TWI778952B - 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 - Google Patents

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 Download PDF

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TWI778952B
TWI778952B TW106103697A TW106103697A TWI778952B TW I778952 B TWI778952 B TW I778952B TW 106103697 A TW106103697 A TW 106103697A TW 106103697 A TW106103697 A TW 106103697A TW I778952 B TWI778952 B TW I778952B
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crystal form
formula
compound
trifluoroacetate salt
compound represented
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TW106103697A
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Chinese (zh)
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TW201728591A (zh
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照中 丁
孫飛
胡迎虎
周義龍
王崢
趙銳
楊玲
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大陸商正大天晴藥業集團股份有限公司
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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)
  • Engineering & Computer Science (AREA)
  • Biotechnology (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)
TW106103697A 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 TWI778952B (zh)

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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

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TW201728591A TW201728591A (zh) 2017-08-16
TWI778952B true TWI778952B (zh) 2022-10-01

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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
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
AU2017213628B2 (en) 2016-02-05 2021-07-29 Denali Therapeutics Inc. Inhibitors of receptor-interacting protein kinase 1
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
MX2021009496A (es) 2019-02-08 2021-09-08 Progeneer Inc Complejo de colesterol-agonista del receptor 7 u 8 tipo larga distancia, y uso del mismo.
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
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
JP7690222B2 (ja) 2020-08-04 2025-06-10 プロジェニア インコーポレイテッド 動力学的制御が可能なアジュバントを含むmRNAワクチン
EP4194008A4 (en) 2020-08-04 2025-01-08 Progeneer Inc. Kinetically acting adjuvant ensemble
EP4463229A1 (en) 2022-01-12 2024-11-20 Denali Therapeutics Inc. Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,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

Citations (2)

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WO2014056953A1 (en) * 2012-10-10 2014-04-17 Janssen R&D Ireland Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
WO2015168279A1 (en) * 2014-05-01 2015-11-05 Novartis Ag Compounds and compositions as toll-like receptor 7 agonists

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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
EA026557B1 (ru) 2008-12-09 2017-04-28 Джилид Сайэнс, Инк. Промежуточные соединения для получения модуляторов толл-подобных рецепторов
CA2826295C (en) 2011-02-04 2020-10-20 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
CA2890201A1 (en) * 2012-11-20 2014-05-30 Glaxosmithkline Llc Novel compounds
KR102139847B1 (ko) * 2014-05-01 2020-07-31 노파르티스 아게 톨-유사 수용체 7 효능제로서의 화합물 및 조성물
CN110759916B (zh) * 2014-08-15 2021-02-19 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
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
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

Patent Citations (2)

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WO2014056953A1 (en) * 2012-10-10 2014-04-17 Janssen R&D Ireland Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
WO2015168279A1 (en) * 2014-05-01 2015-11-05 Novartis Ag Compounds and compositions as toll-like receptor 7 agonists

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EA201891772A1 (ru) 2019-01-31
JP6877450B2 (ja) 2021-05-26
ZA201805240B (en) 2024-09-25
PH12018501641B1 (en) 2021-03-26
WO2017133687A1 (zh) 2017-08-10
KR20180104118A (ko) 2018-09-19
AR107550A1 (es) 2018-05-09
US20190031666A1 (en) 2019-01-31
UA121276C2 (uk) 2020-04-27
CN108602833B (zh) 2020-07-28
ES2834304T3 (es) 2021-06-17
MY198137A (en) 2023-08-07
CN107043377A (zh) 2017-08-15
MX374300B (es) 2025-03-06
TW201728591A (zh) 2017-08-16
NZ745023A (en) 2022-09-30
AU2017214135B2 (en) 2020-08-13
HK1259182A1 (zh) 2019-11-29
CA3013521A1 (en) 2017-08-10
EP3412674B1 (en) 2020-09-16
CA3013521C (en) 2022-07-12
EP3412674A1 (en) 2018-12-12
IL260981B (en) 2022-05-01
EP3412674A4 (en) 2019-07-17
MX2018009503A (es) 2018-12-11
CN108602833A (zh) 2018-09-28
PH12018501641A1 (en) 2019-06-03
EA037048B1 (ru) 2021-01-29
JP2019504103A (ja) 2019-02-14
HUE052210T2 (hu) 2021-04-28
BR112018015878A2 (pt) 2018-12-26
DK3412674T3 (da) 2020-11-09
KR102393281B1 (ko) 2022-05-02
AU2017214135A1 (en) 2018-08-23
SG11201806688QA (en) 2018-09-27
CL2018002101A1 (es) 2018-12-07
US10683296B2 (en) 2020-06-16

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