TWI754629B - Tlr7促效劑的晶型a、其製備方法、藥物組合物和用途 - Google Patents

Tlr7促效劑的晶型a、其製備方法、藥物組合物和用途 Download PDF

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TWI754629B
TWI754629B TW106103695A TW106103695A TWI754629B TW I754629 B TWI754629 B TW I754629B TW 106103695 A TW106103695 A TW 106103695A TW 106103695 A TW106103695 A TW 106103695A TW I754629 B TWI754629 B TW I754629B
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Taiwan
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crystal form
formula
compound
compound represented
aforementioned
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TW106103695A
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Chinese (zh)
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TW201728589A (zh
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照中 丁
孫飛
胡迎虎
周義龍
王崢
趙銳
楊玲
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大陸商正大天晴藥業集團股份有限公司
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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)
TW106103695A 2016-02-05 2017-02-03 Tlr7促效劑的晶型a、其製備方法、藥物組合物和用途 TWI754629B (zh)

Applications Claiming Priority (2)

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

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TW201728589A TW201728589A (zh) 2017-08-16
TWI754629B true TWI754629B (zh) 2022-02-11

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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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WO2007024707A2 (en) * 2005-08-22 2007-03-01 The Regents Of The University Of California Tlr agonists
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
WO2014081643A1 (en) * 2012-11-20 2014-05-30 Glaxosmithkline Llc Novel compounds
WO2014081645A1 (en) * 2012-11-20 2014-05-30 Glaxosmithkline Llc Novel compounds
WO2014081644A1 (en) * 2012-11-20 2014-05-30 Glaxosmithkline Llc Novel compounds

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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
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.
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

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WO2007024707A2 (en) * 2005-08-22 2007-03-01 The Regents Of The University Of California Tlr agonists
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
WO2014081643A1 (en) * 2012-11-20 2014-05-30 Glaxosmithkline Llc Novel compounds
WO2014081645A1 (en) * 2012-11-20 2014-05-30 Glaxosmithkline Llc Novel compounds
WO2014081644A1 (en) * 2012-11-20 2014-05-30 Glaxosmithkline Llc Novel compounds

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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
EA035951B1 (ru) 2020-09-04
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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