CN111989329A - 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 - Google Patents

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 Download PDF

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CN111989329A
CN111989329A CN201980019867.2A CN201980019867A CN111989329A CN 111989329 A CN111989329 A CN 111989329A CN 201980019867 A CN201980019867 A CN 201980019867A CN 111989329 A CN111989329 A CN 111989329A
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CN111989329B (zh
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朱永强
杨杨
海鸥
刘兆刚
冯超
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Nanling Chuangte Pharmaceutical Technology Co ltd
Jiangsu Chia Tai Fenghai Pharmaceutical Co Ltd
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • 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
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    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
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    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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Abstract

本发明公开了一种结构如式I氘代3‑(4，5‑取代氨基嘧啶)苯基化合物的单甲磺酸盐晶型及其制备方法，所述晶型稳定性高，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。
Figure DDA0002685994080000011

Description

PCT国内申请，说明书已公开。

Claims (15)

  1. PCT国内申请，权利要求书已公开。
CN201980019867.2A 2018-03-16 2019-03-15 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 Active CN111989329B (zh)

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Application Number Priority Date Filing Date Title
CN2018102200034 2018-03-16
CN201810220003.4A CN110272420A (zh) 2018-03-16 2018-03-16 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
PCT/CN2019/078200 WO2019174623A1 (zh) 2018-03-16 2019-03-15 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

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JP (1) JP7383622B2 (zh)
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AU (1) AU2019233209B2 (zh)
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AU2017326029B2 (en) * 2016-09-19 2019-11-21 Nanjing Chuangte Pharmaceutical Technology Co., Ltd Deuterated 3-(4,5-substituted pyrimidinamine) phenyl derivatives and applications thereof
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
CA3222537A1 (en) 2021-05-14 2022-11-17 Nanjing Chuangte Pharmaceutical Technology Co., Ltd Pharmaceutical formulations
CN114058652B (zh) * 2021-11-24 2024-05-14 大连万福制药有限公司 一种合成乙酰乙酸（n-苄基-n-甲基）氨基乙酯的方法

Citations (2)

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Publication number Priority date Publication date Assignee Title
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
CN107344934A (zh) * 2016-05-04 2017-11-14 江苏正大丰海制药有限公司 药物活性物质的固体形式

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CN104140418B (zh) * 2014-08-15 2016-08-24 常州润诺生物科技有限公司 2-(2，4，5-取代苯胺)嘧啶衍生物及其用途
CN111170998B (zh) * 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
CN107840847A (zh) * 2016-09-19 2018-03-27 江苏正大丰海制药有限公司 氘代3‑(4,5‑取代氨基嘧啶)苯基衍生物及其应用
AU2017326029B2 (en) * 2016-09-19 2019-11-21 Nanjing Chuangte Pharmaceutical Technology Co., Ltd Deuterated 3-(4,5-substituted pyrimidinamine) phenyl derivatives and applications thereof
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN107344934A (zh) * 2016-05-04 2017-11-14 江苏正大丰海制药有限公司 药物活性物质的固体形式

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EP3747887A4 (en) 2021-04-14
EP3747887A1 (en) 2020-12-09
WO2019174623A1 (zh) 2019-09-19
US20210053971A1 (en) 2021-02-25
KR20200121351A (ko) 2020-10-23
CN111989329B (zh) 2022-07-26
CA3093982A1 (en) 2019-09-19
JP2021516243A (ja) 2021-07-01
JP7383622B2 (ja) 2023-11-20
AU2019233209A1 (en) 2020-10-22
AU2019233209B2 (en) 2022-02-17
CA3093982C (en) 2023-09-26
CN110272420A (zh) 2019-09-24
US11629144B2 (en) 2023-04-18

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