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PE20010917A1 - Forma cristalina de eplerenona que muestra un aumento en la velocidad de disolucion - Google Patents

Forma cristalina de eplerenona que muestra un aumento en la velocidad de disolucion

Info

Publication number
PE20010917A1
PE20010917A1 PE2000001300A PE0013002000A PE20010917A1 PE 20010917 A1 PE20010917 A1 PE 20010917A1 PE 2000001300 A PE2000001300 A PE 2000001300A PE 0013002000 A PE0013002000 A PE 0013002000A PE 20010917 A1 PE20010917 A1 PE 20010917A1
Authority
PE
Peru
Prior art keywords
eplerenone
refers
crystal
dicarboxylate
crystaline
Prior art date
Application number
PE2000001300A
Other languages
English (en)
Inventor
Kathleen P Barton
Chris Y Yan
Marlon V Carlos
Subhash Desai
Leonard J Ferro
Scott Ganser
Henry T Gaud
Clay R Little
Martha S Mudipalli
Mark A Pietz
Daniel R Pilipauskas
Yuen-Lung L Sing
Glenn L Stahl
Joseph J Wieczorek
Thomas B Borchardt
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 PE20010917A1 publication Critical patent/PE20010917A1/es

Links

Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)

Abstract

SE REFIERE A LA FORMA H DE EPLERENONA (METIL HIDROGENO 9,11-EPOXI-17-HIDROXI-3-OXOPREGN-4-ENE-7,21-DICARBOXILATO, g-LACTONA) QUE TIENE UNA DISOLUCION RAPIDA EN MEDIO ACUOSO Y SE CARACTERIZA POR PRESENTARSE EN FORMA DE CRISTAL ORTOROMBICO; PATRON DE DIFRACCION DE RAYOS X; PUNTO DE FUSION DE 247°C A 251°C; TAMANO DE PARTICULAS D90 INFERIOR A 400µm; TAMBIEN SE REFIERE A UNA DROGA QUE COMPRENDE DE 90% A 100% DE LA FORMA H Y EL RESTO CONSISTE DE EPLERENONA CRISTALINA FORMA L CON UN SISTEMA DE CRISTALES MONOCLINICOS; FORMA SOLVATADA DE EPLERENONA CRISTALINA, EPLERENONA AMORFA; UTILIZANDOSE DE 10mg A 1000mg. TAMBIEN SE REFIERE A i)UN METODO PARA PREPARAR LA FORMA H; ii)EPLERENONA AMORFA LIBRE DE LA FORMA CRISTALINA; iii)METODO PARA PROMOVER LA CRISTALIZACION DE LA FORMA H DE EPLERENONA QUE COMPRENDE BANAR LA SOLUCION ANTES DE LA CRISTALIZACION CON COMPUESTOS DE BANADO QUE EN FORMA SUSTANCIAL SON CRISTALOGRAFICAMENTE ISOESTRUCTURAL CON LA EPLERENONA FORMA H COMO 7-METILHIDROGENO 4O,5O,9O; 11O-DIEPOXIDO-17-HIDROXI-3-OXO-17O-PREGNAN-7O,21-DICARBOXILATO. LA EPLERENONA ES UN ANTAGONISTA DEL RECEPTOR DE ALDOSTERONA
PE2000001300A 1999-12-08 2000-12-06 Forma cristalina de eplerenona que muestra un aumento en la velocidad de disolucion PE20010917A1 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US16969099P 1999-12-08 1999-12-08
US16963999P 1999-12-08 1999-12-08
US16968299P 1999-12-08 1999-12-08
US16955699P 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
PE20010917A1 true PE20010917A1 (es) 2001-09-10

Family

ID=27558585

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001300A PE20010917A1 (es) 1999-12-08 2000-12-06 Forma cristalina de eplerenona que muestra un aumento en la velocidad de disolucion

Country Status (17)

Country Link
EP (1) EP1177204A2 (es)
JP (1) JP2003516414A (es)
KR (1) KR100607923B1 (es)
CN (2) CN1152886C (es)
AU (1) AU784946B2 (es)
BR (1) BR0008057A (es)
CA (1) CA2362669A1 (es)
CO (1) CO5280211A1 (es)
EA (1) EA007934B1 (es)
HU (1) HUP0203032A3 (es)
IL (3) IL144764A0 (es)
MX (1) MXPA01008056A (es)
MY (1) MY131878A (es)
NO (1) NO20013856L (es)
NZ (2) NZ530028A (es)
PE (1) PE20010917A1 (es)
WO (1) WO2001042272A2 (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0308475A (pt) * 2002-03-20 2005-01-11 Pharmacia Corp Formulação de eplerenona estável na armazenagem
US7235655B2 (en) 2002-03-22 2007-06-26 Pharmacia & Upjohn Company Processes to prepare eplerenone
CA2582496A1 (en) 2007-03-20 2008-09-20 Apotex Pharmachem Inc. Improved process for the preparation and purification of eplerenone
ES2641144T3 (es) 2010-05-10 2017-11-07 Inserm (Institut National De La Santé Et De La Recherche Medicale) Métodos y composiciones para el tratamiento de la acumulación de líquido en y/o bajo la retina
US9241944B2 (en) 2010-06-16 2016-01-26 Institut National De La Santé Et De La Recherche Médicale (Inserm) Methods and compositions for stimulating reepithelialisation during wound healing
WO2017064121A1 (en) 2015-10-13 2017-04-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of choroidal neovascularisation
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
WO2018019843A1 (en) 2016-07-26 2018-02-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Antagonist of mineralocorticoid receptor for the treatment of osteoarthritis
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
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
WO2023204729A1 (ru) * 2022-04-19 2023-10-26 Общество с ограниченной ответственностью "Гелеспон" Фармацевтические композиции на основе новой субстанции 4-[2-(1н-имидазол-4-ил)-этилкарбамоил]-бутановой кислоты и способ получения субстанции
CN120754115A (zh) * 2025-05-23 2025-10-10 远大医药（中国）有限公司 一种含依普利酮组合物及其药物制剂、制备方法和用途

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4559332A (en) * 1983-04-13 1985-12-17 Ciba Geigy Corporation 20-Spiroxanes and analogues having an open ring E, processes for their manufacture, and pharmaceutical preparations thereof
ES2186017T3 (es) * 1996-12-11 2003-05-01 Searle & Co Procedimientos para la preparacion de delta 4,5-esteroides 3-ceto-7alfa-alcoxicarbonil-sustituidos y compuestos intermedios de utilidad en los mismos.
EP1165136B1 (en) * 1999-03-05 2003-09-10 G.D. Searle LLC Combination therapy of angiotensin converting enzyme inhibitor and epoxy-steroidal aldosterone antagonist for treatment of cardiovascular disease

Also Published As

Publication number Publication date
CN1377365A (zh) 2002-10-30
EA200100871A1 (ru) 2002-04-25
MXPA01008056A (es) 2003-07-21
NZ513961A (en) 2004-02-27
KR100607923B1 (ko) 2006-08-04
IL144764A (en) 2007-08-19
CA2362669A1 (en) 2001-06-14
CN1557833A (zh) 2004-12-29
HK1050536A1 (en) 2003-06-27
HUP0203032A2 (hu) 2002-12-28
CO5280211A1 (es) 2003-05-30
JP2003516414A (ja) 2003-05-13
MY131878A (en) 2007-09-28
NO20013856L (no) 2001-10-08
BR0008057A (pt) 2002-04-23
NZ530028A (en) 2005-08-26
WO2001042272A3 (en) 2001-11-29
HUP0203032A3 (en) 2003-04-28
IL176511A (en) 2007-08-19
WO2001042272A2 (en) 2001-06-14
KR20010112261A (ko) 2001-12-20
AU2049201A (en) 2001-06-18
WO2001042272A9 (en) 2002-12-12
IL144764A0 (en) 2002-06-30
EP1177204A2 (en) 2002-02-06
EA007934B1 (ru) 2007-02-27
AU784946B2 (en) 2006-08-03
CN1152886C (zh) 2004-06-09
NO20013856D0 (no) 2001-08-08

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