EA023222B8 - Пиразолилхиноксалиновые ингибиторы киназы - Google Patents

Пиразолилхиноксалиновые ингибиторы киназы

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Publication number
EA023222B8
EA023222B8 EA201291143A EA201291143A EA023222B8 EA 023222 B8 EA023222 B8 EA 023222B8 EA 201291143 A EA201291143 A EA 201291143A EA 201291143 A EA201291143 A EA 201291143A EA 023222 B8 EA023222 B8 EA 023222B8
Authority
EA
Eurasian Patent Office
Prior art keywords
kinase inhibitors
compounds
pyrazolyl
quinazoline kinase
pyrazolyl quinazoline
Prior art date
Application number
EA201291143A
Other languages
English (en)
Russian (ru)
Other versions
EA023222B1 (ru
EA201291143A1 (ru
Inventor
Гордон Саксти
Кристофер Уилльям Мюррей
Валерио Бердини
Гилберт Эбай Безонг
Кристофер Чарльз Фредерик Хамлетт
Кристофер Норберт Джонсон
Стивен Джон Вудхэд
Майкл Ридер
Дэвид Чарльз Рис
Лоранс Анн Мевеллек
Патрик Рене Анжибо
Эдди Жан Эдгар Фрейн
Том Корнелис Хортенсе Говартс
Йохан Эрвин Эдмонд Вертс
Тимоти Пьетро Сурен Перера
Роналдус Арнодус Хендрика Йозеф Гилиссен
Бертольд Вробловски
Жан Фернан Арман Лакрамп
Александра Папаникос
Оливье Алексис Жорж Керолль
Элизабет Тереза Жанна Паскье
Изабелль Нелль Констанс Пилатт
Паскаль Гислен Андре Бонне
Вернер Констант Йохан Эмбрехтс
Рхалид Аккари
Ливен Мерпул
Original Assignee
Астекс Терапьютикс Лимитед
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 Астекс Терапьютикс Лимитед filed Critical Астекс Терапьютикс Лимитед
Publication of EA201291143A1 publication Critical patent/EA201291143A1/ru
Publication of EA023222B1 publication Critical patent/EA023222B1/ru
Publication of EA023222B8 publication Critical patent/EA023222B8/ru

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
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    • 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
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6524Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms

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  • Life Sciences & Earth Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Epidemiology (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
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  • Hematology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Otolaryngology (AREA)
  • Obesity (AREA)
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  • Gastroenterology & Hepatology (AREA)
EA201291143A 2010-04-30 2011-04-28 Пиразолилхиноксалиновые ингибиторы киназы EA023222B8 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32988410P 2010-04-30 2010-04-30
GB201007286A GB201007286D0 (en) 2010-04-30 2010-04-30 New compounds
PCT/GB2011/050851 WO2011135376A1 (en) 2010-04-30 2011-04-28 Pyrazolyl quinazoline kinase inhibitors

Publications (3)

Publication Number Publication Date
EA201291143A1 EA201291143A1 (ru) 2013-05-30
EA023222B1 EA023222B1 (ru) 2016-05-31
EA023222B8 true EA023222B8 (ru) 2017-04-28

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EA201291143A EA023222B8 (ru) 2010-04-30 2011-04-28 Пиразолилхиноксалиновые ингибиторы киназы
EA201500278A EA028599B1 (ru) 2010-04-30 2011-04-28 Пиразолилхиноксалиновые ингибиторы киназы

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Families Citing this family (103)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101641339B (zh) 2007-02-01 2013-07-17 雷斯韦洛吉克斯公司 用于预防和治疗心血管疾病的化合物
AU2010224523B2 (en) 2009-03-18 2014-05-08 Resverlogix Corp. Novel anti-inflammatory agents
MX374414B (es) 2009-04-22 2025-03-06 Resverlogix Corp Nuevos agentes anti-inflamatorios.
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
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
WO2013059740A1 (en) 2011-10-21 2013-04-25 Foundation Medicine, Inc. Novel alk and ntrk1 fusion molecules and uses thereof
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
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
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
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
ES2916220T3 (es) 2012-07-11 2022-06-29 Blueprint Medicines Corp Inhibidores del receptor de factor de crecimiento de fibroblasto
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
JP6307087B2 (ja) * 2012-10-15 2018-04-04 レスバーロジックス コーポレイション ベンズアミド化合物の合成に有用な化合物
HK1214830A1 (zh) 2012-11-05 2016-08-05 Foundation Medicine, Inc. 新型ntrk1融合分子及其应用
CA2890346A1 (en) 2012-11-05 2014-05-08 Foundation Medicine, Inc. Novel fusion molecules and uses thereof
WO2014085486A2 (en) 2012-11-30 2014-06-05 Waters Technologies Corporation Methods and apparatus for the analysis of vitamin d metabolites
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
EP3939614A1 (en) 2013-01-18 2022-01-19 Foundation Medicine, Inc. Methods of treating cholangiocarcinoma
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
ES2892423T3 (es) 2013-03-15 2022-02-04 Celgene Car Llc Compuestos de heteroarilo y usos de los mismos
AU2014228746B2 (en) * 2013-03-15 2018-08-30 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
JP6449244B2 (ja) 2013-04-19 2019-01-09 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Fgfr抑制剤としての二環式複素環
GB201307577D0 (en) * 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
CN104163794A (zh) * 2013-10-17 2014-11-26 中国药科大学 2-氨基芳环类血管内皮生长因子受体(vegfr)抑制剂及其制备方法和用途
SMT202200292T1 (it) 2013-10-25 2022-09-14 Blueprint Medicines Corp Inibitori del recettore del fattore di crescita dei fibroblasti
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
RU2715236C2 (ru) * 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
CA2943687C (en) * 2014-03-26 2024-02-13 Astex Therapeutics Ltd Combinations of an fgfr inhibitor and an igf1r inhibitor
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
CN105017227B (zh) * 2014-07-08 2018-03-09 四川百利药业有限责任公司 N‑(1h‑吡唑‑5‑基)喹唑啉‑4‑胺类化合物
KR102344105B1 (ko) 2014-08-18 2021-12-29 에자이 알앤드디 매니지먼트 가부시키가이샤 모노시클릭 피리딘 유도체의 염 및 이의 결정
KR102839867B1 (ko) 2014-09-26 2025-07-28 얀센 파마슈티카 엔브이 Fgfr 억제제를 사용한 치료에 반응할 암 환자를 확인하는 데 있어서 fgfr 돌연변이 유전자 패널의 사용
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles 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
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
ES2751669T3 (es) 2015-02-20 2020-04-01 Incyte Corp Heterociclos bicíclicos como inhibidores FGFR
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CN107530356A (zh) 2015-03-13 2018-01-02 雷斯韦洛吉克斯公司 用于治疗补体相关疾病之组合物及治疗方法
JP6503450B2 (ja) 2015-03-25 2019-04-17 国立研究開発法人国立がん研究センター 胆管癌治療剤
US10478494B2 (en) * 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
TWI703984B (zh) * 2015-04-03 2020-09-11 英商阿斯特克斯治療有限公司 用於癌症治療之fgfr/pd-1組合療法
US11542247B2 (en) 2015-09-23 2023-01-03 Janssen Pharmaceutica Nv Bi-heteroaryl substitute 1,4-benzodiazepines and uses thereof for the treatment of cancer
ES2811845T3 (es) 2015-09-23 2021-03-15 Janssen Pharmaceutica Nv Heterociclos tricíclicos para el tratamiento del cáncer
CN105596330B (zh) * 2015-12-11 2018-10-16 深圳市坤健创新药物研究院 虚拟筛选化合物在制备激酶抑制剂中的应用和药物
SG10201913213WA (en) 2015-12-17 2020-03-30 Eisai R&D Man Co Ltd Therapeutic agent for breast cancer
CN107459519A (zh) 2016-06-06 2017-12-12 上海艾力斯医药科技有限公司 稠合嘧啶哌啶环衍生物及其制备方法和应用
WO2018049233A1 (en) 2016-09-08 2018-03-15 Nicolas Stransky Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors
JP7206188B2 (ja) * 2016-10-10 2023-01-17 ディベロップメント センター フォー バイオテクノロジー Iii型受容体チロシンキナーゼ阻害剤としてのキノキサリン化合物
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JOP20190280A1 (ar) 2017-06-02 2019-12-02 Janssen Pharmaceutica Nv مثبطات fgfr2 لعلاج سرطان الأوعية الصفراوية
US10717703B2 (en) * 2017-08-21 2020-07-21 Celgene Corporation Processes for the preparation of (S)-tert-butyl 4,5-diamino-5-oxopentanoate
US11661411B2 (en) 2017-12-01 2023-05-30 Board Of Regents Of The University Of Nebraska Quinoxaline compounds and uses thereof
CN111712245A (zh) 2018-03-28 2020-09-25 卫材R&D管理有限公司 用于肝细胞癌的治疗剂
WO2019209083A1 (ko) * 2018-04-26 2019-10-31 재단법인 의약바이오컨버젼스연구단 mTOR 저해제로서의 신규 화합물 및 이의 용도
CN119241541A (zh) 2018-05-04 2025-01-03 因赛特公司 Fgfr抑制剂的固体形式和其制备方法
PE20210919A1 (es) 2018-05-04 2021-05-19 Incyte Corp Sales de un inhibidor de fgfr
JP7761485B2 (ja) 2018-09-21 2025-10-28 ヤンセン ファーマシューティカ エヌ.ベー. 胆管癌の処置
US12180207B2 (en) 2018-12-19 2024-12-31 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases
EP3898615A1 (en) * 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
CA3130460A1 (en) 2019-03-29 2020-10-08 Anne Elizabeth O'HAGAN Fgfr tyrosine kinase inhibitors for the treatment of urothelial carcinoma
WO2020201138A1 (en) 2019-03-29 2020-10-08 Janssen Pharmaceutica Nv Fgfr tyrosine kinase inhibitors for the treatment of urothelial carcinoma
WO2020208592A1 (en) * 2019-04-12 2020-10-15 Dr. Reddy’S Laboratories Limited Process for preparation of erdafitinib, its purification and amorphous solid dispersion
CN111909044A (zh) * 2019-05-09 2020-11-10 南京爱德程医药科技有限公司 2-(烷基氨基)乙基苯甲酸酯类化合物的合成方法
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TWI759829B (zh) * 2019-08-23 2022-04-01 財團法人生物技術開發中心 作為第iii型受體酪胺酸激酶抑制劑之雜環吡唑衍生物
EP4034118A1 (en) 2019-09-26 2022-08-03 Janssen Pharmaceutica NV Use of fgfr inhibitors in fgfr-genetically altered cancers to enhance patient response to immune checkpoint inhibitors in sequential treatment settings
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN110790677B (zh) * 2019-11-05 2022-04-29 浙江工业大学 一种金刚烷甲酰胺类化合物及其制备方法和应用
AU2020391161A1 (en) 2019-11-25 2022-06-09 Amgen Inc. Heterocyclic compounds as Delta-5 Desaturase inhibitors and methods of use
IL293001A (en) 2019-12-04 2022-07-01 Incyte Corp Derivatives of fgfr repressors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN113024517A (zh) * 2019-12-09 2021-06-25 武汉九州钰民医药科技有限公司 一种制备厄达替尼的方法
CN113024518A (zh) * 2019-12-09 2021-06-25 武汉九州钰民医药科技有限公司 一种厄达替尼的制备方法
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4076449A4 (en) * 2020-01-17 2023-12-06 Beta Pharma, Inc. PYRIDAZINE AND 1,2,4-TRIAZINE DERIVATIVES AS FGFR KINASE INHIBITORS
BR112022015827A2 (pt) 2020-02-12 2022-10-04 Janssen Pharmaceutica Nv Inibidores de tirosina quinase de fgfr para o tratamento de câncer de bexiga invasivo não muscular de alto risco
TWI900527B (zh) 2020-02-12 2025-10-11 比利時商健生藥品公司 用於治療尿路上皮癌的fgfr酪胺酸激酶抑制劑和抗pd1藥劑
US20240010632A1 (en) 2020-08-17 2024-01-11 Teva Pharmaceuticals International Gmbh Solid state forms of erdafitinib salts and processes for preparation of erdafitinib
CN112920167B (zh) * 2020-08-19 2022-08-26 四川大学华西医院 靶向fgfr和hdac的双靶点抑制剂及其制备方法和应用、药物组合物及药剂
CA3191538A1 (en) 2020-09-14 2022-03-17 Ademi Elena SANTIAGO-WALKER Fgfr inhibitor combination therapies
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Fgfr阻害剤及びネクチン-4標的化剤を含む併用療法
BR112023023935A2 (pt) 2021-05-19 2024-01-30 Janssen Pharmaceutica Nv Inibidores de tirosina quinase de fgfr para o tratamento de tumores sólidos avançados
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CN117858872A (zh) 2021-06-22 2024-04-09 缆图药品公司 用于治疗癌症的杂环egfr抑制剂
JP2024538993A (ja) 2021-10-12 2024-10-28 タリス バイオメディカル エルエルシー エルダフィチニブ製剤及び膀胱内投与のためのシステム
KR20240115979A (ko) 2021-11-08 2024-07-26 프로젠토스 테라퓨틱스, 인크. 혈소판-유래 성장 인자 수용체(pdgfr) 알파 억제제 및 이의 용도
JP2025507590A (ja) * 2022-02-18 2025-03-21 タリス バイオメディカル エルエルシー エルダフィチニブ製剤及び膀胱内投与のための浸透圧システム
CN115108926B (zh) * 2022-04-02 2023-06-20 上海工程技术大学 一种用于制备厄达替尼的中间体化合物及制备方法
CN120813357A (zh) 2023-02-13 2025-10-17 詹森药业有限公司 用于治疗高风险非肌层浸润性膀胱癌的fgfr酪氨酸激酶抑制剂
WO2024173377A1 (en) 2023-02-13 2024-08-22 Taris Biomedical Llc Erdafitinib for intravesical administration for use in the treatment of bladder cancer
CN119101036A (zh) * 2023-06-08 2024-12-10 广州六顺生物科技有限公司 喹喔啉类化合物及其应用
WO2025059602A1 (en) 2023-09-14 2025-03-20 Taris Biomedical Llc Methods of treating bladder cancer using intravesical administration of erdafitinib
CN119350298A (zh) * 2024-10-09 2025-01-24 沈阳药科大学 一种厄达替尼的制备方法以及用于该方法的中间体化合物

Family Cites Families (128)

* 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
US5882864A (en) 1995-07-31 1999-03-16 Urocor Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
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
BR9809501A (pt) 1997-05-28 2000-06-20 Rhone Poulenc Rorer Pharma Composto, composição farmacêutica, e, processos para inibir a atividade da tirosina quinase pdgf, para inibir a atividade da tirosina quinase lck, para inibir a proliferação celular, diferenciação ou liberação de mediador em um paciente, para tratar uma patologia ligada a um distúrbio hiperproliferativo, para tratar a restenose, e, para tratar inflamação em um paciente
US6235740B1 (en) 1997-08-25 2001-05-22 Bristol-Myers Squibb Co. Imidazoquinoxaline protein tyrosine kinase inhibitors
UA71555C2 (en) 1997-10-06 2004-12-15 Zentaris Gmbh Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives
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
CA2393896A1 (en) 1999-09-15 2001-03-22 Warner-Lambert Company Pteridinones as kinase inhibitors
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
EP1458383B1 (en) 2001-12-18 2007-11-21 Merck & Co., Inc. Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5
US7402585B2 (en) 2001-12-24 2008-07-22 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
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
US7208493B2 (en) 2002-10-03 2007-04-24 Targegen, Inc. Vasculostatic agents and methods of use thereof
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
ATE433967T1 (de) 2003-01-17 2009-07-15 Warner Lambert Co 2-aminopyridin-substituierteheterocyclen als inhibitoren der zellulären proliferation
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
US7244739B2 (en) 2003-05-14 2007-07-17 Torreypines Therapeutics, Inc. Compounds and uses thereof in modulating amyloid beta
NZ544112A (en) 2003-05-23 2010-01-29 Zentaris Gmbh Novel pyridopyrazines and use thereof as kinase modulators
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
AU2004259000A1 (en) 2003-07-21 2005-02-03 Bethesda Pharmaceuticals, Inc. Design and synthesis of optimized ligands for PPAR
EP1651631A1 (en) 2003-08-01 2006-05-03 Genelabs Technologies, Inc. Bicyclic imidazol derivatives against flaviviridae
PL1673092T3 (pl) 2003-10-17 2008-01-31 4 Aza Ip Nv Pochodne pterydyny podstawione heterocyklem i ich zastosowanie w leczeniu
AU2004288709B2 (en) 2003-11-07 2011-01-06 Novartis Vaccines And Diagnostics, Inc. Methods for synthesizing quinolinone compounds
AU2004295058B9 (en) 2003-11-20 2011-06-30 Janssen Pharmaceutica N.V. 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(ADP-ribose) polymerase inhibitors
WO2005054231A1 (en) 2003-11-24 2005-06-16 F.Hoffmann-La Roche Ag Pyrazolyl and imidazolyl pyrimidines
EP2228369A1 (en) 2003-12-23 2010-09-15 Astex Therapeutics Ltd. Pyrazole derivatives as protein kinase modulators
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
NZ553087A (en) 2004-08-31 2010-12-24 Astrazeneca Ab Quinazolinone derivatives and their use as B-raf inhibitors
EP1805174A1 (en) 2004-10-14 2007-07-11 F.Hoffmann-La Roche Ag 1,5-naphthyridine azolidinones having cdk1 antiproliferative activity
WO2006040568A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as b raf inhibitors
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
JP2008530030A (ja) 2005-02-14 2008-08-07 バイオノミックス リミテッド 新規なチューブリン重合阻害剤
EP1853261B1 (de) 2005-03-03 2017-01-11 Universität des Saarlandes Selektive hemmstoffe humaner corticoidsynthasen
EP1881986A2 (en) 2005-05-12 2008-01-30 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1881981A1 (en) 2005-05-18 2008-01-30 Wyeth 4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of tpl2 kinase and methods of making and using the same
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
CN101296909B (zh) 2005-08-26 2011-10-12 默克雪兰诺有限公司 吡嗪衍生物及其作为pi3k抑制剂的应用
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
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
MY159523A (en) 2005-12-21 2017-01-13 Janssen Pharmaceutica Nv Triazolopyridazines as tyrosine kinase modulators
WO2007125405A2 (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
WO2007135027A1 (de) 2006-05-24 2007-11-29 Boehringer Ingelheim International Gmbh Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
TWI398252B (zh) 2006-05-26 2013-06-11 Novartis Ag 吡咯并嘧啶化合物及其用途
WO2008003702A2 (en) 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg Fused bicyclic compounds interacting with the histamine h4 receptor
EP2081928B1 (en) 2006-11-10 2014-02-26 Bristol-Myers Squibb Company Pyrrolo-pyridine kinase inhibitors
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
CA2672828A1 (en) 2006-12-13 2008-06-26 Schering Corporation Methods of treatment
BRPI0720695A2 (pt) 2006-12-21 2014-02-18 Plexxikon Inc Compostos e métodos para modulação de cinase, e indicações para estes
EA200900819A1 (ru) 2006-12-22 2010-02-26 Новартис Аг Хиназолины для ингибирования pdk1
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
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
EP2150255A4 (en) * 2007-05-10 2011-10-05 Glaxosmithkline Llc CHINOXALINE DERIVATIVES AS P13 KINASE INHIBITORS
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
CN101784520B (zh) 2007-06-20 2014-07-02 田边三菱制药株式会社 磺酰基丙二酰胺衍生物和其药物用途
JP5548123B2 (ja) 2007-06-21 2014-07-16 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 6−{ジフルオロ[6−(1−メチル−1H−ピラゾル−4−イル)[1,2,4]トリアゾロ[4,3−b]ピリダジン−3−イル]メチル}キノリンの多形および水和物の形態、塩、ならびに製造方法
WO2009009016A1 (en) 2007-07-06 2009-01-15 Osi Pharmaceuticals, Inc. Combination anti-cancer therapy
US7981903B2 (en) 2007-08-08 2011-07-19 Glaxosmithkline Llc 2-[2-{phenylamino}-1H-pyrrolo[2,3-D]pyrimidin-4-yl)amino] benzamide derivatives as IGF-1R inhibitors for the treatment of cancer
EP2173354A4 (en) * 2007-08-09 2011-10-05 Glaxosmithkline Llc CHINOXALIN DERIVATIVES AS PI3 KINASE INHIBITORS
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
KR101580482B1 (ko) 2007-11-16 2015-12-28 인사이트 홀딩스 코포레이션 야누스 키나제 억제제로서의 4-피라졸릴-n-아릴피리미딘-2-아민 및 4-피라졸릴-n-헤테로아릴피리미딘-2-아민
CA2722992A1 (en) 2008-05-05 2009-11-12 Schering Corporation Sequential administration of chemotherapeutic agents for treatment of cancer
GEP20125502B (en) 2008-05-23 2012-04-25 Novartis Ag Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
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
AU2010206161B2 (en) 2009-01-21 2014-08-07 Basilea Pharmaceutica Ag Novel bicyclic antibiotics
US20110288090A1 (en) 2009-02-02 2011-11-24 Armstrong Donna J Inhibitors of AKT Activity
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
MX353776B (es) 2009-06-12 2018-01-29 Abivax Compuestos utiles para tratar cancer.
EP2473504B1 (en) 2009-09-03 2015-02-25 Bioenergenix Heterocyclic compounds for the inhibition of pask
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
CN110269856A (zh) 2010-03-30 2019-09-24 维颂公司 多取代芳族化合物作为凝血酶的抑制剂
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
CN103153062B (zh) 2010-05-24 2015-07-15 因特利凯有限责任公司 杂环化合物及其用途
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
US8987257B2 (en) 2011-01-31 2015-03-24 Novartis Ag Heterocyclic derivatives
WO2012106556A2 (en) 2011-02-02 2012-08-09 Amgen Inc. Methods and compositons relating to inhibition of igf-1r
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
JP2014519813A (ja) 2011-04-25 2014-08-21 オーエスアイ・ファーマシューティカルズ,エルエルシー 癌薬剤発見、診断、および治療におけるemt遺伝子シグネチャーの使用
WO2013032951A1 (en) 2011-08-26 2013-03-07 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2755657B1 (en) 2011-09-14 2017-11-29 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2757885B1 (en) 2011-09-21 2017-03-15 Neupharma, Inc. Certain chemical entites, compositions, and methods
WO2013052699A2 (en) 2011-10-04 2013-04-11 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
PT2771342T (pt) 2011-10-28 2016-08-17 Novartis Ag Derivados de purina e o seu uso no tratamento de doença
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
GB201118654D0 (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
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
HK1205528A1 (en) 2012-03-08 2015-12-18 Astellas Pharma Inc. Novel fgfr3 fusion product
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
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
EP3939614A1 (en) 2013-01-18 2022-01-19 Foundation Medicine, Inc. Methods of treating cholangiocarcinoma
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
US10028956B2 (en) 2013-08-02 2018-07-24 Ignyta, Inc. Methods of treating various cancers using an AXL/cMET inhibitor in combination with other agents
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
CA2943687C (en) 2014-03-26 2024-02-13 Astex Therapeutics Ltd Combinations of an fgfr inhibitor and an igf1r inhibitor
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
JO3512B1 (ar) * 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
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
US20160243228A1 (en) 2015-02-19 2016-08-25 Bioclin Therapeutics, Inc. Methods, compositions, and kits for treatment of cancer
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer

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