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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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)
  • 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)
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

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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

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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

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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
SI2906563T1 (en) * 2012-10-10 2018-06-29 Janssen Sciences Ireland Uc Derivatives of pyrrolo (3,2-d) pyrimidine for the treatment of viral infections and other diseases
CA2890198A1 (en) * 2012-11-20 2014-05-30 Diane Mary Coe Novel compounds
RU2643371C2 (ru) * 2012-11-20 2018-02-01 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Новые соединения
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
MX362341B (es) 2014-05-01 2019-01-11 Novartis Ag Compuestos y composiciones como agonistas del receptor tipo toll 7.
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
SI3190113T1 (sl) 2014-08-15 2021-09-30 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Pirolopirimidinske spojine, ki se uporabljajo kot agonist TLR7
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
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

Also Published As

Publication number Publication date
HK1259170A1 (zh) 2019-11-29
EA035951B1 (ru) 2020-09-04
AU2017215801B2 (en) 2020-09-10
US20190040071A1 (en) 2019-02-07
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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