EA202191531A1 - Терапевтически активные стероидные производные - Google Patents

Терапевтически активные стероидные производные

Info

Publication number
EA202191531A1
EA202191531A1 EA202191531A EA202191531A EA202191531A1 EA 202191531 A1 EA202191531 A1 EA 202191531A1 EA 202191531 A EA202191531 A EA 202191531A EA 202191531 A EA202191531 A EA 202191531A EA 202191531 A1 EA202191531 A1 EA 202191531A1
Authority
EA
Eurasian Patent Office
Prior art keywords
relates
therapeutically active
steroid derivatives
active steroid
diseases
Prior art date
Application number
EA202191531A
Other languages
English (en)
Inventor
Леена Хирвеля
Марйо Хакола
Тэро Линнанен
Паси Коскимиэс
Камилла Штерншанц
Original Assignee
Форендо Фарма Лтд
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 Форендо Фарма Лтд filed Critical Форендо Фарма Лтд
Publication of EA202191531A1 publication Critical patent/EA202191531A1/ru

Links

Classifications

    • 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)
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0052—Nitrogen only at position 16(17)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Изобретение относится к соединениям формулы (I) и их фармацевтически приемлемым солямгде R1-R4 такие, как определены в формуле изобретения. Изобретение также относится к их применению в качестве ингибиторов 17-HSD1 и в лечении или профилактике заболеваний или расстройств, зависимых от стероидных гормонов, таких как заболевания или расстройства, зависимые от стероидных гормонов, требующие ингибирования 17-HSD1 фермента и/или требующие снижения концентрации эндогенного эстрадиола. Настоящее изобретение также относится к получению вышеуказанных соединений и к фармацевтическим композициям, содержащим, в качестве активного ингредиента, одно или несколько вышеуказанных соединений или их фармацевтически приемлемых солей.
EA202191531A 2018-12-05 2019-12-05 Терапевтически активные стероидные производные EA202191531A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FI20186056 2018-12-05
PCT/FI2019/050874 WO2020115371A1 (en) 2018-12-05 2019-12-05 Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1

Publications (1)

Publication Number Publication Date
EA202191531A1 true EA202191531A1 (ru) 2021-09-03

Family

ID=69005734

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202191531A EA202191531A1 (ru) 2018-12-05 2019-12-05 Терапевтически активные стероидные производные

Country Status (15)

Country Link
US (1) US20220041647A1 (ru)
EP (1) EP3891167A1 (ru)
JP (1) JP7417608B2 (ru)
KR (1) KR20210114390A (ru)
CN (1) CN113412269A (ru)
AU (2) AU2019393005B2 (ru)
BR (1) BR112021010598A2 (ru)
CA (1) CA3122049C (ru)
CL (1) CL2021001468A1 (ru)
EA (1) EA202191531A1 (ru)
IL (1) IL283588A (ru)
MX (1) MX2021006452A (ru)
SG (1) SG11202105795XA (ru)
UA (1) UA126881C2 (ru)
WO (1) WO2020115371A1 (ru)

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999046279A2 (en) 1998-03-11 1999-09-16 Endorecherche, Inc. INHIBITORS OF TYPE 5 AND TYPE 3 17β-HYDROXYSTEROID DEHYDROGENASE AND METHODS FOR THEIR USE
GB9929302D0 (en) 1999-12-11 2000-02-02 Univ Cardiff Benzyl tetralins compositions and uses thereof
EP1423381B1 (en) 2001-09-06 2007-01-03 Schering Corporation 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
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
AR042046A1 (es) 2002-11-18 2005-06-08 Schering Corp Inhibidores de 17 beta-hidroxiesteroide deshidrogenasa de tipo 3 para el tratamiento de enfermedades que dependen de androgenos
MXPA05006485A (es) 2002-12-17 2005-08-26 Schering Corp Inhibidores de la 17 beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgeno.
WO2004085345A2 (en) 2003-03-21 2004-10-07 Yale University 15α-SUBSTITUTED ESTRADIOL CARBOXYLIC ACID ESTERS AS LOCALLY ACTIVE ESTROGENS
GB0306718D0 (en) 2003-03-24 2003-04-30 Sterix Ltd Compound
US20040224935A1 (en) 2003-04-07 2004-11-11 Endorecherche, Inc. Topical antiandrogenic steroids
US7754709B2 (en) 2003-06-10 2010-07-13 Solvay Pharmaceuticals Bv Tetracyclic thiophenepyrimidinone compounds as inhibitors of 17β hydroxysteroid dehydrogenase compounds
US7465739B2 (en) 2003-06-10 2008-12-16 Solvay Pharmaceuticals B.V. Compounds and their use in therapy
TWI331154B (en) 2003-11-12 2010-10-01 Solvay Pharm Gmbh Novel 17-hydroxysteroid dehydrogenase type i inhibitors
US7378426B2 (en) 2004-03-01 2008-05-27 Bristol-Myers Squibb Company Fused heterotricyclic compounds as inhibitors of 17β-hydroxysteroid dehydrogenase 3
DE102004032673A1 (de) 2004-07-02 2006-01-26 Schering Ag Neue 2-substituierte D-Homo-estra-1,3,5(10)-triene als Inhibitoren der 17ß-Hydroxysteroiddehydrogenase Typ 1
DE102004032674A1 (de) 2004-07-02 2006-01-26 Schering Ag Neue 2-substituierte Estra-1,3,5(10)-trien-17-one als Inhibitoren der 17β-Hydroxysteroiddehydrogenase Typ 1
UA89964C2 (ru) 2004-09-08 2010-03-25 Н.В. Органон 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ
AU2006251154B2 (en) 2005-05-26 2012-06-28 Solvay Pharmaceuticals Gmbh 17beta-HSD1 and STS inhibitors
US8030298B2 (en) * 2005-05-26 2011-10-04 Abbott Products Gmbh 17β-HSD1 and STS inhibitors
ES2424395T3 (es) 2006-09-19 2013-10-01 Abbott Products Gmbh Derivados de estratrieno y sus usos como inhibidores de la 17-beta-hidroxiesteroide-deshidrogenasa
US8288367B2 (en) * 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
JP5264760B2 (ja) * 2006-11-30 2013-08-14 アボット プロダクツ ゲゼルシャフト ミット ベシュレンクテル ハフツング 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
US9284345B2 (en) 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
CN102272077A (zh) 2008-11-20 2011-12-07 哈佛学院董事会 有机化合物的氟化
EP3013846B1 (en) 2013-06-25 2017-08-09 Forendo Pharma Ltd Therapeutically active 17-nitrogen substituted estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxysteroid dehydrogenase
WO2014207311A1 (en) 2013-06-25 2014-12-31 Forendo Pharma Ltd Therapeutically active estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxy-steroid dehydrogenase, type 1
WO2014207309A1 (en) 2013-06-25 2014-12-31 Forendo Pharma Ltd Therapeutically active estratrienthiazole derivatives as inhibitors of 17 b-hydroxysteroid dehydrogenase, type 1
CA3066196C (en) * 2017-06-08 2023-08-29 Forendo Pharma Ltd 15.beta.-[3-propanamido]-substituted estra-1,3,5(10)-trien-17-one compounds and their 17-oximes for use in inhibition of 17.beta.-hydroxysteroid dehydro-genases

Also Published As

Publication number Publication date
UA126881C2 (uk) 2023-02-15
CL2021001468A1 (es) 2022-01-28
AU2019393005B2 (en) 2022-12-15
JP7417608B2 (ja) 2024-01-18
MX2021006452A (es) 2021-09-28
KR20210114390A (ko) 2021-09-23
CN113412269A (zh) 2021-09-17
CA3122049C (en) 2023-10-17
CA3122049A1 (en) 2020-06-11
JP2022510386A (ja) 2022-01-26
AU2022279473A1 (en) 2023-02-02
WO2020115371A1 (en) 2020-06-11
AU2019393005A1 (en) 2021-07-29
EP3891167A1 (en) 2021-10-13
IL283588A (en) 2021-07-29
BR112021010598A2 (pt) 2021-08-24
US20220041647A1 (en) 2022-02-10
SG11202105795XA (en) 2021-06-29

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