JP5061109B2 - 抗性腺刺激剤としての9,11−コルテキソロンのC3−C1017α−エステル類 - Google Patents
抗性腺刺激剤としての9,11−コルテキソロンのC3−C1017α−エステル類 Download PDFInfo
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- JP5061109B2 JP5061109B2 JP2008530439A JP2008530439A JP5061109B2 JP 5061109 B2 JP5061109 B2 JP 5061109B2 JP 2008530439 A JP2008530439 A JP 2008530439A JP 2008530439 A JP2008530439 A JP 2008530439A JP 5061109 B2 JP5061109 B2 JP 5061109B2
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P15/08—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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- 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
- A61P15/16—Masculine contraceptives
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Reproductive Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Pregnancy & Childbirth (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
i)性腺刺激ホルモンの分泌を抑制し、その結果として男性ホルモンの生成を抑制すること;
ii)アンドロゲン類からそれらの生理学的に活性な代謝物への変換をブロックすること;
iii)組織内におけるアンドロゲン類の直接的作用を阻害すること
である(非特許文献1参照)。
体重50〜60gを有する両性のウィスターラットを使用した。オスを去勢し、その翌日に、未去勢のメスと体側に沿って外科的に一体化した(パラビオーシス)。この実験手順において、オスの去勢は、その体内において即時の性腺刺激ホルモンの過分泌を誘起し、その性腺刺激ホルモンは、パラビオーゼ結合を介してメスに到達した際に卵巣の成長を刺激する。パラビオーシスの日から開始して、オスへの皮下注射によって、1mgおよび5mgの用量にて9,11−デヒドロコルテキソロン17α−ブチレート、およびその類似体(コルテキソロン17α−プロピオネート)を毎日注射した。正の対照としてプロゲステロンを使用し、同様の手順によって、0.5mgおよび2mgの用量にて投与した。
第1表は、9,11−デヒドロコルテキソロン17α−ブチレートが、性腺刺激ホルモンの分泌に対して、用量に相関して強力かつ著しい阻害効果を有することを示す。この効果は、パラビオーゼ結合中のメスの卵巣の重量の%減少から明らかであり、1mgの試験化合物を投与した場合に59%減少し、および5mgの同化合物を投与した場合に96%減少する。
Claims (12)
- 前記医薬が性腺刺激ホルモンの分泌に関連する疾患の治療に用いられる請求項1に記載の使用。
- 前記医薬が計画的に投与することができる請求項1または2に記載の使用。
- 前記計画的方法が:注射可能な溶液および/または懸濁液、タブレット、カプセル、ペレット、経口投与用溶液および/または懸濁液、小球、鼻用スプレー、膣用座薬、および他の座薬から選択される請求項3に記載の使用。
- 前記医薬が、単位用量あたり0.1mgから1000mgまで変化する量で投与される請求項3または4に記載の使用。
- 前記医薬が、単位用量あたり0.5mgから500mgまで変化する量で投与される請求項5に記載の使用。
- 前記医薬が局所的に投与することができる請求項1または2に記載の使用。
- 前記局所的方法が:クリーム、軟膏、ローション、ゲル、皮膚用スプレーおよび/または経皮吸収パッチから選択される請求項7に記載の使用。
- 前記医薬が、0.01質量%から25質量%まで変化する量で投与される請求項7または8に記載の使用。
- 前記医薬が、0.01質量%から2質量%まで変化する量で投与される請求項9に記載の使用。
- 注射可能な溶液および/または懸濁液、タブレット、カプセル、ペレット、経口投与用溶液および/または懸濁液、経皮吸収パッチ、座薬、小球、膣用座薬、クリーム、軟膏、ローション、皮膚用および/または鼻用スプレー、および/またはゲルの形態にある請求項11に記載の薬剤配合物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IT001695A ITMI20051695A1 (it) | 2005-09-14 | 2005-09-14 | Uso di 17a-esteri c3-c10 del 9,11-deidrocortexolone cme agenti anti-gonadotropinici |
ITMI2005A001695 | 2005-09-14 | ||
PCT/EP2006/062995 WO2007031349A1 (en) | 2005-09-14 | 2006-06-08 | Use of c3-c10 17alfa-esters of 9,11-dehydrocortexolone as anti-gonadotrophic agents. |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2009507879A JP2009507879A (ja) | 2009-02-26 |
JP5061109B2 true JP5061109B2 (ja) | 2012-10-31 |
Family
ID=37134232
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2008530439A Expired - Fee Related JP5061109B2 (ja) | 2005-09-14 | 2006-06-08 | 抗性腺刺激剤としての9,11−コルテキソロンのC3−C1017α−エステル類 |
Country Status (11)
Country | Link |
---|---|
US (1) | US20090023696A1 (ja) |
EP (1) | EP1959965A1 (ja) |
JP (1) | JP5061109B2 (ja) |
KR (1) | KR20080056719A (ja) |
CN (1) | CN101267826B (ja) |
AU (1) | AU2006291445A1 (ja) |
CA (1) | CA2622502A1 (ja) |
IL (1) | IL190045A0 (ja) |
IT (1) | ITMI20051695A1 (ja) |
NZ (1) | NZ566580A (ja) |
WO (1) | WO2007031349A1 (ja) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ITMI20071616A1 (it) | 2007-08-03 | 2009-02-04 | Cosmo Spa | Processo enzimatico per l'ottenimento di 17-alfa monoesteri del cortexolone e/o suoi 9,11-deidroderivati. |
EP3006453A1 (en) | 2014-10-08 | 2016-04-13 | Cosmo Technologies Ltd. | 17alpha-monoesters and 17alpha,21-diesters of cortexolone for use in the treatment of tumors |
EP3108879A1 (en) | 2015-06-25 | 2016-12-28 | Cassiopea S.p.A. | High concentration formulation |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3780177A (en) * | 1967-06-16 | 1973-12-18 | Warner Lambert Co | 17-butyrate,21-ester derivatives of 6alpha,9alpha-difluoroprednisolone,compositions and use |
ITMI20011762A1 (it) * | 2001-08-10 | 2003-02-10 | Cosmo Spa | Esteri di 17alfa,21-diidrossipregnene, loro uso come agenti anti-androgenetici e procedimenti per la loro preparazione |
-
2005
- 2005-09-14 IT IT001695A patent/ITMI20051695A1/it unknown
-
2006
- 2006-06-08 US US12/066,754 patent/US20090023696A1/en not_active Abandoned
- 2006-06-08 KR KR1020087007295A patent/KR20080056719A/ko not_active Application Discontinuation
- 2006-06-08 NZ NZ566580A patent/NZ566580A/en not_active IP Right Cessation
- 2006-06-08 EP EP06777284A patent/EP1959965A1/en not_active Withdrawn
- 2006-06-08 JP JP2008530439A patent/JP5061109B2/ja not_active Expired - Fee Related
- 2006-06-08 WO PCT/EP2006/062995 patent/WO2007031349A1/en active Application Filing
- 2006-06-08 CN CN200680033517.4A patent/CN101267826B/zh not_active Expired - Fee Related
- 2006-06-08 CA CA002622502A patent/CA2622502A1/en not_active Abandoned
- 2006-06-08 AU AU2006291445A patent/AU2006291445A1/en not_active Abandoned
-
2008
- 2008-03-10 IL IL190045A patent/IL190045A0/en unknown
Also Published As
Publication number | Publication date |
---|---|
JP2009507879A (ja) | 2009-02-26 |
CA2622502A1 (en) | 2007-03-22 |
NZ566580A (en) | 2011-03-31 |
ITMI20051695A1 (it) | 2007-03-15 |
AU2006291445A1 (en) | 2007-03-22 |
KR20080056719A (ko) | 2008-06-23 |
CN101267826A (zh) | 2008-09-17 |
US20090023696A1 (en) | 2009-01-22 |
CN101267826B (zh) | 2010-12-01 |
IL190045A0 (en) | 2008-12-29 |
WO2007031349A1 (en) | 2007-03-22 |
EP1959965A1 (en) | 2008-08-27 |
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