EA201992826A1 - 15бета-[3-пропанамидо]-замещенные эстра-1,3,5(10)-триен-17-оны и их 17-оксимы для применения в ингибировании 17бета-гидроксистероиддегидрогеназ - Google Patents

15бета-[3-пропанамидо]-замещенные эстра-1,3,5(10)-триен-17-оны и их 17-оксимы для применения в ингибировании 17бета-гидроксистероиддегидрогеназ

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Publication number
EA201992826A1
EA201992826A1 EA201992826A EA201992826A EA201992826A1 EA 201992826 A1 EA201992826 A1 EA 201992826A1 EA 201992826 A EA201992826 A EA 201992826A EA 201992826 A EA201992826 A EA 201992826A EA 201992826 A1 EA201992826 A1 EA 201992826A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibition
hydroxysteroiddehydrogenases
15beta
17beta
propanamido
Prior art date
Application number
EA201992826A
Other languages
English (en)
Inventor
Лена Хирвеля
Марьо Хакола
Теро Линнанен
Паси Коскимиес
Камилла Штьерншанц
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 EA201992826A1 publication Critical patent/EA201992826A1/ru

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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
    • A61K31/565—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
    • 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
    • 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
    • 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
    • C07J41/0005—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
    • C07J41/0016—Oximes
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

Изобретение относится к соединениям формулы (I) и их фармацевтически приемлемым солям, где R1-R4 являются такими, как определено в формуле изобретения. Изобретение также относится к их применению в качестве ингибиторов 17-HSD1 (17-гидроксистероиддегидрогеназа 1 типа) и в лечении или предупреждении зависимых от стероидных гормонов заболеваний или расстройств, таких как зависимые от стероидных гормонов заболевания или расстройства, при которых необходимо ингибирование фермента 17-HSD1 и/или при которых необходимо уменьшение концентрации эндогенного эстрадиола. Настоящее изобретение также относится к получению вышеупомянутых соединений и к фармацевтическим композициям, содержащим в качестве активного(ых) ингредиента(ов) одно или более из вышеупомянутых соединений или их фармацевтически приемлемых солей.
EA201992826A 2017-06-08 2018-06-07 15бета-[3-пропанамидо]-замещенные эстра-1,3,5(10)-триен-17-оны и их 17-оксимы для применения в ингибировании 17бета-гидроксистероиддегидрогеназ EA201992826A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FI20175530 2017-06-08
PCT/FI2018/050427 WO2018224736A2 (en) 2017-06-08 2018-06-07 Therapeutically active steroidal derivatives

Publications (1)

Publication Number Publication Date
EA201992826A1 true EA201992826A1 (ru) 2020-05-14

Family

ID=62716091

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201992826A EA201992826A1 (ru) 2017-06-08 2018-06-07 15бета-[3-пропанамидо]-замещенные эстра-1,3,5(10)-триен-17-оны и их 17-оксимы для применения в ингибировании 17бета-гидроксистероиддегидрогеназ

Country Status (19)

Country Link
US (3) US10717761B2 (ru)
EP (1) EP3634975B1 (ru)
JP (3) JP7064515B2 (ru)
KR (1) KR102420512B1 (ru)
CN (2) CN110945007B (ru)
AU (1) AU2018279205B2 (ru)
BR (1) BR112019025782A2 (ru)
CA (1) CA3066196C (ru)
CL (1) CL2019003562A1 (ru)
DK (1) DK3634975T3 (ru)
EA (1) EA201992826A1 (ru)
FI (1) FI3634975T3 (ru)
IL (2) IL294140B1 (ru)
MX (2) MX2022000747A (ru)
NZ (1) NZ760155A (ru)
SG (1) SG11201911776PA (ru)
UA (1) UA126342C2 (ru)
WO (1) WO2018224736A2 (ru)
ZA (1) ZA201908404B (ru)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 一种雌二醇衍生物、其制备方法及其在医药上的用途

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PL343862A1 (en) 1998-03-11 2001-09-10 Endorech 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
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
CA2506290C (en) 2002-11-18 2012-04-24 Schering Corporation 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
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
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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

Also Published As

Publication number Publication date
AU2018279205B2 (en) 2021-04-15
CN115716860A (zh) 2023-02-28
NZ760155A (en) 2022-09-30
ZA201908404B (en) 2023-11-29
MX2022000747A (es) 2023-01-24
US20220127303A1 (en) 2022-04-28
JP7401576B2 (ja) 2023-12-19
CA3066196A1 (en) 2018-12-13
IL294140A (en) 2022-08-01
US20180354984A1 (en) 2018-12-13
JP2020522539A (ja) 2020-07-30
JP2022065030A (ja) 2022-04-26
EP3634975B1 (en) 2024-02-28
KR102420512B1 (ko) 2022-07-13
IL271218A (en) 2020-01-30
DK3634975T3 (da) 2024-05-27
CL2019003562A1 (es) 2020-06-12
US20200317718A1 (en) 2020-10-08
MX2019014677A (es) 2022-04-01
AU2018279205A1 (en) 2020-01-16
FI3634975T3 (fi) 2024-05-03
EP3634975A2 (en) 2020-04-15
WO2018224736A2 (en) 2018-12-13
US11254703B2 (en) 2022-02-22
SG11201911776PA (en) 2020-01-30
JP7064515B2 (ja) 2022-05-10
US10717761B2 (en) 2020-07-21
CA3066196C (en) 2023-08-29
JP2024028916A (ja) 2024-03-05
UA126342C2 (uk) 2022-09-21
WO2018224736A3 (en) 2019-01-17
IL294140B1 (en) 2024-05-01
CN110945007A (zh) 2020-03-31
KR20200023362A (ko) 2020-03-04
BR112019025782A2 (pt) 2020-06-23
CN110945007B (zh) 2022-11-18

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