CA3013682C - Maleate salt of a pyrrolo[3,2-d]pyrimidine compound as tlr7 agonist and crystalline forms c, d and e thereof - Google Patents

Maleate salt of a pyrrolo[3,2-d]pyrimidine compound as tlr7 agonist and crystalline forms c, d and e thereof Download PDF

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Publication number
CA3013682C
CA3013682C CA3013682A CA3013682A CA3013682C CA 3013682 C CA3013682 C CA 3013682C CA 3013682 A CA3013682 A CA 3013682A CA 3013682 A CA3013682 A CA 3013682A CA 3013682 C CA3013682 C CA 3013682C
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Prior art keywords
crystal form
compound
formula
maleate
virus infection
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CA3013682A
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English (en)
French (fr)
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CA3013682A1 (en
Inventor
Zhaozhong DING
Fei Sun
Yinghu HU
Yilong ZHOU
Zheng Wang
Ling Yang
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/01Hydrocarbons
    • A61K31/015Hydrocarbons carbocyclic
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA3013682A 2016-02-05 2017-02-04 Maleate salt of a pyrrolo[3,2-d]pyrimidine compound as tlr7 agonist and crystalline forms c, d and e thereof Active CA3013682C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610082030.0 2016-02-05
CN201610082030.0A CN107043380A (zh) 2016-02-05 2016-02-05 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
PCT/CN2017/072890 WO2017133683A1 (zh) 2016-02-05 2017-02-04 一种tlr7激动剂的马来酸盐、其晶型c、晶型d、晶型e及其制备方法和用途

Publications (2)

Publication Number Publication Date
CA3013682A1 CA3013682A1 (en) 2017-08-10
CA3013682C true CA3013682C (en) 2022-06-21

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CA3013682A Active CA3013682C (en) 2016-02-05 2017-02-04 Maleate salt of a pyrrolo[3,2-d]pyrimidine compound as tlr7 agonist and crystalline forms c, d and e thereof

Country Status (23)

Country Link
US (2) US10780091B2 (https=)
EP (1) EP3412671B1 (https=)
JP (1) JP6898336B2 (https=)
KR (1) KR102393279B1 (https=)
CN (2) CN107043380A (https=)
AR (1) AR107547A1 (https=)
AU (1) AU2017215800B2 (https=)
CA (1) CA3013682C (https=)
CL (1) CL2018002089A1 (https=)
DK (1) DK3412671T3 (https=)
EA (1) EA038794B1 (https=)
ES (1) ES2834303T3 (https=)
HU (1) HUE052211T2 (https=)
IL (1) IL260965B (https=)
MX (1) MX374295B (https=)
MY (1) MY196762A (https=)
NZ (1) NZ745231A (https=)
PH (1) PH12018501644B1 (https=)
SG (1) SG11201806682TA (https=)
TW (1) TWI778951B (https=)
UA (1) UA123781C2 (https=)
WO (1) WO2017133683A1 (https=)
ZA (1) ZA201805185B (https=)

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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
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
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
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

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ATE283855T1 (de) 1996-07-03 2004-12-15 Sumitomo Pharma Neue purinderivate
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ES2577514T3 (es) 2005-08-22 2016-07-15 The Regents Of The University Of California Antagonistas de TLR
CA2691444C (en) 2007-06-29 2016-06-14 Gilead Sciences, Inc. Purine derivatives and their use as modulators of toll-like receptor 7
CA2707030A1 (en) 2007-08-03 2009-02-12 Pfizer Limited Imidazopyridinones
ES2467108T3 (es) 2008-12-09 2014-06-11 Gilead Sciences, Inc. Moduladores de receptores tipo toll
EP2670244B1 (en) 2011-02-04 2018-04-11 Duquesne University of The Holy Spirit Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity and methods of treating a patient
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
US9550785B2 (en) 2012-11-20 2017-01-24 Glaxosmithkline Llc Pyrrolopyrimidines as therapeutic agents for the treatment of diseases
KR20150085081A (ko) 2012-11-20 2015-07-22 글락소스미스클라인 엘엘씨 신규 화합물
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KR20160124157A (ko) 2014-02-20 2016-10-26 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 인간 인터페론의 유도인자로서의 피롤로[3,2]피리미딘 유도체
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
EA032487B1 (ru) 2014-05-01 2019-06-28 Новартис Аг Соединения и композиции в качестве агонистов toll-подобного рецептора 7
HUE054672T2 (hu) 2014-08-15 2021-09-28 Chia Tai Tianqing Pharmaceutical Group Co Ltd TLR7 agonistaként alkalmazott pirrolopirimidin vegyületek
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TWI714661B (zh) 2015-11-05 2021-01-01 法商賽諾菲公司 新穎念珠藻素化合物及接合物、其製備與其治療用途
CA3004173C (en) 2015-11-05 2020-07-14 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. 7-(thiazol-5-yl)pyrrolopyrimidine compound as tlr7 agonist
CR20180310A (es) 2015-11-05 2018-11-30 Basf Se Oxadiazoles sustituidos para combatir hongod fitopatógenos
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
CN107043377A (zh) * 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 一种tlr7激动剂的三氟乙酸盐、晶型b及其制备方法、药物组合物和用途
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
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

Also Published As

Publication number Publication date
HK1259175A1 (zh) 2019-11-29
US20200368241A1 (en) 2020-11-26
IL260965B (en) 2022-02-01
SG11201806682TA (en) 2018-09-27
CN107043380A (zh) 2017-08-15
JP2019505532A (ja) 2019-02-28
AR107547A1 (es) 2018-05-09
EA038794B1 (ru) 2021-10-20
NZ745231A (en) 2022-07-29
US20190070179A1 (en) 2019-03-07
PH12018501644B1 (en) 2022-09-07
PH12018501644A1 (en) 2019-06-03
EP3412671A4 (en) 2019-07-24
DK3412671T3 (da) 2020-11-09
MX2018009500A (es) 2018-12-11
ZA201805185B (en) 2024-08-28
BR112018015881A2 (pt) 2018-12-26
UA123781C2 (uk) 2021-06-02
KR20180104116A (ko) 2018-09-19
AU2017215800B2 (en) 2020-08-20
CN108602830B (zh) 2020-07-28
JP6898336B2 (ja) 2021-07-07
US10780091B2 (en) 2020-09-22
HUE052211T2 (hu) 2021-04-28
EP3412671B1 (en) 2020-09-16
WO2017133683A1 (zh) 2017-08-10
CL2018002089A1 (es) 2018-12-07
MY196762A (en) 2023-05-03
ES2834303T3 (es) 2021-06-17
KR102393279B1 (ko) 2022-05-02
CA3013682A1 (en) 2017-08-10
AU2017215800A1 (en) 2018-08-30
EP3412671A1 (en) 2018-12-12
CN108602830A (zh) 2018-09-28
TWI778951B (zh) 2022-10-01
TW201728588A (zh) 2017-08-16
MX374295B (es) 2025-03-06
EA201891770A1 (ru) 2019-01-31

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