CA3013518C - Tlr7 agonist crystalline form a, preparation method and use thereof - Google Patents
Tlr7 agonist crystalline form a, preparation method and use thereof Download PDFInfo
- Publication number
- CA3013518C CA3013518C CA3013518A CA3013518A CA3013518C CA 3013518 C CA3013518 C CA 3013518C CA 3013518 A CA3013518 A CA 3013518A CA 3013518 A CA3013518 A CA 3013518A CA 3013518 C CA3013518 C CA 3013518C
- Authority
- CA
- Canada
- Prior art keywords
- crystal form
- compound
- formula
- preparing
- virus infection
- 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.)
- Active
Links
Classifications
-
- 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
-
- 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)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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 (2)
| Publication Number | Publication Date |
|---|---|
| CA3013518A1 CA3013518A1 (en) | 2017-08-10 |
| CA3013518C true CA3013518C (en) | 2022-07-19 |
Family
ID=59499348
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3013518A Active CA3013518C (en) | 2016-02-05 | 2017-02-04 | Tlr7 agonist crystalline form a, preparation method and use thereof |
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
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US10947245B2 (en) | Crystal form A of 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine for inhibiting toll-like receptor activity | |
| CA3013521C (en) | Trifluoroacetate salt of a pyrrolo[3,2-d]pyrimidin compound as tlr7 agonist and crystalline form b thereof | |
| CA3013682C (en) | Maleate salt of a pyrrolo[3,2-d]pyrimidine compound as tlr7 agonist and crystalline forms c, d and e thereof | |
| HK1259182B (en) | Tlr7 agonist trifluoroacetate salt and crystalline form b thereof, preparation methods and uses | |
| HK1259170B (en) | Tlr7 agonist crystalline form a, preparation method and use thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20200225 |
|
| MPN | Maintenance fee for patent paid |
Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 8TH ANNIV.) - STANDARD Year of fee payment: 8 |
|
| U00 | Fee paid |
Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED Effective date: 20241205 |
|
| U11 | Full renewal or maintenance fee paid |
Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT Effective date: 20241205 Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL Effective date: 20241205 |
|
| MPN | Maintenance fee for patent paid |
Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 9TH ANNIV.) - STANDARD Year of fee payment: 9 |
|
| U00 | Fee paid |
Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED Effective date: 20251202 |
|
| U11 | Full renewal or maintenance fee paid |
Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL Effective date: 20251202 |