CN101481352A - 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 - Google Patents

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 Download PDF

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Publication number
CN101481352A
CN101481352A CNA2008100003466A CN200810000346A CN101481352A CN 101481352 A CN101481352 A CN 101481352A CN A2008100003466 A CNA2008100003466 A CN A2008100003466A CN 200810000346 A CN200810000346 A CN 200810000346A CN 101481352 A CN101481352 A CN 101481352A
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CN
China
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compound
hydroxyl
alkyl
general formula
carboxylic acid
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Pending
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CNA2008100003466A
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English (en)
Chinese (zh)
Inventor
邓炳初
吕贺军
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Shanghai Hengrui Pharmaceutical Co Ltd
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Shanghai Hengrui Pharmaceutical Co Ltd
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Application filed by Shanghai Hengrui Pharmaceutical Co Ltd filed Critical Shanghai Hengrui Pharmaceutical Co Ltd
Priority to CNA2008100003466A priority Critical patent/CN101481352A/zh
Priority to KR1020107017630A priority patent/KR101556808B1/ko
Priority to UAA201008616A priority patent/UA101172C2/ru
Priority to BRPI0907234-9A priority patent/BRPI0907234B1/pt
Priority to PCT/CN2009/000001 priority patent/WO2009092276A1/zh
Priority to AU2009207966A priority patent/AU2009207966B2/en
Priority to MX2010007553A priority patent/MX2010007553A/es
Priority to CN2009800001980A priority patent/CN101679286B/zh
Priority to JP2010541680A priority patent/JP5441269B2/ja
Priority to RU2010127786/04A priority patent/RU2488582C2/ru
Priority to PT97034904T priority patent/PT2236500E/pt
Priority to EP09703490.4A priority patent/EP2236500B1/en
Priority to US12/812,119 priority patent/US8367710B2/en
Priority to HK10102994.0A priority patent/HK1134818B/xx
Priority to ES09703490.4T priority patent/ES2533366T3/es
Priority to CA2711535A priority patent/CA2711535C/en
Publication of CN101481352A publication Critical patent/CN101481352A/zh
Priority to ZA2010/04794A priority patent/ZA201004794B/en
Priority to US13/742,633 priority patent/US20130123507A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic 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
    • C07D231/08—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/14—Heterocyclic 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
    • C07D231/18—One oxygen or sulfur atom
    • C07D231/20—One oxygen atom attached in position 3 or 5
    • C07D231/22—One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/14—Heterocyclic 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
    • C07D231/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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)
CNA2008100003466A 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 Pending CN101481352A (zh)

Priority Applications (18)

Application Number Priority Date Filing Date Title
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
RU2010127786/04A RU2488582C2 (ru) 2008-01-10 2009-01-04 Бициклозамещенные азопроизводные пиразолона, способ их получения и фармацевтическое применение
PT97034904T PT2236500E (pt) 2008-01-10 2009-01-04 Derivados azo de pirazolona substituída com biciclo, processo para a sua preparação e a sua utilização farmacêutica
BRPI0907234-9A BRPI0907234B1 (pt) 2008-01-10 2009-01-04 Derivados de pirazolona-azo biciclo-substituído, seu uso, seu intermediário e seus processos de preparação, composição farmacêutica e deu uso
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
AU2009207966A AU2009207966B2 (en) 2008-01-10 2009-01-04 Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof
MX2010007553A MX2010007553A (es) 2008-01-10 2009-01-04 Derivados de azopirazolona biciclo-sustituidos, procedimiento de preparacion y uso farmaceutico de los mismos.
CN2009800001980A CN101679286B (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
JP2010541680A JP5441269B2 (ja) 2008-01-10 2009-01-04 ビシクロ置換ピラゾロン−アゾ誘導体、その調製プロセス及び製薬学的使用
KR1020107017630A KR101556808B1 (ko) 2008-01-10 2009-01-04 비씨클로-치환된 피라졸론 아조 유도체, 그 제조 방법 및 약학적 용도
UAA201008616A UA101172C2 (ru) 2008-01-10 2009-01-04 Бициклозамещенные пиразолоназопроизводные, способ их получения и фармацевтическое применение
EP09703490.4A EP2236500B1 (en) 2008-01-10 2009-01-04 Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof
US12/812,119 US8367710B2 (en) 2008-01-10 2009-01-04 Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof
HK10102994.0A HK1134818B (en) 2008-01-10 2009-01-04 Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof
ES09703490.4T ES2533366T3 (es) 2008-01-10 2009-01-04 Derivados azoicos de pirazolona biciclo-sustituidos, procedimiento de preparacion y utilización farmacéutica de los mismos
CA2711535A CA2711535C (en) 2008-01-10 2009-01-04 Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof
ZA2010/04794A ZA201004794B (en) 2008-01-10 2010-07-07 Bicyclo-substituted pyrazolon azo derivatives,preparation process and pharmaceutical use thereof
US13/742,633 US20130123507A1 (en) 2008-01-10 2013-01-16 Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
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

Publications (1)

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CN101481352A true CN101481352A (zh) 2009-07-15

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CNA2008100003466A Pending 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
CN2009800001980A Active CN101679286B (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

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CN2009800001980A Active CN101679286B (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

Country Status (15)

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

Cited By (9)

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WO2010142137A1 (zh) * 2009-06-11 2010-12-16 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盐,及其制备方法和应用
WO2013152683A1 (zh) * 2012-04-11 2013-10-17 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
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
WO2018133818A1 (zh) * 2017-01-19 2018-07-26 江苏恒瑞医药股份有限公司 一种双环取代吡唑酮偶氮类衍生物的制备方法及其中间体
CN110028497A (zh) * 2018-01-11 2019-07-19 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
WO2020143593A1 (zh) * 2019-01-08 2020-07-16 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
CN112062699A (zh) * 2020-11-13 2020-12-11 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
CN112220766A (zh) * 2016-01-22 2021-01-15 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
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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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
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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
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
WO2023143364A1 (zh) * 2022-01-25 2023-08-03 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
CN120383561A (zh) * 2025-03-26 2025-07-29 浙江本立科技股份有限公司 一种三氯甲基喹啉和2-取代乙酸联产喹啉酰氯和2-取代乙酰氯的方法

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CN102159217A (zh) * 2009-06-11 2011-08-17 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盐,及其制备方法和应用
CN102159217B (zh) * 2009-06-11 2012-10-03 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盐,及其制备方法和应用
US8642637B2 (en) 2009-06-11 2014-02-04 Jiangsu Hengrui Medicine Co., Ltd. Salts of bicyclo-substituted pyrazolon azo derivatives, preparation method and use thereof
US9120762B2 (en) 2009-06-11 2015-09-01 Jiangsu Hengrui Medicine Co., Ltd. Salts of bicyclo-substituted pyrazolon azo derivatives, preparation method and use thereof
WO2013152683A1 (zh) * 2012-04-11 2013-10-17 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
CN103360317A (zh) * 2012-04-11 2013-10-23 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
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
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
CN112220766A (zh) * 2016-01-22 2021-01-15 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
CN112220766B (zh) * 2016-01-22 2023-08-11 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
CN108884052A (zh) * 2017-01-19 2018-11-23 江苏恒瑞医药股份有限公司 一种双环取代吡唑酮偶氮类衍生物的制备方法及其中间体
WO2018133818A1 (zh) * 2017-01-19 2018-07-26 江苏恒瑞医药股份有限公司 一种双环取代吡唑酮偶氮类衍生物的制备方法及其中间体
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
CN108884052B (zh) * 2017-01-19 2025-07-11 江苏恒瑞医药股份有限公司 一种双环取代吡唑酮偶氮类衍生物的制备方法及其中间体
CN110028497A (zh) * 2018-01-11 2019-07-19 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
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
WO2020143593A1 (zh) * 2019-01-08 2020-07-16 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
CN112062699A (zh) * 2020-11-13 2020-12-11 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
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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US20100316601A1 (en) 2010-12-16
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