DK3412672T3 - Krystalform A af 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-D]pyrimidin-4-amin som TLR7-agonist, fremstillingsfremgangsmåde og anvendelse deraf - Google Patents

Krystalform A af 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-D]pyrimidin-4-amin som TLR7-agonist, fremstillingsfremgangsmåde og anvendelse deraf Download PDF

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Publication number
DK3412672T3
DK3412672T3 DK17747004.4T DK17747004T DK3412672T3 DK 3412672 T3 DK3412672 T3 DK 3412672T3 DK 17747004 T DK17747004 T DK 17747004T DK 3412672 T3 DK3412672 T3 DK 3412672T3
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Denmark
Prior art keywords
pyrrolo
pyrrolidin
pyrimidin
ylmethyl
butoxy
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DK17747004.4T
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Danish (da)
English (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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    • 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
    • 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)
  • 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)
DK17747004.4T 2016-02-05 2017-02-04 Krystalform A af 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-D]pyrimidin-4-amin som TLR7-agonist, fremstillingsfremgangsmåde og anvendelse deraf DK3412672T3 (da)

Applications Claiming Priority (2)

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
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 (1)

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DK3412672T3 true DK3412672T3 (da) 2020-10-19

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DK17747004.4T DK3412672T3 (da) 2016-02-05 2017-02-04 Krystalform A af 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-D]pyrimidin-4-amin som TLR7-agonist, fremstillingsfremgangsmåde og anvendelse deraf

Country Status (27)

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

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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

Family Cites Families (14)

* Cited by examiner, † Cited by third party
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
DK2906563T3 (en) 2012-10-10 2018-06-06 Janssen Sciences Ireland Uc PYRROLO [3,2-D] PYRIMIDINE DERIVATIVES FOR TREATING VIRUS INFECTIONS AND OTHER DISEASES
BR112015011439A2 (pt) 2012-11-20 2017-07-11 Glaxosmithkline Llc composto, composição farmacêutica, composição de vacina, e, uso de um composto
EA028480B1 (ru) * 2012-11-20 2017-11-30 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Новые соединения
AU2013348217B2 (en) * 2012-11-20 2016-10-06 Glaxosmithkline Llc Novel compounds
PL3137470T3 (pl) 2014-05-01 2021-10-11 Novartis Ag Związki i kompozycje jako agonisty receptora toll-like 7
HRP20210927T1 (hr) * 2014-08-15 2021-09-03 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Spojevi pirolopirimidina koje se koriste kao agonist tlr7
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
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

Also Published As

Publication number Publication date
CN107043379A (zh) 2017-08-15
UA121161C2 (uk) 2020-04-10
CA3013518A1 (en) 2017-08-10
AU2017215801B2 (en) 2020-09-10
ZA201805186B (en) 2024-08-28
EP3412672B1 (en) 2020-07-15
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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