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ES2546291T3 - 17-Alfa-sustituida, 11-beta-sustituida-4-arilo y 21-sustituida 19-norpregnadienodionas como agentes antiprogestacionales - Google Patents

17-Alfa-sustituida, 11-beta-sustituida-4-arilo y 21-sustituida 19-norpregnadienodionas como agentes antiprogestacionales Download PDF

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Publication number
ES2546291T3
ES2546291T3 ES10010646.7T ES10010646T ES2546291T3 ES 2546291 T3 ES2546291 T3 ES 2546291T3 ES 10010646 T ES10010646 T ES 10010646T ES 2546291 T3 ES2546291 T3 ES 2546291T3
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ES
Spain
Prior art keywords
substituted
norpregnadienodiones
beta
aryl
alpha
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
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ES10010646.7T
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English (en)
Inventor
Hyun K. Kim
Richard P. Blye
Pemmaraju N. Rao
James W. Cessas
Carmie K. Acosta
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US Department of Health and Human Services
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US Department of Health and Human Services
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Filing date
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Priority claimed from US09/526,855 external-priority patent/US6900193B1/en
Application filed by US Department of Health and Human Services filed Critical US Department of Health and Human Services
Application granted granted Critical
Publication of ES2546291T3 publication Critical patent/ES2546291T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • 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
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P5/36—Antigestagens
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0016—Oximes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
    • C07J7/0045—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/0085—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by an halogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuesto que tienen la fórmula general:**Fórmula** en la que R1 es -C(O)CH3; R2 es acetoxi; R3 es acetoxi; R4 es etilo; y X es >=O; R1 es -C(O)CH3; R2 es -SAc; R3 es acetoxi; R4 es metilo; y X es >=O; R1 es -C(O)CH3; R2 es metoxi; R3 es metoxi; R4 es metilo; y X es >=O; R1 es -C(O)CH3; R2 es metoxi; R3 es acetoxi; R4 es metilo; X es >=O; R1 es -C(O)CH3; R2 es H; R3 es OH; R4 es metilo; y X es >=O; R1 es -C(O)CH3; R2 es Br; R3 es OH; R4 es metilo; y X es >=O; R1 es -C(O)CH3; R2 es acetoxi; R3 es OH; R4 es metilo; y X es >=O; R1 es -C(O)CH3; R2 es -SAc; R3 es OH; R4 es metilo; y X es >=O; o R1 es -C(O)CH3; R2 es metoxi; R3 es OH; R4 es metilo; y X es >=O.

Description

imagen1

Claims (1)

  1. imagen1
ES10010646.7T 2000-03-17 2001-03-16 17-Alfa-sustituida, 11-beta-sustituida-4-arilo y 21-sustituida 19-norpregnadienodionas como agentes antiprogestacionales Expired - Lifetime ES2546291T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/526,855 US6900193B1 (en) 1996-05-01 2000-03-17 Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
US526855 2000-03-17

Publications (1)

Publication Number Publication Date
ES2546291T3 true ES2546291T3 (es) 2015-09-22

Family

ID=24099075

Family Applications (3)

Application Number Title Priority Date Filing Date
ES10010646.7T Expired - Lifetime ES2546291T3 (es) 2000-03-17 2001-03-16 17-Alfa-sustituida, 11-beta-sustituida-4-arilo y 21-sustituida 19-norpregnadienodionas como agentes antiprogestacionales
ES01918812T Expired - Lifetime ES2307604T3 (es) 2000-03-17 2001-03-16 19-norpregnadienodiona 17-a sustituidos, 11-b-sustituido-4-arilo y 21-sustituidos como nuevos agentes antiprogestacionales.
ES10010647.5T Expired - Lifetime ES2546336T3 (es) 2000-03-17 2001-03-16 19-norpregnadienodiona 17-alfa-sustituida, 11-beta-sustituida-4-arilo y 21-sustituida como agentes antiprogestacionales

Family Applications After (2)

Application Number Title Priority Date Filing Date
ES01918812T Expired - Lifetime ES2307604T3 (es) 2000-03-17 2001-03-16 19-norpregnadienodiona 17-a sustituidos, 11-b-sustituido-4-arilo y 21-sustituidos como nuevos agentes antiprogestacionales.
ES10010647.5T Expired - Lifetime ES2546336T3 (es) 2000-03-17 2001-03-16 19-norpregnadienodiona 17-alfa-sustituida, 11-beta-sustituida-4-arilo y 21-sustituida como agentes antiprogestacionales

Country Status (11)

Country Link
EP (4) EP2033965A3 (es)
JP (2) JP5417562B2 (es)
AT (1) ATE396197T1 (es)
AU (2) AU4584901A (es)
CA (1) CA2403756C (es)
CY (1) CY1108281T1 (es)
DE (1) DE60134126D1 (es)
DK (1) DK1265911T3 (es)
ES (3) ES2546291T3 (es)
PT (1) PT1265911E (es)
WO (1) WO2001074840A2 (es)

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ES2546291T3 (es) * 2000-03-17 2015-09-22 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services 17-Alfa-sustituida, 11-beta-sustituida-4-arilo y 21-sustituida 19-norpregnadienodionas como agentes antiprogestacionales
ES2212912B1 (es) * 2003-01-22 2005-10-01 Crystal Pharma, S.A. Procedimiento para la obtencion de 17alfa-acetoxi-11beta-(4-n,n-dimetilaminofenil)-19-norpregna-4,9-dien-3,20-diona.
WO2007103510A2 (en) * 2006-03-08 2007-09-13 Danco Laboratories Llc Methods, dosing regimens & medications using anti-progestational agents for the treatment of disorders
MX343130B (es) * 2006-10-24 2016-10-26 Repros Therapeutics Inc Composiciones y métodos para suprimir la proliferación endometrial.
HU228636B1 (en) 2007-06-27 2013-04-29 Richter Gedeon Nyrt Industrial method for the synthesis of 17-acetoxy-11betha-4[-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione and the key intermediates of the process
TW201002736A (en) * 2008-04-28 2010-01-16 Repros Therapeutics Inc Compositions and methods for treating progesterone-dependent conditions
TWI539953B (zh) * 2008-04-28 2016-07-01 瑞波若斯治療學公司 用於治療乳癌之組成物和方法
TWI477276B (zh) 2008-04-28 2015-03-21 Repros Therapeutics Inc 抗黃體素給藥方案
HUP0900171A2 (hu) 2009-03-20 2010-12-28 Richter Gedeon Nyrt 17-acetoxi-11ß-[4-(dimetil-amino)-fenil]-21-metoxi-19-norpregna-4,9-dién-3,20-dion új kristályos módosulata és eljárás elõállítására
PT2419108T (pt) * 2009-04-14 2016-11-07 Hra Pharma Lab Método para contracepção quando necessária
HUP0900487A2 (hu) 2009-08-05 2011-03-28 Richter Gedeon Nyrt 17-acetoxi-11ß-[4-(dimetil-amino)-fenil]-21-metoxi-19-norpregna-4,9-dién-3,20-dion új kristályos polimorf módosulata és eljárás elõállítására
UA113283C2 (xx) * 2010-12-23 2017-01-10 19-норстероїди і їх застосування для лікування прогестеронзалежних станів
CN102516345B (zh) * 2011-11-01 2014-11-26 上海优拓医药科技有限公司 醋酸乌利司他及其关键中间体的制备方法
US9109005B2 (en) * 2012-02-23 2015-08-18 Boehringer Ingelheim International Gmbh Method for manufacturing of ciclesonide
BR112014029131B1 (pt) 2012-05-31 2021-03-09 Allergan Pharmaceuticals International Limited cápsula de mucoadesivo
CN102702296B (zh) * 2012-06-19 2014-09-03 山东诚创医药技术开发有限公司 环-3,20-双(1,2-亚乙基缩醛)-17α-羟基-17β-乙酰基-雌甾-5(10),9(11)-二烯-3-酮的制备方法
CN102942612A (zh) * 2012-10-30 2013-02-27 四川大学 一种合成醋酸乌利司他的新方法
HK1211852A1 (en) 2012-11-02 2016-06-03 Repros Therapeutics Inc. Methods and compositions for treating progesterone-dependent conditions
CN103073612B (zh) * 2013-02-04 2015-11-04 山东大学 醋酸乌利司他关键中间体的制备方法
HU230319B1 (hu) * 2013-10-01 2016-01-28 Richter Gedeon Nyrt. Ipari eljárás szteroid hatóanyagok előállítására
CN104774231A (zh) * 2014-01-13 2015-07-15 上海医药工业研究院 17α-羟基-19-去甲孕甾-4,9-二烯-3,20-二酮的制备工艺
HU230381B1 (hu) 2014-02-17 2016-03-29 Richter Gedeon Nyrt Ipari eljárás szteroid intermedier előállítására
CN107840865A (zh) * 2016-09-20 2018-03-27 天津金耀集团有限公司 一种甲泼尼龙的制备方法

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Also Published As

Publication number Publication date
ES2307604T3 (es) 2008-12-01
EP2348031A2 (en) 2011-07-27
WO2001074840A3 (en) 2002-05-02
ES2546336T3 (es) 2015-09-22
EP2348030B1 (en) 2015-05-06
DK1265911T3 (da) 2008-09-29
JP2003529604A (ja) 2003-10-07
DE60134126D1 (de) 2008-07-03
CA2403756A1 (en) 2001-10-11
JP2012051935A (ja) 2012-03-15
EP2348031B9 (en) 2016-08-10
CY1108281T1 (el) 2014-02-12
ATE396197T1 (de) 2008-06-15
AU2001245849B2 (en) 2007-01-04
AU4584901A (en) 2001-10-15
EP2348031B1 (en) 2015-06-17
EP1265911B1 (en) 2008-05-21
EP1265911A2 (en) 2002-12-18
EP2033965A2 (en) 2009-03-11
PT1265911E (pt) 2008-10-09
EP2348030A2 (en) 2011-07-27
EP2348030A3 (en) 2012-05-09
EP2348031A3 (en) 2012-05-09
WO2001074840A2 (en) 2001-10-11
EP2033965A3 (en) 2012-09-19
CA2403756C (en) 2010-02-09
JP5417562B2 (ja) 2014-02-19

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