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 PL17747004T priority patent/PL3412672T3/pl
Priority to BR112018015880-1A priority patent/BR112018015880B1/pt
Priority to KR1020187024627A priority patent/KR102393280B1/ko
Priority to JP2018540799A priority patent/JP6889171B2/ja
Priority to AU2017215801A priority patent/AU2017215801B2/en
Priority to MX2018009501A priority patent/MX374297B/es
Priority to US16/075,297 priority patent/US10442811B2/en
Priority to EP17747004.4A priority patent/EP3412672B1/en
Priority to HRP20201644TT priority patent/HRP20201644T1/hr
Priority to NZ744884A priority patent/NZ744884A/en
Priority to PCT/CN2017/072891 priority patent/WO2017133684A1/zh
Priority to PT177470044T priority patent/PT3412672T/pt
Priority to HUE17747004A priority patent/HUE051399T2/hu
Priority to DK17747004.4T priority patent/DK3412672T3/da
Priority to SI201730461T priority patent/SI3412672T1/sl
Priority to EA201891768A priority patent/EA035951B1/ru
Priority to ES17747004T priority patent/ES2830443T3/es
Priority to HK19101219.2A priority patent/HK1259170B/zh
Priority to CN201780009747.5A priority patent/CN108602831B9/zh
Priority to CA3013518A priority patent/CA3013518C/en
Priority to SG11201806683UA priority patent/SG11201806683UA/en
Priority to UAA201809129A priority patent/UA121161C2/uk
Priority to LTEP17747004.4T priority patent/LT3412672T/lt
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 PH12018501643A priority patent/PH12018501643A1/en
Priority to IL260968A priority patent/IL260968B/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)
  • 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)
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
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
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
KR1020187024627A KR102393280B1 (ko) 2016-02-05 2017-02-04 Tlr7 작용제 결정형 a, 이의 제조 방법 및 용도
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
AU2017215801A AU2017215801B2 (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
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
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
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
NZ744884A NZ744884A (en) 2016-02-05 2017-02-04 Tlr7 agonist crystalline form a, preparation method and use thereof
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
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
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
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
EA201891768A EA035951B1 (ru) 2016-02-05 2017-02-04 Кристаллическая форма a агониста tlr7, ее способ получения и использование
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
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
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
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
CA3013518A CA3013518C (en) 2016-02-05 2017-02-04 Tlr7 agonist crystalline form a, preparation method and use thereof
SG11201806683UA SG11201806683UA (en) 2016-02-05 2017-02-04 Tlr7 agonist crystalline form a, preparation method and use thereof
UAA201809129A UA121161C2 (uk) 2016-02-05 2017-02-04 Кристалічна форма a агоніста tlr7, її спосіб одержання і використання
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
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
PH12018501643A PH12018501643A1 (en) 2016-02-05 2018-08-02 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
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

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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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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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JP (1) JP6889171B2 (https=)
KR (1) KR102393280B1 (https=)
CN (2) CN107043379A (https=)
AR (1) AR107548A1 (https=)
AU (1) AU2017215801B2 (https=)
CA (1) CA3013518C (https=)
CL (1) CL2018002092A1 (https=)
DK (1) DK3412672T3 (https=)
EA (1) EA035951B1 (https=)
ES (1) ES2830443T3 (https=)
HR (1) HRP20201644T1 (https=)
HU (1) HUE051399T2 (https=)
IL (1) IL260968B (https=)
LT (1) LT3412672T (https=)
MX (1) MX374297B (https=)
NZ (1) NZ744884A (https=)
PH (1) PH12018501643A1 (https=)
PL (1) PL3412672T3 (https=)
PT (1) PT3412672T (https=)
SG (1) SG11201806683UA (https=)
SI (1) SI3412672T1 (https=)
TW (1) TWI754629B (https=)
UA (1) UA121161C2 (https=)
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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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TN2018000112A1 (en) 2015-10-29 2019-10-04 Novartis Ag Antibody conjugates comprising toll-like receptor agonist
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
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
CN113543788B (zh) * 2019-04-23 2023-12-19 正大天晴药业集团股份有限公司 一种tlr7激动剂的固体药物组合物
JP7811014B2 (ja) 2020-03-02 2026-02-04 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
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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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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

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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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TWI754629B (zh) 2022-02-11
EA035951B1 (ru) 2020-09-04
ES2830443T3 (es) 2021-06-03
US20190040071A1 (en) 2019-02-07
UA121161C2 (uk) 2020-04-10
MX2018009501A (es) 2018-12-11
JP2019505533A (ja) 2019-02-28
TW201728589A (zh) 2017-08-16
CL2018002092A1 (es) 2018-12-07
PL3412672T3 (pl) 2021-01-25
IL260968B (en) 2022-05-01
LT3412672T (lt) 2020-11-10
NZ744884A (en) 2022-09-30
KR102393280B1 (ko) 2022-05-02
DK3412672T3 (da) 2020-10-19
CN108602831B (zh) 2020-11-03
CN108602831A (zh) 2018-09-28
EA201891768A1 (ru) 2019-01-31
EP3412672A4 (en) 2019-07-17
CA3013518A1 (en) 2017-08-10
JP6889171B2 (ja) 2021-06-18
CN108602831B9 (zh) 2020-12-04
HK1259170A1 (zh) 2019-11-29
US10947245B2 (en) 2021-03-16
US20200039988A1 (en) 2020-02-06
ZA201805186B (en) 2024-08-28
AU2017215801A1 (en) 2018-08-23
SG11201806683UA (en) 2018-09-27
PH12018501643A1 (en) 2019-06-03
AU2017215801B2 (en) 2020-09-10
MX374297B (es) 2025-03-06
PT3412672T (pt) 2020-11-11
EP3412672A1 (en) 2018-12-12
EP3412672B1 (en) 2020-07-15
US10442811B2 (en) 2019-10-15
KR20180104117A (ko) 2018-09-19
CA3013518C (en) 2022-07-19
WO2017133684A1 (zh) 2017-08-10
AR107548A1 (es) 2018-05-09
SI3412672T1 (sl) 2021-02-26
BR112018015880A2 (pt) 2018-12-26
HRP20201644T1 (hr) 2020-12-25
HUE051399T2 (hu) 2021-03-01

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