CN100413881C - 依匹乐酮晶形 - Google Patents

依匹乐酮晶形 Download PDF

Info

Publication number
CN100413881C
CN100413881C CNB008057710A CN00805771A CN100413881C CN 100413881 C CN100413881 C CN 100413881C CN B008057710 A CNB008057710 A CN B008057710A CN 00805771 A CN00805771 A CN 00805771A CN 100413881 C CN100413881 C CN 100413881C
Authority
CN
China
Prior art keywords
eplerenone
crystalline form
solvent
composition
compound
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.)
Expired - Fee Related
Application number
CNB008057710A
Other languages
English (en)
Chinese (zh)
Other versions
CN1433427A (zh
Inventor
K·P·巴顿
H·T·戈德
S·甘泽
C·R·利特勒
P·S·穆迪帕利
T·B·波沙德特
M·V·卡洛斯
S·德赛
L·J·菲罗
M·A·皮茨
D·R·皮利保斯卡斯
Y·-L·L·邢
G·L·斯塔尔
J·J·维佐雷克
C·Y·彦
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.)
Pharmacia LLC
Original Assignee
Pharmacia 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
Application filed by Pharmacia LLC filed Critical Pharmacia LLC
Publication of CN1433427A publication Critical patent/CN1433427A/zh
Application granted granted Critical
Publication of CN100413881C publication Critical patent/CN100413881C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Images

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)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Inorganic Compounds Of Heavy Metals (AREA)
  • Developing Agents For Electrophotography (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CNB008057710A 1999-12-08 2000-12-04 依匹乐酮晶形 Expired - Fee Related CN100413881C (zh)

Applications Claiming Priority (12)

Application Number Priority Date Filing Date Title
US16960899P 1999-12-08 1999-12-08
US16955699P 1999-12-08 1999-12-08
US16963999P 1999-12-08 1999-12-08
US16980799P 1999-12-08 1999-12-08
US16968399P 1999-12-08 1999-12-08
US16970799P 1999-12-08 1999-12-08
US60/169608 1999-12-08
US60/169807 1999-12-08
US60/169556 1999-12-08
US60/169683 1999-12-08
US60/169639 1999-12-08
US60/169707 1999-12-08

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CNA2008101319733A Division CN101317848A (zh) 1999-12-08 2000-12-04 依匹乐酮晶形

Publications (2)

Publication Number Publication Date
CN1433427A CN1433427A (zh) 2003-07-30
CN100413881C true CN100413881C (zh) 2008-08-27

Family

ID=27558586

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB008057710A Expired - Fee Related CN100413881C (zh) 1999-12-08 2000-12-04 依匹乐酮晶形

Country Status (18)

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

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP2977084B1 (en) 2010-05-10 2017-07-05 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and compositions for the treatment of fluid accumulation in and/ or under the retina
JP6180930B2 (ja) 2010-06-16 2017-08-16 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 創傷治癒過程における再上皮化を刺激するための方法及び組成物
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
CN113173968A (zh) * 2021-03-19 2021-07-27 江苏康思尔医药科技有限公司 一种依普利酮的纯化方法
US20240366632A1 (en) 2021-08-31 2024-11-07 Institut National de la Santé et de la Recherche Médicale Methods for the treatment of ocular rosacea

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998025948A2 (en) * 1996-12-11 1998-06-18 G.D. Searle & Co. Processes for preparation of 9,11-epoxy steroids and intermediates useful therein

Family Cites Families (36)

* 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
US4826689A (en) * 1984-05-21 1989-05-02 University Of Rochester Method for making uniformly sized particles from water-insoluble organic compounds
FR2634376B1 (fr) * 1988-07-21 1992-04-17 Farmalyoc Nouvelle forme unitaire, solide et poreuse comprenant des microparticules et/ou des nanoparticules, ainsi que sa preparation
IT1227626B (it) * 1988-11-28 1991-04-23 Vectorpharma Int Farmaci supportati aventi velocita' di dissoluzione aumentata e procedimento per la loro preparazione
IT1243390B (it) * 1990-11-22 1994-06-10 Vectorpharma Int Composizioni farmaceutiche in forma di particelle atte al rilascio controllato di sostanze farmacologicamente attive e procedimento per la loro preparazione.
US5552160A (en) * 1991-01-25 1996-09-03 Nanosystems L.L.C. Surface modified NSAID nanoparticles
US5145684A (en) * 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
NZ248813A (en) * 1992-11-25 1995-06-27 Eastman Kodak Co Polymeric grinding media used in grinding pharmaceutical substances
US5346702A (en) * 1992-12-04 1994-09-13 Sterling Winthrop Inc. Use of non-ionic cloud point modifiers to minimize nanoparticle aggregation during sterilization
US5298262A (en) * 1992-12-04 1994-03-29 Sterling Winthrop Inc. Use of ionic cloud point modifiers to prevent particle aggregation during sterilization
US5302401A (en) * 1992-12-09 1994-04-12 Sterling Winthrop Inc. Method to reduce particle size growth during lyophilization
US5340564A (en) * 1992-12-10 1994-08-23 Sterling Winthrop Inc. Formulations comprising olin 10-G to prevent particle aggregation and increase stability
US5336507A (en) * 1992-12-11 1994-08-09 Sterling Winthrop Inc. Use of charged phospholipids to reduce nanoparticle aggregation
US5429824A (en) * 1992-12-15 1995-07-04 Eastman Kodak Company Use of tyloxapole as a nanoparticle stabilizer and dispersant
US5352459A (en) * 1992-12-16 1994-10-04 Sterling Winthrop Inc. Use of purified surface modifiers to prevent particle aggregation during sterilization
US5587143A (en) * 1994-06-28 1996-12-24 Nanosystems L.L.C. Butylene oxide-ethylene oxide block copolymer surfactants as stabilizer coatings for nanoparticle compositions
US5585108A (en) * 1994-12-30 1996-12-17 Nanosystems L.L.C. Formulations of oral gastrointestinal therapeutic agents in combination with pharmaceutically acceptable clays
US5560932A (en) * 1995-01-10 1996-10-01 Nano Systems L.L.C. Microprecipitation of nanoparticulate pharmaceutical agents
US5665331A (en) * 1995-01-10 1997-09-09 Nanosystems L.L.C. Co-microprecipitation of nanoparticulate pharmaceutical agents with crystal growth modifiers
US5662883A (en) * 1995-01-10 1997-09-02 Nanosystems L.L.C. Microprecipitation of micro-nanoparticulate pharmaceutical agents
US5569448A (en) * 1995-01-24 1996-10-29 Nano Systems L.L.C. Sulfated nonionic block copolymer surfactants as stabilizer coatings for nanoparticle compositions
US5571536A (en) * 1995-02-06 1996-11-05 Nano Systems L.L.C. Formulations of compounds as nanoparticulate dispersions in digestible oils or fatty acids
US5560931A (en) * 1995-02-14 1996-10-01 Nawosystems L.L.C. Formulations of compounds as nanoparticulate dispersions in digestible oils or fatty acids
US5503723A (en) * 1995-02-08 1996-04-02 Eastman Kodak Company Isolation of ultra small particles
US5534270A (en) * 1995-02-09 1996-07-09 Nanosystems Llc Method of preparing stable drug nanoparticles
US5518738A (en) * 1995-02-09 1996-05-21 Nanosystem L.L.C. Nanoparticulate nsaid compositions
US5622938A (en) * 1995-02-09 1997-04-22 Nano Systems L.L.C. Sugar base surfactant for nanocrystals
US5591456A (en) * 1995-02-10 1997-01-07 Nanosystems L.L.C. Milled naproxen with hydroxypropyl cellulose as a dispersion stabilizer
US5573783A (en) * 1995-02-13 1996-11-12 Nano Systems L.L.C. Redispersible nanoparticulate film matrices with protective overcoats
US5510118A (en) * 1995-02-14 1996-04-23 Nanosystems Llc Process for preparing therapeutic compositions containing nanoparticles
US5580579A (en) * 1995-02-15 1996-12-03 Nano Systems L.L.C. Site-specific adhesion within the GI tract using nanoparticles stabilized by high molecular weight, linear poly (ethylene oxide) polymers
US5747001A (en) * 1995-02-24 1998-05-05 Nanosystems, L.L.C. Aerosols containing beclomethazone nanoparticle dispersions
US5565188A (en) * 1995-02-24 1996-10-15 Nanosystems L.L.C. Polyalkylene block copolymers as surface modifiers for nanoparticles
US5718919A (en) * 1995-02-24 1998-02-17 Nanosystems L.L.C. Nanoparticles containing the R(-)enantiomer of ibuprofen
EA009176B1 (ru) * 1995-12-11 2007-12-28 Дж.Д.Серл Энд Ко. Способ получения 7-альфа-карбоксил-9,11-эпоксистероидов и промежуточных продуктов, используемых для их получения, и общий способ эпоксидирования по олефиновым двойным связям
DE60005159T2 (de) * 1999-03-05 2004-07-22 G.D. Searle Llc, Chicago Kombinationstherapie von angiotensin-konvertierendem enzym hemmer und epoxy-steroidalem aldosteron antagonist zur behandlung von kardiovaskulären erkrankungen

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998025948A2 (en) * 1996-12-11 1998-06-18 G.D. Searle & Co. Processes for preparation of 9,11-epoxy steroids and intermediates useful therein

Also Published As

Publication number Publication date
JP2003515611A (ja) 2003-05-07
AR074665A2 (es) 2011-02-02
CN1433427A (zh) 2003-07-30
US20090149431A1 (en) 2009-06-11
IL144757A (en) 2007-07-24
KR20020003192A (ko) 2002-01-10
JP4219105B2 (ja) 2009-02-04
IL144757A0 (en) 2002-06-30
KR100584104B1 (ko) 2006-05-30
AU2041101A (en) 2001-06-18
CO5280205A1 (es) 2003-05-30
EA200100869A1 (ru) 2002-04-25
NO20013857L (no) 2001-10-08
WO2001041535A2 (en) 2001-06-14
HUP0201457A2 (en) 2002-08-28
BR0008054A (pt) 2002-03-12
WO2001041535A3 (en) 2001-11-22
HUP0201457A3 (en) 2003-07-28
EP1175434A2 (en) 2002-01-30
EA008449B1 (ru) 2007-06-29
WO2001041535A9 (en) 2002-07-04
NZ513962A (en) 2004-08-27
MY143571A (en) 2011-05-31
HK1057220A1 (zh) 2004-03-19
CA2362845A1 (en) 2001-06-14
NO20013857D0 (no) 2001-08-08
PE20010918A1 (es) 2001-09-10
JP2007016043A (ja) 2007-01-25

Similar Documents

Publication Publication Date Title
US9062047B2 (en) Crystalline form of pyrimido[6,1-A] isoquinolin-4-one compound
US20090149431A1 (en) Eplerenone Drug Substance Having High Phase Purity
AU784946B2 (en) Eplerenone crystalline form exhibiting enhanced dissolution rate
CN101317848A (zh) 依匹乐酮晶形
CN110590740A (zh) 一种阿帕鲁胺化合物及其药物制剂
US20020045746A1 (en) Eplerenone crystalline form
US20050267302A1 (en) Eplerenone crystalline form exhibiting enhanced dissolution rate
AU2004242560B2 (en) Eplerenone crystalline form
US20020038021A1 (en) Eplerenone crystalline form exhibiting enhanced dissolution rate
HK1057220B (en) Eplerenone crystalline form
US20050159594A1 (en) Eplerenone crystal form exhibiting enhanced dissolution rate
HK1125841A (en) Eplerenone crystalline form
EP1505072A2 (en) Eplerenone crystalline form exhiniting enhanced dissolution rate
EP1580193A2 (en) Eplerenone crystalline form
US20030083493A1 (en) Eplerenone drug substance having high phase purity
CN102317276A (zh) 包含氨基磺酸6-氧代-6，7，8，9，10，11-六氢环庚三烯并[c]色烯-3-基酯和其多晶型物的固体药物组合物
MXPA01008057A (en) Eplerenone crystalline form
TWI290558B (en) Eplerenone crystalline form exhibiting enhanced dissolution rate
NZ540941A (en) Process for producing amorphous form of eplerenone exhibiting enhanced dissolution rate

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1057220

Country of ref document: HK

C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20080827

Termination date: 20111204