ES2320626T5 - Procedimiento para la preparación de drospirenona - Google Patents

Procedimiento para la preparación de drospirenona

Info

Publication number
ES2320626T5
ES2320626T5 ES01250277T ES01250277T ES2320626T5 ES 2320626 T5 ES2320626 T5 ES 2320626T5 ES 01250277 T ES01250277 T ES 01250277T ES 01250277 T ES01250277 T ES 01250277T ES 2320626 T5 ES2320626 T5 ES 2320626T5
Authority
ES
Spain
Prior art keywords
drospirenone
procedure
preparation
15beta
16beta
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 - Lifetime
Application number
ES01250277T
Other languages
English (en)
Other versions
ES2320626T3 (es
Inventor
Joerg-Thorsten Mohr
Klaus Nickisch
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.)
Bayer Pharma AG
Bayer Intellectual Property GmbH
Original Assignee
Bayer Pharma AG
Bayer Intellectual Property GmbH
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=7803224&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2320626(T5) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Pharma AG, Bayer Intellectual Property GmbH filed Critical Bayer Pharma AG
Publication of ES2320626T3 publication Critical patent/ES2320626T3/es
Application granted granted Critical
Publication of ES2320626T5 publication Critical patent/ES2320626T5/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids 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
    • C07J53/002—Carbocyclic rings fused
    • C07J53/004—3 membered carbocyclic rings
    • C07J53/007—3 membered carbocyclic rings in position 6-7
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids 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
    • C07J53/002—Carbocyclic rings fused
    • C07J53/004—3 membered carbocyclic rings
    • C07J53/008—3 membered carbocyclic rings in position 15/16

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Fats And Perfumes (AREA)
  • Polyesters Or Polycarbonates (AREA)

Abstract

Procedimiento para la preparación de drospirenona (6beta,7beta;15beta,16beta-dimetilen-3-oxo-17alfa-pregn-4-eno-21,17carbolactona, DRSP) mediante separación del agua a partir de la 6beta,7beta;15beta,16beta-dimetilen-5beta-hidroxi-3-oxo-17alfa androstano-21,17-carbolactona por adición de un ácido o un ácido de Lewis.
ES01250277T 1996-08-12 1997-08-11 Procedimiento para la preparación de drospirenona Expired - Lifetime ES2320626T5 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19633685A DE19633685C1 (de) 1996-08-12 1996-08-12 Verfahren zur Herstellung von Drospirenon (6beta,7beta;15 beta,16beta-Dimethyl-en-3-oxo-17alpha-pregn-4-en-21,17-carbolacton, DRSP) sowie 7alpha-(3-Hydroxy-1-propyl)-6beta,7beta;15beta, 16beta-dimethylen-5beta-androstan-3beta,5,17beta-triol (ZK 92836) und 6beta,7beta;15beta,16beta-dimethylen-5beta-hydroxy-3-oxo-17alpha-androstan-21,17-carbolacton (90965) als Zwischenprodukte des Verfahrens
DE19633685 1996-08-12

Publications (2)

Publication Number Publication Date
ES2320626T3 ES2320626T3 (es) 2009-05-27
ES2320626T5 true ES2320626T5 (es) 2013-09-05

Family

ID=7803224

Family Applications (4)

Application Number Title Priority Date Filing Date
ES09100011.7T Expired - Lifetime ES2438941T3 (es) 1996-08-12 1997-08-11 Procedimiento para la preparación de drospirenona (6beta,7beta;15beta,16beta-dimetilen-3-oxo-17alfa-pregn-4-eno-21,17-carbolactona, DRSP)
ES97937562T Active ES2175451T7 (es) 1996-08-12 1997-08-11 Procedimiento para la preparacióon de drospirenona y sus productos intermedios.
ES01250278T Expired - Lifetime ES2335860T3 (es) 1996-08-12 1997-08-11 Procedimiento para la preparacion de 6beta,7beta;15beta,16beta-dimetilen-5beta-hidroxi-3-oxo-17alfa-androstano-21,17-carbolactona.
ES01250277T Expired - Lifetime ES2320626T5 (es) 1996-08-12 1997-08-11 Procedimiento para la preparación de drospirenona

Family Applications Before (3)

Application Number Title Priority Date Filing Date
ES09100011.7T Expired - Lifetime ES2438941T3 (es) 1996-08-12 1997-08-11 Procedimiento para la preparación de drospirenona (6beta,7beta;15beta,16beta-dimetilen-3-oxo-17alfa-pregn-4-eno-21,17-carbolactona, DRSP)
ES97937562T Active ES2175451T7 (es) 1996-08-12 1997-08-11 Procedimiento para la preparacióon de drospirenona y sus productos intermedios.
ES01250278T Expired - Lifetime ES2335860T3 (es) 1996-08-12 1997-08-11 Procedimiento para la preparacion de 6beta,7beta;15beta,16beta-dimetilen-5beta-hidroxi-3-oxo-17alfa-androstano-21,17-carbolactona.

Country Status (26)

Country Link
US (2) US6121465A (es)
EP (4) EP2168974B1 (es)
JP (1) JP3333524B2 (es)
KR (1) KR100473297B1 (es)
CN (1) CN1158300C (es)
AT (3) ATE446966T1 (es)
AU (1) AU729149B2 (es)
BG (1) BG62776B1 (es)
BR (1) BR9711060A (es)
CA (1) CA2261137C (es)
CZ (1) CZ297255B6 (es)
DE (4) DE19633685C1 (es)
DK (4) DK0918791T3 (es)
EA (1) EA001947B1 (es)
ES (4) ES2438941T3 (es)
HU (1) HU223106B1 (es)
IL (1) IL127963A (es)
IS (1) IS2100B (es)
NZ (1) NZ333697A (es)
PL (1) PL187474B1 (es)
PT (4) PT1149841E (es)
SI (3) SI1149841T1 (es)
SK (1) SK283546B6 (es)
TR (1) TR199900262T2 (es)
UA (1) UA55423C2 (es)
WO (1) WO1998006738A1 (es)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19633685C1 (de) 1996-08-12 1997-10-09 Schering Ag Verfahren zur Herstellung von Drospirenon (6beta,7beta;15 beta,16beta-Dimethyl-en-3-oxo-17alpha-pregn-4-en-21,17-carbolacton, DRSP) sowie 7alpha-(3-Hydroxy-1-propyl)-6beta,7beta;15beta, 16beta-dimethylen-5beta-androstan-3beta,5,17beta-triol (ZK 92836) und 6beta,7beta;15beta,16beta-dimethylen-5beta-hydroxy-3-oxo-17alpha-androstan-21,17-carbolacton (90965) als Zwischenprodukte des Verfahrens
DK1380301T3 (da) 1999-08-31 2009-04-20 Bayer Schering Pharma Ag Farmaceutisk sammensætning af ethinylestradiol og drospirenon til anvendelse som svangerskabsforebyggende middel
US6787531B1 (en) * 1999-08-31 2004-09-07 Schering Ag Pharmaceutical composition for use as a contraceptive
EP2305267A3 (en) 1999-08-31 2011-08-17 Bayer Schering Pharma Aktiengesellschaft Pharmaceutical combination of ethinylestradiol and drospirenone for use as a contraceptive
AU2001225413B2 (en) * 2000-01-18 2005-06-23 Bayer Schering Pharma Aktiengesellschaft Drospirenone for hormone replacement therapy
US20020132801A1 (en) * 2001-01-11 2002-09-19 Schering Aktiengesellschaft Drospirenone for hormone replacement therapy
WO2003006027A1 (en) 2001-07-13 2003-01-23 Schering Aktiengesellschaft Combination of drospirenone and an estrogen sulphamate for hrt
BR0309780A (pt) 2002-04-26 2005-03-22 Schering Aktiengellschaft Tratamento da hipertensão em mulheres recebendo terapia de reposição hormonal
US7786101B2 (en) * 2002-11-05 2010-08-31 Bayer Schering Pharma Ag Cardiovascular protection using anti-aldosteronic progestins
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.
ITMI20040367A1 (it) * 2004-03-01 2004-06-01 Ind Chimica Srl Processo per la preparazione di drospirenone
HUP0402465A2 (en) * 2004-11-30 2006-07-28 Richter Gedeon Vegyeszet Industrial process for preparing 17-hydroxy-6-betha, 7-betha, 15-betha, 16-betha-bis-methylene-3-oxo-17-alpha-pregn-4-ene-21-carboxylic acid gamma lacton and the main intermediates of the process
HUP0402466A2 (en) * 2004-11-30 2006-07-28 Richter Gedeon Vegyeszet Industrial process for preparing 17-hydroxy-6-betha, 7-betha, 15-betha, 16-betha-bis-methylene-3-oxo-17-alpha-pregn-4-ene-21-carboxylic acid gamma lacton and the main, intermediates of the process
DE102004058300B4 (de) * 2004-12-02 2016-09-15 Austriamicrosystems Ag Schaltungsanordnung zur Erzeugung eines komplexen Signals und Verwendung in einem Hochfrequenz-Sender oder -Empfänger
ITMI20042338A1 (it) 2004-12-06 2005-03-06 Ind Chimica Srl Processo per la preparazione di drospirenone
PT2527356T (pt) * 2005-07-21 2018-03-26 Bayer Ip Gmbh Processo para a produção de 3-oxo-pregn-4-eno-21,17-carbolactonas através da oxidação isenta de metais de 17-(3-hidroxipropil)-3,17-diidroxiandrostanos
US7319154B2 (en) 2005-07-21 2008-01-15 Bayer Schering Pharma Ag Process for the production of 3-oxo-pregn-4-ene-21, 17-carbolactones by the metal free oxidation of 17-(3-hydroxypropyl)-3, 17-dihydroxyandrostanes
ES2311927T5 (es) * 2005-07-21 2014-09-08 Bayer Pharma Aktiengesellschaft Proceso para la producción de 3-oxo-pregn-4-en-21,17-carbolactonas por la oxidación sin metales de 17-(3-hidroxipropil)-3,17-dihidroxiandrostanos
WO2007127266A2 (en) 2006-04-27 2007-11-08 Covidien Ag Electrode pad packaging systems and methods
EP1902711A1 (en) * 2006-09-20 2008-03-26 KAIROSmed GmbH Oral modified release formulations containing Drospirenon and 8-Prenylnaringenin for use in Hormone Replacement Therapy (HRT)
MX2008016571A (es) * 2007-05-01 2009-03-09 Sicor Inc Proceso para preparar drospirenona y su intermediarios.
DE102007030596B3 (de) * 2007-06-28 2009-03-12 Bayer Schering Pharma Aktiengesellschaft Verfahren zur Herstellung von 17-(3-Hydroxypropyl)-17-hydroxysteroiden
EP2265629B1 (en) * 2008-03-05 2015-06-24 Evestra, Inc. Bismethylene-17 carbolactones and related uses
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
CA2752805A1 (en) 2009-02-18 2010-08-26 Bayer Pharma Aktiengesellschaft Formulation comprising drospirenone for subcutaneous or intramuscular administration
US20120114757A1 (en) 2009-02-18 2012-05-10 Bayer Pharma Aktiengesellschaft Particles comprising drospirenone encapsulated in a polymer
US8334375B2 (en) * 2009-04-10 2012-12-18 Evestra, Inc. Methods for the preparation of drospirenone
ES2432063T3 (es) * 2009-06-16 2013-11-29 Crystal Pharma, S.A.U. Procedimiento para la obtención de 17-espirolactonas en esteroides
DE102009031909B4 (de) 2009-07-01 2017-02-09 Heyl Chemisch-Pharmazeutische Fabrik Gmbh & Co. Kg Verfahren zur Herstellung von Drospirenon aus Prasteron
CN102395596B (zh) 2010-03-16 2013-02-13 台州太法药业有限公司 屈螺酮制备方法
CN101830959B (zh) * 2010-05-27 2012-07-18 杭州龙山化工有限公司 一种曲螺酮的合成方法
US11351122B1 (en) 2010-07-28 2022-06-07 Laboratorios Leon Farma Sa Synthetic progestogens and pharmaceutical compositions comprising the same
AR081670A1 (es) 2010-06-29 2012-10-10 Leon Farma Sa Lab Composicion farmaceutica que comprende drospirenona y kit anticonceptivo
US10849857B2 (en) 2010-07-28 2020-12-01 Laboratorios Leon Farma Sa Pharmaceutical compositions comprising active drugs, contraceptive kits comprising active drugs, and methods of administering the same
US9603860B2 (en) 2010-07-28 2017-03-28 Laboratorios Leon Farma Sa Pharmaceutical compositions comprising active drugs, contraceptive kits comprising active drugs, and methods of administering the same
ES2419663T3 (es) 2010-08-03 2013-08-21 Newchem S.P.A. Métodos para la preparación de Drospirenona y productos intermedios de la misma
WO2012107513A1 (en) 2011-02-10 2012-08-16 Crystal Pharma, S.A.U. Process for obtaining drospirenone
ITMI20111383A1 (it) 2011-07-25 2013-01-26 Ind Chimica Srl Processo per la preparazione di drospirenone
BR112014010590A2 (pt) * 2011-11-04 2017-05-02 Bayer Ip Gmbh 18-metil-6,7-metilen-3-oxo-17-pregn-4-eno-21,17?-carbolactonas, preparações farmacêuticas contendo os compostos mencionados e seu uso na terapia da endometriose
CA2856324C (en) 2011-11-22 2019-08-13 Industriale Chimica S.R.L. Process for the preparation of drospirenone
EP2597101A1 (en) 2011-11-22 2013-05-29 Industriale Chimica S.R.L. Process for the preparation of drospirenone
ES2651145T3 (es) 2013-02-20 2018-01-24 Industriale Chimica S.R.L. Proceso para la preparación de drospirenona
HUE032858T2 (en) 2013-04-12 2017-11-28 Ind Chimica Srl Method for producing drospirenone
JP6827962B2 (ja) 2015-06-23 2021-02-10 ラボラトリオス レオン ファーマ エスエー 過剰体重に影響される女性患者のためのドロスピレノン系避妊薬
EP3108889A1 (en) 2015-06-23 2016-12-28 Philippe Perrin Drospirenone-based contraceptive for a female patient affected with excess weight
CN113387993A (zh) * 2021-07-06 2021-09-14 江西百思康瑞药业有限公司 一种屈螺酮的合成方法
EP4134082A1 (en) 2021-08-12 2023-02-15 Chemo Research, S.L. Method for treating endometriosis and providing effective contraception
WO2023152658A1 (en) 2022-02-10 2023-08-17 Lupin Limited Slow release drospirenone tablet composition
EP4486311A1 (en) 2022-03-01 2025-01-08 Chemo Research, S.L. Chewable oral contraceptive

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DE2652761C2 (de) 1976-11-16 1985-11-21 Schering AG, 1000 Berlin und 4709 Bergkamen 15,16-Methylen-Spirolactone, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
DE3022337A1 (de) * 1980-06-11 1982-01-07 Schering Ag Berlin Und Bergkamen, 1000 Berlin Praeparate zur kontrazeption und zur behandlung gynaekologischer stoerungen
DE3042136A1 (de) * 1980-11-03 1982-06-09 Schering Ag, 1000 Berlin Und 4619 Bergkamen Verfahren zur herstellung von 3 (beta), 7 (beta) -dihydroxy- (delta) (pfeil hoch)5(pfeil hoch) -steroiden
EP0075189B1 (en) * 1981-09-21 1985-08-28 Schering Aktiengesellschaft 3-beta,7-beta,15-alpha-trihydroxy-5-androsten-17-one, its 3,15-dipivalate, and its preparation
DE3414508A1 (de) * 1984-04-13 1985-10-24 Schering AG, 1000 Berlin und 4709 Bergkamen Mehrfach tritiierte steroid-20.17-spirolactone und ihre verwendung als tracersubstanzen
DE3626838A1 (de) * 1986-08-08 1988-02-11 Schering Ag Verfahren zur herstellung von 17(alpha)-pregnan-21,17-carbolactonen
US5106995A (en) * 1989-05-05 1992-04-21 Isp Investments Inc. Production of lactones from diols
DE19633685C1 (de) 1996-08-12 1997-10-09 Schering Ag Verfahren zur Herstellung von Drospirenon (6beta,7beta;15 beta,16beta-Dimethyl-en-3-oxo-17alpha-pregn-4-en-21,17-carbolacton, DRSP) sowie 7alpha-(3-Hydroxy-1-propyl)-6beta,7beta;15beta, 16beta-dimethylen-5beta-androstan-3beta,5,17beta-triol (ZK 92836) und 6beta,7beta;15beta,16beta-dimethylen-5beta-hydroxy-3-oxo-17alpha-androstan-21,17-carbolacton (90965) als Zwischenprodukte des Verfahrens

Also Published As

Publication number Publication date
SI1149840T2 (sl) 2013-08-30
US6933395B1 (en) 2005-08-23
PL187474B1 (pl) 2004-07-30
SK283546B6 (sk) 2003-09-11
SI1149840T1 (sl) 2009-06-30
EP1149840A3 (de) 2004-12-01
DK1149841T3 (da) 2010-03-08
NZ333697A (en) 2000-08-25
AU729149B2 (en) 2001-01-25
EP2168974A3 (de) 2013-03-06
CA2261137C (en) 2005-03-15
EP1149841A3 (de) 2004-12-01
ES2320626T3 (es) 2009-05-27
UA55423C2 (uk) 2003-04-15
PT1149841E (pt) 2010-01-29
AU4014497A (en) 1998-03-06
CN1223662A (zh) 1999-07-21
PT918791E (pt) 2002-09-30
KR100473297B1 (ko) 2005-03-07
EP2168974A2 (de) 2010-03-31
EP1149840A2 (de) 2001-10-31
EP0918791A1 (de) 1999-06-02
DK0918791T3 (da) 2002-07-15
ES2335860T3 (es) 2010-04-06
KR20000029939A (ko) 2000-05-25
EP1149841B1 (de) 2009-10-28
BR9711060A (pt) 1999-08-17
JP2000516226A (ja) 2000-12-05
EP0918791B1 (de) 2002-04-03
HK1021190A1 (en) 2000-06-02
DK1149840T3 (da) 2009-04-27
PL331530A1 (en) 1999-07-19
JP3333524B2 (ja) 2002-10-15
ATE215557T1 (de) 2002-04-15
DE59706887D1 (de) 2002-05-08
ES2438941T3 (es) 2014-07-21
CA2261137A1 (en) 1998-02-19
DE59712991D1 (de) 2009-02-26
BG62776B1 (bg) 2000-07-31
PT1149840E (pt) 2009-03-31
DK1149840T4 (da) 2013-07-01
EP1149840B1 (de) 2009-01-07
ATE446966T1 (de) 2009-11-15
SI0918791T1 (en) 2002-12-31
TR199900262T2 (xx) 1999-03-22
US6121465A (en) 2000-09-19
EP1149840B2 (de) 2013-05-15
ATE420098T1 (de) 2009-01-15
PT2168974E (pt) 2014-08-26
ES2175451T7 (es) 2012-11-19
ES2175451T3 (es) 2002-11-16
ES2438941T1 (es) 2014-01-20
HU223106B1 (hu) 2004-03-29
HUP9903089A3 (en) 2001-07-30
DE59713018D1 (de) 2009-12-10
BG102976A (en) 1999-08-31
SK19499A3 (en) 1999-10-08
DK2168974T3 (da) 2014-08-11
CZ297255B6 (cs) 2006-10-11
EA199900153A1 (ru) 1999-06-24
IS2100B (is) 2006-04-12
WO1998006738A1 (de) 1998-02-19
CZ47099A3 (cs) 1999-05-12
CN1158300C (zh) 2004-07-21
IS4965A (is) 1999-01-29
SI1149841T1 (sl) 2010-02-26
EP1149841A2 (de) 2001-10-31
IL127963A0 (en) 1999-11-30
DK1149840T5 (da) 2013-09-30
IL127963A (en) 2004-06-20
DE19633685C1 (de) 1997-10-09
EA001947B1 (ru) 2001-10-22
EP0918791B3 (de) 2012-01-18
EP0918791B8 (de) 2003-01-08
EP2168974B1 (de) 2014-07-02

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