AR090161A1 - Derivados heterociclicos nitrogenados con accion sobre el cancer de vejiga - Google Patents

Derivados heterociclicos nitrogenados con accion sobre el cancer de vejiga

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Publication number
AR090161A1
AR090161A1 ARP130100588A ARP130100588A AR090161A1 AR 090161 A1 AR090161 A1 AR 090161A1 AR P130100588 A ARP130100588 A AR P130100588A AR P130100588 A ARP130100588 A AR P130100588A AR 090161 A1 AR090161 A1 AR 090161A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
lower alkyl
aromatic heterocyclic
heterocyclic group
aromatic
Prior art date
Application number
ARP130100588A
Other languages
English (en)
Inventor
Iikubo Kazuhiko
Hisamichi Hiroyuki
Kawamoto Yuichiro
Moritomo Hiroyuki
Suzuki Tomoyuki
Futami Takashi
Suzuki Atsushi
Tsunoyama Kazuhisa
Asaumi Makoto
Tomiyama Hiroshi
Noda Atsushi
Iwai Yoshinori
Tokuzaki Kazuo
Okada Haruki
Miyasaka Kozo
Kameda Minoru
Kuriwaki Ikumi
Original Assignee
Astellas Pharma Inc
Kotobuki Pharmaceutical Co 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 Astellas Pharma Inc, Kotobuki Pharmaceutical Co Ltd filed Critical Astellas Pharma Inc
Publication of AR090161A1 publication Critical patent/AR090161A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D403/02—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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

Se proporciona un compuesto como un agente preventivo y/o terapéutico para el cáncer de vejiga. Como resultado de estudios en compuestos que tienen una acción inhibidora de FGFR, los compuestos heterocíclicos aromáticos que contienen nitrógeno de la presente tienen una acción inhibidora sobre FGFR1, FGFR2 y/o FGFR3, en particular, FGFR3 mutante. El compuesto heterocíclico aromático que contiene nitrógeno se puede usar en forma de un agente terapéutico para diversos cánceres relacionados con FGFR1, FGFR2 y/o FGFR3, tales como cáncer de pulmón y cáncer de mama resistente a terapia hormonal, cáncer de estómago, cáncer de mama triple negativo, cáncer de endometrio, cáncer de vejiga y glioblastoma, en particular como un agente preventivo y/o terapéutico para cáncer de vejiga FGFR3-positivo mutante. Reivindicación 1: Un compuesto de la fórmula (1) o a su sal, (caracterizado porque X e Y, iguales o diferentes entre sí, son CH o N, siempre que X e Y no sean simultáneamente N; L¹ es -alquileno inferior-, -alquileno inferior-O-, -O-alquileno inferior- o -alquinileno inferior-; Z es N o CH; R¹, iguales o diferentes entre sí, son alquilo inferior opcionalmente sustituido con halógeno, -O-(alquilo inferior opcionalmente sustituido con halógeno), halógeno, ciano o -N(alquilo inferior)₂; p es un número entero de 2 a 4; anillo W es un anillo carbocíclico aromático opcionalmente sustituido, un anillo heterocíclico aromático opcionalmente sustituido o un anillo heterocíclico no aromático opcionalmente sustituido; Q es -L²-R² o R³; L² es un anillo heterocíclico aromático opcionalmente sustituido o un anillo heterocíclico no aromático opcionalmente sustituido; R² es un grupo heterocíclico no aromático opcionalmente sustituido con alquilo inferior, cicloalquilo opcionalmente sustituido, alquilo inferior opcionalmente sustituido con uno o varios grupos seleccionados del grupo que consiste en -OH y -O-alquilo inferior, -C(O)-R⁰, -C(O)-cicloalquilo opcionalmente sustituido, -NH-R⁰, -N(alquilo inferior)-R⁰, un grupo -L³-heterocíclico no aromático opcionalmente sustituido o H; R⁰ es alquilo inferior opcionalmente sustituido con -OH; R³ es (i) alquilo inferior opcionalmente sustituido con uno o varios grupos seleccionados del grupo que consiste en -C(O)OH, -OH, -O-R⁰, amino opcionalmente sustituido con uno o dos R⁰, carbamoilo opcionalmente sustituido con uno o dos R⁰, un grupo heterocíclico aromático opcionalmente sustituido, un grupo heterocíclico no aromático opcionalmente sustituido y un grupo -C(O)-heterocíclico no aromático opcionalmente sustituido; (ii) -O-(alquilo inferior opcionalmente sustituido con uno o varios grupos seleccionados del grupo que consiste en -C(O)OH, -OH, -O-R⁰, carbamoilo opcionalmente sustituido con uno o dos R⁰, un grupo heterocíclico no aromático opcionalmente sustituido y un grupo -C(O)-heterocíclico no aromático opcionalmente sustituido); (iii) -NH-(alquilo inferior opcionalmente sustituido con uno o varios grupos seleccionados del grupo que consiste en -OH, un grupo heterocíclico no aromático opcionalmente sustituido con alquilo inferior y carbamoilo opcionalmente sustituido con uno o dos R⁰); (iv) -N(alquilo inferior)-(alquilo inferior opcionalmente sustituido con uno o varios grupos seleccionados del grupo que consiste en -OH, un grupo heterocíclico no aromático opcionalmente sustituido con alquilo inferior y carbamoilo opcionalmente sustituido con uno o dos R⁰); (v) -C(O)OH; (vi) grupo -C(O)-heterocíclico no aromático opcionalmente sustituido; (vii) -O-(un grupo heterocíclico no aromático opcionalmente sustituido con alquilo inferior); o (viii) carbamoilo opcionalmente sustituido con uno o dos R⁰; y L³ es un enlace, -NH-, -N(alquilo inferior)- o alquileno inferior).
ARP130100588A 2012-02-28 2013-02-26 Derivados heterociclicos nitrogenados con accion sobre el cancer de vejiga AR090161A1 (es)

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JP2012042065 2012-02-28

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US (2) US9464077B2 (es)
EP (1) EP2821402B1 (es)
JP (1) JP5343177B1 (es)
KR (1) KR102032007B1 (es)
CN (1) CN104144915B (es)
AR (1) AR090161A1 (es)
AU (2) AU2013227139B2 (es)
BR (1) BR112014018868B1 (es)
CA (1) CA2866611C (es)
EA (1) EA026953B1 (es)
ES (1) ES2746288T3 (es)
HK (1) HK1203201A1 (es)
IL (1) IL234313A (es)
MX (1) MX349120B (es)
PH (1) PH12014501925A1 (es)
PL (1) PL2821402T3 (es)
PT (1) PT2821402T (es)
TW (1) TWI542581B (es)
UA (1) UA114501C2 (es)
WO (1) WO2013129369A1 (es)
ZA (1) ZA201406201B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2865388C (en) 2012-03-08 2022-01-04 Astellas Pharma Inc. Novel fgfr3 fusion
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
JP6382194B2 (ja) * 2012-07-24 2018-08-29 ザ トラスティーズ オブ コロンビア ユニバーシティ イン ザ シティ オブ ニューヨーク 融合タンパク質およびその方法
EP2902489B9 (en) * 2012-09-27 2018-02-07 Chugai Seiyaku Kabushiki Kaisha Fgfr3 fusion gene and pharmaceutical drug targeting same
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
WO2014139145A1 (en) 2013-03-15 2014-09-18 Hutchison Medipharma Limited Novel pyrimidine and pyridine compounds and usage thereof
TW201605452A (zh) * 2013-08-28 2016-02-16 安斯泰來製藥股份有限公司 以嘧啶化合物作爲有效成分之醫藥組成物
UA116920C2 (uk) 2013-10-18 2018-05-25 ЕЙСАЙ Ар ЕНД Ді МЕНЕДЖМЕНТ КО., ЛТД. Інгібітори fgfr4
EA028614B1 (ru) * 2014-05-22 2017-12-29 Общество С Ограниченной Ответственностью "Русские Фармацевтические Технологии" Селективные ингибиторы, нарушающие взаимодействие рецептора фактора роста фибробластов и frs2, для профилактики и лечения рака
MX369646B (es) 2014-08-18 2019-11-15 Eisai R&D Man Co Ltd Sal de derivado de piridina monociclico y su cristal.
CN113957146A (zh) * 2014-09-26 2022-01-21 詹森药业有限公司 使用fgfr突变基因组鉴定将对用fgfr抑制剂进行治疗有反应的癌症患者
MX2017013248A (es) 2015-04-14 2018-07-06 Eisai R&D Man Co Ltd Compuesto del inhibidor fgfr4 cristalino y usos del mismo.
CN104940748A (zh) * 2015-06-09 2015-09-30 林正兴 一种治疗胃癌的药物组合物
CN106928275B (zh) * 2015-12-29 2020-10-02 齐鲁制药有限公司 螺环胺类芳基磷氧化合物的制备方法及其中间体和晶型
US11357769B2 (en) 2016-05-10 2022-06-14 Eisai R&D Management Co., Ltd. Drug combinations for reducing cell viability and/or cell proliferation
US10654836B2 (en) * 2016-05-20 2020-05-19 Zhejiang Hisun Pharmaceutical Co., Ltd. Pyrimidine derivative, method for preparing same and use thereof in medicine
CN111247150B (zh) 2017-08-15 2022-11-08 石药集团中奇制药技术（石家庄）有限公司 Fgfr抑制剂及其医药用途
JPWO2019189241A1 (ja) 2018-03-28 2021-03-18 エーザイ・アール・アンド・ディー・マネジメント株式会社 肝細胞癌治療剤
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
AU2021416682B2 (en) * 2021-01-11 2024-01-11 Guangzhou Salustier Biosciences Co., Ltd. 2-aminopyrimidine compound and pharmaceutical composition thereof and application thereof
CN112851587A (zh) * 2021-01-21 2021-05-28 药雅科技(上海)有限公司 一种用于治疗癌症的炔类杂环化合物及其制备方法与用途

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA04007637A (es) 2002-02-08 2004-11-10 Smithkline Beecham Corp Compuestos de pirimidina.
WO2005002673A1 (en) * 2003-07-03 2005-01-13 Astex Therapeutics Limited Raf kinase inhibitors
EP1863794A2 (en) * 2005-03-16 2007-12-12 Targegen, Inc. Pyrimidine compounds and methods of use
US7754717B2 (en) 2005-08-15 2010-07-13 Amgen Inc. Bis-aryl amide compounds and methods of use
US20070161645A1 (en) 2005-11-02 2007-07-12 Targegen, Inc. Thiazole inhibitors targeting resistant kinase mutations
BRPI0620408B8 (pt) 2005-12-21 2021-05-25 Novartis Ag derivados de pirimidinil aril uréia sendo inibidores de fgf, seus usos, e preparação farmacêutica
US8030487B2 (en) * 2006-07-07 2011-10-04 Targegen, Inc. 2-amino—5-substituted pyrimidine inhibitors
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
ES2364864T3 (es) 2006-12-21 2011-09-15 Astrazeneca Ab Acilaminopirazoles como inhibidores de fgfr.
EP2195312B1 (en) 2007-10-09 2012-11-21 Merck Patent GmbH Pyridine derivatives useful as glucokinase activators
WO2009056886A1 (en) * 2007-11-01 2009-05-07 Astrazeneca Ab Pyrimidine derivatives and their use as modulators of fgfr activity
CN102123989A (zh) 2008-06-19 2011-07-13 阿斯利康(瑞典)有限公司 吡唑化合物436

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