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WO2011022596A3 - Preparation of bazedoxifene and its salts - Google Patents

Preparation of bazedoxifene and its salts Download PDF

Info

Publication number
WO2011022596A3
WO2011022596A3 PCT/US2010/046091 US2010046091W WO2011022596A3 WO 2011022596 A3 WO2011022596 A3 WO 2011022596A3 US 2010046091 W US2010046091 W US 2010046091W WO 2011022596 A3 WO2011022596 A3 WO 2011022596A3
Authority
WO
WIPO (PCT)
Prior art keywords
bazedoxifene
salts
preparation
processes
pharmaceutically acceptable
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2010/046091
Other languages
French (fr)
Other versions
WO2011022596A2 (en
Inventor
Rakeshwar Bandichhor
Amarnath Reddy Lekkala
Pranab Haldar
Ravi Kumar Mylavarapu
China Malakondaiah Golla
Raghunath Vagwala
Vijaya Kumar Karri
Swapna Akula
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Dr Reddys Laboratories Ltd
Dr Reddys Laboratories Inc
Original Assignee
Dr Reddys Laboratories Ltd
Dr Reddys Laboratories Inc
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 Dr Reddys Laboratories Ltd, Dr Reddys Laboratories Inc filed Critical Dr Reddys Laboratories Ltd
Publication of WO2011022596A2 publication Critical patent/WO2011022596A2/en
Publication of WO2011022596A3 publication Critical patent/WO2011022596A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Processes for preparing bazedoxifene and its pharmaceutically acceptable salts, substantially free from process related impurities and process intermediates.
PCT/US2010/046091 2009-08-21 2010-08-20 Preparation of bazedoxifene and its salts Ceased WO2011022596A2 (en)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
IN1996/CHE/2009 2009-08-21
IN1996CH2009 2009-08-21
US30534410P 2010-02-17 2010-02-17
US61/305,344 2010-02-17
IN1362CH2010 2010-05-14
IN1362/CHE/2010 2010-05-14
US36080510P 2010-07-01 2010-07-01
US61/360,805 2010-07-01

Publications (2)

Publication Number Publication Date
WO2011022596A2 WO2011022596A2 (en) 2011-02-24
WO2011022596A3 true WO2011022596A3 (en) 2011-07-28

Family

ID=43607597

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/046091 Ceased WO2011022596A2 (en) 2009-08-21 2010-08-20 Preparation of bazedoxifene and its salts

Country Status (1)

Country Link
WO (1) WO2011022596A2 (en)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012007453A1 (en) * 2010-07-14 2012-01-19 Sandoz Ag Crystalline compound of 1-[4-(2-azepan-1-ylethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol
US8569483B2 (en) 2011-06-21 2013-10-29 Divi's Laboratories, Ltd. Process for the preparation of bazedoxifene acetate and intermediates thereof
WO2013001511A1 (en) 2011-06-30 2013-01-03 Sandoz Ag Novel salt intermediates for the synthesis of bazedoxifene acetate and process thereof
CN102690225B (en) * 2012-04-11 2014-12-24 南京友杰医药科技有限公司 New synthetic method of bazedoxifene
CN104151265B (en) * 2013-05-13 2016-10-05 上海医药工业研究院 The preparation method of bazedoxifene acetate intermediate
WO2014186325A1 (en) 2013-05-15 2014-11-20 Indiana University Research And Technology Corporation Processes and intermediates for preparing indole pharmaceuticals
CN103739540B (en) * 2014-01-20 2016-05-04 华润赛科药业有限责任公司 A kind of preparation method of bazedoxifene acetate intermediate
CN103772261B (en) * 2014-03-04 2015-02-18 苏州立新制药有限公司 Preparation method of bazedoxifene
CN103864665B (en) * 2014-03-04 2016-03-02 苏州特瑞药业有限公司 The preparation method of bazedoxifene acetate
CN105085365B (en) * 2014-05-12 2018-06-19 四川科伦药业股份有限公司 The preparation method of bazedoxifene acetate and its intermediate
CN104311468A (en) * 2014-09-24 2015-01-28 万特制药(海南)有限公司 Bazedoxifene impurity synthesis method
CN104370796B (en) * 2014-11-21 2016-09-14 扬子江药业集团有限公司 A kind of preparation method of bazedoxifene acetate polymorph b
CN104569202B (en) * 2015-01-05 2020-07-07 万特制药(海南)有限公司 A kind of method for separating and measuring bazedoxifene acetate and related substances
KR101806782B1 (en) 2015-09-07 2018-01-10 주식회사 경보제약 Method for the preparation of high purity Bazedoxifene Acetate
CN106810487B (en) * 2015-11-27 2020-03-17 四川科伦药物研究院有限公司 Efficient preparation method of bazedoxifene
CN107033062B (en) * 2017-03-24 2019-10-29 梯尔希（南京）药物研发有限公司 A kind of preparation method of Bazedoxifene derivative
IT201900001923A1 (en) 2019-02-11 2020-08-11 Erregierre Spa BAZEDOXIFENE SALTS USEFUL FOR THE PREPARATION OF BAZEDOXIFENE ACETATE

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6479535B1 (en) * 1998-05-15 2002-11-12 Wyeth 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations
WO2009012734A2 (en) * 2007-07-25 2009-01-29 Zentiva A.S. New salts of bazedoxifene

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6479535B1 (en) * 1998-05-15 2002-11-12 Wyeth 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations
WO2009012734A2 (en) * 2007-07-25 2009-01-29 Zentiva A.S. New salts of bazedoxifene

Also Published As

Publication number Publication date
WO2011022596A2 (en) 2011-02-24

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