ATE225367T1 - Verfahren zur herstellung von 3-keto-7alpha- alkoxycarbonyl- delta4,5-steroiden sowie zwischenprodukte - Google Patents

Verfahren zur herstellung von 3-keto-7alpha- alkoxycarbonyl- delta4,5-steroiden sowie zwischenprodukte

Info

Publication number
ATE225367T1
ATE225367T1 AT97954126T AT97954126T ATE225367T1 AT E225367 T1 ATE225367 T1 AT E225367T1 AT 97954126 T AT97954126 T AT 97954126T AT 97954126 T AT97954126 T AT 97954126T AT E225367 T1 ATE225367 T1 AT E225367T1
Authority
AT
Austria
Prior art keywords
group
alkoxycarbonyl
hydroxyalkyl
alkoxyalkyl
aryloxy
Prior art date
Application number
AT97954126T
Other languages
English (en)
Inventor
John S Ng
Chin Liu
Dennis K Anderson
Jon P Lawson
Joseph Wieczorek
Sastry A Kunda
Leo J Letendre
Mark J Pozzo
Yuen-Lung L Sing
Ping T Wang
Edward E Yonan
Richard M Weier
Thomas R Kowar
Julio A Baez
Bernhard Erb
Original Assignee
Searle & Co
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=26709541&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE225367(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Searle & Co filed Critical Searle & Co
Application granted granted Critical
Publication of ATE225367T1 publication Critical patent/ATE225367T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J75/00Processes for the preparation of steroids in general
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P33/00Preparation of steroids
    • C12P33/06Hydroxylating
    • C12P33/08Hydroxylating at 11 position
    • C12P33/10Hydroxylating at 11 position at 11 alpha-position
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D301/00Preparation of oxiranes
    • C07D301/02Synthesis of the oxirane ring
    • C07D301/03Synthesis of the oxirane ring by oxidation of unsaturated compounds, or of mixtures of unsaturated and saturated compounds
    • C07D301/12Synthesis of the oxirane ring by oxidation of unsaturated compounds, or of mixtures of unsaturated and saturated compounds with hydrogen peroxide or inorganic peroxides or peracids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0059Estrane derivatives substituted in position 17 by a keto group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/001Lactones
    • C07J21/003Lactones at position 17
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J53/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J53/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002Carbocyclic rings fused
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes
    • C07J71/0015Oxiranes at position 9(11)
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P33/00Preparation of steroids
    • C12P33/005Degradation of the lateral chains at position 17

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Microbiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Engineering & Computer Science (AREA)
  • Toxicology (AREA)
  • Inorganic Chemistry (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Catalysts (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
AT97954126T 1996-12-11 1997-12-11 Verfahren zur herstellung von 3-keto-7alpha- alkoxycarbonyl- delta4,5-steroiden sowie zwischenprodukte ATE225367T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US3331596P 1996-12-11 1996-12-11
US4938897P 1997-06-11 1997-06-11
PCT/US1997/023090 WO1998025948A2 (en) 1996-12-11 1997-12-11 Processes for preparation of 9,11-epoxy steroids and intermediates useful therein

Publications (1)

Publication Number Publication Date
ATE225367T1 true ATE225367T1 (de) 2002-10-15

Family

ID=26709541

Family Applications (2)

Application Number Title Priority Date Filing Date
AT97954126T ATE225367T1 (de) 1996-12-11 1997-12-11 Verfahren zur herstellung von 3-keto-7alpha- alkoxycarbonyl- delta4,5-steroiden sowie zwischenprodukte
AT01111209T ATE375992T1 (de) 1996-12-11 1997-12-11 Epoxidierungsverfahren

Family Applications After (1)

Application Number Title Priority Date Filing Date
AT01111209T ATE375992T1 (de) 1996-12-11 1997-12-11 Epoxidierungsverfahren

Country Status (21)

Country Link
US (1) US6610844B2 (de)
EP (1) EP0944644B1 (de)
JP (1) JP2001509792A (de)
KR (1) KR100523409B1 (de)
CN (1) CN100369927C (de)
AT (2) ATE225367T1 (de)
AU (1) AU733559B2 (de)
BR (1) BR9714510A (de)
CA (1) CA2273343C (de)
DE (2) DE69716116T2 (de)
DK (1) DK0944644T3 (de)
ES (2) ES2293944T3 (de)
HK (1) HK1043370B (de)
IL (1) IL130182A0 (de)
NO (1) NO314149B1 (de)
NZ (1) NZ336004A (de)
PL (1) PL189459B1 (de)
PT (1) PT944644E (de)
RO (1) RO120710B1 (de)
RU (1) RU2005121439A (de)
WO (1) WO1998025948A2 (de)

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EP1580193A3 (de) * 1999-12-08 2010-06-23 Pharmacia Corporation Kristalline Form von Eplerenon
EP1505072A3 (de) * 1999-12-08 2006-06-21 Pharmacia Corporation Kristalline Form von Eplerenon mit verbesserter Lösegeschwindigkeit
CA2362669A1 (en) * 1999-12-08 2001-06-14 Pharmacia Corporation Eplerenone crystalline form exhibiting enhanced dissolution rate
IL144757A0 (en) * 1999-12-08 2002-06-30 Pharmacia Corp Eplerenone crystalline form
US6716829B2 (en) 2000-07-27 2004-04-06 Pharmacia Corporation Aldosterone antagonist and cyclooxygenase-2 inhibitor combination therapy to prevent or treat inflammation-related cardiovascular disorders
US20020111337A1 (en) * 2000-08-28 2002-08-15 Fedde Kenton N. Use of an aldosterone receptor antagonist to improve cognitive function
EP1352054A2 (de) 2000-10-30 2003-10-15 Pharmacia Corporation 11 alpha hydroxylase und oxidoreductase aus aspergillus ochraceus
US7235655B2 (en) 2002-03-22 2007-06-26 Pharmacia & Upjohn Company Processes to prepare eplerenone
EP1487859B1 (de) * 2002-03-22 2008-08-13 Pharmacia & Upjohn Company LLC Verfahren zur herstellung von eplerenon
CN1694897A (zh) 2002-11-06 2005-11-09 法玛西亚普强责任有限公司 7-羧基取代的甾族化合物的制备方法
RU2289586C2 (ru) * 2002-11-07 2006-12-20 Фармация Энд Апджон Компани Ллс Способ получения 7-замещенных стероидных соединений, соединения, способы получения эплеренона, продукт
CL2004000574A1 (es) * 2003-03-21 2005-02-11 Pharmacia Corp Sa Organizada B Proceso para preparar un compuesto 17-espirolactona o la sal de lactona abierta por carbonilacion del correspondiente 17-alquenil o alquinil derivado, los intermediarios que se usan y su proceso de obtencion.
WO2005000869A1 (en) * 2003-05-29 2005-01-06 Washington University Neuroactive 13,24-cyclo-18,21-dinorcholanes and structurally-related pentacyclic steroids
TW200602352A (en) * 2004-03-22 2006-01-16 Upjohn Co Improved process for the preparation of 9,11 epoxy steroids
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US8222237B2 (en) * 2008-11-25 2012-07-17 Evestra, Inc. Progestational 3-(6,6-ethylene-17B-hydroxy-3-oxo-17A-pregna-4-ene-17A-yl)propionic acid G-lactones
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
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
US9562068B2 (en) 2014-10-17 2017-02-07 Industriale Chimica, S.R.L. Process for the preparation of 7 α-(methoxycarbonyl)-3-OXO-17alpha-pregn-4,9(11)-dien-21,17-carbolactone, a useful intermediate for the synthesis of molecules with pharmacological activity
WO2017055248A1 (en) 2015-09-28 2017-04-06 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of heart failure
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
CN105541960A (zh) * 2016-02-22 2016-05-04 浙江仙琚制药股份有限公司 17α-羟基-3-氧代-γ-内酯-孕甾-4-烯-(7α,9α)-二羧酸内酯的制备方法
US20190262363A1 (en) 2016-07-26 2019-08-29 INSERM (Institut National de la Santé et de la Recherche Médicale Antagonist of mineralocorticoid receptor for the treatment of osteoarthritis
CN106349326A (zh) * 2016-07-29 2017-01-25 北京万全德众医药生物技术有限公司 依普利酮杂质a的制备方法
CN107602652A (zh) * 2017-10-11 2018-01-19 浙江仙琚制药股份有限公司 制备6β‑甲基泼尼松龙的方法
CN108445236B (zh) * 2018-02-07 2021-04-20 深圳市新产业生物医学工程股份有限公司 甾体类衍生物和其保存液以及其应用
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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
CN115433252A (zh) * 2022-08-24 2022-12-06 浙江亚瑟医药有限公司 一种δ9(11)-坎利酮的制备方法

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Also Published As

Publication number Publication date
AU733559B2 (en) 2001-05-17
DK0944644T3 (da) 2003-02-03
CA2273343C (en) 2006-10-10
DE69738225T2 (de) 2008-07-17
AU5798398A (en) 1998-07-03
RO120710B1 (ro) 2006-06-30
US6610844B2 (en) 2003-08-26
EP0944644B1 (de) 2002-10-02
WO1998025948A3 (en) 1998-10-15
CN1253564A (zh) 2000-05-17
CA2273343A1 (en) 1998-06-18
RU2005121439A (ru) 2007-01-20
HK1043370B (en) 2008-08-01
DE69738225D1 (de) 2007-11-29
WO1998025948A2 (en) 1998-06-18
NZ336004A (en) 2001-04-27
NO992825L (no) 1999-07-29
BR9714510A (pt) 2000-11-28
PL189459B1 (pl) 2005-08-31
NO314149B1 (no) 2003-02-03
ATE375992T1 (de) 2007-11-15
DE69716116D1 (de) 2002-11-07
IL130182A0 (en) 2000-06-01
NO992825D0 (no) 1999-06-10
JP2001509792A (ja) 2001-07-24
KR100523409B1 (ko) 2005-10-24
ES2186017T3 (es) 2003-05-01
PT944644E (pt) 2003-02-28
EP0944644A2 (de) 1999-09-29
DE69716116T2 (de) 2003-09-04
PL334084A1 (en) 2000-01-31
CN100369927C (zh) 2008-02-20
ES2293944T3 (es) 2008-04-01
KR20050009765A (ko) 2005-01-25
HK1043370A1 (en) 2002-09-13
US20030055274A1 (en) 2003-03-20

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