NO20070605L - New 2-substituted D-homoostra-1,3,5 (10) -trienes as inhibitor of 17 (3-hydroxysteroid dehydrogenases type-1). - Google Patents
New 2-substituted D-homoostra-1,3,5 (10) -trienes as inhibitor of 17 (3-hydroxysteroid dehydrogenases type-1).Info
- Publication number
- NO20070605L NO20070605L NO20070605A NO20070605A NO20070605L NO 20070605 L NO20070605 L NO 20070605L NO 20070605 A NO20070605 A NO 20070605A NO 20070605 A NO20070605 A NO 20070605A NO 20070605 L NO20070605 L NO 20070605L
- Authority
- NO
- Norway
- Prior art keywords
- sub
- sup
- trienes
- substituted
- homoostra
- Prior art date
Links
- 102000009878 3-Hydroxysteroid Dehydrogenases Human genes 0.000 title 1
- 108010020420 3-Hydroxysteroid Dehydrogenases Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 102100037426 17-beta-hydroxysteroid dehydrogenase type 1 Human genes 0.000 abstract 1
- 101710147298 17-beta-hydroxysteroid dehydrogenase type 1 Proteins 0.000 abstract 1
- 101710174215 Estradiol 17-beta-dehydrogenase 1 Proteins 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000000262 estrogen Substances 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
-
- 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
- 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
- A61P5/30—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
- A61P5/32—Antioestrogens
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)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
The invention relates to novel 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula (I) wherein R<SUP>2</SUP> represents a C<SUB>1</SUB>-C<SUB>8</SUB> alkyl, a C<SUB>1</SUB>-C<SUB>8</SUB> alkyloxy group or a halogen atom, R<SUP>13</SUP> represents a hydrogen atom or a methyl group, and R<SUP>17</SUP> represents a hydrogen atom or a fluorine atom. The invention also relates to the pharmaceutically acceptable salts of said compounds, to the production thereof, and to the use of the same as medicaments for the prophylaxis and treatment of oestrogen-dependent diseases that can be influenced by the inhibition of 17ß-hydroxysteroid dehydrogenase type 1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102004032673A DE102004032673A1 (en) | 2004-07-02 | 2004-07-02 | New 2-substituted D-homo-estra-1,3,5 (10) -trienes as inhibitors of 17ß-hydroxysteroid dehydrogenase type 1 |
| PCT/EP2005/007314 WO2006003012A1 (en) | 2004-07-02 | 2005-07-04 | NOVEL 2-SUBSTITUTED D-HOMO-ESTRA-1,3,5(10)-TRIENES AS INHIBITORS OF 17ß-HYDROXYSTEROID DEHYDROGENASE TYPE 1 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NO20070605L true NO20070605L (en) | 2007-02-01 |
Family
ID=35106828
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20070605A NO20070605L (en) | 2004-07-02 | 2007-02-01 | New 2-substituted D-homoostra-1,3,5 (10) -trienes as inhibitor of 17 (3-hydroxysteroid dehydrogenases type-1). |
Country Status (24)
| Country | Link |
|---|---|
| EP (1) | EP1763534B1 (en) |
| JP (1) | JP4871274B2 (en) |
| KR (1) | KR20070035059A (en) |
| CN (1) | CN1980949B (en) |
| AT (1) | ATE458744T1 (en) |
| AU (1) | AU2005259329B8 (en) |
| BR (1) | BRPI0511394A (en) |
| CA (1) | CA2571760C (en) |
| CR (1) | CR8854A (en) |
| DE (2) | DE102004032673A1 (en) |
| DK (1) | DK1763534T3 (en) |
| EA (1) | EA011455B1 (en) |
| EC (1) | ECSP077160A (en) |
| ES (1) | ES2340401T3 (en) |
| HR (1) | HRP20100230T1 (en) |
| IL (1) | IL180171A0 (en) |
| MX (1) | MX2007000108A (en) |
| NO (1) | NO20070605L (en) |
| NZ (1) | NZ552515A (en) |
| PL (1) | PL1763534T3 (en) |
| PT (1) | PT1763534E (en) |
| UA (1) | UA92324C2 (en) |
| WO (1) | WO2006003012A1 (en) |
| ZA (1) | ZA200700958B (en) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8030298B2 (en) | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
| US8080540B2 (en) | 2006-09-19 | 2011-12-20 | Abbott Products Gmbh | Therapeutically active triazoles and their use |
| US8288367B2 (en) | 2006-11-30 | 2012-10-16 | Solvay Pharmaceuticals Gmbh | Substituted estratriene derivatives as 17BETA HSD inhibitors |
| DE102007015169A1 (en) | 2007-03-27 | 2008-10-02 | Universität des Saarlandes Campus Saarbrücken | 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-dependent diseases |
| DE102007040243A1 (en) | 2007-08-25 | 2009-02-26 | Universität des Saarlandes | 17beta-hydroxysteriod dehydrogenase type 1 inhibitors for the treatment of hormone-dependent diseases |
| JP6556125B2 (en) | 2013-06-25 | 2019-08-07 | フォレンド ファーマ リミテッド | Therapeutically active 17-nitrogen substituted estratrienthiazole derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase |
| TW201512215A (en) | 2013-06-25 | 2015-04-01 | Forendo Pharma Ltd | Therapeutically active estratrien-thiazole derivatives |
| JP6456373B2 (en) | 2013-06-25 | 2019-01-23 | フォレンド ファーマ リミテッド | 17β-Hydroxysteroid dehydrogenase type 1 inhibitor with therapeutic activity as an estratrienthiazole derivative |
| JP6545266B2 (en) | 2014-12-23 | 2019-07-17 | フォレンド ファーマ リミテッド | Prodrugs of 17.BETA.-HSD1 inhibitors |
| CN107207561B (en) | 2014-12-23 | 2020-03-31 | 佛恩多制药有限公司 | Prodrugs of 17 β -HSD 1-inhibitors |
| CZ307437B6 (en) | 2016-06-07 | 2018-08-22 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. | 15β-substituted estrone derivatives as selective inhibitors of 17β-hydroxysteoid dehydrogenases |
| HRP20240679T1 (en) | 2017-06-08 | 2024-08-16 | Organon R&D Finland Ltd | 17-oximes of 15.beta.-[3-propanamido]-substituted estra-1,3,5(10)-trien-17-ones for use in inhibition of 17.beta.-hydroxysteroid dehydrogenases |
| JP7417608B2 (en) | 2018-12-05 | 2024-01-18 | フォレンド ファーマ リミテッド | Estra-1,3,5(10)-triene compounds fused with a pyrazole ring at the 16(17) position as 17-HSD1 inhibitors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3005835A (en) * | 1960-09-13 | 1961-10-24 | Searle & Co | D-homo-18-norestra-1, 3, 5(10)-trien-17alpha-ones and intermediates thereto |
| GB1346691A (en) * | 1970-06-12 | 1974-02-13 | Inst Khim Prirodnykh Soedineny | Stereospecific method for preparing estrane compounds of natural configuration |
| JPH06279488A (en) * | 1993-03-29 | 1994-10-04 | Kuraray Co Ltd | New steroid derivative and osteoporosis treatment agent |
| HUP0101809A3 (en) * | 1998-03-11 | 2002-07-29 | Endorech Inc Sainte Foy | Inhibitors of type 5 and type 3 17betha-hydroxysteroid dehydrogenase and methods for their use |
| DE10151365A1 (en) * | 2001-10-17 | 2003-04-30 | Schering Ag | New 17-chloro-D-homosteroids, useful as estrogen receptor ligands for female or male contraception or treating benign or malignant proliferative diseases of the ovary |
| JP2004529107A (en) * | 2001-02-27 | 2004-09-24 | シエーリング アクチエンゲゼルシャフト | Use of ERβ-selective ligands to modulate fertility and compounds useful therefor |
| WO2003017973A1 (en) * | 2001-08-31 | 2003-03-06 | Pantarhei Bioscience B.V. | A method of treating benign gynaecological disorders and a drug delivery vehicle for use in such a method |
| DE10307103A1 (en) * | 2003-02-19 | 2004-09-09 | Schering Ag | Anti-tumor effective 2-substituted D-homostra-1,3,5 (10) -trien-3-yl sulfamate |
| DE102004032674A1 (en) * | 2004-07-02 | 2006-01-26 | Schering Ag | New 2-substituted Estra-1,3,5 (10) -triene-17-ones as inhibitors of 17β-hydroxysteroid dehydrogenase type 1 |
-
2004
- 2004-07-02 DE DE102004032673A patent/DE102004032673A1/en not_active Ceased
-
2005
- 2005-04-07 UA UAA200701040A patent/UA92324C2/en unknown
- 2005-07-04 EA EA200700103A patent/EA011455B1/en not_active IP Right Cessation
- 2005-07-04 ES ES05768705T patent/ES2340401T3/en not_active Expired - Lifetime
- 2005-07-04 PL PL05768705T patent/PL1763534T3/en unknown
- 2005-07-04 DE DE502005009091T patent/DE502005009091D1/en not_active Expired - Lifetime
- 2005-07-04 MX MX2007000108A patent/MX2007000108A/en active IP Right Grant
- 2005-07-04 BR BRPI0511394-6A patent/BRPI0511394A/en not_active IP Right Cessation
- 2005-07-04 NZ NZ552515A patent/NZ552515A/en not_active IP Right Cessation
- 2005-07-04 AU AU2005259329A patent/AU2005259329B8/en not_active Expired - Fee Related
- 2005-07-04 JP JP2007518557A patent/JP4871274B2/en not_active Expired - Fee Related
- 2005-07-04 AT AT05768705T patent/ATE458744T1/en active
- 2005-07-04 PT PT05768705T patent/PT1763534E/en unknown
- 2005-07-04 WO PCT/EP2005/007314 patent/WO2006003012A1/en not_active Ceased
- 2005-07-04 CN CN2005800225714A patent/CN1980949B/en not_active Expired - Fee Related
- 2005-07-04 KR KR1020077002617A patent/KR20070035059A/en not_active Ceased
- 2005-07-04 HR HR20100230T patent/HRP20100230T1/en unknown
- 2005-07-04 EP EP05768705A patent/EP1763534B1/en not_active Expired - Lifetime
- 2005-07-04 DK DK05768705.5T patent/DK1763534T3/en active
- 2005-07-04 CA CA2571760A patent/CA2571760C/en not_active Expired - Fee Related
-
2006
- 2006-12-19 IL IL180171A patent/IL180171A0/en unknown
-
2007
- 2007-01-10 EC EC2007007160A patent/ECSP077160A/en unknown
- 2007-01-11 CR CR8854A patent/CR8854A/en not_active Application Discontinuation
- 2007-02-01 ZA ZA200700958A patent/ZA200700958B/en unknown
- 2007-02-01 NO NO20070605A patent/NO20070605L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| IL180171A0 (en) | 2007-06-03 |
| EP1763534B1 (en) | 2010-02-24 |
| EA200700103A1 (en) | 2007-08-31 |
| KR20070035059A (en) | 2007-03-29 |
| AU2005259329B8 (en) | 2011-11-24 |
| CA2571760A1 (en) | 2006-01-12 |
| CR8854A (en) | 2007-08-28 |
| PL1763534T3 (en) | 2010-07-30 |
| HRP20100230T1 (en) | 2010-06-30 |
| HK1103745A1 (en) | 2007-12-28 |
| ES2340401T3 (en) | 2010-06-02 |
| DE502005009091D1 (en) | 2010-04-08 |
| BRPI0511394A (en) | 2007-12-04 |
| EP1763534A1 (en) | 2007-03-21 |
| DK1763534T3 (en) | 2010-05-17 |
| ZA200700958B (en) | 2008-07-30 |
| WO2006003012A1 (en) | 2006-01-12 |
| ECSP077160A (en) | 2007-02-28 |
| AU2005259329A1 (en) | 2006-01-12 |
| DE102004032673A1 (en) | 2006-01-26 |
| JP4871274B2 (en) | 2012-02-08 |
| UA92324C2 (en) | 2010-10-25 |
| JP2008504337A (en) | 2008-02-14 |
| EA011455B1 (en) | 2009-04-28 |
| CN1980949A (en) | 2007-06-13 |
| CA2571760C (en) | 2011-11-22 |
| ATE458744T1 (en) | 2010-03-15 |
| MX2007000108A (en) | 2007-03-09 |
| NZ552515A (en) | 2010-07-30 |
| CN1980949B (en) | 2010-05-05 |
| PT1763534E (en) | 2010-04-27 |
| AU2005259329B2 (en) | 2011-11-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC2A | Withdrawal, rejection or dismissal of laid open patent application |