-02-26 Emory University PHOSPHOTIDYLINOSITOL 3-KINASES INHIBITORS
PT3464266T (pt) 2016-06-01 2021-11-23 Bayer Pharma AG Indazóis substituídos para tratamento e prevenção de doenças alérgicas e/ou inflamatórias em animais
WO2018057588A1 (en) * 2016-09-21 2018-03-29 Vertex Pharmaceuticals Incorporated Furo[3,2-b]pyridine compounds useful as inhibitors of the par-2 signaling pathway
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
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
JP7595413B2 (ja) 2016-11-30 2024-12-06 ケース ウエスタン リザーブ ユニバーシティ １５－ｐｇｄｈ阻害剤とコルチコステロイドおよび／またはｔｎｆ阻害剤との組み合わせならびにその使用
WO2018145080A1 (en) 2017-02-06 2018-08-09 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase activity
KR20240097982A (ko) 2017-05-23 2024-06-27 메이 파마, 아이엔씨. 병용 요법
MA49921A (fr) 2017-08-14 2021-05-12 Mei Pharma Inc Polythérapie
CA3102279A1 (en) 2018-06-01 2019-12-05 Cornell University Combination therapy for pi3k-associated disease or disorder
BR112021004371A2 (pt) 2018-09-11 2021-05-25 Curis Inc. terapia em combinação com um inibidor de fosfoinositídeo 3-quinase com uma porção de ligação a zinco
JP7598642B2 (ja) * 2018-10-12 2024-12-12 ボード オブ リージェンツ オブ ザ ユニヴァーシティー オブ ネブラスカ ホスホジエステラーゼ阻害剤
PE20212246A1 (es) 2018-11-21 2021-11-24 Univ Case Western Reserve Composiciones y metodos para modular la actividad de deshidrogenasas de cadena corta
WO2020132071A1 (en) 2018-12-19 2020-06-25 Shy Therapeutics. Llc Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and f1brotic disease
AU2021207804A1 (en) 2020-01-13 2022-09-01 Verge Analytics, Inc. Substituted pyrazolo-pyrimidines and uses thereof
WO2021247841A1 (en) * 2020-06-03 2021-12-09 Yumanity Therapeutics, Inc. Purines and methods of their use
MX2023005436A (es) * 2020-11-10 2023-07-25 Foghorn Therapeutics Inc Compuestos y usos de estos.
US20240226126A1 (en) * 2021-06-16 2024-07-11 The Board Of Trustees Of The Leland Stanford Junior University Compositions for treatment of psoriasis
KR20230047047A (ko) * 2021-09-30 2023-04-06 한미약품 주식회사 PIKfyve 키나아제 억제제
IL316531A (en) 2022-05-11 2024-12-01 Foghorn Therapeutics Inc Compounds and their uses

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1470356A1 (de) * 1964-01-15 1970-04-30 Thomae Gmbh Dr K Neue Thieno[3,2-d]pyrimidine und Verfahren zu ihrer Herstellung
BE754606A (fr) * 1969-08-08 1971-02-08 Thomae Gmbh Dr K Nouvelles 2-aminoalcoylamino-thieno(3,2-d)pyrimidines et leurs procedesde fabrication
BE759493A (fr) * 1969-11-26 1971-05-25 Thomae Gmbh Dr K Nouvelles 2-(5-nitro-2-furyl)-thieno(3,2-d) pyrimidines et procedes pour les fabriquer
US3763156A (en) * 1970-01-28 1973-10-02 Boehringer Sohn Ingelheim 2-heterocyclic amino-4-morpholinothieno(3,2-d)pyrimidines
RO62428A (fr) 1971-05-04 1978-01-15 Thomae Gmbh Dr K Procede pour la preparation des thyeno-(3,2-d)-pyrimidines
CH592668A5 (enExample) * 1973-10-02 1977-10-31 Delalande Sa
GB1570494A (en) 1975-11-28 1980-07-02 Ici Ltd Thienopyrimidine derivatives and their use as pesticides
US4196207A (en) 1977-05-23 1980-04-01 Ici Australia Limited Process for controlling eradicating or preventing infestations of animals by Ixodid ticks
US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
KR100774855B1 (ko) * 2000-04-27 2007-11-08 아스텔라스세이야쿠 가부시키가이샤 축합 헤테로아릴 유도체
ATE290882T1 (de) * 2001-01-16 2005-04-15 Glaxo Group Ltd Pharmazeutische mischung gegen krebs, die ein 4- chinazolinamin in kombination mit paclitaxel, carboplatin or vinorelbine enthält
WO2003035618A2 (en) * 2001-10-24 2003-05-01 Iconix Pharmaceuticals, Inc. Modulators of phosphoinositide 3-kinase
WO2003034997A2 (en) * 2001-10-24 2003-05-01 Iconix Pharmaceuticals, Inc. Modulators of phosphoinositide 3-kinase
AU2003255845A1 (en) * 2002-08-22 2004-03-11 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
ES2217956B1 (es) * 2003-01-23 2006-04-01 Almirall Prodesfarma, S.A. Nuevos derivados de 4-aminotieno(2,3-d)pirimidin-6-carbonitrilo.
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
KR101402474B1 (ko) 2006-04-26 2014-06-19 제넨테크, 인크. 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물
US20110230476A1 (en) * 2009-09-09 2011-09-22 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof

Cited By (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102498115A (zh) * 2009-08-20 2012-06-13 卡鲁斯治疗有限公司 作为磷酸肌醇3-激酶抑制剂的三环杂环化合物
CN102498115B (zh) * 2009-08-20 2016-12-07 卡鲁斯治疗有限公司 作为磷酸肌醇3-激酶抑制剂的三环杂环化合物
CN102625708A (zh) * 2009-09-09 2012-08-01 阿维拉制药公司 Pi3激酶抑制剂及其用途
CN102781923A (zh) * 2010-01-26 2012-11-14 贝林格尔.英格海姆国际有限公司 5-炔基-嘧啶化合物
CN102781923B (zh) * 2010-01-26 2016-03-02 贝林格尔.英格海姆国际有限公司 5-炔基-嘧啶化合物
CN105461736A (zh) * 2011-04-01 2016-04-06 柯瑞斯公司 具有锌结合位的磷脂酰肌醇3-激酶抑制剂
CN105461736B (zh) * 2011-04-01 2018-06-12 柯瑞斯公司 具有锌结合位的磷脂酰肌醇3-激酶抑制剂
CN103957902A (zh) * 2011-10-13 2014-07-30 基因泰克公司 药理学诱导的胃酸过少的治疗
CN102643272A (zh) * 2011-12-30 2012-08-22 沈阳药科大学 新的噻吩并[3,2-d]嘧啶类化合物
CN102643272B (zh) * 2011-12-30 2015-03-11 沈阳药科大学 新的噻吩并[3,2-d]嘧啶类化合物
CN107098846A (zh) * 2016-02-26 2017-08-29 中国医学科学院药物研究所 N-酰基磺酰胺类FBPase抑制剂、其制备方法、药物组合物及用途
CN107098846B (zh) * 2016-02-26 2020-10-09 中国医学科学院药物研究所 N-酰基磺酰胺类FBPase抑制剂、其制备方法、药物组合物及用途
CN111032662A (zh) * 2017-06-21 2020-04-17 尚医治疗有限责任公司 与ras超家族相互作用的用于治疗癌症、炎性疾病、ras蛋白病和纤维化疾病的化合物
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