CN115427397A - 硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用 - Google Patents

硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用 Download PDF

Info

Publication number
CN115427397A
CN115427397A CN202180024008.XA CN202180024008A CN115427397A CN 115427397 A CN115427397 A CN 115427397A CN 202180024008 A CN202180024008 A CN 202180024008A CN 115427397 A CN115427397 A CN 115427397A
Authority
CN
China
Prior art keywords
solvent
methyl
ether
oxy
isobutyryl
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
CN202180024008.XA
Other languages
English (en)
Other versions
CN115427397B (zh
Inventor
吴亮
周琛
邓一军
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.)
Shanghai Yahong Pharmaceutical Technology Co ltd
Jiangsu Yahong Pharmaceutical Technology Co ltd
Original Assignee
Shanghai Yahong Pharmaceutical Technology Co ltd
Jiangsu Yahong Pharmaceutical Technology 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 Shanghai Yahong Pharmaceutical Technology Co ltd, Jiangsu Yahong Pharmaceutical Technology Co ltd filed Critical Shanghai Yahong Pharmaceutical Technology Co ltd
Publication of CN115427397A publication Critical patent/CN115427397A/zh
Application granted granted Critical
Publication of CN115427397B publication Critical patent/CN115427397B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further 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
    • 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

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

本发明涉及硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用。A晶型的X‑射线粉末衍射图谱包括位于5.74±0.2°、6.78±0.2°、10.86±0.2°、13.54±0.2°、16.70±0.2°和22.65±0.2°处的特征峰。B晶型的X‑射线粉末衍射图谱包括位于5.44±0.2°、10.90±0.2°、14.09±0.2°、16.17±0.2°、17.92±0.2°、20.66±0.2°和23.13±0.2°处的特征峰。与硝羟喹啉相比，本发明的A晶型和B晶型，不易染色，对设备要求低，更利于工业生产化；性质稳定，更利于工业生产上的质量控制和药物药效的稳定性。

Description

PCT国内申请，说明书已公开。

Claims (19)

  1. PCT国内申请，权利要求书已公开。
CN202180024008.XA 2020-03-30 2021-03-30 硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用 Active CN115427397B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2020102361476 2020-03-30
CN202010236147 2020-03-30
PCT/CN2021/084057 WO2021197338A1 (zh) 2020-03-30 2021-03-30 硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用

Publications (2)

Publication Number Publication Date
CN115427397A true CN115427397A (zh) 2022-12-02
CN115427397B CN115427397B (zh) 2024-01-26

Family

ID=77929313

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180024008.XA Active CN115427397B (zh) 2020-03-30 2021-03-30 硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用

Country Status (11)

Country Link
US (1) US20230119296A1 (zh)
EP (1) EP4129983A4 (zh)
JP (1) JP2023519276A (zh)
KR (1) KR20230008047A (zh)
CN (1) CN115427397B (zh)
AU (1) AU2021245884A1 (zh)
BR (1) BR112022017437A2 (zh)
CA (1) CA3171261A1 (zh)
MX (1) MX2022011768A (zh)
TW (1) TW202144329A (zh)
WO (1) WO2021197338A1 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022502510A (ja) * 2018-09-29 2022-01-11 江▲蘇▼▲亞▼虹医▲薬▼科技股▲フン▼有限公司Jiangsu Yahong Meditech Co., Ltd ニトロキソリンプロドラッグ及びその使用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4749406A (en) * 1983-10-18 1988-06-07 Ciba-Geigy Corporation Quinoline derivatives and compositions thereof for the protection of cultivated plants
CN102239149A (zh) * 2008-10-06 2011-11-09 约翰·霍普金斯大学 喹啉化合物作为血管新生、人类甲硫氨酰氨肽酶、以及sirt1的抑制剂,以及治疗病症的方法
WO2011150338A1 (en) * 2010-05-27 2011-12-01 Zafgen Corporation Methods of treating obesity
CN111295372A (zh) * 2018-09-29 2020-06-16 江苏亚虹医药科技有限公司 硝羟喹啉前药及其用途
CN111514142A (zh) * 2020-05-29 2020-08-11 江苏亚虹医药科技有限公司 含硝羟喹啉前药的药物组合物及其制备方法和应用
CN111646936A (zh) * 2020-06-22 2020-09-11 江苏亚虹医药科技有限公司 芳香醚类化合物的制备方法

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4749406A (en) * 1983-10-18 1988-06-07 Ciba-Geigy Corporation Quinoline derivatives and compositions thereof for the protection of cultivated plants
CN102239149A (zh) * 2008-10-06 2011-11-09 约翰·霍普金斯大学 喹啉化合物作为血管新生、人类甲硫氨酰氨肽酶、以及sirt1的抑制剂,以及治疗病症的方法
WO2011150338A1 (en) * 2010-05-27 2011-12-01 Zafgen Corporation Methods of treating obesity
CN111295372A (zh) * 2018-09-29 2020-06-16 江苏亚虹医药科技有限公司 硝羟喹啉前药及其用途
CN111514142A (zh) * 2020-05-29 2020-08-11 江苏亚虹医药科技有限公司 含硝羟喹啉前药的药物组合物及其制备方法和应用
CN111646936A (zh) * 2020-06-22 2020-09-11 江苏亚虹医药科技有限公司 芳香醚类化合物的制备方法

Also Published As

Publication number Publication date
WO2021197338A1 (zh) 2021-10-07
CA3171261A1 (en) 2021-10-07
AU2021245884A1 (en) 2022-09-29
JP2023519276A (ja) 2023-05-10
TW202144329A (zh) 2021-12-01
MX2022011768A (es) 2022-10-18
KR20230008047A (ko) 2023-01-13
BR112022017437A2 (pt) 2022-10-18
CN115427397B (zh) 2024-01-26
US20230119296A1 (en) 2023-04-20
EP4129983A4 (en) 2024-03-13
EP4129983A1 (en) 2023-02-08

Similar Documents

Publication Publication Date Title
CN107531682B (zh) B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途
WO2011095059A1 (zh) 达沙替尼多晶型物及其制备方法和药物组合物
US10752595B2 (en) Crystalline forms of a bromodomain and extraterminal protein inhibitor drug, processes for preparation thereof, and use thereof
CN109195980B (zh) 一种钠-葡萄糖协同转运蛋白抑制剂药物的新晶型及其制备方法和用途
WO2009093127A2 (en) Substantially pure and a stable crystalline form of bosentan
EP4006031A1 (en) Dihydro-pyrrolo-pyrimidine selective jak2 inhibitor
CN114773342A (zh) Mrtx849化合物的晶型及其制备方法和用途
CN114605406A (zh) Amg510化合物的晶型及其制备方法和用途
CN115427397B (zh) 硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用
EP2874628B1 (en) Salts and hydrates of antipsychotics
WO2023193563A1 (zh) 一种噻吩并吡啶化合物的晶型a、制备方法及其药物组合物
WO2019134455A1 (zh) Acalabrutinib的新晶型及其制备方法和用途
EP3315493B1 (en) Phenyl amino pyrimidine compound or polymorph of salt thereof
EP3941472B1 (en) Crystalline and amorphous forms of-(5-((4-ethylpiperazin-1-yl)methyl)pyridine-2-yl)-5-fluoro-4-(3-isopropyl-2-methyl-2 <ns1:i>h</ns1:i>?-indazol-5-yl)pyrimidin-2-amine and its salts, and preparation methods and therapeutic uses thereof
EP4083040A1 (en) Irak4 inhibitor crystal and preparation method therefor
EP3179858B1 (en) Forms and compositions of an erk inhibitor
US10138206B2 (en) Amorphous form of lomitapide mesylate
EP3674306B1 (en) Thienopyridine derivatives containing an ethylenic ester, preparation method therefor and use thereof
WO2019105359A1 (zh) Acalabrutinib的晶型及其制备方法和用途
WO2020053660A1 (en) Solid forms of a bet inhibitor
WO2018082596A1 (en) Solid forms of an adamantyl compound, compositions and uses thereof
EP4230625A1 (en) Crystal form of multi-substituted benzene ring compound maleate, and preparation method therefor and use thereof
CN110903291B (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
CN116478141B (zh) 氘代kras抑制剂药物及用途
CN111484489B (zh) 无定形的b-raf激酶二聚体抑制剂

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
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40076636

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant