KR102393279B1 - Tlr7 작용제 말레에이트 염, 이의 결정형 c, d 및 e, 말레에이트 염 및 결정형의 제조 방법 및 용도 - Google Patents

Tlr7 작용제 말레에이트 염, 이의 결정형 c, d 및 e, 말레에이트 염 및 결정형의 제조 방법 및 용도 Download PDF

Info

Publication number
KR102393279B1
KR102393279B1 KR1020187024626A KR20187024626A KR102393279B1 KR 102393279 B1 KR102393279 B1 KR 102393279B1 KR 1020187024626 A KR1020187024626 A KR 1020187024626A KR 20187024626 A KR20187024626 A KR 20187024626A KR 102393279 B1 KR102393279 B1 KR 102393279B1
Authority
KR
South Korea
Prior art keywords
crystalline
formula
compound
maleate
ray powder
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
KR1020187024626A
Other languages
English (en)
Korean (ko)
Other versions
KR20180104116A (ko
Inventor
자오종 딩
페이 순
잉후 후
이룽 주
젱 왕
링 양
Original Assignee
치아타이 티안큉 파마수티컬 그룹 주식회사
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 치아타이 티안큉 파마수티컬 그룹 주식회사 filed Critical 치아타이 티안큉 파마수티컬 그룹 주식회사
Publication of KR20180104116A publication Critical patent/KR20180104116A/ko
Application granted granted Critical
Publication of KR102393279B1 publication Critical patent/KR102393279B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/01Hydrocarbons
    • A61K31/015Hydrocarbons carbocyclic
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1020187024626A 2016-02-05 2017-02-04 Tlr7 작용제 말레에이트 염, 이의 결정형 c, d 및 e, 말레에이트 염 및 결정형의 제조 방법 및 용도 Active KR102393279B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610082030.0 2016-02-05
CN201610082030.0A CN107043380A (zh) 2016-02-05 2016-02-05 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
PCT/CN2017/072890 WO2017133683A1 (zh) 2016-02-05 2017-02-04 一种tlr7激动剂的马来酸盐、其晶型c、晶型d、晶型e及其制备方法和用途

Publications (2)

Publication Number Publication Date
KR20180104116A KR20180104116A (ko) 2018-09-19
KR102393279B1 true KR102393279B1 (ko) 2022-05-02

Family

ID=59500111

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020187024626A Active KR102393279B1 (ko) 2016-02-05 2017-02-04 Tlr7 작용제 말레에이트 염, 이의 결정형 c, d 및 e, 말레에이트 염 및 결정형의 제조 방법 및 용도

Country Status (23)

Country Link
US (2) US10780091B2 (https=)
EP (1) EP3412671B1 (https=)
JP (1) JP6898336B2 (https=)
KR (1) KR102393279B1 (https=)
CN (2) CN107043380A (https=)
AR (1) AR107547A1 (https=)
AU (1) AU2017215800B2 (https=)
CA (1) CA3013682C (https=)
CL (1) CL2018002089A1 (https=)
DK (1) DK3412671T3 (https=)
EA (1) EA038794B1 (https=)
ES (1) ES2834303T3 (https=)
HU (1) HUE052211T2 (https=)
IL (1) IL260965B (https=)
MX (1) MX374295B (https=)
MY (1) MY196762A (https=)
NZ (1) NZ745231A (https=)
PH (1) PH12018501644B1 (https=)
SG (1) SG11201806682TA (https=)
TW (1) TWI778951B (https=)
UA (1) UA123781C2 (https=)
WO (1) WO2017133683A1 (https=)
ZA (1) ZA201805185B (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
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
CN116322751A (zh) 2020-08-04 2023-06-23 蛋白科技先锋 包含能够动力学控制的佐剂的mRNA疫苗
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
US20230355750A1 (en) 2020-08-04 2023-11-09 Progeneer Inc. Kinetically acting adjuvant ensemble

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013103967A1 (en) 2012-01-05 2013-07-11 Northeastern University Allosteric modulators of cb1 cannabinoid receptors
JP2014504644A (ja) 2011-02-04 2014-02-24 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

Family Cites Families (24)

* 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
ATE283855T1 (de) 1996-07-03 2004-12-15 Sumitomo Pharma Neue purinderivate
NZ504800A (en) 1997-11-28 2001-10-26 Sumitomo Pharma 6-Amino-9-benzyl-8-hydroxy-purine derivatives and interferon inducers, antiviral agents, anticancer agents and therapeutic agents for immunologic diseases thereof
ES2577514T3 (es) 2005-08-22 2016-07-15 The Regents Of The University Of California Antagonistas de TLR
CA2691444C (en) 2007-06-29 2016-06-14 Gilead Sciences, Inc. Purine derivatives and their use as modulators of toll-like receptor 7
CA2707030A1 (en) 2007-08-03 2009-02-12 Pfizer Limited Imidazopyridinones
ES2467108T3 (es) 2008-12-09 2014-06-11 Gilead Sciences, Inc. Moduladores de receptores tipo toll
LT2906563T (lt) * 2012-10-10 2018-06-11 Janssen Sciences Ireland Uc Pirolo[3,2-d]pirimidino dariniai virusinių infekcijų ir kitų ligų gydymui
US9550785B2 (en) 2012-11-20 2017-01-24 Glaxosmithkline Llc Pyrrolopyrimidines as therapeutic agents for the treatment of diseases
KR20150085081A (ko) 2012-11-20 2015-07-22 글락소스미스클라인 엘엘씨 신규 화합물
MX358025B (es) 2012-11-20 2018-08-02 Glaxosmithkline Llc Star Compuestos novedosos.
KR20160124157A (ko) 2014-02-20 2016-10-26 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 인간 인터페론의 유도인자로서의 피롤로[3,2]피리미딘 유도체
JP6484253B2 (ja) * 2014-05-01 2019-03-13 ノバルティス アーゲー Toll様受容体7アゴニストとしての化合物および組成物
EA032487B1 (ru) 2014-05-01 2019-06-28 Новартис Аг Соединения и композиции в качестве агонистов toll-подобного рецептора 7
HUE054672T2 (hu) 2014-08-15 2021-09-28 Chia Tai Tianqing Pharmaceutical Group Co Ltd TLR7 agonistaként alkalmazott pirrolopirimidin vegyületek
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
CN105732635A (zh) 2014-12-29 2016-07-06 南京明德新药研发股份有限公司 一类Toll样受体7激动剂
TWI714661B (zh) 2015-11-05 2021-01-01 法商賽諾菲公司 新穎念珠藻素化合物及接合物、其製備與其治療用途
CA3004173C (en) 2015-11-05 2020-07-14 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. 7-(thiazol-5-yl)pyrrolopyrimidine compound as tlr7 agonist
CR20180310A (es) 2015-11-05 2018-11-30 Basf Se Oxadiazoles sustituidos para combatir hongod fitopatógenos
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
CN107043377A (zh) * 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 一种tlr7激动剂的三氟乙酸盐、晶型b及其制备方法、药物组合物和用途
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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014504644A (ja) 2011-02-04 2014-02-24 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

Also Published As

Publication number Publication date
HK1259175A1 (zh) 2019-11-29
US20200368241A1 (en) 2020-11-26
IL260965B (en) 2022-02-01
SG11201806682TA (en) 2018-09-27
CN107043380A (zh) 2017-08-15
JP2019505532A (ja) 2019-02-28
AR107547A1 (es) 2018-05-09
EA038794B1 (ru) 2021-10-20
NZ745231A (en) 2022-07-29
US20190070179A1 (en) 2019-03-07
PH12018501644B1 (en) 2022-09-07
PH12018501644A1 (en) 2019-06-03
EP3412671A4 (en) 2019-07-24
DK3412671T3 (da) 2020-11-09
MX2018009500A (es) 2018-12-11
ZA201805185B (en) 2024-08-28
BR112018015881A2 (pt) 2018-12-26
UA123781C2 (uk) 2021-06-02
KR20180104116A (ko) 2018-09-19
CA3013682C (en) 2022-06-21
AU2017215800B2 (en) 2020-08-20
CN108602830B (zh) 2020-07-28
JP6898336B2 (ja) 2021-07-07
US10780091B2 (en) 2020-09-22
HUE052211T2 (hu) 2021-04-28
EP3412671B1 (en) 2020-09-16
WO2017133683A1 (zh) 2017-08-10
CL2018002089A1 (es) 2018-12-07
MY196762A (en) 2023-05-03
ES2834303T3 (es) 2021-06-17
CA3013682A1 (en) 2017-08-10
AU2017215800A1 (en) 2018-08-30
EP3412671A1 (en) 2018-12-12
CN108602830A (zh) 2018-09-28
TWI778951B (zh) 2022-10-01
TW201728588A (zh) 2017-08-16
MX374295B (es) 2025-03-06
EA201891770A1 (ru) 2019-01-31

Similar Documents

Publication Publication Date Title
KR102393280B1 (ko) Tlr7 작용제 결정형 a, 이의 제조 방법 및 용도
KR102393281B1 (ko) Tlr7 작용제 트리플루오로아세테이트 염 및 이의 결정형 b, 제조방법 및 용도
KR102393279B1 (ko) Tlr7 작용제 말레에이트 염, 이의 결정형 c, d 및 e, 말레에이트 염 및 결정형의 제조 방법 및 용도
HK1259182B (zh) 一种tlr7激动剂的三氟乙酸盐、晶型b、制备方法和用途
HK1259175B (zh) 一种tlr7激动剂的马来酸盐、其晶型c、晶型d、晶型e及其制备方法和用途

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

A201 Request for examination
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

D13-X000 Search requested

St.27 status event code: A-1-2-D10-D13-srh-X000

D14-X000 Search report completed

St.27 status event code: A-1-2-D10-D14-srh-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-OTH-PR1001 (AS PROVIDED BY THE NATIONAL OFFICE)

Year of fee payment: 4