IL260981B - The trifluoroacetate salt of the tlr7 agonist type b crystal structure, preparation, and methods of use - Google Patents
The trifluoroacetate salt of the tlr7 agonist type b crystal structure, preparation, and methods of useInfo
- Publication number
- IL260981B IL260981B IL260981A IL26098118A IL260981B IL 260981 B IL260981 B IL 260981B IL 260981 A IL260981 A IL 260981A IL 26098118 A IL26098118 A IL 26098118A IL 260981 B IL260981 B IL 260981B
- Authority
- IL
- Israel
- Prior art keywords
- crystalline form
- preparation methods
- trifluoroacetate salt
- tlr7 agonist
- tlr7
- Prior art date
Links
- 229940124615 TLR 7 agonist Drugs 0.000 title 1
- VFRSADQPWYCXDG-LEUCUCNGSA-N ethyl (2s,5s)-5-methylpyrrolidine-2-carboxylate;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.CCOC(=O)[C@@H]1CC[C@H](C)N1 VFRSADQPWYCXDG-LEUCUCNGSA-N 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Physics & Mathematics (AREA)
- Condensed Matter Physics & Semiconductors (AREA)
- Crystallography & Structural Chemistry (AREA)
- General Physics & Mathematics (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610081899.3A CN107043377A (zh) | 2016-02-05 | 2016-02-05 | 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 |
| PCT/CN2017/072894 WO2017133687A1 (zh) | 2016-02-05 | 2017-02-04 | 一种tlr7激动剂的三氟乙酸盐、晶型b、制备方法和用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL260981B true IL260981B (en) | 2022-05-01 |
Family
ID=59500539
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL260981A IL260981B (en) | 2016-02-05 | 2018-08-05 | The trifluoroacetate salt of the tlr7 agonist type b crystal structure, preparation, and methods of use |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US10683296B2 (enExample) |
| EP (1) | EP3412674B1 (enExample) |
| JP (1) | JP6877450B2 (enExample) |
| KR (1) | KR102393281B1 (enExample) |
| CN (2) | CN107043377A (enExample) |
| AR (1) | AR107550A1 (enExample) |
| AU (1) | AU2017214135B2 (enExample) |
| CA (1) | CA3013521C (enExample) |
| CL (1) | CL2018002101A1 (enExample) |
| DK (1) | DK3412674T3 (enExample) |
| EA (1) | EA037048B1 (enExample) |
| ES (1) | ES2834304T3 (enExample) |
| HU (1) | HUE052210T2 (enExample) |
| IL (1) | IL260981B (enExample) |
| MX (1) | MX374300B (enExample) |
| MY (1) | MY198137A (enExample) |
| NZ (1) | NZ745023A (enExample) |
| PH (1) | PH12018501641B1 (enExample) |
| SG (1) | SG11201806688QA (enExample) |
| TW (1) | TWI778952B (enExample) |
| UA (1) | UA121276C2 (enExample) |
| WO (1) | WO2017133687A1 (enExample) |
| ZA (1) | ZA201805240B (enExample) |
Families Citing this family (12)
| 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 |
| US9815850B2 (en) | 2016-02-05 | 2017-11-14 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| 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 |
| 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 |
| WO2022031021A1 (ko) | 2020-08-04 | 2022-02-10 | 성균관대학교산학협력단 | 동력학적 제어가 가능한 아주번트를 포함하는 mrna 백신 |
| 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 |
| EP4463229A1 (en) | 2022-01-12 | 2024-11-20 | Denali Therapeutics Inc. | Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide |
| 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 (11)
| 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 |
| 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 |
| WO2015168269A1 (en) * | 2014-05-01 | 2015-11-05 | Novartis Ag | Compounds and compositions as toll-like receptor 7 agonists |
| SG11201608299TA (en) * | 2014-05-01 | 2016-11-29 | Novartis Ag | Compounds and compositions as toll-like receptor 7 agonists |
| 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 |
| 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 |
-
2016
- 2016-02-05 CN CN201610081899.3A patent/CN107043377A/zh active Pending
-
2017
- 2017-02-03 TW TW106103697A patent/TWI778952B/zh active
- 2017-02-04 UA UAA201809128A patent/UA121276C2/uk unknown
- 2017-02-04 JP JP2018540797A patent/JP6877450B2/ja active Active
- 2017-02-04 CN CN201780009751.1A patent/CN108602833B/zh active Active
- 2017-02-04 ES ES17747007T patent/ES2834304T3/es active Active
- 2017-02-04 EA EA201891772A patent/EA037048B1/ru not_active IP Right Cessation
- 2017-02-04 EP EP17747007.7A patent/EP3412674B1/en active Active
- 2017-02-04 MY MYPI2018702700A patent/MY198137A/en unknown
- 2017-02-04 KR KR1020187024629A patent/KR102393281B1/ko active Active
- 2017-02-04 US US16/075,303 patent/US10683296B2/en active Active
- 2017-02-04 AU AU2017214135A patent/AU2017214135B2/en active Active
- 2017-02-04 CA CA3013521A patent/CA3013521C/en active Active
- 2017-02-04 HU HUE17747007A patent/HUE052210T2/hu unknown
- 2017-02-04 SG SG11201806688QA patent/SG11201806688QA/en unknown
- 2017-02-04 DK DK17747007.7T patent/DK3412674T3/da active
- 2017-02-04 MX MX2018009503A patent/MX374300B/es active IP Right Grant
- 2017-02-04 NZ NZ745023A patent/NZ745023A/en unknown
- 2017-02-04 WO PCT/CN2017/072894 patent/WO2017133687A1/zh not_active Ceased
- 2017-02-06 AR ARP170100299A patent/AR107550A1/es not_active Application Discontinuation
-
2018
- 2018-08-02 PH PH12018501641A patent/PH12018501641B1/en unknown
- 2018-08-03 ZA ZA2018/05240A patent/ZA201805240B/en unknown
- 2018-08-03 CL CL2018002101A patent/CL2018002101A1/es unknown
- 2018-08-05 IL IL260981A patent/IL260981B/en unknown
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