CN109134409B - 盐酸美呋哌瑞多晶型物及其制备方法与应用 - Google Patents

盐酸美呋哌瑞多晶型物及其制备方法与应用 Download PDF

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Publication number
CN109134409B
CN109134409B CN201710449281.2A CN201710449281A CN109134409B CN 109134409 B CN109134409 B CN 109134409B CN 201710449281 A CN201710449281 A CN 201710449281A CN 109134409 B CN109134409 B CN 109134409B
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hydrochloride
water
alcohol
mefurazapirone
powder diffraction
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Chinese (zh)
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CN109134409A (zh
Inventor
杨春皓
缪泽鸿
谭村
宦霞娟
丁健
陈奕
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Fukang Biotechnology (Shanghai) Co.,Ltd.
Shanghai Institute of Materia Medica of CAS
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Shanghai Institute of Materia Medica of CAS
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Priority to CN201710449281.2A priority Critical patent/CN109134409B/zh
Application filed by Shanghai Institute of Materia Medica of CAS filed Critical Shanghai Institute of Materia Medica of CAS
Priority to EP18818471.7A priority patent/EP3643708B1/en
Priority to US16/623,297 priority patent/US11174237B2/en
Priority to JP2020519169A priority patent/JP7432503B2/ja
Priority to SG11201912281PA priority patent/SG11201912281PA/en
Priority to KR1020207000951A priority patent/KR102458566B1/ko
Priority to CA3067336A priority patent/CA3067336C/en
Priority to AU2018286057A priority patent/AU2018286057B2/en
Priority to PCT/CN2018/089222 priority patent/WO2018228205A1/zh
Priority to TW107120585A priority patent/TWI675027B/zh
Publication of CN109134409A publication Critical patent/CN109134409A/zh
Priority to ZA2020/00224A priority patent/ZA202000224B/en
Priority to JP2021194722A priority patent/JP2022060192A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201710449281.2A 2017-06-14 2017-06-14 盐酸美呋哌瑞多晶型物及其制备方法与应用 Active CN109134409B (zh)

Priority Applications (12)

Application Number Priority Date Filing Date Title
CN201710449281.2A CN109134409B (zh) 2017-06-14 2017-06-14 盐酸美呋哌瑞多晶型物及其制备方法与应用
PCT/CN2018/089222 WO2018228205A1 (zh) 2017-06-14 2018-05-31 盐酸美呋哌瑞多晶型物及其制备方法与应用
JP2020519169A JP7432503B2 (ja) 2017-06-14 2018-05-31 塩酸メフパリブの多形体およびその製造方法と使用
SG11201912281PA SG11201912281PA (en) 2017-06-14 2018-05-31 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, preparation method therefor and application thereof
KR1020207000951A KR102458566B1 (ko) 2017-06-14 2018-05-31 메푸파리브 히드로클로라이드 다결정형 물질 및 이의 제조방법과 응용
CA3067336A CA3067336C (en) 2017-06-14 2018-05-31 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, preparation method therefor and application thereof
EP18818471.7A EP3643708B1 (en) 2017-06-14 2018-05-31 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, preparation method therefor and application thereof
US16/623,297 US11174237B2 (en) 2017-06-14 2018-05-31 2-[4-(meihylaminomethyl)phenyl]-5-fluoro- benzofuran-7-carboxamide hydrochloride polymorph, preparation method therefor and application thereof
AU2018286057A AU2018286057B2 (en) 2017-06-14 2018-05-31 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, preparation method therefor and application thereof
TW107120585A TWI675027B (zh) 2017-06-14 2018-06-14 鹽酸美呋哌瑞多晶型物及其製備方法與應用
ZA2020/00224A ZA202000224B (en) 2017-06-14 2020-01-13 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, preparation method therefor and application thereof
JP2021194722A JP2022060192A (ja) 2017-06-14 2021-11-30 塩酸メフパリブの多形体およびその製造方法と使用

Applications Claiming Priority (1)

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CN109134409B true CN109134409B (zh) 2023-09-29

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US (1) US11174237B2 (enExample)
EP (1) EP3643708B1 (enExample)
JP (2) JP7432503B2 (enExample)
KR (1) KR102458566B1 (enExample)
CN (1) CN109134409B (enExample)
AU (1) AU2018286057B2 (enExample)
CA (1) CA3067336C (enExample)
SG (1) SG11201912281PA (enExample)
TW (1) TWI675027B (enExample)
WO (1) WO2018228205A1 (enExample)
ZA (1) ZA202000224B (enExample)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109134409B (zh) * 2017-06-14 2023-09-29 中国科学院上海药物研究所 盐酸美呋哌瑞多晶型物及其制备方法与应用
CN111320596B (zh) * 2018-12-14 2024-07-05 甫康（上海）健康科技有限责任公司 盐酸美呋哌瑞多晶型物及其制备方法
EP4112049A4 (en) * 2020-02-24 2024-07-24 Fukang (Shanghai) Health Technology Co., Ltd. ANTI-CORONAVIRUS APPLICATION OF POLY ADP-RIBOSE POLYMERASE INHIBITOR

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CN102627620A (zh) * 2012-04-10 2012-08-08 江苏先声药物研究有限公司 一类苯并呋喃衍生物及其医药应用
WO2013117120A1 (zh) * 2012-02-09 2013-08-15 中国科学院上海药物研究所 2-芳基苯并呋喃-7-甲酰胺类化合物、其制备方法及用途
CN104003979A (zh) * 2013-02-21 2014-08-27 上海汇伦生命科技有限公司 苯并咪唑-2-哌嗪类化合物、其药物组合物及其制备方法和用途
CN104003940A (zh) * 2014-06-16 2014-08-27 华东理工大学 2,4-二氟-5-(酞嗪酮-1-甲基)-苯甲酰哌嗪类化合物及其用途
WO2015032328A1 (zh) * 2013-09-03 2015-03-12 四川海思科制药有限公司 茚满衍生物及其制备方法和在医药上的应用

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CN109134409B (zh) * 2017-06-14 2023-09-29 中国科学院上海药物研究所 盐酸美呋哌瑞多晶型物及其制备方法与应用
CN111320596B (zh) * 2018-12-14 2024-07-05 甫康（上海）健康科技有限责任公司 盐酸美呋哌瑞多晶型物及其制备方法

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WO2013117120A1 (zh) * 2012-02-09 2013-08-15 中国科学院上海药物研究所 2-芳基苯并呋喃-7-甲酰胺类化合物、其制备方法及用途
CN102627620A (zh) * 2012-04-10 2012-08-08 江苏先声药物研究有限公司 一类苯并呋喃衍生物及其医药应用
CN104003979A (zh) * 2013-02-21 2014-08-27 上海汇伦生命科技有限公司 苯并咪唑-2-哌嗪类化合物、其药物组合物及其制备方法和用途
WO2015032328A1 (zh) * 2013-09-03 2015-03-12 四川海思科制药有限公司 茚满衍生物及其制备方法和在医药上的应用
CN104003940A (zh) * 2014-06-16 2014-08-27 华东理工大学 2,4-二氟-5-(酞嗪酮-1-甲基)-苯甲酰哌嗪类化合物及其用途

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US20200172502A1 (en) 2020-06-04
TW201904952A (zh) 2019-02-01
US11174237B2 (en) 2021-11-16
AU2018286057A1 (en) 2020-01-30
TWI675027B (zh) 2019-10-21
EP3643708C0 (en) 2025-09-24
ZA202000224B (en) 2021-08-25
EP3643708A4 (en) 2021-02-24
KR102458566B1 (ko) 2022-10-24
JP2022060192A (ja) 2022-04-14
EP3643708A1 (en) 2020-04-29
CA3067336A1 (en) 2018-12-20
EP3643708B1 (en) 2025-09-24
JP2020524707A (ja) 2020-08-20
CA3067336C (en) 2022-11-15
SG11201912281PA (en) 2020-01-30
JP7432503B2 (ja) 2024-02-16
AU2018286057B2 (en) 2021-03-18
WO2018228205A1 (zh) 2018-12-20
KR20200014924A (ko) 2020-02-11
CN109134409A (zh) 2019-01-04

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