WO2009017098A1 - トロンボポエチン受容体アゴニスト作用を有する光学活性な化合物を含有する医薬組成物およびその中間体 - Google Patents

トロンボポエチン受容体アゴニスト作用を有する光学活性な化合物を含有する医薬組成物およびその中間体 Download PDF

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Publication number
WO2009017098A1
WO2009017098A1 PCT/JP2008/063541 JP2008063541W WO2009017098A1 WO 2009017098 A1 WO2009017098 A1 WO 2009017098A1 JP 2008063541 W JP2008063541 W JP 2008063541W WO 2009017098 A1 WO2009017098 A1 WO 2009017098A1
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WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
composition containing
optically active
receptor agonist
agonist activity
Prior art date
Application number
PCT/JP2008/063541
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English (en)
French (fr)
Inventor
Masami Takayama
Noriyuki Kurose
Original Assignee
Shionogi & 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
Priority to ES08791776.1T priority Critical patent/ES2528196T3/es
Priority to RU2010107169/04A priority patent/RU2476429C2/ru
Application filed by Shionogi & Co., Ltd. filed Critical Shionogi & Co., Ltd.
Priority to DK08791776.1T priority patent/DK2184279T3/en
Priority to SI200831361T priority patent/SI2184279T1/sl
Priority to CA2694567A priority patent/CA2694567C/en
Priority to JP2009525398A priority patent/JP5164181B2/ja
Priority to MX2010001082A priority patent/MX2010001082A/es
Priority to CN2008801104301A priority patent/CN101809008B/zh
Priority to AU2008283357A priority patent/AU2008283357B2/en
Priority to BRPI0814891-0A priority patent/BRPI0814891A2/pt
Priority to US12/671,476 priority patent/US8530668B2/en
Priority to PL08791776T priority patent/PL2184279T3/pl
Priority to EP08791776.1A priority patent/EP2184279B1/en
Publication of WO2009017098A1 publication Critical patent/WO2009017098A1/ja
Priority to US13/766,752 priority patent/US8889722B2/en
Priority to HRP20150062AT priority patent/HRP20150062T1/hr
Priority to NL300998C priority patent/NL300998I2/nl
Priority to FR19C1043C priority patent/FR19C1043I2/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
    • C07D277/38—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

　トロンボポエチン受容体アゴニスト作用を有する光学活性な４－フェニルチアゾール誘導体および該化合物を有効成分として含有する医薬組成物を創製し、経口投与可能な血小板産生調節剤を提供する。 　式： （式中、Ｒ１はハロゲン原子又はＣ１－Ｃ３アルキルオキシ；Ｒ２はＣ１－Ｃ８アルキル；Ｒ３はＣ１－Ｃ８アルキル；Ｒ４及びＲ５はそれぞれ独立して、フッ素原子又は塩素原子；Ｒ６はＣ１－Ｃ３アルキル又はＣ１－Ｃ３アルキルオキシ；＊は付された炭素原子が不斉炭素であることを示す）で示される光学活性な化合物、その製薬上許容される塩、又はそれらの溶媒和物を有効成分として含有する医薬組成物。
PCT/JP2008/063541 2007-07-31 2008-07-29 トロンボポエチン受容体アゴニスト作用を有する光学活性な化合物を含有する医薬組成物およびその中間体 WO2009017098A1 (ja)

Priority Applications (17)

Application Number Priority Date Filing Date Title
EP08791776.1A EP2184279B1 (en) 2007-07-31 2008-07-29 Pharmaceutical composition containing optically active compound having thrombopoietin receptor agonist activity and intermediate thereof
CN2008801104301A CN101809008B (zh) 2007-07-31 2008-07-29 含有具血小板生成素受体激动作用的光学活性化合物的药物组合物及其中间体
DK08791776.1T DK2184279T3 (en) 2007-07-31 2008-07-29 PHARMACEUTICAL PREPARATION CONTAINING AN OPTICAL ACTIVE RELATIONSHIP WITH THE TROMBOPOPIETY INRECEPTOR AGONIST ACTIVITY AND AN INTERMEDIATE PRODUCT THEREOF
SI200831361T SI2184279T1 (sl) 2007-07-31 2008-07-29 Farmacevtski sestavek, ki vsebuje optično aktivno spojino z aktivnostjo agonista receptorja trombopoetina in njene vmesne spojine
CA2694567A CA2694567C (en) 2007-07-31 2008-07-29 Pharmaceutical composition containing optically active compound having thrombopoietin receptor agonist activity and intermediate thereof
JP2009525398A JP5164181B2 (ja) 2007-07-31 2008-07-29 トロンボポエチン受容体アゴニスト作用を有する光学活性な化合物を含有する医薬組成物およびその中間体
MX2010001082A MX2010001082A (es) 2007-07-31 2008-07-29 Composicion farmaceutica que contiene compuesto opticamente activo que tiene actividad agonista del receptor de trombopoyetina y compuesto intermedio para el mismo.
ES08791776.1T ES2528196T3 (es) 2007-07-31 2008-07-29 Composición farmacéutica que contiene un compuesto ópticamente activo con actividad agonista del receptor de trombopoyetina, y compuesto intermedio para la misma
AU2008283357A AU2008283357B2 (en) 2007-07-31 2008-07-29 Pharmaceutical composition containing optically active compound having thrombopoietin receptor agonist activity and intermediate thereof
US12/671,476 US8530668B2 (en) 2007-07-31 2008-07-29 Pharmaceutical composition containing optically active compound having thrombopoietin receptor agonist activity, and intermediate therefor
BRPI0814891-0A BRPI0814891A2 (pt) 2007-07-31 2008-07-29 Composição farmacêutica contendo composto oticamente ativo tendo atividade agonista de receptor de trombopoietina, e intermediário do mesmo.
PL08791776T PL2184279T3 (pl) 2007-07-31 2008-07-29 Kompozycja farmaceutyczna zawierająca związek optycznie czynny mający aktywność agonisty receptora trombopoetyny i jego półprodukt
RU2010107169/04A RU2476429C2 (ru) 2007-07-31 2008-07-29 Фармацевтическая композиция, содержащая оптически активное соединение, обладающее активностью агониста рецептора тромбопоэтина, и промежуточное соединение для этого
US13/766,752 US8889722B2 (en) 2007-07-31 2013-02-13 Pharmaceutical composition containing optically active compound having thrombopoietin receptor agonist activity, and intermediate therefor
HRP20150062AT HRP20150062T1 (hr) 2007-07-31 2015-01-19 Farmaceutski pripravak koji sadrži optički aktivan spoj koji sadrži agonist receptora trombopoietina i njegov međuprodukt
NL300998C NL300998I2 (nl) 2007-07-31 2019-06-27 Lusutrombopag of farmaceutisch aanvaardbare zouten of solvaten daarvan
FR19C1043C FR19C1043I2 (fr) 2007-07-31 2019-06-28 Composition pharmaceutique contenant un compose actif sur le plan optique possedant une activite d'agoniste du recepteur de la thrombopoietine et son intermediaire

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007198590 2007-07-31
JP2007-198590 2007-07-31

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US12/671,476 A-371-Of-International US8530668B2 (en) 2007-07-31 2008-07-29 Pharmaceutical composition containing optically active compound having thrombopoietin receptor agonist activity, and intermediate therefor
US13/766,752 Division US8889722B2 (en) 2007-07-31 2013-02-13 Pharmaceutical composition containing optically active compound having thrombopoietin receptor agonist activity, and intermediate therefor

Publications (1)

Publication Number Publication Date
WO2009017098A1 true WO2009017098A1 (ja) 2009-02-05

Family

ID=40304328

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/063541 WO2009017098A1 (ja) 2007-07-31 2008-07-29 トロンボポエチン受容体アゴニスト作用を有する光学活性な化合物を含有する医薬組成物およびその中間体

Country Status (21)

Country Link
US (2) US8530668B2 (ja)
EP (1) EP2184279B1 (ja)
JP (1) JP5164181B2 (ja)
KR (1) KR20100027243A (ja)
CN (4) CN103450110B (ja)
AU (1) AU2008283357B2 (ja)
BR (1) BRPI0814891A2 (ja)
CA (1) CA2694567C (ja)
CY (1) CY1116190T1 (ja)
DK (1) DK2184279T3 (ja)
ES (1) ES2528196T3 (ja)
FR (1) FR19C1043I2 (ja)
HR (1) HRP20150062T1 (ja)
MX (1) MX2010001082A (ja)
NL (1) NL300998I2 (ja)
PL (1) PL2184279T3 (ja)
PT (1) PT2184279E (ja)
RU (1) RU2476429C2 (ja)
SI (1) SI2184279T1 (ja)
TW (1) TWI422371B (ja)
WO (1) WO2009017098A1 (ja)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012043709A1 (ja) 2010-09-30 2012-04-05 塩野義製薬株式会社 難溶性薬物の溶解性改善製剤
WO2015093586A1 (ja) * 2013-12-20 2015-06-25 塩野義製薬株式会社 トロンボポエチン受容体アゴニスト作用を有する光学活性な化合物およびその中間体の製造方法
JP2017145242A (ja) * 2016-02-12 2017-08-24 塩野義製薬株式会社 重度の肝機能障害のある患者のためのルストロンボパグを含有する血小板産生促進剤
WO2018045907A1 (zh) 2016-09-08 2018-03-15 四川科伦博泰生物医药股份有限公司 一种新型2-酰氨基噻唑衍生物及其制备方法与用途
US10085973B2 (en) 2012-06-29 2018-10-02 Shionogi & Co., Ltd. Pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity
WO2020116447A1 (ja) * 2018-12-04 2020-06-11 塩野義製薬株式会社 難溶性薬物の固体分散体
JP2021525230A (ja) * 2018-06-08 2021-09-24 シチュアン ケルン ファーマシューティカル リサーチ インスティテュート カンパニー リミテッド ４−フェニルチアゾール誘導体の結晶形およびその調製方法

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US20140047572A1 (en) * 2012-08-13 2014-02-13 University Of Rochester Thrombopoietin mimetics for the treatment of radiation or chemical induced bone marrow injury
CN105412930A (zh) * 2015-08-07 2016-03-23 军事医学科学院华南干细胞与再生医学研究中心 血小板生成素受体激动剂在促进造血干细胞归巢中的用途
CN106083759B (zh) * 2016-06-15 2022-02-15 上海丸全化学科技有限公司 一种芦曲泊帕的全新合成工艺
CN106565625B (zh) * 2016-11-04 2018-01-30 杭州励德生物科技有限公司 一种抗血小板减少症新药Lusutrombopag中间体的制备方法
CN109311831B (zh) * 2017-02-14 2021-07-09 四川科伦药物研究院有限公司 4-苯基噻唑衍生物的晶型及其制备方法
CN109970678B (zh) * 2017-12-28 2024-03-08 四川科伦药物研究院有限公司 4-苯基噻唑衍生物无定形及其制备方法和用途

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KR101849808B1 (ko) 2010-09-30 2018-04-17 시오노기세이야쿠가부시키가이샤 난용성 약물의 용해성 개선 제제
US20130203723A1 (en) * 2010-09-30 2013-08-08 Satoshi Sakuma Preparation for Improving Solubility of Poorly Soluble Drug
JP5557146B2 (ja) * 2010-09-30 2014-07-23 塩野義製薬株式会社 難溶性薬物の溶解性改善製剤
JP2014141518A (ja) * 2010-09-30 2014-08-07 Shionogi & Co Ltd 難溶性薬物の溶解性改善製剤
EP2623100B1 (en) * 2010-09-30 2023-07-05 Shionogi & Co., Ltd. Preparation for improving solubility of poorly soluble drug
US9427402B2 (en) * 2010-09-30 2016-08-30 Shionogi & Co. Ltd. Preparation for improving solubility of poorly soluble drug
WO2012043709A1 (ja) 2010-09-30 2012-04-05 塩野義製薬株式会社 難溶性薬物の溶解性改善製剤
US10085973B2 (en) 2012-06-29 2018-10-02 Shionogi & Co., Ltd. Pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity
CN105992761A (zh) * 2013-12-20 2016-10-05 盐野义制药株式会社 具有血小板生成素受体激动作用的光学活性的化合物及其中间体的制备方法
JPWO2015093586A1 (ja) * 2013-12-20 2017-03-23 塩野義製薬株式会社 トロンボポエチン受容体アゴニスト作用を有する光学活性な化合物およびその中間体の製造方法
WO2015093586A1 (ja) * 2013-12-20 2015-06-25 塩野義製薬株式会社 トロンボポエチン受容体アゴニスト作用を有する光学活性な化合物およびその中間体の製造方法
JP2017145242A (ja) * 2016-02-12 2017-08-24 塩野義製薬株式会社 重度の肝機能障害のある患者のためのルストロンボパグを含有する血小板産生促進剤
WO2018045907A1 (zh) 2016-09-08 2018-03-15 四川科伦博泰生物医药股份有限公司 一种新型2-酰氨基噻唑衍生物及其制备方法与用途
JP2021525230A (ja) * 2018-06-08 2021-09-24 シチュアン ケルン ファーマシューティカル リサーチ インスティテュート カンパニー リミテッド ４−フェニルチアゾール誘導体の結晶形およびその調製方法
WO2020116447A1 (ja) * 2018-12-04 2020-06-11 塩野義製薬株式会社 難溶性薬物の固体分散体

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CN101809008A (zh) 2010-08-18
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