MX2009005950A - Compuestos inhibidores de fosfoinositido 3-quinasas y metodos de uso. - Google Patents

Compuestos inhibidores de fosfoinositido 3-quinasas y metodos de uso.

Info

Publication number
MX2009005950A
MX2009005950A MX2009005950A MX2009005950A MX2009005950A MX 2009005950 A MX2009005950 A MX 2009005950A MX 2009005950 A MX2009005950 A MX 2009005950A MX 2009005950 A MX2009005950 A MX 2009005950A MX 2009005950 A MX2009005950 A MX 2009005950A
Authority
MX
Mexico
Prior art keywords
methods
compounds
phosphoinositide
kinase inhibitor
inhibitor compounds
Prior art date
Application number
MX2009005950A
Other languages
English (en)
Inventor
Bing-Yan Zhu
Daniel P Sutherlin
Georgette Castanedo
Richard Goldsmith
Janet Gunzner
Tim Heffron
Alan Olivero
Steven Staben
Irina Chuckowree
Adrian FOLKES
Tracy Bayliss
Sally Oxenford
Nan Chi Wan
Simon Mathieu
Original Assignee
Genentech Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39188533&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MX2009005950(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Genentech Inc filed Critical Genentech Inc
Publication of MX2009005950A publication Critical patent/MX2009005950A/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Abstract

Compuestos de las Fórmulas Ia-d donde X es S u O, mor es un grupo morfolina, y R3 es un grupo heteroarilo monocíclico, e incluyendo estereoisómeros, isómeros geométricos, tautámeros, solvatos, metabolitos y sales farmacéuticamente aceptables de los mismos, son útiles para modular la actividad de lípido quinasas incluyendo PI3K, y para tratar trastornos tal como cáncer mediado por lípido quinasas. Se divulgan métodos para usar los compuestos de Fórmula Ia-d para diagnóstico, prevención o tratamiento in vitro, in situ e in vivo de estos trastornos en células de mamíferos, o condiciones patológicas asociadas.
MX2009005950A 2006-12-07 2007-12-05 Compuestos inhibidores de fosfoinositido 3-quinasas y metodos de uso. MX2009005950A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US87344806P 2006-12-07 2006-12-07
US97725707P 2007-10-03 2007-10-03
PCT/US2007/086543 WO2008070740A1 (en) 2006-12-07 2007-12-05 Phosphoinositide 3-kinase inhibitor compounds and methods of use

Publications (1)

Publication Number Publication Date
MX2009005950A true MX2009005950A (es) 2009-10-12

Family

ID=39188533

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2009005950A MX2009005950A (es) 2006-12-07 2007-12-05 Compuestos inhibidores de fosfoinositido 3-quinasas y metodos de uso.

Country Status (22)

Country Link
US (3) US7888352B2 (es)
EP (2) EP2114949A1 (es)
JP (1) JP5284977B2 (es)
KR (1) KR101460816B1 (es)
AR (1) AR064155A1 (es)
AU (1) AU2007329352B2 (es)
BR (1) BRPI0717923A2 (es)
CA (1) CA2671782C (es)
CL (1) CL2007003520A1 (es)
CO (1) CO6190615A2 (es)
CR (1) CR10915A (es)
EC (1) ECSP099496A (es)
ES (1) ES2544082T3 (es)
MA (1) MA31146B1 (es)
MX (1) MX2009005950A (es)
MY (1) MY180595A (es)
NO (1) NO20092566L (es)
NZ (1) NZ578162A (es)
PE (1) PE20081679A1 (es)
RU (1) RU2468027C2 (es)
TW (1) TWI499420B (es)
WO (1) WO2008070740A1 (es)

Families Citing this family (119)

* 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
AU2007243457B2 (en) * 2006-04-26 2012-02-23 F. Hoffmann-La Roche Ag Pharmaceutical compounds
CL2007003520A1 (es) 2006-12-07 2008-08-22 Piramed Ltd Genentech Inc Compuestos derivados de heterociclos sustituidos con morfolina, inhibidores de la actividad pi3 quinasa; composicion farmaceutica que comprende a dichos compuestos; kit farmaceutico; y su uso para el tratamiento profilactico o terapeutico del cancer.
JP5500990B2 (ja) 2006-12-07 2014-05-21 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ホスホイノシチド３−キナーゼ阻害剤化合物及び使用方法
JP5539190B2 (ja) * 2007-06-12 2014-07-02 エフ．ホフマン−ラ ロシュ アーゲー チアゾロピリミジン類及びホスファチジルイノシトール−３キナーゼのインヒビターとしてのそれらの使用
KR101584823B1 (ko) * 2007-09-12 2016-01-22 제넨테크, 인크. 포스포이노시타이드 3-키나제 저해제 화합물과 화학치료제의 배합물 및 이의 사용방법
CN101932587A (zh) * 2007-09-24 2010-12-29 吉宁特有限公司 噻唑并嘧啶pi3k抑制剂化合物及使用方法
US8354528B2 (en) 2007-10-25 2013-01-15 Genentech, Inc. Process for making thienopyrimidine compounds
GB0721095D0 (en) * 2007-10-26 2007-12-05 Piramed Ltd Pharmaceutical compounds
CN101945870B (zh) 2007-12-19 2012-10-03 健泰科生物技术公司 5-苯氨基咪唑并吡啶和使用方法
JP5520831B2 (ja) 2007-12-19 2014-06-11 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
CN101945875B (zh) 2007-12-21 2013-04-24 健泰科生物技术公司 氮杂吲嗪及其使用方法
KR20210131473A (ko) 2008-03-18 2021-11-02 제넨테크, 인크. 항-ｈｅｒ２ 항체-약물 접합체와 화학요법제의 병용물, 및 사용 방법
TW201018681A (en) * 2008-07-31 2010-05-16 Genentech Inc Pyrimidine compounds, compositions and methods of use
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
CA2739901A1 (en) 2008-10-17 2010-04-22 Akaal Pharma Pty Ltd S1p receptors modulators
CN102186845B (zh) * 2008-10-17 2016-09-07 阿卡制药有限公司 S1p受体调节剂以及它们的用途
TWI558710B (zh) 2009-01-08 2016-11-21 古利斯股份有限公司 具有鋅連接部位的磷酸肌醇３－激酶抑制劑
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
JP5709766B2 (ja) * 2009-03-12 2015-04-30 ジェネンテック， インコーポレイテッド 造血器腫瘍の治療のためのホスホイノシチド３キナーゼ阻害剤化合物と化学療法剤の併用
CN102361878A (zh) 2009-03-24 2012-02-22 住友化学株式会社 用于制备硼酸酯化合物的方法
KR20130026364A (ko) * 2009-05-27 2013-03-13 제넨테크, 인크. Ｐ110 델타에 대해 선택적인 비시클릭 피리미딘 ｐｉ3ｋ 억제제 화합물 및 사용 방법
SG182247A1 (en) * 2009-05-27 2012-08-30 Hoffmann La Roche Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
US20100331305A1 (en) * 2009-06-24 2010-12-30 Genentech, Inc. Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use
WO2011029802A1 (en) 2009-09-08 2011-03-17 F. Hoffmann-La Roche Ag 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
NZ599090A (en) 2009-09-28 2014-02-28 Hoffmann La Roche Benzoxepin pi3k inhibitor compounds and methods of use
WO2011054620A1 (en) * 2009-10-12 2011-05-12 F. Hoffmann-La Roche Ag Combinations of a pi3k inhibitor and a mek inhibitor
WO2011049625A1 (en) 2009-10-20 2011-04-28 Mansour Samadpour Method for aflatoxin screening of products
EA027123B1 (ru) 2009-11-05 2017-06-30 Ризен Фармасьютикалз С.А. Ингибиторы киназы pi3k
US8828990B2 (en) * 2009-11-12 2014-09-09 Genentech, Inc. N-7 substituted purine and pyrazolopyrimine compounds, compositions and methods of use
US8288381B2 (en) * 2009-11-12 2012-10-16 Genentech, Inc. N-9 substituted purine compounds, compositions and methods of use
CA2786294A1 (en) 2010-02-22 2011-08-25 F. Hoffmann-La Roche Ag Pyrido[3,2-d]pyrimidine pi3k delta inhibitor compounds and methods of use
WO2011120911A1 (en) 2010-03-30 2011-10-06 Novartis Ag Pkc inhibitors for the treatment of b-cell lymphoma having chronic active b-cell-receptor signalling
ES2536780T3 (es) 2010-07-14 2015-05-28 F. Hoffmann-La Roche Ag Compuestos de purina selectivos para I3 p110 delta, y métodos de uso
ES2530545T3 (es) 2010-12-16 2015-03-03 Hoffmann La Roche Compuestos tricíclicos inhibidores de la PI3K y métodos de uso
JP5766820B2 (ja) 2011-02-09 2015-08-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｐｉ３キナーゼ阻害剤としての複素環化合物
CA2825966A1 (en) 2011-03-21 2012-09-27 F. Hoffmann-La Roche Ag Benzoxazepin compounds selective for pi3k p110 delta and methods of use
PT3111938T (pt) 2011-04-01 2019-07-10 Curis Inc Inibidores de fosfoinoritide 3-quinase com uma fração de ligação ao zinco
CN107337659A (zh) 2011-05-04 2017-11-10 理森制药股份公司 作为蛋白激酶调节剂的新颖化合物
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
KR20140040728A (ko) 2011-06-03 2014-04-03 에프. 호프만-라 로슈 아게 Pi3k 억제제 화합물을 사용한 중피종 치료 방법
EP2763985B1 (en) * 2011-10-07 2016-06-22 Cellzome Limited {(4-(4-morpholino-dihydrothieno[3,4-d]pyrimidin-2-yl)aryl}urea or carbamate derivatives as mtor inhibitors
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
CN103450204B (zh) * 2012-05-31 2016-08-17 中国科学院上海药物研究所 吡咯[2，1-f][1，2，4]并三嗪类化合物，其制备方法及用途
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
MY169987A (en) 2012-07-04 2019-06-19 Rhizen Pharmaceuticals Sa Selective pi3k delta inhibitors
US9145411B2 (en) 2012-08-02 2015-09-29 Asana Biosciences, Llc Substituted amino-pyrimidine derivatives
RU2680096C2 (ru) 2012-08-21 2019-02-15 ОПКО ФАРМАСЬЮТИКАЛС, Эл Эл Си Липосомальные препараты
MX361157B (es) * 2012-08-30 2018-11-28 Hoffmann La Roche Compuestos inhibidores de pi3k de dioxino- y oxazin-[2,3-d]pirimid ina y métodos de uso.
JP6123097B2 (ja) 2012-10-10 2017-05-10 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト チエノピリミジン化合物を製造するための方法
US20150258127A1 (en) 2012-10-31 2015-09-17 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for preventing antiphospholipid syndrome (aps)
AR096178A1 (es) 2013-05-06 2015-12-09 Hoffmann La Roche Procedimiento para la preparacion de intermediarios de acido boronico.
WO2014203129A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Combinations of benzopyran compounds, compositions and uses thereof
CN105985354B (zh) * 2015-02-09 2020-10-02 南京盖特医药技术有限公司 嘧啶衍生物、细胞毒性剂、药物组合物及其应用
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
CN107635560A (zh) 2015-06-29 2018-01-26 豪夫迈·罗氏有限公司 用他塞利昔布进行治疗的方法
JP6522807B2 (ja) * 2015-07-02 2019-05-29 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ベンゾオキサゼピンオキサゾリジノン化合物及び使用方法
EP3778607B1 (en) 2015-07-02 2023-08-30 F. Hoffmann-La Roche AG Benzoxazepin oxazolidinone compounds and methods of use
WO2017013270A1 (en) 2015-07-23 2017-01-26 Universite De Strasbourg Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy
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
US20180133223A1 (en) * 2016-11-02 2018-05-17 Curis, Inc. Combination therapy with a phosphoinositide 3-kinase inhibitor with a zinc binding moiety
MA47107B1 (fr) 2016-12-22 2021-11-30 Amgen Inc Dérivés de benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine et pyrido[2,3-d]pyrimidine en tant qu'inhibiteurs de kras g12c pour le traitement de cancer du poumon, du pancréas ou de l'intestin
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3661924A1 (en) 2017-07-31 2020-06-10 The Trustees of Columbia University in the City of New York Compounds, compositionals, and methods for treating t-cell acute lymphoblastic leukemia
IL272512B (en) 2017-09-08 2022-07-01 Amgen Inc kras g12c inhibitors and methods of using them
WO2019145177A1 (en) 2018-01-23 2019-08-01 Basf Se Bromination of pyridine derivatives
US10596165B2 (en) 2018-02-12 2020-03-24 resTORbio, Inc. Combination therapies
ES2929292T3 (es) 2018-04-10 2022-11-28 Neuropore Therapies Inc Derivados de morfolina como inhibidores de Vps34
MX2020011582A (es) 2018-05-04 2020-11-24 Amgen Inc Inhibidores de kras g12c y metodos para su uso.
CA3098574A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
US10988485B2 (en) 2018-05-10 2021-04-27 Amgen Inc. KRAS G12C inhibitors and methods of using the same
ES2938987T3 (es) 2018-06-01 2023-04-18 Amgen Inc Inhibidores de KRAS G12c y métodos de uso de los mismos
US20190375749A1 (en) 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
US11285156B2 (en) 2018-06-12 2022-03-29 Amgen Inc. Substituted piperazines as KRAS G12C inhibitors
WO2019241789A1 (en) 2018-06-15 2019-12-19 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
EP3849554A4 (en) 2018-09-11 2022-06-01 Curis, Inc. POLYTHERAPY WITH A PHOSPHOINONOSITIDE 3-KINASE INHIBITOR HAVING A ZINC-BINDING METAL
JP2020090482A (ja) 2018-11-16 2020-06-11 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
WO2020106640A1 (en) 2018-11-19 2020-05-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
WO2020103897A1 (zh) * 2018-11-22 2020-05-28 上海迪诺医药科技有限公司 杂环稠合嘧啶衍生物、其药物组合物及应用
WO2020132651A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
EP3898592A1 (en) 2018-12-20 2021-10-27 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
MX2021007158A (es) 2018-12-20 2021-08-16 Amgen Inc Heteroarilamidas utiles como inhibidores de kif18a.
CA3123871A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
TW202038957A (zh) 2018-12-21 2020-11-01 日商第一三共股份有限公司 抗體-藥物結合物與激酶抑制劑之組合
KR20210146288A (ko) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. 이환식 헤테로사이클릴 화합물 및 이의 용도
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
BR112021023277A2 (pt) 2019-05-21 2022-01-04 Amgen Inc Formas em estado sólido
AU2020325115A1 (en) 2019-08-02 2022-03-17 Amgen Inc. Pyridine derivatives as KIF18A inhibitors
CA3146693A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
JP2022542394A (ja) 2019-08-02 2022-10-03 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤として有用なヘテロアリールアミド
AU2020324406A1 (en) 2019-08-02 2022-03-17 Amgen Inc. KIF18A inhibitors
WO2021076655A1 (en) 2019-10-15 2021-04-22 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
MX2022004656A (es) 2019-10-24 2022-05-25 Amgen Inc Derivados de piridopirimidina utiles como inhibidores de kras g12c y kras g12d en el tratamiento del cancer.
TW202132315A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras 抑制劑
AU2020379734A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
CN114867735A (zh) 2019-11-04 2022-08-05 锐新医药公司 Ras抑制剂
CN114901662A (zh) 2019-11-08 2022-08-12 锐新医药公司 双环杂芳基化合物及其用途
US20230192681A1 (en) 2019-11-14 2023-06-22 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
AR120456A1 (es) 2019-11-14 2022-02-16 Amgen Inc Síntesis mejorada del compuesto inhibidor de g12c de kras
CN114980976A (zh) 2019-11-27 2022-08-30 锐新医药公司 共价ras抑制剂及其用途
CA3163680A1 (en) 2019-12-05 2021-06-10 David John O'neill Rapamycin analogs and uses thereof
US20230028414A1 (en) 2019-12-16 2023-01-26 Amgen Inc. Dosing regimen of kras g12c inhibitor
CA3163703A1 (en) 2020-01-07 2021-07-15 Steve Kelsey Shp2 inhibitor dosing and methods of treating cancer
CN115916194A (zh) 2020-06-18 2023-04-04 锐新医药公司 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法
CN116209438A (zh) 2020-09-03 2023-06-02 锐新医药公司 使用sos1抑制剂治疗具有shp2突变的恶性疾病
CN116457358A (zh) 2020-09-15 2023-07-18 锐新医药公司 作为ras抑制剂以治疗癌症的吲哚衍生物
TW202241885A (zh) 2020-12-22 2022-11-01 大陸商上海齊魯銳格醫藥研發有限公司 Ｓｏｓ１抑制劑及其用途
TW202309052A (zh) 2021-05-05 2023-03-01 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
IL308195A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors for cancer treatment
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors

Family Cites Families (55)

* 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
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
DE1959403A1 (de) 1969-11-26 1971-06-03 Thomae Gmbh Dr K Neue 2-(5-Nitro-2-furyl)-thieno[3,2-d]pyrimidine und Verfahren zu ihrer Herstellung
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
DE2050814A1 (de) 1970-10-16 1972-04-20 Dr. Karl Thomae Gmbh, 7950 Biberach Neue Verfahren zur Herstellung von 2-(5-Nitro-2-furyl)-thieno eckige Klammer auf 3,2-d eckige Klammer zu pyrimidinen
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 (es) 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
ZA782648B (en) 1977-05-23 1979-06-27 Ici Australia Ltd The prevention,control or eradication of infestations of ixodid ticks
US5583024A (en) 1985-12-02 1996-12-10 The Regents Of The University Of California Recombinant expression of Coleoptera luciferase
US5075305A (en) 1991-03-18 1991-12-24 Warner-Lambert Company Compound, composition and use
WO1993013664A2 (en) 1992-01-11 1993-07-22 Schering Agrochemicals Limited Biheterocyclic fungicidal compounds
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
US5846824A (en) 1994-02-07 1998-12-08 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
US5654307A (en) * 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
JPH08175990A (ja) 1994-12-19 1996-07-09 Mitsubishi Chem Corp Ｐｉ３キナーゼ阻害剤とその製造法
JPH08176070A (ja) 1994-12-19 1996-07-09 Mitsubishi Chem Corp ジデプシド誘導体及びｐｉ３キナーゼ阻害剤
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
GB9521987D0 (en) 1995-10-26 1996-01-03 Ludwig Inst Cancer Res Phosphoinositide 3-kinase modulators
AUPO903897A0 (en) 1997-09-08 1997-10-02 Commonwealth Scientific And Industrial Research Organisation Organic boronic acid derivatives
US6602677B1 (en) 1997-09-19 2003-08-05 Promega Corporation Thermostable luciferases and methods of production
SK6652000A3 (en) 1997-11-11 2002-05-09 Pfizer Prod Inc Thienopyrimidine and thienopyridine derivatives useful as anticancer agents
US6187777B1 (en) 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
JP2001247477A (ja) 2000-03-03 2001-09-11 Teikoku Hormone Mfg Co Ltd 抗腫瘍剤
US6608053B2 (en) 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
KR100774855B1 (ko) 2000-04-27 2007-11-08 아스텔라스세이야쿠 가부시키가이샤 축합 헤테로아릴 유도체
EP1353693B1 (en) 2001-01-16 2005-03-16 Glaxo Group Limited Pharmaceutical combination containing a 4-quinazolineamine and paclitaxel, carboplatin or vinorelbine for the treatment of cancer
CA2454976C (en) 2001-07-26 2011-05-10 Santen Pharmaceutical Co., Ltd. Therapeutic agent for glaucoma comprising compound having pi3 kinase inhibitory action as active ingredient
US6703414B2 (en) 2001-09-14 2004-03-09 Arizona Board Of Regents On Behalf Of The University Of Arizona Device and method for treating restenosis
DE10148883A1 (de) * 2001-10-04 2003-04-10 Merck Patent Gmbh Pyrimidinderivate
WO2003034997A2 (en) 2001-10-24 2003-05-01 Iconix Pharmaceuticals, Inc. Modulators of phosphoinositide 3-kinase
AU2002349912A1 (en) 2001-10-24 2003-05-06 Iconix Pharmaceuticals, Inc. Modulators of phosphoinositide 3-kinase
CA2464924A1 (en) 2001-10-30 2003-05-08 Pharmacia Corporation Heteroaromatic carboxamide derivatives for the treatment of inflammation
JP2006500327A (ja) 2002-07-10 2006-01-05 アプライド リサーチ システムズ エーアールエス ホールディング ナームロゼ フェンノートシャップ ***の運動性を増大させるための化合物の使用
US20040092561A1 (en) 2002-11-07 2004-05-13 Thomas Ruckle Azolidinone-vinyl fused -benzene derivatives
WO2004007491A1 (en) 2002-07-10 2004-01-22 Applied Research Systems Ars Holding N.V. Azolidinone-vinyl fused-benzene derivatives
WO2004017950A2 (en) 2002-08-22 2004-03-04 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.
WO2006040966A1 (ja) 2004-10-08 2006-04-20 Astellas Pharma Inc. 芳香環縮合ピリミジン誘導体
GB0423653D0 (en) * 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
MX2008013583A (es) 2006-04-26 2008-10-31 Genentech Inc Compuestos del inhibidor de fosfoinositido 3-cinasa y composiciones farmaceuticas que los contienen.
KR20090021155A (ko) 2006-04-26 2009-02-27 에프. 호프만-라 로슈 아게 Ｐｉ3ｋ 억제제로서의 피리미딘 유도체
BRPI0710874A2 (pt) 2006-04-26 2012-02-14 Hoffmann La Roche compostos de tienopirimidina, processos de produção dos referidos compostos, composições farmacêuticas contendo os mesmos, kit, produto, e usos dos compostos
AU2007243457B2 (en) * 2006-04-26 2012-02-23 F. Hoffmann-La Roche Ag Pharmaceutical compounds
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
JP5500990B2 (ja) 2006-12-07 2014-05-21 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ホスホイノシチド３−キナーゼ阻害剤化合物及び使用方法
CL2007003520A1 (es) 2006-12-07 2008-08-22 Piramed Ltd Genentech Inc Compuestos derivados de heterociclos sustituidos con morfolina, inhibidores de la actividad pi3 quinasa; composicion farmaceutica que comprende a dichos compuestos; kit farmaceutico; y su uso para el tratamiento profilactico o terapeutico del cancer.

Also Published As

Publication number Publication date
PE20081679A1 (es) 2008-12-18
US8383620B2 (en) 2013-02-26
EP2518074A1 (en) 2012-10-31
BRPI0717923A2 (pt) 2013-10-22
TW200829253A (en) 2008-07-16
US20130129820A1 (en) 2013-05-23
JP2010512338A (ja) 2010-04-22
CO6190615A2 (es) 2010-08-19
ECSP099496A (es) 2009-09-29
CA2671782C (en) 2017-01-10
CL2007003520A1 (es) 2008-08-22
TWI499420B (zh) 2015-09-11
US20110097349A1 (en) 2011-04-28
AR064155A1 (es) 2009-03-18
CR10915A (es) 2009-08-31
RU2009125897A (ru) 2011-01-20
US8993563B2 (en) 2015-03-31
MA31146B1 (fr) 2010-02-01
CA2671782A1 (en) 2008-06-12
EP2114949A1 (en) 2009-11-11
NO20092566L (no) 2009-09-07
KR101460816B1 (ko) 2014-11-12
NZ578162A (en) 2011-12-22
MY180595A (en) 2020-12-03
US7888352B2 (en) 2011-02-15
US20080242665A1 (en) 2008-10-02
AU2007329352A1 (en) 2008-06-12
KR20090108016A (ko) 2009-10-14
WO2008070740A1 (en) 2008-06-12
ES2544082T3 (es) 2015-08-27
EP2518074B1 (en) 2015-07-22
JP5284977B2 (ja) 2013-09-11
RU2468027C2 (ru) 2012-11-27
AU2007329352B2 (en) 2013-01-17

Similar Documents

Publication Publication Date Title
MX2009005950A (es) Compuestos inhibidores de fosfoinositido 3-quinasas y metodos de uso.
MX2009005925A (es) Compuestos inhibidores de fosfoinositida 3-quinasa y los metodos de uso.
TW200801012A (en) Phosphoinositide 3-kinase inhibitor compounds and methods of use
MX338504B (es) Combinaciones de compuestos inhibidores de fosfoinosituro 3-cinasa y agentes quimioterapeuticos, y metodos de uso.
SG10201407781SA (en) Benzoxepin PI3K Inhibitor Compounds And Methods Of Use
WO2010105008A3 (en) Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents for the treatment of hematopoietic malignancies
WO2007127175A3 (en) Pharmaceutical compounds
MX2010010659A (es) Compuestos de benzopirano y benzoxepina, inhibidores de fosfoinoinositida 3-cinasas y metodos para utilizarlos.
WO2007027855A3 (en) Raf inhibitor compounds and methods of use thereof
MX2011012520A (es) Compuestos inhibidores de pi3k de pirimidina biciclicos selectivos para p110 delta y metodos de uso de los mismos.
AU2009312464A8 (en) Triazine, pyrimidine and pyridine analogs and their use as therapeutic agents and diagnostic probes
WO2009111278A3 (en) Raf inhibitor compounds and methods of use thereof
WO2006125101A3 (en) Raf inhibitor compounds and methods of use thereof
PH12013501779B1 (en) Pyrrolopyridines as kinase inhibitors
WO2007146824A3 (en) Quinoline compounds and methods of use
SG151286A1 (en) 5-substituted-2-phenylamino-benzamide as mek inhibitor
TW200800996A (en) Heterobicyclic pyrazole compounds and methods of use
NZ609448A (en) Tricyclic pi3k inhibitor compounds and methods of use
NO20090580L (no) Syklopenta[D]pyrimidiner som AKT-proteinkinaseinhibitorer
SG170101A1 (en) 2-pyrazinone derivatives for the treatment of disease or condition in which inhibition of neutrophil elastase activity is beneficial.
WO2008028141A3 (en) Raf inhibitor compounds and methods of use thereof
WO2011025938A3 (en) Raf inhibitor compounds and methods of use thereof
NO20064951L (no) 1,3,4-oksadiazol-2-oner som PPAR delta-modulatorer og deres anvendelse
WO2007109251A3 (en) Tumor necrosis factor alpha inhibitors and their use in the treatment of human diseases
SG178900A1 (en) Raf inhibitor compounds and methods of use thereof

Legal Events

Date Code Title Description
HH Correction or change in general
FG Grant or registration