JP2019520321A5 - - Google Patents
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- Publication number
- JP2019520321A5 JP2019520321A5 JP2018558377A JP2018558377A JP2019520321A5 JP 2019520321 A5 JP2019520321 A5 JP 2019520321A5 JP 2018558377 A JP2018558377 A JP 2018558377A JP 2018558377 A JP2018558377 A JP 2018558377A JP 2019520321 A5 JP2019520321 A5 JP 2019520321A5
- Authority
- JP
- Japan
- Prior art keywords
- chrysabolol
- solvent
- crystalline form
- free form
- free
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 239000002904 solvent Substances 0.000 claims 17
- 239000012046 mixed solvent Substances 0.000 claims 13
- 238000000634 powder X-ray diffraction Methods 0.000 claims 12
- 239000007787 solid Substances 0.000 claims 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 8
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 6
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 6
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 6
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 6
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 5
- 150000002576 ketones Chemical class 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims 4
- 239000000725 suspension Substances 0.000 claims 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical group CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 3
- 150000004292 cyclic ethers Chemical class 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 238000003756 stirring Methods 0.000 claims 3
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 2
- 206010012434 Dermatitis allergic Diseases 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 150000001298 alcohols Chemical class 0.000 claims 2
- -1 alkyl nitrile Chemical class 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 2
- 150000004945 aromatic hydrocarbons Chemical class 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- 238000002425 crystallisation Methods 0.000 claims 2
- 230000008025 crystallization Effects 0.000 claims 2
- 238000001035 drying Methods 0.000 claims 2
- 150000008282 halocarbons Chemical class 0.000 claims 2
- 238000000926 separation method Methods 0.000 claims 2
- JWUJQDFVADABEY-UHFFFAOYSA-N 2-methyltetrahydrofuran Chemical compound CC1CCCO1 JWUJQDFVADABEY-UHFFFAOYSA-N 0.000 claims 1
- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 claims 1
- UIHCLUNTQKBZGK-UHFFFAOYSA-N Methyl isobutyl ketone Natural products CCC(C)C(C)=O UIHCLUNTQKBZGK-UHFFFAOYSA-N 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 150000001338 aliphatic hydrocarbons Chemical class 0.000 claims 1
- 150000005215 alkyl ethers Chemical class 0.000 claims 1
- 238000005119 centrifugation Methods 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 claims 1
- 229940011051 isopropyl acetate Drugs 0.000 claims 1
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
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 |
|---|---|---|---|
| CN201610301832.6 | 2016-05-09 | ||
| CN201610301832 | 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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019520321A JP2019520321A (ja) | 2019-07-18 |
| JP2019520321A5 true JP2019520321A5 (enExample) | 2020-06-11 |
Family
ID=60266671
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US11773113B2 (enExample) |
| EP (1) | EP3456722B1 (enExample) |
| JP (3) | JP2019520321A (enExample) |
| KR (1) | KR102221472B1 (enExample) |
| CN (2) | CN108884111A (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)
| 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 |
| ES2949908T3 (es) * | 2018-01-09 | 2023-10-03 | Halcyon Labs Private Ltd | Proceso para la preparación de Crisaborol y sus intermedios |
| 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 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN191496B (enExample) * | 1999-07-30 | 2003-12-06 | Ranbaxy Lab Ltd | |
| GB2383042A (en) * | 2001-10-18 | 2003-06-18 | Cipla Ltd | Amorphous alendronate sodium |
| KR101426220B1 (ko) | 2005-02-16 | 2014-08-05 | 아나코르 파마슈티칼스 인코포레이티드 | 보론함유 소분자 |
| CN106008583A (zh) | 2005-12-30 | 2016-10-12 | 安纳考尔医药公司 | 含硼的小分子 |
| CN101505603A (zh) * | 2005-12-30 | 2009-08-12 | 安纳考尔医药公司 | 含硼的小分子 |
| CA2933994A1 (en) * | 2006-02-16 | 2007-08-23 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules as anti-inflammatory agents |
| BRPI0713010A2 (pt) * | 2006-06-12 | 2012-10-09 | Anacor Pharmaceuticals Inc | compostos para o tratamento de doença periodontal |
| US20070286822A1 (en) | 2006-06-12 | 2007-12-13 | Anacor Pharmaceuticals Inc. | Compounds for the Treatment of Periodontal Disease |
| RU2015109165A (ru) * | 2008-03-06 | 2015-11-10 | Анакор Фармасьютикалз, Инк. | Борсодержащие малые молекулы в качестве противовоспалительных агентов |
| RU2724053C2 (ru) | 2015-11-30 | 2020-06-19 | Анакор Фармасьютикалз, Инк. | Фармацевтические составы для местного применения для лечения связанных с воспалением состояний |
| WO2017203514A1 (en) * | 2016-05-26 | 2017-11-30 | Perrigo Api Ltd | Polymorphs of crisaborole and production processes therefor |
-
2017
- 2017-05-09 MX MX2018013742A patent/MX380022B/es unknown
- 2017-05-09 WO PCT/CN2017/083631 patent/WO2017193914A1/zh not_active Ceased
- 2017-05-09 CN CN201780009362.9A patent/CN108884111A/zh active Pending
- 2017-05-09 CA CA3023851A patent/CA3023851C/en active Active
- 2017-05-09 SG SG11201809984PA patent/SG11201809984PA/en unknown
- 2017-05-09 EP EP17795532.5A patent/EP3456722B1/en active Active
- 2017-05-09 KR KR1020187035217A patent/KR102221472B1/ko active Active
- 2017-05-09 CN CN202411806904.3A patent/CN119751489A/zh active Pending
- 2017-05-09 US US16/099,839 patent/US11773113B2/en active Active
- 2017-05-09 BR BR112018073017-3A patent/BR112018073017B1/pt active IP Right Grant
- 2017-05-09 JP JP2018558377A patent/JP2019520321A/ja not_active Withdrawn
- 2017-05-09 AU AU2017262235A patent/AU2017262235C1/en active Active
-
2018
- 2018-11-08 IL IL262878A patent/IL262878A/en unknown
- 2018-11-22 ZA ZA2018/07892A patent/ZA201807892B/en unknown
-
2021
- 2021-06-29 JP JP2021107201A patent/JP2021167327A/ja active Pending
-
2023
- 2023-06-12 JP JP2023096006A patent/JP2023116645A/ja active Pending
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