JP6576325B2 - ヘテロアリール化合物およびそれらの使用 - Google Patents

ヘテロアリール化合物およびそれらの使用 Download PDF

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Publication number
JP6576325B2
JP6576325B2 JP2016503031A JP2016503031A JP6576325B2 JP 6576325 B2 JP6576325 B2 JP 6576325B2 JP 2016503031 A JP2016503031 A JP 2016503031A JP 2016503031 A JP2016503031 A JP 2016503031A JP 6576325 B2 JP6576325 B2 JP 6576325B2
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compound
pharmaceutically acceptable
acceptable salt
ring
substituted
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JP2016519673A5 (enExample
JP2016519673A (ja
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ローラ アクリアン ディーアゴスティーノ，
ローラ アクリアン ディーアゴスティーノ，
ロバート ジン タム シン，
ロバート ジン タム シン，
デチャン ニウ，
デチャン ニウ，
ジョセフ ジョン マクドナルド，
ジョセフ ジョン マクドナルド，
ゼンドン ズー，
ゼンドン ズー，
ハイボウ リウ，
ハイボウ リウ，
ホルモズ マズディヤスニ，
ホルモズ マズディヤスニ，
ラッセル シー． ペター，
ラッセル シー． ペター，
ジャスウィンダー シン，
ジャスウィンダー シン，
マシュー バラーグ，
マシュー バラーグ，
グロス，　アレクサンダー
アレクサンダー グロス，
マーク ムンソン，
マーク ムンソン，
ダレン ハービー，
ダレン ハービー，
アンドリュー ショルト，
アンドリュー ショルト，
サチン マニアー，
サチン マニアー，
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Sanofi SA
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Sanofi SA
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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2016503031A 2013-03-15 2014-03-14 ヘテロアリール化合物およびそれらの使用 Expired - Fee Related JP6576325B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361793113P 2013-03-15 2013-03-15
US61/793,113 2013-03-15
EP14305361.9 2014-03-13
EP14305361 2014-03-13
PCT/US2014/029270 WO2014144737A1 (en) 2013-03-15 2014-03-14 Heteroaryl compounds and uses thereof

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JP2016519673A JP2016519673A (ja) 2016-07-07
JP2016519673A5 JP2016519673A5 (enExample) 2017-04-20
JP6576325B2 true JP6576325B2 (ja) 2019-09-18

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US (1) US9663524B2 (enExample)
EP (1) EP2968337B1 (enExample)
JP (1) JP6576325B2 (enExample)
KR (1) KR102219695B1 (enExample)
CN (2) CN111793068A (enExample)
AU (1) AU2014228746B2 (enExample)
BR (1) BR112015022191A8 (enExample)
EA (1) EA036160B1 (enExample)
MA (1) MA38393B1 (enExample)
MX (1) MX374558B (enExample)
PE (1) PE20151776A1 (enExample)
SG (1) SG11201507478VA (enExample)
WO (1) WO2014144737A1 (enExample)

Families Citing this family (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
SI2861595T1 (sl) 2012-06-13 2017-04-26 Incyte Holdings Corporation Substituirane triciklične spojine kot inhibitorji fgfr
SMT202100451T1 (it) 2012-07-11 2021-09-14 Blueprint Medicines Corp Inibitori del recettore di crescita dei fibroblasti
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
UA120248C2 (uk) 2013-03-15 2019-11-11 Селджен Кар Ллс Гетероарильні сполуки та їх застосування
US9663524B2 (en) 2013-03-15 2017-05-30 Celgene Car Llc Substituted pyrido[2,3-d]pyrimidines as protein kinase inhibitors
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
CA2924206C (en) * 2013-10-18 2022-10-25 Eisai R&D Management Co., Ltd. Pyrimidine fgfr4 inhibitors
AU2014339972B9 (en) 2013-10-25 2019-05-30 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
EP3060563B1 (en) 2013-10-25 2018-05-02 Novartis AG Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
EP3172213B1 (en) 2014-07-21 2021-09-22 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
WO2016014542A1 (en) 2014-07-21 2016-01-28 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
EP3177295A4 (en) 2014-08-08 2018-06-13 Dana Farber Cancer Institute, Inc. Uses of salt-inducible kinase (sik) inhibitors
PL3200786T3 (pl) 2014-10-03 2020-03-31 Novartis Ag Zastosowanie pochodnych pirydylowych o skondensowanym układzie bicyklicznym jako inhibitorów fgfr4
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
SG10201913036RA (en) 2015-02-20 2020-02-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
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
US9802917B2 (en) 2015-03-25 2017-10-31 Novartis Ag Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide
RU2017134379A (ru) 2015-03-25 2019-04-03 Новартис Аг Формилированные n-гетероциклические производные в качестве ингибиторов fgfr4
EP3283465B1 (en) 2015-04-14 2021-01-06 Eisai R&D Management Co., Ltd. Crystalline fgfr4 inhibitor compound and uses thereof
WO2017196854A1 (en) 2016-05-10 2017-11-16 Eisai R&D Management Co., Ltd. Drug combinations for reducing cell viability and/or cell proliferation
KR20180002053A (ko) * 2016-06-28 2018-01-05 한미약품 주식회사 신규한 헤테로시클릭 유도체 화합물 및 이의 용도
KR20190075043A (ko) * 2016-07-05 2019-06-28 더 브로드 인스티튜트, 인코퍼레이티드 비시클릭 우레아 키나제 억제제 및 그의 용도
US11241435B2 (en) 2016-09-16 2022-02-08 The General Hospital Corporation Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis
WO2018055503A1 (en) 2016-09-20 2018-03-29 Novartis Ag Combination comprising a pd-1 antagonist and an fgfr4 inhibitor
PT3534902T (pt) 2016-11-02 2022-12-07 Novartis Ag Combinações de inibidores de fgfr4 e quelantes de ácidos biliares
RU2747260C2 (ru) * 2016-12-19 2021-04-29 Аббиско Тхерапеутицс Цо., Лтд. Ингибитор рфрф4, способ его получения и его фармацевтическое применение
RU2019129727A (ru) 2017-02-28 2021-03-30 Зэ Дженерал Хоспитал Корпорэйшн Применения пиримидопиримидинонов в качестве ингибиторов sik
CN108503593B (zh) * 2017-02-28 2021-04-27 暨南大学 2-氨基嘧啶类化合物及其应用
WO2018213219A1 (en) * 2017-05-15 2018-11-22 University Of Houston System Pyrido[2,3-d]pyrimidin-7ones and related compounds as inhibitors of protein kinases
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN110914267B (zh) * 2017-07-19 2022-07-12 江苏奥赛康药业有限公司 嘧啶并吡啶酮或者吡啶并吡啶酮类化合物及其应用
WO2019029541A1 (zh) * 2017-08-08 2019-02-14 南京药捷安康生物科技有限公司 成纤维细胞生长因子受体抑制剂及其用途
CN109745325B (zh) * 2017-11-08 2022-02-15 上海翰森生物医药科技有限公司 Fgfr4抑制剂、其制备方法和用途
CN110386921A (zh) * 2018-04-23 2019-10-29 南京药捷安康生物科技有限公司 成纤维细胞生长因子受体抑制剂化合物
KR20210018264A (ko) 2018-05-04 2021-02-17 인사이트 코포레이션 Fgfr 억제제의 염
PL3788047T3 (pl) 2018-05-04 2025-04-14 Incyte Corporation Stałe postacie inhibitora fgfr i sposoby ich otrzymywania
CN111868058B (zh) * 2018-05-25 2023-06-13 上海和誉生物医药科技有限公司 一种fgfr抑制剂、其制备方法和在药学上的应用
CN110577524B (zh) * 2018-06-07 2022-01-28 北京大学深圳研究生院 一种激酶选择性抑制剂
WO2019242587A1 (zh) * 2018-06-19 2019-12-26 上海和誉生物医药科技有限公司 一种高选择性FGFR i抑制剂及其制备方法和应用
CA3103335C (en) 2018-09-14 2023-10-03 Abbisko Therapeutics Co., Ltd. Fgfr inhibitor, preparation method therefor and application thereof
WO2020140054A1 (en) 2018-12-28 2020-07-02 Spv Therapeutics Inc. Cyclin-dependent kinase inhibitors
WO2020177067A1 (en) 2019-03-05 2020-09-10 Bioardis Llc Aromatic derivatives, preparation methods, and medical uses thereof
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
JP7378488B2 (ja) * 2019-03-08 2023-11-13 ショウヤオ ホールディングス（ベイジン） カンパニー， リミテッド Ｆｇｆｒ４キナーゼ阻害剤、その製造方法及び用途
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
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
KR102333854B1 (ko) 2019-10-24 2021-12-06 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 신규한 피리디닐트리아진 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물
GB201915828D0 (en) * 2019-10-31 2019-12-18 Cancer Research Tech Ltd Compounds, compositions and therapeutic uses thereof
CN114901659A (zh) 2019-11-26 2022-08-12 施万生物制药研发Ip有限责任公司 作为jak抑制剂的稠合嘧啶吡啶酮化合物
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR102382613B1 (ko) * 2020-01-15 2022-04-06 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 7-아미노-3,4-디히드로피리미도피리미딘-2-온 유도체 및 이를 포함하는 치료용 약학 조성물
KR20230160375A (ko) * 2021-03-26 2023-11-23 항저우 아펠로아 메디슨 리서치 인스티튜트 씨오.,엘티디. 이중환 헤테로고리 fgfr4 억제제, 이를 포함한 약물 조성물 및 제제 또한 그의 적용
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
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN113527311B (zh) * 2021-08-23 2022-05-06 中南大学湘雅医院 Fgfr4抑制剂、组合物及其在药物制备中的用途
WO2023039828A1 (en) * 2021-09-17 2023-03-23 Nutshell Biotech (Shanghai) Co., Ltd. Fused ring compounds as inhibitors of fgfr4 tyrosine kinases
CN113912602B (zh) * 2021-10-14 2023-05-05 温州医科大学 一种2-氧代-1,2-二氢-1,6-萘啶-7-基类化合物及其制备方法和用途
WO2024199388A1 (zh) * 2023-03-29 2024-10-03 微境生物医药科技(上海)有限公司 作为myt1抑制剂的化合物
EP4509142A1 (en) 2023-08-16 2025-02-19 Ona Therapeutics S.L. Fgfr4 as target in cancer treatment
CN120775123A (zh) * 2025-09-12 2025-10-14 怀化市恒渝新材料有限公司 一种光引发剂制备方法、光引发剂及其应用

Family Cites Families (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
US4709016A (en) 1982-02-01 1987-11-24 Northeastern University Molecular analytical release tags and their use in chemical analysis
US5516931A (en) 1982-02-01 1996-05-14 Northeastern University Release tag compounds producing ketone signal groups
US4650750A (en) 1982-02-01 1987-03-17 Giese Roger W Method of chemical analysis employing molecular release tag compounds
TJ342B (en) * 1994-11-14 2002-10-06 Warner Lambert Co Derivatives of 6-aryl pyrido Ä2,3-dÜ pyrimidines and naphthyridines pharmaceutical composition possess inhibiting effect of cellular proliferation pr ovoking protein tyrosine kinase and method of inhibiting cellular proliferation
GB9508535D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivative
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
DE19802377A1 (de) 1998-01-22 1999-08-19 Max Planck Gesellschaft Verwendung von Inhibitoren für die Behandlung von RTK-Überfunktions-bedingten Störungen, insbesondere von Krebs
SK17532000A3 (sk) 1998-05-26 2002-08-06 Warner-Lambert Company Prípadne substituované 3,4-dihydrogenované pyrimidíny, ich použitie a farmaceutické formulácie na ich báze
CZ20011394A3 (cs) 1998-10-23 2001-12-12 F. Hoffmann-La Roche Ag Derivát bicyklických, dusík obsahujících heterocyklických sloučenin, způsob jeho přípravy a farmaceutický prostředek, který ho obsahuje
CA2393896A1 (en) 1999-09-15 2001-03-22 Warner-Lambert Company Pteridinones as kinase inhibitors
CZ20021744A3 (cs) 1999-10-21 2002-08-14 F. Hoffmann-La Roche Ag Bicyklické dusíkové heterocykly substituované heteroalkylaminoskupinou jako inhibitory P38 proteinkinázy
BR0014973A (pt) 1999-10-21 2002-07-16 Hoffmann La Roche Ag G Heterociclos de nitrogênio bicìclico de alquilamino substituìdo como inibidores de proteìna quinase p38
AR030053A1 (es) 2000-03-02 2003-08-13 Smithkline Beecham Corp 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas
AU2001277032A1 (en) * 2000-08-04 2002-02-18 Warner Lambert Company 2-(4-pyridyl)amino-6-dialkoxyphenyl-pyrido(2,3-d)pyrimidin-7 ones
US6518276B2 (en) 2000-08-31 2003-02-11 Syntex (U.S.A.) Llc 7-oxo-pyridopyrimidines (II)
EP1315726A1 (en) 2000-08-31 2003-06-04 F. Hoffmann-La Roche Ag 7- oxo pyridopyrimidines as inhibitors of cellular proliferation
US6506749B2 (en) 2000-08-31 2003-01-14 Syntex (U.S.A.) Llc 7-oxo-pyridopyrimidines (I)
EP1315727B1 (en) 2000-08-31 2005-06-29 F. Hoffmann-La Roche Ag 7-oxo pyridopyrimidines
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
US7365205B2 (en) 2001-06-20 2008-04-29 Daiichi Sankyo Company, Limited Diamine derivatives
US7196090B2 (en) 2002-07-25 2007-03-27 Warner-Lambert Company Kinase inhibitors
AU2003250475A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc 5,6-fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
US7084270B2 (en) 2002-08-14 2006-08-01 Hoffman-La Roche Inc. Pyrimido compounds having antiproliferative activity
TW200413381A (en) 2002-11-04 2004-08-01 Hoffmann La Roche Novel amino-substituted dihydropyrimido [4,5-d]pyrimidinone derivatives, their manufacture and use as pharmaceutical agents
US7112676B2 (en) 2002-11-04 2006-09-26 Hoffmann-La Roche Inc. Pyrimido compounds having antiproliferative activity
US7098332B2 (en) * 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
CA2510298A1 (en) 2002-12-20 2004-07-15 Pharmacia Corporation Acyclic pyrazole compounds
US20050009849A1 (en) 2003-01-03 2005-01-13 Veach Darren R. Pyridopyrimidine kinase inhibitors
KR100864393B1 (ko) * 2003-04-10 2008-10-20 에프. 호프만-라 로슈 아게 피리미도 화합물
MXPA05011103A (es) 2003-04-16 2005-12-12 Hoffmann La Roche Compuestos de quinazolina.
AU2004260689B8 (en) * 2003-07-29 2008-05-15 Irm Llc Compounds and compositions as protein kinase inhibitors
MXPA06003996A (es) 2003-10-08 2006-07-05 Irm Llc Compuestos y composiciones como inhibidores de la proteina cinasa.
CA2550245A1 (en) 2003-12-19 2005-07-21 Five Prime Therapeutics, Inc. Fibroblast growth factor receptors 1, 2, 3, and 4 as targets for therapeutic intervention
JP5520433B2 (ja) 2004-01-21 2014-06-11 エモリー ユニバーシティー 病原体感染を処置するためのチロシンキナーゼインヒビターの組成物および使用
WO2005105097A2 (en) 2004-04-28 2005-11-10 Gpc Biotech Ag Pyridopyrimidines for treating inflammatory and other diseases
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
BRPI0514691A (pt) 2004-08-31 2008-06-17 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, processo para preparar o mesmo, composição farmacêutica, e, uso de um composto ou um sal farmaceuticamente aceitável do mesmo
KR100853975B1 (ko) 2004-08-31 2008-08-25 에프. 호프만-라 로슈 아게 3-페닐 디히드로피리미도[4,5-ｄ]피리미디논의 아미드유도체, 이의 제조 방법 및 약제로서의 용도
CA2576924A1 (en) 2004-08-31 2006-03-09 F. Hoffmann-La Roche Ag Amide derivatives of 7-amino-3-phenyl-dihydropyrimido [4,5-d]pyrimidinones, their manufacture and use as pharmaceutical agents
US20070054916A1 (en) * 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
WO2006038112A1 (en) 2004-10-01 2006-04-13 Warner-Lambert Company Llc Use of kinase inhibitors to promote neochondrogenesis
JP5111113B2 (ja) 2004-12-13 2012-12-26 サネシス ファーマシューティカルズ， インコーポレイテッド Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン
US20060142312A1 (en) * 2004-12-23 2006-06-29 Pfizer Inc C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones
JP5079500B2 (ja) 2005-04-28 2012-11-21 協和発酵キリン株式会社 ２−アミノキナゾリン誘導体
BRPI0611733A2 (pt) 2005-06-10 2010-09-28 Irm Llc compostos que mantêm pluripotência de células-tronco embriÈnicas
WO2006137421A1 (ja) 2005-06-21 2006-12-28 Kyowa Hakko Kogyo Co., Ltd. 局所投与剤
EP1910542B1 (en) 2005-07-22 2009-12-02 Five Prime Therapeutics, Inc. Compositions and methods of treating disease with fgfr fusion proteins
US20090298844A1 (en) 2005-07-26 2009-12-03 John Pollard Abl kinase inhibition
KR100832593B1 (ko) * 2005-11-08 2008-05-27 한미약품 주식회사 신호전달 저해제로서의 퀴나졸린 유도체 및 이의 제조방법
US7618982B2 (en) 2005-12-19 2009-11-17 Nerviano Medical Sciences S.R.L. Heteroarylpyrrolopyridinones active as kinase inhibitors
MEP3808A (xx) 2005-12-21 2010-02-10 Novartis Ag Derivati pirimidinil aril uree kao fgf inhibitori
CA2631777A1 (en) 2005-12-22 2007-07-05 Wyeth Substituted isoquinoline-1,3(2h,4h)-diones, 1-thioxo-1,4-dihydro-2h-isoquinoline-3-ones and 1,4-dihydro-3(2h)-isoquinolones and use thereof as kinase inhibitor
CA2649102A1 (en) * 2006-05-11 2007-11-22 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2007136465A2 (en) 2006-05-15 2007-11-29 Irm Llc Compositions and methods for fgf receptor kinases inhibitors
EP1914234A1 (en) 2006-10-16 2008-04-23 GPC Biotech Inc. Pyrido[2,3-d]pyrimidines and their use as kinase inhibitors
CA2665384A1 (en) 2006-10-16 2008-04-24 Gpc Biotech Inc. Pyrido [2, 3-d] pyrimidines and their use as kinase inhibitors
WO2008150260A1 (en) 2007-06-06 2008-12-11 Gpc Biotech, Inc. 8-oxy-2-aminopyrido (2, 3-d) pyrimidin-7-one derivatives as kinase inhibitors and anticancer agents
WO2008051820A2 (en) 2006-10-20 2008-05-02 Swagelok Company Dc arc start with universal input
EP2094698A1 (en) 2006-11-09 2009-09-02 F. Hoffmann-Roche AG Substituted 6-phenyl-pyrido [2,3-d]pyrimidin-7-one derivatives as kinase inhibitors and methods for using the same
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
AU2007337886C1 (en) 2006-12-22 2014-10-16 Astex Therapeutics Limited Bicyclic heterocyclic compounds as FGFR inhibitors
ATE490243T1 (de) * 2006-12-27 2010-12-15 Sanofi Aventis Cycloalkylaminsubstituierte isochinolin- und isochinolinonderivate
CA2673921C (en) * 2006-12-27 2015-10-20 Sanofi-Aventis New substituted isoquinoline and isoquinolinone derivatives
EP2168966B1 (en) 2007-06-15 2016-09-28 Msd K.K. Bicycloaniline derivative
GB0720038D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
US8216783B2 (en) 2008-04-14 2012-07-10 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Over-expression and mutation of a tyrosine kinase receptor FGFR4 in tumors
EP2112150B1 (en) 2008-04-22 2013-10-16 Forma Therapeutics, Inc. Improved raf inhibitors
EP2269993B1 (en) 2008-04-23 2013-02-27 Kyowa Hakko Kirin Co., Ltd. 2-aminoquinazoline derivative
EP2282995B1 (en) * 2008-05-23 2015-08-26 Novartis AG Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
US20100121052A1 (en) 2008-06-20 2010-05-13 Rama Jain Novel compounds for treating proliferative diseases
NZ589843A (en) 2008-06-27 2012-12-21 Avila Therapeutics Inc Pyrimidine heteroaryl compounds and uses thereof as protein kinase inhibitors
CN105574346A (zh) 2008-09-05 2016-05-11 新基阿维罗米克斯研究公司 多肽偶联物与不可逆抑制剂的设计方法和检测方法
WO2010067888A1 (en) 2008-12-12 2010-06-17 Banyu Pharmaceutical Co.,Ltd. Dihydropyrimidopyrimidine derivatives
AU2009325398A1 (en) 2008-12-12 2010-06-17 Msd K.K. Dihydropyrimidopyrimidine derivative
EP2379559B1 (en) 2009-01-06 2017-10-25 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
NZ598705A (en) * 2009-09-16 2014-06-27 Celgene Avilomics Res Inc Protein kinase conjugates and inhibitors
AR079257A1 (es) 2009-12-07 2012-01-04 Novartis Ag Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas
UA109888C2 (uk) 2009-12-07 2015-10-26 ІЗОЛЬОВАНЕ АНТИТІЛО АБО ЙОГО ФРАГМЕНТ, ЩО ЗВ'ЯЗУЄТЬСЯ З β-КЛОТО, РЕЦЕПТОРАМИ FGF І ЇХНІМИ КОМПЛЕКСАМИ
JP2013514986A (ja) 2009-12-18 2013-05-02 ノバルティス アーゲー 血液癌の処置方法
GB201007286D0 (en) * 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
CN103501610A (zh) 2011-03-09 2014-01-08 西建阿维拉米斯研究公司 Pi3激酶抑制剂和其用途
WO2012138975A1 (en) * 2011-04-07 2012-10-11 Genentech, Inc. Anti-fgfr4 antibodies and methods of use
BR112013029508B1 (pt) 2011-05-17 2022-05-03 Principia Biopharma, Inc. Composto, composição farmacêutica, e, uso do referido composto
CN102887895B (zh) 2011-07-22 2016-08-24 山东轩竹医药科技有限公司 吡啶并嘧啶类mTOR抑制剂
BR112014010631A2 (pt) 2011-11-04 2017-04-25 Afraxis Holdings Inc inibidores de pak para o tratamento da síndrome do x frágil
KR101652229B1 (ko) 2012-06-07 2016-08-30 데시페라 파마슈티칼스, 엘엘씨. 증식성 질환의 치료를 위한 키나제 저해제로서 유용한 다이하이드로나프타이리딘 및 관련 화합물
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
SMT202100451T1 (it) 2012-07-11 2021-09-14 Blueprint Medicines Corp Inibitori del recettore di crescita dei fibroblasti
TWI629266B (zh) 2012-12-28 2018-07-11 藍印藥品公司 纖維母細胞生長因子受體之抑制劑
US9663524B2 (en) 2013-03-15 2017-05-30 Celgene Car Llc Substituted pyrido[2,3-d]pyrimidines as protein kinase inhibitors
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
CA2917667A1 (en) 2013-07-09 2015-01-15 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
EP3628749A1 (en) 2013-07-30 2020-04-01 Blueprint Medicines Corporation Ntrk2 fusions
EP3027654B1 (en) 2013-07-30 2019-09-25 Blueprint Medicines Corporation Pik3c2g fusions
BR112016008541B1 (pt) 2013-10-17 2022-11-22 Blueprint Medicines Corporation Composto ou sal farmaceuticamente aceitável, uso do mesmo para tratar mastocistose, tumor do estroma gastrointestinal e leucemia, e composição farmacêutica
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
CA2924206C (en) 2013-10-18 2022-10-25 Eisai R&D Management Co., Ltd. Pyrimidine fgfr4 inhibitors
AU2014339972B9 (en) 2013-10-25 2019-05-30 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors

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