JP2007538025A - エストラジオールプロドラッグ - Google Patents

エストラジオールプロドラッグ Download PDF

Info

Publication number: JP2007538025A
Authority: JP; Japan
Prior art keywords: group; trien; sulfamoylbenzoate; hydroxyestradi; methoxy
Prior art date: 2004-05-21
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.): Pending

Application number

JP2007517046A

Other languages

English (en)

Japanese (ja)

Other versions

JP2007538025A5 (es

Inventor

ビルバ，ラルフ

ドレーシャー，ペーター

リンク，スフェン

エルガー，バルター

シュナイダー，ビルギット

ヒリシュ，アレクサンダー

レデルセン，グドルン

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Bayer Pharma AG

Original Assignee

Bayer Schering Pharma AG

Priority date (The priority date 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 date listed.)

2004-05-21

Filing date

2005-05-10

Publication date

2007-12-27

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34969196&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP2007538025(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2005-05-10 Application filed by Bayer Schering Pharma AG filed Critical Bayer Schering Pharma AG

2007-12-27 Publication of JP2007538025A publication Critical patent/JP2007538025A/ja

2008-06-26 Publication of JP2007538025A5 publication Critical patent/JP2007538025A5/ja

Status Pending legal-status Critical Current

Links

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 title claims description 19
229930182833 estradiol Natural products 0.000 title claims description 19
229960005309 estradiol Drugs 0.000 title claims description 19
239000000651 prodrug Substances 0.000 title claims description 6
229940002612 prodrug Drugs 0.000 title claims description 6
150000001875 compounds Chemical class 0.000 claims abstract description 51
238000004519 manufacturing process Methods 0.000 claims abstract description 8
239000008177 pharmaceutical agent Substances 0.000 claims abstract description 6
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 6
238000000034 method Methods 0.000 claims abstract description 5
239000000262 estrogen Substances 0.000 claims description 52
229940011871 estrogen Drugs 0.000 claims description 51
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 37
229910052739 hydrogen Inorganic materials 0.000 claims description 27
230000000694 effects Effects 0.000 claims description 21
125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 21
-1 trimethylsilyloxy group Chemical group 0.000 claims description 21
HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 18
238000006243 chemical reaction Methods 0.000 claims description 18
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 18
125000005843 halogen group Chemical group 0.000 claims description 17
WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical group OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 12
125000000217 alkyl group Chemical group 0.000 claims description 10
150000003431 steroids Chemical class 0.000 claims description 10
238000011282 treatment Methods 0.000 claims description 10
125000003118 aryl group Chemical group 0.000 claims description 9
229910052731 fluorine Inorganic materials 0.000 claims description 9
125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 8
125000002560 nitrile group Chemical group 0.000 claims description 8
125000004469 siloxy group Chemical group [SiH3]O* 0.000 claims description 8
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 7
239000001257 hydrogen Substances 0.000 claims description 7
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 7
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical group CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 6
229910052801 chlorine Inorganic materials 0.000 claims description 6
125000001153 fluoro group Chemical group F* 0.000 claims description 6
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 6
XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 5
150000003839 salts Chemical class 0.000 claims description 5
XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical group CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims description 4
201000010099 disease Diseases 0.000 claims description 4
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 4
229940088597 hormone Drugs 0.000 claims description 4
239000005556 hormone Substances 0.000 claims description 4
230000005764 inhibitory process Effects 0.000 claims description 4
239000000583 progesterone congener Substances 0.000 claims description 4
NVBFHJWHLNUMCV-UHFFFAOYSA-N sulfamide Chemical compound NS(N)(=O)=O NVBFHJWHLNUMCV-UHFFFAOYSA-N 0.000 claims description 4
KDNIOKSLVIGAAN-UHFFFAOYSA-N 2-sulfamoylbenzoic acid Chemical compound NS(=O)(=O)C1=CC=CC=C1C(O)=O KDNIOKSLVIGAAN-UHFFFAOYSA-N 0.000 claims description 3
206010060862 Prostate cancer Diseases 0.000 claims description 3
208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
239000003418 antiprogestin Substances 0.000 claims description 3
125000001309 chloro group Chemical group Cl* 0.000 claims description 3
MRKZAZMYXYSBDG-UHFFFAOYSA-N cyclopentyl propanoate Chemical group CCC(=O)OC1CCCC1 MRKZAZMYXYSBDG-UHFFFAOYSA-N 0.000 claims description 3
NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical group CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 claims description 3
206010006187 Breast cancer Diseases 0.000 claims description 2
208000026310 Breast neoplasm Diseases 0.000 claims description 2
201000009273 Endometriosis Diseases 0.000 claims description 2
238000002657 hormone replacement therapy Methods 0.000 claims description 2
QAHVHSLSRLSVGS-UHFFFAOYSA-N sulfamoyl chloride Chemical compound NS(Cl)(=O)=O QAHVHSLSRLSVGS-UHFFFAOYSA-N 0.000 claims description 2
FOKNEOPXGZGGBW-UHFFFAOYSA-N sulfamoyl isocyanate Chemical compound NS(=O)(=O)N=C=O FOKNEOPXGZGGBW-UHFFFAOYSA-N 0.000 claims description 2
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230000004064 dysfunction Effects 0.000 claims 1
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230000001076 estrogenic effect Effects 0.000 abstract description 16
125000002345 steroid group Chemical group 0.000 abstract 1
239000000243 solution Substances 0.000 description 39
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UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 25
238000005160 1H NMR spectroscopy Methods 0.000 description 24
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 24
239000000126 substance Substances 0.000 description 23
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 21
210000003743 erythrocyte Anatomy 0.000 description 21
239000000463 material Substances 0.000 description 20
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 19
238000012360 testing method Methods 0.000 description 19
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CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 16
238000001704 evaporation Methods 0.000 description 13
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BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 description 12
BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 description 12
UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 12
235000017557 sodium bicarbonate Nutrition 0.000 description 12
229910000030 sodium bicarbonate Inorganic materials 0.000 description 12
229960002568 ethinylestradiol Drugs 0.000 description 11
230000012010 growth Effects 0.000 description 11
210000002381 plasma Anatomy 0.000 description 11
238000003756 stirring Methods 0.000 description 10
239000000203 mixture Substances 0.000 description 9
239000003826 tablet Substances 0.000 description 9
QOSSAOTZNIDXMA-UHFFFAOYSA-N Dicylcohexylcarbodiimide Chemical compound C1CCCCC1N=C=NC1CCCCC1 QOSSAOTZNIDXMA-UHFFFAOYSA-N 0.000 description 8
229910052943 magnesium sulfate Inorganic materials 0.000 description 8
235000019341 magnesium sulphate Nutrition 0.000 description 8
239000012074 organic phase Substances 0.000 description 8
239000003960 organic solvent Substances 0.000 description 8
FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 description 8
210000004369 blood Anatomy 0.000 description 7
239000008280 blood Substances 0.000 description 7
239000013067 intermediate product Substances 0.000 description 7
239000002244 precipitate Substances 0.000 description 7
102000004881 Angiotensinogen Human genes 0.000 description 6
108090001067 Angiotensinogen Proteins 0.000 description 6
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
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238000002560 therapeutic procedure Methods 0.000 description 6
JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 6
NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonium chloride Substances [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 description 5
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239000004480 active ingredient Substances 0.000 description 5
239000002671 adjuvant Substances 0.000 description 5
235000011114 ammonium hydroxide Nutrition 0.000 description 5
210000000988 bone and bone Anatomy 0.000 description 5
125000004432 carbon atom Chemical group C* 0.000 description 5
239000003981 vehicle Substances 0.000 description 5
XWEBTVZIZWEJOO-UHFFFAOYSA-N 3-chlorosulfonylbenzoyl chloride Chemical compound ClC(=O)C1=CC=CC(S(Cl)(=O)=O)=C1 XWEBTVZIZWEJOO-UHFFFAOYSA-N 0.000 description 4
108010051696 Growth Hormone Proteins 0.000 description 4
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YXYXCSOJKUAPJI-ZBRFXRBCSA-N [(8r,9s,13s,14s,17s)-17-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-yl] sulfamate Chemical compound NS(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 YXYXCSOJKUAPJI-ZBRFXRBCSA-N 0.000 description 4
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229940125904 compound 1 Drugs 0.000 description 4
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DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 description 3
RUOXWQNWRLQUBE-UHFFFAOYSA-N 2-chloro-4-sulfamoylbenzoic acid Chemical compound NS(=O)(=O)C1=CC=C(C(O)=O)C(Cl)=C1 RUOXWQNWRLQUBE-UHFFFAOYSA-N 0.000 description 3
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MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 3
YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
UCAGLBKTLXCODC-UHFFFAOYSA-N carzenide Chemical compound NS(=O)(=O)C1=CC=C(C(O)=O)C=C1 UCAGLBKTLXCODC-UHFFFAOYSA-N 0.000 description 3
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Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Endocrinology (AREA)
Diabetes (AREA)
Reproductive Health (AREA)
Gynecology & Obstetrics (AREA)
Steroid Compounds (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

JP2007517046A 2004-05-21 2005-05-10 エストラジオールプロドラッグ Pending JP2007538025A (ja)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
DE102004025966A DE102004025966A1 (de)	2004-05-21	2004-05-21	Estradiol-Prodrugs
PCT/EP2005/005254 WO2005113574A1 (de)	2004-05-21	2005-05-10	Aminosulfonyl- oder aminosulfonylamino-substituierte phenyl-ester als estradiol-prodrugs

Publications (2)

Publication Number	Publication Date
JP2007538025A true JP2007538025A (ja)	2007-12-27
JP2007538025A5 JP2007538025A5 (es)	2008-06-26

Family

ID=34969196

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2007517046A Pending JP2007538025A (ja)	2004-05-21	2005-05-10	エストラジオールプロドラッグ

Country Status (11)

Country	Link
EP (1)	EP1747230A1 (es)
JP (1)	JP2007538025A (es)
AR (1)	AR050335A1 (es)
DE (1)	DE102004025966A1 (es)
GT (1)	GT200500121A (es)
PA (1)	PA8633701A1 (es)
PE (1)	PE20060359A1 (es)
SV (1)	SV2006002121A (es)
TW (1)	TW200613315A (es)
UY (1)	UY28909A1 (es)
WO (1)	WO2005113574A1 (es)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JP2007538027A (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	エストリオール及びエステトロールプロドラッグ類

Families Citing this family (7)

* Cited by examiner, † Cited by third party
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
DE102005057225A1 (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
EP3019172B1 (en) *	2013-07-11	2019-09-25	Evestra, Inc.	Pro-drug forming compounds
CN115368427B (zh) *	2022-08-17	2024-02-13	南宁师范大学	雌二醇硒氰酸酯类化合物及其制备方法与应用

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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
JP2007538027A (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	エストリオール及びエステトロールプロドラッグ類

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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 DE102004025966A patent/DE102004025966A1/de not_active Withdrawn
2005
- 2005-05-10 JP JP2007517046A patent/JP2007538025A/ja active Pending
- 2005-05-10 EP EP05747458A patent/EP1747230A1/de not_active Withdrawn
- 2005-05-10 WO PCT/EP2005/005254 patent/WO2005113574A1/de not_active Ceased
- 2005-05-19 UY UY28909A patent/UY28909A1/es not_active Application Discontinuation
- 2005-05-20 PE PE2005000557A patent/PE20060359A1/es not_active Application Discontinuation
- 2005-05-20 TW TW094116503A patent/TW200613315A/zh unknown
- 2005-05-20 GT GT200500121A patent/GT200500121A/es unknown
- 2005-05-20 AR ARP050102083A patent/AR050335A1/es unknown
- 2005-05-20 PA PA20058633701A patent/PA8633701A1/es unknown
- 2005-05-23 SV SV2005002121A patent/SV2006002121A/es not_active Application Discontinuation

Patent Citations (8)

* Cited by examiner, † Cited by third party
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
JP2007538027A (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	エストリオール及びエステトロールプロドラッグ類

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JP2007538027A (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	エストリオール及びエステトロールプロドラッグ類

Also Published As

Publication number	Publication date
PA8633701A1 (es)	2006-07-03
GT200500121A (es)	2006-01-30
WO2005113574A1 (de)	2005-12-01
DE102004025966A1 (de)	2005-12-15
AR050335A1 (es)	2006-10-18
PE20060359A1 (es)	2006-05-25
EP1747230A1 (de)	2007-01-31
UY28909A1 (es)	2005-12-30
TW200613315A (en)	2006-05-01
SV2006002121A (es)	2006-02-15

Publication	Publication Date	Title
US7534780B2 (en)	2009-05-19	Estradiol prodrugs
US9096639B2 (en)	2015-08-04	17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-acyloxyalkylene phenyl derivatives, methods for the production thereof and use thereof for treating diseases
JP6130087B1 (ja)	2017-05-17	１７−ヒドロキシ−１７−ペンタフルオロエチル−エストラ−４，９（１０）−ジエン−１１−アリール誘導体、その製造方法、その誘導体を利用した諸疾患の治療
CN103827133B (zh)	2015-11-25	雌甾-1,3,5(10),16-四烯-3-甲酰胺衍生物、其制备方法、包含其的药物制剂及其用于制备药物的用途
CN102834405B (zh)	2015-09-09	孕酮受体拮抗剂
CN102596985B (zh)	2017-05-24	17‑羟基‑17‑五氟乙基‑雌‑4，9(10)‑二烯‑11‑芳基衍生物、其制备方法及其用于治疗疾病的用途
JP2007538025A (ja)	2007-12-27	エストラジオールプロドラッグ
CN102471366B (zh)	2015-12-16	17-羟基-17-五氟乙基雌-4，9(10)-二烯11-苯亚甲基衍生物、其制备方法及其用于治疗疾病的用途
US20050277625A1 (en)	2005-12-15	Estriol and estetrol prodrugs
JP2007538026A (ja)	2007-12-27	アンドロゲン作用を有するステロイドプロドラッグ
JP2007538027A (ja)	2007-12-27	エストリオール及びエステトロールプロドラッグ類
US20050282793A1 (en)	2005-12-22	Steroid prodrugs with androgenic action
JP2009517426A (ja)	2009-04-30	ＥＲβ−選択物質のプロドラッグ類、それらの製造方法、及びそれらの化合物を含む医薬組成物
JP2009517427A (ja)	2009-04-30	ＥＲβ−選択性物質のプロドラッグ、それらを製造する方法およびこれらの化合物を含んでなる医薬組成物
KR20070020454A (ko)	2007-02-21	안드로겐 효과를 가지는 스테로이드 프로드러그
NZ622081B2 (en)	2016-02-02	Estra-1,3,5(10),16-tetraene-3-carboxamide derivatives, process for preparation thereof, pharmaceutical preparations comprising them, and use thereof for production of medicaments
HK1171456B (en)	2015-08-14	17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl derivatives, methods for the production thereof and use thereof for treating diseases
HK1077832B (en)	2010-03-19	17α-ALKYL-17β-OXY-ESTRATRIENES AND INTERMEDIATES FOR THE FRODUCTION THEREOF, AND USE OF SAID 17α-ALKYL-17β-OXY-ESTRATRIENES FOR PRODUCING MEDICAMENTS AND PHARMACEUTICAL PREPARATIONS
HK1079215B (en)	2008-02-06	17α-ALKYL-17β-OXY-ESTRATRIENES, USES THEREOF AND PHARMACEUTICAL PREPARATIONS

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2011-11-02	A02	Decision of refusal	Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20111101

JP2007538025A - エストラジオールプロドラッグ - Google Patents

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Applications Claiming Priority (2)

Publications (2)

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ID=34969196

Family Applications (1)

Country Status (11)

Cited By (1)

Families Citing this family (7)

Citations (8)

Family Cites Families (3)

Patent Citations (8)

Cited By (1)

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