CN109415314A - 尼达尼布的新晶型及其制备方法及其用途 - Google Patents

尼达尼布的新晶型及其制备方法及其用途 Download PDF

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Publication number
CN109415314A
CN109415314A CN201780031371.8A CN201780031371A CN109415314A CN 109415314 A CN109415314 A CN 109415314A CN 201780031371 A CN201780031371 A CN 201780031371A CN 109415314 A CN109415314 A CN 109415314A
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China
Prior art keywords
methyl
values
phenyi
thyl
piperazin
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CN201780031371.8A
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English (en)
Inventor
孟晓明
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Shanghai Begreat Pharmatech
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Shanghai Begreat Pharmatech
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Publication of CN109415314A publication Critical patent/CN109415314A/zh
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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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/32—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by aldehydo- or ketonic radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/04—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Indole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明公开了3‑Z‑[1‑(4‑(N‑((4‑甲基‑哌嗪‑1‑基)‑甲基羰基)‑N‑甲基‑氨基)‑苯氨基)‑1‑苯基‑亚甲基]‑6‑甲氧羰基‑2‑吲哚满酮(尼达尼布)的新多晶型及其制备方法和药用用途。所发现尼达尼布乙磺酸盐晶型I、乙磺酸盐晶型III和双羟萘酸盐晶型I，与现有晶型相比，新晶型在溶解度、稳定性、控制释放速度或制备工艺方面具有明显优势。

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。
CN201780031371.8A 2016-05-19 2017-05-19 尼达尼布的新晶型及其制备方法及其用途 Pending CN109415314A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610347601 2016-05-19
CN2016103476019 2016-05-19
PCT/CN2017/084984 WO2017198202A1 (zh) 2016-05-19 2017-05-19 尼达尼布的新晶型及其制备方法及其用途

Publications (1)

Publication Number Publication Date
CN109415314A true CN109415314A (zh) 2019-03-01

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CN201780031371.8A Pending CN109415314A (zh) 2016-05-19 2017-05-19 尼达尼布的新晶型及其制备方法及其用途

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CN (1) CN109415314A (zh)
WO (1) WO2017198202A1 (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112239459B (zh) * 2019-07-19 2021-11-26 中国科学院上海药物研究所 稠环嘧啶氨基化合物、其制备方法、药物组合物及应用
CN113024439A (zh) * 2021-03-28 2021-06-25 郑州大学 尼达尼布乙磺酸盐新晶型ⅰ的制备

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1671660A (zh) * 2002-07-24 2005-09-21 贝林格尔英格海姆法玛两合公司 3－z－[1－(4－(n－((4－甲基－哌嗪－1－基)－甲羰基)－n－甲基－氨基)－苯氨基)－1－苯基－亚甲基]－6－甲氧羰基－2－吲哚满酮－单乙烷磺酸盐及其作为药物组合物的用途
CN101883756A (zh) * 2007-12-03 2010-11-10 贝林格尔.英格海姆国际有限公司 制备二氢吲哚酮衍生物的方法
CN105001143A (zh) * 2015-07-24 2015-10-28 南京正大天晴制药有限公司 一种制备高纯度乙磺酸尼达尼布的方法
CN105418483A (zh) * 2015-12-15 2016-03-23 南京艾德凯腾生物医药有限责任公司 一种结晶型乙磺酸尼达尼布的制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20091445A1 (es) * 2007-12-03 2009-10-19 Boehringer Ingelheim Int Derivados de indolinona y procedimiento para su fabricacion
CN104844499B (zh) * 2015-06-05 2017-03-08 北京康立生医药技术开发有限公司 一锅法制备尼达尼布的合成方法
CN105461609B (zh) * 2015-12-25 2019-08-23 杭州新博思生物医药有限公司 一种尼达尼布的制备方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1671660A (zh) * 2002-07-24 2005-09-21 贝林格尔英格海姆法玛两合公司 3－z－[1－(4－(n－((4－甲基－哌嗪－1－基)－甲羰基)－n－甲基－氨基)－苯氨基)－1－苯基－亚甲基]－6－甲氧羰基－2－吲哚满酮－单乙烷磺酸盐及其作为药物组合物的用途
CN101883756A (zh) * 2007-12-03 2010-11-10 贝林格尔.英格海姆国际有限公司 制备二氢吲哚酮衍生物的方法
CN105001143A (zh) * 2015-07-24 2015-10-28 南京正大天晴制药有限公司 一种制备高纯度乙磺酸尼达尼布的方法
CN105418483A (zh) * 2015-12-15 2016-03-23 南京艾德凯腾生物医药有限责任公司 一种结晶型乙磺酸尼达尼布的制备方法

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