JP2017105763A5 - - Google Patents
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- Publication number
- JP2017105763A5 JP2017105763A5 JP2016229721A JP2016229721A JP2017105763A5 JP 2017105763 A5 JP2017105763 A5 JP 2017105763A5 JP 2016229721 A JP2016229721 A JP 2016229721A JP 2016229721 A JP2016229721 A JP 2016229721A JP 2017105763 A5 JP2017105763 A5 JP 2017105763A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical formulation
- topical pharmaceutical
- formulation according
- mono
- benzoxaborole
- 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.)
- Granted
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 13
- 230000000699 topical effect Effects 0.000 claims 12
- 235000019271 petrolatum Nutrition 0.000 claims 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 5
- 239000004322 Butylated hydroxytoluene Substances 0.000 claims 3
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 claims 3
- SHWNNYZBHZIQQV-UHFFFAOYSA-J EDTA monocalcium diisodium salt Chemical compound [Na+].[Na+].[Ca+2].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O SHWNNYZBHZIQQV-UHFFFAOYSA-J 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 3
- 229940095259 butylated hydroxytoluene Drugs 0.000 claims 3
- 235000010354 butylated hydroxytoluene Nutrition 0.000 claims 3
- USZAGAREISWJDP-UHFFFAOYSA-N crisaborole Chemical compound C=1C=C2B(O)OCC2=CC=1OC1=CC=C(C#N)C=C1 USZAGAREISWJDP-UHFFFAOYSA-N 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- 239000012188 paraffin wax Substances 0.000 claims 3
- 239000003871 white petrolatum Substances 0.000 claims 3
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 102000019034 Chemokines Human genes 0.000 claims 1
- 108010012236 Chemokines Proteins 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 229940125772 JTE-052 Drugs 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 239000004012 Tofacitinib Substances 0.000 claims 1
- OGBUMNBNEWYMNJ-UHFFFAOYSA-N batilol Chemical class CCCCCCCCCCCCCCCCCCOCC(O)CO OGBUMNBNEWYMNJ-UHFFFAOYSA-N 0.000 claims 1
- LOWWYYZBZNSPDT-ZBEGNZNMSA-N delgocitinib Chemical compound C[C@H]1CN(C(=O)CC#N)[C@@]11CN(C=2C=3C=CNC=3N=CN=2)CC1 LOWWYYZBZNSPDT-ZBEGNZNMSA-N 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- UJLAWZDWDVHWOW-YPMHNXCESA-N tofacitinib Chemical compound C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-YPMHNXCESA-N 0.000 claims 1
- 229960001350 tofacitinib Drugs 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562260716P | 2015-11-30 | 2015-11-30 | |
| US62/260716 | 2015-11-30 | ||
| US201662420987P | 2016-11-11 | 2016-11-11 | |
| US62/420987 | 2016-11-11 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017105763A JP2017105763A (ja) | 2017-06-15 |
| JP2017105763A5 true JP2017105763A5 (enExample) | 2020-01-09 |
| JP6725403B2 JP6725403B2 (ja) | 2020-07-15 |
Family
ID=57471943
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016229721A Active JP6725403B2 (ja) | 2015-11-30 | 2016-11-28 | 炎症関連状態を処置するための局所医薬製剤 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US20170152273A1 (enExample) |
| EP (2) | EP3831389A1 (enExample) |
| JP (1) | JP6725403B2 (enExample) |
| KR (1) | KR102106230B1 (enExample) |
| CN (1) | CN108366958A (enExample) |
| AU (1) | AU2016362668C1 (enExample) |
| BR (1) | BR112018010464B1 (enExample) |
| CA (1) | CA2949614C (enExample) |
| CY (1) | CY1123845T1 (enExample) |
| DK (1) | DK3383363T3 (enExample) |
| ES (1) | ES2858311T3 (enExample) |
| HK (1) | HK1257818A1 (enExample) |
| HU (1) | HUE053115T2 (enExample) |
| IL (1) | IL259693B2 (enExample) |
| MX (1) | MX378145B (enExample) |
| NZ (1) | NZ742208A (enExample) |
| PL (1) | PL3383363T3 (enExample) |
| PT (1) | PT3383363T (enExample) |
| RU (1) | RU2724053C2 (enExample) |
| SG (2) | SG10202112628UA (enExample) |
| SI (1) | SI3383363T1 (enExample) |
| TW (1) | TWI627974B (enExample) |
| WO (1) | WO2017093857A1 (enExample) |
| ZA (1) | ZA201802920B (enExample) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10265265B2 (en) | 2007-03-15 | 2019-04-23 | Drug Delivery Solutions Limited | Topical composition |
| KR20170122777A (ko) | 2015-03-04 | 2017-11-06 | 반다 파마슈티칼즈, 인코퍼레이티드. | 트라디피턴트에 의한 치료 방법 |
| US11773106B2 (en) | 2015-10-16 | 2023-10-03 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US10550126B2 (en) | 2015-10-16 | 2020-02-04 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| RU2018117889A (ru) | 2015-10-16 | 2019-11-20 | Эббви Инк. | СПОСОБЫ ПОЛУЧЕНИЯ (3S,4R)-3-ЭТИЛ-4-(3H-ИМИДАЗО[1,2-a]ПИРРОЛО[2,3-e]-ПИРАЗИН-8-ИЛ)-N-(2,2,2-ТРИФТОРЭТИЛ)ПИРРОЛИДИН-1-КАРБОКСАМИДА И ЕГО ТВЕРДОФАЗНЫХ ФОРМ |
| US11365198B2 (en) | 2015-10-16 | 2022-06-21 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11524964B2 (en) | 2015-10-16 | 2022-12-13 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11512092B2 (en) | 2015-10-16 | 2022-11-29 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US12365689B2 (en) | 2015-10-16 | 2025-07-22 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11447506B2 (en) | 2016-05-09 | 2022-09-20 | Anacor Pharmaceuticals, Inc. | Crystal forms of crisaborole in free form and preparation method and use thereof |
| MX380022B (es) * | 2016-05-09 | 2025-03-11 | Anacor Pharmaceuticals Inc | Formas cristalinas de crisaborol en forma libre, metodo de preparacion y uso de las mismas |
| WO2017203514A1 (en) * | 2016-05-26 | 2017-11-30 | Perrigo Api Ltd | Polymorphs of crisaborole and production processes therefor |
| GB201701583D0 (en) * | 2017-01-31 | 2017-03-15 | Drug Delivery Solutions Ltd | Topical composition |
| US20200172560A1 (en) * | 2017-06-05 | 2020-06-04 | Glenmark Life Science Limited | Process for preparation of crisaborole |
| US12011437B1 (en) | 2017-06-07 | 2024-06-18 | Arcutis Biotherapeutics, Inc. | Roflumilast formulations with an improved pharmacokinetic profile |
| US9895359B1 (en) * | 2017-06-07 | 2018-02-20 | Arcutis, Inc. | Inhibition of crystal growth of roflumilast |
| US20200155524A1 (en) * | 2018-11-16 | 2020-05-21 | Arcutis, Inc. | Method for reducing side effects from administration of phosphodiesterase-4 inhibitors |
| US20210161870A1 (en) | 2017-06-07 | 2021-06-03 | Arcutis Biotherapeutics, Inc. | Roflumilast formulations with an improved pharmacokinetic profile |
| US12042487B2 (en) | 2018-11-16 | 2024-07-23 | Arcutis Biotherapeutics, Inc. | Method for reducing side effects from administration of phosphodiesterase-4 inhibitors |
| US11129818B2 (en) | 2017-06-07 | 2021-09-28 | Arcutis Biotherapeutics, Inc. | Topical roflumilast formulation having improved delivery and plasma half life |
| US11534493B2 (en) | 2017-09-22 | 2022-12-27 | Arcutis Biotherapeutics, Inc. | Pharmaceutical compositions of roflumilast in aqueous blends of water-miscible, pharmaceutically acceptable solvents |
| US10329311B1 (en) | 2017-12-21 | 2019-06-25 | Olon S.P.A. | Process for the preparation of crisaborole |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| CN109985000B (zh) * | 2017-12-29 | 2022-09-02 | 苏州旺山旺水生物医药有限公司 | 克立硼罗微乳组合物 |
| 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 |
| SG11202007558YA (en) | 2018-02-09 | 2020-09-29 | Nestle Skin Health Sa | Nemolizumab in the treatment of atopic dermatitis with moderate to severe excoriation |
| EP3542788A1 (en) | 2018-03-19 | 2019-09-25 | MC2 Therapeutics Limited | Topical composition comprising calcipotriol and betamethasone dipropionate |
| CN108210462A (zh) * | 2018-03-29 | 2018-06-29 | 苏州尚宜佳生物科技有限公司 | 一种克立硼罗局部缓释脂质体的制法与应用 |
| CN108324724A (zh) * | 2018-04-10 | 2018-07-27 | 苏州芝宇生物科技有限公司 | 一种克立硼罗可溶性膜制剂的制法及其应用 |
| CN110464702A (zh) * | 2018-05-09 | 2019-11-19 | 上海键合医药科技有限公司 | 一种克立硼罗的软膏剂及其制备方法 |
| MX2020013192A (es) | 2018-06-04 | 2021-08-16 | Arcutis Inc | Metodo y formulacion para mejorar el tiempo de retraso de penetracion en la piel de roflumilast. |
| CN108992454B (zh) | 2018-06-20 | 2020-06-02 | 合肥医工医药股份有限公司 | 一种治疗皮肤炎症性疾病的复方药物组合物 |
| CN108785379A (zh) * | 2018-06-26 | 2018-11-13 | 苏州尚宜佳生物科技有限公司 | 一种克立硼罗清凉缓释膜及其制备方法 |
| CN108524648A (zh) * | 2018-06-26 | 2018-09-14 | 苏州尚宜佳生物科技有限公司 | 一种克立硼罗复合保健缓释膜及其制备方法 |
| CN108785372A (zh) * | 2018-06-27 | 2018-11-13 | 苏州尚宜佳生物科技有限公司 | 一种克立硼罗燥湿利尿缓释膜及其制备方法 |
| CN108938603A (zh) * | 2018-06-27 | 2018-12-07 | 苏州尚宜佳生物科技有限公司 | 一种缓释效果好的克立硼罗缓释膜及其制备方法 |
| CN108938602A (zh) * | 2018-07-02 | 2018-12-07 | 苏州尚宜佳生物科技有限公司 | 一种吸收效果好的克立硼罗缓释膜及其制备方法 |
| CN108926547A (zh) * | 2018-07-02 | 2018-12-04 | 苏州尚宜佳生物科技有限公司 | 一种粘贴效果好的克立硼罗缓释膜及其制备方法 |
| CN108853063A (zh) * | 2018-07-04 | 2018-11-23 | 苏州尚宜佳生物科技有限公司 | 一种透气效果好的克立硼罗缓释膜的制备方法 |
| CN108853062A (zh) * | 2018-07-04 | 2018-11-23 | 苏州尚宜佳生物科技有限公司 | 一种肤感克立硼罗缓释膜的制备方法 |
| CN108853064A (zh) * | 2018-07-09 | 2018-11-23 | 苏州尚宜佳生物科技有限公司 | 一种防水透气克立硼罗缓释膜的制备方法 |
| CN108653246A (zh) * | 2018-07-09 | 2018-10-16 | 苏州尚宜佳生物科技有限公司 | 一种防水效果好的克立硼罗缓释膜的制备方法 |
| WO2020025910A1 (en) | 2018-07-31 | 2020-02-06 | Drug Delivery Solutions Limited | Topical composition |
| WO2020051230A1 (en) * | 2018-09-04 | 2020-03-12 | X-Rx, Inc. | Amorphous pharmaceutical compositions and uses thereof |
| US20220002306A1 (en) * | 2018-09-29 | 2022-01-06 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | Crystal form of upadacitinib and preparation method and use thereof |
| CN111217819B (zh) * | 2018-11-27 | 2021-05-14 | 杭州科巢生物科技有限公司 | 乌帕替尼的合成方法 |
| CA3119773A1 (en) | 2018-11-30 | 2020-06-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| CN114929227A (zh) * | 2019-09-30 | 2022-08-19 | 艾伯维公司 | 用乌帕替尼治疗脊柱关节炎和银屑病 |
| CN115397411B (zh) * | 2020-04-23 | 2025-08-22 | 浙江养生堂天然药物研究所有限公司 | 药物组合及其用途 |
| BR112022025728A2 (pt) * | 2020-06-17 | 2023-01-03 | Kymera Therapeutics Inc | Agentes de degradação de irak e usos dos mesmos |
| BR112023002533A2 (pt) * | 2020-08-20 | 2023-03-14 | Pfizer | Formulações tópicas estáveis de 1(r)-4-(5-(4-metóxi-3-propoxifenil)piridin-3-il)-1,2-oxaborolan-2-ol |
| CN112168774A (zh) * | 2020-11-04 | 2021-01-05 | 南京康川济医药科技有限公司 | 一种巴瑞克替尼乳膏及其制备方法和应用 |
| EP4255393B1 (en) | 2020-12-04 | 2025-05-28 | Arcutis Biotherapeutics, Inc. | Topical roflumilast formulation having antifungal properties |
| MX2023007852A (es) | 2020-12-30 | 2023-07-07 | Kymera Therapeutics Inc | Degradadores de cinasas asociadas al receptor de interleucina-1 (irak) y usos de los mismos. |
| AU2022220869A1 (en) | 2021-02-15 | 2023-08-24 | Kymera Therapeutics, Inc. | Irak4 degraders and uses thereof |
| EP4422635A4 (en) | 2021-10-29 | 2025-11-26 | Kymera Therapeutics Inc | IRAQ4 DEGRADATION AGENTS AND THEIR SYNTHESIS |
| MX2024008192A (es) | 2021-12-28 | 2024-09-10 | Arcutis Biotherapeutics Inc | Espumas en aerosol de roflumilast topico. |
| AU2022435654A1 (en) * | 2022-01-20 | 2024-08-01 | Renata Pharmaceutical (Ireland) Limited | Sustained release pharmaceutical composition of upadacitinib |
| AU2023214044A1 (en) | 2022-01-31 | 2024-08-08 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| JP2025530005A (ja) | 2022-09-15 | 2025-09-09 | アーキュティス・バイオセラピューティクス・インコーポレーテッド | ロフルミラスト及び大量のロフルミラストを溶解可能な溶媒の医薬組成物 |
| 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 |
| CN116715687A (zh) * | 2023-05-25 | 2023-09-08 | 福建南方制药股份有限公司 | 一种工业化制备克立硼罗晶型i的方法 |
| CN119345120B (zh) * | 2024-12-26 | 2025-03-14 | 新基元(北京)医药科技有限公司 | 一种克立硼罗软膏及其制备方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4282216A (en) * | 1977-04-20 | 1981-08-04 | Johnson & Johnson | Topical anti-inflammatory drug therapy |
| CA2597982C (en) | 2005-02-16 | 2014-07-08 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules |
| RS54108B1 (sr) | 2006-02-16 | 2015-12-31 | Anacor Pharmaceuticals Inc. | Mali molekuli koji sadrže boron kao agensi protiv zapaljenja |
| JP5745279B2 (ja) * | 2008-01-09 | 2015-07-08 | 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 | 抗炎症剤としてのホウ素含有小分子 |
| EP2187893A4 (en) | 2008-03-06 | 2012-02-22 | Anacor Pharmaceuticals Inc | SMALL BORON-CONTAINING MOLECULES AS ANTI-INFLAMMATORY AGENTS |
| EP2564857B1 (en) * | 2008-03-06 | 2017-05-03 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules as anti-inflammatory agents |
| US8716478B2 (en) | 2010-01-27 | 2014-05-06 | Anacor Pharmaceuticals, Inc. | Boron-containing small molecules |
| GB201402070D0 (en) * | 2014-02-07 | 2014-03-26 | Galapagos Nv | Pharmaceutical compositions for the treatment of inflammatory disorders |
-
2016
- 2016-11-23 DK DK16805522.6T patent/DK3383363T3/da active
- 2016-11-23 PL PL16805522T patent/PL3383363T3/pl unknown
- 2016-11-23 HU HUE16805522A patent/HUE053115T2/hu unknown
- 2016-11-23 SI SI201631089T patent/SI3383363T1/sl unknown
- 2016-11-23 KR KR1020187018210A patent/KR102106230B1/ko active Active
- 2016-11-23 SG SG10202112628UA patent/SG10202112628UA/en unknown
- 2016-11-23 MX MX2018006578A patent/MX378145B/es unknown
- 2016-11-23 HK HK19100162.1A patent/HK1257818A1/zh unknown
- 2016-11-23 PT PT168055226T patent/PT3383363T/pt unknown
- 2016-11-23 EP EP20215322.7A patent/EP3831389A1/en active Pending
- 2016-11-23 CN CN201680069997.3A patent/CN108366958A/zh active Pending
- 2016-11-23 SG SG11201803728YA patent/SG11201803728YA/en unknown
- 2016-11-23 WO PCT/IB2016/057073 patent/WO2017093857A1/en not_active Ceased
- 2016-11-23 NZ NZ742208A patent/NZ742208A/en unknown
- 2016-11-23 ES ES16805522T patent/ES2858311T3/es active Active
- 2016-11-23 EP EP16805522.6A patent/EP3383363B1/en active Active
- 2016-11-23 AU AU2016362668A patent/AU2016362668C1/en active Active
- 2016-11-23 RU RU2018119295A patent/RU2724053C2/ru active
- 2016-11-23 BR BR112018010464-7A patent/BR112018010464B1/pt active IP Right Grant
- 2016-11-23 IL IL259693A patent/IL259693B2/en unknown
- 2016-11-25 CA CA2949614A patent/CA2949614C/en active Active
- 2016-11-28 JP JP2016229721A patent/JP6725403B2/ja active Active
- 2016-11-29 TW TW105139318A patent/TWI627974B/zh active
- 2016-11-30 US US15/364,347 patent/US20170152273A1/en not_active Abandoned
-
2018
- 2018-05-04 ZA ZA2018/02920A patent/ZA201802920B/en unknown
-
2019
- 2019-06-25 US US16/451,107 patent/US20190308994A1/en not_active Abandoned
-
2021
- 2021-02-25 CY CY20211100160T patent/CY1123845T1/el unknown
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