CA3013521C - Trifluoroacetate salt of a pyrrolo[3,2-d]pyrimidin compound as tlr7 agonist and crystalline form b thereof - Google Patents

Trifluoroacetate salt of a pyrrolo[3,2-d]pyrimidin compound as tlr7 agonist and crystalline form b thereof Download PDF

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Publication number
CA3013521C
CA3013521C CA3013521A CA3013521A CA3013521C CA 3013521 C CA3013521 C CA 3013521C CA 3013521 A CA3013521 A CA 3013521A CA 3013521 A CA3013521 A CA 3013521A CA 3013521 C CA3013521 C CA 3013521C
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Prior art keywords
compound
formula
crystal form
trifluoroacetate
virus infection
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CA3013521A
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English (en)
French (fr)
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CA3013521A1 (en
Inventor
Zhaozhong DING
Fei Sun
Yinghu HU
Yilong ZHOU
Zheng Wang
Rui Zhao
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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    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (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)
CA3013521A 2016-02-05 2017-02-04 Trifluoroacetate salt of a pyrrolo[3,2-d]pyrimidin compound as tlr7 agonist and crystalline form b thereof Active CA3013521C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610081899.3 2016-02-05
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
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

Publications (2)

Publication Number Publication Date
CA3013521A1 CA3013521A1 (en) 2017-08-10
CA3013521C true CA3013521C (en) 2022-07-12

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CA3013521A Active 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

Country Status (23)

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

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
IL287136B2 (en) 2016-02-05 2023-09-01 Denali Therapeutics Inc Receptor inhibitors - interacting with protein kinase 1
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
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
US20230346924A1 (en) 2020-08-04 2023-11-02 Progeneer Inc. Mrna vaccine comprising adjuvant capable of kinetic control
WO2022031011A1 (ko) 2020-08-04 2022-02-10 성균관대학교산학협력단 동력학적으로 작용하는 아주번트 앙상블
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
US11999750B2 (en) 2022-01-12 2024-06-04 Denali Therapeutics Inc. Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido [3,2-B][1,4]oxazepin-3-yl)-4H-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
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
WO2010077613A1 (en) 2008-12-09 2010-07-08 Gilead Sciences, Inc. Modulators of toll-like receptors
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
WO2013103967A1 (en) * 2012-01-05 2013-07-11 Northeastern University Allosteric modulators of cb1 cannabinoid receptors
NZ705589A (en) * 2012-10-10 2019-05-31 Janssen Sciences Ireland Uc Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
US9550785B2 (en) * 2012-11-20 2017-01-24 Glaxosmithkline Llc Pyrrolopyrimidines as therapeutic agents for the treatment of diseases
WO2015168269A1 (en) * 2014-05-01 2015-11-05 Novartis Ag Compounds and compositions as toll-like receptor 7 agonists
WO2015168279A1 (en) * 2014-05-01 2015-11-05 Novartis Ag Compounds and compositions as toll-like receptor 7 agonists
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
LT3190113T (lt) 2014-08-15 2021-08-25 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Pirolopirimidino junginiai, naudotini kaip tlr7 agonistai
CN105732635A (zh) 2014-12-29 2016-07-06 南京明德新药研发股份有限公司 一类Toll样受体7激动剂

Also Published As

Publication number Publication date
EP3412674A4 (en) 2019-07-17
AU2017214135B2 (en) 2020-08-13
KR102393281B1 (ko) 2022-05-02
AR107550A1 (es) 2018-05-09
JP6877450B2 (ja) 2021-05-26
JP2019504103A (ja) 2019-02-14
EP3412674A1 (en) 2018-12-12
CN108602833A (zh) 2018-09-28
HUE052210T2 (hu) 2021-04-28
SG11201806688QA (en) 2018-09-27
MX374300B (es) 2025-03-06
PH12018501641B1 (en) 2021-03-26
US20190031666A1 (en) 2019-01-31
IL260981B (en) 2022-05-01
DK3412674T3 (da) 2020-11-09
WO2017133687A1 (zh) 2017-08-10
EA037048B1 (ru) 2021-01-29
PH12018501641A1 (en) 2019-06-03
EA201891772A1 (ru) 2019-01-31
MX2018009503A (es) 2018-12-11
HK1259182A1 (zh) 2019-11-29
TW201728591A (zh) 2017-08-16
US10683296B2 (en) 2020-06-16
BR112018015878A2 (pt) 2018-12-26
NZ745023A (en) 2022-09-30
CN107043377A (zh) 2017-08-15
TWI778952B (zh) 2022-10-01
CA3013521A1 (en) 2017-08-10
CL2018002101A1 (es) 2018-12-07
MY198137A (en) 2023-08-07
ES2834304T3 (es) 2021-06-17
EP3412674B1 (en) 2020-09-16
UA121276C2 (uk) 2020-04-27
AU2017214135A1 (en) 2018-08-23
KR20180104118A (ko) 2018-09-19
CN108602833B (zh) 2020-07-28
ZA201805240B (en) 2024-09-25

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CA3013521C (en) Trifluoroacetate salt of a pyrrolo[3,2-d]pyrimidin compound as tlr7 agonist and crystalline form b thereof
CA3013518C (en) Tlr7 agonist crystalline form a, preparation method and use thereof
CA3013682C (en) Maleate salt of a pyrrolo[3,2-d]pyrimidine compound as tlr7 agonist and crystalline forms c, d and e thereof
HK1259182B (zh) 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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