EA037048B1 - Трифторацетатная соль агониста tlr7 и ее кристаллическая форма b, способы получения и использование - Google Patents

Трифторацетатная соль агониста tlr7 и ее кристаллическая форма b, способы получения и использование Download PDF

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Publication number
EA037048B1
EA037048B1 EA201891772A EA201891772A EA037048B1 EA 037048 B1 EA037048 B1 EA 037048B1 EA 201891772 A EA201891772 A EA 201891772A EA 201891772 A EA201891772 A EA 201891772A EA 037048 B1 EA037048 B1 EA 037048B1
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EA
Eurasian Patent Office
Prior art keywords
compound
formula
crystalline form
trifluoroacetate
crystalline
Prior art date
Application number
EA201891772A
Other languages
English (en)
Russian (ru)
Other versions
EA201891772A1 (ru
Inventor
Чжаочжун Дин
Фей Сунь
Инху Ху
Илун Чжоу
Чжэн Ван
Жуй Чжао
Лин Ян
Original Assignee
Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд.
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Application filed by Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд. filed Critical Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд.
Publication of EA201891772A1 publication Critical patent/EA201891772A1/ru
Publication of EA037048B1 publication Critical patent/EA037048B1/ru

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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
    • 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
    • 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
    • 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

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  • 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)
EA201891772A 2016-02-05 2017-02-04 Трифторацетатная соль агониста tlr7 и ее кристаллическая форма b, способы получения и использование EA037048B1 (ru)

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 (2)

Publication Number Publication Date
EA201891772A1 EA201891772A1 (ru) 2019-01-31
EA037048B1 true EA037048B1 (ru) 2021-01-29

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EA201891772A EA037048B1 (ru) 2016-02-05 2017-02-04 Трифторацетатная соль агониста tlr7 и ее кристаллическая форма b, способы получения и использование

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)

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* Cited by examiner, † Cited by third party
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

Citations (4)

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WO2014056953A1 (en) * 2012-10-10 2014-04-17 Janssen R&D Ireland Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
WO2015168279A1 (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
WO2016107536A1 (zh) * 2014-12-29 2016-07-07 南京明德新药研发股份有限公司 一类Toll样受体7激动剂

Family Cites Families (7)

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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
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
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014056953A1 (en) * 2012-10-10 2014-04-17 Janssen R&D Ireland Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
WO2015168279A1 (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
WO2016107536A1 (zh) * 2014-12-29 2016-07-07 南京明德新药研发股份有限公司 一类Toll样受体7激动剂

Also Published As

Publication number Publication date
MY198137A (en) 2023-08-07
HK1259182A1 (zh) 2019-11-29
EP3412674B1 (en) 2020-09-16
EP3412674A1 (en) 2018-12-12
EP3412674A4 (en) 2019-07-17
BR112018015878A2 (pt) 2018-12-26
SG11201806688QA (en) 2018-09-27
CA3013521A1 (en) 2017-08-10
NZ745023A (en) 2022-09-30
AU2017214135A1 (en) 2018-08-23
UA121276C2 (uk) 2020-04-27
HUE052210T2 (hu) 2021-04-28
CN108602833A (zh) 2018-09-28
AR107550A1 (es) 2018-05-09
TWI778952B (zh) 2022-10-01
PH12018501641B1 (en) 2021-03-26
IL260981B (en) 2022-05-01
TW201728591A (zh) 2017-08-16
MX2018009503A (es) 2018-12-11
US10683296B2 (en) 2020-06-16
KR102393281B1 (ko) 2022-05-02
CN107043377A (zh) 2017-08-15
ZA201805240B (en) 2024-09-25
ES2834304T3 (es) 2021-06-17
AU2017214135B2 (en) 2020-08-13
CA3013521C (en) 2022-07-12
WO2017133687A1 (zh) 2017-08-10
PH12018501641A1 (en) 2019-06-03
US20190031666A1 (en) 2019-01-31
DK3412674T3 (da) 2020-11-09
CL2018002101A1 (es) 2018-12-07
KR20180104118A (ko) 2018-09-19
JP6877450B2 (ja) 2021-05-26
MX374300B (es) 2025-03-06
CN108602833B (zh) 2020-07-28
JP2019504103A (ja) 2019-02-14
EA201891772A1 (ru) 2019-01-31

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