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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crystal form
formula
compound
compound represented
aforementioned
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TW106103695A
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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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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline 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)

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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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TN2018000112A1 (en) 2015-10-29 2019-10-04 Novartis Ag Antibody conjugates comprising toll-like receptor agonist
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
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
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
JP7287708B2 (ja) 2019-02-08 2023-06-06 プロジェニア インコーポレイテッド Toll-like受容体7または8アゴニストとコレステロールの結合体およびその用途
WO2020188448A1 (en) * 2019-03-15 2020-09-24 Janssen Sciences Ireland Unlimited Company Toll-like receptor agonists for use in the treatment of hepatitis b
CN113543788B (zh) * 2019-04-23 2023-12-19 正大天晴药业集团股份有限公司 一种tlr7激动剂的固体药物组合物
JP7811014B2 (ja) 2020-03-02 2026-02-04 プロジェニア インコーポレイテッド 病原菌外壁成分基盤の生病原体模倣ナノ粒子及びその製造方法
JP2023536954A (ja) 2020-08-04 2023-08-30 プロジェニア インコーポレイテッド 活性化部位が一時的に不活性化したトール様受容体7または8作用薬と機能性薬物の結合体およびその用途
US20230355750A1 (en) 2020-08-04 2023-11-09 Progeneer Inc. Kinetically acting adjuvant ensemble
CN116322751A (zh) 2020-08-04 2023-06-23 蛋白科技先锋 包含能够动力学控制的佐剂的mRNA疫苗
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

Citations (5)

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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
ES2467108T3 (es) 2008-12-09 2014-06-11 Gilead Sciences, Inc. Moduladores de receptores tipo toll
EP2800569B1 (en) * 2012-01-05 2018-07-25 Northeastern University Allosteric modulators of cb1 cannabinoid receptors
LT2906563T (lt) * 2012-10-10 2018-06-11 Janssen Sciences Ireland Uc Pirolo[3,2-d]pirimidino dariniai virusinių infekcijų ir kitų ligų gydymui
JP6484253B2 (ja) * 2014-05-01 2019-03-13 ノバルティス アーゲー Toll様受容体7アゴニストとしての化合物および組成物
HUE054672T2 (hu) 2014-08-15 2021-09-28 Chia Tai Tianqing Pharmaceutical Group Co Ltd TLR7 agonistaként alkalmazott pirrolopirimidin vegyületek
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)

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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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EA035951B1 (ru) 2020-09-04
ES2830443T3 (es) 2021-06-03
US20190040071A1 (en) 2019-02-07
UA121161C2 (uk) 2020-04-10
MX2018009501A (es) 2018-12-11
JP2019505533A (ja) 2019-02-28
TW201728589A (zh) 2017-08-16
CL2018002092A1 (es) 2018-12-07
PL3412672T3 (pl) 2021-01-25
IL260968B (en) 2022-05-01
LT3412672T (lt) 2020-11-10
NZ744884A (en) 2022-09-30
KR102393280B1 (ko) 2022-05-02
DK3412672T3 (da) 2020-10-19
CN108602831B (zh) 2020-11-03
CN108602831A (zh) 2018-09-28
EA201891768A1 (ru) 2019-01-31
EP3412672A4 (en) 2019-07-17
CA3013518A1 (en) 2017-08-10
JP6889171B2 (ja) 2021-06-18
CN108602831B9 (zh) 2020-12-04
HK1259170A1 (zh) 2019-11-29
US10947245B2 (en) 2021-03-16
US20200039988A1 (en) 2020-02-06
ZA201805186B (en) 2024-08-28
AU2017215801A1 (en) 2018-08-23
SG11201806683UA (en) 2018-09-27
PH12018501643A1 (en) 2019-06-03
AU2017215801B2 (en) 2020-09-10
MX374297B (es) 2025-03-06
PT3412672T (pt) 2020-11-11
EP3412672A1 (en) 2018-12-12
EP3412672B1 (en) 2020-07-15
US10442811B2 (en) 2019-10-15
KR20180104117A (ko) 2018-09-19
CA3013518C (en) 2022-07-19
WO2017133684A1 (zh) 2017-08-10
AR107548A1 (es) 2018-05-09
SI3412672T1 (sl) 2021-02-26
BR112018015880A2 (pt) 2018-12-26
CN107043379A (zh) 2017-08-15
HRP20201644T1 (hr) 2020-12-25
HUE051399T2 (hu) 2021-03-01

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