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WO2018193090A3 - Process for preparation of eliglustat hemitartrate and intermediates thereof - Google Patents

Process for preparation of eliglustat hemitartrate and intermediates thereof Download PDF

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Publication number
WO2018193090A3
WO2018193090A3 PCT/EP2018/060185 EP2018060185W WO2018193090A3 WO 2018193090 A3 WO2018193090 A3 WO 2018193090A3 EP 2018060185 W EP2018060185 W EP 2018060185W WO 2018193090 A3 WO2018193090 A3 WO 2018193090A3
Authority
WO
WIPO (PCT)
Prior art keywords
intermediates
preparation
eliglustat hemitartrate
eliglustat
hemitartrate
Prior art date
Application number
PCT/EP2018/060185
Other languages
French (fr)
Other versions
WO2018193090A2 (en
Inventor
Kanaram Hanumanprasad KUMAWAT
Brijesh Rajendrakumar PATEL
Nilesh Mansukhlal Thumar
Joseph Prabahar UPADHYAY
Joseph Prabahar Koilpillai
Virendrakumar Agarwal
Parva Yogeshchandra Purohit
Arif Badrulhusan Siddiqui
Krushnakant Natvarbhai PATEL
Vipul Veljibhai GONDALIYA
Ankit Ramjibhai BUHA
Original Assignee
Amneal Pharmaceuticals Company Gmbh
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 Amneal Pharmaceuticals Company Gmbh filed Critical Amneal Pharmaceuticals Company Gmbh
Publication of WO2018193090A2 publication Critical patent/WO2018193090A2/en
Publication of WO2018193090A3 publication Critical patent/WO2018193090A3/en

Links

Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Process for preparation of eliglustat hemitartrate and intermediates thereof Processes for preparation of eliglustat hemitartrate and intermediates thereof are provided. A stable amorphous form of eliglustat hemitartrate pharmaceutical compositions including the amorphous form of eliglustat hemitartrate, and their uses are also provided.
PCT/EP2018/060185 2017-04-21 2018-04-20 Process for preparation of eliglustat hemitartrate and intermediates thereof WO2018193090A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN201721014151 2017-04-21
IN201721014151 2018-03-05

Publications (2)

Publication Number Publication Date
WO2018193090A2 WO2018193090A2 (en) 2018-10-25
WO2018193090A3 true WO2018193090A3 (en) 2019-01-03

Family

ID=62111029

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2018/060185 WO2018193090A2 (en) 2017-04-21 2018-04-20 Process for preparation of eliglustat hemitartrate and intermediates thereof

Country Status (1)

Country Link
WO (1) WO2018193090A2 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ625712A (en) 2009-11-27 2016-02-26 Genzyme Corp An amorphous and a crystalline form of genz 112638 hemitartrate as inhibitor of glucosylceramide synthase
CN110759885B (en) * 2018-07-27 2021-10-22 中国医学科学院药物研究所 Method for preparing photoactive igloot
CN110878079A (en) * 2018-12-31 2020-03-13 北京启慧生物医药有限公司 Preparation method of high-purity eliagliptat
EP3941917A4 (en) * 2019-03-22 2022-12-21 Piramal Pharma Limited An improved process for the preparation of eliglustat and its intermediate
CN116120274A (en) * 2021-11-12 2023-05-16 曙方(上海)医药科技有限公司 Eliglustat pharmaceutically acceptable salt and its crystal form

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004101558A1 (en) * 2003-05-13 2004-11-25 F. Hoffmann-La Roche Ag 2-imidazo-benzothiazoles as adenosine receptor ligands
US7615753B2 (en) * 2003-12-30 2009-11-10 Commissariat A L'energie Atomique Radiation detecting system with double resetting pulse count
WO2011066352A1 (en) * 2009-11-27 2011-06-03 Genzyme Corporation An amorphous and a crystalline form of genz 112638 hemitartrat as inhibitor of glucosylceramide synthase

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0211379B8 (en) 2001-07-16 2021-05-25 Genzyme Corp synthesis of udp-glucose inhibitors: n-acyl-sphingosine glycosyltransferase
US6916802B2 (en) 2002-04-29 2005-07-12 Genzyme Corporation Amino ceramide-like compounds and therapeutic methods of use
WO2016001885A2 (en) 2014-07-03 2016-01-07 Dr. Reddy’S Laboratories Limited Amorphous form of eliglustat hemitartarate
CN105646442A (en) 2015-10-27 2016-06-08 北京凯莱天成医药科技有限公司 Preparation method of eliglustat

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004101558A1 (en) * 2003-05-13 2004-11-25 F. Hoffmann-La Roche Ag 2-imidazo-benzothiazoles as adenosine receptor ligands
US7615753B2 (en) * 2003-12-30 2009-11-10 Commissariat A L'energie Atomique Radiation detecting system with double resetting pulse count
WO2011066352A1 (en) * 2009-11-27 2011-06-03 Genzyme Corporation An amorphous and a crystalline form of genz 112638 hemitartrat as inhibitor of glucosylceramide synthase

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"/1 -(C) FILE REGISTRY RN -2138286-91-4 REGISTRY ED -Entered STN: 02 Nov 2017 CN -Octanamide, N-[2-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-oxo-1-(1- pyrrolidinylmethyl)ethyl]-(CA INDEX NAME) MF -C23 H34 N2 O4 SR -Chemical Catalog Supplier: Enamine LLC LC -STN Files: CHEMCATS", 2 November 2017, article CHEMICAL ABSTRACTS OHIO: "/1 -(C) FILE REGISTRY RN -2138286-91-4 REGISTRY ED -Entered STN: 02 Nov 2017 CN -Octanamide, N-[2-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-oxo-1-(1- pyrrolidinylmethyl)ethyl]-(CA INDEX NAME) MF -C23 H34 N2 O4 SR -Chemical Catalog Supplier: Enamine LLC LC -STN Files: CHEMCATS", XP055491732 *

Also Published As

Publication number Publication date
WO2018193090A2 (en) 2018-10-25

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