AU2009207966B2 - Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof - Google Patents

Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof Download PDF

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Publication number
AU2009207966B2
AU2009207966B2 AU2009207966A AU2009207966A AU2009207966B2 AU 2009207966 B2 AU2009207966 B2 AU 2009207966B2 AU 2009207966 A AU2009207966 A AU 2009207966A AU 2009207966 A AU2009207966 A AU 2009207966A AU 2009207966 B2 AU2009207966 B2 AU 2009207966B2
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Prior art keywords
mixture
methyl
mmol
carboxylic acid
dihydro
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AU2009207966A1 (en
Inventor
Yiqian Chen
Hongbo Fei
Hejun Lu
Peng Cho Tang
Li Wang
Shenglan Wang
Hao Zheng
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D231/08Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with oxygen or sulfur atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • C07D231/22One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2009207966A 2008-01-10 2009-01-04 Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof Active AU2009207966B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN200810000346.6 2008-01-10
CNA2008100003466A CN101481352A (zh) 2008-01-10 2008-01-10 双环取代吡唑酮偶氮类衍生物、其制备方法及其在医药上的应用
PCT/CN2009/000001 WO2009092276A1 (zh) 2008-01-10 2009-01-04 双环取代吡唑酮偶氮类衍生物、其制备方法及其在医药上的应用

Publications (2)

Publication Number Publication Date
AU2009207966A1 AU2009207966A1 (en) 2009-07-30
AU2009207966B2 true AU2009207966B2 (en) 2013-03-21

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AU2009207966A Active AU2009207966B2 (en) 2008-01-10 2009-01-04 Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof

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US (2) US8367710B2 (https=)
EP (1) EP2236500B1 (https=)
JP (1) JP5441269B2 (https=)
KR (1) KR101556808B1 (https=)
CN (2) CN101481352A (https=)
AU (1) AU2009207966B2 (https=)
BR (1) BRPI0907234B1 (https=)
CA (1) CA2711535C (https=)
ES (1) ES2533366T3 (https=)
MX (1) MX2010007553A (https=)
PT (1) PT2236500E (https=)
RU (1) RU2488582C2 (https=)
UA (1) UA101172C2 (https=)
WO (1) WO2009092276A1 (https=)
ZA (1) ZA201004794B (https=)

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SE0302486D0 (sv) * 2003-09-18 2003-09-18 Astrazeneca Ab Novel compounds
CN101921232A (zh) * 2009-06-11 2010-12-22 上海恒瑞医药有限公司 双环取代吡唑酮偶氮类衍生物的盐,其制备方法及其在医药上的应用
JP5704073B2 (ja) * 2009-10-23 2015-04-22 日産化学工業株式会社 縮環へテロ環化合物及びトロンボポエチンレセプター活性化剤
CN103360317B (zh) * 2012-04-11 2016-12-14 齐鲁制药有限公司 双环取代吡唑酮偶氮类衍生物、其制备方法及用途
CN103724206A (zh) * 2014-01-17 2014-04-16 青岛农业大学 化合物2-溴-4-氟-6-硝基苯酚的制备方法和农用生物活性
WO2015111085A2 (en) * 2014-01-27 2015-07-30 Cadila Healthcare Limited Processes for the preparation of eltrombopag and pharmaceutically acceptable salts, solvates and intermediates thereof
US9849077B2 (en) 2014-03-10 2017-12-26 Mary Kay Inc. Skin lightening compositions
CN104592033A (zh) * 2014-12-30 2015-05-06 杭州和泽医药科技有限公司 一种艾曲波帕关键中间体的合成方法
CN106994120B (zh) * 2016-01-22 2021-05-14 江苏恒瑞医药股份有限公司 一种含有双环取代吡唑酮偶氮类衍生物或其盐的药物组合物及其制备方法
TW201726129A (zh) * 2016-01-22 2017-08-01 江蘇恆瑞醫藥股份有限公司 一種含有雙環取代吡唑酮偶氮類衍生物或其鹽的藥物組成物及其製備方法
TWI762556B (zh) * 2017-01-19 2022-05-01 大陸商江蘇恆瑞醫藥股份有限公司 一種雙環取代吡唑酮偶氮類衍生物的製備方法及其中間體
CN110028497B (zh) * 2018-01-11 2020-11-17 江苏恒瑞医药股份有限公司 一种血小板生成素模拟物的乙醇胺盐的结晶形式及制备方法
CN113226463A (zh) * 2019-01-08 2021-08-06 江苏恒瑞医药股份有限公司 双环取代吡唑酮偶氮类衍生物的给药方案
CN112062699B (zh) * 2020-11-13 2021-02-26 苏州开元民生科技股份有限公司 一种邻氨基苯硫酚的制备方法
WO2022228551A1 (zh) * 2021-04-30 2022-11-03 江苏恒瑞医药股份有限公司 一种血小板生成素受体激动剂的给药方案
US20250144077A1 (en) * 2022-01-25 2025-05-08 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Dosage regimen for thrombopoietin receptor agonist
WO2025140275A1 (zh) * 2023-12-25 2025-07-03 江苏恒瑞医药股份有限公司 取代吡唑啉偶氮衍生物的磷酸酯化合物或其可药用盐

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WO2001089457A2 (en) * 2000-05-25 2001-11-29 Smithkline Beecham Corporation Thrombopoietin mimetics
WO2004096154A2 (en) * 2003-04-29 2004-11-11 Smithkline Beecham Corporation Methods for treating degenerative diseases/injuries
WO2007062078A2 (en) * 2005-11-23 2007-05-31 Ligand Pharmaceuticals Inc. Thrombopoietin activity modulating compounds and methods

Also Published As

Publication number Publication date
JP5441269B2 (ja) 2014-03-12
BRPI0907234B1 (pt) 2021-08-10
JP2011509263A (ja) 2011-03-24
PT2236500E (pt) 2015-04-07
RU2010127786A (ru) 2012-02-20
KR101556808B1 (ko) 2015-10-01
CA2711535C (en) 2015-12-15
BRPI0907234A2 (pt) 2020-08-04
KR20100120141A (ko) 2010-11-12
ES2533366T3 (es) 2015-04-09
CN101679286A (zh) 2010-03-24
US20100316601A1 (en) 2010-12-16
RU2488582C2 (ru) 2013-07-27
WO2009092276A1 (zh) 2009-07-30
EP2236500B1 (en) 2014-12-24
HK1134818A1 (en) 2010-05-14
AU2009207966A1 (en) 2009-07-30
MX2010007553A (es) 2010-10-04
EP2236500A1 (en) 2010-10-06
CA2711535A1 (en) 2009-07-30
CN101481352A (zh) 2009-07-15
EP2236500A4 (en) 2012-08-22
CN101679286B (zh) 2011-06-08
UA101172C2 (ru) 2013-03-11
US20130123507A1 (en) 2013-05-16
US8367710B2 (en) 2013-02-05
ZA201004794B (en) 2011-09-28

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