AP4060A - Anticancer pyridopyrazines via the inhibition of fgfr kinases - Google Patents

Anticancer pyridopyrazines via the inhibition of fgfr kinases

Info

Publication number
AP4060A
AP4060A AP2014007540A AP2014007540A AP4060A AP 4060 A AP4060 A AP 4060A AP 2014007540 A AP2014007540 A AP 2014007540A AP 2014007540 A AP2014007540 A AP 2014007540A AP 4060 A AP4060 A AP 4060A
Authority
AP
ARIPO
Prior art keywords
pyridopyrazines
anticancer
inhibition
fgfr kinases
fgfr
Prior art date
Application number
AP2014007540A
Other languages
English (en)
Other versions
AP2014007540A0 (en
Inventor
Valerio Berdini
Gordon Saxty
Patrick Rene Angibaud
Olivier Alexis Georges Querolle
Virginie Sophie Poncelet
Bruno Roux
Lieven Meerpoel
Original Assignee
Astex Therapeutics Ltd
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 Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of AP2014007540A0 publication Critical patent/AP2014007540A0/xx
Application granted granted Critical
Publication of AP4060A publication Critical patent/AP4060A/en

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
    • 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
    • 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
    • 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)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AP2014007540A 2011-10-28 2012-10-26 Anticancer pyridopyrazines via the inhibition of fgfr kinases AP4060A (en)

Applications Claiming Priority (3)

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
PCT/GB2012/052672 WO2013061080A1 (en) 2011-10-28 2012-10-26 Anticancer pyridopyrazines via the inhibition of fgfr kinases

Publications (2)

Publication Number Publication Date
AP2014007540A0 AP2014007540A0 (en) 2014-03-31
AP4060A true AP4060A (en) 2017-03-08

Family

ID=45373584

Family Applications (1)

Application Number Title Priority Date Filing Date
AP2014007540A AP4060A (en) 2011-10-28 2012-10-26 Anticancer pyridopyrazines via the inhibition of fgfr kinases

Country Status (33)

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

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
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
GB201118656D0 (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
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
AR098145A1 (es) * 2013-10-25 2016-05-04 Novartis Ag Compuestos derivados de piridilo bicíclicos fusionados como inhibidores de fgfr4
AU2014338549B2 (en) 2013-10-25 2017-05-25 Novartis Ag Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
US10736900B2 (en) * 2014-03-26 2020-08-11 Astex Therapeutics Ltd Combinations of an FGFR inhibitor and an IGF1R inhibitor
AU2015238301B2 (en) * 2014-03-26 2020-06-25 Astex Therapeutics Ltd Combinations
US9951047B2 (en) 2014-08-18 2018-04-24 Eisai R&D Management Co., Ltd. Salt of monocyclic pyridine derivative and crystal thereof
PL3200786T3 (pl) * 2014-10-03 2020-03-31 Novartis Ag Zastosowanie pochodnych pirydylowych o skondensowanym układzie bicyklicznym jako inhibitorów fgfr4
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
US20180015079A1 (en) 2015-03-25 2018-01-18 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
WO2017050864A1 (en) 2015-09-23 2017-03-30 Janssen Pharmaceutica Nv New compounds
MX378230B (es) 2015-09-23 2025-03-10 Janssen Pharmaceutica Nv 1,4-benzodiazepinas biheteroarilo sustituidas y usos de las mismas para el tratamiento del cáncer.
US10208024B2 (en) 2015-10-23 2019-02-19 Array Biopharma Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases
KR102486722B1 (ko) 2015-12-17 2023-01-11 에자이 알앤드디 매니지먼트 가부시키가이샤 유방암 치료제
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
WO2018028664A1 (zh) * 2016-08-12 2018-02-15 江苏豪森药业集团有限公司 Fgfr4抑制剂及其制备方法和应用
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
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
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
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
EP4085055A1 (en) 2019-12-30 2022-11-09 Tyra Biosciences, Inc. Aminopyrimidine compounds
US20240002365A1 (en) * 2020-01-17 2024-01-04 Beta Pharma, Inc. Pyridazine and 1,2,4-triazine derivatives as fgfr kinase inhibitors
TW202241906A (zh) 2020-12-30 2022-11-01 美商泰拉生物科學公司 吲唑化合物
TW202246243A (zh) 2021-02-26 2022-12-01 美商泰拉生物科學公司 胺基嘧啶化合物及其使用方法
CN119731165A (zh) 2022-06-29 2025-03-28 泰拉生物科学公司 吲唑化合物
WO2024006883A1 (en) 2022-06-29 2024-01-04 Tyra Biosciences, Inc. Polymorphic compounds and uses thereof
WO2024138112A1 (en) 2022-12-22 2024-06-27 Tyra Biosciences, Inc. Indazole compounds
WO2025129014A1 (en) 2023-12-15 2025-06-19 Tyra Biosciences, Inc. Indazole compounds for the treatment of cancer
WO2025222097A1 (en) 2024-04-19 2025-10-23 Tyra Biosciences, Inc. Indazole-based protac degraders and their anticancer activity

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999017759A2 (en) * 1997-10-06 1999-04-15 Asta Medica Aktiengesellschaft Methods of modulating serine/threonine protein kinase function with 5-azaquinoxaline-based compounds
WO2008138878A2 (en) * 2007-05-10 2008-11-20 Æterna Zentaris Gmbh Novel pyridopyrazine derivatives, process of manufacturing and uses thereof

Family Cites Families (115)

* 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
EP0763537A3 (en) 1993-05-14 1997-10-22 Genentech Inc Non-peptides farnesyl transfer 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
SK157999A3 (en) 1997-05-28 2000-06-12 Rhone Poulenc Rorer Pharma Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p561ck tyrosine kinases
JP2002534512A (ja) 1999-01-15 2002-10-15 ノボ ノルディスク アクティーゼルスカブ 非ペプチドglp−1アゴニスト
CN1373763A (zh) 1999-09-15 2002-10-09 沃尼尔·朗伯公司 作为激酶抑制剂的蝶啶酮
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
KR101029281B1 (ko) 2001-12-24 2011-04-18 아스트라제네카 아베 오로라 키나제의 억제제로서 치환된 퀴나졸린 유도체
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
CA2480800C (en) 2002-04-08 2008-09-23 Mark T. Bilodeau Inhibitors of akt activity
US20040097725A1 (en) 2002-07-10 2004-05-20 Norman Herron 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
JP4560483B2 (ja) 2002-10-03 2010-10-13 ターゲジェン インコーポレーティッド 血管静態化物質およびそれらの使用法
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
MXPA05007503A (es) 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
MXPA05012281A (es) 2003-05-14 2006-05-19 Torreypines Therapeutics Inc Compuestos y uso de los mismos en la modulacion beta amiloide.
DE502004008322D1 (de) * 2003-05-23 2008-12-04 Aterna Zentaris Gmbh Neue pyridopyrazine und deren verwendung als modulatoren von kinasen
DE10323345A1 (de) * 2003-05-23 2004-12-16 Zentaris Gmbh Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren
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
JP2007501189A (ja) 2003-08-01 2007-01-25 ジェネラブス テクノロジーズ,インコーポレイテッド フラビウイルス科に対する二環式イミダゾール誘導体
ATE369862T1 (de) 2003-10-17 2007-09-15 4 Aza Ip Nv Heterocyclus-substituierte pteridin-derivate und ihre verwendung in der therapie
WO2005047244A2 (en) 2003-11-07 2005-05-26 Chiron Corporation Inhibition of fgfr3 and treatment of multiple myeloma
MXPA06005687A (es) 2003-11-20 2006-08-17 Janssen Pharmaceutica Nv 2-quinolinonas y 2-quinoxalinonas sustituidas con 6-alquenilo y 6-fenilalquilo como inhibidores de la poli(adenosin fosfato-ribosa)polimerasa.
CN100554264C (zh) 2003-11-24 2009-10-28 弗·哈夫曼-拉罗切有限公司 吡唑基与咪唑基嘧啶
EP1706385B1 (en) 2003-12-23 2010-10-06 Astex Therapeutics Limited Pyrazole derivatives as protein kinase modulators
US7205316B2 (en) 2004-05-12 2007-04-17 Abbott Laboratories Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
US7098222B2 (en) 2004-05-12 2006-08-29 Abbott Laboratories Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
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
US7268231B2 (en) 2004-10-14 2007-09-11 Hoffmann-La Roche Inc. 1,5-Naphthyridine azolinone
CN102861019B (zh) 2004-12-24 2016-05-25 诺华股份有限公司 治疗或预防神经性疼痛的药物
US8278290B2 (en) 2005-02-14 2012-10-02 Biononics Limited Tubulin polymerisation inhibitors
US9271963B2 (en) 2005-03-03 2016-03-01 Universitat Des Saarlandes Selective inhibitors of human corticosteroid synthases
AU2006247833A1 (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
BRPI0615233A2 (pt) 2005-08-26 2011-05-10 Serono Lab derivados de pirazina e uso dos mesmos como inibidores p13k
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
CA2628039A1 (en) 2005-11-11 2007-05-18 Aeterna Zentaris Gmbh Novel 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
JP5292102B2 (ja) 2005-12-21 2013-09-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ チロシンキナーゼ調節剤としてのトリアゾロピリダジン類
CA2651072A1 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
GB0609621D0 (en) 2006-05-16 2006-06-21 Astrazeneca Ab Novel co-crystal
ATE549338T1 (de) 2006-05-24 2012-03-15 Boehringer Ingelheim Int Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
CA2657702A1 (en) 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs Wetenschappelijk Onderzoek E N Patieentenzorg Quinazolines and related heterocyclic comp0unds, 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
JP2010513278A (ja) 2006-12-13 2010-04-30 シェーリング コーポレイション Igf1rインヒビターを用いた癌の処置方法
BRPI0720695A2 (pt) 2006-12-21 2014-02-18 Plexxikon Inc Compostos e métodos para modulação de cinase, e indicações para estes
AR064491A1 (es) 2006-12-22 2009-04-08 Astex Therapeutics Ltd Derivados de imidazo[1, 2-a]pirimidina, un proceso para su preparacion, una composicion farmaceutica que los comprende y su uso en el tratamiento de enfermedades mediadas por las quinasas fgfr.
US20100216767A1 (en) 2006-12-22 2010-08-26 Mina Aikawa Quinazolines for pdk1 inhibition
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
JP5498786B2 (ja) 2007-06-20 2014-05-21 田辺三菱製薬株式会社 新規なマロン酸スルホンアミド誘導体およびその医薬用途
WO2008155378A1 (en) 2007-06-21 2008-12-24 Janssen Pharmaceutica Nv 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
JP2010535804A (ja) 2007-08-09 2010-11-25 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キナーゼ阻害薬としてのキノキサリン誘導体
WO2009019518A1 (en) 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect
US20090054304A1 (en) 2007-08-23 2009-02-26 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
CA2704599C (en) 2007-11-16 2015-05-12 Incyte Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
EP2282739A2 (en) 2008-05-05 2011-02-16 Schering Corporation Sequential administration of chemotherapeutic agents for treatment of cancer
EA021421B1 (ru) 2008-05-23 2015-06-30 Новартис Аг Производные хинолинов и хиноксалинов в качестве ингибиторов протеинтирозинкиназы, способ их получения, содержащая их фармацевтическая композиция и способ лечения заболеваний с применением таких соединений
EP2356116A1 (en) 2008-11-20 2011-08-17 OSI Pharmaceuticals, Inc. Substituted pyrroloý2,3-b¨-pyridines and-pyrazines
CA2750047A1 (en) 2009-01-21 2010-07-29 Basilea Pharmaceutica Ag Novel bicyclic antibiotics
AU2010208480A1 (en) 2009-02-02 2011-07-28 Msd K.K. Inhibitors of Akt activity
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
CA2764024C (en) 2009-06-12 2017-12-05 Splicos Quinoline and isoquinoline compounds useful for treating cancer
PH12012500382A1 (en) 2009-09-03 2012-10-22 Bioenergenix Heterocyclic compounds for the inhibition of pask
EP2473498A1 (en) 2009-09-04 2012-07-11 Bayer Pharma Aktiengesellschaft Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors
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
SG184243A1 (en) 2010-03-30 2012-10-30 Verseon Corp Multisubstituted aromatic compounds as inhibitors of thrombin
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
WO2011146591A1 (en) 2010-05-19 2011-11-24 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
WO2011149937A1 (en) 2010-05-24 2011-12-01 Intellikine, Inc. Heterocyclic compounds and uses thereof
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
EP2670753B1 (en) 2011-01-31 2016-10-19 Novartis AG Novel heterocyclic derivatives
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
JP6002223B2 (ja) 2011-08-26 2016-10-05 ニューファーマ, インコーポレイテッド 特定の化学的実体、組成物、および方法
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
WO2013052699A2 (en) 2011-10-04 2013-04-11 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
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
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
EA023935B1 (ru) 2011-10-28 2016-07-29 Новартис Аг Производные пурина и их применение для лечения заболевания
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
CA2865388C (en) 2012-03-08 2022-01-04 Astellas Pharma Inc. Novel fgfr3 fusion
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
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
US10736900B2 (en) 2014-03-26 2020-08-11 Astex Therapeutics Ltd Combinations of an FGFR inhibitor and an IGF1R inhibitor
AU2015238301B2 (en) 2014-03-26 2020-06-25 Astex Therapeutics Ltd Combinations
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999017759A2 (en) * 1997-10-06 1999-04-15 Asta Medica Aktiengesellschaft Methods of modulating serine/threonine protein kinase function with 5-azaquinoxaline-based compounds
WO2008138878A2 (en) * 2007-05-10 2008-11-20 Æterna Zentaris Gmbh Novel pyridopyrazine derivatives, process of manufacturing and uses thereof

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