MA38694A2 - Dérivés thérapeutiquement actifs d'estratriène-thiazole à substitution azote en position 17 en tant qu'inhibiteurs de la 17bêta.-hydroxystéroïde déshydrogénase - Google Patents

Dérivés thérapeutiquement actifs d'estratriène-thiazole à substitution azote en position 17 en tant qu'inhibiteurs de la 17bêta.-hydroxystéroïde déshydrogénase

Info

Publication number
MA38694A2
MA38694A2 MA38694A MA38694A MA38694A2 MA 38694 A2 MA38694 A2 MA 38694A2 MA 38694 A MA38694 A MA 38694A MA 38694 A MA38694 A MA 38694A MA 38694 A2 MA38694 A2 MA 38694A2
Authority
MA
Morocco
Prior art keywords
substituted
inhibitors
17beta
natrium
therapeutically active
Prior art date
Application number
MA38694A
Other languages
English (en)
Other versions
MA38694B1 (fr
Inventor
Maire Eloranta
Leena Hirvelae
Lauri Kangas
Pasi Koskimies
Risto Lammintausta
Mikko Unkila
Original Assignee
Forendo Pharma Ltd
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.)
Filing date
Publication date
Application filed by Forendo Pharma Ltd filed Critical Forendo Pharma Ltd
Publication of MA38694A2 publication Critical patent/MA38694A2/fr
Publication of MA38694B1 publication Critical patent/MA38694B1/fr

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036Nitrogen-containing hetero ring
    • C07J71/0042Nitrogen only
    • C07J71/0052Nitrogen only at position 16(17)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036Nitrogen-containing hetero ring
    • C07J71/0057Nitrogen and oxygen
    • C07J71/0068Nitrogen and oxygen at position 16(17)

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

L'invention concerne des composés de formule (i) et des sel pharmaceutiquement acceptables de ceux-ci, dans laquelle r2 à r7 sont tels que définis dans les revendications. L'invention concerne en outre leur utilisation en tant qu'inhibiteurs de la 17ß-hsd et pour le traitement ou la prévention de maladies ou troubles dépendant des hormones stéroïdes, tels que des maladies ou troubles dépendant des hormones stéroïdiennes exigeant l'inhibition de l'enzyme 17ß-hsd1 et/ou exigeant la réduction de la concentration en estradiol endogène. La présente invention concerne également la préparation des composés susmentionnés et de compositions pharmaceutiques comprenant en tant que principe(s) actif(s) un ou plusieurs des composés susmentionnés ou leurs sels pharmaceutiquement acceptables.
MA38694A 2013-06-25 2014-06-25 Dérivés thérapeutiquement actifs d'estratriène-thiazole à substitution azote en position 17 en tant qu'inhibiteurs de la 17bêta.-hydroxystéroïde déshydrogénase MA38694B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FI20135694 2013-06-25
PCT/FI2014/050518 WO2014207310A1 (fr) 2013-06-25 2014-06-25 Dérivés thérapeutiquement actifs d'estratriène-thiazole à substitution azote en position 17 en tant qu'inhibiteurs de la 17bêta.-hydroxystéroïde déshydrogénase

Publications (2)

Publication Number Publication Date
MA38694A2 true MA38694A2 (fr) 2017-12-29
MA38694B1 MA38694B1 (fr) 2020-01-31

Family

ID=51220584

Family Applications (1)

Application Number Title Priority Date Filing Date
MA38694A MA38694B1 (fr) 2013-06-25 2014-06-25 Dérivés thérapeutiquement actifs d'estratriène-thiazole à substitution azote en position 17 en tant qu'inhibiteurs de la 17bêta.-hydroxystéroïde déshydrogénase

Country Status (18)

Country Link
US (1) US9663549B2 (fr)
EP (1) EP3013846B1 (fr)
JP (1) JP6556125B2 (fr)
KR (1) KR20160042873A (fr)
CN (1) CN105518015B (fr)
AR (1) AR096729A1 (fr)
AU (1) AU2014300894A1 (fr)
BR (1) BR112015031846A8 (fr)
CA (1) CA2914667A1 (fr)
EA (1) EA201690077A1 (fr)
HK (1) HK1217495A1 (fr)
IL (1) IL242968A0 (fr)
MA (1) MA38694B1 (fr)
MX (1) MX2015017879A (fr)
SG (1) SG11201510251TA (fr)
TN (1) TN2015000555A1 (fr)
TW (1) TW201534612A (fr)
WO (1) WO2014207310A1 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
CN114644673B (zh) * 2020-12-19 2023-12-26 上海喀露蓝科技有限公司 一种雌二醇衍生物、其制备方法及其在医药上的用途
IL326489A (en) * 2023-08-15 2026-04-01 Univ Laval 17 irreversible HSD1 inhibitors in the cell
CN120607578A (zh) * 2024-03-08 2025-09-09 长春金赛药业有限责任公司 17β-HSD1抑制剂化合物、药物组合物及其应用
WO2026057048A1 (fr) * 2024-09-13 2026-03-19 长春金赛药业有限责任公司 INHIBITEUR DE LA 17β-HSD1, COMPOSITION PHARMACEUTIQUE ET UTILISATION DE CELUI-CI

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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
WO2000007996A2 (fr) 1998-08-07 2000-02-17 Chiron Corporation Modulateurs de recepteurs d'oestrogenes
GB9929302D0 (en) 1999-12-11 2000-02-02 Univ Cardiff Benzyl tetralins compositions and uses thereof
EP1343803A2 (fr) * 2000-11-27 2003-09-17 EntreMed, Inc. Estrogenes substitues en position 2 comme agents antiangiogeniques
PE20030703A1 (es) 2001-09-06 2003-08-21 Schering Corp Inhibidores de la 17b-hidroxiesteroide deshidrogenasa tipo 3
EP1436281B1 (fr) 2001-10-17 2010-06-16 Schering Corporation Piperidine- et piperazineacetamines en tant qu'inhibiteurs de 17 beta hydroxysteroide deshydrogenase de type 3 servant a traiter des maladies dependantes des androgenes
US6750248B2 (en) 2001-11-09 2004-06-15 National University Of Singapore Methods for preparing an estrogenic preparation and isolated estrogenic compounds from a plant and uses thereof
WO2004046111A1 (fr) 2002-11-18 2004-06-03 Schering Corporation Inhibiteurs de la 17beta-hydroxysteroide deshydrogenase de type 3 utilises pour le traitement de maladies androgeno-dependantes
DE60323765D1 (de) 2002-12-17 2008-11-06 Schering Corp Inhibitoren der 17 beta-hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten
US7015211B2 (en) 2003-03-21 2006-03-21 Yale University 15α-substituted estradiol carboxylic acid esters as locally active estrogens
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Also Published As

Publication number Publication date
EA201690077A1 (ru) 2016-09-30
WO2014207310A1 (fr) 2014-12-31
CN105518015B (zh) 2017-09-15
BR112015031846A2 (pt) 2017-07-25
US9663549B2 (en) 2017-05-30
KR20160042873A (ko) 2016-04-20
JP6556125B2 (ja) 2019-08-07
EP3013846B1 (fr) 2017-08-09
EP3013846A1 (fr) 2016-05-04
AR096729A1 (es) 2016-01-27
TN2015000555A1 (en) 2017-04-06
MA38694B1 (fr) 2020-01-31
HK1217495A1 (zh) 2017-01-13
CN105518015A (zh) 2016-04-20
JP2016523886A (ja) 2016-08-12
MX2015017879A (es) 2017-03-01
US20170081357A1 (en) 2017-03-23
CA2914667A1 (fr) 2014-12-31
IL242968A0 (en) 2016-02-01
TW201534612A (zh) 2015-09-16
SG11201510251TA (en) 2016-01-28
AU2014300894A1 (en) 2016-01-28
BR112015031846A8 (pt) 2018-03-06

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