JPH10507741A - エストラ−1,3,5(10)−トリエン誘導体を含有する医薬製剤 - Google Patents
エストラ−1,3,5(10)−トリエン誘導体を含有する医薬製剤Info
- Publication number
- JPH10507741A JPH10507741A JP8506899A JP50689996A JPH10507741A JP H10507741 A JPH10507741 A JP H10507741A JP 8506899 A JP8506899 A JP 8506899A JP 50689996 A JP50689996 A JP 50689996A JP H10507741 A JPH10507741 A JP H10507741A
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- JP
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- Prior art keywords
- hydroxy
- trien
- estradi
- estra
- group
- 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.)
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
- C07J53/002—Carbocyclic rings fused
- C07J53/004—3 membered carbocyclic 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
-
- 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
-
- 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
-
- 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
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- 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
- A61P15/12—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
- A61P15/18—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
-
- 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
- A61P5/18—Drugs for disorders of the endocrine system of the parathyroid 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.有効成分として、C3位に、一般式 R−SO2−O− 式中、Rは基R1R2Nであり、ここで、 R1およびR2は互いに独立し、水素原子、C1−C5アルキル基またはN原子と一 緒になってC原子4ないし6個を含むポリメチレンイミノ基もしくはモルホリノ 基を示す で示される基を有するエストラ−1,3,5(10)−トリエン誘導体を含有す る医薬製剤。 2.一般式I: 式中、Rは基R1R2Nであり、ここで、 R1およびR2は互いに独立し、水素原子、C1−C5アルキル基またはN原子と一 緒になってC原子4ないし6個を含むポリメチレンイミノ基もしくはモルホリノ 基を示し、 R3は水素原子、ヒドロキシ基またはC原子1ないし5個を含むアルコキシ基で あり、 R4は水素原子またはC1−C5アルキル基であり、 R5は水素原子、ヒドロキシ基、エステル化されたヒドロキシ基、1ないし5C 原子を含むハロアルキルまたはアルコキシ基であり、 R6およびR7は水素原子であるか、または一緒になってメチレン基を形成し、 R8、R9およびR10は、互いに独立し、水素原子またはヒドロキシ基であり、 B環は所望により1または2個の二重結合を含み、または、所望により、 R9は炭素原子5個以下を含むアルキニル基であり、または R9およびR10は一緒になって酸素原子を形成し、または R6およびR9はビニレンまたはエチレン基を示す で示される有効成分を含有することを特徴とする、請求項1記載の医薬製剤。 3.17β−ヒドロキシ−エストラ−1,3,5(10)−トリエン−3−イ ルスルファメート、 17β−ヒドロキシ−エストラ−1,3,5(10)−トリエン−3−イル N ,N−ジエチルスルファメート、 17β−ヒドロキシ−エストラ−1,3,5(10)−トリエン−3−イル N ,N−ジメチルスルファメート、 17β−ヒドロキシ−エストラ−1,3,5(10),7−テトラエン−3−イ ル N,N−ジエチルスルファメート、 17β−ヒドロキシ−エストラ−1,3,5(10),6,8−ペンタエン−3 −イル N,N−ジメチルスルファメート、 17−オキソ−エストラ−1,3,5(10)−トリエン−3−イル スルファ メート、 17−オキソ−エストラ−1,3,5(10)−トリエン−3−イル N,N− ジメチルスルファメート、 17−オキソ−エストラ−1,3,5(10)−トリエン−3−イル N,N− ジエチルスルファメート、 16α,17β−ジヒドロキシ−エストラ−1,3,5(10)−トリエン−3 −イル スルファメート、 16α,17β−ジヒドロキシ−エストラ−1,3,5(10)−トリエン−3 −イルN,N−ジメチルスルファメート、 16α,17β−ジヒドロキシ−エストラ−1,3,5(10)−トリエン−3 −イル N,N−ジエチルスルファメート、 2,17β−ジヒドロキシ−エストラ−1,3,5(10)−トリエン−3−イ ル N,N−ジメチルスルファメート、 2−メトキシ−17β−ヒドロキシ−エストラ−1,3,5(10)−トリエン −3−イル N,N−ジエチルスルファメート、 17β−ヒドロキシ−19−ノル−17α−プレグナ−1,3,5(10)−ト リエン−20−イン−3−イル スルファメート、 17β−ヒドロキシ−19−ノル−17α−プレグナ−1,3,5(10)−ト リエン−20−イン−3−イル N−メチルスルファメート、 17β−ヒドロキシ−19−ノル−17α−プレグナ−1,3,5(10)−ト リエン−20−イン−3−イル N,N−ジメチルスルファメート、 17β−ヒドロキシ−19−ノル−17α−プレグナ−1,3,5(10)−ト リエン−20−イン−3−イル N,N−ジエチルスルファメート、 17β−ヒドロキシ−19−ノル−17α−プレグナ−1,3,5(10)−ト リエン−20−イン−3−イル ピロリジノスルホネート、 17β−ヒドロキシ−14α,15α−メチレン−エストラ−1,3,5(10 )−トリエン−3−イル N,N−ジメチルスルファメート、 17β−ヒドロキシ−14α,15α−メチレン−エストラ−1,3,5(10 )−トリエン−3−イル N,N−ジエチルスルファメート、 17β−ヒドロキシ−14α,15α−メチレン−エストラ−1,3,5(10 )−トリエン−3−イル ピロリジノスルホネート、 17β−ヒドロキシ−14α,15α−メチレン−エストラ−1,3,5(10 )−トリエン−3−イル モルホリノスルホネート、 17β−ヒドロキシ−14α,15α−メチレン−エストラ−1,3,5(10 )−トリエン−3−イル N−メチルスルファメート、 17β−ヒドロキシ−14α,15α−メチレン−エストラ−1,3,5(10 )−トリエン−3−イル スルファメート、 17β−ヒドロキシ−14α,15α−メチレン−エストラ−1,3,5(10 ),7−テトラエン−3−イル N,N−ジメチルスルファメート、 17β−ヒドロキシ−14α,15α−メチレン−エストラ−1,3,5(10 ) ,6,8−ペンタエン−3−イル N,N−ジエチルスルファメート、 17β−ヒドロキシ−14α,15α−メチレン−エストラ−1,3,5(10 ),8−テトラエン−3−イル N,N−ジメチルスルファメート、 11β−クロロメチル−17β−ヒドロキシ−エストラ−1,3,5(10)− トリエン−3−イル N,N−ジメチルスルファメート、 17β−ヒドロキシ−14α,17α−ビニレン−エストラ−1,3,5(10 )−トリエン−3−イル N,N−ジエチルスルファメート、 14α,17α−エチレン−17β−ヒドロキシ−エストラ−1,3,5(10 )−トリエン−3−イル ピロリジノスルホネート、 16α,17β−ジヒドロキシ−14α,17α−エチレン−エストラ−1,3 ,5(10)−トリエン−3−イル N,N−ジエチルスルファメート、 17β−ヒドロキシ−7α−メチル−エストラ−1,3,5(10)−トリエン −3,11β−ジイル 3−N,N−ジメチルスルファメート−11−ニトレー ト、および 17β−ヒドロキシ−11β−メトキシ−19−ノル−17α−プレグナ−1, 3,5(10)−トリエン−20−イン−3−イル N,N−ジメチルスルファ メート を含有することを特徴とする、請求項1または2記載の医薬製剤。 4.錠剤、制御放出性錠剤、ロゼンジ、丸剤、カプセル剤、フィルム錠および 制御放出性フィルム錠の形である、請求項1ないし3の何れか1項に記載のエス トラ−1,3,5(10)−トリエン誘導体を含有する医薬製剤。 5.ホルモン性避妊、更年期ホルモン代償療法、並びに乳癌および前立腺癌の ような婦人病および男性病の処置用のものである、上記請求項の何れか1項に記 載の医薬製剤。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE4429398A DE4429398C2 (de) | 1994-08-09 | 1994-08-09 | Verwendung von Estra-1,3,5(10)-trien-Derivaten zur hormonalen Kontrazeption |
DE4429398.4 | 1994-08-09 | ||
PCT/DE1995/000879 WO1996005217A1 (de) | 1994-08-09 | 1995-07-03 | Pharmazeutische zusammensetzungen mit estra-1,3,5(10)-trien-derivaten |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH10507741A true JPH10507741A (ja) | 1998-07-28 |
JP4023820B2 JP4023820B2 (ja) | 2007-12-19 |
Family
ID=6526061
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50689996A Expired - Lifetime JP4023820B2 (ja) | 1994-08-09 | 1995-07-03 | エストラ−1,3,5(10)−トリエン誘導体を含有する医薬製剤 |
Country Status (23)
Country | Link |
---|---|
US (2) | US6569844B1 (ja) |
EP (1) | EP0775156B1 (ja) |
JP (1) | JP4023820B2 (ja) |
KR (1) | KR100243537B1 (ja) |
CN (1) | CN1160404A (ja) |
AT (1) | ATE248853T1 (ja) |
AU (1) | AU2974295A (ja) |
BG (1) | BG63273B1 (ja) |
BR (1) | BR9508868A (ja) |
CA (1) | CA2196678A1 (ja) |
CZ (1) | CZ289452B6 (ja) |
DE (4) | DE4429398C2 (ja) |
DK (1) | DK0775156T3 (ja) |
ES (1) | ES2206515T3 (ja) |
IL (1) | IL114780A0 (ja) |
MY (1) | MY114394A (ja) |
NO (1) | NO970569L (ja) |
PL (1) | PL181636B1 (ja) |
PT (1) | PT775156E (ja) |
RU (1) | RU2179442C2 (ja) |
SK (1) | SK283644B6 (ja) |
UA (1) | UA48143C2 (ja) |
WO (1) | WO1996005217A1 (ja) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2005501849A (ja) * | 2001-08-13 | 2005-01-20 | シエーリング アクチエンゲゼルシャフト | 抗腫瘍性として活性な2−アルコキシエストラジオール・スルファメート |
JP2006517947A (ja) * | 2003-02-19 | 2006-08-03 | シエーリング アクチエンゲゼルシャフト | 抗腫瘍活性2−置換18a−ホモエストラ−1,3,5(10)−トリエン−3−イルスルファメート |
JP2009298797A (ja) * | 1998-04-17 | 2009-12-24 | Ortho Mcneil Pharmaceut Inc | 葉酸を含有する製薬学的組成物並びに関連する方法及び送達系 |
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GB9625334D0 (en) * | 1996-12-05 | 1997-01-22 | Imperial College | Compound |
US6642220B1 (en) | 1996-12-05 | 2003-11-04 | Sterix Limited | Compounds that inhibit oestrone sulphatase; compositions thereof; and methods employing the same |
DE19712488A1 (de) | 1997-03-25 | 1998-10-01 | Knoell Hans Forschung Ev | Steroidsulfamate, Verfahren zu ihrer Herstellung und Anwendung derselben |
DE19753363A1 (de) * | 1997-12-02 | 1999-06-10 | Jenapharm Gmbh | 15-Methyl-cyclopropanosteroide und Verfahren zu ihrer Herstellung |
DE19821831A1 (de) * | 1998-05-15 | 1999-11-18 | Jenapharm Gmbh | Pharmazeutische Präparate zur gezielten Substitution des Estrogenmangels im Zentralnervensystem |
DE19834931A1 (de) * | 1998-07-28 | 2000-02-24 | Jenapharm Gmbh | Verwendung von biogenen Estrogenen zur Hormonsubstitutionstherapie |
DE19906152B4 (de) | 1999-02-10 | 2005-02-10 | Jenapharm Gmbh & Co. Kg | Wirkstoffhaltige Laminate für Transdermalsysteme |
CA2383650A1 (en) | 1999-08-31 | 2001-04-19 | Jenapharm Gmbh & Co. Kg | Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives |
DE10027887A1 (de) * | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
GB0025788D0 (en) * | 2000-10-20 | 2000-12-06 | Sterix Ltd | Use |
JP2004521951A (ja) | 2001-07-13 | 2004-07-22 | シエーリング アクチエンゲゼルシャフト | Hrtのためのドロスピレノン及びエストロゲンスルファメートの組み合わせ |
US8026229B2 (en) * | 2001-08-13 | 2011-09-27 | Sterix Limited | Antitumor-active 2-alkoxyestradiol sulfamates |
TWI252111B (en) * | 2001-12-14 | 2006-04-01 | Solvay Pharm Gmbh | Matrix film tablet with controlled release of a natural mixture of conjugated estrogens |
EP1358882A1 (en) * | 2002-04-30 | 2003-11-05 | Schering Aktiengesellschaft | Use of estriol sulfamate prodrugs for the treatment of autoimmune diseases |
DE10307104A1 (de) | 2003-02-19 | 2004-09-23 | Schering Ag | Antitumor wirksame 2-substituierte Estra-1,3,5(10)-trien-3-yl sulfamate |
DE10307103A1 (de) * | 2003-02-19 | 2004-09-09 | Schering Ag | Antitumor wirksame 2-substituierte D-Homostra-1,3,5(10)-trien-3-yl sulfamate |
EP1603933A2 (en) * | 2003-03-13 | 2005-12-14 | Nitromed, Inc. | Nitrosated and nitrosylated compounds, compositions and methods of use |
US7534780B2 (en) * | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
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US20070197488A1 (en) * | 2005-11-29 | 2007-08-23 | Olaf Peters | Prodrugs of ERbeta-selective substances, process for their production, and pharmaceutical compositions that contain these compounds |
US20070123500A1 (en) * | 2005-11-29 | 2007-05-31 | Gerd Mueller | Prodrugs of ERbeta-selective substances, processes for their preparation and pharmaceutical compositions comprising these compounds |
US20070135399A1 (en) * | 2005-11-30 | 2007-06-14 | Ralf Wyrwa | Heteroaromatic sulphonamide prodrugs |
US20070135375A1 (en) * | 2005-11-30 | 2007-06-14 | Ralf Wyrwa | Sulfamoyl sulfonate prodrugs |
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CN105753924B (zh) * | 2016-02-03 | 2017-11-10 | 中国药科大学 | 新型甾体类选择性雌激素受体调节剂、其制备方法及其医药用途 |
US10624903B2 (en) | 2017-10-19 | 2020-04-21 | Evestra, Inc. | Longer-acting progestin prodrug contraceptives |
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RU2087479C1 (ru) * | 1989-11-29 | 1997-08-20 | Шеринг Аг | Эстратриены, содержащие мостик |
GB9118478D0 (en) * | 1991-08-29 | 1991-10-16 | Imperial College | Steroid sulphatase inhibitors |
JP2700595B2 (ja) * | 1992-05-21 | 1998-01-21 | 呉羽化学工業株式会社 | アゾール誘導体を含有する抗アロマターゼ剤 |
DE4222316A1 (de) * | 1992-07-03 | 1994-01-05 | Schering Ag | Verfahren zur Herstellung von Etheno- und Ethano-16â,17µ-Steroiddiolen und deren Derivaten |
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1994
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1995
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- 1995-07-03 AU AU29742/95A patent/AU2974295A/en not_active Abandoned
- 1995-07-03 BR BR9508868A patent/BR9508868A/pt not_active Application Discontinuation
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1997
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2009298797A (ja) * | 1998-04-17 | 2009-12-24 | Ortho Mcneil Pharmaceut Inc | 葉酸を含有する製薬学的組成物並びに関連する方法及び送達系 |
JP2009298796A (ja) * | 1998-04-17 | 2009-12-24 | Ortho Mcneil Pharmaceut Inc | 葉酸を含有する製薬学的組成物並びに関連する方法及び送達系 |
JP2005501849A (ja) * | 2001-08-13 | 2005-01-20 | シエーリング アクチエンゲゼルシャフト | 抗腫瘍性として活性な2−アルコキシエストラジオール・スルファメート |
JP2006517947A (ja) * | 2003-02-19 | 2006-08-03 | シエーリング アクチエンゲゼルシャフト | 抗腫瘍活性2−置換18a−ホモエストラ−1,3,5(10)−トリエン−3−イルスルファメート |
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