CN109689657A - 氘代3-(4,5-取代氨基嘧啶)苯基衍生物及其应用 - Google Patents

氘代3-(4,5-取代氨基嘧啶)苯基衍生物及其应用 Download PDF

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Publication number
CN109689657A
CN109689657A CN201780056474.XA CN201780056474A CN109689657A CN 109689657 A CN109689657 A CN 109689657A CN 201780056474 A CN201780056474 A CN 201780056474A CN 109689657 A CN109689657 A CN 109689657A
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compound
egfr
cancer
pharmaceutically acceptable
added
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CN201780056474.XA
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CN109689657B (zh
Inventor
朱永强
刘兆刚
冯超
胡诗合
陈浩
白恩赫
王佳
石晶淼
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Nanling Chuangte Pharmaceutical Technology Co ltd
Jiangsu Chia Tai Fenghai Pharmaceutical Co Ltd
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Nanling Chuangte Pharmaceutical Technology Co ltd
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Priority claimed from CN201610833361.3A external-priority patent/CN107840847A/zh
Priority claimed from CN201710413610.8A external-priority patent/CN108976229A/zh
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    • 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
    • C07D471/06—Peri-condensed systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Abstract

本发明公开了一类氘代3‑(4,5‑取代氨基嘧啶)苯基衍生物及其应用，其为具有式(I)结构的化合物或其药学上可接受的盐，这些化合物或其盐可通过某些突变形式的表皮生长因子受体而用于疾病或病况的治疗或预防，可以有效抑制多种肿瘤细胞的生长，并对EGFR、Her家族其他蛋白酶产生抑制作用，可用于制备抗肿瘤药物。

Description

PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN201780056474.XA 2016-09-19 2017-09-18 氘代3-(4,5-取代氨基嘧啶)苯基衍生物及其应用 Active CN109689657B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2016108333613 2016-09-19
CN201610833361.3A CN107840847A (zh) 2016-09-19 2016-09-19 氘代3‑(4,5‑取代氨基嘧啶)苯基衍生物及其应用
CN201710413610.8A CN108976229A (zh) 2017-06-05 2017-06-05 氘代3-(4,5-取代氨基嘧啶)苯基衍生物及其应用
CN2017104136108 2017-06-05
PCT/CN2017/102027 WO2018050108A1 (zh) 2016-09-19 2017-09-18 氘代3-(4,5-取代氨基嘧啶)苯基衍生物及其应用

Publications (2)

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CN109689657A true CN109689657A (zh) 2019-04-26
CN109689657B CN109689657B (zh) 2021-06-11

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US (1) US10654851B2 (zh)
EP (1) EP3498708B1 (zh)
JP (1) JP6746794B2 (zh)
KR (1) KR102245280B1 (zh)
CN (1) CN109689657B (zh)
AU (1) AU2017326029B2 (zh)
CA (1) CA3037097C (zh)
ES (1) ES2863925T3 (zh)
WO (1) WO2018050108A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110272420A (zh) * 2018-03-16 2019-09-24 江苏正大丰海制药有限公司 氘代3-(4,5-取代氨基嘧啶)苯基化合物单甲磺酸盐晶型及其制备方法
WO2022237889A1 (zh) 2021-05-14 2022-11-17 南京创特医药科技有限公司 药用组合物
CN115286542B (zh) * 2022-07-27 2023-08-15 浙江工业大学 一种亚磺酸酯类化合物的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104140418A (zh) * 2014-08-15 2014-11-12 朱孝云 新的2-(2,4,5-取代苯胺)嘧啶衍生物及其用途
WO2015175632A1 (en) * 2014-05-13 2015-11-19 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CN105175396A (zh) * 2011-07-27 2015-12-23 阿斯利康(瑞典)有限公司 取代的4-甲氧基-n3-(嘧啶-2-基)苯-1,3-二胺化合物及其盐
WO2016054987A1 (zh) * 2014-10-11 2016-04-14 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113121575A (zh) * 2014-08-25 2021-07-16 四川海思科制药有限公司 一种(取代的苯基)(取代的嘧啶)胺基衍生物及其制备方法和药物用途
CN107344934B (zh) * 2016-05-04 2019-08-23 江苏正大丰海制药有限公司 药物活性物质的固体形式
CN110272420A (zh) * 2018-03-16 2019-09-24 江苏正大丰海制药有限公司 氘代3-(4,5-取代氨基嘧啶)苯基化合物单甲磺酸盐晶型及其制备方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105175396A (zh) * 2011-07-27 2015-12-23 阿斯利康(瑞典)有限公司 取代的4-甲氧基-n3-(嘧啶-2-基)苯-1,3-二胺化合物及其盐
WO2015175632A1 (en) * 2014-05-13 2015-11-19 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CN104140418A (zh) * 2014-08-15 2014-11-12 朱孝云 新的2-(2,4,5-取代苯胺)嘧啶衍生物及其用途
WO2016054987A1 (zh) * 2014-10-11 2016-04-14 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用

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Publication number Publication date
WO2018050108A1 (zh) 2018-03-22
US10654851B2 (en) 2020-05-19
JP6746794B2 (ja) 2020-08-26
KR20190046875A (ko) 2019-05-07
US20190225610A1 (en) 2019-07-25
AU2017326029A1 (en) 2019-04-11
AU2017326029B2 (en) 2019-11-21
JP2019529551A (ja) 2019-10-17
EP3498708B1 (en) 2021-01-13
EP3498708A1 (en) 2019-06-19
CA3037097C (en) 2021-06-29
CA3037097A1 (en) 2018-03-22
EP3498708A4 (en) 2019-08-21
CN109689657B (zh) 2021-06-11
ES2863925T3 (es) 2021-10-13
KR102245280B1 (ko) 2021-04-27

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Address after: Room 933, building a, phase I, Zhongdan Ecological Life Science Industrial Park, no.3-1, xinjinhu Road, Jiangbei new district, Nanjing City, Jiangsu Province, 210000

Patentee after: NANLING CHUANGTE PHARMACEUTICAL TECHNOLOGY Co.,Ltd.

Patentee after: JIANGSU CHIA TAI FENGHAI PHARMACEUTICAL Co.,Ltd.

Address before: Room 933, building a, phase I, Zhongdan Ecological Life Science Industrial Park, no.3-1, xinjinhu Road, Jiangbei new district, Nanjing City, Jiangsu Province, 210000

Patentee before: NANLING CHUANGTE PHARMACEUTICAL TECHNOLOGY Co.,Ltd.