ES2830443T3 - 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 - Google Patents

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 Download PDF

Info

Publication number
ES2830443T3
ES2830443T3 ES17747004T ES17747004T ES2830443T3 ES 2830443 T3 ES2830443 T3 ES 2830443T3 ES 17747004 T ES17747004 T ES 17747004T ES 17747004 T ES17747004 T ES 17747004T ES 2830443 T3 ES2830443 T3 ES 2830443T3
Authority
ES
Spain
Prior art keywords
crystalline form
compound
formula
crystalline
composition
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
ES17747004T
Other languages
English (en)
Spanish (es)
Inventor
Zhaozhong Ding
Fei Sun
Yinghu Hu
Yilong Zhou
Zheng Wang
Rui Zhao
Ling Yang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Original Assignee
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Chia Tai Tianqing Pharmaceutical Group Co Ltd filed Critical Chia Tai Tianqing Pharmaceutical Group Co Ltd
Application granted granted Critical
Publication of ES2830443T3 publication Critical patent/ES2830443T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • 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)
ES17747004T 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 Active ES2830443T3 (es)

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)

Publication Number Publication Date
ES2830443T3 true ES2830443T3 (es) 2021-06-03

Family

ID=59499348

Family Applications (1)

Application Number Title Priority Date Filing Date
ES17747004T Active 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

Country Status (27)

Country Link
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)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20180229A (es) 2015-10-29 2018-08-24 Novartis Ag Conjugados de anticuerpos que comprenden un agonista del receptor tipo toll
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
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
BR112021015577A2 (pt) 2019-02-08 2021-10-05 Research & Business Foundation Sungkyunkwan University Complexo-colesterol agonista do receptor toll-like 7 ou 8 e uso do mesmo
ES3070986T3 (en) 2019-03-15 2026-06-18 Chia Tai Tianqing Pharmaceutical Group Co Ltd Toll-like receptor agonists for use in the treatment of hepatitis b
SG11202111488YA (en) * 2019-04-23 2021-11-29 Chia Tai Tianqing Pharmaceutical Group Co Ltd Solid pharmaceutical composition comprising tlr7 agonist
CN115666637A (zh) 2020-03-02 2023-01-31 蛋白科技先锋 基于病原体细胞壁骨架的模拟活病原体的纳米粒子及其制备方法
EP4194008A4 (en) 2020-08-04 2025-01-08 Progeneer Inc. Kinetically acting adjuvant ensemble
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
WO2022031021A1 (ko) 2020-08-04 2022-02-10 성균관대학교산학협력단 동력학적 제어가 가능한 아주번트를 포함하는 mrna 백신
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
WO2025110816A1 (ko) 2023-11-23 2025-05-30 프로지니어 주식회사 암의 치료를 위한 활성화 부위가 일시적으로 비활성화된 톨-유사 수용체 7 또는 8 작용자와 항암 치료의 병용요법

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
CA2620182A1 (en) * 2005-08-22 2007-03-01 Dennis A. Carson Tlr agonists
UY32306A (es) 2008-12-09 2010-07-30 Gilead Sciences Inc Derivados de pteridinona y pirimidinodiazepinona y composiciones farmacéuticas que modulan en forma selectiva los receptores tipo toll, métodos y usos
JP5813785B2 (ja) 2011-02-04 2015-11-17 デュケイン ユニバーシティー オブ ザ ホリー スピリット 抗チューブリン活性を有する二環式および三環式のピリミジンチロシンキナーゼ阻害剤ならびに患者の処置方法
WO2013103967A1 (en) 2012-01-05 2013-07-11 Northeastern University Allosteric modulators of cb1 cannabinoid receptors
MX386924B (es) * 2012-10-10 2025-03-19 Janssen Sciences Ireland Uc Derivados pirrolo[3,2-d]pirimidínicos para el tratamiento de infecciones víricas y otras enfermedades.
JP6216387B2 (ja) 2012-11-20 2017-10-18 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーGlaxoSmithKline LLC 新規化合物
KR20150085081A (ko) * 2012-11-20 2015-07-22 글락소스미스클라인 엘엘씨 신규 화합물
SMT201700378T1 (it) * 2012-11-20 2017-09-07 Glaxosmithkline Llc Nuovi composti
WO2015168269A1 (en) 2014-05-01 2015-11-05 Novartis Ag Compounds and compositions as toll-like receptor 7 agonists
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
CN112898308B (zh) * 2014-08-15 2026-08-07 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
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
MX374297B (es) 2025-03-06
HUE051399T2 (hu) 2021-03-01
PT3412672T (pt) 2020-11-11
JP2019505533A (ja) 2019-02-28
US10947245B2 (en) 2021-03-16
KR102393280B1 (ko) 2022-05-02
CA3013518C (en) 2022-07-19
TWI754629B (zh) 2022-02-11
EA035951B1 (ru) 2020-09-04
HK1259170A1 (zh) 2019-11-29
CN108602831B9 (zh) 2020-12-04
AR107548A1 (es) 2018-05-09
AU2017215801A1 (en) 2018-08-23
DK3412672T3 (da) 2020-10-19
SI3412672T1 (sl) 2021-02-26
KR20180104117A (ko) 2018-09-19
IL260968B (en) 2022-05-01
EP3412672B1 (en) 2020-07-15
SG11201806683UA (en) 2018-09-27
PH12018501643A1 (en) 2019-06-03
US10442811B2 (en) 2019-10-15
HRP20201644T1 (hr) 2020-12-25
AU2017215801B2 (en) 2020-09-10
LT3412672T (lt) 2020-11-10
EA201891768A1 (ru) 2019-01-31
CA3013518A1 (en) 2017-08-10
CL2018002092A1 (es) 2018-12-07
WO2017133684A1 (zh) 2017-08-10
ZA201805186B (en) 2024-08-28
NZ744884A (en) 2022-09-30
US20190040071A1 (en) 2019-02-07
CN108602831B (zh) 2020-11-03
EP3412672A1 (en) 2018-12-12
US20200039988A1 (en) 2020-02-06
CN107043379A (zh) 2017-08-15
MX2018009501A (es) 2018-12-11
EP3412672A4 (en) 2019-07-17
TW201728589A (zh) 2017-08-16
PL3412672T3 (pl) 2021-01-25
JP6889171B2 (ja) 2021-06-18
CN108602831A (zh) 2018-09-28
UA121161C2 (uk) 2020-04-10
BR112018015880A2 (pt) 2018-12-26

Similar Documents

Publication Publication Date Title
ES2834304T3 (es) Sal de trifluoroacetato de un agonista de TLR7 y forma cristalina B de la misma, métodos de preparación y usos
ES2834303T3 (es) Sal de maleato de agonista de TLR7, formas cristalinas C, D y E de la misma, métodos de preparación y usos de la sal de maleato y las formas cristalinas
US10947245B2 (en) 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
BR112018015881B1 (pt) Sal de maleato de agonista de tlr7, formas cristalinas, c, d e e, seusprocessos de preparação e seus usos, e composições cristalina efarmacêutica
BR112018015880B1 (pt) Forma cristalina a de agonista de tlr7, seu uso e seu processo de preparação, composição cristalina, e composição farmacêutica
BR112018015878B1 (pt) Forma cristalina b de sal de trifluoracetato agonista de tlr7, seu processo de preparação, composições cristalina e farmacêutica, e seus usos