JPH09505802A - 1,3,5▲(10)▼−エストラトリエンの経口活性誘導体 - Google Patents
1,3,5▲(10)▼−エストラトリエンの経口活性誘導体Info
- Publication number
- JPH09505802A JPH09505802A JP7509336A JP50933695A JPH09505802A JP H09505802 A JPH09505802 A JP H09505802A JP 7509336 A JP7509336 A JP 7509336A JP 50933695 A JP50933695 A JP 50933695A JP H09505802 A JPH09505802 A JP H09505802A
- Authority
- JP
- Japan
- Prior art keywords
- ester
- nitrate
- compound
- trihydroxy
- triene
- 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.)
- Granted
Links
Classifications
-
- 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
- C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
-
- 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
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P5/30—Oestrogens
Landscapes
- 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)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Steroid Compounds (AREA)
- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式: (上式中、 R1 は水素、低級アルキル、シクロアルキルおよび低級アシルから成る群より 選択され; R2 は水素および低級アルキルから成る群より選択され; R3 は水素、ヒドロキシおよび低級アルコキシから成る群より選択され; R4 は水素および低級アルキルから成る群より選択され;そして R5 は水素およびニトレートから成る群より選択される) により表される化合物。 2.R5 がニトレートである、請求項1の化合物。 3.R3 とR4 が水素である、請求項1の化合物。 4.R1 がHである、請求項1の化合物。 5.R1 がアセチルである、請求項1の化合物。 6.R5 がニトレートである、請求項5の化合物。 7.R2 がメチルである、請求項1の化合物。 8.R5 がニトレートである、請求項7の化合物。 9.(+)−3,11β,17β−トリヒドロキシエストラ−1,3,5(10)− トリエン 3−アセテート 11,17−ジニトレートエス テル、 (+)−3,11β,17β−トリヒドロキシエストラ−1,3,5(10)−トリエ ン 11,17−ジニトレートエステル、 (+)−3,11β,17β−トリヒドロキシ−7α−メチルエストラ−1,3,5 (10)−トリエン 3−アセテート 11,17−ジニトレートエステル、 (+)−3,11β,17β−トリヒドロキシ−7α−メチルエストラ−1,3,5 (10)−トリエン 11,17−ジニトレートエステル、および (+)−7α−メチルエストラジオール 17β−ニトレートエステル から成る群より選択される、請求項1の化合物。 10.雌の哺乳動物においてエストロゲン様効果を生じさせるのに有用な医薬組 成物であって、医薬上許容される賦形剤と共に有効量の請求項1の化合物を含ん で成る医薬組成物。 11.前記化合物が (+)−3,11β,17β−トリヒドロキシエストラ−1,3,5(10)−トリエ ン 3−アセテート 11,17−ジニトレートエステル、 (+)−3,11β,17β−トリヒドロキシエストラ−1,3,5(10)−トリエ ン 11,17−ジニトレートエステル、 (+)−3,11β,17β−トリヒドロキシ−7α−メチルエストラ−1,3,5 (10)−トリエン 3−アセテート 11,17−ジニトレートエステル、 (+)−3,11β,17β−トリヒドロキシ−7α−メチルエストラ−1,3,5 (10)−トリエン 11,17−ジニトレートエステル、および (+)−7α−メチルエストラジオール 17β−ニトレートエステル から成る群より選択される、請求項10の医薬組成物。 12.エストロゲン様効果を達成するために雌の哺乳動物を治療する方法であっ て、前記哺乳動物に有効量の請求項10の医薬組成物を投与することを含んで成る 方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/122,853 | 1993-09-17 | ||
US08/122,853 US5554603A (en) | 1993-09-17 | 1993-09-17 | Orally active derivatives of 1,3,5(10)-estratriene |
PCT/US1994/010393 WO1995007925A1 (en) | 1993-09-17 | 1994-09-15 | Orally active derivatives of 1,3,5(10)-estratriene |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH09505802A true JPH09505802A (ja) | 1997-06-10 |
JP3993228B2 JP3993228B2 (ja) | 2007-10-17 |
Family
ID=22405185
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50933695A Expired - Fee Related JP3993228B2 (ja) | 1993-09-17 | 1994-09-15 | 1、3、5▲(10)▼−エストラトリエンの経口活性誘導体 |
Country Status (11)
Country | Link |
---|---|
US (1) | US5554603A (ja) |
EP (1) | EP0719276B1 (ja) |
JP (1) | JP3993228B2 (ja) |
AT (1) | ATE160573T1 (ja) |
AU (1) | AU700576B2 (ja) |
CA (1) | CA2171740C (ja) |
DE (1) | DE69407057T2 (ja) |
DK (1) | DK0719276T3 (ja) |
ES (1) | ES2110258T3 (ja) |
GR (1) | GR3025872T3 (ja) |
WO (1) | WO1995007925A1 (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2013523745A (ja) * | 2010-03-28 | 2013-06-17 | エベストラ・インコーポレイテッド | 膣内薬物送達デバイス |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6548491B2 (en) | 1997-12-24 | 2003-04-15 | Sri International | Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use |
US6054446A (en) * | 1997-12-24 | 2000-04-25 | Sri International | Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use |
US6503896B1 (en) | 1997-12-24 | 2003-01-07 | Sri International | Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use |
DE19906159A1 (de) * | 1999-02-09 | 2000-08-10 | Schering Ag | 16-Hydroxyestratriene als selektiv wirksame Estrogene |
EP1603933A2 (en) * | 2003-03-13 | 2005-12-14 | Nitromed, Inc. | Nitrosated and nitrosylated compounds, compositions and methods of use |
EP1749017A2 (en) * | 2004-05-27 | 2007-02-07 | MIGENIX Corp. | Compounds and methods for cytoprotection |
WO2009111574A2 (en) * | 2008-03-05 | 2009-09-11 | Evestra, Inc. | BISMETHYLENE-17α CARBOLACTONES AND RELATED USES |
CA2725578A1 (en) * | 2008-04-24 | 2009-10-29 | Evestra, Inc. | Oral contraceptive dosage forms comprising a progestogen dispersed in an enteric polymer and further comprising an estrogen |
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 |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1074493A (en) * | 1963-06-12 | 1967-07-05 | Roussel Uclaf | Novel estrane derivatives and processes for preparing them |
FR5241M (ja) * | 1966-02-24 | 1967-07-17 | ||
NL135316C (ja) * | 1966-11-18 | |||
GB1332784A (en) * | 1969-11-21 | 1973-10-03 | Glaxo Lab Ltd | Nitrates of steroid 11 beta-ols |
US3980681A (en) * | 1969-11-21 | 1976-09-14 | Peter Job Sykes | Process for the preparation of 11-β-nitro-oxysteroids |
US4705783A (en) * | 1985-06-25 | 1987-11-10 | Sri International | 9α, 11β-substituted and 11β-substituted estranes |
-
1993
- 1993-09-17 US US08/122,853 patent/US5554603A/en not_active Expired - Lifetime
-
1994
- 1994-09-15 DK DK94928126T patent/DK0719276T3/da active
- 1994-09-15 JP JP50933695A patent/JP3993228B2/ja not_active Expired - Fee Related
- 1994-09-15 DE DE69407057T patent/DE69407057T2/de not_active Expired - Lifetime
- 1994-09-15 WO PCT/US1994/010393 patent/WO1995007925A1/en active IP Right Grant
- 1994-09-15 AU AU77284/94A patent/AU700576B2/en not_active Expired
- 1994-09-15 CA CA002171740A patent/CA2171740C/en not_active Expired - Lifetime
- 1994-09-15 EP EP94928126A patent/EP0719276B1/en not_active Expired - Lifetime
- 1994-09-15 ES ES94928126T patent/ES2110258T3/es not_active Expired - Lifetime
- 1994-09-15 AT AT94928126T patent/ATE160573T1/de not_active IP Right Cessation
-
1998
- 1998-01-12 GR GR980400045T patent/GR3025872T3/el unknown
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2013523745A (ja) * | 2010-03-28 | 2013-06-17 | エベストラ・インコーポレイテッド | 膣内薬物送達デバイス |
Also Published As
Publication number | Publication date |
---|---|
EP0719276A1 (en) | 1996-07-03 |
AU700576B2 (en) | 1999-01-07 |
DE69407057D1 (de) | 1998-01-08 |
CA2171740C (en) | 2005-07-26 |
CA2171740A1 (en) | 1995-03-23 |
US5554603A (en) | 1996-09-10 |
ATE160573T1 (de) | 1997-12-15 |
WO1995007925A1 (en) | 1995-03-23 |
GR3025872T3 (en) | 1998-04-30 |
JP3993228B2 (ja) | 2007-10-17 |
DE69407057T2 (de) | 1998-04-09 |
DK0719276T3 (da) | 1998-08-10 |
AU7728494A (en) | 1995-04-03 |
ES2110258T3 (es) | 1998-02-01 |
EP0719276B1 (en) | 1997-11-26 |
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