ATE539752T1 - Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung - Google Patents

Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung

Info

Publication number
ATE539752T1
ATE539752T1 AT07811344T AT07811344T ATE539752T1 AT E539752 T1 ATE539752 T1 AT E539752T1 AT 07811344 T AT07811344 T AT 07811344T AT 07811344 T AT07811344 T AT 07811344T AT E539752 T1 ATE539752 T1 AT E539752T1
Authority
AT
Austria
Prior art keywords
pi3k
cancer treatment
mek
modulators
mek modulators
Prior art date
Application number
AT07811344T
Other languages
German (de)
English (en)
Inventor
Dana Aftab
A Laird
Peter Lamb
Jean-Francois Martini
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
Application granted granted Critical
Publication of ATE539752T1 publication Critical patent/ATE539752T1/de

Links

Classifications

    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (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)
AT07811344T 2006-08-16 2007-08-16 Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung ATE539752T1 (de)

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

Publications (1)

Publication Number Publication Date
ATE539752T1 true ATE539752T1 (de) 2012-01-15

Family

ID=38819883

Family Applications (1)

Application Number Title Priority Date Filing Date
AT07811344T ATE539752T1 (de) 2006-08-16 2007-08-16 Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung

Country Status (8)

Country Link
US (3) US20100075947A1 (enExample)
EP (1) EP2056829B9 (enExample)
JP (5) JP2010500994A (enExample)
CN (2) CN104784695A (enExample)
AT (1) ATE539752T1 (enExample)
AU (1) AU2007284562B2 (enExample)
CA (1) CA2658725A1 (enExample)
WO (1) WO2008021389A2 (enExample)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2006302415B2 (en) * 2005-10-07 2012-09-13 Exelixis, Inc. Azetidines as MEK inhibitors for the treatment of proliferative diseases
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
KR20140105621A (ko) * 2005-10-07 2014-09-01 엑셀리시스, 인코포레이티드 ＰＩ３Ｋα의 피리도피리미디논 억제제
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
ATE539752T1 (de) 2006-08-16 2012-01-15 Exelixis Inc Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung
ATE514695T1 (de) 2006-09-15 2011-07-15 Pfizer Prod Inc Pyrido(2,3-d)pyrimidinonverbindungen und ihre verwendung als pi3-inhibitoren
CN105106199A (zh) * 2006-12-14 2015-12-02 埃克塞利希斯股份有限公司 使用mek抑制剂的方法
US8614215B2 (en) * 2007-02-22 2013-12-24 Merck Serono Sa Quinoxaline inhibitors of phosphoinositide-3-kinases (PI3Ks)
WO2008124085A2 (en) * 2007-04-03 2008-10-16 Exelixis, Inc. Methods of using combinations of mek and jak-2 inhibitors
CA2683641C (en) * 2007-04-10 2016-08-16 Exelixis, Inc. Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k alpha
BRPI0810175A2 (pt) * 2007-04-11 2014-12-30 Exelixis Inc Inibidores pirididopirinidinona de p13k alfa
AU2008239668B2 (en) 2007-04-11 2013-11-07 Exelixis, Inc. Combination therapies comprising quinoxaline inhibitors of PI3K-alpha for use in the treatment of cancer
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
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
US8476282B2 (en) * 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
WO2010053182A1 (ja) * 2008-11-10 2010-05-14 協和発酵キリン株式会社 キヌレニン産生抑制剤
US9084781B2 (en) 2008-12-10 2015-07-21 Novartis Ag MEK mutations conferring resistance to MEK inhibitors
JP5728683B2 (ja) 2009-09-04 2015-06-03 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 チロシンスレオニンキナーゼ阻害剤としての置換アミノキノキサリン
WO2011038380A2 (en) * 2009-09-28 2011-03-31 Glaxosmithkline Llc Combination
TWI428336B (zh) * 2009-10-12 2014-03-01 Hoffmann La Roche Ｐｉ３ｋ抑制劑及ｍｅｋ抑制劑之組合
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
MX360932B (es) 2010-02-25 2018-11-21 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.
EP2545187B1 (en) 2010-03-09 2018-09-05 Dana-Farber Cancer Institute, Inc. Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy
CA2806734A1 (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
EP2598660B1 (en) 2010-07-26 2017-03-15 Biomatrica, INC. Compositions for stabilizing dna, rna and proteins in blood 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
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
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
EP2640387A4 (en) * 2010-11-19 2014-08-20 Glaxosmithkline Ip No 2 Ltd METHOD OF TREATMENT USING BRAF INHIBITOR
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
WO2013043840A1 (en) 2011-09-22 2013-03-28 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
CN104284896B (zh) 2012-03-14 2016-06-01 拜耳知识产权有限责任公司 取代的咪唑并哒嗪
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
EP3176170B1 (en) 2012-06-13 2018-11-14 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
AU2013328929B2 (en) 2012-10-12 2018-01-04 Exelixis, Inc. Novel process for making compounds for use in the treatment of cancer
US20150265679A1 (en) 2012-11-02 2015-09-24 The United States Of America, As Represented By Secretary, Department Of Health And Human Services Method of reducing adverse effects in a cancer patient undregoing treatment with a mek inhibitor
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
HK1217117A1 (zh) 2012-12-20 2016-12-23 生物马特里卡公司 用於使pcr试剂稳定化的制剂和方法
KR20150130451A (ko) 2013-03-15 2015-11-23 제넨테크, 인크. 암 치료 방법 및 항암제 내성 예방을 위한 방법
SG10201708520YA (en) 2013-04-19 2017-12-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
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
EP3122358B1 (en) 2014-03-26 2020-12-16 Astex Therapeutics Ltd. Combinations of fgfr- and cmet-inhibitors for the treatment of cancer
ES2786373T3 (es) 2014-06-10 2020-10-09 Biomatrica Inc Estabilización de trombocitos a temperaturas ambiente
US20170114323A1 (en) 2014-06-19 2017-04-27 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
NZ728498A (en) * 2014-07-16 2022-07-01 Dev Ct Biotechnology Quinoxaline compounds, method for preparing the same and use thereof
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
MX373169B (es) 2015-02-20 2020-04-24 Incyte Holdings Corp Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr).
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
WO2017100212A1 (en) 2015-12-08 2017-06-15 Biomatrica, Inc. Reduction of erythrocyte sedimentation rate
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
WO2018217757A1 (en) * 2017-05-22 2018-11-29 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
CR20240498A (es) 2018-05-04 2025-01-08 Incyte Corp FORMAS SÓLIDAS DE UN INHIBIDOR DE FGFR Y PROCESOS PARA PREPARARLAS (Divisional EXP. 2020-0590)
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
SG11202011366SA (en) * 2018-05-21 2020-12-30 Nerviano Medical Sciences Srl Heterocondensed pyridones compounds and their use as idh inhibitors
CA3120351A1 (en) * 2018-11-20 2020-05-28 Nflection Therapeutics, Inc. Aryl-aniline and heteroaryl-aniline compounds for treatment of skin cancers
US12378240B2 (en) 2018-11-20 2025-08-05 Nflection Therapeutics, Inc. Naphthyridinone-aniline compounds for treatment of dermal disorders
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
CN117551073A (zh) 2018-11-20 2024-02-13 恩福莱克逊治疗有限公司 用于治疗皮肤疾病噻吩基苯胺化合物
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
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
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JOP20220083A1 (ar) 2019-10-14 2023-01-30 Incyte Corp حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN115038700B (zh) 2019-11-08 2025-07-25 内尔维亚诺医疗科学公司 偕二取代的杂环化合物及其作为idh抑制剂的用途
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
PE20221504A1 (es) 2019-12-04 2022-09-30 Incyte Corp Derivados de un inhibidor de fgfr
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
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
JP2024522188A (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
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2023288100A1 (en) * 2021-07-16 2023-01-19 Celator Pharmaceuticals, Inc. Liposomal formulations of bcl inhibitors
CA3238962A1 (en) 2021-11-23 2023-06-01 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
WO1998033798A2 (en) 1997-02-05 1998-08-06 Warner Lambert Company Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell 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
US20080255162A1 (en) * 2004-05-04 2008-10-16 Warner-Lambert Company Llc Pyrrolyl Substituted Pyrido[2,3-D]Pyrimidin-7-Ones and Derivatives Thereof as Therapeutic Agents
GT200500287A (es) * 2004-10-13 2006-04-17 Analogos de 17-hidroxiwortmanina como inhibidores de pi3k
SI1802579T1 (sl) * 2004-10-20 2014-03-31 Merck Serono Sa Derivati 3-arilaminopiridina
BRPI0615233A2 (pt) 2005-08-26 2011-05-10 Serono Lab derivados de pirazina e uso dos mesmos como inibidores p13k
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
KR20140105621A (ko) * 2005-10-07 2014-09-01 엑셀리시스, 인코포레이티드 ＰＩ３Ｋα의 피리도피리미디논 억제제
AU2006302415B2 (en) * 2005-10-07 2012-09-13 Exelixis, Inc. Azetidines as MEK inhibitors for the treatment of proliferative diseases
CA2624965A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. Pyridopyrimidinone inhibitors of pi3k.alpha.
ATE539752T1 (de) 2006-08-16 2012-01-15 Exelixis Inc Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung
CN105106199A (zh) * 2006-12-14 2015-12-02 埃克塞利希斯股份有限公司 使用mek抑制剂的方法
CA2683641C (en) 2007-04-10 2016-08-16 Exelixis, Inc. Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k alpha
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
BRPI0810175A2 (pt) 2007-04-11 2014-12-30 Exelixis Inc Inibidores pirididopirinidinona de p13k alfa
AU2008239668B2 (en) 2007-04-11 2013-11-07 Exelixis, Inc. Combination therapies comprising quinoxaline inhibitors of PI3K-alpha for use in the treatment of cancer
PA8843901A1 (es) 2008-09-30 2010-05-26 INHIBIDORES DE PIRIMIDINONA DE PI3K( ALFA) Y m TOR
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

Also Published As

Publication number Publication date
HK1130438A1 (en) 2009-12-31
EP2056829B9 (en) 2012-09-26
WO2008021389A3 (en) 2008-07-17
EP2056829A2 (en) 2009-05-13
WO2008021389A2 (en) 2008-02-21
JP2017226702A (ja) 2017-12-28
JP2014122243A (ja) 2014-07-03
JP2010500994A (ja) 2010-01-14
US20120302545A1 (en) 2012-11-29
AU2007284562A1 (en) 2008-02-21
AU2007284562B2 (en) 2013-05-02
JP2016074743A (ja) 2016-05-12
CN101528231A (zh) 2009-09-09
CN104784695A (zh) 2015-07-22
CA2658725A1 (en) 2008-02-21
JP2013151570A (ja) 2013-08-08
US8642584B2 (en) 2014-02-04
WO2008021389A8 (en) 2009-03-12
US20100075947A1 (en) 2010-03-25
US20140100215A1 (en) 2014-04-10
EP2056829B1 (en) 2012-01-04

Similar Documents

Publication Publication Date Title
ATE539752T1 (de) Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung
TR200906131T1 (tr) Aktivin -actrIIa antagonistleri ve göğüs kanserinin tedavi e
CY1122522T1 (el) Μετα αρσενικωδες νατριο για χρηση στην αγωγη του πολλαπλου μυελωματος
EA201300810A1 (ru) Противораковая терапия с использованием двойных ингибиторов киназ аврора/мек
CY1109741T1 (el) Sns-595 και μεθοδοι χρησης αυτου
ECSP10010007A (es) Tratamiento con ligandos alpha-7-selectivos
TW200716141A (en) Compositions and methods for treatment for neoplasms
MX2011006150A (es) Compuestos inhibidores de cinasa.
MX2011013739A (es) Composiciones y metodos para reducir trigliceridos sin elevar los niveles de ldl-c en un sujeto en terapia de estatina concomitante.
EA200970737A1 (ru) Оксабициклогептаны и оксабициклогептены, их получение и применение
CY1115535T1 (el) Αναστολεις δραστικοτητας ακτ
CO6351714A2 (es) Tratamiento para diabetes en pacientes inapropiados para terapia con metformina
EA201171367A1 (ru) Винилиндазолильные соединения
WO2010118063A3 (en) Pyruvate kinase m2 modulators, therapeutic compositions and related methods of use
JO2788B1 (en) Amido phenoxyendazole compounds beneficial as C-MET inhibitors
DK1866324T3 (da) Phosphoramidatderivater af nukleosidforbindelser til anvendelse i behandlingen af cancer
EA201071248A1 (ru) Дизамещенные фталазиновые антагонисты пути hedgehog
NO20072179L (no) Kombinasjon av en SRC kinase inhibitor og en. BCR-ABL inhibitor for behandling av proleferative sykdommer
EA200971068A1 (ru) Триазолиламинопиримидиновые соединения
MX2009005300A (es) Combinacion de un inhibidor de acido desoxirribonucleico polimerasa-alfa y un inhibidor de una cinasa de punto de verificacion para trastornos proliferativos.
NO20093542L (no) Inhibering av tumormetastase ved hjelp av anti-neuropilin 2-antistoffer
WO2009158374A3 (en) Inhibitors of akt activity
WO2008112129A3 (en) Treatment of carcinomas with a combination of egf-pathway and telomerase inhibitors
NO20081292L (no) Pentasykliske kinaseinhibitorer
MX2010008994A (es) Combinacion que comprende paclitaxel para el tratamiento del cancer de ovario.