EA035951B1 - Кристаллическая форма a агониста tlr7, ее способ получения и использование - Google Patents

Кристаллическая форма a агониста tlr7, ее способ получения и использование Download PDF

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Publication number
EA035951B1
EA035951B1 EA201891768A EA201891768A EA035951B1 EA 035951 B1 EA035951 B1 EA 035951B1 EA 201891768 A EA201891768 A EA 201891768A EA 201891768 A EA201891768 A EA 201891768A EA 035951 B1 EA035951 B1 EA 035951B1
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EA
Eurasian Patent Office
Prior art keywords
compound
formula
crystalline form
crystalline
composition
Prior art date
Application number
EA201891768A
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English (en)
Russian (ru)
Other versions
EA201891768A1 (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 EA201891768A1 publication Critical patent/EA201891768A1/ru
Publication of EA035951B1 publication Critical patent/EA035951B1/ru

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    • 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
    • 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
    • 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)
  • 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)
EA201891768A 2016-02-05 2017-02-04 Кристаллическая форма a агониста tlr7, ее способ получения и использование EA035951B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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
EA201891768A1 EA201891768A1 (ru) 2019-01-31
EA035951B1 true EA035951B1 (ru) 2020-09-04

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EA201891768A EA035951B1 (ru) 2016-02-05 2017-02-04 Кристаллическая форма a агониста tlr7, ее способ получения и использование

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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)

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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

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CN104780924A (zh) * 2012-11-20 2015-07-15 葛兰素史克有限责任公司 新颖的化合物
CN104780923A (zh) * 2012-11-20 2015-07-15 葛兰素史克有限责任公司 新颖的化合物
CN104837840A (zh) * 2012-10-10 2015-08-12 爱尔兰詹森科学公司 用于治疗病毒感染及其他疾病的吡咯并[3,2-d]嘧啶衍生物
WO2015168269A1 (en) * 2014-05-01 2015-11-05 Novartis Ag Compounds and compositions as toll-like receptor 7 agonists
WO2016023511A1 (zh) * 2014-08-15 2016-02-18 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

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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
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
SMT201700378T1 (it) * 2012-11-20 2017-09-07 Glaxosmithkline Llc Nuovi composti
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
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

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104837840A (zh) * 2012-10-10 2015-08-12 爱尔兰詹森科学公司 用于治疗病毒感染及其他疾病的吡咯并[3,2-d]嘧啶衍生物
CN104780924A (zh) * 2012-11-20 2015-07-15 葛兰素史克有限责任公司 新颖的化合物
CN104780923A (zh) * 2012-11-20 2015-07-15 葛兰素史克有限责任公司 新颖的化合物
WO2015168269A1 (en) * 2014-05-01 2015-11-05 Novartis Ag Compounds and compositions as toll-like receptor 7 agonists
WO2016023511A1 (zh) * 2014-08-15 2016-02-18 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

Also Published As

Publication number Publication date
MX374297B (es) 2025-03-06
HUE051399T2 (hu) 2021-03-01
PT3412672T (pt) 2020-11-11
JP2019505533A (ja) 2019-02-28
US10947245B2 (en) 2021-03-16
KR102393280B1 (ko) 2022-05-02
CA3013518C (en) 2022-07-19
TWI754629B (zh) 2022-02-11
HK1259170A1 (zh) 2019-11-29
CN108602831B9 (zh) 2020-12-04
AR107548A1 (es) 2018-05-09
AU2017215801A1 (en) 2018-08-23
DK3412672T3 (da) 2020-10-19
SI3412672T1 (sl) 2021-02-26
KR20180104117A (ko) 2018-09-19
IL260968B (en) 2022-05-01
EP3412672B1 (en) 2020-07-15
SG11201806683UA (en) 2018-09-27
PH12018501643A1 (en) 2019-06-03
US10442811B2 (en) 2019-10-15
HRP20201644T1 (hr) 2020-12-25
AU2017215801B2 (en) 2020-09-10
LT3412672T (lt) 2020-11-10
EA201891768A1 (ru) 2019-01-31
ES2830443T3 (es) 2021-06-03
CA3013518A1 (en) 2017-08-10
CL2018002092A1 (es) 2018-12-07
WO2017133684A1 (zh) 2017-08-10
ZA201805186B (en) 2024-08-28
NZ744884A (en) 2022-09-30
US20190040071A1 (en) 2019-02-07
CN108602831B (zh) 2020-11-03
EP3412672A1 (en) 2018-12-12
US20200039988A1 (en) 2020-02-06
CN107043379A (zh) 2017-08-15
MX2018009501A (es) 2018-12-11
EP3412672A4 (en) 2019-07-17
TW201728589A (zh) 2017-08-16
PL3412672T3 (pl) 2021-01-25
JP6889171B2 (ja) 2021-06-18
CN108602831A (zh) 2018-09-28
UA121161C2 (uk) 2020-04-10
BR112018015880A2 (pt) 2018-12-26

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