KR101364412B1 - 17β-ＨＳＤ1 및 ＳＴＳ 억제제들 - Google Patents

17β-ＨＳＤ1 및 ＳＴＳ 억제제들 Download PDF

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KR101364412B1
KR101364412B1 KR1020077028969A KR20077028969A KR101364412B1 KR 101364412 B1 KR101364412 B1 KR 101364412B1 KR 1020077028969 A KR1020077028969 A KR 1020077028969A KR 20077028969 A KR20077028969 A KR 20077028969A KR 101364412 B1 KR101364412 B1 KR 101364412B1
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South Korea
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alkyl
group
estra
hydroxy
optionally substituted
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KR20080012960A (ko
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요세프 매싱어
하인리히-후버트 토울
베티나 후센
파시 코스키미에스
리라 피르카라
미카엘 베스케
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애보트 프러덕츠 게엠베하
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0052—Nitrogen only at position 16(17)
    • 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
    • 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
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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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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
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    • A61P13/08—Drugs for disorders of the urinary system of the prostate
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    • A61P27/02—Ophthalmic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/00—Drugs for disorders of the endocrine system
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    • A61P5/28—Antiandrogens
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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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
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0057—Nitrogen and oxygen
    • C07J71/0068—Nitrogen and oxygen at position 16(17)

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  • 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)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020077028969A 2005-05-26 2006-05-24 17β-ＨＳＤ1 및 ＳＴＳ 억제제들 Expired - Fee Related KR101364412B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP05104534 2005-05-26
EP05104534.2 2005-05-26
PCT/EP2006/062587 WO2006125800A1 (en) 2005-05-26 2006-05-24 17β-HSD1 AND STS INHIBITORS

Publications (2)

Publication Number Publication Date
KR20080012960A KR20080012960A (ko) 2008-02-12
KR101364412B1 true KR101364412B1 (ko) 2014-02-21

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KR1020077028969A Expired - Fee Related KR101364412B1 (ko) 2005-05-26 2006-05-24 17β-ＨＳＤ1 및 ＳＴＳ 억제제들

Country Status (15)

Country Link
EP (1) EP1888615B1 (cg-RX-API-DMAC7.html)
JP (1) JP5268635B2 (cg-RX-API-DMAC7.html)
KR (1) KR101364412B1 (cg-RX-API-DMAC7.html)
CN (2) CN101189251B (cg-RX-API-DMAC7.html)
AU (1) AU2006251154B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0611623A2 (cg-RX-API-DMAC7.html)
CA (1) CA2609726C (cg-RX-API-DMAC7.html)
ES (1) ES2388297T3 (cg-RX-API-DMAC7.html)
IL (1) IL187620A (cg-RX-API-DMAC7.html)
MX (1) MX2007014736A (cg-RX-API-DMAC7.html)
NO (1) NO20076616L (cg-RX-API-DMAC7.html)
RU (1) RU2412196C2 (cg-RX-API-DMAC7.html)
UA (1) UA92348C2 (cg-RX-API-DMAC7.html)
WO (1) WO2006125800A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA200709854B (cg-RX-API-DMAC7.html)

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US8080540B2 (en) 2006-09-19 2011-12-20 Abbott Products Gmbh Therapeutically active triazoles and their use
AU2007327653B2 (en) * 2006-11-30 2013-04-18 Solvay Pharmaceuticals Gmbh Substituted estratrien derivatives as 17beta HSD inhibitors
US8288367B2 (en) 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
US11072632B2 (en) 2011-03-25 2021-07-27 UNIVERSITé LAVAL Inhibitors of 17β-HSD1, 17β-HSD3 and 17β-HSD10
SG195118A1 (en) 2011-06-01 2013-12-30 Estetra S A Process for the production of estetrol intermediates
PT2714712T (pt) 2011-06-01 2016-11-08 Estetra Sprl Processo para a produção de intermediários de estetrol
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
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
TW201512215A (zh) 2013-06-25 2015-04-01 Forendo Pharma Ltd 治療活性雌三烯噻唑衍生物
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
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
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
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
LT3310346T (lt) 2015-06-18 2021-06-10 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio
LT3310345T (lt) 2015-06-18 2021-06-25 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio
DK3701944T3 (da) 2015-06-18 2022-03-14 Estetra Srl Oro-dispergerbar doseringsenhed indeholdende en estetrolkomponent
CR20180042A (es) 2015-06-18 2018-05-03 Mithra Pharmaceuticals S A Unidad de dosificación orodispersable que contiene un componente estetrol.
CN105963301B (zh) * 2016-04-26 2018-12-28 兰州大学 以人fkbp51蛋白为靶点的先导化合物及筛选方法与应用
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
KR102712911B1 (ko) 2016-08-05 2024-10-04 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 월경통 및 생리통의 관리방법
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
TWI801561B (zh) 2018-04-19 2023-05-11 比利時商依思特拉私人有限責任公司 化合物及其用於緩解絕經相關症狀的用途
CN111989105B (zh) 2018-04-19 2024-07-19 埃斯特拉私人有限责任公司 化合物以及它们在缓解绝经相关症状中的用途
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
TWI893101B (zh) 2020-04-16 2025-08-11 比利時商埃斯特拉有限責任公司 具有降低之副作用之避孕組成物
US20240082208A1 (en) * 2021-01-08 2024-03-14 Industry-Academic Cooperation Foundation, Yonsei University Antiviral pharmaceutical composition comprising steroid sulfatase inhibitor

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Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
EP0367576A2 (en) * 1988-10-31 1990-05-09 Endorecherche Inc. Estrogen nucleus derivatives for use in the inhibition of sex steroid activity

Non-Patent Citations (1)

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Title
Poirier D. et. al, Tetrahedron, Vol. 47, No. 37, pages 7751-7766 *

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BRPI0611623A2 (pt) 2010-09-21
JP5268635B2 (ja) 2013-08-21
EP1888615B1 (en) 2012-05-16
ZA200709854B (en) 2009-03-25
CA2609726A1 (en) 2006-11-30
RU2007147416A (ru) 2009-07-10
KR20080012960A (ko) 2008-02-12
CA2609726C (en) 2013-10-01
ES2388297T3 (es) 2012-10-11
AU2006251154A1 (en) 2006-11-30
IL187620A0 (en) 2008-03-20
AU2006251154B2 (en) 2012-06-28
IL187620A (en) 2014-03-31
MX2007014736A (es) 2008-02-15
CN102796160A (zh) 2012-11-28
HK1117538A1 (en) 2009-01-16
JP2008545678A (ja) 2008-12-18
CN101189251A (zh) 2008-05-28
WO2006125800A1 (en) 2006-11-30
RU2412196C2 (ru) 2011-02-20
NO20076616L (no) 2008-02-01
CN101189251B (zh) 2012-09-12
EP1888615A1 (en) 2008-02-20
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