ES2152671T3 - Derivados de progesterona sustituidos en posicion 21 como nuevos agentes antiprogestacionales. - Google Patents

Derivados de progesterona sustituidos en posicion 21 como nuevos agentes antiprogestacionales.

Info

Publication number
ES2152671T3
ES2152671T3 ES97923523T ES97923523T ES2152671T3 ES 2152671 T3 ES2152671 T3 ES 2152671T3 ES 97923523 T ES97923523 T ES 97923523T ES 97923523 T ES97923523 T ES 97923523T ES 2152671 T3 ES2152671 T3 ES 2152671T3
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ES
Spain
Prior art keywords
rent
selected member
treat
group formed
aciloxi
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
ES97923523T
Other languages
English (en)
Inventor
Hyun K Kim
Richard P Blye
Pemmaraju N Rao
James W Cessac
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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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 ES2152671T3 publication Critical patent/ES2152671T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • 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
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/006—Ketals at position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • 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
    • 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
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • 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
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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
    • 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
    • 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
    • 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

Landscapes

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

Abstract

SE DESCRIBE UN COMPUESTO QUE TIENE LA FORMULA GENERAL (I) EN LA QUE R 1 ES UN MIEMBRO SELECCIONADO ENTRE EL GRUPO FORMADO POR - OCH 3 , - SCH 3 , - N(CH 3 ) 2 , NHCH 3 , - CHO, - COCH 3 Y - CHOHCH 3 ; R 2 ES UN MIEMBRO SELECCIONADO ENTRE EL GRUPO FORMADO POR HALOGENO, ALQUILO, ACILO, HIDROXI, ALCOXI, ACILOXI, CARBONATO DE ALQUILO, CIPIONILOXI, S - ALQUILO Y S - ACILO; R 3 ES UN MIEMBRO SELECCIONADO ENTRE EL GRUPO FORMADO POR ALQUILO, HIDROXI, ALCOXI Y ACILOXI; R 4 ES UN MIEMBRO SELECCIONADO ENTRE EL GR UPO FORMADO POR HIDROGENO Y ALQUILO; Y X ES UN MIEMBRO SELECCIONADO ENTRE EL GRUPO FORMADO POR - O Y - N - OR S UP,5 , EN DONDE R 5 ES UN MIEMBRO ELEGIDO ENTRE EL GRUPO FORMADO POR HIDROGENO Y ALQUILO; ADEMAS, A FIN DE OBTENER LOS COMPUESTOS DE FORMULA (I), LA PRESENTE INVENCION PRESENTA PROCEDIMIENTOS EN LOS QUE SE UTILIZAN VENTAJOSAMENTE LOS COMPUESTOS DE FORMULA (I), INTER ALIA, PARA ANTAGONIZAR LA PROGESTERONA ENDOGENA; INDUCIR LA MENSTRUACION, TRATAR LA ENDOMETRIOSIS; TRATAR LA DISMENORREA; TRATAR LOS TUMORES DEPENDIENTES DE LAS HORMONAS ENDOCRINAS; TRATAR LOS FIBROIDES UTERINOS; INHIBIR LA PROLIFERACION ENDOMETRIAL UTERINA; INDUCIR EL PARTO, Y COMO CONTRACEPTIVO.
ES97923523T 1996-05-01 1997-04-30 Derivados de progesterona sustituidos en posicion 21 como nuevos agentes antiprogestacionales. Expired - Lifetime ES2152671T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US1662896P 1996-05-01 1996-05-01

Publications (1)

Publication Number Publication Date
ES2152671T3 true ES2152671T3 (es) 2001-02-01

Family

ID=21778122

Family Applications (1)

Application Number Title Priority Date Filing Date
ES97923523T Expired - Lifetime ES2152671T3 (es) 1996-05-01 1997-04-30 Derivados de progesterona sustituidos en posicion 21 como nuevos agentes antiprogestacionales.

Country Status (13)

Country Link
US (4) US6861415B2 (es)
EP (1) EP0900234B1 (es)
JP (1) JP4260886B2 (es)
AT (1) ATE194358T1 (es)
AU (1) AU710139B2 (es)
CA (2) CA2668824A1 (es)
DE (1) DE69702450T2 (es)
DK (1) DK0900234T3 (es)
ES (1) ES2152671T3 (es)
GR (1) GR3034562T3 (es)
HU (1) HU230492B1 (es)
PT (1) PT900234E (es)
WO (1) WO1997041145A1 (es)

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US6020328A (en) * 1998-03-06 2000-02-01 Research Triangle Institute 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US5962444A (en) * 1998-05-29 1999-10-05 Research Triangle Institute 17β-nitro-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US6262042B1 (en) * 1998-05-29 2001-07-17 Research Triangle Institute 17β-amino and hydroxylamino-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
AR025457A1 (es) * 1999-08-31 2002-11-27 Schering Ag Mesoprogestinas (moduladores de receptores de progesterona) para el tratamiento y la prevencion de trastornos ginecologicos benignos hormona-dependientes
US6740645B1 (en) * 1999-09-03 2004-05-25 Research Triangle Institute 17β-acyl-17α-propynyl-11β-(cyclic amino) aryl steroids and their derivatives having antagonist hormonal properties
US6768014B2 (en) 1999-12-29 2004-07-27 The United States Of America As Represented By The Department Of Health And Human Services PROCESS FOR PREPARING 17α-ACETOXY-11β-[4-N,N(DIMETHYLAMINO)PHENYL]-21-METHOXY-19-NORPREGNA-4,9-DIENE-3,20-DIONE, INTERMEDIATES USEFUL IN THE PROCESS , AND PROCESSES FOR PREPARING SUCH INTERMEDIATES
DK1265911T3 (da) * 2000-03-17 2008-09-29 Us Gov Health & Human Serv 17-alfa-substitueret-11-beta-substitueret-4-aryl og 21-substitueret 19-norpregnadiendion som antiprogestationelle midler
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FR2832065B1 (fr) * 2001-11-13 2004-11-05 Besins Int Belgique Composition pharmaceutique a base de progesterone micronisee son procede de preparation et ses utilisations
US8044223B2 (en) * 2003-04-04 2011-10-25 Bridge Organics Co. Crystalline 19-norsteroids
AU2005265357B2 (en) * 2004-07-09 2011-04-07 Laboratoire Hra Pharma Sustained release compositions containing progesterone receptor modulators
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KR20080055956A (ko) * 2005-09-29 2008-06-19 레프로스 쎄라피우틱스 아이엔씨. 향상된 생체이용률을 가지며, 스테로이드 유도체와폴리글리콜리세드 글리세리드를 포함하는 제제
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US9517240B2 (en) 2006-09-26 2016-12-13 The Regents Of The University Of California Methods and compositions for cancer prevention and treatment
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TWI455716B (zh) * 2006-10-24 2014-10-11 Repros Therapeutics Inc 選擇性黃體激素受體調節劑用於製造治療雌激素依賴性病症之藥物的用途
ES2643318T3 (es) 2006-10-24 2017-11-22 Repros Therapeutics Inc. Composiciones y métodos para suprimir la proliferación endometrial
EA200970646A1 (ru) * 2006-12-28 2009-12-30 Репрос Терапьютикс Инк. Способы и составы для улучшения биодоступности антипрогестинов
HRP20160689T1 (hr) * 2007-04-20 2016-07-15 Preglem S.A. Selektivni modulatori progesterona za tretman uterinog krvarenja
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
US20090118253A1 (en) * 2007-11-05 2009-05-07 Repros Therapeutics Inc. Compositions and methods for treating dysfunctional uterine bleeding
US8299050B2 (en) * 2008-01-29 2012-10-30 Laboratoire Hra-Pharma Method for treating uterine fibroids
TW201002736A (en) * 2008-04-28 2010-01-16 Repros Therapeutics Inc Compositions and methods for treating progesterone-dependent conditions
TWI477276B (zh) * 2008-04-28 2015-03-21 Repros Therapeutics Inc 抗黃體素給藥方案
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
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
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DE102010007722A1 (de) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesteronrezeptorantagonisten
BR112012023281A2 (pt) * 2010-03-22 2016-05-17 Repros Therapeutics Inc composto ou sal do mesmo, composição farmacêutica, métodos para produzir efeito antiprogestacional em paciente e para tratar condição dependente de progesterona e usos de composto ou sal do mesmo farmaceuticamente aceitável do mesmo e de composição
UA113283C2 (xx) * 2010-12-23 2017-01-10 19-норстероїди і їх застосування для лікування прогестеронзалежних станів
EP2664325A1 (en) * 2012-05-16 2013-11-20 PregLem S.A. Methods for preventing or treating androgen mediated diseases
EP2854763B1 (en) 2012-05-31 2018-09-26 Repros Therapeutics Inc. Formulations for vaginal delivery of antiprogestins
CN103772468B (zh) * 2012-10-19 2017-04-05 华润紫竹药业有限公司 醋酸特拉司酮及其中间体的制备方法和用途
JP6343619B2 (ja) 2012-11-02 2018-06-13 レプロス セラピューティクス インコーポレイティド プロゲステロン依存性病態を処置する方法およびその組成物
HU230319B1 (hu) * 2013-10-01 2016-01-28 Richter Gedeon Nyrt. Ipari eljárás szteroid hatóanyagok előállítására
CN104774233A (zh) * 2014-01-13 2015-07-15 上海医药工业研究院 3-(亚乙二氧基)-17β-氰基-17α-三甲基硅氧基-雌-5(10),9(11)-二烯的制备工艺
HU230381B1 (hu) 2014-02-17 2016-03-29 Richter Gedeon Nyrt Ipari eljárás szteroid intermedier előállítására
DE202020102472U1 (de) * 2020-05-04 2020-12-09 Disphar International Bv Orale Form von Mifepriston zur Verwendung bei Zervixreifung und Geburtseinleitung

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US20020025951A1 (en) 2002-02-28
JP4260886B2 (ja) 2009-04-30
HUP9903515A3 (en) 2000-04-28
HU230492B1 (hu) 2016-08-29
DE69702450D1 (de) 2000-08-10
WO1997041145A1 (en) 1997-11-06
HUP9903515A2 (hu) 2000-03-28
EP0900234A1 (en) 1999-03-10
ATE194358T1 (de) 2000-07-15
US7087591B2 (en) 2006-08-08
CA2668824A1 (en) 1997-11-06
CA2253673C (en) 2009-09-08
GR3034562T3 (en) 2001-01-31
US20060276443A1 (en) 2006-12-07
US8003629B2 (en) 2011-08-23
US6861415B2 (en) 2005-03-01
CA2253673A1 (en) 1997-11-06
AU2930497A (en) 1997-11-19
EP0900234B1 (en) 2000-07-05
PT900234E (pt) 2000-12-29
JP2000509396A (ja) 2000-07-25
DK0900234T3 (da) 2000-11-06
US20050143364A1 (en) 2005-06-30
DE69702450T2 (de) 2001-03-08
US7759330B2 (en) 2010-07-20

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