AR074665A2 - Formula cristalina no solvatada de eplerenona (forma l), sustancia farmacologica y composicion farmaceutica que la comprenden - Google Patents

Formula cristalina no solvatada de eplerenona (forma l), sustancia farmacologica y composicion farmaceutica que la comprenden

Info

Publication number
AR074665A2
AR074665A2 ARP090104744A ARP090104744A AR074665A2 AR 074665 A2 AR074665 A2 AR 074665A2 AR P090104744 A ARP090104744 A AR P090104744A AR P090104744 A ARP090104744 A AR P090104744A AR 074665 A2 AR074665 A2 AR 074665A2
Authority
AR
Argentina
Prior art keywords
eplerenone
understand
pharmaceutical composition
prepare
crystalline
Prior art date
Application number
ARP090104744A
Other languages
English (en)
Inventor
Clay Little
Yuen-Lung Sing
Marlon Carlos
Leonard Ferro
Daniel Pilipauskas
Glenn Stahl
Subhash Desai
Kathleen Barton
Henry GAUD
Joseph Wieczorek
Chris Yan
Thomas B Borchardt
Partha S Mudipalli
Mark A Pietz
Scott Ganser
Original Assignee
Pharmacia Corp
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 Pharmacia Corp filed Critical Pharmacia Corp
Publication of AR074665A2 publication Critical patent/AR074665A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J19/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 by a lactone ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes
    • C07J71/0015—Oxiranes at position 9(11)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • 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
    • A61P5/28—Antiandrogens
    • 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
    • A61P5/34—Gestagens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Inorganic Compounds Of Heavy Metals (AREA)
  • Developing Agents For Electrophotography (AREA)

Abstract

Una forma cristalina (Forma L) de la droga eplerenona antagonista del receptor de la aldosterona con una estabilidad física relativamente alta a temperaturas normales de almacenamiento y uso. Se proporcionan composiciones farmacéuticas que incluyen la eplerenona de Forma L, opcionalmente acompanada por una o más de otras formas en estado sólido de la eplerenona, en una cantidad total de dosaje unitario de eplerenona de entre aproximadamente 10 y aproximadamente 1000 mg, y que además incluyen uno o más excipientes aceptables para uso farmacéutico. Se proporcionan procesos para preparar eplerenona de Forma L y para preparar composiciones que incluyen a la eplerenona de Forma L. También se proporciona un método para la profilaxis y/o el tratamiento de una condición o trastorno mediados por la aldosterona, que incluye administrar a un sujeto una cantidad de epIerenona eficaz en términos terapéuticos, donde por lo menos una fracción de la eplerenona presente es eplerenona de Forma L. Reivindicación 1: Una forma cristalina no solvatada de eplerenona (Forma L) caracterizada porque comprende: e) una celda unitaria que comprende un sistema cristalino monoclínico y un grupo espacial de P21; y f) un patrón de difracción de Rayos X del polvo que comprende picos a 8,0 ñ 0,2, 12,4 ñ 0,2, 12,8 ñ 0,2, y 13,3 ñ 0,2 grados a 2theta medidos a una longitud de onda de 1,54056 A.
ARP090104744A 1999-12-08 2009-12-07 Formula cristalina no solvatada de eplerenona (forma l), sustancia farmacologica y composicion farmaceutica que la comprenden AR074665A2 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US16968399P 1999-12-08 1999-12-08
US16963999P 1999-12-08 1999-12-08
US16955699P 1999-12-08 1999-12-08
US16970799P 1999-12-08 1999-12-08
US16980799P 1999-12-08 1999-12-08
US16960899P 1999-12-08 1999-12-08

Publications (1)

Publication Number Publication Date
AR074665A2 true AR074665A2 (es) 2011-02-02

Family

ID=27558586

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090104744A AR074665A2 (es) 1999-12-08 2009-12-07 Formula cristalina no solvatada de eplerenona (forma l), sustancia farmacologica y composicion farmaceutica que la comprenden

Country Status (19)

Country Link
US (1) US20090149431A1 (es)
EP (1) EP1175434A2 (es)
JP (2) JP4219105B2 (es)
KR (1) KR100584104B1 (es)
CN (1) CN100413881C (es)
AR (1) AR074665A2 (es)
AU (1) AU2041101A (es)
BR (1) BR0008054A (es)
CA (1) CA2362845A1 (es)
CO (1) CO5280205A1 (es)
EA (1) EA008449B1 (es)
HK (1) HK1057220A1 (es)
HU (1) HUP0201457A3 (es)
IL (2) IL144757A0 (es)
MY (1) MY143571A (es)
NO (1) NO20013857L (es)
NZ (1) NZ513962A (es)
PE (1) PE20010918A1 (es)
WO (1) WO2001041535A2 (es)

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ITMI20010821A1 (it) * 2001-04-17 2002-10-17 Gienne Pharma S P A Impiego di composti derivati dallo spirolattone per inibire l'azione pro-fibrigenetica delle cellule stellate epatiche e delle cellule musco
US7235655B2 (en) 2002-03-22 2007-06-26 Pharmacia & Upjohn Company Processes to prepare eplerenone
CA2796307A1 (en) 2010-05-10 2011-11-17 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods and compositions for the treatment of fluid accumulation in and/ or under the retina
WO2011157798A1 (en) 2010-06-16 2011-12-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for stimulating reepithelialisation during wound healing
CN104844681B (zh) * 2014-02-13 2016-06-01 合肥久诺医药科技有限公司 一种l晶型依普利酮的精制方法
JP6835836B2 (ja) 2015-10-13 2021-02-24 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 脈絡膜血管新生の処置のための方法及び医薬組成物
EP3490606B8 (en) 2016-07-26 2024-04-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Antagonist of mineralocorticoid receptor for the treatment of osteoarthritis
CN108059648A (zh) * 2017-12-30 2018-05-22 合肥久诺医药科技有限公司 一种依普利酮溶剂合物及其制备方法
WO2023031277A1 (en) 2021-08-31 2023-03-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of ocular rosacea

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Also Published As

Publication number Publication date
PE20010918A1 (es) 2001-09-10
WO2001041535A3 (en) 2001-11-22
WO2001041535A9 (en) 2002-07-04
IL144757A (en) 2007-07-24
EA008449B1 (ru) 2007-06-29
NO20013857L (no) 2001-10-08
NZ513962A (en) 2004-08-27
US20090149431A1 (en) 2009-06-11
EA200100869A1 (ru) 2002-04-25
JP2003515611A (ja) 2003-05-07
JP2007016043A (ja) 2007-01-25
EP1175434A2 (en) 2002-01-30
HK1057220A1 (en) 2004-03-19
KR20020003192A (ko) 2002-01-10
NO20013857D0 (no) 2001-08-08
CA2362845A1 (en) 2001-06-14
JP4219105B2 (ja) 2009-02-04
KR100584104B1 (ko) 2006-05-30
AU2041101A (en) 2001-06-18
CN100413881C (zh) 2008-08-27
CO5280205A1 (es) 2003-05-30
BR0008054A (pt) 2002-03-12
IL144757A0 (en) 2002-06-30
MY143571A (en) 2011-05-31
CN1433427A (zh) 2003-07-30
HUP0201457A2 (en) 2002-08-28
HUP0201457A3 (en) 2003-07-28
WO2001041535A2 (en) 2001-06-14

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