JP2024518370A - (r)-オキシブチニンd-リンゴ酸塩の固体形態 - Google Patents

(r)-オキシブチニンd-リンゴ酸塩の固体形態 Download PDF

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Publication number
JP2024518370A
JP2024518370A JP2023567201A JP2023567201A JP2024518370A JP 2024518370 A JP2024518370 A JP 2024518370A JP 2023567201 A JP2023567201 A JP 2023567201A JP 2023567201 A JP2023567201 A JP 2023567201A JP 2024518370 A JP2024518370 A JP 2024518370A
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Prior art keywords
oxybutynin
crystalline
malate
salt
malate salt
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JP2023567201A
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Japanese (ja)
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JP2024518370A5 (enExample
Inventor
ジョンストン,ショーン
モルナー,デニス
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アプニメッド,インコーポレイテッド(デラウェア)
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Priority claimed from PCT/US2021/030571 external-priority patent/WO2021226020A1/en
Application filed by アプニメッド,インコーポレイテッド(デラウェア) filed Critical アプニメッド,インコーポレイテッド(デラウェア)
Publication of JP2024518370A publication Critical patent/JP2024518370A/ja
Publication of JP2024518370A5 publication Critical patent/JP2024518370A5/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/02Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C219/20Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C221/00Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/42Separation; Purification; Stabilisation; Use of additives
    • C07C51/43Separation; Purification; Stabilisation; Use of additives by change of the physical state, e.g. crystallisation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255Tartaric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2023567201A 2021-05-04 2022-05-04 (r)-オキシブチニンd-リンゴ酸塩の固体形態 Pending JP2024518370A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
USPCT/US2021/030571 2021-05-04
PCT/US2021/030571 WO2021226020A1 (en) 2020-05-05 2021-05-04 Polymorphic forms of (r)-oxybutynin hydrochloride
US202163248684P 2021-09-27 2021-09-27
US63/248,684 2021-09-27
PCT/US2022/027573 WO2022235726A1 (en) 2021-05-04 2022-05-04 Solid forms of (r)-oxybutynin d-malate

Publications (2)

Publication Number Publication Date
JP2024518370A true JP2024518370A (ja) 2024-05-01
JP2024518370A5 JP2024518370A5 (enExample) 2025-05-21

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Family Applications (1)

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JP2023567201A Pending JP2024518370A (ja) 2021-05-04 2022-05-04 (r)-オキシブチニンd-リンゴ酸塩の固体形態

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Country Link
US (1) US20240217918A1 (enExample)
EP (1) EP4334281A1 (enExample)
JP (1) JP2024518370A (enExample)
KR (1) KR20240004600A (enExample)
AU (1) AU2022270639A1 (enExample)
CA (1) CA3215373A1 (enExample)
WO (1) WO2022235726A1 (enExample)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110087042A1 (en) * 2008-02-04 2011-04-14 Matrix Laboratories Limited Crystalline oxybutynin and process for preparing the same
CN104370760A (zh) * 2013-11-29 2015-02-25 江苏汉邦科技有限公司 模拟移动床色谱拆分奥昔布宁对映体的方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
KR102874891B1 (ko) 2018-01-30 2025-10-21 애프니메드, 인코포레이티드 (델라웨어) 수면 무호흡증을 치료하기 위한 방법 및 조성물

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110087042A1 (en) * 2008-02-04 2011-04-14 Matrix Laboratories Limited Crystalline oxybutynin and process for preparing the same
CN104370760A (zh) * 2013-11-29 2015-02-25 江苏汉邦科技有限公司 模拟移动床色谱拆分奥昔布宁对映体的方法

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
J F KACHUR ET AL., THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol. 247, no. 3, JPN6025052059, December 1988 (1988-12-01), pages 867 - 872, ISSN: 0005756847 *
小嶌隆史: "医薬品開発における結晶性選択の効率化を目指して", 薬剤学, vol. 68, no. 5, JPN6009053757, 1 September 2008 (2008-09-01), pages 344 - 349, ISSN: 0005756842 *
浅原 照三, 溶剤ハンドブック, JPN6011026738, 1985, pages 47 - 51, ISSN: 0005756846 *
社団法人日本化学会, 化学便覧応用化学編第6版, vol. 第4章化学合成技術, JPN6009048258, 30 January 2003 (2003-01-30), pages 178, ISSN: 0005756844 *
芦澤一英, 医薬品の多形現象と晶析の科学, JPN6018028449, 2002, pages 56 - 102, ISSN: 0005756843 *
高田則幸: "創薬段階における原薬Formスクリーニングと選択", PHARM STAGE, vol. 6, no. 10, JPN6009053755, 15 January 2007 (2007-01-15), pages 20 - 25, ISSN: 0005756845 *

Also Published As

Publication number Publication date
CA3215373A1 (en) 2022-11-10
AU2022270639A1 (en) 2023-12-14
US20240217918A1 (en) 2024-07-04
KR20240004600A (ko) 2024-01-11
EP4334281A1 (en) 2024-03-13
WO2022235726A1 (en) 2022-11-10

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