JP2010500994A - Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法 - Google Patents

Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法 Download PDF

Info

Publication number
JP2010500994A
JP2010500994A JP2009524671A JP2009524671A JP2010500994A JP 2010500994 A JP2010500994 A JP 2010500994A JP 2009524671 A JP2009524671 A JP 2009524671A JP 2009524671 A JP2009524671 A JP 2009524671A JP 2010500994 A JP2010500994 A JP 2010500994A
Authority
JP
Japan
Prior art keywords
amino
phenyl
quinoxalin
methyloxy
sulfonyl
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
JP2009524671A
Other languages
English (en)
Japanese (ja)
Other versions
JP2010500994A5 (cg-RX-API-DMAC7.html
Inventor
ダナ ティー． アフタブ，
エー． ダグラス レアード，
ピーター ラム，
ジャン−フランソア アー． マルチーニ，
Original Assignee
エグゼリクシス， インコーポレイテッド
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
Application filed by エグゼリクシス， インコーポレイテッド filed Critical エグゼリクシス， インコーポレイテッド
Publication of JP2010500994A publication Critical patent/JP2010500994A/ja
Publication of JP2010500994A5 publication Critical patent/JP2010500994A5/ja
Pending legal-status Critical Current

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
    • A61K31/495—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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
JP2009524671A 2006-08-16 2007-08-16 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法 Pending JP2010500994A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83830706P 2006-08-16 2006-08-16
PCT/US2007/018057 WO2008021389A2 (en) 2006-08-16 2007-08-16 Using pi3k and mek modulators in treatments of cancer

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2013102030A Division JP2013151570A (ja) 2006-08-16 2013-05-14 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法

Publications (2)

Publication Number Publication Date
JP2010500994A true JP2010500994A (ja) 2010-01-14
JP2010500994A5 JP2010500994A5 (cg-RX-API-DMAC7.html) 2011-03-31

Family

ID=38819883

Family Applications (5)

Application Number Title Priority Date Filing Date
JP2009524671A Pending JP2010500994A (ja) 2006-08-16 2007-08-16 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP2013102030A Withdrawn JP2013151570A (ja) 2006-08-16 2013-05-14 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP2014067502A Pending JP2014122243A (ja) 2006-08-16 2014-03-28 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP2016019549A Withdrawn JP2016074743A (ja) 2006-08-16 2016-02-04 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP2017194176A Pending JP2017226702A (ja) 2006-08-16 2017-10-04 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法

Family Applications After (4)

Application Number Title Priority Date Filing Date
JP2013102030A Withdrawn JP2013151570A (ja) 2006-08-16 2013-05-14 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP2014067502A Pending JP2014122243A (ja) 2006-08-16 2014-03-28 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP2016019549A Withdrawn JP2016074743A (ja) 2006-08-16 2016-02-04 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP2017194176A Pending JP2017226702A (ja) 2006-08-16 2017-10-04 Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法

Country Status (8)

Country Link
US (3) US20100075947A1 (cg-RX-API-DMAC7.html)
EP (1) EP2056829B9 (cg-RX-API-DMAC7.html)
JP (5) JP2010500994A (cg-RX-API-DMAC7.html)
CN (2) CN101528231A (cg-RX-API-DMAC7.html)
AT (1) ATE539752T1 (cg-RX-API-DMAC7.html)
AU (1) AU2007284562B2 (cg-RX-API-DMAC7.html)
CA (1) CA2658725A1 (cg-RX-API-DMAC7.html)
WO (1) WO2008021389A2 (cg-RX-API-DMAC7.html)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010513288A (ja) * 2006-12-14 2010-04-30 エグゼリクシス， インコーポレイテッド Ｍｅｋ阻害剤の使用方法
JP2013507415A (ja) * 2009-10-12 2013-03-04 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｐｉ３ｋ阻害剤とｍｅｋ阻害剤の併用
JP2013151570A (ja) * 2006-08-16 2013-08-08 Exelixis Inc Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP2013543008A (ja) * 2010-11-19 2013-11-28 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド Ｂｒａｆ阻害剤による治療方法
JP2020520949A (ja) * 2017-05-22 2020-07-16 ユニバーシティ オブ ヴァージニア パテント ファウンデーションＵｎｉｖｅｒｓｉｔｙ Ｏｆ Ｖｅｒｇｉｎｉａ Ｐａｔｅｎｔ Ｆｏｕｎｄａｔｉｏｎ 組成物、並びにミトコンドリア脱共役剤を調製及び使用する方法
JP2021525247A (ja) * 2018-05-21 2021-09-24 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 複素縮合ピリドン化合物及びｉｄｈ阻害剤としてのこれらの使用
JP2022511730A (ja) * 2018-11-20 2022-02-01 エヌフレクション セラピューティクス インコーポレイテッド 皮膚障害の処置のためのシアノアリール－アニリン化合物

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013201011B2 (en) * 2005-10-07 2016-04-21 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
NZ608667A (en) * 2005-10-07 2014-08-29 Exelixis Inc N-(3-amino-quinoxalin-2-yl)-sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
HRP20130902T1 (hr) * 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
CA2622755C (en) * 2005-10-07 2017-01-31 Exelixis, Inc. Azetidines as mek inhibitors
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
MY146420A (en) 2006-09-15 2012-08-15 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors
ZA200904857B (en) * 2007-02-22 2010-09-29 Merck Serono Sa Quinoxaline compounds and use thereof
WO2008124085A2 (en) * 2007-04-03 2008-10-16 Exelixis, Inc. Methods of using combinations of mek and jak-2 inhibitors
DK2139484T3 (da) * 2007-04-10 2013-10-21 Exelixis Inc Fremgangsmåder til behandling af cancer ved brug af pyridopyrimidinon-inhibitorer af PI3K-alfa
AU2008239596B2 (en) * 2007-04-11 2013-08-15 Exelixis, Inc. Pyrido [2,3-D] pyrimidin-7-one compounds as inhibitors of PI3K-alpha for the treatment of cancer
RS53020B (sr) * 2007-04-11 2014-04-30 Exelixis Inc. Kombinovane terapije koje sadrže hinoksalin inhibitor pi3k-alfa za upotrebu u lečenju kancera
AU2008239655B2 (en) * 2007-04-11 2013-06-20 Exelixis, Inc. Pyrido (2, 3-d) pyrimidin-7-one compounds as inhibitors of PI3k-alpha for the treatment of cancer
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US8541415B2 (en) 2008-05-14 2013-09-24 University of Pittsburgh—of the Commonwealth System of Higher Education Targeting an HIV-1 nef-host cell kinase complex
GB0815947D0 (en) * 2008-09-02 2008-10-08 Univ Dundee Compounds
US8476282B2 (en) * 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
EP2374802B1 (en) 2008-11-10 2014-04-23 Kyowa Hakko Kirin Co., Ltd. Kynurenine production inhibitor
EP2370568B1 (en) 2008-12-10 2017-07-19 Dana-Farber Cancer Institute, Inc. Mek mutations conferring resistance to mek inhibitors
WO2011026579A1 (en) 2009-09-04 2011-03-10 Bayer Schering Pharma Aktiengesellschaft Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
AU2010298020B8 (en) * 2009-09-28 2013-10-10 Glaxosmithkline Llc Combination
WO2011100319A1 (en) * 2010-02-09 2011-08-18 Exelixis, Inc. Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors
MX340392B (es) 2010-02-25 2016-07-06 Dana Farber Cancer Inst Inc Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf.
JP5985401B2 (ja) 2010-03-09 2016-09-06 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド 第一の癌療法に対する耐性を現に有するか、または、そのような耐性を生じる患者において癌を診断および治療する方法
US9376709B2 (en) 2010-07-26 2016-06-28 Biomatrica, Inc. Compositions for stabilizing DNA and RNA in blood and other biological samples during shipping and storage at ambient temperatures
WO2012018639A2 (en) 2010-07-26 2012-02-09 Biomatrica, Inc. Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures
CA2812089C (en) 2010-09-14 2020-02-18 Exelixis Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
EA201390582A1 (ru) * 2010-10-20 2013-09-30 Мерк Сероно С.А. Женева Способ получения замещенных n-(3-аминохиноксалин-2-ил)сульфонамидов и их промежуточных n-(3-хлорхиноксалин-2-ил)сульфонамидов
DE102010048800A1 (de) 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
WO2012065057A2 (en) * 2010-11-12 2012-05-18 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
CN102718750B (zh) * 2011-03-31 2015-03-11 中国人民解放军军事医学科学院毒物药物研究所 含吖啶环的氨基吡啶类衍生物及其用途
MX351133B (es) 2011-09-22 2017-10-03 Exelixis Inc Metodo para tratar osteoporosis.
KR20140096083A (ko) 2011-11-01 2014-08-04 엑셀리시스, 인코포레이티드 림프증식성 악성종양의 치료를 위한 포스파티딜이노시톨 3-키나아제 저해제로서 ｎ­（3­｛［（3­｛［2­클로로­5­（메톡시）페닐］아미노｝퀴녹살린­2­일）아미노］설포닐｝페닐）­2­메틸알라닌아미드
WO2013067306A1 (en) * 2011-11-02 2013-05-10 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
CN103204822B (zh) 2012-01-17 2014-12-03 上海科州药物研发有限公司 作为蛋白激酶抑制剂的苯并噁唑化合物及其制备方法和用途
WO2013135612A1 (en) 2012-03-14 2013-09-19 Bayer Intellectual Property Gmbh Substituted imidazopyridazines
US20150141470A1 (en) 2012-05-08 2015-05-21 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
EP3495367B1 (en) 2012-06-13 2020-09-30 Incyte Holdings Corporation Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
AU2013328929B2 (en) 2012-10-12 2018-01-04 Exelixis, Inc. Novel process for making compounds for use in the treatment of cancer
EP2916859B1 (en) 2012-11-02 2017-06-28 The U.S.A. as represented by the Secretary, Department of Health and Human Services Method of reducing adverse effects in a cancer patient undergoing treatment with a mek inhibitor
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
WO2014100755A2 (en) 2012-12-20 2014-06-26 Biomatrica, Inc. Formulations and methods for stabilizing pcr reagents
US20160143910A1 (en) 2013-03-15 2016-05-26 Constellation Pharmaceuticals, Inc. Methods of treating cancer and preventing cancer drug resistance
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
EA201600002A1 (ru) 2013-06-11 2016-06-30 Байер Фарма Акциенгезельшафт Производные пролекарства замещенных триазолопиридинов
EP3632208A1 (en) 2013-06-13 2020-04-08 Biomatrica, INC. Cell stabilization
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
EP3154338B1 (en) 2014-06-10 2020-01-29 Biomatrica, INC. Stabilization of thrombocytes at ambient temperatures
US20170114323A1 (en) 2014-06-19 2017-04-27 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
MX385110B (es) * 2014-07-16 2025-03-11 Dev Ct Biotechnology Compuestos de quinoxalina, método para preparar los mismos y uso de los mismos.
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AR105483A1 (es) 2015-06-30 2017-10-11 Exelixis Inc Sal de fumarato cristalina de (s)-[3,4-difluoro-2-(2-fluoro-4-yodofenilamino)fenil][3-hidroxi-3-(piperidin-2-il)azetidin-1-il]-metanona
KR102787387B1 (ko) 2015-12-08 2025-03-26 바이오매트리카 인코포레이티드 적혈구 침강 속도의 감소
CA3059192A1 (en) 2016-05-26 2017-11-30 The Regents Of The University Of California Compounds and methods for hematopoietic regeneration
US11633415B2 (en) 2017-03-31 2023-04-25 The Broad Institute, Inc. Compounds and methods useful for treating or preventing cancers
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US20210188763A1 (en) * 2017-11-29 2021-06-24 The Regents Of The University Of California Compounds and methods for hematopoietic regeneration
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
CN112566912A (zh) 2018-05-04 2021-03-26 因赛特公司 Fgfr抑制剂的盐
US12378240B2 (en) 2018-11-20 2025-08-05 Nflection Therapeutics, Inc. Naphthyridinone-aniline compounds for treatment of dermal disorders
AU2019383310B2 (en) * 2018-11-20 2025-08-14 H. Lee Moffitt Cancer Center & Research Institute Aryl-aniline and heteroaryl-aniline compounds for treatment of skin cancers
CA3120352A1 (en) * 2018-11-20 2020-05-28 Nflection Therapeutics, Inc. Thienyl-aniline compounds for treatment of dermal disorders
EP3883554A4 (en) * 2018-11-20 2022-11-23 NFlection Therapeutics, Inc. Aryl-aniline and heteroaryl-aniline compounds for treatment of birthmarks
WO2020185532A1 (en) 2019-03-08 2020-09-17 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
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4055015B1 (en) 2019-11-08 2025-04-02 Nerviano Medical Sciences S.r.l. Gem-disubstituted heterocyclic compounds and their use as idh inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
ES2836551A1 (es) * 2020-08-11 2021-06-25 Molik Candelo Holmes Fármaco andreaquivi C34H34N6O6S
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
US12371667B2 (en) 2021-05-13 2025-07-29 Washington University Enhanced methods for inducing and maintaining naive human pluripotent stem cells
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環
TW202320802A (zh) * 2021-07-16 2023-06-01 美商塞萊托藥品股份有限公司 Ｂｃｌ抑制劑之脂質體調配物
US12310950B2 (en) 2021-11-23 2025-05-27 Nflection Therapeutics, Inc. Formulations of pyrrolopyridine-aniline compounds

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001509805A (ja) * 1997-02-05 2001-07-24 ワーナー−ランバート・コンパニー 細胞増殖阻害剤としてのピリド〔２，３−ｄ〕ピリミジンおよび４−アミノピリミジン
US20040009993A1 (en) * 2001-12-11 2004-01-15 Pharmacia Italia S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
WO2005105801A1 (en) * 2004-05-04 2005-11-10 Warner-Lambert Company Llc Pyrrolyl substituted pyrido[2,3-d]pyrimidin-7-ones and derivatives thereof as therapeutic agents
WO2006045514A1 (en) * 2004-10-20 2006-05-04 Applied Research Systems Ars Holding N.V. 3-arylamino pyridine derivatives
WO2007044813A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2007044515A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. Azetidines as mek inhibitors for the treatment of proliferative diseases
WO2007044698A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ501277A (en) * 1997-07-01 2002-12-20 Warner Lambert Co -2(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
EP1799699A1 (en) * 2004-10-13 2007-06-27 Wyeth Analogs of 17-hydroxywortmannin as pi3k inhibitors
US8071597B2 (en) 2005-08-26 2011-12-06 Merck Serono Sa Pyrazine compounds and uses as PI3K inhibitors
CA2658725A1 (en) 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
AU2007334402B2 (en) * 2006-12-14 2014-02-13 Exelixis, Inc. Methods of using MEK inhibitors
DK2139484T3 (da) 2007-04-10 2013-10-21 Exelixis Inc Fremgangsmåder til behandling af cancer ved brug af pyridopyrimidinon-inhibitorer af PI3K-alfa
RS53020B (sr) 2007-04-11 2014-04-30 Exelixis Inc. Kombinovane terapije koje sadrže hinoksalin inhibitor pi3k-alfa za upotrebu u lečenju kancera
AU2008239655B2 (en) 2007-04-11 2013-06-20 Exelixis, Inc. Pyrido (2, 3-d) pyrimidin-7-one compounds as inhibitors of PI3k-alpha for the treatment of cancer
AU2008239596B2 (en) 2007-04-11 2013-08-15 Exelixis, Inc. Pyrido [2,3-D] pyrimidin-7-one compounds as inhibitors of PI3K-alpha for the treatment of cancer
TW201018685A (en) 2008-09-30 2010-05-16 Exelixis Inc Pyridopyrimidinone inhibitors of PI3Kα and mTOR
WO2011100319A1 (en) 2010-02-09 2011-08-18 Exelixis, Inc. Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001509805A (ja) * 1997-02-05 2001-07-24 ワーナー−ランバート・コンパニー 細胞増殖阻害剤としてのピリド〔２，３−ｄ〕ピリミジンおよび４−アミノピリミジン
US20040009993A1 (en) * 2001-12-11 2004-01-15 Pharmacia Italia S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
WO2005105801A1 (en) * 2004-05-04 2005-11-10 Warner-Lambert Company Llc Pyrrolyl substituted pyrido[2,3-d]pyrimidin-7-ones and derivatives thereof as therapeutic agents
WO2006045514A1 (en) * 2004-10-20 2006-05-04 Applied Research Systems Ars Holding N.V. 3-arylamino pyridine derivatives
WO2007044813A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2007044515A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. Azetidines as mek inhibitors for the treatment of proliferative diseases
WO2007044698A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013151570A (ja) * 2006-08-16 2013-08-08 Exelixis Inc Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP2010513288A (ja) * 2006-12-14 2010-04-30 エグゼリクシス， インコーポレイテッド Ｍｅｋ阻害剤の使用方法
JP2013507415A (ja) * 2009-10-12 2013-03-04 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｐｉ３ｋ阻害剤とｍｅｋ阻害剤の併用
JP2015038110A (ja) * 2009-10-12 2015-02-26 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｐｉ３ｋ阻害剤とｍｅｋ阻害剤の併用
JP2013543008A (ja) * 2010-11-19 2013-11-28 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド Ｂｒａｆ阻害剤による治療方法
JP2020520949A (ja) * 2017-05-22 2020-07-16 ユニバーシティ オブ ヴァージニア パテント ファウンデーションＵｎｉｖｅｒｓｉｔｙ Ｏｆ Ｖｅｒｇｉｎｉａ Ｐａｔｅｎｔ Ｆｏｕｎｄａｔｉｏｎ 組成物、並びにミトコンドリア脱共役剤を調製及び使用する方法
JP2021525247A (ja) * 2018-05-21 2021-09-24 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 複素縮合ピリドン化合物及びｉｄｈ阻害剤としてのこれらの使用
JP7304896B2 (ja) 2018-05-21 2023-07-07 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 複素縮合ピリドン化合物及びｉｄｈ阻害剤としてのこれらの使用
JP2022511730A (ja) * 2018-11-20 2022-02-01 エヌフレクション セラピューティクス インコーポレイテッド 皮膚障害の処置のためのシアノアリール－アニリン化合物
JP7406264B2 (ja) 2018-11-20 2023-12-27 エヌフレクション セラピューティクス インコーポレイテッド 皮膚障害の処置のためのシアノアリール－アニリン化合物

Also Published As

Publication number Publication date
US20120302545A1 (en) 2012-11-29
EP2056829B1 (en) 2012-01-04
CN104784695A (zh) 2015-07-22
US20140100215A1 (en) 2014-04-10
US20100075947A1 (en) 2010-03-25
CN101528231A (zh) 2009-09-09
US8642584B2 (en) 2014-02-04
AU2007284562A1 (en) 2008-02-21
HK1130438A1 (en) 2009-12-31
JP2014122243A (ja) 2014-07-03
JP2016074743A (ja) 2016-05-12
WO2008021389A8 (en) 2009-03-12
WO2008021389A2 (en) 2008-02-21
CA2658725A1 (en) 2008-02-21
WO2008021389A3 (en) 2008-07-17
EP2056829B9 (en) 2012-09-26
EP2056829A2 (en) 2009-05-13
ATE539752T1 (de) 2012-01-15
JP2017226702A (ja) 2017-12-28
JP2013151570A (ja) 2013-08-08
AU2007284562B2 (en) 2013-05-02

Similar Documents

Publication Publication Date Title
JP2017226702A (ja) Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP5709821B2 (ja) ホスファチジルイノシトール３−キナーゼインヒビターとその使用方法
JP5726515B2 (ja) Ｐｉ３ｋ−アルファのキナゾリン阻害剤を用いた阻害による治療方法
JP2009525337A (ja) Ｊａｋ−２調節因子としての４−アリール−２−アミノ−ピリミジン類又は４−アリール−２−アミノアルキル−ピリミジン類と使用方法
TW200306838A (en) Chemical compounds
HK1130438B (en) Using pi3k and mek modulators in treatments of cancer
HK1119697B (en) N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
HK1162170A (en) N-(3-phenylamino-quinoxalin-2-yl)-benzenesulfonamide derivatives as phosphatidylinositol 3-kinase inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100813

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20100813

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110214

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20121220

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130319

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130327

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20130419

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20130426

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130514

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130808

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20131129