WO2021259396A3 - 一种亚硝胺杂质、能够减少亚硝胺杂质生成的伐尼克兰药物组合物及其制备与应用 - Google Patents

一种亚硝胺杂质、能够减少亚硝胺杂质生成的伐尼克兰药物组合物及其制备与应用 Download PDF

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Publication number
WO2021259396A3
WO2021259396A3 PCT/CN2021/122654 CN2021122654W WO2021259396A3 WO 2021259396 A3 WO2021259396 A3 WO 2021259396A3 CN 2021122654 W CN2021122654 W CN 2021122654W WO 2021259396 A3 WO2021259396 A3 WO 2021259396A3
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nitrosamine
impurities
pharmaceutical composition
varenicline
preparation
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PCT/CN2021/122654
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English (en)
French (fr)
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WO2021259396A2 (zh
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魏彦君
巴萨瓦拉杰·希达贡纳瓦
李锋
孙中亚
裴慧
杜文峰
王建
孔猛
刘希望
邢艳平
徐青景
Original Assignee
威智医药有限公司
山东威智百科药业有限公司
山东威智中科药业有限公司
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Priority claimed from CN202110961274.7A external-priority patent/CN115707703A/zh
Priority claimed from CN202110997332.1A external-priority patent/CN113908131A/zh
Application filed by 威智医药有限公司, 山东威智百科药业有限公司, 山东威智中科药业有限公司 filed Critical 威智医药有限公司
Priority to CN202180100142.3A priority Critical patent/CN117715910A/zh
Priority to KR1020247005635A priority patent/KR20240038022A/ko
Publication of WO2021259396A2 publication Critical patent/WO2021259396A2/zh
Publication of WO2021259396A3 publication Critical patent/WO2021259396A3/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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • C07D471/08—Bridged systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
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  • Addiction (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Agronomy & Crop Science (AREA)
  • Biophysics (AREA)
  • Psychiatry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

公开了一种亚硝胺杂质、能够减少亚硝胺杂质生成的伐尼克兰药物组合物及其制备与应用。药物组合物通过在仲胺化合物或其组合物中加入药学上可接受的酸，能够有效抑制和减少亚硝胺杂质的生成，提高仲胺化合物或其组合物的稳定性，将亚硝胺基因毒性杂质含量控制在较低水平，符合安全性要求。
PCT/CN2021/122654 2021-08-20 2021-10-08 一种亚硝胺杂质、能够减少亚硝胺杂质生成的伐尼克兰药物组合物及其制备与应用 WO2021259396A2 (zh)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN202180100142.3A CN117715910A (zh) 2021-08-20 2021-10-08 一种亚硝胺杂质、能够减少亚硝胺杂质生成的伐尼克兰药物组合物及其制备与应用
KR1020247005635A KR20240038022A (ko) 2021-08-20 2021-10-08 니트로사민 불순물, 니트로사민 불순물 생성을 줄일 수 있는 바레니클린 약학 조성물 및 그 제조와 응용

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN202110961274.7 2021-08-20
CN202110961274.7A CN115707703A (zh) 2021-08-20 2021-08-20 亚硝胺化合物、其制备方法、在检测酒石酸伐尼克兰原料药或制剂中的应用及检测方法
CN202110997332.1 2021-08-27
CN202110997332.1A CN113908131A (zh) 2021-08-27 2021-08-27 一种能够减少亚硝胺杂质生成的伐尼克兰药物组合物及其制备与应用

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WO2021259396A2 WO2021259396A2 (zh) 2021-12-30
WO2021259396A3 true WO2021259396A3 (zh) 2022-06-30

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KR (1) KR20240038022A (zh)
CN (1) CN117715910A (zh)
WO (1) WO2021259396A2 (zh)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023286077A1 (en) * 2021-07-10 2023-01-19 Jubilant Generics Limited Oral pharmaceutical compositions of varenicline or its pharmaceutically acceptable salts thereof
WO2023275413A2 (en) * 2021-12-23 2023-01-05 Medichem, S.A. Solid pharmaceutical formulations of varenicline
EP4241775A1 (en) * 2022-03-11 2023-09-13 Par Pharmaceutical, Inc. Tablet comprising varenicline and process of preparation thereof
US11602537B2 (en) * 2022-03-11 2023-03-14 Par Pharmaceutical, Inc. Varenicline compound and process of manufacture thereof
WO2023228027A1 (en) * 2022-05-23 2023-11-30 V-Ensure Pharma Technologies Private Limited A tablet composition of mirabegron
WO2024069649A1 (en) * 2022-09-27 2024-04-04 Inventia Healthcare Limited Compositions with reduced nitrosamine impurities

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CN117715910A (zh) 2024-03-15
WO2021259396A2 (zh) 2021-12-30

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