AU2007284562B2 - Using PI3K and MEK modulators in treatments of cancer - Google Patents

Using PI3K and MEK modulators in treatments of cancer Download PDF

Info

Publication number
AU2007284562B2
AU2007284562B2 AU2007284562A AU2007284562A AU2007284562B2 AU 2007284562 B2 AU2007284562 B2 AU 2007284562B2 AU 2007284562 A AU2007284562 A AU 2007284562A AU 2007284562 A AU2007284562 A AU 2007284562A AU 2007284562 B2 AU2007284562 B2 AU 2007284562B2
Authority
AU
Australia
Prior art keywords
phenyl
amino
methyloxy
alkyl
bis
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.)
Ceased
Application number
AU2007284562A
Other languages
English (en)
Other versions
AU2007284562A1 (en
Inventor
Dana T. Aftab
A. Douglas Laird
Peter Lamb
Jean-Francois A. Martini
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
Publication of AU2007284562A1 publication Critical patent/AU2007284562A1/en
Application granted granted Critical
Publication of AU2007284562B2 publication Critical patent/AU2007284562B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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)
  • 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)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
AU2007284562A 2006-08-16 2007-08-16 Using PI3K and MEK modulators in treatments of cancer Ceased AU2007284562B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US83830706P 2006-08-16 2006-08-16
US60/838,307 2006-08-16
PCT/US2007/018057 WO2008021389A2 (en) 2006-08-16 2007-08-16 Using pi3k and mek modulators in treatments of cancer

Publications (2)

Publication Number Publication Date
AU2007284562A1 AU2007284562A1 (en) 2008-02-21
AU2007284562B2 true AU2007284562B2 (en) 2013-05-02

Family

ID=38819883

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2007284562A Ceased AU2007284562B2 (en) 2006-08-16 2007-08-16 Using PI3K and MEK modulators in treatments of cancer

Country Status (8)

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

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0617162B8 (pt) * 2005-10-07 2021-05-25 Exelixis Inc compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos
HRP20110498T1 (hr) * 2005-10-07 2011-08-31 Exelixis Azetidini kao inhibitori mek za liječenje proliferativnih bolesti
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
CN101395155A (zh) * 2005-10-07 2009-03-25 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
CN101528231A (zh) 2006-08-16 2009-09-09 埃克塞利希斯股份有限公司 在癌症的治疗中使用pi3k和mek调控剂
DK2074122T5 (da) 2006-09-15 2014-03-17 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidin0n-forbindelser og anvendelse deraf som pi3 inhibitorer
WO2008076415A1 (en) 2006-12-14 2008-06-26 Exelixis, Inc. Methods of using mek inhibitors
NZ578229A (en) * 2007-02-22 2012-02-24 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
JP2010523670A (ja) 2007-04-10 2010-07-15 エクセリクシス， インク． Ｐｉ３ｋアルファのピリドピリミジノン阻害剤を使用した治療方法
EP2142543B8 (en) * 2007-04-11 2013-07-03 Exelixis, Inc. Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
BRPI0810208A2 (pt) * 2007-04-11 2014-10-21 Exelixis Inc Combinação de terapias compreendendo inibidores p13k-alpha à base de quinoxalina para uso no tratamento do câncer.
CN101711249A (zh) * 2007-04-11 2010-05-19 埃克塞里艾克西斯公司 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物
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
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
EP2370568B1 (en) 2008-12-10 2017-07-19 Dana-Farber Cancer Institute, Inc. Mek mutations conferring resistance to mek inhibitors
CA2772790C (en) 2009-09-04 2017-06-27 Benjamin Bader Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
MX2012003779A (es) * 2009-09-28 2012-06-01 Glaxosmithkline Llc Combinacion.
KR101489045B1 (ko) * 2009-10-12 2015-02-02 에프. 호프만-라 로슈 아게 Ｐｉ3ｋ 억제자 및 ｍｅｋ 억제자의 조합
UY33221A (es) * 2010-02-09 2011-09-30 Univ California MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA
EP3028699B1 (en) 2010-02-25 2018-03-21 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
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
US9845489B2 (en) 2010-07-26 2017-12-19 Biomatrica, Inc. Compositions for stabilizing DNA, RNA and proteins in saliva and other biological samples during shipping and storage at ambient temperatures
CA2806670A1 (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
EP2616442B8 (en) 2010-09-14 2018-10-17 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
DE102010048800A1 (de) 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
BR112013009643A2 (pt) * 2010-10-20 2016-07-19 Merck Serono S A Geneva método para preparar n-(3-amino-quinoxalin-2-il)-sulfonamidas substituídas e seus intermediários n-(3-cloo-quinoxalin-2-il)-sulfonamidas
WO2012065057A2 (en) * 2010-11-12 2012-05-18 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
CA2818544A1 (en) * 2010-11-19 2012-05-24 Glaxosmithkline Intellectual Property (No.2) Limited Method of treatment with 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
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
CN104302294A (zh) 2011-11-01 2015-01-21 埃克塞利希斯股份有限公司 用于治疗淋巴组织增生性恶性肿瘤的作为磷脂酰肌醇3-激酶抑制剂的n-(3-{[(3-{[2-氯-5-(甲氧基)苯基]氨基}喹喔啉-2-基)氨基]磺酰基}苯基)-2-甲基丙氨酰胺
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
ES2704744T3 (es) 2012-06-13 2019-03-19 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
MA38085B1 (fr) 2012-10-12 2018-11-30 Exelixis Inc Nouveau procédé pour la production de composés à utiliser dans le traitement du 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
US9725703B2 (en) 2012-12-20 2017-08-08 Biomatrica, Inc. Formulations and methods for stabilizing PCR reagents
WO2014144850A1 (en) 2013-03-15 2014-09-18 Genentech, Inc. Methods of treating cancer and preventing cancer drug resistance
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
RS56034B1 (sr) 2013-06-11 2017-09-29 Bayer Pharma AG Derivati prolekova supstituisanih triazolopiridina
CN105491883B (zh) 2013-06-13 2018-11-02 生物马特里卡公司 细胞稳定化
JP6752715B2 (ja) 2014-03-26 2020-09-09 アステックス、セラピューティックス、リミテッドＡｓｔｅｘ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｉｍｉｔｅｄ 組合せ
CN106572650B (zh) 2014-06-10 2021-08-31 生物马特里卡公司 在环境温度下稳定凝血细胞
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
TWI719960B (zh) 2015-02-10 2021-03-01 英商阿斯迪克治療公司 新穎組成物
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MX373169B (es) 2015-02-20 2020-04-24 Incyte Holdings Corp Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr).
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
SG11201804776SA (en) 2015-12-08 2018-07-30 Biomatrica Inc Reduction of erythrocyte sedimentation rate
WO2017205795A1 (en) 2016-05-26 2017-11-30 The Regents Of The University Of California Compounds and methods for hematopoietic regeneration
WO2018183936A1 (en) * 2017-03-31 2018-10-04 The Broad Institute, Inc. Compounds and methods useful for treating or preventing cancers
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
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019108800A1 (en) * 2017-11-29 2019-06-06 The Regents Of The University Of California Compounds and methods for hematopoietic regeneration
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
CR20200590A (es) 2018-05-04 2021-04-26 Incyte Corp Formas sólidas de un inhibidor de fgfr y procesos para prepararlas
ES2929406T3 (es) * 2018-05-21 2022-11-29 Nerviano Medical Sciences Srl Compuestos de piridonas heterocondensadas y su uso como inhibidores de IDH
MA55143A (fr) * 2018-11-20 2021-09-29 H Lee Moffitt Cancer Center & Res Institute Inc Composés aryl-aniline et hétéroaryl-aniline pour le traitement de cancers de la peau
US12466818B2 (en) 2018-11-20 2025-11-11 Nflection Therapeutics, Inc. Thienyl-aniline compounds for treatment of dermal disorders
CN113473986B (zh) 2018-11-20 2024-10-11 恩福莱克逊治疗有限公司 用于治疗皮肤疾病萘啶酮苯胺化合物
WO2020106307A1 (en) * 2018-11-20 2020-05-28 Nflection Therapeutics, Inc. Aryl-aniline and heteroaryl-aniline compounds for treatment of birthmarks
AU2019383311B2 (en) 2018-11-20 2024-12-05 Nflection Therapeutics, Inc. Cyanoaryl-aniline compounds for treatment of dermal disorders
WO2020185532A1 (en) 2019-03-08 2020-09-17 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
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之雙環雜環
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
ES3033669T3 (en) 2019-11-08 2025-08-06 Nerviano Medical Sciences Srl 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
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
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
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12447163B2 (en) * 2021-07-16 2025-10-21 Jazz Pharmaceuticals Therapeutics, Inc. Liposomal formulations of Bcl inhibitors
KR20240125577A (ko) 2021-11-23 2024-08-19 엔플렉션 테라퓨틱스, 인코포레이티드 피롤로피리딘-아닐린 화합물의 제형

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040009993A1 (en) * 2001-12-11 2004-01-15 Pharmacia Italia S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
WO2006045514A1 (en) * 2004-10-20 2006-05-04 Applied Research Systems Ars Holding N.V. 3-arylamino pyridine derivatives

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2301194T3 (es) 1997-02-05 2008-06-16 Warner-Lambert Company Llc Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular.
CA2290509A1 (en) * 1997-07-01 1999-01-14 Warner-Lambert Company 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as mek inhibitors
ATE373659T1 (de) * 2004-05-04 2007-10-15 Warner Lambert Co Pyrrolylsubstituierte pyrido(2,3-d)pyrimidin-7- one und derivate davon als therapeutische mittel
PE20060608A1 (es) * 2004-10-13 2006-08-22 Wyeth Corp Analogos de 17-hidroxiwortmanina como inhibidores de pi3k
AU2006283846B2 (en) 2005-08-26 2012-04-05 Merck Serono Sa Pyrazine derivatives and use as PI3K inhibitors
HRP20110498T1 (hr) * 2005-10-07 2011-08-31 Exelixis Azetidini kao inhibitori mek za liječenje proliferativnih bolesti
BRPI0617162B8 (pt) 2005-10-07 2021-05-25 Exelixis Inc compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos
US8247408B2 (en) * 2005-10-07 2012-08-21 Exelixis, Inc. Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer
CN101395155A (zh) 2005-10-07 2009-03-25 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
CN101528231A (zh) 2006-08-16 2009-09-09 埃克塞利希斯股份有限公司 在癌症的治疗中使用pi3k和mek调控剂
WO2008076415A1 (en) * 2006-12-14 2008-06-26 Exelixis, Inc. Methods of using mek inhibitors
JP2010523670A (ja) 2007-04-10 2010-07-15 エクセリクシス， インク． Ｐｉ３ｋアルファのピリドピリミジノン阻害剤を使用した治療方法
CN101711249A (zh) 2007-04-11 2010-05-19 埃克塞里艾克西斯公司 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物
EP2142543B8 (en) 2007-04-11 2013-07-03 Exelixis, Inc. Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
BRPI0810208A2 (pt) 2007-04-11 2014-10-21 Exelixis Inc Combinação de terapias compreendendo inibidores p13k-alpha à base de quinoxalina para uso no tratamento do câncer.
WO2010039740A1 (en) 2008-09-30 2010-04-08 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα AND MTOR
UY33221A (es) 2010-02-09 2011-09-30 Univ California MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040009993A1 (en) * 2001-12-11 2004-01-15 Pharmacia Italia S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
WO2006045514A1 (en) * 2004-10-20 2006-05-04 Applied Research Systems Ars Holding N.V. 3-arylamino pyridine derivatives

Also Published As

Publication number Publication date
EP2056829B1 (en) 2012-01-04
JP2010500994A (ja) 2010-01-14
HK1130438A1 (en) 2009-12-31
US20120302545A1 (en) 2012-11-29
EP2056829B9 (en) 2012-09-26
US8642584B2 (en) 2014-02-04
WO2008021389A8 (en) 2009-03-12
CN104784695A (zh) 2015-07-22
CA2658725A1 (en) 2008-02-21
ATE539752T1 (de) 2012-01-15
CN101528231A (zh) 2009-09-09
JP2017226702A (ja) 2017-12-28
US20100075947A1 (en) 2010-03-25
US20140100215A1 (en) 2014-04-10
AU2007284562A1 (en) 2008-02-21
JP2013151570A (ja) 2013-08-08
JP2016074743A (ja) 2016-05-12
WO2008021389A2 (en) 2008-02-21
WO2008021389A3 (en) 2008-07-17
JP2014122243A (ja) 2014-07-03
EP2056829A2 (en) 2009-05-13

Similar Documents

Publication Publication Date Title
AU2007284562B2 (en) Using PI3K and MEK modulators in treatments of cancer
AU2006302179C1 (en) N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
US10155765B2 (en) Carboxamide inhibitors of IRAK4 activity
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
RU2559895C2 (ru) Азотосодержащие производные гетероарилов
WO2009017838A2 (en) Combinations of jak-2 inhibitors and other agents
EA015937B1 (ru) Производные пиразина и их применение в качестве ингибиторов pi3k
JP2017536369A (ja) Ｉｒａｋインヒビターとしてのヘテロアリール化合物及びその使用
CN101827525A (zh) 激酶抑制剂化合物
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
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
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired