JP2014500316A - プロゲステロン依存性状態を治療するための新規19−ノルステロイドおよびその使用方法 - Google Patents

プロゲステロン依存性状態を治療するための新規19−ノルステロイドおよびその使用方法 Download PDF

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JP2014500316A
JP2014500316A JP2013546126A JP2013546126A JP2014500316A JP 2014500316 A JP2014500316 A JP 2014500316A JP 2013546126 A JP2013546126 A JP 2013546126A JP 2013546126 A JP2013546126 A JP 2013546126A JP 2014500316 A JP2014500316 A JP 2014500316A
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alkyl
compound
salt
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alkoxy
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JP2014500316A5 (enExample
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ジョセフ エス. ポドルスキ,
ロナルド ディー. ウィール,
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レプロス セラピューティクス インコーポレイティド
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Priority claimed from PCT/US2010/062068 external-priority patent/WO2011119194A1/en
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Publication of JP2014500316A publication Critical patent/JP2014500316A/ja
Publication of JP2014500316A5 publication Critical patent/JP2014500316A5/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/36Antigestagens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J5/00Normal 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
    • C07J5/0046Normal 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
    • C07J5/0053Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001Normal 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
    • C07J7/004Normal 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
    • C07J7/0045Normal 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

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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)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)
JP2013546126A 2010-12-23 2011-09-08 プロゲステロン依存性状態を治療するための新規19−ノルステロイドおよびその使用方法 Withdrawn JP2014500316A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
USPCT/US2010/062068 2010-12-23
PCT/US2010/062068 WO2011119194A1 (en) 2010-03-22 2010-12-23 Compositions and methods for non-toxic delivery of antiprogestins
PCT/US2011/050859 WO2012087389A1 (en) 2010-12-23 2011-09-08 Novel 19-nor-steroids and their use for treating progesterone-dependent conditions

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2016135644A Division JP2016180004A (ja) 2010-12-23 2016-07-08 プロゲステロン依存性状態を治療するための新規19−ノルステロイドおよびその使用方法

Publications (2)

Publication Number Publication Date
JP2014500316A true JP2014500316A (ja) 2014-01-09
JP2014500316A5 JP2014500316A5 (enExample) 2014-10-09

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JP2013546126A Withdrawn JP2014500316A (ja) 2010-12-23 2011-09-08 プロゲステロン依存性状態を治療するための新規19−ノルステロイドおよびその使用方法
JP2016135644A Pending JP2016180004A (ja) 2010-12-23 2016-07-08 プロゲステロン依存性状態を治療するための新規19−ノルステロイドおよびその使用方法

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JP2016135644A Pending JP2016180004A (ja) 2010-12-23 2016-07-08 プロゲステロン依存性状態を治療するための新規19−ノルステロイドおよびその使用方法

Country Status (13)

Country Link
US (1) US20130274234A1 (enExample)
EP (1) EP2655394A1 (enExample)
JP (2) JP2014500316A (enExample)
KR (1) KR20130132955A (enExample)
CN (1) CN103403017A (enExample)
AU (1) AU2011345341B2 (enExample)
CA (1) CA2820877A1 (enExample)
MX (1) MX2013006732A (enExample)
NZ (1) NZ612295A (enExample)
SG (1) SG191207A1 (enExample)
UA (1) UA113283C2 (enExample)
WO (1) WO2012087389A1 (enExample)
ZA (1) ZA201304381B (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201704858PA (en) 2012-05-31 2017-07-28 Repros Therapeutics Inc Formulations and methods for vaginal delivery of antiprogestins
EP2914268B1 (en) * 2012-11-02 2018-07-04 Repros Therapeutics Inc. Methods and compositions for treating progesterone-dependent conditions
MX384159B (es) * 2014-05-05 2025-03-14 Repros Therapeutics Inc Formulaciones y métodos para el suministro vaginal de antiprogestinas.

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0184471A1 (fr) * 1984-11-29 1986-06-11 Roussel-Uclaf Produit comprenant une substance antiprogestomimétique et une substance utérotonique
JPH03505582A (ja) * 1988-06-23 1991-12-05 リサーチ・トライアングル・インスティテゥート 11β―置換プロゲステロン類縁体
US6020328A (en) * 1998-03-06 2000-02-01 Research Triangle Institute 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
JP2000509396A (ja) * 1996-05-01 2000-07-25 アメリカ合衆国 新規の抗プロゲステロンとしての21―置換プロゲステロン誘導体
JP2003529604A (ja) * 2000-03-17 2003-10-07 ザ ガバメント オブ ザ ユナイテッド ステイツ オブ アメリカ, リプレゼンテッド バイ ザ セクレタリー オブ ヘルス アンド ヒューマン サービシーズ 抗プロゲステロン剤としての17−α−置換−11−β−置換−4−アリールおよび21−置換19−ノルプレグナジエンジオン
US6900193B1 (en) * 1996-05-01 2005-05-31 The United States Of America As Represented By The Department Of Health And Human Services Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
WO2009061569A1 (en) * 2007-11-05 2009-05-14 Repros Therapeutics Inc. Compositions and methods for treating dysfunctional uterine bleeding
JP2010507685A (ja) * 2006-10-24 2010-03-11 レプロス セラピューティクス インコーポレイティド 子宮内膜増殖を抑制するための組成物および方法
JP2011518845A (ja) * 2008-04-28 2011-06-30 レプロス セラピューティクス インコーポレイティド 抗プロゲスチンの投薬処方計画
JP2011518883A (ja) * 2008-04-28 2011-06-30 レプロス セラピューティクス インコーポレイティド 乳癌を治療するための組成物および方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2521565B1 (fr) 1982-02-17 1985-07-05 Dior Sa Parfums Christian Melange pulverulent de constituants lipidiques et de constituants hydrophobes, procede pour le preparer, phases lamellaires lipidiques hydratees et procede de fabrication, compositions pharmaceutiques ou cosmetiques comportant des phases lamellaires lipidiques hydratees
FR2534487B1 (fr) 1982-10-15 1988-06-10 Dior Christian Parfums Procede d'homogeneisation de dispersions de phases lamellaires lipidiques hydratees, et suspensions obtenues par ce procede
ATE151286T1 (de) 1983-11-14 1997-04-15 Columbia Lab Inc Bioadhäsive mittel
US5077211A (en) 1988-07-06 1991-12-31 Applied Genetics, Inc. Purification and administration of dna repair enzymes

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0184471A1 (fr) * 1984-11-29 1986-06-11 Roussel-Uclaf Produit comprenant une substance antiprogestomimétique et une substance utérotonique
JPH03505582A (ja) * 1988-06-23 1991-12-05 リサーチ・トライアングル・インスティテゥート 11β―置換プロゲステロン類縁体
JP2000509396A (ja) * 1996-05-01 2000-07-25 アメリカ合衆国 新規の抗プロゲステロンとしての21―置換プロゲステロン誘導体
US6861415B2 (en) * 1996-05-01 2005-03-01 The United States Of America As Represented By The Department Of Health And Human Services 21-substituted progesterone derivatives as new antiprogestational agents
US6900193B1 (en) * 1996-05-01 2005-05-31 The United States Of America As Represented By The Department Of Health And Human Services Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
US6020328A (en) * 1998-03-06 2000-02-01 Research Triangle Institute 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
JP2002505334A (ja) * 1998-03-06 2002-02-19 リサーチ・トライアングル・インスティチュート アゴニスト又はアンタゴニストホルモン特性を有する20−ケト−11β−アリールステロイドとその誘導体
JP2003529604A (ja) * 2000-03-17 2003-10-07 ザ ガバメント オブ ザ ユナイテッド ステイツ オブ アメリカ, リプレゼンテッド バイ ザ セクレタリー オブ ヘルス アンド ヒューマン サービシーズ 抗プロゲステロン剤としての17−α−置換−11−β−置換−4−アリールおよび21−置換19−ノルプレグナジエンジオン
JP2010507685A (ja) * 2006-10-24 2010-03-11 レプロス セラピューティクス インコーポレイティド 子宮内膜増殖を抑制するための組成物および方法
WO2009061569A1 (en) * 2007-11-05 2009-05-14 Repros Therapeutics Inc. Compositions and methods for treating dysfunctional uterine bleeding
JP2011518845A (ja) * 2008-04-28 2011-06-30 レプロス セラピューティクス インコーポレイティド 抗プロゲスチンの投薬処方計画
JP2011518883A (ja) * 2008-04-28 2011-06-30 レプロス セラピューティクス インコーポレイティド 乳癌を治療するための組成物および方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JPN6015028263; Curr. Opin. Obstet. Gynecol. 21, 2009, 318-324 *
JPN6015028265; Steroids 63, 1998, 50-57 *

Also Published As

Publication number Publication date
AU2011345341B2 (en) 2016-10-20
US20130274234A1 (en) 2013-10-17
WO2012087389A1 (en) 2012-06-28
EP2655394A1 (en) 2013-10-30
AU2011345341A1 (en) 2013-07-04
NZ612295A (en) 2014-07-25
CA2820877A1 (en) 2012-06-28
SG191207A1 (en) 2013-07-31
JP2016180004A (ja) 2016-10-13
MX2013006732A (es) 2013-07-17
ZA201304381B (en) 2014-03-26
CN103403017A (zh) 2013-11-20
UA113283C2 (xx) 2017-01-10
KR20130132955A (ko) 2013-12-05

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