KR102219695B1 - 헤테로아릴 화합물 및 이의 용도 - Google Patents

헤테로아릴 화합물 및 이의 용도 Download PDF

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KR102219695B1
KR102219695B1 KR1020157029048A KR20157029048A KR102219695B1 KR 102219695 B1 KR102219695 B1 KR 102219695B1 KR 1020157029048 A KR1020157029048 A KR 1020157029048A KR 20157029048 A KR20157029048 A KR 20157029048A KR 102219695 B1 KR102219695 B1 KR 102219695B1
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KR20150131237A (ko
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로라 아쿨리안 다고스티노
로버트 티진 탐 스진
더창 뉴
조셉 존 맥도날드
정둥 주
하이보 류
호르모츠 마츠디야스니
러셀 씨. 피터
저스윈더 싱
매튜 바라크
알렉산더 그로스
마크 먼슨
대런 하비
앤드류 숄티
사친 마니아르
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셀젠 카르 엘엘씨
사노피
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Reproductive Health (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
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KR1020157029048A 2013-03-15 2014-03-14 헤테로아릴 화합물 및 이의 용도 Expired - Fee Related KR102219695B1 (ko)

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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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US (1) US9663524B2 (https=)
EP (1) EP2968337B1 (https=)
JP (1) JP6576325B2 (https=)
KR (1) KR102219695B1 (https=)
CN (2) CN105307657B (https=)
AU (1) AU2014228746B2 (https=)
BR (1) BR112015022191A8 (https=)
EA (1) EA036160B1 (https=)
MA (1) MA38393B1 (https=)
MX (1) MX374558B (https=)
PE (1) PE20151776A1 (https=)
SG (1) SG11201507478VA (https=)
WO (1) WO2014144737A1 (https=)

Families Citing this family (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
SG11201500125QA (en) 2012-07-11 2015-02-27 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
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
EP3943087A1 (en) 2013-03-15 2022-01-26 Celgene CAR LLC Heteroaryl compounds and uses thereof
US9321786B2 (en) 2013-03-15 2016-04-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CN105307657B (zh) 2013-03-15 2020-07-10 西建卡尔有限责任公司 杂芳基化合物和其用途
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
PH12016500676B1 (en) 2013-10-18 2022-07-20 Eisai R&D Man Co Ltd Pyrimidine fgfr4 inhibitors
TN2016000115A1 (en) 2013-10-25 2017-07-05 Novartis Ag Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors.
RS63405B1 (sr) 2013-10-25 2022-08-31 Blueprint Medicines Corp Inhibitori receptora faktora rasta fibroblasta
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
AU2015292818B2 (en) 2014-07-21 2020-01-16 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
US10457691B2 (en) 2014-07-21 2019-10-29 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
CA2955082A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (sik) inhibitors
JP6585167B2 (ja) 2014-10-03 2019-10-02 ノバルティス アーゲー Fgfr4阻害剤としての縮環二環式ピリジル誘導体の使用
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
US9580423B2 (en) 2015-02-20 2017-02-28 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
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
AU2016238436A1 (en) 2015-03-25 2017-08-17 Novartis Ag Formylated N-heterocyclic derivatives as FGFR4 inhibitors
KR102548229B1 (ko) 2015-04-14 2023-06-27 에자이 알앤드디 매니지먼트 가부시키가이샤 결정질 fgfr4 억제제 화합물 및 그의 용도
JP7372740B2 (ja) 2016-05-10 2023-11-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 細胞生存性及び/又は細胞増殖を低減するための薬物の組み合わせ
KR20180002053A (ko) * 2016-06-28 2018-01-05 한미약품 주식회사 신규한 헤테로시클릭 유도체 화합물 및 이의 용도
WO2018009544A1 (en) * 2016-07-05 2018-01-11 The Broad Institute, Inc. Bicyclic urea kinase inhibitors and uses thereof
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
SG11201903911UA (en) 2016-11-02 2019-05-30 Novartis Ag Combinations of fgfr4 inhibitors and bile acid sequestrants
AU2017378943B2 (en) * 2016-12-19 2020-06-18 Abbisko Therapeutics Co., Ltd. FGFR4 inhibitor, preparation method therefor and pharmaceutical use thereof
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
AU2018226771B2 (en) 2017-02-28 2023-11-23 Dana-Farber Cancer Institute, Inc. Uses of pyrimidopyrimidinones as SIK inhibitors
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
WO2019015593A1 (zh) * 2017-07-19 2019-01-24 江苏奥赛康药业股份有限公司 嘧啶并吡啶酮或者吡啶并吡啶酮类化合物及其应用
CN109384790B (zh) * 2017-08-08 2022-05-10 药捷安康(南京)科技股份有限公司 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
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
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
US12351576B2 (en) 2018-09-14 2025-07-08 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
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US20220185811A1 (en) * 2019-03-08 2022-06-16 Shouyao Holdings (beijing) Co., Ltd. Fgfr4 kinase inhibitor and preparation method therefor and use thereof
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
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 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
US11697648B2 (en) 2019-11-26 2023-07-11 Theravance Biopharma R&D Ip, Llc Fused pyrimidine pyridinone compounds as JAK inhibitors
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Fgfr阻害剤の誘導体
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic 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
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4317143A4 (en) * 2021-03-26 2025-01-15 Hangzhou Apeloa Medicine Research Institute Co., Ltd. BICYCLIC HETEROCYCLIC FGFR4 INHIBITOR, PHARMACEUTICAL COMPOSITION AND PREPARATION THEREOF AND USE THEREOF
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CA3220155A1 (en) 2021-06-09 2022-12-15 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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003512378A (ja) 1999-10-21 2003-04-02 エフ.ホフマン−ラ ロシュ アーゲー p38プロテインキナーゼのインヒビターとしてのヘテロアルキルアミノ置換二環式窒素複素環
JP2007500725A (ja) 2003-07-29 2007-01-18 アイアールエム・リミテッド・ライアビリティ・カンパニー プロテインキナーゼ阻害剤としての化合物および組成物
JP2009514947A (ja) 2005-11-08 2009-04-09 ハンミ ファーム. シーオー., エルティーディー. 多重阻害剤としてのキナゾリン誘導体及びその製造方法
JP2010514720A (ja) 2006-12-27 2010-05-06 サノフィ−アベンティス 新規な置換イソキノリン及びイソキノリノン誘導体

Family Cites Families (98)

* 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
US4650750A (en) 1982-02-01 1987-03-17 Giese Roger W Method of chemical analysis employing molecular release tag compounds
US5516931A (en) 1982-02-01 1996-05-14 Northeastern University Release tag compounds producing ketone signal groups
PL181893B1 (pl) * 1994-11-14 2001-10-31 Warner Lambert Co Zwiazki bedace pochodnymi pirymidyny i naftyrydyny oraz preparat farmaceutyczny zawierajacy je PL PL PL
GB9508535D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivative
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
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
TR200003429T2 (tr) 1998-05-26 2001-07-23 Warner-Lambert Company Hücresel çoğalma inhibitörleri olarak bisiklik pirimidinler ve bisiklik 3,4-dihidropirimidinler.
HK1041483B (zh) 1998-10-23 2004-12-24 霍夫曼-拉罗奇有限公司 雙環氮雜環
US7169778B2 (en) 1999-09-15 2007-01-30 Warner-Lambert Company Pteridinones as kinase inhibitors
CZ20021743A3 (cs) 1999-10-21 2002-08-14 F. Hoffmann-La Roche Ag Bicyklické dusíkové heterocykly substituované alkylaminoskupinou jako inhibitory P38 proteinkinázy
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
US7022711B2 (en) * 2000-08-04 2006-04-04 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)
US6506749B2 (en) 2000-08-31 2003-01-14 Syntex (U.S.A.) Llc 7-oxo-pyridopyrimidines (I)
CA2420286A1 (en) 2000-08-31 2002-03-07 F. Hoffmann-La Roche Ag 7-oxo pyridopyrimidines as inhibitors of a cellular proliferation
CA2420122A1 (en) 2000-08-31 2002-03-07 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
WO2003000657A1 (en) 2001-06-20 2003-01-03 Daiichi Pharmaceutical Co., Ltd. Diamine derivatives
US7196090B2 (en) 2002-07-25 2007-03-27 Warner-Lambert Company Kinase inhibitors
WO2004014869A2 (en) 2002-08-13 2004-02-19 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
US7112676B2 (en) 2002-11-04 2006-09-26 Hoffmann-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
US7098332B2 (en) * 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
ZA200504898B (en) 2002-12-20 2006-11-29 Pharmacia Corp Acyclic pyrazole compounds
WO2004063195A1 (en) 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
WO2004089955A1 (en) 2003-04-10 2004-10-21 F.Hoffmann-La Roche Ag Pyrimido compounds
JP2006523638A (ja) 2003-04-16 2006-10-19 エフ.ホフマン−ラ ロシュ アーゲー キナゾリン化合物
AU2004279427B2 (en) 2003-10-08 2008-07-03 Irm Llc Compounds and compositions as protein kinase inhibitors
EP1697420A2 (en) 2003-12-19 2006-09-06 Five Prime Therapeutics, Inc. Fibroblast growth factor receptors 1, 2, 3, and 4 as targets for therapeutic intervention
ATE481134T1 (de) 2004-01-21 2010-10-15 Univ Emory Zusammensetzungen und verwendung von tyrosinkinase-hemmern zur behandlung von pathogenen infektionen
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
JP2008510690A (ja) 2004-08-31 2008-04-10 エフ.ホフマン−ラ ロシュ アーゲー 3−フェニル−ジヒドロピリミド[4,5−d]ピリミジノンのアミド誘導体、これらの製造、及び医薬品としての使用
AU2005279337A1 (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
CA2577275A1 (en) 2004-08-31 2006-03-09 Astrazeneca Ab Quinazolinone derivatives and their use as b-raf inhibitors
WO2006038112A1 (en) 2004-10-01 2006-04-13 Warner-Lambert Company Llc Use of kinase inhibitors to promote neochondrogenesis
US20070054916A1 (en) * 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
US7767687B2 (en) 2004-12-13 2010-08-03 Biogen Idec Ma Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
US20060142312A1 (en) * 2004-12-23 2006-06-29 Pfizer Inc C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones
US7906522B2 (en) 2005-04-28 2011-03-15 Kyowa Hakko Kirin Co., Ltd 2-aminoquinazoline derivatives
EP1899344A1 (en) 2005-06-10 2008-03-19 Irm, Llc Compounds that maintain pluripotency of embryonic stem cells
WO2006137421A1 (ja) 2005-06-21 2006-12-28 Kyowa Hakko Kogyo Co., Ltd. 局所投与剤
EP2083081A1 (en) 2005-07-22 2009-07-29 Five Prime Therapeutics, Inc. Compositions and methods of treating disease with FGFR fusion proteins
CA2616517A1 (en) 2005-07-26 2007-02-01 Vertex Pharmaceuticals Incorporated Abl kinase inhibition
US7618982B2 (en) 2005-12-19 2009-11-17 Nerviano Medical Sciences S.R.L. Heteroarylpyrrolopyridinones active as kinase inhibitors
GEP20105074B (en) 2005-12-21 2010-09-10 Novartis Ag Pyrimidinyl aryl urea derivatives being fgf inhibitors
AU2006331765A1 (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
PL2027123T3 (pl) * 2006-05-11 2011-09-30 Irm Llc Związki i kompozycje jako inhibitory kinaz białkowych
MX2008014618A (es) 2006-05-15 2008-11-28 Irm Llc Composiciones y metodos para inhibidores de cinasas del receptor fgf.
WO2008047307A1 (en) 2006-10-16 2008-04-24 Gpc Biotech Inc. Pyrido [2, 3-d] pyrimidines and their use as kinase inhibitors
EP1914234A1 (en) 2006-10-16 2008-04-23 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
US8129659B2 (en) 2006-10-20 2012-03-06 Swagelok Company Apparatus having DC arc start in parallel with welder power supply
WO2008055842A1 (en) 2006-11-09 2008-05-15 F. Hoffmann-La 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
HRP20150642T1 (hr) 2006-12-22 2015-08-14 Astex Therapeutics Limited BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a
RU2468011C2 (ru) * 2006-12-27 2012-11-27 Санофи-Авентис Замещенные циклоалкиламином производные изохинолина и изохинолинона
JP5129812B2 (ja) 2007-06-15 2013-01-30 Msd株式会社 ビシクロアニリン誘導体
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
CN102015660A (zh) 2008-04-23 2011-04-13 协和发酵麒麟株式会社 2-氨基喹唑啉衍生物
ES2554513T3 (es) * 2008-05-23 2015-12-21 Novartis Ag Derivados de quinolinas y quinoxalinas como inhibidores de la proteína tirosina quinasa
US20100121052A1 (en) 2008-06-20 2010-05-13 Rama Jain Novel compounds for treating proliferative diseases
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
JP2012501654A (ja) * 2008-09-05 2012-01-26 アビラ セラピューティクス, インコーポレイテッド 不可逆的インヒビターの設計のためのアルゴリズム
AU2009325398A1 (en) 2008-12-12 2010-06-17 Msd K.K. Dihydropyrimidopyrimidine derivative
AU2009325400A1 (en) 2008-12-12 2010-06-17 Msd K.K. Dihydropyrimidopyrimidine derivatives
EP3828185B1 (en) * 2009-01-06 2024-11-20 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
US9556426B2 (en) * 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
UA109888C2 (uk) 2009-12-07 2015-10-26 ІЗОЛЬОВАНЕ АНТИТІЛО АБО ЙОГО ФРАГМЕНТ, ЩО ЗВ'ЯЗУЄТЬСЯ З β-КЛОТО, РЕЦЕПТОРАМИ FGF І ЇХНІМИ КОМПЛЕКСАМИ
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
WO2011075620A1 (en) 2009-12-18 2011-06-23 Novartis Ag Method for treating haematological cancers
GB201007286D0 (en) * 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
CA2829558A1 (en) * 2011-03-09 2012-09-13 Celgene Avilomics Research, Inc. Pi3 kinase inhibitors and uses thereof
CA2828890A1 (en) * 2011-04-07 2012-10-11 Genentech, Inc. Anti-fgfr4 antibodies and methods of use
ES2770550T3 (es) 2011-05-17 2020-07-02 Univ California Inhibidores de quinasa
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
JP2015501786A (ja) 2011-11-04 2015-01-19 アフラクシス・ホールディングス・インコーポレイテッドAfraxis Holdings,Inc. 脆弱x症候群を治療するためのpak阻害剤
SI3366293T1 (sl) 2012-06-07 2020-08-31 Deciphera Pharmaceuticals, Llc Dihidronafthiridini in sorodne spojine uporabne kot kinazni inhibitorji za zdravljenje proliferativnih bolezni
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
SG11201500125QA (en) 2012-07-11 2015-02-27 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
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
CN105307657B (zh) 2013-03-15 2020-07-10 西建卡尔有限责任公司 杂芳基化合物和其用途
WO2014160521A1 (en) 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
US9321786B2 (en) 2013-03-15 2016-04-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US9783504B2 (en) 2013-07-09 2017-10-10 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
EP3027654B1 (en) 2013-07-30 2019-09-25 Blueprint Medicines Corporation Pik3c2g fusions
EP3628749A1 (en) 2013-07-30 2020-04-01 Blueprint Medicines Corporation Ntrk2 fusions
SI3057969T1 (sl) 2013-10-17 2018-10-30 Blueprint Medicines Corporation Sestavki, uporabni za zdravljenje motenj, povezanih s KIT
WO2015058129A1 (en) 2013-10-17 2015-04-23 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
PH12016500676B1 (en) 2013-10-18 2022-07-20 Eisai R&D Man Co Ltd Pyrimidine fgfr4 inhibitors
RS63405B1 (sr) 2013-10-25 2022-08-31 Blueprint Medicines Corp Inhibitori receptora faktora rasta fibroblasta
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003512378A (ja) 1999-10-21 2003-04-02 エフ.ホフマン−ラ ロシュ アーゲー p38プロテインキナーゼのインヒビターとしてのヘテロアルキルアミノ置換二環式窒素複素環
JP2007500725A (ja) 2003-07-29 2007-01-18 アイアールエム・リミテッド・ライアビリティ・カンパニー プロテインキナーゼ阻害剤としての化合物および組成物
JP2009514947A (ja) 2005-11-08 2009-04-09 ハンミ ファーム. シーオー., エルティーディー. 多重阻害剤としてのキナゾリン誘導体及びその製造方法
JP2010514720A (ja) 2006-12-27 2010-05-06 サノフィ−アベンティス 新規な置換イソキノリン及びイソキノリノン誘導体

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US9663524B2 (en) 2017-05-30
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