JP5264760B2 - １７β−ＨＳＤインヒビターとしての置換エストラトリエン誘導体 - Google Patents
１７β−ＨＳＤインヒビターとしての置換エストラトリエン誘導体 Download PDFInfo
- Publication number
- JP5264760B2 JP5264760B2 JP2009538695A JP2009538695A JP5264760B2 JP 5264760 B2 JP5264760 B2 JP 5264760B2 JP 2009538695 A JP2009538695 A JP 2009538695A JP 2009538695 A JP2009538695 A JP 2009538695A JP 5264760 B2 JP5264760 B2 JP 5264760B2
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- alkyl
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- 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.)
- Expired - Fee Related
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- 0 CC(C)CN[C@@](C)C*(C)C Chemical compound CC(C)CN[C@@](C)C*(C)C 0.000 description 15
- OJAWOLWHEQUTDE-UHFFFAOYSA-N Cc1c[n](C)nn1 Chemical compound Cc1c[n](C)nn1 OJAWOLWHEQUTDE-UHFFFAOYSA-N 0.000 description 2
- NPUPLICHXRMWME-PWDJNIGWSA-N CC(CC1)([C@@H](C(CCC(Nc2ncc(C)[s]2)=O)C2)[C@H]3[C@H]1c1ccc(B(O)O)cc1CC3)C2=O Chemical compound CC(CC1)([C@@H](C(CCC(Nc2ncc(C)[s]2)=O)C2)[C@H]3[C@H]1c1ccc(B(O)O)cc1CC3)C2=O NPUPLICHXRMWME-PWDJNIGWSA-N 0.000 description 1
- WOHMEVGISLPSMX-XCXAMNFTSA-N C[C@](CC1)([C@@H]([C@@H](CCCC(N2CCOCC2)=O)C2)[C@H](CCc3c4)[C@H]1c3ccc4C(N)=O)C2=O Chemical compound C[C@](CC1)([C@@H]([C@@H](CCCC(N2CCOCC2)=O)C2)[C@H](CCc3c4)[C@H]1c3ccc4C(N)=O)C2=O WOHMEVGISLPSMX-XCXAMNFTSA-N 0.000 description 1
- JBHCJQHXSMJWAN-VDCFHBLUSA-N C[C@](CC1)([C@@H]([C@@H](CCCC(N2CCOCC2)=O)C2)[C@H]3[C@H]1c1ccc(B(O)O)cc1CC3)C2=O Chemical compound C[C@](CC1)([C@@H]([C@@H](CCCC(N2CCOCC2)=O)C2)[C@H]3[C@H]1c1ccc(B(O)O)cc1CC3)C2=O JBHCJQHXSMJWAN-VDCFHBLUSA-N 0.000 description 1
- TZURBUPZHKQKBZ-XVIQTGGASA-N C[C@](CC1)([C@@H]([C@H](CCC(O)=O)C2)C(CCc3c4)[C@H]1c3ccc4O)C2(F)F Chemical compound C[C@](CC1)([C@@H]([C@H](CCC(O)=O)C2)C(CCc3c4)[C@H]1c3ccc4O)C2(F)F TZURBUPZHKQKBZ-XVIQTGGASA-N 0.000 description 1
- SCRNPEDEBGMDDD-QXFIWZMKSA-N C[C@](CC1)([C@@H]([C@H](CCCC(O)=O)C2)[C@H](CCc3c4)[C@H]1c3ccc4O)C2=O Chemical compound C[C@](CC1)([C@@H]([C@H](CCCC(O)=O)C2)[C@H](CCc3c4)[C@H]1c3ccc4O)C2=O SCRNPEDEBGMDDD-QXFIWZMKSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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-
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- A—HUMAN NECESSITIES
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-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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- A—HUMAN NECESSITIES
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- A—HUMAN NECESSITIES
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- A61P5/00—Drugs for disorders of the endocrine system
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal 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
- C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
-
- 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
- C07J41/0044—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group
-
- 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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06125138.5 | 2006-11-30 | ||
| EP06125138 | 2006-11-30 | ||
| PCT/EP2007/062856 WO2008065100A1 (en) | 2006-11-30 | 2007-11-27 | Substituted estratrien derivatives as 17beta hsd inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010511010A JP2010511010A (ja) | 2010-04-08 |
| JP2010511010A5 JP2010511010A5 (cg-RX-API-DMAC7.html) | 2010-11-18 |
| JP5264760B2 true JP5264760B2 (ja) | 2013-08-14 |
Family
ID=38198108
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009538695A Expired - Fee Related JP5264760B2 (ja) | 2006-11-30 | 2007-11-27 | １７β−ＨＳＤインヒビターとしての置換エストラトリエン誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP2099814A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5264760B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN101568547B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2007327653B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2671075A1 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2009005201A (cg-RX-API-DMAC7.html) |
| RU (1) | RU2453554C2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2008065100A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11072632B2 (en) | 2011-03-25 | 2021-07-27 | UNIVERSITé LAVAL | Inhibitors of 17β-HSD1, 17β-HSD3 and 17β-HSD10 |
| DE102011083725A1 (de) | 2011-09-29 | 2013-04-04 | Bayer Pharma AG | Estra-1,3,5(10),16-tetraen-3-carboxamid-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
| WO2013078413A1 (en) * | 2011-11-22 | 2013-05-30 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Modulators of lipid storage |
| PE20150353A1 (es) | 2012-07-10 | 2015-03-28 | Bayer Pharma AG | Derivados de estra-1,3,5(10),16-tetraeno 3-sustituidos, metodos para su preparacion, preparaciones farmaceuticas que los contienen, asi como su uso para la preparacion de medicamentos |
| ES2678993T3 (es) | 2013-02-21 | 2018-08-21 | Bayer Pharma Aktiengesellschaft | Estra-1,3,5(10),16-tetraeno-3-carboxamidas para la inhibición de la 17beta-hidroxiesteroide deshidrogenada (AKR1C3) |
| TW201512215A (zh) * | 2013-06-25 | 2015-04-01 | Forendo Pharma Ltd | 治療活性雌三烯噻唑衍生物 |
| JP6556125B2 (ja) * | 2013-06-25 | 2019-08-07 | フォレンド ファーマ リミテッド | １７β−ヒドロキシステロイドデヒドロゲナーゼの阻害剤としての治療的に活性な１７−窒素置換エストラトリエンチアゾール誘導体 |
| JP6456373B2 (ja) * | 2013-06-25 | 2019-01-23 | フォレンド ファーマ リミテッド | １７β−ヒドロキシステロイドデヒドロゲナーゼ タイプ１の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体 |
| US10112962B2 (en) * | 2014-07-02 | 2018-10-30 | Xavier University | Boron-based prodrug strategy for increased bioavailability and lower-dosage requirements for drug molecules containing at least one phenol (or aromatic hydroxyl) group |
| CN107207561B (zh) * | 2014-12-23 | 2020-03-31 | 佛恩多制药有限公司 | 17β-HSD1–抑制剂的前药 |
| JP6545266B2 (ja) | 2014-12-23 | 2019-07-17 | フォレンド ファーマ リミテッド | １７β‐ＨＳＤ１抑制剤のプロドラッグ |
| CZ307437B6 (cs) | 2016-06-07 | 2018-08-22 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. | 15β-substituované deriváty estronu jako selektivní inhibitory 17β-hydroxysteoiddehydrogenáz |
| HRP20240679T1 (hr) | 2017-06-08 | 2024-08-16 | Organon R&D Finland Ltd | 17-oksimi 15.beta.-[3-propanamido]-supstituiranih etera-1,3,5(10)-trien-17-ona za uporabu u inhibiciji 17.beta.-hidroksisteroid dehidrogenaza |
| JP7417608B2 (ja) | 2018-12-05 | 2024-01-18 | フォレンド ファーマ リミテッド | １７－ｈｓｄ１阻害剤としての１６（１７）位でピラゾール環と縮合しているエストラ－１，３，５（１０）－トリエン化合物 |
| IT201900004041A1 (it) * | 2019-03-20 | 2020-09-20 | Farmabios Spa | Procedimento per la preparazione di un derivato del fulvestrant |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| GB0025788D0 (en) * | 2000-10-20 | 2000-12-06 | Sterix Ltd | Use |
| TWI331154B (en) * | 2003-11-12 | 2010-10-01 | Solvay Pharm Gmbh | Novel 17-hydroxysteroid dehydrogenase type i inhibitors |
| US8030298B2 (en) * | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
| CN101189251B (zh) * | 2005-05-26 | 2012-09-12 | 索尔瓦药物有限公司 | 17β-HSD1和STS抑制剂 |
-
2007
- 2007-11-27 AU AU2007327653A patent/AU2007327653B2/en not_active Ceased
- 2007-11-27 CA CA002671075A patent/CA2671075A1/en not_active Abandoned
- 2007-11-27 RU RU2009124589/04A patent/RU2453554C2/ru not_active IP Right Cessation
- 2007-11-27 EP EP07847383A patent/EP2099814A1/en not_active Withdrawn
- 2007-11-27 MX MX2009005201A patent/MX2009005201A/es active IP Right Grant
- 2007-11-27 CN CN200780048224.8A patent/CN101568547B/zh not_active Expired - Fee Related
- 2007-11-27 WO PCT/EP2007/062856 patent/WO2008065100A1/en not_active Ceased
- 2007-11-27 JP JP2009538695A patent/JP5264760B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JP2010511010A (ja) | 2010-04-08 |
| RU2453554C2 (ru) | 2012-06-20 |
| AU2007327653B2 (en) | 2013-04-18 |
| WO2008065100A1 (en) | 2008-06-05 |
| AU2007327653A1 (en) | 2008-06-05 |
| EP2099814A1 (en) | 2009-09-16 |
| CN101568547B (zh) | 2014-06-25 |
| HK1134298A1 (en) | 2010-04-23 |
| RU2009124589A (ru) | 2011-01-10 |
| CA2671075A1 (en) | 2008-06-05 |
| CN101568547A (zh) | 2009-10-28 |
| MX2009005201A (es) | 2009-05-27 |
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