CN101568547B - 作为17βHSD抑制剂的被取代的雌三烯衍生物 - Google Patents

作为17βHSD抑制剂的被取代的雌三烯衍生物 Download PDF

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CN101568547B
CN101568547B CN200780048224.8A CN200780048224A CN101568547B CN 101568547 B CN101568547 B CN 101568547B CN 200780048224 A CN200780048224 A CN 200780048224A CN 101568547 B CN101568547 B CN 101568547B
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formula
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compounds
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CN101568547A (zh
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J·梅辛格
B·胡森
U·肖恩
H-H·托勒
P·科斯基米斯
M·昂基拉
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Abbott Healthcare Products BV
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Solvay Pharmaceuticals BV
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/10—Anti-acne agents
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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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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    • A61P5/00—Drugs for disorders of the endocrine system
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    • A61P5/32—Antioestrogens
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    • 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
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  • 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)
CN200780048224.8A 2006-11-30 2007-11-27 作为17βHSD抑制剂的被取代的雌三烯衍生物 Expired - Fee Related CN101568547B (zh)

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 (2)

Publication Number Publication Date
CN101568547A CN101568547A (zh) 2009-10-28
CN101568547B true CN101568547B (zh) 2014-06-25

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CN200780048224.8A Expired - Fee Related CN101568547B (zh) 2006-11-30 2007-11-27 作为17βHSD抑制剂的被取代的雌三烯衍生物

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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)

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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

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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
US6541463B1 (en) * 1998-03-11 2003-04-01 Endorecherche, Inc. Inhibitors of type 5 and type 3 17β-hydroxysteroid dehydrogenase and methods for their use
WO2005047303A2 (en) * 2003-11-12 2005-05-26 Solvay Pharmaceuticals Gmbh NOVEL 17β HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS

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GB0025788D0 (en) * 2000-10-20 2000-12-06 Sterix Ltd Use
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

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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
US6541463B1 (en) * 1998-03-11 2003-04-01 Endorecherche, Inc. Inhibitors of type 5 and type 3 17β-hydroxysteroid dehydrogenase and methods for their use
WO2005047303A2 (en) * 2003-11-12 2005-05-26 Solvay Pharmaceuticals Gmbh NOVEL 17β HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS

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Vanessa Ahmed,et al..Boronic acids as inhibitors of steroid sulfatase.《Bioorganic & Medicinal Chemistry》.2006,第41卷8564-8573. *

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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
JP5264760B2 (ja) 2013-08-14
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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