JP2019520321A - フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用 - Google Patents

フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用 Download PDF

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JP2019520321A
JP2019520321A JP2018558377A JP2018558377A JP2019520321A JP 2019520321 A JP2019520321 A JP 2019520321A JP 2018558377 A JP2018558377 A JP 2018558377A JP 2018558377 A JP2018558377 A JP 2018558377A JP 2019520321 A JP2019520321 A JP 2019520321A
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crystalline form
solvent
solid
crystalline
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JP2019520321A5 (enExample
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チェン ミンファ
チェン ミンファ
チャン ヤンフェン
チャン ヤンフェン
ルー フェイ
ルー フェイ
シャー ナン
シャー ナン
チャン シャンユー
チャン シャンユー
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アナコール ファーマシューティカルズ，インコーポレイテッド
アナコール ファーマシューティカルズ，インコーポレイテッド
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Application filed by アナコール ファーマシューティカルズ，インコーポレイテッド, アナコール ファーマシューティカルズ，インコーポレイテッド filed Critical アナコール ファーマシューティカルズ，インコーポレイテッド
Publication of JP2019520321A publication Critical patent/JP2019520321A/ja
Publication of JP2019520321A5 publication Critical patent/JP2019520321A5/ja
Priority to JP2021107201A priority Critical patent/JP2021167327A/ja
Priority to JP2023096006A priority patent/JP2023116645A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Analysing Materials By The Use Of Radiation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2018558377A 2016-05-09 2017-05-09 フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用 Withdrawn JP2019520321A (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2021107201A JP2021167327A (ja) 2016-05-09 2021-06-29 フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用
JP2023096006A JP2023116645A (ja) 2016-05-09 2023-06-12 フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610301832 2016-05-09
CN201610301832.6 2016-05-09
PCT/CN2017/083631 WO2017193914A1 (zh) 2016-05-09 2017-05-09 克立硼罗游离形式的晶型及其制备方法和用途

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JP2021107201A Division JP2021167327A (ja) 2016-05-09 2021-06-29 フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用

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JP2019520321A true JP2019520321A (ja) 2019-07-18
JP2019520321A5 JP2019520321A5 (enExample) 2020-06-11

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JP2018558377A Withdrawn JP2019520321A (ja) 2016-05-09 2017-05-09 フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用
JP2021107201A Pending JP2021167327A (ja) 2016-05-09 2021-06-29 フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用
JP2023096006A Pending JP2023116645A (ja) 2016-05-09 2023-06-12 フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用

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JP2021107201A Pending JP2021167327A (ja) 2016-05-09 2021-06-29 フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用
JP2023096006A Pending JP2023116645A (ja) 2016-05-09 2023-06-12 フリー体のクリサボロールの結晶形ならびにそれらの調製方法および使用

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US (1) US11773113B2 (enExample)
EP (1) EP3456722B1 (enExample)
JP (3) JP2019520321A (enExample)
KR (1) KR102221472B1 (enExample)
CN (2) CN119751489A (enExample)
AU (1) AU2017262235C1 (enExample)
BR (1) BR112018073017B1 (enExample)
CA (1) CA3023851C (enExample)
IL (1) IL262878A (enExample)
MX (1) MX380022B (enExample)
SG (1) SG11201809984PA (enExample)
WO (1) WO2017193914A1 (enExample)
ZA (1) ZA201807892B (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10329311B1 (en) * 2017-12-21 2019-06-25 Olon S.P.A. Process for the preparation of crisaborole
PL3737685T3 (pl) * 2018-01-09 2023-10-02 Halcyon Labs Private Limited Sposób wytwarzania kryzaborolu i jego związków pośrednich
US10597410B2 (en) 2018-02-02 2020-03-24 Dipharma Francis S.R.L. Intermediates and process for the preparation of a crystalline form of a topical anti-inflammatory agent
CN110780005B (zh) * 2019-11-14 2022-07-29 江苏海岸药业有限公司 一种克立硼罗原料及其合成中间体的分析方法
CN111983123A (zh) * 2020-08-14 2020-11-24 江苏海岸药业有限公司 用于治疗皮肤疾病的克立硼罗制剂的体外评价方法
CN112375093A (zh) * 2020-11-13 2021-02-19 江苏知原药业股份有限公司 一种克立硼罗晶型化合物及其制备方法
CN113087733A (zh) * 2021-04-06 2021-07-09 南京科默生物医药有限公司 克立硼罗的晶型a、晶型b、晶型c、晶型d、晶型e及其制备方法
WO2024047571A1 (en) * 2022-09-01 2024-03-07 Savoi Guilherme Crisaborole cocrystal derivatives
CN115417890A (zh) * 2022-09-24 2022-12-02 中山万远新药研发有限公司 克立硼罗的新晶型及其制备方法与用途

Citations (2)

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JP2003506329A (ja) * 1999-07-30 2003-02-18 ランバクシー ラボラトリーズ リミテッド セフポドキシメプロキセチルの改良アモルファス形態
JP2005521636A (ja) * 2001-10-18 2005-07-21 シプラ・リミテッド 薬剤的に許容されるアモルファス形態のアレンドロ酸塩

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CA2597982C (en) 2005-02-16 2014-07-08 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
KR20080110984A (ko) 2005-12-30 2008-12-22 아나코르 파마슈티칼스 인코포레이티드 보론함유 소분자
CN101505603A (zh) * 2005-12-30 2009-08-12 安纳考尔医药公司 含硼的小分子
RS54108B1 (sr) * 2006-02-16 2015-12-31 Anacor Pharmaceuticals Inc. Mali molekuli koji sadrže boron kao agensi protiv zapaljenja
WO2007146965A2 (en) * 2006-06-12 2007-12-21 Anacor Pharmaceuticals, Inc. Compounds for the treatment of periodontal disease
US20070286822A1 (en) 2006-06-12 2007-12-13 Anacor Pharmaceuticals Inc. Compounds for the Treatment of Periodontal Disease
EP2564857B1 (en) * 2008-03-06 2017-05-03 Anacor Pharmaceuticals, Inc. Boron-containing small molecules as anti-inflammatory agents
DK3383363T3 (da) * 2015-11-30 2021-01-18 Anacor Pharmaceuticals Inc Topiske farmaceutiske formuleringer til behandling af inflammatorisk-relaterede tilstande
WO2017203514A1 (en) * 2016-05-26 2017-11-30 Perrigo Api Ltd Polymorphs of crisaborole and production processes therefor

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003506329A (ja) * 1999-07-30 2003-02-18 ランバクシー ラボラトリーズ リミテッド セフポドキシメプロキセチルの改良アモルファス形態
JP2005521636A (ja) * 2001-10-18 2005-07-21 シプラ・リミテッド 薬剤的に許容されるアモルファス形態のアレンドロ酸塩

Non-Patent Citations (5)

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Title
"晶析の課題：粒径分布と多形制御・晶核生成メカニズム解明の重要性", 粉体工学会誌, vol. 38, no. 4, JPN6021003350, 2001, pages 251 - 259, ISSN: 0004439275 *
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 19, no. 8, JPN6020025668, 2009, pages 2129 - 2132, ISSN: 0004439271 *
平山令明, 有機化合物結晶作製ハンドブック, JPN6014035600, 2008, pages 17 - 23, ISSN: 0004439273 *
杉本功、高橋嘉輝: "溶媒和物、非晶質固体と医薬品製剤", 紛体工学会誌, vol. 22, no. 2, JPN6017004373, 1985, pages 85 - 97, ISSN: 0004439274 *
芦澤一英: "塩・結晶形の最適化と結晶化技術", PHARM TECH JAPAN, vol. 18, no. 10, JPN6013060608, 2002, pages 81 - 96, ISSN: 0004439272 *

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AU2017262235C1 (en) 2020-08-20
BR112018073017A2 (pt) 2019-02-19
US11773113B2 (en) 2023-10-03
EP3456722B1 (en) 2025-12-10
EP3456722A4 (en) 2019-12-18
WO2017193914A1 (zh) 2017-11-16
SG11201809984PA (en) 2018-12-28
JP2021167327A (ja) 2021-10-21
KR102221472B1 (ko) 2021-03-02
NZ748385A (en) 2022-03-25
MX380022B (es) 2025-03-11
KR20190005195A (ko) 2019-01-15
CN119751489A (zh) 2025-04-04
JP2023116645A (ja) 2023-08-22
IL262878A (en) 2018-12-31
BR112018073017B1 (pt) 2022-06-14
RU2018142490A (ru) 2020-06-10
MX2018013742A (es) 2019-08-01
CA3023851A1 (en) 2017-11-16
RU2018142490A3 (enExample) 2020-06-10
NZ786020A (en) 2025-06-27
EP3456722A1 (en) 2019-03-20
US20230234974A1 (en) 2023-07-27
AU2017262235A1 (en) 2018-12-06
AU2017262235B2 (en) 2019-09-19
ZA201807892B (en) 2021-06-30
CA3023851C (en) 2021-01-26
CN108884111A (zh) 2018-11-23

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