WO2022111729A1 - 作为Cdc7抑制剂的盐型及其晶型 - Google Patents
作为Cdc7抑制剂的盐型及其晶型 Download PDFInfo
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- WO2022111729A1 WO2022111729A1 PCT/CN2021/134435 CN2021134435W WO2022111729A1 WO 2022111729 A1 WO2022111729 A1 WO 2022111729A1 CN 2021134435 W CN2021134435 W CN 2021134435W WO 2022111729 A1 WO2022111729 A1 WO 2022111729A1
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- 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
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- C07—ORGANIC CHEMISTRY
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Abstract
Description
引湿性分类 | 引湿增重* |
潮解 | 吸收足量水分形成液体 |
极具引湿性 | 引湿增重不小于15% |
有引湿性 | 引湿增重小于15%但不小于2% |
略有引湿性 | 引湿增重小于2%但不小于0.2% |
无或几乎无引湿性 | 引湿增重小于0.2% |
名称 | 生产厂家 |
384孔微孔板 | Greiner |
384孔化合物板 | Costar |
CDC7/DBF4Active | Signal Chem |
PDKtide | Signal Chem |
Kinase分析缓冲液III | Signal Chem |
DTT(0.1M) | Signal Chem |
ADP-Glo Kinase Assay | Promega |
名称 | 生产厂家 | 型号 |
VICTOR Nivo | PerkinElmer | VICTOR Nivo 5F |
名称 | 生产厂家 | 型号 |
Envision | PerkinElmer | EXT |
细胞类型 | 细胞名称 | 细胞生长方式 | 细胞培养基 | 细胞来源 |
人结直肠癌细胞 | Colo-205 | 贴壁 | RPMI 1640+10%FBS+1%双抗 | 普诺赛生物 |
细胞名称 | 铺板密度(细胞/孔) | 化合物孵育天数(天) |
COLO205 | 3000 | 3 |
Claims (14)
- 根据权利要求1所述的式(II)化合物的晶型,所述晶型的X-射线粉末衍射图谱包含在2θ值为11.46±0.20°、24.03±0.20°和25.16±0.20°处的特征峰。
- 根据权利要求2所述的式(II)化合物的晶型,所述晶型的X-射线粉末衍射图谱包含在2θ值为11.46±0.20°、12.06±0.20°、16.96±0.20°、17.60±0.20°、18.48±0.20°、19.55±0.20°、24.03±0.20°和25.16±0.20°处的特征峰;或者,所述晶型的X-射线粉末衍射图谱包含在2θ值为6.46°±0.20°、9.36°±0.20°、11.46°±0.20°、12.06°±0.20°、12.39°±0.20°、12.89°±0.20°、13.37°±0.20°、13.87°±0.20°、14.09°±0.20°、16.10°±0.20°、16.96°±0.20°、17.19°±0.20°、17.60°±0.20°、18.48°±0.20°、18.75°±0.20°、19.37°±0.20°、19.55°±0.20°、21.21°±0.20°、21.65°±0.20°、22.36°±0.20°、23.06°±0.20°、23.42°±0.20°、23.74°±0.20°、24.03°±0.20°、25.16°±0.20°、25.47°±0.20°、26.59°±0.20°、27.32°±0.20°、28.11°±0.20°、28.77°±0.20°、29.73°±0.20°、31.81°±0.20°、33.09°±0.20°、33.80°±0.20°、34.19°±0.20°、35.49°±0.20°、35.99°±0.20°、37.66°±0.20°、38.14°±0.20°、38.77°±0.20°和39.38°±0.20°处的特征峰;或者,所述晶型具有如下的X-射线粉末衍射图谱数据:;典型地,其X-射线粉末衍射图谱如图1所示。
- 根据权利要求2-3中任一项所述的式(II)化合物的晶型,所述晶型的DSC曲线在230.7℃±3℃处有一个吸热峰的起始点;典型地,其DSC曲线图谱如图4所示。
- 根据权利要求1所述的式(II)化合物的晶型,所述晶型的X-射线粉末衍射图谱包含在2θ值为5.86±0.20°、17.64±0.20°和24.89±0.20°处的特征峰。
- 根据权利要求5所述的式(II)化合物的晶型,所述晶型的X-射线粉末衍射图谱包含在2θ值为5.86±0.20°、10.17±0.20°、11.73±0.20°、15.83±0.20°、17.64±0.20°、23.59±0.20°、24.89±0.20°和25.80±0.20°处的特征峰;或者,所述晶型的X-射线粉末衍射图谱包含在2θ值为5.86°±0.20°、10.17°±0.20°、11.73°± 0.20°、12.57°±0.20°、14.15°±0.20°、14.40°±0.20°、15.23°±0.20°、15.83°±0.20°、16.26°±0.20°、16.71°±0.20°、17.64°±0.20°、18.04°±0.20°、18.73°±0.20°、19.99°±0.20°、20.57°±0.20°、21.08°±0.20°、23.59°±0.20°、24.36°±0.20°、24.89°±0.20°、25.41°±0.20°、25.80°±0.20°、27.20°±0.20°、27.90°±0.20°、28.90°±0.20°、29.39°±0.20°、29.70°±0.20°、30.52°±0.20°、30.81°±0.20°、31.99°±0.20°、34.29°±0.20°、35.83°±0.20°、39.64°±0.20°、28.90°±0.20°、29.39°±0.20°、29.70°±0.20°、30.52°±0.20°、30.81°±0.20°、31.99°±0.20°、34.29°±0.20°、35.83°±0.20°和39.64°±0.20°处的特征峰;或者,所述晶型具有如下的X-射线粉末衍射图谱数据:;典型地,其X-射线粉末衍射图谱如图2所示。
- 根据权利要求5-6中任一项所述的式(II)化合物的晶型,所述晶型的DSC曲线在65.1℃±3℃、113.7℃±3℃、208.8℃±3℃和221.1℃±3℃处有吸热峰的起始点;典型地,其DSC曲线图谱如图7所示。
- 根据权利要求1所述的式(II)化合物的晶型,所述晶型的X-射线粉末衍射图谱包含在2θ值为7.40±0.20°、11.21±0.20°和22.18±0.20°处的特征峰。
- 根据权利要求8所述的式(II)化合物的晶型,所述晶型的X-射线粉末衍射图谱包含在2θ值为7.40±0.20°、11.21±0.20°、13.95±0.20°、15.01±0.20°、15.72±0.20°、20.61±0.20°、22.18±0.20°和23.82±0.20°处的特征峰;或者,所述晶型的X-射线粉末衍射图谱包含在2θ值为7.40°±0.20°、10.50°±0.20°、11.21°±0.20°、11.81°±0.20°、13.05°±0.20°、13.95°±0.20°、15.01°±0.20°、15.72°、16.28°、17.64°、18.35°、18.73°、19.53°、20.14°、20.61°、22.18°、22.51°、23.82°、24.37°、25.49°、26.36°±0.20°、27.19°±0.20°、28.93°±0.20°、30.70°±0.20°、31.60°±0.20°、32.50°±0.20°和34.33°±0.20°处的特征峰;或者,所述晶型具有如下的X-射线粉末衍射图谱数据:;典型地,其X-射线粉末衍射图谱如图3所示。
- 根据权利要求8-9中任一项所述的式(II)化合物的晶型,所述晶型的DSC曲线在219.9℃±3℃处有一个吸热峰的起始点;典型地,其DSC曲线图谱如图9所示。
- 结晶组合物,其包含根据权利要求1-10中任一项所述的式(II)化合物的晶型,其中所述权利要求1-10中任一项所述的式(II)化合物的晶型占所述结晶组合物重量的50%以上,较好是75%以上,更好是90%以上,最好是95%以上。
- 药物组合物,其包含根据权利要求1-10中任一项所述的式(II)化合物或其晶型或权利要求12所述的结晶组合物,以及任选的药学上可接受的辅料。
- 权利要求1-10中任一项所述的式(II)化合物或其晶型、权利要求12所述的结晶组合物或权利要求13所述的药物组合物在预防或治疗由Cdc7激酶介导的疾病中的用途,或者在制备用于预防或治疗由Cdc7激酶介导的疾病的药物中的用途;优选地,所述由Cdc7激酶介导的疾病为肿瘤;更优选地,所述肿瘤为结直肠癌或胰腺癌。
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CA3199631A CA3199631A1 (en) | 2020-11-30 | 2021-11-30 | Salt form used as cdc7 inhibitor and crystal form thereof |
KR1020237020672A KR20230116005A (ko) | 2020-11-30 | 2021-11-30 | Cdc7 억제제로 사용되는 염 형태 및 이의 결정 형태 |
CN202180078292.9A CN116472046A (zh) | 2020-11-30 | 2021-11-30 | 作为Cdc7抑制剂的盐型及其晶型 |
AU2021386437A AU2021386437A1 (en) | 2020-11-30 | 2021-11-30 | Salt form used as cdc7 inhibitor and crystal form thereof |
EP21897229.7A EP4253388A1 (en) | 2020-11-30 | 2021-11-30 | Salt form used as cdc7 inhibitor and crystal form thereof |
JP2023528549A JP2023551134A (ja) | 2020-11-30 | 2021-11-30 | Cdc7阻害剤としての塩及びその結晶形 |
US18/253,846 US20240025920A1 (en) | 2020-11-30 | 2021-11-30 | Salt form used as cdc7 inhibitor and crystal form thereof |
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CN115090329A (zh) * | 2022-06-29 | 2022-09-23 | 陕西师范大学 | 一种Cu-二硫苏糖醇纳米仿生漆酶及其降解污染物和检测肾上腺素的应用 |
Citations (3)
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CN102844320A (zh) * | 2010-02-17 | 2012-12-26 | 武田药品工业株式会社 | 杂环化合物 |
CN108779126A (zh) * | 2016-03-28 | 2018-11-09 | 武田药品工业株式会社 | 2-[(2s)-1-氮杂双环[2.2.2]辛-2-基]-6-(3-甲基-1h-吡唑-4-基)噻吩并[3,2-d]嘧啶-4(3h)-酮半水合物的结晶形式 |
WO2020239107A1 (zh) * | 2019-05-30 | 2020-12-03 | 正大天晴药业集团股份有限公司 | 作为Cdc7抑制剂的四并环类化合物 |
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Publication number | Priority date | Publication date | Assignee | Title |
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CN102844320A (zh) * | 2010-02-17 | 2012-12-26 | 武田药品工业株式会社 | 杂环化合物 |
CN108779126A (zh) * | 2016-03-28 | 2018-11-09 | 武田药品工业株式会社 | 2-[(2s)-1-氮杂双环[2.2.2]辛-2-基]-6-(3-甲基-1h-吡唑-4-基)噻吩并[3,2-d]嘧啶-4(3h)-酮半水合物的结晶形式 |
WO2020239107A1 (zh) * | 2019-05-30 | 2020-12-03 | 正大天晴药业集团股份有限公司 | 作为Cdc7抑制剂的四并环类化合物 |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN115090329A (zh) * | 2022-06-29 | 2022-09-23 | 陕西师范大学 | 一种Cu-二硫苏糖醇纳米仿生漆酶及其降解污染物和检测肾上腺素的应用 |
CN115090329B (zh) * | 2022-06-29 | 2024-01-23 | 陕西师范大学 | 一种Cu-二硫苏糖醇纳米仿生漆酶及其降解污染物和检测肾上腺素的应用 |
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CA3199631A1 (en) | 2022-06-02 |
JP2023551134A (ja) | 2023-12-07 |
TW202227457A (zh) | 2022-07-16 |
CN116472046A (zh) | 2023-07-21 |
EP4253388A1 (en) | 2023-10-04 |
US20240025920A1 (en) | 2024-01-25 |
KR20230116005A (ko) | 2023-08-03 |
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