TWI602814B - 透過抑制fgfr激酶之具有抗癌性的吡啶並吡嗪衍生物化合物 - Google Patents

透過抑制fgfr激酶之具有抗癌性的吡啶並吡嗪衍生物化合物 Download PDF

Info

Publication number
TWI602814B
TWI602814B TW101139220A TW101139220A TWI602814B TW I602814 B TWI602814 B TW I602814B TW 101139220 A TW101139220 A TW 101139220A TW 101139220 A TW101139220 A TW 101139220A TW I602814 B TWI602814 B TW I602814B
Authority
TW
Taiwan
Prior art keywords
alkyl
substituted
group
compound
hydroxy
Prior art date
Application number
TW101139220A
Other languages
English (en)
Chinese (zh)
Other versions
TW201333004A (zh
Inventor
派瑞克 芮妮 安吉波特
奧立弗 亞歷克西斯 喬治 圭羅
維吉尼 蘇菲 龐斯列
布魯諾 羅斯
列文 蜜爾波爾
戈登 沙克斯緹
瓦雷里歐 波帝尼
Original Assignee
阿斯迪克治療公司
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 阿斯迪克治療公司 filed Critical 阿斯迪克治療公司
Publication of TW201333004A publication Critical patent/TW201333004A/zh
Application granted granted Critical
Publication of TWI602814B publication Critical patent/TWI602814B/zh

Links

Classifications

    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW101139220A 2011-10-28 2012-10-24 透過抑制fgfr激酶之具有抗癌性的吡啶並吡嗪衍生物化合物 TWI602814B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161552888P 2011-10-28 2011-10-28
GBGB1118656.6A GB201118656D0 (en) 2011-10-28 2011-10-28 New compounds

Publications (2)

Publication Number Publication Date
TW201333004A TW201333004A (zh) 2013-08-16
TWI602814B true TWI602814B (zh) 2017-10-21

Family

ID=45373584

Family Applications (1)

Application Number Title Priority Date Filing Date
TW101139220A TWI602814B (zh) 2011-10-28 2012-10-24 透過抑制fgfr激酶之具有抗癌性的吡啶並吡嗪衍生物化合物

Country Status (33)

Country Link
US (2) US9309242B2 (enExample)
EP (1) EP2776435B1 (enExample)
JP (1) JP6169583B2 (enExample)
KR (1) KR102066496B1 (enExample)
CN (1) CN104011051B (enExample)
AP (1) AP4060A (enExample)
AR (1) AR088567A1 (enExample)
AU (1) AU2012328170B2 (enExample)
BR (1) BR112014010206B8 (enExample)
CA (1) CA2853390C (enExample)
CL (1) CL2014001065A1 (enExample)
CO (1) CO6940422A2 (enExample)
CR (1) CR20140190A (enExample)
DK (1) DK2776435T3 (enExample)
EA (1) EA027563B1 (enExample)
EC (1) ECSP14013325A (enExample)
ES (1) ES2688868T3 (enExample)
GB (1) GB201118656D0 (enExample)
HR (1) HRP20181533T1 (enExample)
IL (1) IL232083B (enExample)
IN (1) IN2014MN00948A (enExample)
JO (1) JO3419B1 (enExample)
LT (1) LT2776435T (enExample)
MX (1) MX353654B (enExample)
MY (1) MY185666A (enExample)
NI (1) NI201400032A (enExample)
PH (1) PH12014500867A1 (enExample)
SG (1) SG11201401055XA (enExample)
SI (1) SI2776435T1 (enExample)
TW (1) TWI602814B (enExample)
UA (1) UA111386C2 (enExample)
UY (1) UY34418A (enExample)
WO (1) WO2013061080A1 (enExample)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
MX367723B (es) * 2013-10-25 2019-09-03 Novartis Ag Compuestos de anillos fusionados bicíclicos derivados de piridilo como inhibidores de fgfr4.
AR098145A1 (es) * 2013-10-25 2016-05-04 Novartis Ag Compuestos derivados de piridilo bicíclicos fusionados como inhibidores de fgfr4
KR102479696B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 Fgfr 억제제 및 igf1r 억제제의 조합물
MX370099B (es) 2014-03-26 2019-12-02 Astex Therapeutics Ltd Combinación que comprende un inhibidor de fgfr y un inhibidor de cmet para el tratamiento del cáncer.
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
ES2914072T3 (es) 2014-08-18 2022-06-07 Eisai R&D Man Co Ltd Sal de derivado de piridina monocíclico y su cristal
EP3200786B1 (en) 2014-10-03 2019-08-28 Novartis AG Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
TWI695837B (zh) 2014-12-04 2020-06-11 比利時商健生藥品公司 作為激酶調節劑之三唑並嗒
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
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
EP3275442B1 (en) 2015-03-25 2021-07-28 National Cancer Center Therapeutic agent for bile duct cancer
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
CA2996857C (en) 2015-09-23 2024-05-21 Janssen Pharmaceutica Nv Quinoxaline, quinoline and quinazolinone derivative compounds for the treatment of cancer
KR102691777B1 (ko) 2015-09-23 2024-08-02 얀센 파마슈티카 엔브이 비-헤테로아릴 치환된 1,4-벤조디아제핀 및 암의 치료를 위한 이의 용도
AU2016341445B2 (en) 2015-10-23 2020-08-27 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases
RU2730503C2 (ru) 2015-12-17 2020-08-24 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Терапевтическое средство для лечения рака молочной железы
WO2017164705A1 (ko) * 2016-03-24 2017-09-28 재단법인 대구경북첨단의료산업진흥재단 신규한 피리딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 fgfr 관련 질환의 예방 또는 치료용 약학적 조성물
EP3498707A4 (en) 2016-08-12 2020-04-08 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. FGFR4 INHIBITOR, PREPARATION METHOD THEREOF AND USE THEREOF
CN108101857B (zh) * 2016-11-24 2021-09-03 韶远科技(上海)有限公司 制取2-氨基-3-溴-6-氯吡嗪的可放大工艺
CN108264510A (zh) * 2017-01-02 2018-07-10 上海喆邺生物科技有限公司 一种选择性抑制激酶化合物及其用途
EP3777860A4 (en) 2018-03-28 2021-12-15 Eisai R&D Management Co., Ltd. THERAPEUTIC FOR HEPATOCELLULAR CARCINOMA
JP2022515197A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド がんを治療するためのfgfr阻害剤としての7-((3,5-ジメトキシフェニル)アミノ)キノキサリン誘導体
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
EP4085055A1 (en) 2019-12-30 2022-11-09 Tyra Biosciences, Inc. Aminopyrimidine compounds
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
CN114945367A (zh) * 2020-01-17 2022-08-26 贝达医药公司 作为fgfr激酶抑制剂的哒嗪和1,2,4-三嗪衍生物
PE20240687A1 (es) 2020-12-30 2024-04-10 Tyra Biosciences Inc Compuestos de indazol como inhibidores de cinasas
JP2024509795A (ja) 2021-02-26 2024-03-05 タイラ・バイオサイエンシーズ・インコーポレイテッド アミノピリミジン化合物及びその使用方法
CA3259217A1 (en) 2022-06-29 2024-01-04 Tyra Biosciences Inc INDAZOLE COMPOUNDS
IL317807A (en) 2022-06-29 2025-02-01 Tyra Biosciences Inc Polymorphic compounds and their uses
WO2024138112A1 (en) 2022-12-22 2024-06-27 Tyra Biosciences, Inc. Indazole compounds
TW202535368A (zh) 2023-12-15 2025-09-16 美商泰拉生物科學公司 吲唑化合物
WO2025222097A1 (en) 2024-04-19 2025-10-23 Tyra Biosciences, Inc. Indazole-based protac degraders and their anticancer activity

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008138878A2 (en) * 2007-05-10 2008-11-20 Æterna Zentaris Gmbh Novel pyridopyrazine derivatives, process of manufacturing and uses thereof

Family Cites Families (116)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2940972A (en) 1957-06-27 1960-06-14 Thomae Gmbh Dr K Tri-and tetra-substituted pteridine derivatives
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
GB9125001D0 (en) 1991-11-25 1992-01-22 Ici Plc Heterocyclic compounds
WO1994026723A2 (en) 1993-05-14 1994-11-24 Genentech, Inc. ras FARNESYL TRANSFERASE INHIBITORS
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
US6331555B1 (en) 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
WO1998004689A1 (en) 1995-07-31 1998-02-05 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
TW472045B (en) 1996-09-25 2002-01-11 Astra Ab Protein kinase C inhibitor compounds, method for their preparation, pharmaceutical composition thereof and intermediate used for their preparation
IL133009A0 (en) 1997-05-28 2001-03-19 Aventis Pharm Prod Inc Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
UA71555C2 (en) * 1997-10-06 2004-12-15 Zentaris Gmbh Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives
WO2000042026A1 (en) 1999-01-15 2000-07-20 Novo Nordisk A/S Non-peptide glp-1 agonists
MXPA02001108A (es) 1999-09-15 2002-08-20 Warner Lambert Co Pieridinonas como inhibidores de la cinasa.
DE10013318A1 (de) 2000-03-17 2001-09-20 Merck Patent Gmbh Formulierung enthaltend Chinoxalinderivate
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
JP4286146B2 (ja) 2001-12-18 2009-06-24 メルク エンド カムパニー インコーポレーテッド メタボトロピックグルタミン酸受容体−5のヘテロアリール置換ピラゾール系調節剤
NZ533440A (en) 2001-12-24 2006-08-31 Astrazeneca Ab Substituted quinazoline derivatives as inhibitors of aurora kinases
JP2003213463A (ja) 2002-01-17 2003-07-30 Sumitomo Chem Co Ltd 金属腐食防止剤および洗浄液
WO2003086394A1 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
US6962995B2 (en) 2002-07-10 2005-11-08 E. I. Du Pont De Nemours And Company Charge transport compositions and electronic devices made with such compositions
US7825132B2 (en) 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
KR20120032574A (ko) 2002-10-03 2012-04-05 탈자진 인코포레이티드 혈관항상성 유지제 및 그의 사용 방법
AR043059A1 (es) 2002-11-12 2005-07-13 Bayer Pharmaceuticals Corp Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos
US7098332B2 (en) 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
WO2004065378A1 (en) 2003-01-17 2004-08-05 Warner-Lambert Company Llc 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
WO2004098494A2 (en) 2003-04-30 2004-11-18 Cytokinetics, Inc. Compounds, compositions, and methods
WO2004110350A2 (en) 2003-05-14 2004-12-23 Torreypines Therapeutics, Inc. Compouds and uses thereof in modulating amyloid beta
DE10323345A1 (de) * 2003-05-23 2004-12-16 Zentaris Gmbh Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren
ME00541B (me) * 2003-05-23 2011-10-10 Zentaris Gmbh NOVI PIRIDOPIRAZINI I NJlUHOVA UPOTREBA KAO MODULATORA KlNAZA
WO2005007099A2 (en) 2003-07-10 2005-01-27 Imclone Systems Incorporated Pkb inhibitors as anti-tumor agents
CA2533417A1 (en) 2003-07-21 2005-02-03 Mitchell A. Avery Design and synthesis of optimized ligands for ppar
CN1829709A (zh) 2003-08-01 2006-09-06 健亚生物科技公司 对抗黄病毒的双环咪唑衍生物
AU2004283479A1 (en) 2003-10-17 2005-05-06 4 Aza Bioscience Nv Heterocycle-substituted pteridine derivatives and their use in therapy
KR101167573B1 (ko) 2003-11-07 2012-07-30 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 개선된 약학적 성질을 갖는 퀴놀리논 화합물의 약학적으로허용가능한 염
US7855207B2 (en) 2003-11-20 2010-12-21 Janssen Pharmaceutica, Nv 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adpribose) polymerase inhibitors
JP2007512275A (ja) 2003-11-24 2007-05-17 エフ.ホフマン−ラ ロシュ アーゲー ピラゾリルおよびイミダゾリルピリミジン
HRP20100675T1 (hr) 2003-12-23 2011-01-31 Astex Therapeutics Limited Derivati pirazola kao modulatori protein kinaze
US7098222B2 (en) 2004-05-12 2006-08-29 Abbott Laboratories Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
US7205316B2 (en) 2004-05-12 2007-04-17 Abbott Laboratories Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
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
JP2008516905A (ja) 2004-10-14 2008-05-22 エフ.ホフマン−ラ ロシュ アーゲー Cdk1抗増殖活性を有する1,5−ナフチリジンアゾリジノン
NZ555334A (en) 2004-12-24 2010-05-28 Spinifex Pharm Pty Ltd Method of treatment or prophylaxis of a neuropathic condition using AT2 receptor antagonist
NZ556686A (en) 2005-02-14 2010-01-29 Bionomics Ltd Novel tubulin polymerisation inhibitors
US9271963B2 (en) 2005-03-03 2016-03-01 Universitat Des Saarlandes Selective inhibitors of human corticosteroid synthases
CA2606017A1 (en) 2005-05-12 2006-11-23 Merck & Co., Inc. Tyrosine kinase inhibitors
BRPI0611521A2 (pt) 2005-05-18 2010-09-14 Wyeth Corp inibidores de 4,6-diamino-[1,7]naftiridina-3-carbonitrila de quìnase tpl2 e métodos de fabricação e uso dos mesmos
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
JP5226513B2 (ja) 2005-08-26 2013-07-03 メルク セローノ ソシエテ アノニム ピラジン誘導体及びその使用
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
KR101400905B1 (ko) 2005-11-11 2014-05-29 아에테르나 젠타리스 게엠베하 신규한 피리도피라진 및 키나제의 조절제로서의 이의 용도
AU2006331912B2 (en) 2005-12-21 2012-08-30 Janssen Pharmaceutica, N.V. Triazolopyridazines as tyrosine kinase modulators
US7998978B2 (en) 2006-05-01 2011-08-16 Pfizer Inc. Substituted 2-amino-fused heterocyclic compounds
GB0609621D0 (en) 2006-05-16 2006-06-21 Astrazeneca Ab Novel co-crystal
CA2653117A1 (en) 2006-05-24 2007-11-29 Boehringer Ingelheim International Gmbh Substituted pteridines substituted with a four-membered heterocycle
US20100016293A1 (en) 2006-07-03 2010-01-21 Rogier Adriaan Smits Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use
JP2008127446A (ja) 2006-11-20 2008-06-05 Canon Inc 1,5−ナフチリジン化合物及び有機発光素子
US20110262525A1 (en) 2006-12-13 2011-10-27 Schering Corporation Methods of treatment
CA2673736A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
JP2010514693A (ja) 2006-12-22 2010-05-06 ノバルティス アーゲー Pdk1阻害のためのキナゾリン
CN101679408B (zh) 2006-12-22 2016-04-27 Astex治疗学有限公司 作为fgfr抑制剂的双环杂环化合物
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
JP2010526823A (ja) 2007-05-10 2010-08-05 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Pi3キナーゼ阻害物質としてのキノキサリン誘導体
JP2010529031A (ja) 2007-05-29 2010-08-26 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Pi3キナーゼ阻害剤としてのナフチリジン誘導体
AR066879A1 (es) 2007-06-08 2009-09-16 Novartis Ag Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus
CA2690226C (en) 2007-06-20 2012-07-24 Mitsubishi Tanabe Pharma Corporation Novel malonic acid sulfonamide derivative and pharmaceutical use thereof
EP2170894A1 (en) 2007-06-21 2010-04-07 Janssen Pharmaceutica N.V. Polymorphic and hydrate forms, salts and process for preparing 6-{difluoro[6-(1-methyl-1h-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline
WO2009019518A1 (en) 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect
EP2173354A4 (en) 2007-08-09 2011-10-05 Glaxosmithkline Llc CHINOXALIN DERIVATIVES AS PI3 KINASE INHIBITORS
US20090054304A1 (en) 2007-08-23 2009-02-26 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
CN101910152B (zh) 2007-11-16 2014-08-06 因塞特公司 作为janus激酶抑制剂的4-吡唑基-n-芳基嘧啶-2-胺和4-吡唑基-n-杂芳基嘧啶-2-胺
MX2010012064A (es) 2008-05-05 2010-12-06 Schering Corp Uso secuencial de agentes quimioterapeuticos citotoxicos para el tratamiento de cancer.
ES2554513T3 (es) 2008-05-23 2015-12-21 Novartis Ag Derivados de quinolinas y quinoxalinas como inhibidores de la proteína tirosina quinasa
JP2012509342A (ja) 2008-11-20 2012-04-19 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 置換ピロロ[2,3−b]−ピリジンおよび−ピラジン
WO2010084152A1 (en) 2009-01-21 2010-07-29 Basilea Pharmaceutica Ag Novel bicyclic antibiotics
WO2010088177A1 (en) 2009-02-02 2010-08-05 Merck Sharp & Dohme Corp. Inhibitors of akt activity
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
WO2010143169A2 (en) 2009-06-12 2010-12-16 Société Splicos Compounds useful for treating aids
KR101650981B1 (ko) 2009-09-03 2016-08-24 바이오에너제닉스 Pask의 억제를 위한 복소환 화합물
CN102596932A (zh) 2009-09-04 2012-07-18 拜耳医药股份有限公司 作为酪氨酸苏氨酸激酶抑制剂的取代氨基喹喔啉
US20110123545A1 (en) 2009-11-24 2011-05-26 Bristol-Myers Squibb Company Combination of vegfr2 and igf1r inhibitors for the treatment of proliferative diseases
EP2332939A1 (en) 2009-11-26 2011-06-15 Æterna Zentaris GmbH Novel Naphthyridine derivatives and the use thereof as kinase inhibitors
SG10201502484SA (en) 2010-03-30 2015-05-28 Verseon Corp Multisubstituted aromatic compounds as inhibitors of thrombin
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
US8513421B2 (en) 2010-05-19 2013-08-20 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
US9096590B2 (en) 2010-05-24 2015-08-04 Intellikine Llc Substituted benzoxazoles as PI3 kinase inhibitors
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
CN102532141A (zh) 2010-12-08 2012-07-04 中国科学院上海药物研究所 [1,2,4]三唑并[4,3-b][1,2,4]三嗪类化合物、其制备方法和用途
TW201309700A (zh) 2011-01-31 2013-03-01 Novartis Ag 新穎雜環衍生物
EP2678018A4 (en) 2011-02-23 2015-09-30 Intellikine Llc COMBINATION OF CHINESE HEMMER AND USES THEREOF
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
ES2725790T3 (es) 2011-08-26 2019-09-27 Neupharma Inc Algunas entidades químicas, composiciones, y métodos
WO2013040515A1 (en) 2011-09-14 2013-03-21 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2013043935A1 (en) 2011-09-21 2013-03-28 Neupharma, Inc. Certain chemical entites, compositions, and methods
CA2850763A1 (en) 2011-10-04 2013-04-11 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
WO2013061305A1 (en) 2011-10-28 2013-05-02 Novartis Ag Novel purine derivatives and their use in the treatment of disease
KR20200046135A (ko) 2012-03-08 2020-05-06 아스테라스 세이야쿠 가부시키가이샤 신규 fgfr3 융합체
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
KR102479696B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 Fgfr 억제제 및 igf1r 억제제의 조합물
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
MX370099B (es) 2014-03-26 2019-12-02 Astex Therapeutics Ltd Combinación que comprende un inhibidor de fgfr y un inhibidor de cmet para el tratamiento del cáncer.
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
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008138878A2 (en) * 2007-05-10 2008-11-20 Æterna Zentaris Gmbh Novel pyridopyrazine derivatives, process of manufacturing and uses thereof

Also Published As

Publication number Publication date
US20140288053A1 (en) 2014-09-25
CN104011051A (zh) 2014-08-27
PH12014500867A1 (en) 2014-06-30
US9309242B2 (en) 2016-04-12
BR112014010206B1 (pt) 2020-12-08
LT2776435T (lt) 2018-10-10
MX2014004855A (es) 2014-08-21
MY185666A (en) 2021-05-28
ES2688868T3 (es) 2018-11-07
AP2014007540A0 (en) 2014-03-31
CO6940422A2 (es) 2014-05-09
DK2776435T3 (en) 2018-10-15
CN104011051B (zh) 2017-05-10
AU2012328170B2 (en) 2017-08-24
BR112014010206A2 (pt) 2017-05-16
SG11201401055XA (en) 2014-09-26
NI201400032A (es) 2015-11-24
IL232083A0 (en) 2014-05-28
JP2014534211A (ja) 2014-12-18
AR088567A1 (es) 2014-06-18
US10045982B2 (en) 2018-08-14
EP2776435B1 (en) 2018-06-27
MX353654B (es) 2018-01-22
EA201490891A1 (ru) 2014-09-30
CA2853390C (en) 2020-12-15
AP4060A (en) 2017-03-08
AU2012328170A1 (en) 2014-05-22
UA111386C2 (uk) 2016-04-25
UY34418A (es) 2013-05-31
TW201333004A (zh) 2013-08-16
JO3419B1 (ar) 2019-10-20
EA027563B1 (ru) 2017-08-31
CR20140190A (es) 2014-05-26
JP6169583B2 (ja) 2017-07-26
GB201118656D0 (en) 2011-12-07
IN2014MN00948A (enExample) 2015-04-24
HRP20181533T1 (hr) 2018-11-16
KR102066496B1 (ko) 2020-01-15
IL232083B (en) 2018-06-28
CA2853390A1 (en) 2013-05-02
WO2013061080A1 (en) 2013-05-02
SI2776435T1 (sl) 2018-11-30
CL2014001065A1 (es) 2014-07-25
ECSP14013325A (es) 2015-04-30
NZ622702A (en) 2016-08-26
KR20140096034A (ko) 2014-08-04
US20160235744A1 (en) 2016-08-18
BR112014010206B8 (pt) 2021-08-03
EP2776435A1 (en) 2014-09-17

Similar Documents

Publication Publication Date Title
TWI602814B (zh) 透過抑制fgfr激酶之具有抗癌性的吡啶並吡嗪衍生物化合物
CN104507944B (zh) 作为fgfr抑制剂的蝶啶
KR102341202B1 (ko) Fgfr 키나제 조절제로서 유용한 퀴나졸리논 유도체
KR102086871B1 (ko) Fgfr 키나제의 억제를 통한 항암 벤조피라진
KR102134204B1 (ko) 신규 화합물
KR20140096033A (ko) 신규 화합물
HK1197411A (en) Anticancer pyridopyrazines via the inhibition of fgfr kinases
HK1197411B (en) Anticancer pyridopyrazines via the inhibition of fgfr kinases