JP2013512252A - グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩 - Google Patents

グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩 Download PDF

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JP2013512252A
JP2013512252A JP2012541183A JP2012541183A JP2013512252A JP 2013512252 A JP2013512252 A JP 2013512252A JP 2012541183 A JP2012541183 A JP 2012541183A JP 2012541183 A JP2012541183 A JP 2012541183A JP 2013512252 A JP2013512252 A JP 2013512252A
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patient
hemi
tartrate
formula
salt
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JP2013512252A5 (enExample
Inventor
リウ，ハンラン
ウィリス，クリス
バルトワジ，レヌー
コープランド，ダイアン・ピー
ハリアナワラ，アビザー
スケル，ジェフリー
マーシャル，ジョン
コクリング，ジャンメイ
パレス，ジェラード
ピーターシュミット，ジュディス
シーゲル，クレイグ
チェン，セン
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Genzyme Corp
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Genzyme Corp
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Application filed by Genzyme Corp filed Critical Genzyme Corp
Publication of JP2013512252A publication Critical patent/JP2013512252A/ja
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    • 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
    • C07D405/06—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 only aliphatic carbon atoms
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Steroid Compounds (AREA)
  • Molecular Biology (AREA)
JP2012541183A 2009-11-27 2010-11-24 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩 Pending JP2013512252A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US26474809P 2009-11-27 2009-11-27
US61/264,748 2009-11-27
PCT/US2010/057952 WO2011066352A1 (en) 2009-11-27 2010-11-24 An amorphous and a crystalline form of genz 112638 hemitartrat as inhibitor of glucosylceramide synthase

Related Child Applications (2)

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JP2015134942A Division JP6370264B2 (ja) 2009-11-27 2015-07-06 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2016041843A Division JP6452635B2 (ja) 2009-11-27 2016-03-04 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩

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JP2013512252A true JP2013512252A (ja) 2013-04-11
JP2013512252A5 JP2013512252A5 (enExample) 2014-01-16

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JP2012541183A Pending JP2013512252A (ja) 2009-11-27 2010-11-24 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2015134942A Active JP6370264B2 (ja) 2009-11-27 2015-07-06 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2016041843A Active JP6452635B2 (ja) 2009-11-27 2016-03-04 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2018167432A Active JP7150528B2 (ja) 2009-11-27 2018-09-07 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2020136889A Pending JP2020189873A (ja) 2009-11-27 2020-08-14 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2023101301A Pending JP2023116764A (ja) 2009-11-27 2023-06-21 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩

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JP2015134942A Active JP6370264B2 (ja) 2009-11-27 2015-07-06 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2016041843A Active JP6452635B2 (ja) 2009-11-27 2016-03-04 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2018167432A Active JP7150528B2 (ja) 2009-11-27 2018-09-07 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2020136889A Pending JP2020189873A (ja) 2009-11-27 2020-08-14 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩
JP2023101301A Pending JP2023116764A (ja) 2009-11-27 2023-06-21 グルコシルセラミドシンターゼの阻害剤としての非晶質及び結晶型のｇｅｎｚ１１２６３８ヘミ酒石酸塩

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AR (3) AR079152A1 (enExample)
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DK (3) DK3133070T3 (enExample)
DO (2) DOP2012000141A (enExample)
EA (3) EA201890254A3 (enExample)
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TN (1) TN2012000237A1 (enExample)
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JP2024525229A (ja) * 2021-07-05 2024-07-10 エースニューロン・ソシエテ・アノニム グリコシダーゼインヒビターを含む医薬
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CN107445938B (zh) * 2016-05-31 2020-04-03 北京启慧生物医药有限公司 依利格鲁司他半酒石酸盐的结晶形式、制备方法和含有所述结晶形式的药用组合物
CN106349210A (zh) * 2016-08-24 2017-01-25 北京阳光诺和药物研究有限公司 一种制备酒石酸艾力骨司坦的方法
EP3318277A1 (en) 2016-11-04 2018-05-09 Institut du Cerveau et de la Moelle Epiniere-ICM Inhibitors of glucosylceramide synthase for the treatment of motor neuron diseases
WO2018193090A2 (en) 2017-04-21 2018-10-25 Amneal Pharmaceuticals Company Gmbh Process for preparation of eliglustat hemitartrate and intermediates thereof
WO2018225085A1 (en) 2017-06-05 2018-12-13 Cipla Limited Stable solid dispersions of eliglustat hemitartrate
AU2018283289B2 (en) * 2017-06-16 2021-03-25 Beta Pharma, Inc. Pharmaceutical formulations of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and salts thereof
EP3664798B1 (en) 2017-08-08 2025-10-29 Amneal Pharmaceuticals LLC Pharmaceutical composition comprising eliglustat
US12472144B2 (en) * 2017-08-08 2025-11-18 Amneal Pharmaceuticals Llc Pharmaceutical composition comprising eliglustat
BR112020011056A2 (pt) * 2017-12-15 2020-11-17 Genzyme Corporation métodos para o tratamento da doença de gaucher
WO2019123476A1 (en) * 2017-12-20 2019-06-27 Sarudbhava Formulations Private Limited Stable amorphous eliglustat premix and process for the preparation thereof
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CN110878079A (zh) * 2018-12-31 2020-03-13 北京启慧生物医药有限公司 一种高纯度依利格鲁司他的制备方法
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