ES2175451T3 - Procedimiento para la preparacion de drospirenona y sus productos intermedios. - Google Patents

Procedimiento para la preparacion de drospirenona y sus productos intermedios.

Info

Publication number
ES2175451T3
ES2175451T3 ES97937562T ES97937562T ES2175451T3 ES 2175451 T3 ES2175451 T3 ES 2175451T3 ES 97937562 T ES97937562 T ES 97937562T ES 97937562 T ES97937562 T ES 97937562T ES 2175451 T3 ES2175451 T3 ES 2175451T3
Authority
ES
Spain
Prior art keywords
procedure
drospirenone
preparation
intermediate products
dimetilen
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
ES97937562T
Other languages
English (en)
Other versions
ES2175451T7 (es
Inventor
Jorg-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
Original Assignee
Schering AG
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=ES2175451(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering AG filed Critical Schering AG
Publication of ES2175451T3 publication Critical patent/ES2175451T3/es
Application granted granted Critical
Publication of ES2175451T7 publication Critical patent/ES2175451T7/es
Active 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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pyrane Compounds (AREA)
  • Polyesters Or Polycarbonates (AREA)
  • Fats And Perfumes (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

PROCEDIMIENTO PARA LA PREPARACION DE DROSPIRENONA (6 BE ,7 BE ;15 BE ,16 BE - DIMETILEN - 3 - OXO - 17 AL PREGN - 4 EN - 21,17 - CARBOLACTONA, DRSP) (I) Y 7 AL - (3 - HIDROXI 1 - PROPIL) - 6 BE ,7 BE ;15 BE ,16 BE DIMETILEN - 5 BE - AN DROSTANO - 3 BE ,5,17 BE - TRIOL (ZK 92836), Y 6 BE ,7 BE ;15BE ,16 BE - DIMETILEN - 5 BE HIDROXI - 3 - OXO - 17 AL - A NDROSTAN - 21,17 - CARBOLACTONA (ZK 90965) COMO PRODUCTOS INTERMEDIOS DEL PROCEDIMIENTO.
ES97937562T 1996-08-12 1997-08-11 Procedimiento para la preparacióon de drospirenona y sus productos intermedios. Active ES2175451T7 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19633685 1996-08-12
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

Publications (2)

Publication Number Publication Date
ES2175451T3 true ES2175451T3 (es) 2002-11-16
ES2175451T7 ES2175451T7 (es) 2012-11-19

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)
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.
ES97937562T Active ES2175451T7 (es) 1996-08-12 1997-08-11 Procedimiento para la preparacióon de drospirenona y sus productos intermedios.
ES01250277T Expired - Lifetime ES2320626T5 (es) 1996-08-12 1997-08-11 Procedimiento para la preparación de drospirenona

Family Applications Before (2)

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)
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.

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES01250277T Expired - Lifetime ES2320626T5 (es) 1996-08-12 1997-08-11 Procedimiento para la preparación de drospirenona

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) ATE215557T1 (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) DK1149840T5 (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) PT918791E (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
EP2305267A3 (en) 1999-08-31 2011-08-17 Bayer Schering Pharma Aktiengesellschaft Pharmaceutical combination of ethinylestradiol and drospirenone for use as a contraceptive
JP4354667B2 (ja) 1999-08-31 2009-10-28 バイエル・シエーリング・ファーマ・アクチエンゲゼルシャフト 避妊薬としての使用へのエチニルエストラジオールとドロスピレノンの医薬用組合せ
US6787531B1 (en) * 1999-08-31 2004-09-07 Schering Ag Pharmaceutical composition for use as a contraceptive
KR100913910B1 (ko) * 2000-01-18 2009-08-26 바이엘 쉐링 파마 악티엔게젤샤프트 호르몬 보충 요법용 드로스피렌온
US20020132801A1 (en) * 2001-01-11 2002-09-19 Schering Aktiengesellschaft Drospirenone for hormone replacement therapy
JP2004521951A (ja) 2001-07-13 2004-07-22 シエーリング アクチエンゲゼルシャフト Ｈｒｔのためのドロスピレノン及びエストロゲンスルファメートの組み合わせ
KR20040104632A (ko) 2002-04-26 2004-12-10 쉐링 악티엔게젤샤프트 호르몬 대체 요법을 받는 여성에서 고혈압의 치료
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
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
EP2527356B1 (en) * 2005-07-21 2018-01-03 Bayer Intellectual Property GmbH 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
DE502005004948D1 (de) * 2005-07-21 2008-09-18 Bayer Schering Pharma Ag Verfahren zur Herstellung von 3-Oxo-pregn-4-en-21,17-carbolactonen durch die metallfreie Oxidation von 17-(3-hydroxypropyl)-3,17-dihydroxyandrostanen
US20070255381A1 (en) 2006-04-27 2007-11-01 Peter Meyer 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)
WO2008137050A2 (en) 2007-05-01 2008-11-13 Sicor Inc. A process for preparing drospirenone and intermediate thereof
DE102007030596B3 (de) * 2007-06-28 2009-03-12 Bayer Schering Pharma Aktiengesellschaft Verfahren zur Herstellung von 17-(3-Hydroxypropyl)-17-hydroxysteroiden
WO2009111574A2 (en) * 2008-03-05 2009-09-11 Evestra, Inc. BISMETHYLENE-17α 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
WO2010094623A1 (en) 2009-02-18 2010-08-26 Bayer Schering Pharma Aktiengesellschaft Formulation comprising drospirenone for subcutaneous or intramuscular administration
WO2010094624A1 (en) 2009-02-18 2010-08-26 Bayer Schering 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
WO2011113196A1 (zh) * 2010-03-16 2011-09-22 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
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
US11351122B1 (en) 2010-07-28 2022-06-07 Laboratorios Leon Farma Sa Synthetic progestogens and pharmaceutical compositions comprising 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
EP2597101A1 (en) 2011-11-22 2013-05-29 Industriale Chimica S.R.L. Process for the preparation of drospirenone
PL2782924T3 (pl) 2011-11-22 2017-07-31 Industriale Chimica S.R.L. Proces otrzymywania drospirenonu
WO2014128525A1 (en) 2013-02-20 2014-08-28 Industriale Chimica S.R.L. Process for the preparation of drospirenone
BR112015025816B1 (pt) 2013-04-12 2021-02-02 Industriale Chimica S.R.L processo para a preparação de drospirenona
RS65196B1 (sr) 2015-06-23 2024-03-29 Laboratorios Leon Farma Sa Kontraceptivno sredstvo na bazi drospirenona za pacijentkinje sa viškom težine
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
WO2023165988A1 (en) 2022-03-01 2023-09-07 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
KR20000029939A (ko) 2000-05-25
BG102976A (en) 1999-08-31
NZ333697A (en) 2000-08-25
SI1149840T1 (sl) 2009-06-30
PT918791E (pt) 2002-09-30
CN1158300C (zh) 2004-07-21
IS4965A (is) 1999-01-29
DK2168974T3 (da) 2014-08-11
US6933395B1 (en) 2005-08-23
CZ47099A3 (cs) 1999-05-12
DK1149841T3 (da) 2010-03-08
JP2000516226A (ja) 2000-12-05
EP1149841A3 (de) 2004-12-01
ES2320626T3 (es) 2009-05-27
EP2168974A2 (de) 2010-03-31
KR100473297B1 (ko) 2005-03-07
IL127963A (en) 2004-06-20
HK1021190A1 (en) 2000-06-02
IS2100B (is) 2006-04-12
PT1149841E (pt) 2010-01-29
ATE420098T1 (de) 2009-01-15
EP0918791B1 (de) 2002-04-03
SK283546B6 (sk) 2003-09-11
UA55423C2 (uk) 2003-04-15
CZ297255B6 (cs) 2006-10-11
ES2335860T3 (es) 2010-04-06
PT1149840E (pt) 2009-03-31
SI1149840T2 (sl) 2013-08-30
EA199900153A1 (ru) 1999-06-24
DE59712991D1 (de) 2009-02-26
BR9711060A (pt) 1999-08-17
ES2320626T5 (es) 2013-09-05
HU223106B1 (hu) 2004-03-29
HUP9903089A3 (en) 2001-07-30
EA001947B1 (ru) 2001-10-22
DK1149840T3 (da) 2009-04-27
DE59713018D1 (de) 2009-12-10
SI0918791T1 (en) 2002-12-31
WO1998006738A1 (de) 1998-02-19
TR199900262T2 (xx) 1999-03-22
EP0918791B3 (de) 2012-01-18
ES2438941T3 (es) 2014-07-21
DK1149840T4 (da) 2013-07-01
EP2168974A3 (de) 2013-03-06
PL187474B1 (pl) 2004-07-30
EP1149841A2 (de) 2001-10-31
ES2438941T1 (es) 2014-01-20
EP1149841B1 (de) 2009-10-28
EP1149840B2 (de) 2013-05-15
EP1149840A3 (de) 2004-12-01
EP1149840B1 (de) 2009-01-07
ES2175451T7 (es) 2012-11-19
EP0918791A1 (de) 1999-06-02
BG62776B1 (bg) 2000-07-31
JP3333524B2 (ja) 2002-10-15
EP2168974B1 (de) 2014-07-02
SI1149841T1 (sl) 2010-02-26
DK0918791T3 (da) 2002-07-15
AU729149B2 (en) 2001-01-25
ATE446966T1 (de) 2009-11-15
CN1223662A (zh) 1999-07-21
DE59706887D1 (de) 2002-05-08
EP1149840A2 (de) 2001-10-31
US6121465A (en) 2000-09-19
PT2168974E (pt) 2014-08-26
EP0918791B8 (de) 2003-01-08
PL331530A1 (en) 1999-07-19
CA2261137A1 (en) 1998-02-19
DE19633685C1 (de) 1997-10-09
IL127963A0 (en) 1999-11-30
AU4014497A (en) 1998-03-06
CA2261137C (en) 2005-03-15
DK1149840T5 (da) 2013-09-30
SK19499A3 (en) 1999-10-08
ATE215557T1 (de) 2002-04-15

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