CN109071499A - 2-[(2r)-2-甲基-2-吡咯烷基]-1h-苯并咪唑-7-甲酰胺二盐酸盐的晶型a及其制备方法 - Google Patents

2-[(2r)-2-甲基-2-吡咯烷基]-1h-苯并咪唑-7-甲酰胺二盐酸盐的晶型a及其制备方法 Download PDF

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Publication number
CN109071499A
CN109071499A CN201780013661.XA CN201780013661A CN109071499A CN 109071499 A CN109071499 A CN 109071499A CN 201780013661 A CN201780013661 A CN 201780013661A CN 109071499 A CN109071499 A CN 109071499A
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crystal form
preparation
compound
formula
present
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陈敏华
张炎锋
刘凯
张晓宇
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Crystal Pharmatech Co Ltd
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Crystal Pharmatech Co Ltd
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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

提供了2‑[(2R)‑2‑甲基‑2‑吡咯烷基]‑1H‑苯并咪唑‑7‑甲酰胺二盐酸盐的晶型A及其制备方法和用途。晶型A的X射线粉末衍射图在2theta值为8.3°±0.2°、26.7°±0.2°和16.1°±0.2°处具有特征峰。晶型A与现有的晶型相比具有出乎意料的优异溶解性、机械和存储稳定性以及粒度分布，是比已经报道的晶型更理想的晶体形式，更符合药用要求，对未来该药物的优化和开发具有重要价值。

Description

PCT国内申请，说明书已公开。

Claims (13)

  1. PCT国内申请，权利要求书已公开。
CN201780013661.XA 2016-03-09 2017-03-08 2-[(2r)-2-甲基-2-吡咯烷基]-1h-苯并咪唑-7-甲酰胺二盐酸盐的晶型a及其制备方法 Pending CN109071499A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610132878X 2016-03-09
CN201610132878 2016-03-09
PCT/CN2017/075990 WO2017152846A1 (zh) 2016-03-09 2017-03-08 2-[(2r)-2-甲基-2-吡咯烷基]-1h-苯并咪唑-7-甲酰胺二盐酸盐的晶型a及其制备方法

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Publication Number Publication Date
CN109071499A true CN109071499A (zh) 2018-12-21

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CN201780013661.XA Pending CN109071499A (zh) 2016-03-09 2017-03-08 2-[(2r)-2-甲基-2-吡咯烷基]-1h-苯并咪唑-7-甲酰胺二盐酸盐的晶型a及其制备方法

Country Status (3)

Country Link
US (1) US20190092756A1 (zh)
CN (1) CN109071499A (zh)
WO (1) WO2017152846A1 (zh)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101155797A (zh) * 2005-04-11 2008-04-02 艾博特公司 在2-位上被一个季碳原子取代的1h-苯并咪唑-4-甲酰胺化合物是有效的parp抑制剂
CN101821269A (zh) * 2007-10-12 2010-09-01 雅培制药有限公司 2-((r)-2-甲基吡咯烷-2-基)-1h-苯并咪唑-4-甲酰胺晶形2
CN105130961A (zh) * 2015-08-06 2015-12-09 苏州晶云药物科技有限公司 Abt-888的晶型b及其制备方法和应用

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX350019B (es) * 2007-10-12 2016-12-09 Abbvie Ireland Unlimited Co Forma cristalina 1 de 2-((r)-2-metilpirrolidin-2-il)-1h-bencimidaz ol-4-carboxamida.

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101155797A (zh) * 2005-04-11 2008-04-02 艾博特公司 在2-位上被一个季碳原子取代的1h-苯并咪唑-4-甲酰胺化合物是有效的parp抑制剂
CN101821269A (zh) * 2007-10-12 2010-09-01 雅培制药有限公司 2-((r)-2-甲基吡咯烷-2-基)-1h-苯并咪唑-4-甲酰胺晶形2
CN104230893A (zh) * 2007-10-12 2014-12-24 艾伯维巴哈马有限公司 2-((r)-2-甲基吡咯烷-2-基)-1h-苯并咪唑-4-甲酰胺晶形2
CN105130961A (zh) * 2015-08-06 2015-12-09 苏州晶云药物科技有限公司 Abt-888的晶型b及其制备方法和应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
THOMAS D. PENNING等: "Discovery of the Poly(ADP-ribose) Polymerase (PARP) Inhibitor", 《J. MED. CHEM.》 *

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US20190092756A1 (en) 2019-03-28

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Application publication date: 20181221