LT3590934T - Pirazolilchinoksalino kinazės inhibitoriai - Google Patents

Pirazolilchinoksalino kinazės inhibitoriai

Info

Publication number
LT3590934T
LT3590934T LTEP19175481.1T LT19175481T LT3590934T LT 3590934 T LT3590934 T LT 3590934T LT 19175481 T LT19175481 T LT 19175481T LT 3590934 T LT3590934 T LT 3590934T
Authority
LT
Lithuania
Prior art keywords
kinase inhibitors
pyrazolyl
quinoxaline kinase
pyrazolyl quinoxaline
quinoxaline
Prior art date
Application number
LTEP19175481.1T
Other languages
English (en)
Lithuanian (lt)
Inventor
Gordon Saxty
Christopher William Murray
Valerio Berdini
Gilbert Ebai Besong
Christopher Charles Frederick Hamlett
Christopher Norbert Johnson
Steven John Woodhead
Michael Reader
David Charles Rees
Laurence Anne Mevellec
Patrick René Angibaud
Eddy Jean Edgard Freyne
Tom Cornelis Hortense Govaerts
Johan Erwin Edmond Weerts
Timothy Pietro Suren Perera
Ronaldus Arnodus Hendrika Joseph Gilissen
Berthold Wroblowski
Jean Fernand Armand Lacrampe
Alexandra Papanikos
Olivier Alexis Georges Querolle
Elisabeth Thérèse Jeanne PASQUIER
Isabelle Noëlle Constance PILATTE
Pascal Ghislain Andre Bonnet
Werner Constant Johan Embrechts
Rhalid Akkari
Lieven Meerpoel
Original Assignee
Astex Therapeutics Limited
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 Limited filed Critical Astex Therapeutics Limited
Publication of LT3590934T publication Critical patent/LT3590934T/lt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6524—Heterocyclic 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Otolaryngology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
LTEP19175481.1T 2010-04-30 2011-04-28 Pirazolilchinoksalino kinazės inhibitoriai LT3590934T (lt)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
LT3590934T true LT3590934T (lt) 2021-12-27

Family

ID=42289929

Family Applications (4)

Application Number Title Priority Date Filing Date
LTEP16207610.3T LT3178818T (lt) 2010-04-30 2011-04-28 Pirazolilo chinoksalino kinazės inhibitoriai
LTEP19175481.1T LT3590934T (lt) 2010-04-30 2011-04-28 Pirazolilchinoksalino kinazės inhibitoriai
LTEP11724710.6T LT2563775T (lt) 2010-04-30 2011-04-28 Pirazolilo chinoksalino kinazės inhibitoriai
LTPA2025509C LTPA2025509I1 (OSRAM) 2010-04-30 2025-02-17

Family Applications Before (1)

Application Number Title Priority Date Filing Date
LTEP16207610.3T LT3178818T (lt) 2010-04-30 2011-04-28 Pirazolilo chinoksalino kinazės inhibitoriai

Family Applications After (2)

Application Number Title Priority Date Filing Date
LTEP11724710.6T LT2563775T (lt) 2010-04-30 2011-04-28 Pirazolilo chinoksalino kinazės inhibitoriai
LTPA2025509C LTPA2025509I1 (OSRAM) 2010-04-30 2025-02-17

Country Status (41)

Country Link
US (6) US8895601B2 (OSRAM)
EP (3) EP2563775B1 (OSRAM)
JP (1) JP5639261B2 (OSRAM)
KR (2) KR101933843B1 (OSRAM)
CN (2) CN104725362B (OSRAM)
AP (1) AP3210A (OSRAM)
AR (1) AR080982A1 (OSRAM)
AU (2) AU2011247047B2 (OSRAM)
BR (1) BR112012027509B1 (OSRAM)
CA (1) CA2796204C (OSRAM)
CL (1) CL2012003048A1 (OSRAM)
CR (2) CR20180339A (OSRAM)
CY (2) CY1121882T1 (OSRAM)
DK (3) DK2563775T3 (OSRAM)
EA (2) EA023222B8 (OSRAM)
EC (1) ECSP12012318A (OSRAM)
ES (3) ES2899937T3 (OSRAM)
FI (1) FIC20250009I1 (OSRAM)
FR (1) FR25C1006I1 (OSRAM)
GB (1) GB201007286D0 (OSRAM)
HR (1) HRP20211675T1 (OSRAM)
HU (4) HUE056999T2 (OSRAM)
IL (1) IL222600A (OSRAM)
IN (1) IN2012MN02591A (OSRAM)
JO (1) JO3366B1 (OSRAM)
LT (4) LT3178818T (OSRAM)
ME (1) ME01825B (OSRAM)
MX (2) MX2012012414A (OSRAM)
MY (2) MY189427A (OSRAM)
NL (1) NL301318I2 (OSRAM)
NO (1) NO2025011I1 (OSRAM)
NZ (1) NZ602726A (OSRAM)
PH (1) PH12012501993A1 (OSRAM)
PL (3) PL3178818T3 (OSRAM)
PT (3) PT2563775T (OSRAM)
RS (3) RS62570B1 (OSRAM)
SG (2) SG10201708578QA (OSRAM)
SI (3) SI3178818T1 (OSRAM)
SM (3) SMT201900469T1 (OSRAM)
TW (1) TWI545122B (OSRAM)
WO (1) WO2011135376A1 (OSRAM)

Families Citing this family (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ579355A (en) 2007-02-01 2012-03-30 Resverlogix Corp 2-(Aryl)-4-oxo-quinazoline derivatives
NZ708314A (en) 2009-03-18 2017-08-25 Resverlogix Corp Quinazolinones for use as anticancer agents
ES2821018T3 (es) 2009-04-22 2021-04-23 Resverlogix Corp Nuevos agentes antiinflamatorios
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
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
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
ES2832497T3 (es) 2012-06-13 2021-06-10 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
US8802697B2 (en) 2012-07-11 2014-08-12 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
WO2014060852A2 (en) * 2012-10-15 2014-04-24 Resverlogix Corp. Compounds useful in the synthesis of benzamide compounds
WO2014071419A2 (en) 2012-11-05 2014-05-08 Foundation Medicine, Inc. Novel fusion molecules and uses thereof
AU2013337277B2 (en) 2012-11-05 2018-03-08 Foundation Medicine, Inc. Novel NTRK1 fusion molecules and uses thereof
US9719970B2 (en) 2012-11-30 2017-08-01 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
AU2014207342C1 (en) 2013-01-18 2019-04-04 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
MY181020A (en) 2013-03-15 2020-12-16 Sanofi Sa Heteroaryl compounds and uses thereof
WO2014144737A1 (en) * 2013-03-15 2014-09-18 Celgene Avilomics Research, Inc. 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
PT3395814T (pt) 2013-10-25 2022-07-27 Blueprint Medicines Corp Inibidores do recetor do fator de crescimento de fibroblastos
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
MX373150B (es) 2014-03-26 2020-04-21 Astex Therapeutics Ltd Combinaciones de un inhibidor del factor de crecimiento de fibroblasto (fgfr) y un inhibidor del receptor del factor de crecimiento 1 similar a insulina (igf1r).
US10085982B2 (en) 2014-03-26 2018-10-02 Astex Therapeutics Ltd Combinations
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
CA2956270C (en) 2014-08-18 2022-08-09 Eisai R&D Management Co., Ltd. Salt of monocyclic pyridine derivative and crystal thereof
RS63178B1 (sr) * 2014-09-26 2022-06-30 Janssen Pharmaceutica Nv Upotreba fgfr mutantnih genskih panela u identifikovanju pacijenata sa karcinomom koji će reagovati na lečenje sa inhibitorom fgfr
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
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3617205B1 (en) 2015-02-20 2021-08-04 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2016147053A1 (en) 2015-03-13 2016-09-22 Resverlogix Corp. Compositions and therapeutic methods for the treatment of complement-associated diseases
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
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
BR112018005637B1 (pt) * 2015-09-23 2023-11-28 Janssen Pharmaceutica Nv Compostos derivados de quinoxalina, quinolina e quinazolinona,composições farmacêuticas que os compreende, e uso dos referidos compostos
CN108137546B (zh) * 2015-09-23 2021-07-27 詹森药业有限公司 双杂芳基取代的1,4-苯并二氮杂卓化合物及其用于治疗癌症的用途
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
AU2017342928B2 (en) * 2016-10-10 2021-09-09 Development Center For Biotechnology Quinoxaline compounds as type III receptor tyrosine kinase inhibitors
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
EP3716978B1 (en) 2017-12-01 2023-08-16 Board of Regents of the University of Nebraska N-(phenyl)-n'-(6-quinoxalinyl)-urea derivatives as ikkb inhibitors for the treatment of cancer
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
KR102308134B1 (ko) * 2018-04-26 2021-10-01 재단법인 의약바이오컨버젼스연구단 mTOR 저해제로서의 신규 화합물 및 이의 용도
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
JP2021523121A (ja) 2018-05-04 2021-09-02 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｆｇｆｒ阻害剤の固体形態及びその調製プロセス
MX2021003320A (es) 2018-09-21 2021-05-14 Janssen Pharmaceutica Nv Tratamiento del colangiocarcinoma.
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
WO2020131627A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
JP7747521B2 (ja) 2019-03-29 2025-10-01 ヤンセン ファーマシューティカ エヌ．ベー． 尿路上皮癌の治療のためのｆｇｆｒチロシンキナーゼ阻害剤
SG11202109854RA (en) 2019-03-29 2021-10-28 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
WO2021007269A1 (en) 2019-07-09 2021-01-14 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
JP7709959B2 (ja) 2019-09-26 2025-07-17 ヤンセン ファーマシューティカ エヌ．ベー． 連続的な治療設定における免疫チェックポイント阻害剤に対する患者の応答を高めるためのｆｇｆｒ遺伝子改変癌におけるｆｇｆｒ阻害剤の使用
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11607416B2 (en) 2019-10-14 2023-03-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 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
JP2023505257A (ja) 2019-12-04 2023-02-08 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
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
WO2021146163A1 (en) * 2020-01-17 2021-07-22 Beta Pharma, Inc. Pyridazine and 1,2,4-triazine derivatives as fgfr kinase inhibitors
KR20220140781A (ko) 2020-02-12 2022-10-18 얀센 파마슈티카 엔.브이. 고위험 비근침윤성 방광암 치료를 위한 fgfr 티로신 키나제 억제제
CN115087446A (zh) 2020-02-12 2022-09-20 詹森药业有限公司 用于治疗尿路上皮癌的fgfr酪氨酸激酶抑制剂和抗pd1药剂
WO2022040111A2 (en) 2020-08-17 2022-02-24 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
US20230321087A1 (en) 2020-09-14 2023-10-12 Janssen Pharmaceutica Nv 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
MX2023013802A (es) 2021-05-19 2023-12-06 Janssen Pharmaceutica Nv Inhibidores de tirosina quinasa de fgfr para el tratamiento de tumores solidos avanzados.
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
TW202313610A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之三環雜環
US20240382483A1 (en) 2021-06-22 2024-11-21 Blueprint Medicines Corporation Heterocyclic egfr inhibitors for use in the treatment of cancer
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
JP2024540411A (ja) 2021-11-08 2024-10-31 プロジェントス・セラピューティクス・インコーポレイテッド 血小板由来成長因子受容体（ｐｄｇｆｒ）アルファ阻害剤及びその使用
EP4479055A1 (en) * 2022-02-18 2024-12-25 TARIS Biomedical LLC Erdafitinib formulations and osmotic systems for intravesical administration
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
WO2024170495A1 (en) 2023-02-13 2024-08-22 Janssen Pharmaceutica Nv Fgfr tyrosine kinase inhibitors for the treatment of high-risk non-muscle invasive bladder cancer
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
JPH09500615A (ja) 1993-05-14 1997-01-21 ジェネンテク，インコーポレイテッド Ｒａｓ−ファルネシル転移酵素阻害剤
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
CA2262403C (en) 1995-07-31 2011-09-20 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
ATE500233T1 (de) 1997-05-28 2011-03-15 Aventis Pharma Inc Chinolin und chinoxalinverbindungen die den von blutplättchen abstammenden faktor und/oder p56ick-tyrosinkinase hemmen
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
EP1147094A1 (en) 1999-01-15 2001-10-24 Novo Nordisk A/S Non-peptide glp-1 agonists
CZ2002846A3 (cs) 1999-09-15 2003-02-12 Warner-Lambert Company Pteridinony, jako inhibitory kinasy
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
AU2002359714B2 (en) 2001-12-18 2006-12-21 Merck Sharp & Dohme Corp. Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5
MXPA04006260A (es) 2001-12-24 2005-03-31 Astrazeneca Ab Derivados de quinazolina sustituidos como inhibidores de cinasas aurora.
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
JP4394960B2 (ja) 2002-04-08 2010-01-06 メルク エンド カムパニー インコーポレーテッド Ａｋｔ活性阻害薬
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
CA2500727A1 (en) 2002-10-03 2004-04-15 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
DE602004021558D1 (de) 2003-01-17 2009-07-30 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
JP4847868B2 (ja) 2003-05-14 2011-12-28 ニューロジェネティック ファーマシューティカルズ、 インコーポレイテッド 化合物、及び、アミロイドベータの調節におけるその使用
HRP20090036T3 (en) 2003-05-23 2009-03-31 Æterna 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
WO2005009437A1 (en) 2003-07-21 2005-02-03 Bethesda Pharmaceuticals, Inc. 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
DK1673092T3 (da) 2003-10-17 2007-12-17 4 Aza Ip Nv Heterocyklylsubstituerede pteridinderivater og anvendelsen deraf i terapi
JP4724665B2 (ja) 2003-11-07 2011-07-13 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド キノリノン化合物を合成する方法
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
EP1689740A1 (en) 2003-11-24 2006-08-16 F.Hoffmann-La Roche Ag Pyrazolyl and imidazolyl pyrimidines
JP4928949B2 (ja) * 2003-12-23 2012-05-09 アステックス、セラピューティックス、リミテッド タンパク質キナーゼモジュレーターとしてのピラゾール誘導体
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
AU2005293835A1 (en) 2004-10-14 2006-04-20 F. Hoffmann-La Roche Ag 1,5-Naphthyridine azolidinones having CDK1 antiproliferative activity
CA2583096A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as b raf inhibitors
HRP20130738T1 (hr) 2004-12-24 2013-10-25 Spinifex Pharmaceuticals Pty Ltd Postupak lijeäśenja ili profilakse
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
WO2006092430A1 (de) 2005-03-03 2006-09-08 Universität des Saarlandes Selektive hemmstoffe humaner corticoidsynthasen
JP2008540535A (ja) 2005-05-12 2008-11-20 メルク エンド カムパニー インコーポレーテッド チロシンキナーゼ阻害剤
MX2007014258A (es) 2005-05-18 2008-01-22 Wyeth Corp Inhibidores de 4,6-diamino-[1,7]naftiridin-3-carbonitrilo de la tpl2 cinasa y metodos de fabricacion y uso de los mismos.
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
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
EP1957487A1 (de) 2005-11-11 2008-08-20 AEterna Zentaris GmbH Neue pyridopyrazine und deren verwendung als modulatoren von kinasen
MX2008008277A (es) 2005-12-21 2009-03-04 Janssen Pharmaceutica Nv Triazolopiridazinas como moduladores de tirosina cinasa.
JP2009535393A (ja) 2006-05-01 2009-10-01 ファイザー・プロダクツ・インク 置換２−アミノ縮合複素環式化合物
GB0609621D0 (en) 2006-05-16 2006-06-21 Astrazeneca Ab Novel co-crystal
EP2029600B1 (de) 2006-05-24 2012-03-14 Boehringer Ingelheim International GmbH Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
JP2009541460A (ja) 2006-07-03 2009-11-26 ベレナギング ヴォー クリスタラク ホガー オンダーヴェイル ヴェーテンザパーリク オンダージーク エン パシェンテンゾーク ヒスタミンｈ４受容体と相互作用する縮合二環式化合物
JP5244118B2 (ja) 2006-11-10 2013-07-24 ブリストル−マイヤーズ スクイブ カンパニー 新規キナーゼ阻害剤
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
AU2007334456A1 (en) 2006-12-13 2008-06-26 Merck Sharp & Dohme Corp. Methods of cancer treatment with IGF1R inhibitors
MX2009006688A (es) 2006-12-21 2009-06-30 Plexxikon Inc Compuestos y metodos para modulacion de cinasas, e indicaciones para ello.
AU2007336893A1 (en) 2006-12-22 2008-07-03 Novartis Ag Quinazolines for PDK1 inhibition
EP2114941B1 (en) * 2006-12-22 2015-03-25 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
CL2008001356A1 (es) 2007-05-10 2008-11-14 Smithkline Beecham Corp Compuestos derivados de quinoxalina, inhibidores de la pi3 quinasa _(p13ka, pi3ko, pi3b y/o pi3ky); composicion farmaceutica; uso para tratar un trastorno autoinmune, enfermedad inflamatoria, cardiovascular, neurodegerativa, alergia, asma, enfermedad renal, cancer, rechazo de transplante, lesiones pulmonares.
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
WO2008150827A1 (en) 2007-05-29 2008-12-11 Smithkline Beecham Corporation Naphthyridine, derivatives as p13 kinase inhibitors
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
KR101251933B1 (ko) 2007-06-20 2013-04-09 미쓰비시 타나베 파마 코퍼레이션 신규한 말론산술폰아미드 유도체 및 그 의약 용도
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
EP2173338A1 (en) 2007-07-06 2010-04-14 OSI Pharmaceuticals, Inc. Combination anti-cancer therapy
AR068054A1 (es) 2007-08-08 2009-11-04 Smithkline Beecham Corp Compuestos de pirrolopirimidina
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
UA104849C2 (uk) 2007-11-16 2014-03-25 Інсайт Корпорейшн 4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus
US20110129456A1 (en) 2008-05-05 2011-06-02 Yaolin Wang Sequential Administration of Chemotherapeutic Agents for Treatment of Cancer
KR101257158B1 (ko) 2008-05-23 2013-04-23 노파르티스 아게 단백질 티로신 키나제 억제제로서의 퀴놀린 및 퀴녹살린의 유도체
US8592448B2 (en) 2008-11-20 2013-11-26 OSI Pharmaceuticals, LLC Substituted pyrrolo[2,3-b]-pyridines and -pyrazines
US8716280B2 (en) 2009-01-21 2014-05-06 Basilea Pharmaceutica Ag Bicyclic antibiotics
JP2012516847A (ja) 2009-02-02 2012-07-26 メルク・シャープ・エンド・ドーム・コーポレイション Ａｋｔ活性の阻害剤
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
US9145367B2 (en) 2009-06-12 2015-09-29 Abivax Compounds useful for treating AIDS
CN102656163B (zh) 2009-09-03 2016-01-13 拜奥埃内杰尼克斯公司 抑制pask的杂环化合物
JP5728683B2 (ja) 2009-09-04 2015-06-03 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ チロシンスレオニンキナーゼ阻害剤としての置換アミノキノキサリン
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
CA2829790C (en) 2010-03-30 2018-06-05 Verseon Corporation 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
EP2575462B1 (en) 2010-05-24 2016-06-22 Intellikine, LLC 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
ES2611885T3 (es) 2011-01-31 2017-05-11 Novartis Ag Derivados heterocíclicos novedosos
AU2012212075A1 (en) 2011-02-02 2013-07-18 Amgen Inc. Methods and compositons relating to inhibition of IGF-1R
CN106619647A (zh) 2011-02-23 2017-05-10 因特利凯有限责任公司 激酶抑制剂的组合及其用途
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
EP2702173A1 (en) 2011-04-25 2014-03-05 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
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
US9518029B2 (en) 2011-09-14 2016-12-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9249110B2 (en) 2011-09-21 2016-02-02 Neupharma, Inc. Substituted quinoxalines as B-raf kinase inhibitors
HK1201065A1 (en) 2011-10-04 2015-08-21 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
PL2771342T3 (pl) 2011-10-28 2016-11-30 Nowe pochodne puryny i ich zastosowanie w leczeniu chorób
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
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
KR20220017512A (ko) 2012-03-08 2022-02-11 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
AU2014207342C1 (en) 2013-01-18 2019-04-04 Foundation Medicine, Inc. Methods of treating cholangiocarcinoma
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
JP2016527274A (ja) 2013-08-02 2016-09-08 イグナイタ インコーポレイテッド ＡＸＬ／ｃＭＥＴ阻害剤を単独または他の薬剤と組み合わせて用いて各種がんを治療する方法
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
MX373150B (es) 2014-03-26 2020-04-21 Astex Therapeutics Ltd Combinaciones de un inhibidor del factor de crecimiento de fibroblasto (fgfr) y un inhibidor del receptor del factor de crecimiento 1 similar a insulina (igf1r).
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
US10085982B2 (en) 2014-03-26 2018-10-02 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
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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