CN111819178A - 一种吡唑并杂芳基类衍生物盐酸盐的晶型及制备方法 - Google Patents

一种吡唑并杂芳基类衍生物盐酸盐的晶型及制备方法 Download PDF

Info

Publication number
CN111819178A
CN111819178A CN201980017419.9A CN201980017419A CN111819178A CN 111819178 A CN111819178 A CN 111819178A CN 201980017419 A CN201980017419 A CN 201980017419A CN 111819178 A CN111819178 A CN 111819178A
Authority
CN
China
Prior art keywords
formula
compound
solvent
crystallization
crystal form
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.)
Granted
Application number
CN201980017419.9A
Other languages
English (en)
Other versions
CN111819178B (zh
Inventor
曹笑立
杜振兴
王立坤
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.)
Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
Original Assignee
Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical 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 Jiangsu Hengrui Medicine Co Ltd, Shanghai Hengrui Pharmaceutical Co Ltd filed Critical Jiangsu Hengrui Medicine Co Ltd
Publication of CN111819178A publication Critical patent/CN111819178A/zh
Application granted granted Critical
Publication of CN111819178B publication Critical patent/CN111819178B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

本发明涉及一种吡唑并杂芳基类衍生物盐酸盐的晶型及制备方法。具体地，本发明涉及式(I)所示化合物的二盐酸盐的Ⅰ晶型、Ⅱ晶型、式(I)所示化合物的单盐酸盐的A晶型、B晶型、C晶型及其制备方法。本发明式(I)化合物的晶型具备良好的晶型稳定性，可更好地用于临床治疗。
Figure DDA0002667209580000011

Description

PCT国内申请，说明书已公开。

Claims (25)

  1. PCT国内申请，权利要求书已公开。
CN201980017419.9A 2018-05-25 2019-05-24 一种吡唑并杂芳基类衍生物盐酸盐的晶型及制备方法 Active CN111819178B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2018105125637 2018-05-25
CN201810512563 2018-05-25
PCT/CN2019/088250 WO2019223773A1 (zh) 2018-05-25 2019-05-24 一种吡唑并杂芳基类衍生物盐酸盐的晶型及制备方法

Publications (2)

Publication Number Publication Date
CN111819178A true CN111819178A (zh) 2020-10-23
CN111819178B CN111819178B (zh) 2022-04-12

Family

ID=68615672

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980017419.9A Active CN111819178B (zh) 2018-05-25 2019-05-24 一种吡唑并杂芳基类衍生物盐酸盐的晶型及制备方法

Country Status (11)

Country Link
US (1) US20210188856A1 (zh)
EP (1) EP3808745A4 (zh)
JP (1) JP2021526520A (zh)
KR (1) KR20210013624A (zh)
CN (1) CN111819178B (zh)
AU (1) AU2019272463A1 (zh)
BR (1) BR112020023875A2 (zh)
CA (1) CA3100873A1 (zh)
MX (1) MX2020012651A (zh)
TW (1) TWI704916B (zh)
WO (1) WO2019223773A1 (zh)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008114008A1 (en) * 2007-03-19 2008-09-25 Astrazeneca Ab 9-substituted-8-oxo-adenine compounds as toll-like receptor (tlr7 ) modulators
CN102272134A (zh) * 2008-12-09 2011-12-07 吉里德科学公司 Toll样受体调节剂
CN102666541A (zh) * 2009-10-22 2012-09-12 吉里德科学公司 用于治疗特别是病毒感染的嘌呤或脱氮嘌呤的衍生物
WO2015162075A1 (en) * 2014-04-22 2015-10-29 F. Hoffmann-La Roche Ag 4-amino-imidazoquinoline compounds

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60118754T2 (de) 2000-08-08 2007-01-11 Ortho-Mcneil Pharmaceutical, Inc. Bicyclische verbindungen als h3 rezeptor liganden
AU2004271972B2 (en) 2003-09-05 2010-06-03 Anadys Pharmaceuticals, Inc. TLR7 ligands for the treatment of hepatitis C
ATE532784T1 (de) 2006-02-17 2011-11-15 Pfizer Ltd 3-deazapurinderivate als tlr7-modulatoren
DE602007012881D1 (en) 2006-07-18 2011-04-14 Anadys Pharmaceuticals Inc Carbonat- und carbamat-prodrugs von thiazolo ä4,5-dü-pyrimidinen
CN101917999A (zh) * 2007-11-07 2010-12-15 弗尔德里克斯制药股份有限公司 蛋白质运输的调节
US8865896B2 (en) 2008-01-17 2014-10-21 Astrazeneca Aktiebolag Method for preparing adenine compound
GB0908772D0 (en) 2009-05-21 2009-07-01 Astrazeneca Ab New salts 756
AU2010292102B2 (en) 2009-09-14 2015-04-09 Gilead Sciences, Inc. Modulators of Toll-like receptors
US8895570B2 (en) 2010-12-17 2014-11-25 Astrazeneca Ab Purine derivatives
MY192084A (en) * 2016-11-28 2022-07-26 Jiangsu Hengrui Medicine Co Pyrazolo-heteroaryl derivative, preparation method and medical use thereof
EP3636646A4 (en) * 2017-05-18 2020-12-09 Jiangsu Hengrui Medicine Co., Ltd. HETEROARYL PYRAZOL DERIVATIVE AND MANUFACTURING METHOD FOR IT AND MEDICAL USES THEREOF
TW202027792A (zh) * 2018-09-29 2020-08-01 大陸商江蘇恆瑞醫藥股份有限公司 Ｔｌｒ激動劑與免疫檢查點抑制劑聯合在製備治療腫瘤的藥物中的用途

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008114008A1 (en) * 2007-03-19 2008-09-25 Astrazeneca Ab 9-substituted-8-oxo-adenine compounds as toll-like receptor (tlr7 ) modulators
CN102272134A (zh) * 2008-12-09 2011-12-07 吉里德科学公司 Toll样受体调节剂
CN102666541A (zh) * 2009-10-22 2012-09-12 吉里德科学公司 用于治疗特别是病毒感染的嘌呤或脱氮嘌呤的衍生物
WO2015162075A1 (en) * 2014-04-22 2015-10-29 F. Hoffmann-La Roche Ag 4-amino-imidazoquinoline compounds

Also Published As

Publication number Publication date
JP2021526520A (ja) 2021-10-07
KR20210013624A (ko) 2021-02-04
BR112020023875A2 (pt) 2021-02-09
US20210188856A1 (en) 2021-06-24
WO2019223773A1 (zh) 2019-11-28
TWI704916B (zh) 2020-09-21
EP3808745A1 (en) 2021-04-21
CA3100873A1 (en) 2019-11-28
AU2019272463A1 (en) 2021-01-07
EP3808745A4 (en) 2022-03-09
MX2020012651A (es) 2021-02-02
TW202002965A (zh) 2020-01-16
CN111819178B (zh) 2022-04-12

Similar Documents

Publication Publication Date Title
CN110177793B (zh) 杂芳基并吡唑类衍生物、其制备方法及其在医药上的应用
US8143402B2 (en) Polymorphic forms of a macrocyclic inhibitor of HCV
CN109311891B (zh) 作为jak抑制剂的吡咯并嘧啶化合物的结晶
JP6877450B2 (ja) Ｔｌｒ７アゴニストのトリフルオロ酢酸塩及びその結晶形ｂ、調製方法、並びに使用
IL282632B1 (en) Trifluoromethyl-converted sulfonamide as a selective BCL-2 inhibitor
CN115667246A (zh) 一种哒嗪类衍生物自由碱的晶型及其制备方法和应用
CN110526918B (zh) 一种吡唑并杂芳基类衍生物的晶型及制备方法
JP2022549923A (ja) Ｎヘテロ五員環含有カプシドタンパク質集合阻害剤の結晶形及びその使用
US20230058425A1 (en) Crystal form of pyridopyrimidine derivative and preparation method thereof
CN114728973B (zh) 一种核蛋白抑制剂的晶型及其应用
EP3896063B1 (en) Crystalline forms of the syk inhibitor 5-fluoro-1-methyl-3-[[5-[4-(3-oxetanyl)-1-piperazinyl]-2-pyridinyl]amino]-6-(1h-pyrazol-3-yl)-2(1h)-quinolinone hydrochloride salt (1:1)
CN111819178B (zh) 一种吡唑并杂芳基类衍生物盐酸盐的晶型及制备方法
CN112154144B (zh) 一种1,2,4-三嗪-3-胺类衍生物的晶型及制备方法
EP4438606A1 (en) New crystal form of nucleoside compound and salt thereof
CN110526917B (zh) 一种吡唑并杂芳基类衍生物的可药用盐、晶型及其制备方法
CN112334473B (zh) 一种杂芳基并[4,3-c]嘧啶-5-胺类衍生物的晶型及制备方法
CN112745268B (zh) 苯并咪唑衍生物的晶型及制备方法
CN111484498B (zh) 咪唑并[1,5-a]吡嗪类化合物的晶型及其制备方法
US20230067666A1 (en) Method for preparing coumarin compounds substituted by amidoalkyl at 3-position, the products and related intermediates thereof
CN110903291A (zh) 一种杂芳基并[4,3-c]嘧啶-5-胺类衍生物的盐、盐的晶型及制备方法

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant