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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (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
CN201610082029.8 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
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

Country Status (27)

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

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EP3368092B9 (en) 2015-10-29 2020-07-29 Novartis AG Antibody conjugates comprising toll-like receptor agonist
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
TWI908718B (zh) * 2019-03-15 2025-12-21 大陸商正大天晴藥業集團股份有限公司 類鐸受體促效劑給藥方案
JP2022530444A (ja) * 2019-04-23 2022-06-29 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド Ｔｌｒ７アゴニストを含む固体医薬組成物
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
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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Publication number Priority date Publication date Assignee Title
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
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
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

Family Cites Families (8)

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Publication number Priority date Publication date Assignee Title
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
CN101304748A (zh) * 2005-08-22 2008-11-12 加利福尼亚大学董事会 Tlr激动剂
RS53347B (sr) 2008-12-09 2014-10-31 Gilead Sciences, Inc. Modulatori toll-sličnih receptora
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
EP2800569B1 (en) 2012-01-05 2018-07-25 Northeastern University Allosteric modulators of cb1 cannabinoid receptors
EA028480B1 (ru) * 2012-11-20 2017-11-30 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Новые соединения
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
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
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
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

Also Published As

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

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