JP2007538027A - エストリオール及びエステトロールプロドラッグ類 - Google Patents
エストリオール及びエステトロールプロドラッグ類 Download PDFInfo
- Publication number
- JP2007538027A JP2007538027A JP2007517048A JP2007517048A JP2007538027A JP 2007538027 A JP2007538027 A JP 2007538027A JP 2007517048 A JP2007517048 A JP 2007517048A JP 2007517048 A JP2007517048 A JP 2007517048A JP 2007538027 A JP2007538027 A JP 2007538027A
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- Prior art keywords
- group
- sulfamoylbenzoate
- trien
- compound according
- tert
- Prior art date
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- PROQIPRRNZUXQM-UHFFFAOYSA-N (16alpha,17betaOH)-Estra-1,3,5(10)-triene-3,16,17-triol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4)O)C4C3CCC2=C1 PROQIPRRNZUXQM-UHFFFAOYSA-N 0.000 title claims description 32
- PROQIPRRNZUXQM-ZXXIGWHRSA-N estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 title claims description 32
- 229960001348 estriol Drugs 0.000 title claims description 32
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- 239000000651 prodrug Substances 0.000 title claims description 6
- AJIPIJNNOJSSQC-NYLIRDPKSA-N estetrol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)[C@@H]4O)O)[C@@H]4[C@@H]3CCC2=C1 AJIPIJNNOJSSQC-NYLIRDPKSA-N 0.000 title description 6
- 229950009589 estetrol Drugs 0.000 title description 6
- 150000001875 compounds Chemical class 0.000 claims abstract description 48
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- QMBJSIBWORFWQT-DFXBJWIESA-N Chlormadinone acetate Chemical compound C1=C(Cl)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 QMBJSIBWORFWQT-DFXBJWIESA-N 0.000 claims description 2
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- UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 claims description 2
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- METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 claims description 2
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- METQSPRSQINEEU-HXCATZOESA-N drospirenone Chemical compound C([C@]12[C@H]3C[C@H]3[C@H]3[C@H]4[C@@H]([C@]5(CCC(=O)C=C5[C@@H]5C[C@@H]54)C)CC[C@@]31C)CC(=O)O2 METQSPRSQINEEU-HXCATZOESA-N 0.000 claims description 2
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- 201000010099 disease Diseases 0.000 claims 2
- MZKOZIJYGHDDPN-UHFFFAOYSA-N 2-[tert-butyl(dimethyl)silyl]oxy-4-hydroxy-3-trimethylsilyloxybenzoic acid Chemical compound CC(C)(C)[Si](C)(C)OC1=C(C=CC(=C1O[Si](C)(C)C)O)C(=O)O MZKOZIJYGHDDPN-UHFFFAOYSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims 1
- 229950003621 butoxylate Drugs 0.000 claims 1
- MQWDTXAOPTYTLC-UHFFFAOYSA-N butyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-carboxylate Chemical compound C1CC(C(=O)OCCCC)(C=2C=CC=CC=2)CCN1CCC(C#N)(C=1C=CC=CC=1)C1=CC=CC=C1 MQWDTXAOPTYTLC-UHFFFAOYSA-N 0.000 claims 1
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- 125000002345 steroid group Chemical group 0.000 abstract 1
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- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 25
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Images
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
- A61P15/08—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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P5/26—Androgens
-
- 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
-
- 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
- A61P5/34—Gestagens
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102004025985A DE102004025985A1 (de) | 2004-05-21 | 2004-05-21 | Estriol- und Estetrol-Prodrugs |
| PCT/EP2005/005258 WO2005113576A1 (de) | 2004-05-21 | 2005-05-10 | Aminosulfonyl- oder aminosulfonylamino-substituierte phenyl-ester als estriol-und estetrol-prodrugs |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007538027A true JP2007538027A (ja) | 2007-12-27 |
| JP2007538027A5 JP2007538027A5 (https=) | 2008-06-26 |
Family
ID=34969311
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007517048A Pending JP2007538027A (ja) | 2004-05-21 | 2005-05-10 | エストリオール及びエステトロールプロドラッグ類 |
Country Status (11)
| Country | Link |
|---|---|
| EP (1) | EP1747231A1 (https=) |
| JP (1) | JP2007538027A (https=) |
| AR (1) | AR049108A1 (https=) |
| DE (1) | DE102004025985A1 (https=) |
| GT (1) | GT200500120A (https=) |
| PA (1) | PA8633801A1 (https=) |
| PE (1) | PE20060314A1 (https=) |
| SV (1) | SV2006002122A (https=) |
| TW (1) | TW200612962A (https=) |
| UY (1) | UY28910A1 (https=) |
| WO (1) | WO2005113576A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007538025A (ja) * | 2004-05-21 | 2007-12-27 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | エストラジオールプロドラッグ |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10027887A1 (de) | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| US7534780B2 (en) | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
| DE102005057224A1 (de) * | 2005-11-29 | 2007-05-31 | Bayer Schering Pharma Ag | Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
| DE102005057408A1 (de) * | 2005-11-30 | 2007-05-31 | Bayer Schering Pharma Ag | Sulfamoylsulfonat-Prodrugs |
| CN100396693C (zh) * | 2006-11-08 | 2008-06-25 | 浙江大学 | 1,4-孕二烯-16β-甲基-17α,21-二羟基物的制备方法 |
| CN102079771B (zh) * | 2010-12-10 | 2012-10-03 | 郑州大学 | 具有抗肿瘤活性的雌甾氨基酸酯化合物及其合成方法 |
Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB915129A (en) * | 1958-08-04 | 1963-01-09 | Roussel Uclaf | New steroid compounds and a process for their preparation |
| GB1272688A (en) * | 1968-12-31 | 1972-05-03 | Rech Chimiques Et Ind Mar Lab | Sulphamido-steroids and the preparation thereof |
| WO2001081364A1 (en) * | 2000-04-24 | 2001-11-01 | Kyowa Hakko Kogyo Co., Ltd. | Estra-1,3,5(10)-triene derivatives |
| WO2002000679A2 (en) * | 2000-06-28 | 2002-01-03 | Novartis Ag | 9.alpha.-chloro-6.alpha.-fluoro-17.alpha.-hydroxy-16-methyl-17-beta-methoxycarbonyl-androst-1,4-dienes esterified in position 17.alpha. by a cyclic acyl group |
| JP2003534386A (ja) * | 2000-05-31 | 2003-11-18 | シエーリング アクチエンゲゼルシャフト | スルホンアミド基を有する化合物及びこれらの化合物を含む医薬組成物 |
| WO2005005451A1 (en) * | 2003-07-11 | 2005-01-20 | Glaxo Group Limited | Specific glucocorticosteroid compound having anti- inflammatory activity |
| WO2005047303A2 (en) * | 2003-11-12 | 2005-05-26 | Solvay Pharmaceuticals Gmbh | NOVEL 17β HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS |
| JP2007538025A (ja) * | 2004-05-21 | 2007-12-27 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | エストラジオールプロドラッグ |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5001234A (en) * | 1987-04-16 | 1991-03-19 | The Upjohn Company | Cyclic hydrocarbons with an aminoalkyl sidechain |
| US5116828A (en) * | 1989-10-26 | 1992-05-26 | Nippon Zoki Pharmaceutical Co., Ltd. | Pharmaceutical composition for treatment of osteoporosis |
| US5571933A (en) * | 1994-11-17 | 1996-11-05 | Duquesne University Of The Holy Ghost | Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use |
| DE19712488A1 (de) * | 1997-03-25 | 1998-10-01 | Knoell Hans Forschung Ev | Steroidsulfamate, Verfahren zu ihrer Herstellung und Anwendung derselben |
-
2004
- 2004-05-21 DE DE102004025985A patent/DE102004025985A1/de not_active Ceased
-
2005
- 2005-05-10 WO PCT/EP2005/005258 patent/WO2005113576A1/de not_active Ceased
- 2005-05-10 EP EP05747926A patent/EP1747231A1/de not_active Withdrawn
- 2005-05-10 JP JP2007517048A patent/JP2007538027A/ja active Pending
- 2005-05-19 UY UY28910A patent/UY28910A1/es not_active Application Discontinuation
- 2005-05-20 PA PA20058633801A patent/PA8633801A1/es unknown
- 2005-05-20 PE PE2005000555A patent/PE20060314A1/es not_active Application Discontinuation
- 2005-05-20 AR ARP050102085A patent/AR049108A1/es unknown
- 2005-05-20 TW TW094116505A patent/TW200612962A/zh unknown
- 2005-05-20 GT GT200500120A patent/GT200500120A/es unknown
- 2005-05-23 SV SV2005002122A patent/SV2006002122A/es not_active Application Discontinuation
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB915129A (en) * | 1958-08-04 | 1963-01-09 | Roussel Uclaf | New steroid compounds and a process for their preparation |
| GB1272688A (en) * | 1968-12-31 | 1972-05-03 | Rech Chimiques Et Ind Mar Lab | Sulphamido-steroids and the preparation thereof |
| WO2001081364A1 (en) * | 2000-04-24 | 2001-11-01 | Kyowa Hakko Kogyo Co., Ltd. | Estra-1,3,5(10)-triene derivatives |
| JP2003534386A (ja) * | 2000-05-31 | 2003-11-18 | シエーリング アクチエンゲゼルシャフト | スルホンアミド基を有する化合物及びこれらの化合物を含む医薬組成物 |
| WO2002000679A2 (en) * | 2000-06-28 | 2002-01-03 | Novartis Ag | 9.alpha.-chloro-6.alpha.-fluoro-17.alpha.-hydroxy-16-methyl-17-beta-methoxycarbonyl-androst-1,4-dienes esterified in position 17.alpha. by a cyclic acyl group |
| WO2005005451A1 (en) * | 2003-07-11 | 2005-01-20 | Glaxo Group Limited | Specific glucocorticosteroid compound having anti- inflammatory activity |
| WO2005047303A2 (en) * | 2003-11-12 | 2005-05-26 | Solvay Pharmaceuticals Gmbh | NOVEL 17β HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS |
| JP2007538025A (ja) * | 2004-05-21 | 2007-12-27 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | エストラジオールプロドラッグ |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007538025A (ja) * | 2004-05-21 | 2007-12-27 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | エストラジオールプロドラッグ |
Also Published As
| Publication number | Publication date |
|---|---|
| PE20060314A1 (es) | 2006-05-25 |
| DE102004025985A1 (de) | 2005-12-15 |
| EP1747231A1 (de) | 2007-01-31 |
| SV2006002122A (es) | 2006-05-09 |
| WO2005113576A1 (de) | 2005-12-01 |
| UY28910A1 (es) | 2005-12-30 |
| TW200612962A (en) | 2006-05-01 |
| PA8633801A1 (es) | 2006-03-24 |
| AR049108A1 (es) | 2006-06-28 |
| GT200500120A (es) | 2006-01-24 |
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