CN101528231A - 在癌症的治疗中使用pi3k和mek调控剂 - Google Patents

在癌症的治疗中使用pi3k和mek调控剂 Download PDF

Info

Publication number
CN101528231A
CN101528231A CNA200780038496XA CN200780038496A CN101528231A CN 101528231 A CN101528231 A CN 101528231A CN A200780038496X A CNA200780038496X A CN A200780038496XA CN 200780038496 A CN200780038496 A CN 200780038496A CN 101528231 A CN101528231 A CN 101528231A
Authority
CN
China
Prior art keywords
amino
phenyl
quinoxalin
methoxy
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.)
Withdrawn
Application number
CNA200780038496XA
Other languages
English (en)
Chinese (zh)
Inventor
达纳·T·阿夫塔布
A·D·莱尔德
彼得·拉姆
让-弗朗索瓦·A·马蒂尼
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Exelixis Inc
Original Assignee
Exelixis 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
Application filed by Exelixis Inc filed Critical Exelixis Inc
Priority to CN201510204883.2A priority Critical patent/CN104784695A/zh
Publication of CN101528231A publication Critical patent/CN101528231A/zh
Withdrawn legal-status Critical Current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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNA200780038496XA 2006-08-16 2007-08-16 在癌症的治疗中使用pi3k和mek调控剂 Withdrawn CN101528231A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201510204883.2A CN104784695A (zh) 2006-08-16 2007-08-16 使用pi3k和mek调控剂的方法

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83830706P 2006-08-16 2006-08-16
US60/838,307 2006-08-16

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201510204883.2A Division CN104784695A (zh) 2006-08-16 2007-08-16 使用pi3k和mek调控剂的方法

Publications (1)

Publication Number Publication Date
CN101528231A true CN101528231A (zh) 2009-09-09

Family

ID=38819883

Family Applications (2)

Application Number Title Priority Date Filing Date
CNA200780038496XA Withdrawn CN101528231A (zh) 2006-08-16 2007-08-16 在癌症的治疗中使用pi3k和mek调控剂
CN201510204883.2A Pending CN104784695A (zh) 2006-08-16 2007-08-16 使用pi3k和mek调控剂的方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201510204883.2A Pending CN104784695A (zh) 2006-08-16 2007-08-16 使用pi3k和mek调控剂的方法

Country Status (8)

Country Link
US (3) US20100075947A1 (enExample)
EP (1) EP2056829B9 (enExample)
JP (5) JP2010500994A (enExample)
CN (2) CN101528231A (enExample)
AT (1) ATE539752T1 (enExample)
AU (1) AU2007284562B2 (enExample)
CA (1) CA2658725A1 (enExample)
WO (1) WO2008021389A2 (enExample)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012130160A1 (zh) * 2011-03-31 2012-10-04 中国人民解放军军事医学科学院毒物药物研究所 含吖丁啶环的氨基吡啶类衍生物及其用途
CN103270027A (zh) * 2010-10-20 2013-08-28 默克雪兰诺日内瓦有限公司 制备取代的n-(3-氨基-喹喔啉-2-基)-磺酰胺和它们的中间体n-(3-氯-喹喔啉-2-基)-磺酰胺的方法
CN104689318A (zh) * 2010-11-19 2015-06-10 葛兰素史密斯克莱知识产权（第2号）有限公司 使用braf抑制剂的治疗方法
CN112469719A (zh) * 2018-05-21 2021-03-09 内尔维亚诺医疗科学公司 杂缩合的吡啶酮化合物及其作为idh抑制剂的用途
CN113473978A (zh) * 2018-11-20 2021-10-01 恩福莱克逊治疗有限公司 用于治疗皮肤疾病氰基芳烃-苯胺化合物
CN113645964A (zh) * 2018-11-20 2021-11-12 恩福莱克逊治疗有限公司 用于胎记治疗的芳基苯胺和杂芳基苯胺化合物
CN117088821A (zh) * 2014-07-16 2023-11-21 财团法人生物技术开发中心 喹喔啉化合物、其制造方法及用途

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8044062B2 (en) * 2005-10-07 2011-10-25 Exelixis, Inc. Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha
DE602006021205D1 (de) * 2005-10-07 2011-05-19 Exelixis Inc Azetidine als mek-inhibitoren bei der behandlung proliferativer erkrankungen
ES2513165T3 (es) * 2005-10-07 2014-10-24 Exelixis, Inc. Derivados de N-(3-amino-quinoxalin-2-il)-sulfonamida y su uso como inhibidores de la fosfatidilinositol-3-quinasa
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
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
JP2010500994A (ja) * 2006-08-16 2010-01-14 エグゼリクシス， インコーポレイテッド Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
GEP20115306B (enExample) 2006-09-15 2011-10-10 Pfizer Prod Inc
JP5311673B2 (ja) * 2006-12-14 2013-10-09 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
JP5508027B2 (ja) 2007-02-22 2014-05-28 メルク セローノ ソシエテ アノニム キノキサリン化合物及びその使用
WO2008124085A2 (en) * 2007-04-03 2008-10-16 Exelixis, Inc. Methods of using combinations of mek and jak-2 inhibitors
UA100979C2 (ru) 2007-04-10 2013-02-25 Экселиксис, Инк. Применение пиридопиримидиноновых ингибиторов pi3k альфа для лечения рака
CA2683784A1 (en) * 2007-04-11 2008-10-23 Exelixis, Inc. Pyrido[2,3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
NZ580009A (en) * 2007-04-11 2012-06-29 Exelixis Inc Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer
NZ579945A (en) * 2007-04-11 2012-05-25 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
WO2009139886A2 (en) * 2008-05-14 2009-11-19 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
US8476431B2 (en) * 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
PT2374802E (pt) * 2008-11-10 2014-07-10 Kyowa Hakko Kirin Co Ltd Inibidor de produção de quinurenina
US9084781B2 (en) 2008-12-10 2015-07-21 Novartis Ag MEK mutations conferring resistance to MEK inhibitors
CA2772790C (en) 2009-09-04 2017-06-27 Benjamin Bader Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
BR112012006968A2 (pt) * 2009-09-28 2019-09-24 Glaxosmithkline Llc combinação
US20110086837A1 (en) * 2009-10-12 2011-04-14 Genentech, Inc. Combinations of a pi3k inhibitor and a mek inhibitor
AR080151A1 (es) 2010-02-09 2012-03-14 Exelixis Inc Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia
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.
CN103038364A (zh) 2010-03-09 2013-04-10 达纳－法伯癌症研究所公司 诊断和治疗具有或发展对于第一种癌症治疗的抗性的患者中的癌症的方法
EP2598661B1 (en) 2010-07-26 2017-09-27 Biomatrica, INC. Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures
WO2012018638A2 (en) 2010-07-26 2012-02-09 Biomatrica, Inc. Compositions for stabilizing dna, rna and proteins in blood and other biological samples during shipping and storage at ambient temperatures
TWI642670B (zh) 2010-09-14 2018-12-01 伊塞利克斯公司 Ｐｉ３ｋ-德爾塔抑制劑以及其應用和生產方法
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
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
EP2758057B1 (en) 2011-09-22 2017-05-31 Exelixis, Inc. Method for treating osteoporosis
PE20141794A1 (es) 2011-11-01 2014-12-17 Exelixis Inc N-(3-{[(3-{[2-cloro-5-(metoxi)fenil]amino}quinoxalin-2-il)amino]sulfonil}fenil)-2-metilalaninamida como inhibidor de fosfatidilinositol 3-quinasa para el tratamiento de neoplasias linfoproliferativas
WO2013067306A1 (en) * 2011-11-02 2013-05-10 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors for the treatment of childhood cancers
CN103204827B (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噻二唑化合物及其制备方法和用途
JP6166289B2 (ja) 2012-03-14 2017-07-19 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 置換イミダゾピリダジン
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
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
JP6300042B2 (ja) 2012-10-12 2018-03-28 エグゼリクシス， インコーポレイテッド 癌の処置に使用するための化合物の製造方法
CA2890238A1 (en) 2012-11-02 2014-05-08 Merck Patent Gmbh 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
EP2934572A4 (en) 2012-12-20 2016-11-23 Biomatrica Inc FORMULATIONS AND METHODS FOR STABILIZING PCR REAGENTS
CN105339001A (zh) 2013-03-15 2016-02-17 基因泰克公司 治疗癌症和预防癌症耐药性的方法
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為ｆｇｆｒ抑制劑之雙環雜環
PT3008062T (pt) 2013-06-11 2017-06-07 Bayer Pharma AG Derivados de profármaco de triazolopiridinas substituídas
EP3007556B1 (en) 2013-06-13 2020-05-20 Biomatrica, INC. Cell stabilization
HUE053654T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR- és CMET-inhibitorok kombinációi a rák kezelésére
JP6661554B2 (ja) 2014-06-10 2020-03-11 バイオマトリカ，インク． 周囲温度における血小板の安定化
WO2015196072A2 (en) 2014-06-19 2015-12-23 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
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
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
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
JP6827048B2 (ja) 2015-12-08 2021-02-10 バイオマトリカ，インク． 赤血球沈降速度の低下
US10822299B2 (en) 2016-05-26 2020-11-03 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
US11896591B2 (en) 2017-05-22 2024-02-13 University Of Virginia Patent Foundation Compositions and methods for preparing and using mitochondrial uncouplers
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CA3084491A1 (en) * 2017-11-29 2019-06-06 The Regents Of The University Of California Compounds and methods for hematopoietic regeneration
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
JP7546297B2 (ja) * 2018-11-20 2024-09-06 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チエニル－アニリン化合物
CA3120351A1 (en) * 2018-11-20 2020-05-28 Nflection Therapeutics, Inc. Aryl-aniline and heteroaryl-aniline compounds for treatment of skin cancers
CA3120337A1 (en) 2018-11-20 2020-05-28 Nflection Therapeutics, Inc. Naphthyridinone-aniline compounds for treatment of dermal disorders
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 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
US12521395B2 (en) 2019-11-08 2026-01-13 Nerviano Medical Sciences S.R.L. Gem-disubstituted heterocyclic compounds and their use as IDH inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
ES2836551A1 (es) * 2020-08-11 2021-06-25 Molik Candelo Holmes Fármaco andreaquivi C34H34N6O6S
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
US12371667B2 (en) 2021-05-13 2025-07-29 Washington University Enhanced methods for inducing and maintaining naive human pluripotent stem cells
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN117897140A (zh) * 2021-07-16 2024-04-16 塞拉特药物股份有限公司 用于制备脂质体制剂的方法
EP4436570A4 (en) 2021-11-23 2025-10-22 Nflection Therapeutics Inc FORMULATIONS OF PYRROLOPYRIDINE-ANILINE COMPOUNDS

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69839338T2 (de) 1997-02-05 2008-07-10 Warner-Lambert Company Llc Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation
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
US7019002B2 (en) * 2001-12-11 2006-03-28 Pharmacia & Upjohn, S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
BRPI0510560A (pt) * 2004-05-04 2007-11-20 Warner Lambert Co pirido[2,3-d] pirimidin-7-onas pirrolil substituìdas e seus derivados como agentes terapêuticos
TW200626610A (en) * 2004-10-13 2006-08-01 Wyeth Corp Analogs of 17-hydroxywortmannin as PI3K inhibitors
MX2007004781A (es) * 2004-10-20 2007-05-11 Applied Research Systems Derivados de 3-arilamino piridina.
WO2007023186A1 (en) 2005-08-26 2007-03-01 Laboratoires Serono S.A. Pyrazine derivatives and use as pi3k inhibitors
DE602006021205D1 (de) * 2005-10-07 2011-05-19 Exelixis Inc Azetidine als mek-inhibitoren bei der behandlung proliferativer erkrankungen
ES2513165T3 (es) 2005-10-07 2014-10-24 Exelixis, Inc. Derivados de N-(3-amino-quinoxalin-2-il)-sulfonamida y su uso como inhibidores de la fosfatidilinositol-3-quinasa
US8044062B2 (en) 2005-10-07 2011-10-25 Exelixis, Inc. Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha
US8247408B2 (en) * 2005-10-07 2012-08-21 Exelixis, Inc. Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer
JP2010500994A (ja) 2006-08-16 2010-01-14 エグゼリクシス， インコーポレイテッド Ｐｉ３ｋおよびｍｅｋモジュレーターを使用する方法
JP5311673B2 (ja) * 2006-12-14 2013-10-09 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
UA100979C2 (ru) 2007-04-10 2013-02-25 Экселиксис, Инк. Применение пиридопиримидиноновых ингибиторов pi3k альфа для лечения рака
NZ580009A (en) 2007-04-11 2012-06-29 Exelixis Inc Combination therapies comprising quinoxaline inhibitors of pi3k-alpha for use in the treatment of cancer
NZ579945A (en) 2007-04-11 2012-05-25 Exelixis Inc Pyrido [2,3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
CA2683784A1 (en) 2007-04-11 2008-10-23 Exelixis, Inc. Pyrido[2,3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
AR073524A1 (es) 2008-09-30 2010-11-10 Exelixis Inc Piridopirimidinonas inhibidores de pi3k a y m tor
AR080151A1 (es) 2010-02-09 2012-03-14 Exelixis Inc Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103270027A (zh) * 2010-10-20 2013-08-28 默克雪兰诺日内瓦有限公司 制备取代的n-(3-氨基-喹喔啉-2-基)-磺酰胺和它们的中间体n-(3-氯-喹喔啉-2-基)-磺酰胺的方法
CN104689318A (zh) * 2010-11-19 2015-06-10 葛兰素史密斯克莱知识产权（第2号）有限公司 使用braf抑制剂的治疗方法
WO2012130160A1 (zh) * 2011-03-31 2012-10-04 中国人民解放军军事医学科学院毒物药物研究所 含吖丁啶环的氨基吡啶类衍生物及其用途
CN102718750A (zh) * 2011-03-31 2012-10-10 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
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
CN117088821A (zh) * 2014-07-16 2023-11-21 财团法人生物技术开发中心 喹喔啉化合物、其制造方法及用途
CN112469719A (zh) * 2018-05-21 2021-03-09 内尔维亚诺医疗科学公司 杂缩合的吡啶酮化合物及其作为idh抑制剂的用途
CN112469719B (zh) * 2018-05-21 2024-01-23 内尔维亚诺医疗科学公司 杂缩合的吡啶酮化合物及其作为idh抑制剂的用途
CN113473978A (zh) * 2018-11-20 2021-10-01 恩福莱克逊治疗有限公司 用于治疗皮肤疾病氰基芳烃-苯胺化合物
CN113645964A (zh) * 2018-11-20 2021-11-12 恩福莱克逊治疗有限公司 用于胎记治疗的芳基苯胺和杂芳基苯胺化合物
CN113645964B (zh) * 2018-11-20 2024-10-11 恩福莱克逊治疗有限公司 用于胎记治疗的芳基苯胺和杂芳基苯胺化合物
CN113473978B (zh) * 2018-11-20 2025-03-28 恩福莱克逊治疗有限公司 用于治疗皮肤疾病氰基芳烃-苯胺化合物

Also Published As

Publication number Publication date
ATE539752T1 (de) 2012-01-15
US20120302545A1 (en) 2012-11-29
JP2010500994A (ja) 2010-01-14
JP2017226702A (ja) 2017-12-28
EP2056829B1 (en) 2012-01-04
WO2008021389A3 (en) 2008-07-17
HK1130438A1 (en) 2009-12-31
JP2013151570A (ja) 2013-08-08
US8642584B2 (en) 2014-02-04
AU2007284562B2 (en) 2013-05-02
US20140100215A1 (en) 2014-04-10
EP2056829B9 (en) 2012-09-26
WO2008021389A2 (en) 2008-02-21
US20100075947A1 (en) 2010-03-25
CA2658725A1 (en) 2008-02-21
WO2008021389A8 (en) 2009-03-12
JP2016074743A (ja) 2016-05-12
EP2056829A2 (en) 2009-05-13
JP2014122243A (ja) 2014-07-03
CN104784695A (zh) 2015-07-22
AU2007284562A1 (en) 2008-02-21

Similar Documents

Publication Publication Date Title
CN101528231A (zh) 在癌症的治疗中使用pi3k和mek调控剂
CN101282948A (zh) N-(3-氨基-喹喔啉-2-基)-磺酰胺衍生物及其作为磷脂酰肌醇3-激酶抑制剂的用途
CN101296909B (zh) 吡嗪衍生物及其作为pi3k抑制剂的应用
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
CN102256980A (zh) 3-(3-嘧啶-2-基苄基)-1，2，4-三唑并[4，3-b]嘧啶衍生物
HK1130438B (en) Using pi3k and mek modulators in treatments of cancer
AU2013201011B2 (en) N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C04 Withdrawal of patent application after publication (patent law 2001)
WW01 Invention patent application withdrawn after publication

Application publication date: 20090909