JP2019505532A5 - - Google Patents
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- Publication number
- JP2019505532A5 JP2019505532A5 JP2018540750A JP2018540750A JP2019505532A5 JP 2019505532 A5 JP2019505532 A5 JP 2019505532A5 JP 2018540750 A JP2018540750 A JP 2018540750A JP 2018540750 A JP2018540750 A JP 2018540750A JP 2019505532 A5 JP2019505532 A5 JP 2019505532A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline form
- formula
- ray powder
- 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
- 238000000634 powder X-ray diffraction Methods 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 8
- 238000000034 method Methods 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 6
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 4
- 150000002689 maleic acids Chemical class 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- 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
- 102000008236 Toll-Like Receptor 7 Human genes 0.000 claims 3
- 108010060825 Toll-Like Receptor 7 Proteins 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 238000001035 drying Methods 0.000 claims 3
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 3
- 238000005406 washing Methods 0.000 claims 3
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- ZXEKIIBDNHEJCQ-UHFFFAOYSA-N isobutanol Chemical compound CC(C)CO ZXEKIIBDNHEJCQ-UHFFFAOYSA-N 0.000 claims 2
- 239000011976 maleic acid Substances 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 238000004090 dissolution Methods 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 208000010710 hepatitis C virus infection Diseases 0.000 claims 1
- 150000002688 maleic acid derivatives Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610082030.0 | 2016-02-05 | ||
| CN201610082030.0A CN107043380A (zh) | 2016-02-05 | 2016-02-05 | 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 |
| PCT/CN2017/072890 WO2017133683A1 (zh) | 2016-02-05 | 2017-02-04 | 一种tlr7激动剂的马来酸盐、其晶型c、晶型d、晶型e及其制备方法和用途 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019505532A JP2019505532A (ja) | 2019-02-28 |
| JP2019505532A5 true JP2019505532A5 (2) | 2020-02-27 |
| JP6898336B2 JP6898336B2 (ja) | 2021-07-07 |
Family
ID=59500111
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018540750A Active JP6898336B2 (ja) | 2016-02-05 | 2017-02-04 | Ｔｌｒ７アゴニストのマレイン酸塩、その結晶形ｃ、ｄ及びｅ、マレイン酸塩及び結晶形の調製方法及び使用 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US10780091B2 (2) |
| EP (1) | EP3412671B1 (2) |
| JP (1) | JP6898336B2 (2) |
| KR (1) | KR102393279B1 (2) |
| CN (2) | CN107043380A (2) |
| AR (1) | AR107547A1 (2) |
| AU (1) | AU2017215800B2 (2) |
| CA (1) | CA3013682C (2) |
| CL (1) | CL2018002089A1 (2) |
| DK (1) | DK3412671T3 (2) |
| EA (1) | EA038794B1 (2) |
| ES (1) | ES2834303T3 (2) |
| HU (1) | HUE052211T2 (2) |
| IL (1) | IL260965B (2) |
| MX (1) | MX374295B (2) |
| MY (1) | MY196762A (2) |
| NZ (1) | NZ745231A (2) |
| PH (1) | PH12018501644B1 (2) |
| SG (1) | SG11201806682TA (2) |
| TW (1) | TWI778951B (2) |
| UA (1) | UA123781C2 (2) |
| WO (1) | WO2017133683A1 (2) |
| ZA (1) | ZA201805185B (2) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AU2019272478B2 (en) * | 2018-05-25 | 2024-06-06 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | TLR7 agonist and pharmaceutical combination thereof for treating lung cancer |
| WO2020162705A1 (ko) | 2019-02-08 | 2020-08-13 | 성균관대학교산학협력단 | 톨-유사 수용체 7 또는 8 작용자와 콜레스테롤의 결합체 및 그 용도 |
| CA3170551A1 (en) | 2020-03-02 | 2021-09-10 | Yong Taik Lim | Live-pathogen-mimetic nanoparticles based on pathogen cell wall skeleton, and production method thereof |
| 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 |
| JP7690221B2 (ja) | 2020-08-04 | 2025-06-10 | プロジェニア インコーポレイテッド | 動力学的に作用するアジュバントアンサンブル |
| US20230346924A1 (en) | 2020-08-04 | 2023-11-02 | Progeneer Inc. | Mrna vaccine comprising adjuvant capable of kinetic control |
Family Cites Families (26)
| 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 |
| ES2232871T3 (es) | 1996-07-03 | 2005-06-01 | Sumitomo Pharmaceuticals Company, Limited | Nuevos derivados de purina. |
| DE69817393T2 (de) | 1997-11-28 | 2004-06-17 | Sumitomo Pharmaceuticals Co., Ltd. | Neue heterozyklische verbindungen |
| CN101304748A (zh) | 2005-08-22 | 2008-11-12 | 加利福尼亚大学董事会 | Tlr激动剂 |
| CA2691444C (en) | 2007-06-29 | 2016-06-14 | Gilead Sciences, Inc. | Purine derivatives and their use as modulators of toll-like receptor 7 |
| ES2359123T3 (es) | 2007-08-03 | 2011-05-18 | Pfizer Limited | Imidazopiridinonas. |
| RS53347B (sr) | 2008-12-09 | 2014-10-31 | Gilead Sciences, Inc. | Modulatori toll-sličnih receptora |
| WO2012106522A2 (en) | 2011-02-04 | 2012-08-09 | Duquesne University Of The Holy Spirit | Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity and methods of treating a patient |
| EP2800569B1 (en) | 2012-01-05 | 2018-07-25 | Northeastern University | Allosteric modulators of cb1 cannabinoid receptors |
| DK2906563T3 (en) | 2012-10-10 | 2018-06-06 | Janssen Sciences Ireland Uc | PYRROLO [3,2-D] PYRIMIDINE DERIVATIVES FOR TREATING VIRUS INFECTIONS AND OTHER DISEASES |
| AU2013348217B2 (en) * | 2012-11-20 | 2016-10-06 | Glaxosmithkline Llc | Novel compounds |
| BR112015011439A2 (pt) | 2012-11-20 | 2017-07-11 | Glaxosmithkline Llc | composto, composição farmacêutica, composição de vacina, e, uso de um composto |
| EA028480B1 (ru) | 2012-11-20 | 2017-11-30 | ГЛАКСОСМИТКЛАЙН ЭлЭлСи | Новые соединения |
| KR20160124157A (ko) | 2014-02-20 | 2016-10-26 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 인간 인터페론의 유도인자로서의 피롤로[3,2]피리미딘 유도체 |
| ES2908150T3 (es) | 2014-05-01 | 2022-04-27 | Novartis Ag | Compuestos y composiciones como agonistas del receptor de tipo Toll 7 |
| PL3137470T3 (pl) * | 2014-05-01 | 2021-10-11 | Novartis Ag | Związki i kompozycje jako agonisty receptora toll-like 7 |
| HRP20210927T1 (hr) * | 2014-08-15 | 2021-09-03 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Spojevi pirolopirimidina koje se koriste kao agonist tlr7 |
| 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 |
| CN105732635A (zh) | 2014-12-29 | 2016-07-06 | 南京明德新药研发股份有限公司 | 一类Toll样受体7激动剂 |
| MX2018005388A (es) | 2015-11-05 | 2018-08-16 | Basf Se | Oxadiazoles sustituidos para combatir hongos fitopatogenos. |
| UA121345C2 (uk) | 2015-11-05 | 2020-05-12 | Чіа Тай Тяньцин Фармасьютікал Груп Ко., Лтд. | 7-(тіазол-5-іл)піролопіримідин як агоніст рецептора tlr7 |
| TWI714661B (zh) | 2015-11-05 | 2021-01-01 | 法商賽諾菲公司 | 新穎念珠藻素化合物及接合物、其製備與其治療用途 |
| 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 |
| 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 |
| CN107043377A (zh) | 2016-02-05 | 2017-08-15 | 正大天晴药业集团股份有限公司 | 一种tlr7激动剂的三氟乙酸盐、晶型b及其制备方法、药物组合物和用途 |
| 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 |
-
2016
- 2016-02-05 CN CN201610082030.0A patent/CN107043380A/zh active Pending
-
2017
- 2017-02-03 TW TW106103694A patent/TWI778951B/zh active
- 2017-02-04 KR KR1020187024626A patent/KR102393279B1/ko active Active
- 2017-02-04 SG SG11201806682TA patent/SG11201806682TA/en unknown
- 2017-02-04 CN CN201780009746.0A patent/CN108602830B/zh active Active
- 2017-02-04 HU HUE17747003A patent/HUE052211T2/hu unknown
- 2017-02-04 CA CA3013682A patent/CA3013682C/en active Active
- 2017-02-04 EA EA201891770A patent/EA038794B1/ru unknown
- 2017-02-04 UA UAA201809085A patent/UA123781C2/uk unknown
- 2017-02-04 DK DK17747003.6T patent/DK3412671T3/da active
- 2017-02-04 MY MYPI2018702706A patent/MY196762A/en unknown
- 2017-02-04 MX MX2018009500A patent/MX374295B/es active IP Right Grant
- 2017-02-04 WO PCT/CN2017/072890 patent/WO2017133683A1/zh not_active Ceased
- 2017-02-04 AU AU2017215800A patent/AU2017215800B2/en active Active
- 2017-02-04 PH PH1/2018/501644A patent/PH12018501644B1/en unknown
- 2017-02-04 JP JP2018540750A patent/JP6898336B2/ja active Active
- 2017-02-04 US US16/075,080 patent/US10780091B2/en active Active
- 2017-02-04 EP EP17747003.6A patent/EP3412671B1/en active Active
- 2017-02-04 ES ES17747003T patent/ES2834303T3/es active Active
- 2017-02-04 NZ NZ745231A patent/NZ745231A/en unknown
- 2017-02-06 AR ARP170100296A patent/AR107547A1/es active IP Right Grant
-
2018
- 2018-08-01 ZA ZA2018/05185A patent/ZA201805185B/en unknown
- 2018-08-02 IL IL260965A patent/IL260965B/en unknown
- 2018-08-03 CL CL2018002089A patent/CL2018002089A1/es unknown
-
2020
- 2020-08-12 US US16/991,639 patent/US20200368241A1/en not_active Abandoned
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