BR112017003312A2 - compostos de indazol como inibidores de fgfr quinase, preparação e uso dos mesmos - Google Patents

compostos de indazol como inibidores de fgfr quinase, preparação e uso dos mesmos

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Publication number
BR112017003312A2
BR112017003312A2 BR112017003312-7A BR112017003312A BR112017003312A2 BR 112017003312 A2 BR112017003312 A2 BR 112017003312A2 BR 112017003312 A BR112017003312 A BR 112017003312A BR 112017003312 A2 BR112017003312 A2 BR 112017003312A2
Authority
BR
Brazil
Prior art keywords
preparation
fgfr kinase
application
kinase inhibitor
indazole compound
Prior art date
Application number
BR112017003312-7A
Other languages
English (en)
Chinese (zh)
Other versions
BR112017003312B1 (pt
Inventor
Geng Meiyu
Liu Lei
Jiang Lei
Huang Min
Zha Chuantao
Ai Jing
Wang Lei
Cao Jianhua
Ding Jian
Original Assignee
Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences
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 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences filed Critical Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences
Publication of BR112017003312A2 publication Critical patent/BR112017003312A2/pt
Publication of BR112017003312B1 publication Critical patent/BR112017003312B1/pt

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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

a presente invenção fornece um composto de indazol como um inibidor de fgfr quinase, preparação e uso do mesmo. especificamente, a presente invenção fornece um composto representado pela fórmula (i), em que as definições de cada grupo são descritas no relatório descritivo. o composto da presente invenção tem boa atividade de inibição de fgfr e pode ser usado na preparação de uma série de remédios para tratar doenças relacionadas à atividade de fgfr quinase.
BR112017003312-7A 2014-08-19 2015-08-19 Compostos de indazol como inibidores de fgfr quinase, preparação e uso dos mesmos BR112017003312B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201410409467 2014-08-19
CN201410409467.1 2014-08-19
CN201510073179 2015-02-11
CN201510073179.8 2015-02-11
PCT/CN2015/087556 WO2016026445A1 (zh) 2014-08-19 2015-08-19 作为fgfr激酶抑制剂的吲唑类化合物及其制备和应用

Publications (2)

Publication Number Publication Date
BR112017003312A2 true BR112017003312A2 (pt) 2018-02-27
BR112017003312B1 BR112017003312B1 (pt) 2023-05-02

Family

ID=55350206

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017003312-7A BR112017003312B1 (pt) 2014-08-19 2015-08-19 Compostos de indazol como inibidores de fgfr quinase, preparação e uso dos mesmos

Country Status (14)

Country Link
US (1) US10562900B2 (pt)
EP (1) EP3184521B1 (pt)
JP (1) JP6445684B2 (pt)
KR (2) KR102022866B1 (pt)
CN (1) CN105524048B (pt)
AU (1) AU2015306561B2 (pt)
BR (1) BR112017003312B1 (pt)
CA (1) CA2958503C (pt)
ES (1) ES2904544T3 (pt)
MX (1) MX2017002206A (pt)
MY (1) MY188447A (pt)
PE (1) PE20170774A1 (pt)
RU (1) RU2719428C2 (pt)
WO (1) WO2016026445A1 (pt)

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EP3822273B1 (en) 2012-06-13 2024-04-10 Incyte Holdings Corporation Substituted tricyclic compounds as fgfr inhibitors
SG10201708520YA (en) 2013-04-19 2017-12-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
MY188447A (en) * 2014-08-19 2021-12-09 Shanghai Haihe Pharmaceutical Co Ltd Indazole compounds as fger kinase inhibitor, preparation and use thereof
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CN106279119B (zh) * 2015-05-27 2020-06-16 上海海和药物研究开发有限公司 一种新型激酶抑制剂的制备及其应用
CN105601617B (zh) * 2016-03-24 2019-02-22 山东省科学院生物研究所 一种邻二氮杂环化合物及其制备方法与应用
CN107698593A (zh) * 2016-08-09 2018-02-16 南京天印健华医药科技有限公司 作为fgfr抑制剂的杂环化合物
CN108570052A (zh) * 2017-03-13 2018-09-25 中国科学院上海药物研究所 五元杂环并吡嗪化合物、制备方法、中间体、组合和应用
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN110317173B (zh) * 2018-03-30 2022-10-11 上海奕拓医药科技有限责任公司 用作fgfr不可逆抑制剂的酰胺基吡唑类化合物
CN112867716A (zh) 2018-05-04 2021-05-28 因赛特公司 Fgfr抑制剂的固体形式和其制备方法
CN112566912A (zh) 2018-05-04 2021-03-26 因赛特公司 Fgfr抑制剂的盐
CN108570049A (zh) * 2018-07-24 2018-09-25 上海毕得医药科技有限公司 一种6-氯-1氢-吡唑并[3,4-b]吡啶的合成方法
WO2020038458A1 (zh) * 2018-08-23 2020-02-27 如东凌达生物医药科技有限公司 一类稠环三氮唑类化合物、制备方法和用途
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
EP3725777A1 (en) * 2019-04-17 2020-10-21 Rottapharm Biotech S.r.l. Benzo- and pyrido-pyrazoles as protein kinase inhibitors
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2020366006A1 (en) 2019-10-14 2022-04-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11634424B2 (en) * 2019-11-29 2023-04-25 Medshine Discovery Inc. Diazaindole derivative and use thereof as CHK1 inhibitor
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
CN112521336B (zh) * 2020-02-21 2023-03-28 温州医科大学 一种吲唑类、吡咯并吡啶类化合物及其应用
US20230250106A1 (en) * 2020-07-15 2023-08-10 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
EP4182310A1 (en) * 2020-07-15 2023-05-24 IFM Due, Inc. Compounds and compositions for treating conditions associated with sting activity
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CN113735774B (zh) * 2021-08-31 2023-06-09 四川大学华西医院 一种多激酶抑制剂yth-17的制备方法

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Also Published As

Publication number Publication date
KR20190105679A (ko) 2019-09-17
JP6445684B2 (ja) 2018-12-26
AU2015306561A1 (en) 2017-04-06
RU2017105781A3 (pt) 2019-01-21
RU2719428C2 (ru) 2020-04-17
MY188447A (en) 2021-12-09
MX2017002206A (es) 2018-01-23
EP3184521A4 (en) 2018-01-03
CN105524048A (zh) 2016-04-27
PE20170774A1 (es) 2017-07-04
CN105524048B (zh) 2019-11-12
WO2016026445A1 (zh) 2016-02-25
EP3184521B1 (en) 2021-10-06
CA2958503C (en) 2021-01-19
JP2017532293A (ja) 2017-11-02
ES2904544T3 (es) 2022-04-05
US20170275291A1 (en) 2017-09-28
RU2017105781A (ru) 2018-09-20
BR112017003312B1 (pt) 2023-05-02
KR102022866B1 (ko) 2019-09-19
CA2958503A1 (en) 2016-02-25
EP3184521A1 (en) 2017-06-28
KR102166002B1 (ko) 2020-10-15
US10562900B2 (en) 2020-02-18
KR20170069199A (ko) 2017-06-20
AU2015306561B2 (en) 2018-03-15

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B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
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Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 19/08/2015, OBSERVADAS AS CONDICOES LEGAIS