AU2017215800B2 - TLR7 agonist maleate salt, crystalline forms C, D and E thereof, preparation methods and uses of maleate salt and crystalline forms - Google Patents

TLR7 agonist maleate salt, crystalline forms C, D and E thereof, preparation methods and uses of maleate salt and crystalline forms Download PDF

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Publication number
AU2017215800B2
AU2017215800B2 AU2017215800A AU2017215800A AU2017215800B2 AU 2017215800 B2 AU2017215800 B2 AU 2017215800B2 AU 2017215800 A AU2017215800 A AU 2017215800A AU 2017215800 A AU2017215800 A AU 2017215800A AU 2017215800 B2 AU2017215800 B2 AU 2017215800B2
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Prior art keywords
crystal form
compound
formula
maleate
crystalline composition
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AU2017215800A1 (en
Inventor
Zhaozhong DING
Yinghu HU
Fei Sun
Zheng Wang
Ling Yang
Yilong ZHOU
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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)
AU2017215800A 2016-02-05 2017-02-04 TLR7 agonist maleate salt, crystalline forms C, D and E thereof, preparation methods and uses of maleate salt and crystalline forms Active AU2017215800B2 (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)

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AU2017215800A1 AU2017215800A1 (en) 2018-08-30
AU2017215800B2 true AU2017215800B2 (en) 2020-08-20

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AU2017215800A Active AU2017215800B2 (en) 2016-02-05 2017-02-04 TLR7 agonist maleate salt, crystalline forms C, D and E thereof, preparation methods and uses of maleate salt and crystalline forms

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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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
AU2019272478B2 (en) * 2018-05-25 2024-06-06 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. TLR7 agonist and pharmaceutical combination thereof for treating lung cancer
WO2020162705A1 (ko) 2019-02-08 2020-08-13 성균관대학교산학협력단 톨-유사 수용체 7 또는 8 작용자와 콜레스테롤의 결합체 및 그 용도
CA3170551A1 (en) 2020-03-02 2021-09-10 Yong Taik Lim Live-pathogen-mimetic nanoparticles based on pathogen cell wall skeleton, and production method thereof
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
JP7690221B2 (ja) 2020-08-04 2025-06-10 プロジェニア インコーポレイテッド 動力学的に作用するアジュバントアンサンブル
US20230346924A1 (en) 2020-08-04 2023-11-02 Progeneer Inc. Mrna vaccine comprising adjuvant capable of kinetic control

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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
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

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Also Published As

Publication number Publication date
HK1259175A1 (zh) 2019-11-29
CA3013682A1 (en) 2017-08-10
UA123781C2 (uk) 2021-06-02
AU2017215800A1 (en) 2018-08-30
ZA201805185B (en) 2024-08-28
NZ745231A (en) 2022-07-29
SG11201806682TA (en) 2018-09-27
EP3412671A1 (en) 2018-12-12
MX2018009500A (es) 2018-12-11
JP2019505532A (ja) 2019-02-28
CA3013682C (en) 2022-06-21
US20200368241A1 (en) 2020-11-26
ES2834303T3 (es) 2021-06-17
US10780091B2 (en) 2020-09-22
CL2018002089A1 (es) 2018-12-07
PH12018501644A1 (en) 2019-06-03
CN108602830A (zh) 2018-09-28
JP6898336B2 (ja) 2021-07-07
TWI778951B (zh) 2022-10-01
EA038794B1 (ru) 2021-10-20
DK3412671T3 (da) 2020-11-09
MY196762A (en) 2023-05-03
MX374295B (es) 2025-03-06
EA201891770A1 (ru) 2019-01-31
US20190070179A1 (en) 2019-03-07
PH12018501644B1 (en) 2022-09-07
BR112018015881A2 (pt) 2018-12-26
AR107547A1 (es) 2018-05-09
IL260965B (en) 2022-02-01
CN107043380A (zh) 2017-08-15
KR20180104116A (ko) 2018-09-19
HUE052211T2 (hu) 2021-04-28
KR102393279B1 (ko) 2022-05-02
TW201728588A (zh) 2017-08-16
WO2017133683A1 (zh) 2017-08-10
CN108602830B (zh) 2020-07-28
EP3412671A4 (en) 2019-07-24
EP3412671B1 (en) 2020-09-16

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