AU2005233114A1 - Crystalline polymorph of bazedoxifene acetate - Google Patents

Crystalline polymorph of bazedoxifene acetate Download PDF

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Publication number
AU2005233114A1
AU2005233114A1 AU2005233114A AU2005233114A AU2005233114A1 AU 2005233114 A1 AU2005233114 A1 AU 2005233114A1 AU 2005233114 A AU2005233114 A AU 2005233114A AU 2005233114 A AU2005233114 A AU 2005233114A AU 2005233114 A1 AU2005233114 A1 AU 2005233114A1
Authority
AU
Australia
Prior art keywords
polymorph
composition
bazedoxifene acetate
mixture
weight
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.)
Withdrawn
Application number
AU2005233114A
Other languages
English (en)
Inventor
Kadum A. Ali
Pietro Allegrini
Aldo Belli
Roberto Brescello
Vincenzo Cannata
Malama K. Chibwe
Livius Cotarca
Shridhar G. Gangolli
Carl E. Longfellow
Giorgio Soriato
Massimo Verzini
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.)
Wyeth LLC
Original Assignee
Wyeth LLC
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34965585&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2005233114(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth LLC filed Critical Wyeth LLC
Publication of AU2005233114A1 publication Critical patent/AU2005233114A1/en
Withdrawn legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12Radicals substituted by oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2005233114A 2004-04-07 2005-04-06 Crystalline polymorph of bazedoxifene acetate Withdrawn AU2005233114A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US56058404P 2004-04-07 2004-04-07
US60/560,584 2004-04-07
PCT/US2005/011423 WO2005100314A1 (en) 2004-04-07 2005-04-06 Crystalline polymorph of bazedoxifene acetate

Publications (1)

Publication Number Publication Date
AU2005233114A1 true AU2005233114A1 (en) 2005-10-27

Family

ID=34965585

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2005233114A Withdrawn AU2005233114A1 (en) 2004-04-07 2005-04-06 Crystalline polymorph of bazedoxifene acetate

Country Status (20)

Country Link
US (1) US7683052B2 (https=)
EP (1) EP1732889A1 (https=)
JP (2) JP2007532548A (https=)
KR (1) KR20070004815A (https=)
CN (1) CN1938271A (https=)
AR (1) AR048683A1 (https=)
AU (1) AU2005233114A1 (https=)
BR (1) BRPI0509257A (https=)
CA (1) CA2561296A1 (https=)
EC (1) ECSP066910A (https=)
GT (1) GT200500080A (https=)
IL (1) IL178101A0 (https=)
NO (1) NO20065046L (https=)
PA (1) PA8629201A1 (https=)
PE (1) PE20060173A1 (https=)
RU (1) RU2006132352A (https=)
TW (1) TW200536845A (https=)
UA (1) UA86055C2 (https=)
WO (1) WO2005100314A1 (https=)
ZA (1) ZA200608361B (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20070188A1 (es) * 2005-06-29 2007-03-16 Wyeth Corp Formulaciones de estrogenos conjugados y bazedoxifeno
AU2006283121A1 (en) * 2005-08-24 2007-03-01 Wyeth Bazedoxifene acetate formulations and manufacturing process thereof
PE20090100A1 (es) * 2007-03-30 2009-02-26 Wyeth Corp Metodos de separacion y deteccion de acetato de bacedoxifeno en composiciones farmaceuticas
CZ302358B6 (cs) * 2007-07-25 2011-03-30 Zentiva, A. S. Nové soli bazedoxifenu
CN101977897A (zh) * 2008-02-11 2011-02-16 惠氏有限责任公司 制备乙酸巴多昔芬的多晶型a的方法
WO2009102778A1 (en) * 2008-02-11 2009-08-20 Wyeth Amorphous polymorph of bazedoxifene acetate
ITMI20091109A1 (it) * 2009-06-23 2010-12-24 Wyeth Corp Forma polimorfa d di bazedoxifene acetato e metodi per la sua preparazione
AR078785A1 (es) 2009-10-27 2011-11-30 Wyeth Llc Formulaciones de bazedoxifeno con antioxidantes
EP2407467A1 (de) 2010-07-14 2012-01-18 Sandoz Ag Kristalline Verbindung von 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol und Milchsäure
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
EP2616463A4 (en) 2010-09-14 2014-01-08 Reddys Lab Ltd Dr PREPARATION OF CRYSTALLINE BAZEDOXIFES AND THEIR SALTS
EP2471770A1 (en) 2010-12-28 2012-07-04 Sandoz Ag Method of preparing polymorphic pure form A of bazedoxifene acetate
CN103864664A (zh) * 2012-12-18 2014-06-18 江苏柯菲平医药有限公司 巴多昔芬乙酸盐新晶型及其制备方法
US9751835B2 (en) 2013-05-15 2017-09-05 Indiana University Research And Technology Corporation Processes and intermediates for preparing indole pharmaceuticals
CN103864665B (zh) * 2014-03-04 2016-03-02 苏州特瑞药业有限公司 醋酸巴多昔芬的制备方法
CN104030963A (zh) * 2014-06-30 2014-09-10 四川大学 一种巴多昔芬醋酸盐晶型a的制备方法
CN111004165A (zh) * 2019-12-03 2020-04-14 南京正济医药研究有限公司 一种醋酸巴多昔芬晶型a的制备方法
US11246874B1 (en) 2021-04-20 2022-02-15 Oxygen Biotech LLC Treatment of COVID-19

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5880137A (en) 1996-04-19 1999-03-09 American Home Products Corporation 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents
DE69707189T2 (de) 1996-04-19 2002-06-20 American Home Products Corp., Madison Östrogene Verbindungen
TW397821B (en) 1996-04-19 2000-07-11 American Home Produits Corp 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof
US5780497A (en) 1996-04-19 1998-07-14 American Home Products Corporation 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents
US5998402A (en) 1996-04-19 1999-12-07 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
NZ503793A (en) * 1997-10-15 2002-10-25 Wyeth Corp Novel aryloxy-alkyl-dialkylamines and processes for preparing these compounds
US6005102A (en) 1997-10-15 1999-12-21 American Home Products Corporation Aryloxy-alkyl-dialkylamines
US6479535B1 (en) 1998-05-15 2002-11-12 Wyeth 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations
AR029538A1 (es) 2000-07-06 2003-07-02 Wyeth Corp Composiciones farmaceuticas de agentes estrogenicos
EP1336602A1 (en) 2002-02-13 2003-08-20 Giovanni Scaramuzzino Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
IL165395A0 (en) 2002-06-25 2006-01-15 Wyeth Corp Use of thio-oxubdile derivatives in treatment of hormone-related conditions
PE20060676A1 (es) 2004-04-07 2006-07-24 Wyeth Corp Polimorfo cristalino de acetato de bazedoxifeno

Also Published As

Publication number Publication date
NO20065046L (no) 2006-11-06
GT200500080A (es) 2005-10-31
US20050250762A1 (en) 2005-11-10
JP2007532548A (ja) 2007-11-15
PE20060173A1 (es) 2006-04-12
JP2009007361A (ja) 2009-01-15
BRPI0509257A (pt) 2007-09-11
CA2561296A1 (en) 2005-10-27
TW200536845A (en) 2005-11-16
EP1732889A1 (en) 2006-12-20
US7683052B2 (en) 2010-03-23
AR048683A1 (es) 2006-05-17
ZA200608361B (en) 2010-03-31
PA8629201A1 (es) 2005-11-25
RU2006132352A (ru) 2008-05-20
WO2005100314A1 (en) 2005-10-27
IL178101A0 (en) 2006-12-31
ECSP066910A (es) 2006-12-20
KR20070004815A (ko) 2007-01-09
UA86055C2 (ru) 2009-03-25
CN1938271A (zh) 2007-03-28

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Legal Events

Date Code Title Description
MK12 Application lapsed section 141(1)/reg 8.3(2) - applicant filed a written notice of withdrawal