JP7432503B2 - 塩酸メフパリブの多形体およびその製造方法と使用 - Google Patents

塩酸メフパリブの多形体およびその製造方法と使用 Download PDF

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Publication number
JP7432503B2
JP7432503B2 JP2020519169A JP2020519169A JP7432503B2 JP 7432503 B2 JP7432503 B2 JP 7432503B2 JP 2020519169 A JP2020519169 A JP 2020519169A JP 2020519169 A JP2020519169 A JP 2020519169A JP 7432503 B2 JP7432503 B2 JP 7432503B2
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water
crystal form
hydrochloride
fluorobenzofuran
methylaminomethyl
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JP2020524707A (ja
Inventor
ヤン，チュンハオ
ミャオ，ゼホン
タン，チュン
フアン，シアフアン
ディン，ジィェン
チェン，イー
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Fukang Shanghai health Technology Co ltd
Shanghai Institute of Materia Medica
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Fukang Shanghai health Technology Co ltd
Shanghai Institute of Materia Medica
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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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020519169A 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 Active JP7432503B2 (ja)

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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

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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
CN201710449281.2 2017-06-14
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

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JP7432503B2 true JP7432503B2 (ja) 2024-02-16

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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)
ES (1) ES3055682T3 (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
US20240016775A1 (en) * 2020-02-24 2024-01-18 Fukang (Shanghai) Health Technology Co., Ltd Anti-coronavirus application of poly adp ribose polymerase inhibitor

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015511942A (ja) 2012-02-09 2015-04-23 上海 インスティテュート オブ マテリア メディカ、チャイニーズ アカデミー オブ サイエンシーズＳｈａｎｇｈａｉ Ｉｎｓｔｉｔｕｔｅ Ｏｆ Ｍａｔｅｒｉａ Ｍｅｄｉｃａ， Ｃｈｉｎｅｓｅ Ａｃａｄｅｍｙ Ｏｆ Ｓｃｉｅｎｃｅｓ ２−アリールベンゾフラン−７−カルボキサミド系化合物、その製造方法および用途

Family Cites Families (6)

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Publication number Priority date Publication date Assignee Title
CN102627620B (zh) * 2012-04-10 2015-12-16 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
CN104003979B (zh) * 2013-02-21 2016-08-17 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
CN104003940B (zh) * 2014-06-16 2017-02-15 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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015511942A (ja) 2012-02-09 2015-04-23 上海 インスティテュート オブ マテリア メディカ、チャイニーズ アカデミー オブ サイエンシーズＳｈａｎｇｈａｉ Ｉｎｓｔｉｔｕｔｅ Ｏｆ Ｍａｔｅｒｉａ Ｍｅｄｉｃａ， Ｃｈｉｎｅｓｅ Ａｃａｄｅｍｙ Ｏｆ Ｓｃｉｅｎｃｅｓ ２−アリールベンゾフラン−７−カルボキサミド系化合物、その製造方法および用途

Non-Patent Citations (5)

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Title
ＰＨＡＲＭ ＴＥＣＨ ＪＡＰＡＮ、２００２年、Ｖｏｌ．１８、Ｎｏ．１０、ｐ．１６２９～１６４４
ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＲＥＳＥＡＲＣＨ、１９９５年、Ｖｏｌ．１２、Ｎｏ．７、ｐ．９４５～９５４
平山令明、有機化合物結晶作製ハンドブック、２００８年、ｐ．１７～２３、３７～４０、４５～５１、５７～６５
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緒方章、化学実験操作法 上巻、株式会社南江堂、１９６３年、ｐ．３６６～３９９

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Publication number Publication date
JP2020524707A (ja) 2020-08-20
TWI675027B (zh) 2019-10-21
KR20200014924A (ko) 2020-02-11
WO2018228205A1 (zh) 2018-12-20
ZA202000224B (en) 2021-08-25
AU2018286057A1 (en) 2020-01-30
SG11201912281PA (en) 2020-01-30
EP3643708C0 (en) 2025-09-24
EP3643708A4 (en) 2021-02-24
KR102458566B1 (ko) 2022-10-24
US11174237B2 (en) 2021-11-16
CA3067336C (en) 2022-11-15
TW201904952A (zh) 2019-02-01
CN109134409B (zh) 2023-09-29
JP2022060192A (ja) 2022-04-14
EP3643708A1 (en) 2020-04-29
AU2018286057B2 (en) 2021-03-18
US20200172502A1 (en) 2020-06-04
CA3067336A1 (en) 2018-12-20
EP3643708B1 (en) 2025-09-24
CN109134409A (zh) 2019-01-04
ES3055682T3 (en) 2026-02-13

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