CN107043379A - 一种tlr7激动剂的晶型a、其制备方法和医药用途 - Google Patents

一种tlr7激动剂的晶型a、其制备方法和医药用途 Download PDF

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Publication number
CN107043379A
CN107043379A CN201610082029.8A CN201610082029A CN107043379A CN 107043379 A CN107043379 A CN 107043379A CN 201610082029 A CN201610082029 A CN 201610082029A CN 107043379 A CN107043379 A CN 107043379A
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China
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formula
crystal form
preparation
compound
crystalline
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CN201610082029.8A
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English (en)
Chinese (zh)
Inventor
丁照中
孙飞
胡迎虎
周义龙
王峥
赵锐
杨玲
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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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Application filed by Chia Tai Tianqing Pharmaceutical Group Co Ltd filed Critical Chia Tai Tianqing Pharmaceutical Group Co Ltd
Priority to CN201610082029.8A priority Critical patent/CN107043379A/zh
Priority to TW106103695A priority patent/TWI754629B/zh
Priority to DK17747004.4T priority patent/DK3412672T3/da
Priority to EA201891768A priority patent/EA035951B1/ru
Priority to AU2017215801A priority patent/AU2017215801B2/en
Priority to CN201780009747.5A priority patent/CN108602831B9/zh
Priority to US16/075,297 priority patent/US10442811B2/en
Priority to HK19101219.2A priority patent/HK1259170B/zh
Priority to EP17747004.4A priority patent/EP3412672B1/en
Priority to PL17747004T priority patent/PL3412672T3/pl
Priority to LTEP17747004.4T priority patent/LT3412672T/lt
Priority to PCT/CN2017/072891 priority patent/WO2017133684A1/zh
Priority to SG11201806683UA priority patent/SG11201806683UA/en
Priority to HUE17747004A priority patent/HUE051399T2/hu
Priority to ES17747004T priority patent/ES2830443T3/es
Priority to UAA201809129A priority patent/UA121161C2/uk
Priority to KR1020187024627A priority patent/KR102393280B1/ko
Priority to CA3013518A priority patent/CA3013518C/en
Priority to PT177470044T priority patent/PT3412672T/pt
Priority to SI201730461T priority patent/SI3412672T1/sl
Priority to HRP20201644TT priority patent/HRP20201644T1/hr
Priority to NZ744884A priority patent/NZ744884A/en
Priority to MX2018009501A priority patent/MX374297B/es
Priority to BR112018015880-1A priority patent/BR112018015880B1/pt
Priority to JP2018540799A priority patent/JP6889171B2/ja
Priority to ARP170100297A priority patent/AR107548A1/es
Publication of CN107043379A publication Critical patent/CN107043379A/zh
Priority to ZA2018/05186A priority patent/ZA201805186B/en
Priority to IL260968A priority patent/IL260968B/en
Priority to PH12018501643A priority patent/PH12018501643A1/en
Priority to CL2018002092A priority patent/CL2018002092A1/es
Priority to US16/582,575 priority patent/US10947245B2/en
Pending legal-status Critical Current

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    • 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
    • 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
    • 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)
CN201610082029.8A 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 Pending CN107043379A (zh)

Priority Applications (31)

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
TW106103695A TWI754629B (zh) 2016-02-05 2017-02-03 Ｔｌｒ７促效劑的晶型ａ、其製備方法、藥物組合物和用途
UAA201809129A UA121161C2 (uk) 2016-02-05 2017-02-04 Кристалічна форма a агоніста tlr7, її спосіб одержання і використання
KR1020187024627A KR102393280B1 (ko) 2016-02-05 2017-02-04 Tlr7 작용제 결정형 a, 이의 제조 방법 및 용도
AU2017215801A AU2017215801B2 (en) 2016-02-05 2017-02-04 TLR7 agonist crystalline form a, preparation method and use thereof
CN201780009747.5A CN108602831B9 (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
US16/075,297 US10442811B2 (en) 2016-02-05 2017-02-04 Crystal form A of 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-D] pyrimidin-4-amine, preparation process and use thereof
HK19101219.2A HK1259170B (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
EP17747004.4A EP3412672B1 (en) 2016-02-05 2017-02-04 Crystal form a of 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl) benzyl)-5h-pyrrolo[3,2-d]pyrimidin-4-amine as tlr7 agonist, preparation method and use thereof
PL17747004T PL3412672T3 (pl) 2016-02-05 2017-02-04 Postać krystaliczna A 2-butoksy-7-(4-(pirolidyn-1-ylometylo)benzylo)-5H-pirolo[3,2- d]pirymidyno-4-aminy jako agonisty TLR7, sposób wytwarzania i jej zastosowanie
LTEP17747004.4T LT3412672T (lt) 2016-02-05 2017-02-04 2-butoksi-7-(4-(pirolidin-1-ilmetil) benzil)-5h-pirolo[3,2-d]pirimidin-4-amino, kaip tlr7 agonisto, kristalinė forma, jos gamybos būdas ir panaudojimas
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
SG11201806683UA SG11201806683UA (en) 2016-02-05 2017-02-04 Tlr7 agonist crystalline form a, preparation method and use thereof
HUE17747004A HUE051399T2 (hu) 2016-02-05 2017-02-04 2-butoxi-7-(4-(pirrolidin-1-ilmetil)benzil)-5H-pirrolo[3,2-D]pirimidin-4-amin a kristályformája mint TLR7 agonista, elõállítási eljárása és alkalmazása
ES17747004T ES2830443T3 (es) 2016-02-05 2017-02-04 Forma cristalina A de (2-butoxi-7-(4-(pirrolidin-1-ilmetil)bencil)-5H-pirrolo[3,2-d]pirimidin-4-amina) como agonista de TLR7, método de preparación y uso de la misma
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
CA3013518A CA3013518C (en) 2016-02-05 2017-02-04 Tlr7 agonist crystalline form a, preparation method and use thereof
HRP20201644TT HRP20201644T1 (hr) 2016-02-05 2017-02-04 Kristalni oblik 2-butoksi-7-(4-(pirolidin-1-ilmetil)benzil)-5h-pirolo [3,2-d]pirimidin-4-amina kao agonist tlr7, postupak njegove proizvodnje i njegova uporaba
EA201891768A EA035951B1 (ru) 2016-02-05 2017-02-04 Кристаллическая форма a агониста tlr7, ее способ получения и использование
SI201730461T SI3412672T1 (sl) 2016-02-05 2017-02-04 Kristalna oblika A 2-butoksi-7-(4-(pirolidin-1-ilmetil)benzil)-5H-pirolo(3,2-d)pirimidin -4-amina kot TLR7 agonist, postopek priprave in njena uporaba
PT177470044T PT3412672T (pt) 2016-02-05 2017-02-04 Forma cristalina a de 2-butoxi-7-(4-(pirrolidin-1-ilmetil) benzil)-5h-pirrolo[3,2-d]pirimidin-4-amina como agonista de tlr7, método de preparação e utilização do mesmo
NZ744884A NZ744884A (en) 2016-02-05 2017-02-04 Tlr7 agonist crystalline form a, preparation method and use thereof
MX2018009501A MX374297B (es) 2016-02-05 2017-02-04 Forma cristalina a de agonista de tlr7, metodo de preparacion y uso de la misma
BR112018015880-1A BR112018015880B1 (pt) 2016-02-05 2017-02-04 Forma cristalina a de agonista de tlr7, seu uso e seu processo de preparação, composição cristalina, e composição farmacêutica
JP2018540799A JP6889171B2 (ja) 2016-02-05 2017-02-04 Ｔｌｒ７アゴニスト結晶形ａ、その調製方法及び使用
ARP170100297A AR107548A1 (es) 2016-02-05 2017-02-06 Forma cristalina a de agonista de tlr7, su proceso de preparación y uso
ZA2018/05186A ZA201805186B (en) 2016-02-05 2018-08-01 Tlr7 agonist crystalline form a, preparation method and use thereof
IL260968A IL260968B (en) 2016-02-05 2018-08-02 Type a crystal structure of trl7 agonist, methods of preparation and its uses
PH12018501643A PH12018501643A1 (en) 2016-02-05 2018-08-02 Tlr7 agonist crystalline form a, preparation method and use thereof
CL2018002092A CL2018002092A1 (es) 2016-02-05 2018-08-03 Forma cristalina a de agonista de tlr7, su proceso de preparación y uso
US16/582,575 US10947245B2 (en) 2016-02-05 2019-09-25 Crystal form A of 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine for inhibiting toll-like receptor activity

Applications Claiming Priority (1)

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

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CN201610082029.8A Pending 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
CN201780009747.5A Active CN108602831B9 (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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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)

Cited By (2)

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Publication number Priority date Publication date Assignee Title
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
CN113747899A (zh) * 2019-03-15 2021-12-03 正大天晴药业集团股份有限公司 用于治疗乙型肝炎的Toll样受体激动剂

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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
WO2020162705A1 (ko) 2019-02-08 2020-08-13 성균관대학교산학협력단 톨-유사 수용체 7 또는 8 작용자와 콜레스테롤의 결합체 및 그 용도
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
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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

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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
CN112105620A (zh) * 2018-05-25 2020-12-18 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
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
CN112105620B (zh) * 2018-05-25 2026-02-24 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
CN113747899A (zh) * 2019-03-15 2021-12-03 正大天晴药业集团股份有限公司 用于治疗乙型肝炎的Toll样受体激动剂
CN113747899B (zh) * 2019-03-15 2023-11-21 正大天晴药业集团股份有限公司 用于治疗乙型肝炎的Toll样受体激动剂

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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
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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