AU2017215801B2 - TLR7 agonist crystalline form a, preparation method and use thereof - Google Patents

TLR7 agonist crystalline form a, preparation method and use thereof Download PDF

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Publication number
AU2017215801B2
AU2017215801B2 AU2017215801A AU2017215801A AU2017215801B2 AU 2017215801 B2 AU2017215801 B2 AU 2017215801B2 AU 2017215801 A AU2017215801 A AU 2017215801A AU 2017215801 A AU2017215801 A AU 2017215801A AU 2017215801 B2 AU2017215801 B2 AU 2017215801B2
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Australia
Prior art keywords
compound
crystal form
formula
receptor
toll
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AU2017215801A
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AU2017215801A1 (en
Inventor
Zhaozhong DING
Yinghu HU
Fei Sun
Zheng Wang
Ling Yang
Rui Zhao
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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    • 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)
AU2017215801A 2016-02-05 2017-02-04 TLR7 agonist crystalline form a, preparation method and use thereof Active AU2017215801B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
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
CN201610082029.8 2016-02-05
PCT/CN2017/072891 WO2017133684A1 (zh) 2016-02-05 2017-02-04 一种tlr7激动剂的晶型a、其制备方法和用途

Publications (2)

Publication Number Publication Date
AU2017215801A1 AU2017215801A1 (en) 2018-08-23
AU2017215801B2 true AU2017215801B2 (en) 2020-09-10

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AU2017215801A Active AU2017215801B2 (en) 2016-02-05 2017-02-04 TLR7 agonist crystalline form a, preparation method and use thereof

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US (2) US10442811B2 (enExample)
EP (1) EP3412672B1 (enExample)
JP (1) JP6889171B2 (enExample)
KR (1) KR102393280B1 (enExample)
CN (2) CN107043379A (enExample)
AR (1) AR107548A1 (enExample)
AU (1) AU2017215801B2 (enExample)
CA (1) CA3013518C (enExample)
CL (1) CL2018002092A1 (enExample)
DK (1) DK3412672T3 (enExample)
EA (1) EA035951B1 (enExample)
ES (1) ES2830443T3 (enExample)
HR (1) HRP20201644T1 (enExample)
HU (1) HUE051399T2 (enExample)
IL (1) IL260968B (enExample)
LT (1) LT3412672T (enExample)
MX (1) MX374297B (enExample)
NZ (1) NZ744884A (enExample)
PH (1) PH12018501643A1 (enExample)
PL (1) PL3412672T3 (enExample)
PT (1) PT3412672T (enExample)
SG (1) SG11201806683UA (enExample)
SI (1) SI3412672T1 (enExample)
TW (1) TWI754629B (enExample)
UA (1) UA121161C2 (enExample)
WO (1) WO2017133684A1 (enExample)
ZA (1) ZA201805186B (enExample)

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MA44334A (fr) 2015-10-29 2018-09-05 Novartis Ag Conjugués d'anticorps comprenant un agoniste du récepteur de type toll
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
EP3816166A4 (en) * 2018-05-25 2022-04-06 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Tlr7 agonist and pharmaceutical combination thereof for treating lung cancer
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
US12263172B2 (en) 2019-03-15 2025-04-01 Chia Tai Tianqing Pharmeceutical Group Co., Ltd. Toll-like receptor agonists for use in the treatment of hepatitis b
AU2020263448B2 (en) * 2019-04-23 2025-02-20 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Solid pharmaceutical composition comprising TLR7 agonist
JP2023516372A (ja) 2020-03-02 2023-04-19 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
US20230355750A1 (en) 2020-08-04 2023-11-09 Progeneer Inc. Kinetically acting adjuvant ensemble
WO2022031057A1 (ko) 2020-08-04 2022-02-10 성균관대학교산학협력단 활성화 부위가 일시적으로 비활성화된 톨-유사 수용체 7 또는 8 작용자와 기능성 약물의 결합체 및 그 용도
EP4194006A4 (en) 2020-08-04 2024-12-04 Progeneer Inc. mRNA VACCINE WITH AN ADJUVANT CAPABLE OF KINETIC CONTROL
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 (6)

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CN104780924A (zh) * 2012-11-20 2015-07-15 葛兰素史克有限责任公司 新颖的化合物
CN104780923A (zh) * 2012-11-20 2015-07-15 葛兰素史克有限责任公司 新颖的化合物
CN104837840A (zh) * 2012-10-10 2015-08-12 爱尔兰詹森科学公司 用于治疗病毒感染及其他疾病的吡咯并[3,2-d]嘧啶衍生物
WO2015168269A1 (en) * 2014-05-01 2015-11-05 Novartis Ag Compounds and compositions as toll-like receptor 7 agonists
WO2016023511A1 (zh) * 2014-08-15 2016-02-18 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
CA3013518A1 (en) * 2016-02-05 2017-08-10 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Tlr7 agonist crystalline form a, preparation method and use thereof

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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
ES2577514T3 (es) * 2005-08-22 2016-07-15 The Regents Of The University Of California Antagonistas de TLR
TW201639852A (zh) 2008-12-09 2016-11-16 吉李德科學股份有限公司 用於製備可用作類鐸受體調節劑之化合物的中間體化合物
US9139590B2 (en) * 2011-02-04 2015-09-22 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
NZ707319A (en) * 2012-11-20 2019-09-27 Glaxosmithkline Llc 5h-pyrrolo[3,2-d]pyrimidin-4-amine compounds and their use in the treatment of allergic diseases and other inflammatory conditions
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

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104837840A (zh) * 2012-10-10 2015-08-12 爱尔兰詹森科学公司 用于治疗病毒感染及其他疾病的吡咯并[3,2-d]嘧啶衍生物
CN104780924A (zh) * 2012-11-20 2015-07-15 葛兰素史克有限责任公司 新颖的化合物
CN104780923A (zh) * 2012-11-20 2015-07-15 葛兰素史克有限责任公司 新颖的化合物
WO2015168269A1 (en) * 2014-05-01 2015-11-05 Novartis Ag Compounds and compositions as toll-like receptor 7 agonists
WO2016023511A1 (zh) * 2014-08-15 2016-02-18 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
EP3190113A1 (en) * 2014-08-15 2017-07-12 Chai Tai Tianqing Pharmaceutical Group Co., Ltd. Pyrrolopyrimidine compounds used as tlr7 agonist
CA3013518A1 (en) * 2016-02-05 2017-08-10 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Tlr7 agonist crystalline form a, preparation method and use thereof

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Publication number Publication date
HK1259170A1 (zh) 2019-11-29
EA035951B1 (ru) 2020-09-04
US20190040071A1 (en) 2019-02-07
DK3412672T3 (da) 2020-10-19
EA201891768A1 (ru) 2019-01-31
SI3412672T1 (sl) 2021-02-26
KR102393280B1 (ko) 2022-05-02
ZA201805186B (en) 2024-08-28
JP6889171B2 (ja) 2021-06-18
CN108602831B9 (zh) 2020-12-04
CN108602831B (zh) 2020-11-03
MX374297B (es) 2025-03-06
UA121161C2 (uk) 2020-04-10
AR107548A1 (es) 2018-05-09
KR20180104117A (ko) 2018-09-19
TWI754629B (zh) 2022-02-11
TW201728589A (zh) 2017-08-16
ES2830443T3 (es) 2021-06-03
WO2017133684A1 (zh) 2017-08-10
MX2018009501A (es) 2018-12-11
EP3412672A4 (en) 2019-07-17
LT3412672T (lt) 2020-11-10
CN107043379A (zh) 2017-08-15
JP2019505533A (ja) 2019-02-28
CA3013518C (en) 2022-07-19
HUE051399T2 (hu) 2021-03-01
CN108602831A (zh) 2018-09-28
AU2017215801A1 (en) 2018-08-23
US10947245B2 (en) 2021-03-16
PL3412672T3 (pl) 2021-01-25
EP3412672A1 (en) 2018-12-12
US20200039988A1 (en) 2020-02-06
PT3412672T (pt) 2020-11-11
IL260968B (en) 2022-05-01
EP3412672B1 (en) 2020-07-15
SG11201806683UA (en) 2018-09-27
NZ744884A (en) 2022-09-30
CA3013518A1 (en) 2017-08-10
PH12018501643A1 (en) 2019-06-03
HRP20201644T1 (hr) 2020-12-25
US10442811B2 (en) 2019-10-15
BR112018015880A2 (pt) 2018-12-26
CL2018002092A1 (es) 2018-12-07

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