CN107043377A - 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 - Google Patents

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 Download PDF

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Publication number
CN107043377A
CN107043377A CN201610081899.3A CN201610081899A CN107043377A CN 107043377 A CN107043377 A CN 107043377A CN 201610081899 A CN201610081899 A CN 201610081899A CN 107043377 A CN107043377 A CN 107043377A
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China
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formula
crystal form
compound
pharmaceutical composition
preparation
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CN201610081899.3A
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English (en)
Chinese (zh)
Inventor
丁照中
孙飞
胡迎虎
周义龙
王峥
赵锐
杨玲
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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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Application filed by Chia Tai Tianqing Pharmaceutical Group Co Ltd filed Critical Chia Tai Tianqing Pharmaceutical Group Co Ltd
Priority to CN201610081899.3A priority Critical patent/CN107043377A/zh
Priority to TW106103697A priority patent/TWI778952B/zh
Priority to PCT/CN2017/072894 priority patent/WO2017133687A1/zh
Priority to MX2018009503A priority patent/MX374300B/es
Priority to ES17747007T priority patent/ES2834304T3/es
Priority to EP17747007.7A priority patent/EP3412674B1/en
Priority to NZ745023A priority patent/NZ745023A/en
Priority to US16/075,303 priority patent/US10683296B2/en
Priority to MYPI2018702700A priority patent/MY198137A/en
Priority to AU2017214135A priority patent/AU2017214135B2/en
Priority to CA3013521A priority patent/CA3013521C/en
Priority to JP2018540797A priority patent/JP6877450B2/ja
Priority to DK17747007.7T priority patent/DK3412674T3/da
Priority to CN201780009751.1A priority patent/CN108602833B/zh
Priority to HK19101232.5A priority patent/HK1259182B/zh
Priority to HUE17747007A priority patent/HUE052210T2/hu
Priority to BR112018015878-0A priority patent/BR112018015878B1/pt
Priority to EA201891772A priority patent/EA037048B1/ru
Priority to UAA201809128A priority patent/UA121276C2/uk
Priority to SG11201806688QA priority patent/SG11201806688QA/en
Priority to KR1020187024629A priority patent/KR102393281B1/ko
Priority to ARP170100299A priority patent/AR107550A1/es
Publication of CN107043377A publication Critical patent/CN107043377A/zh
Priority to PH12018501641A priority patent/PH12018501641B1/en
Priority to CL2018002101A priority patent/CL2018002101A1/es
Priority to ZA2018/05240A priority patent/ZA201805240B/en
Priority to IL260981A priority patent/IL260981B/en
Pending legal-status Critical Current

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    • 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
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P31/14Antivirals for RNA viruses
    • 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
    • A61P31/20Antivirals for DNA viruses
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (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)
CN201610081899.3A 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 Pending CN107043377A (zh)

Priority Applications (26)

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
TW106103697A TWI778952B (zh) 2016-02-05 2017-02-03 Tlr7促效劑的三氟乙酸鹽、其晶型b、其製備方法、包含其的藥物組合物及其用途
CN201780009751.1A CN108602833B (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
HUE17747007A HUE052210T2 (hu) 2016-02-05 2017-02-04 Egy TLR7 agonista trifluoracetát sója és annak B kristályos formája, elõállítási eljárások és alkalmazások
ES17747007T ES2834304T3 (es) 2016-02-05 2017-02-04 Sal de trifluoroacetato de un agonista de TLR7 y forma cristalina B de la misma, métodos de preparación y usos
EP17747007.7A EP3412674B1 (en) 2016-02-05 2017-02-04 Trifluoroacetate salt of a tlr7 agonist and crystalline form b thereof, preparation methods and uses
NZ745023A NZ745023A (en) 2016-02-05 2017-02-04 Tlr7 agonist trifluoroacetate salt and crystalline form b thereof, preparation methods and uses
US16/075,303 US10683296B2 (en) 2016-02-05 2017-02-04 TLR7 agonist trifluoroacetate salt and crystalline form B thereof, preparation methods and uses
MYPI2018702700A MY198137A (en) 2016-02-05 2017-02-04 Tlr7 Agonist Trifluoroacetate Salt and Crystalline form B Thereof, Preparation Methods And Uses
AU2017214135A AU2017214135B2 (en) 2016-02-05 2017-02-04 TLR7 agonist trifluoroacetate salt and crystalline form B thereof, preparation methods and uses
CA3013521A CA3013521C (en) 2016-02-05 2017-02-04 Trifluoroacetate salt of a pyrrolo[3,2-d]pyrimidin compound as tlr7 agonist and crystalline form b thereof
JP2018540797A JP6877450B2 (ja) 2016-02-05 2017-02-04 Tlr7アゴニストのトリフルオロ酢酸塩及びその結晶形b、調製方法、並びに使用
DK17747007.7T DK3412674T3 (da) 2016-02-05 2017-02-04 Trifluoracetatsalt af en TLR7-agonist og krystalform B deraf, fremstillingsfremgangsmåder og anvendelser
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
HK19101232.5A HK1259182B (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
MX2018009503A MX374300B (es) 2016-02-05 2017-02-04 Sal de trifluoroacetato de agonista de tlr7 y forma cristalina b de la misma, métodos de preparación y usos.
BR112018015878-0A BR112018015878B1 (pt) 2016-02-05 2017-02-04 Forma cristalina b de sal de trifluoracetato agonista de tlr7, seu processo de preparação, composições cristalina e farmacêutica, e seus usos
EA201891772A EA037048B1 (ru) 2016-02-05 2017-02-04 Трифторацетатная соль агониста tlr7 и ее кристаллическая форма b, способы получения и использование
UAA201809128A UA121276C2 (uk) 2016-02-05 2017-02-04 Трифторацетатна сіль агоніста tlr7 і її кристалічна форма b, способи одержання і використання
SG11201806688QA SG11201806688QA (en) 2016-02-05 2017-02-04 Tlr7 agonist trifluoroacetate salt and crystalline form b thereof, preparation methods and uses
KR1020187024629A KR102393281B1 (ko) 2016-02-05 2017-02-04 Tlr7 작용제 트리플루오로아세테이트 염 및 이의 결정형 b, 제조방법 및 용도
ARP170100299A AR107550A1 (es) 2016-02-05 2017-02-06 Un trifluoroacetato de agonista de tlr7, la forma cristalina b, proceso de preparación y su utilización
PH12018501641A PH12018501641B1 (en) 2016-02-05 2018-08-02 Tlr7 agonist trifluoroacetate salt and crystalline form b thereof, preparation methods and uses
CL2018002101A CL2018002101A1 (es) 2016-02-05 2018-08-03 Un trifluoroacetato de agonista de tlr7, la forma cristalina b, proceso de preparación y su utilización
ZA2018/05240A ZA201805240B (en) 2016-02-05 2018-08-03 Tlr7 agonist trifluoroacetate salt and crystalline form b thereof, preparation methods and uses
IL260981A IL260981B (en) 2016-02-05 2018-08-05 The trifluoroacetate salt of the tlr7 agonist type b crystal structure, preparation, and methods of use

Applications Claiming Priority (1)

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

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CN201610081899.3A Pending 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
CN201780009751.1A Active CN108602833B (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

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Country Status (23)

Country Link
US (1) US10683296B2 (https=)
EP (1) EP3412674B1 (https=)
JP (1) JP6877450B2 (https=)
KR (1) KR102393281B1 (https=)
CN (2) CN107043377A (https=)
AR (1) AR107550A1 (https=)
AU (1) AU2017214135B2 (https=)
CA (1) CA3013521C (https=)
CL (1) CL2018002101A1 (https=)
DK (1) DK3412674T3 (https=)
EA (1) EA037048B1 (https=)
ES (1) ES2834304T3 (https=)
HU (1) HUE052210T2 (https=)
IL (1) IL260981B (https=)
MX (1) MX374300B (https=)
MY (1) MY198137A (https=)
NZ (1) NZ745023A (https=)
PH (1) PH12018501641B1 (https=)
SG (1) SG11201806688QA (https=)
TW (1) TWI778952B (https=)
UA (1) UA121276C2 (https=)
WO (1) WO2017133687A1 (https=)
ZA (1) ZA201805240B (https=)

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WO2019223788A1 (zh) * 2018-05-25 2019-11-28 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

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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
MA44007A (fr) 2016-02-05 2018-12-19 Denali Therapeutics Inc Inhibiteurs du récepteur interagissant avec protéine kinase 1
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
IL314082A (en) 2022-01-12 2024-09-01 Denali Therapeutics Inc Crystal forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido[3,2-b][1,4]oxazapin-3-yl)- H4- 1,2,4-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

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Publication number Priority date Publication date Assignee Title
WO2019223788A1 (zh) * 2018-05-25 2019-11-28 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
CN112105620A (zh) * 2018-05-25 2020-12-18 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
US12128047B2 (en) 2018-05-25 2024-10-29 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. TLR7 agonist and pharmaceutical combination thereof for treating lung cancer
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

Also Published As

Publication number Publication date
US20190031666A1 (en) 2019-01-31
MX374300B (es) 2025-03-06
MX2018009503A (es) 2018-12-11
EA201891772A1 (ru) 2019-01-31
EA037048B1 (ru) 2021-01-29
WO2017133687A1 (zh) 2017-08-10
JP2019504103A (ja) 2019-02-14
PH12018501641A1 (en) 2019-06-03
SG11201806688QA (en) 2018-09-27
CN108602833B (zh) 2020-07-28
NZ745023A (en) 2022-09-30
CL2018002101A1 (es) 2018-12-07
AR107550A1 (es) 2018-05-09
TW201728591A (zh) 2017-08-16
IL260981B (en) 2022-05-01
CA3013521C (en) 2022-07-12
EP3412674B1 (en) 2020-09-16
HUE052210T2 (hu) 2021-04-28
US10683296B2 (en) 2020-06-16
ES2834304T3 (es) 2021-06-17
EP3412674A1 (en) 2018-12-12
DK3412674T3 (da) 2020-11-09
TWI778952B (zh) 2022-10-01
KR20180104118A (ko) 2018-09-19
AU2017214135B2 (en) 2020-08-13
KR102393281B1 (ko) 2022-05-02
MY198137A (en) 2023-08-07
JP6877450B2 (ja) 2021-05-26
PH12018501641B1 (en) 2021-03-26
UA121276C2 (uk) 2020-04-27
BR112018015878A2 (pt) 2018-12-26
CA3013521A1 (en) 2017-08-10
EP3412674A4 (en) 2019-07-17
HK1259182A1 (zh) 2019-11-29
ZA201805240B (en) 2024-09-25
AU2017214135A1 (en) 2018-08-23
CN108602833A (zh) 2018-09-28

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Application publication date: 20170815