JP2019505533A5 - - Google Patents
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- Publication number
- JP2019505533A5 JP2019505533A5 JP2018540799A JP2018540799A JP2019505533A5 JP 2019505533 A5 JP2019505533 A5 JP 2019505533A5 JP 2018540799 A JP2018540799 A JP 2018540799A JP 2018540799 A JP2018540799 A JP 2018540799A JP 2019505533 A5 JP2019505533 A5 JP 2019505533A5
- Authority
- JP
- Japan
- Prior art keywords
- crystal form
- ray powder
- crystalline
- diffraction pattern
- powder diffraction
- 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
- 239000013078 crystal Substances 0.000 claims 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 238000002425 crystallisation Methods 0.000 claims 4
- 230000008025 crystallization Effects 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 239000002904 solvent Substances 0.000 claims 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 2
- ZXEKIIBDNHEJCQ-UHFFFAOYSA-N isobutanol Chemical compound CC(C)CO ZXEKIIBDNHEJCQ-UHFFFAOYSA-N 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims 1
- 102000008236 Toll-Like Receptor 7 Human genes 0.000 claims 1
- 108010060825 Toll-Like Receptor 7 Proteins 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 238000004090 dissolution Methods 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 208000010710 hepatitis C virus infection Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000012046 mixed solvent Substances 0.000 claims 1
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 1
- 238000005406 washing Methods 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610082029.8 | 2016-02-05 | ||
| CN201610082029.8A CN107043379A (zh) | 2016-02-05 | 2016-02-05 | 一种tlr7激动剂的晶型a、其制备方法和医药用途 |
| PCT/CN2017/072891 WO2017133684A1 (zh) | 2016-02-05 | 2017-02-04 | 一种tlr7激动剂的晶型a、其制备方法和用途 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019505533A JP2019505533A (ja) | 2019-02-28 |
| JP2019505533A5 true JP2019505533A5 (enExample) | 2020-02-27 |
| JP6889171B2 JP6889171B2 (ja) | 2021-06-18 |
Family
ID=59499348
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018540799A Active JP6889171B2 (ja) | 2016-02-05 | 2017-02-04 | Ｔｌｒ７アゴニスト結晶形ａ、その調製方法及び使用 |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US10442811B2 (enExample) |
| EP (1) | EP3412672B1 (enExample) |
| JP (1) | JP6889171B2 (enExample) |
| KR (1) | KR102393280B1 (enExample) |
| CN (2) | CN107043379A (enExample) |
| AR (1) | AR107548A1 (enExample) |
| AU (1) | AU2017215801B2 (enExample) |
| CA (1) | CA3013518C (enExample) |
| CL (1) | CL2018002092A1 (enExample) |
| DK (1) | DK3412672T3 (enExample) |
| EA (1) | EA035951B1 (enExample) |
| ES (1) | ES2830443T3 (enExample) |
| HR (1) | HRP20201644T1 (enExample) |
| HU (1) | HUE051399T2 (enExample) |
| IL (1) | IL260968B (enExample) |
| LT (1) | LT3412672T (enExample) |
| MX (1) | MX374297B (enExample) |
| NZ (1) | NZ744884A (enExample) |
| PH (1) | PH12018501643A1 (enExample) |
| PL (1) | PL3412672T3 (enExample) |
| PT (1) | PT3412672T (enExample) |
| SG (1) | SG11201806683UA (enExample) |
| SI (1) | SI3412672T1 (enExample) |
| TW (1) | TWI754629B (enExample) |
| UA (1) | UA121161C2 (enExample) |
| WO (1) | WO2017133684A1 (enExample) |
| ZA (1) | ZA201805186B (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20180229A (es) | 2015-10-29 | 2018-08-24 | Novartis Ag | Conjugados de anticuerpos que comprenden un agonista del receptor tipo toll |
| CN107043378A (zh) * | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种吡咯并[3,2-d]嘧啶类化合物的制备方法及其中间体 |
| CN107043379A (zh) * | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种tlr7激动剂的晶型a、其制备方法和医药用途 |
| CN107043380A (zh) * | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种tlr7激动剂的马来酸盐、其晶型c、晶型d、晶型e、制备方法和用途 |
| CN112105620B (zh) * | 2018-05-25 | 2026-02-24 | 正大天晴药业集团股份有限公司 | 用于治疗肺癌的tlr7激动剂及其药物组合 |
| BR112021015577A2 (pt) | 2019-02-08 | 2021-10-05 | Research & Business Foundation Sungkyunkwan University | Complexo-colesterol agonista do receptor toll-like 7 ou 8 e uso do mesmo |
| ES3070986T3 (en) | 2019-03-15 | 2026-06-18 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Toll-like receptor agonists for use in the treatment of hepatitis b |
| SG11202111488YA (en) * | 2019-04-23 | 2021-11-29 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Solid pharmaceutical composition comprising tlr7 agonist |
| CN115666637A (zh) | 2020-03-02 | 2023-01-31 | 蛋白科技先锋 | 基于病原体细胞壁骨架的模拟活病原体的纳米粒子及其制备方法 |
| EP4194008A4 (en) | 2020-08-04 | 2025-01-08 | Progeneer Inc. | Kinetically acting adjuvant ensemble |
| US20230277525A1 (en) | 2020-08-04 | 2023-09-07 | Progeneer Inc | Conjugate of functional drug and toll-like receptor 7 or 8 agonist of which active site is temporarily inactivated and use thereof |
| WO2022031021A1 (ko) | 2020-08-04 | 2022-02-10 | 성균관대학교산학협력단 | 동력학적 제어가 가능한 아주번트를 포함하는 mrna 백신 |
| CN119431359A (zh) * | 2023-07-28 | 2025-02-14 | 苏州申拓医药科技有限公司 | 一种tlr7/8激动剂的可药用盐、晶型及其制备方法、药物组合物和用途 |
| WO2025110816A1 (ko) | 2023-11-23 | 2025-05-30 | 프로지니어 주식회사 | 암의 치료를 위한 활성화 부위가 일시적으로 비활성화된 톨-유사 수용체 7 또는 8 작용자와 항암 치료의 병용요법 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3376479B2 (ja) * | 1991-08-12 | 2003-02-10 | 武田薬品工業株式会社 | 縮合ピリミジン誘導体、その製造法および用途 |
| CA2620182A1 (en) * | 2005-08-22 | 2007-03-01 | Dennis A. Carson | Tlr agonists |
| UY32306A (es) | 2008-12-09 | 2010-07-30 | Gilead Sciences Inc | Derivados de pteridinona y pirimidinodiazepinona y composiciones farmacéuticas que modulan en forma selectiva los receptores tipo toll, métodos y usos |
| JP5813785B2 (ja) | 2011-02-04 | 2015-11-17 | デュケイン ユニバーシティー オブ ザ ホリー スピリット | 抗チューブリン活性を有する二環式および三環式のピリミジンチロシンキナーゼ阻害剤ならびに患者の処置方法 |
| WO2013103967A1 (en) | 2012-01-05 | 2013-07-11 | Northeastern University | Allosteric modulators of cb1 cannabinoid receptors |
| MX386924B (es) * | 2012-10-10 | 2025-03-19 | Janssen Sciences Ireland Uc | Derivados pirrolo[3,2-d]pirimidínicos para el tratamiento de infecciones víricas y otras enfermedades. |
| JP6216387B2 (ja) | 2012-11-20 | 2017-10-18 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | 新規化合物 |
| KR20150085081A (ko) * | 2012-11-20 | 2015-07-22 | 글락소스미스클라인 엘엘씨 | 신규 화합물 |
| SMT201700378T1 (it) * | 2012-11-20 | 2017-09-07 | Glaxosmithkline Llc | Nuovi composti |
| WO2015168269A1 (en) | 2014-05-01 | 2015-11-05 | Novartis Ag | Compounds and compositions as toll-like receptor 7 agonists |
| CN105367576A (zh) | 2014-08-15 | 2016-03-02 | 正大天晴药业集团股份有限公司 | 作为tlr7激动剂的吡咯并嘧啶化合物 |
| CN112898308B (zh) * | 2014-08-15 | 2026-08-07 | 正大天晴药业集团股份有限公司 | 作为tlr7激动剂的吡咯并嘧啶化合物 |
| CN107043380A (zh) | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种tlr7激动剂的马来酸盐、其晶型c、晶型d、晶型e、制备方法和用途 |
| CN107043379A (zh) * | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种tlr7激动剂的晶型a、其制备方法和医药用途 |
-
2016
- 2016-02-05 CN CN201610082029.8A patent/CN107043379A/zh active Pending
-
2017
- 2017-02-03 TW TW106103695A patent/TWI754629B/zh active
- 2017-02-04 EP EP17747004.4A patent/EP3412672B1/en active Active
- 2017-02-04 US US16/075,297 patent/US10442811B2/en active Active
- 2017-02-04 PL PL17747004T patent/PL3412672T3/pl unknown
- 2017-02-04 UA UAA201809129A patent/UA121161C2/uk unknown
- 2017-02-04 NZ NZ744884A patent/NZ744884A/en unknown
- 2017-02-04 SI SI201730461T patent/SI3412672T1/sl unknown
- 2017-02-04 HU HUE17747004A patent/HUE051399T2/hu unknown
- 2017-02-04 SG SG11201806683UA patent/SG11201806683UA/en unknown
- 2017-02-04 CA CA3013518A patent/CA3013518C/en active Active
- 2017-02-04 HR HRP20201644TT patent/HRP20201644T1/hr unknown
- 2017-02-04 AU AU2017215801A patent/AU2017215801B2/en active Active
- 2017-02-04 MX MX2018009501A patent/MX374297B/es active IP Right Grant
- 2017-02-04 WO PCT/CN2017/072891 patent/WO2017133684A1/zh not_active Ceased
- 2017-02-04 CN CN201780009747.5A patent/CN108602831B9/zh active Active
- 2017-02-04 EA EA201891768A patent/EA035951B1/ru not_active IP Right Cessation
- 2017-02-04 ES ES17747004T patent/ES2830443T3/es active Active
- 2017-02-04 JP JP2018540799A patent/JP6889171B2/ja active Active
- 2017-02-04 KR KR1020187024627A patent/KR102393280B1/ko active Active
- 2017-02-04 PT PT177470044T patent/PT3412672T/pt unknown
- 2017-02-04 LT LTEP17747004.4T patent/LT3412672T/lt unknown
- 2017-02-04 DK DK17747004.4T patent/DK3412672T3/da active
- 2017-02-06 AR ARP170100297A patent/AR107548A1/es not_active Application Discontinuation
-
2018
- 2018-08-01 ZA ZA2018/05186A patent/ZA201805186B/en unknown
- 2018-08-02 IL IL260968A patent/IL260968B/en unknown
- 2018-08-02 PH PH12018501643A patent/PH12018501643A1/en unknown
- 2018-08-03 CL CL2018002092A patent/CL2018002092A1/es unknown
-
2019
- 2019-09-25 US US16/582,575 patent/US10947245B2/en active Active
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