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WO2011029088A3 - Preparation of raloxifene and its salts - Google Patents

Preparation of raloxifene and its salts Download PDF

Info

Publication number
WO2011029088A3
WO2011029088A3 PCT/US2010/047966 US2010047966W WO2011029088A3 WO 2011029088 A3 WO2011029088 A3 WO 2011029088A3 US 2010047966 W US2010047966 W US 2010047966W WO 2011029088 A3 WO2011029088 A3 WO 2011029088A3
Authority
WO
WIPO (PCT)
Prior art keywords
salts
preparation
raloxifene
methylsulfonyloxy
piperidinyl
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/US2010/047966
Other languages
French (fr)
Other versions
WO2011029088A2 (en
Inventor
Mohanty Sandeep
Prashanth Reddy Gaddameedhi
Gunti Murali Mohan
Kesava Reddy
Pavan Kumar Bathini
Venkateswara Reddy Kommareddy
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 WO2011029088A2 publication Critical patent/WO2011029088A2/en
Publication of WO2011029088A3 publication Critical patent/WO2011029088A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61P5/32—Antioestrogens

Landscapes

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

Abstract

The invention provides processes for the preparation of pure raloxifene or its salts, involving hydrolyzing 6-methylsulfonyloxy-2-[(4-methylsulfonyloxy)-phenyl]-3-[4(2-(piperidinyl)ethoxy)benzoyl]benzothiophene hydrochloride, using an aqueous base.
PCT/US2010/047966 2009-09-07 2010-09-07 Preparation of raloxifene and its salts Ceased WO2011029088A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN2163CH2009 2009-09-07
IN2163/CHE/2009 2009-09-07
US31098710P 2010-03-05 2010-03-05
US61/310,987 2010-03-05

Publications (2)

Publication Number Publication Date
WO2011029088A2 WO2011029088A2 (en) 2011-03-10
WO2011029088A3 true WO2011029088A3 (en) 2011-11-24

Family

ID=43650002

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/047966 Ceased WO2011029088A2 (en) 2009-09-07 2010-09-07 Preparation of raloxifene and its salts

Country Status (1)

Country Link
WO (1) WO2011029088A2 (en)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6723739B1 (en) * 1994-05-20 2004-04-20 Eli Lilly And Company Glucopyranoside benzothiophenes
US6756388B1 (en) * 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
WO2009008000A2 (en) * 2007-04-12 2009-01-15 Sun Pharmaceutical Industries Ltd. A process for the preparation of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidino ethoxy) benzoyl]benzo[b]thiophene

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6756388B1 (en) * 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
US6723739B1 (en) * 1994-05-20 2004-04-20 Eli Lilly And Company Glucopyranoside benzothiophenes
WO2009008000A2 (en) * 2007-04-12 2009-01-15 Sun Pharmaceutical Industries Ltd. A process for the preparation of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidino ethoxy) benzoyl]benzo[b]thiophene

Also Published As

Publication number Publication date
WO2011029088A2 (en) 2011-03-10

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