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

Links

Classifications

    • 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
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • 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
    • 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)

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Dermatology (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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107207562B (zh) * 2014-12-23 2020-03-06 佛恩多制药有限公司 17β-HSD1抑制剂的前药
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
UA126342C2 (uk) * 2017-06-08 2022-09-21 Форендо Фарма Лтд 15-бета-[3-пропанамідо]-заміщені естра-1,3,5(10)-трієн-17-он-сполуки і їх 17-оксими для використання в інгібуванні 17-бета-гідроксистероїддегідрогеназ
SG11202105795XA (en) * 2018-12-05 2021-06-29 Forendo Pharma Ltd Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1
CN114644673B (zh) * 2020-12-19 2023-12-26 上海喀露蓝科技有限公司 一种***衍生物、其制备方法及其在医药上的用途

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL343862A1 (en) 1998-03-11 2001-09-10 Endorech Inhibitors of type 5 and type 3 17β−hydroxysteroid dehydrogenase and methods for their use
ATE355279T1 (de) 1998-08-07 2006-03-15 Novartis Vaccines & Diagnostic Pyrazole als modulatoren des östrogenrezeptors
GB9929302D0 (en) 1999-12-11 2000-02-02 Univ Cardiff Benzyl tetralins compositions and uses thereof
JP2004537499A (ja) * 2000-11-27 2004-12-16 エントレメッド インコーポレイテッド 抗血管新生薬
DK1423381T3 (da) 2001-09-06 2007-05-07 Schering Corp 17beta-hydroxysteroid-dehydrogenase type 3-inhibitorer til behandling af androgenafhængige sygdomme
AR036812A1 (es) 2001-10-17 2004-10-06 Schering Corp Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientes
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
CA2506290C (fr) 2002-11-18 2012-04-24 Schering Corporation Inhibiteurs de la 17beta-hydroxysteroide deshydrogenase de type 3 utilises pour le traitement de maladies androgeno-dependantes
JP4585320B2 (ja) 2002-12-17 2010-11-24 シェーリング コーポレイション 男性ホルモン依存性疾患の処置のための１７β−ヒドロキシステロイドデヒドロゲナーゼ３型インヒビター
WO2004085345A2 (fr) 2003-03-21 2004-10-07 Yale University Esters d'acide carboxylique et d'estradiol substitues en 15$g(a) en tant qu'oestrogenes localement actifs
GB0306718D0 (en) 2003-03-24 2003-04-30 Sterix Ltd Compound
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TWI331154B (en) * 2003-11-12 2010-10-01 Solvay Pharm Gmbh Novel 17-hydroxysteroid dehydrogenase type i inhibitors
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UA89964C2 (ru) 2004-09-08 2010-03-25 Н.В. Органон 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ
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US8288367B2 (en) * 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
RU2453554C2 (ru) 2006-11-30 2012-06-20 Зольвай Фармасьютиклз Гмбх Замещенные производные эстратриена как ингибиторы 17бета hsd

Also Published As

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

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