EA201690077A1 - Терапевтически активные производные эстратриен-тиазола - Google Patents

Терапевтически активные производные эстратриен-тиазола

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Publication number
EA201690077A1
EA201690077A1 EA201690077A EA201690077A EA201690077A1 EA 201690077 A1 EA201690077 A1 EA 201690077A1 EA 201690077 A EA201690077 A EA 201690077A EA 201690077 A EA201690077 A EA 201690077A EA 201690077 A1 EA201690077 A1 EA 201690077A1
Authority
EA
Eurasian Patent Office
Prior art keywords
relates
estratrien
thiazole
therapeutically active
active derivatives
Prior art date
Application number
EA201690077A
Other languages
English (en)
Inventor
Майре Элоранта
Лена Хирвеля
Лаури Кангас
Паси Коскимиес
Ристо Ламминтауста
Микко Ункила
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 EA201690077A1 publication Critical patent/EA201690077A1/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
    • A61K31/58—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)
  • 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)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение относится к соединениям формулы (I) и их фармацевтически приемлемым солямгде R2-R7 имеют значения, определенные в формуле изобретения. Изобретение также относится к их применению в качестве ингибиторов 17β-HSD1 и в лечении или профилактике заболеваний или нарушений, зависимых от стероидных гормонов, таких как заболевания или нарушения, зависимые от стероидных гормонов, требующие ингибирования фермента 17β-HSD1 и/или требующие понижения эндогенной концентрации эстрадиола. Настоящее изобретение также относится к получению вышеупомянутых соединений и к фармацевтическим композициям, содержащим в качестве активного ингредиента(ов) одно или более вышеупомянутых соединений или их фармацевтически приемлемых солей.
EA201690077A 2013-06-25 2014-06-25 Терапевтически активные производные эстратриен-тиазола EA201690077A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FI20135694 2013-06-25
PCT/FI2014/050518 WO2014207310A1 (en) 2013-06-25 2014-06-25 Therapeutically active 17-nitrogen substituted estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxysteroid dehydrogenase

Publications (1)

Publication Number Publication Date
EA201690077A1 true EA201690077A1 (ru) 2016-09-30

Family

ID=51220584

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201690077A EA201690077A1 (ru) 2013-06-25 2014-06-25 Терапевтически активные производные эстратриен-тиазола

Country Status (18)

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

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10413557B2 (en) 2014-12-23 2019-09-17 Forendo Pharma Ltd. Prodrugs of 17.BETA.-HSD1-inhibitors
WO2016102775A1 (en) * 2014-12-23 2016-06-30 Forendo Pharma Ltd PRODRUGS OF 17β-HSD1 -INHIBITORS
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
SG11201911776PA (en) * 2017-06-08 2020-01-30 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 dehydrogenases
CA3122049C (en) * 2018-12-05 2023-10-17 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
UY40855A (es) * 2023-08-15 2025-02-28 Univ Laval INHIBIDORES IRREVERSIBLES DE 17ß-HSD1
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 (zh) * 2024-09-13 2026-03-19 长春金赛药业有限责任公司 17β-HSD1抑制剂、药物组合物及其应用

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA00008868A (es) 1998-03-11 2003-04-25 Endorech Inc Inhibidores de dihidrogenasa de 17 -hidroxiesteroide y metodos para su uso.
DE69935335T2 (de) 1998-08-07 2007-11-22 Novartis Vaccines and Diagnostics, Inc., Emeryville Pyrazole als modulatoren des östrogenrezeptors
GB9929302D0 (en) 1999-12-11 2000-02-02 Univ Cardiff Benzyl tetralins compositions and uses thereof
EP1343803A2 (en) * 2000-11-27 2003-09-17 EntreMed, Inc. 2-substituted estrogens as antiangiogenic agents
MY141661A (en) 2001-09-06 2010-05-31 Schering Corp 17b-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
ES2347643T3 (es) 2001-10-17 2010-11-03 Schering Corporation Piperin- y piperazinacetamidas como inhibidores de 17beta hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgenos.
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
ES2345146T3 (es) 2002-11-18 2010-09-16 Schering Corporation Inhibidores de 17beta-hidroxiesteroides deshidrogenasa de tipo 3 para el tratamiento de enfermedades dependientes de androgenos.
AU2003293555A1 (en) 2002-12-17 2004-07-29 Schering Corporation 17 beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
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
US7465739B2 (en) 2003-06-10 2008-12-16 Solvay Pharmaceuticals B.V. Compounds and their use in therapy
US7754709B2 (en) 2003-06-10 2010-07-13 Solvay Pharmaceuticals Bv Tetracyclic thiophenepyrimidinone compounds as inhibitors of 17β hydroxysteroid dehydrogenase compounds
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
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
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
UA89964C2 (ru) 2004-09-08 2010-03-25 Н.В. Органон 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ
CN102796160A (zh) * 2005-05-26 2012-11-28 索尔瓦药物有限公司 17β-HSD1和STS抑制剂
US8030298B2 (en) * 2005-05-26 2011-10-04 Abbott Products Gmbh 17β-HSD1 and STS inhibitors
RU2469042C2 (ru) 2006-09-19 2012-12-10 Зольвай Фармасьютиклз Гмбх Терапевтически активные триазолы и их использование
CN101568547B (zh) 2006-11-30 2014-06-25 索尔瓦药物有限公司 作为17βHSD抑制剂的被取代的雌三烯衍生物
US8288367B2 (en) * 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors

Also Published As

Publication number Publication date
TW201534612A (zh) 2015-09-16
EP3013846A1 (en) 2016-05-04
MA38694B1 (fr) 2020-01-31
HK1217495A1 (zh) 2017-01-13
BR112015031846A2 (pt) 2017-07-25
WO2014207310A1 (en) 2014-12-31
MX2015017879A (es) 2017-03-01
SG11201510251TA (en) 2016-01-28
TN2015000555A1 (en) 2017-04-06
CN105518015A (zh) 2016-04-20
CN105518015B (zh) 2017-09-15
JP6556125B2 (ja) 2019-08-07
US9663549B2 (en) 2017-05-30
BR112015031846A8 (pt) 2018-03-06
KR20160042873A (ko) 2016-04-20
IL242968A0 (en) 2016-02-01
US20170081357A1 (en) 2017-03-23
AU2014300894A1 (en) 2016-01-28
JP2016523886A (ja) 2016-08-12
MA38694A2 (fr) 2017-12-29
CA2914667A1 (en) 2014-12-31
AR096729A1 (es) 2016-01-27
EP3013846B1 (en) 2017-08-09

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