ZA200709854B - 17ß-HSD1 and STS inhibitors - Google Patents

17ß-HSD1 and STS inhibitors

Info

Publication number
ZA200709854B
ZA200709854B ZA200709854A ZA200709854A ZA200709854B ZA 200709854 B ZA200709854 B ZA 200709854B ZA 200709854 A ZA200709854 A ZA 200709854A ZA 200709854 A ZA200709854 A ZA 200709854A ZA 200709854 B ZA200709854 B ZA 200709854B
Authority
ZA
South Africa
Prior art keywords
hsd1
sts inhibitors
sts
inhibitors
Prior art date
Application number
ZA200709854A
Other languages
English (en)
Inventor
Messinger Josef
Thole Heinrich-Hubert
Husen Bettina
Koskimies Pasi
Pirkkala Lila
Weske Michael
Original Assignee
Solvay Pharm Gmbh
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 Solvay Pharm Gmbh filed Critical Solvay Pharm Gmbh
Publication of ZA200709854B publication Critical patent/ZA200709854B/xx

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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
    • C07J71/0042—Nitrogen only
    • C07J71/0052—Nitrogen only at position 16(17)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
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    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P5/28—Antiandrogens
    • 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
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
ZA200709854A 2005-05-26 2006-05-24 17ß-HSD1 and STS inhibitors ZA200709854B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05104534 2005-05-26

Publications (1)

Publication Number Publication Date
ZA200709854B true ZA200709854B (en) 2009-03-25

Family

ID=35276406

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200709854A ZA200709854B (en) 2005-05-26 2006-05-24 17ß-HSD1 and STS inhibitors

Country Status (16)

Country Link
EP (1) EP1888615B1 (zh)
JP (1) JP5268635B2 (zh)
KR (1) KR101364412B1 (zh)
CN (2) CN101189251B (zh)
AU (1) AU2006251154B2 (zh)
BR (1) BRPI0611623A2 (zh)
CA (1) CA2609726C (zh)
ES (1) ES2388297T3 (zh)
HK (1) HK1117538A1 (zh)
IL (1) IL187620A (zh)
MX (1) MX2007014736A (zh)
NO (1) NO20076616L (zh)
RU (1) RU2412196C2 (zh)
UA (1) UA92348C2 (zh)
WO (1) WO2006125800A1 (zh)
ZA (1) ZA200709854B (zh)

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Publication number Priority date Publication date Assignee Title
US8080540B2 (en) 2006-09-19 2011-12-20 Abbott Products Gmbh Therapeutically active triazoles and their use
US8288367B2 (en) 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
EP2099814A1 (en) * 2006-11-30 2009-09-16 Solvay Pharmaceuticals GmbH Substituted estratrien derivatives as 17beta hsd inhibitors
CA2830984C (en) 2011-03-25 2020-02-11 Universite Laval Inhibitors of 17.beta.-hsd1, 17.beta.-hsd3 and 17.beta.-hsd10.
US11053274B2 (en) 2011-06-01 2021-07-06 Estetra S.P.R.L. Process for the production of estetrol intermediates
BR112013030833B1 (pt) 2011-06-01 2019-09-03 Estetra S A processo para a preparação de um composto de fórmula (i) e processo para a preparação de estetrol
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
WO2013078413A1 (en) * 2011-11-22 2013-05-30 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Modulators of lipid storage
CN105518016B (zh) 2013-06-25 2020-10-23 佛恩多制药有限公司 治疗活性的作为1型17β-羟基类固醇脱氢酶抑制剂的雌三烯噻唑衍生物
CN105518015B (zh) 2013-06-25 2017-09-15 佛恩多制药有限公司 治疗活性的作为17β‑羟基类固醇脱氢酶抑制剂的17‑氮取代雌三烯噻唑衍生物
CN105518017B (zh) * 2013-06-25 2020-07-14 佛恩多制药有限公司 治疗活性的作为1型17β-羟基类固醇脱氢酶抑制剂的雌三烯噻唑衍生物
US10413557B2 (en) 2014-12-23 2019-09-17 Forendo Pharma Ltd. Prodrugs of 17.BETA.-HSD1-inhibitors
EP3237430B1 (en) 2014-12-23 2019-03-20 Forendo Pharma Ltd PRODRUGS OF 17ß -HSD1 -INHIBITORS
SI3310345T1 (sl) 2015-06-18 2021-05-31 Estetra Sprl Orodisperzibilna tableta, ki vsebuje estetrol
EP3106148B1 (en) 2015-06-18 2018-03-14 Mithra Pharmaceuticals S.A. Orodispersible dosage unit containing an estetrol component
LT3310346T (lt) 2015-06-18 2021-06-10 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio
PE20180522A1 (es) 2015-06-18 2018-03-14 Mithra Pharmaceuticals S A Unidad de dosificacion orodispersable que contiene un componente estetrol
CN105963301B (zh) * 2016-04-26 2018-12-28 兰州大学 以人fkbp51蛋白为靶点的先导化合物及筛选方法与应用
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
KR20220144885A (ko) 2016-08-05 2022-10-27 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 월경통 및 생리통의 관리방법
WO2018224736A2 (en) 2017-06-08 2018-12-13 Forendo Pharma Ltd Therapeutically active steroidal derivatives
TWI801561B (zh) 2018-04-19 2023-05-11 比利時商依思特拉私人有限責任公司 化合物及其用於緩解絕經相關症狀的用途
JOP20200260A1 (ar) 2018-04-19 2019-10-19 Estetra Sprl مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث
US20220041647A1 (en) 2018-12-05 2022-02-10 Forendo Pharma Ltd Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU208150B (en) * 1988-10-31 1993-08-30 Endorecherche Inc Process for producing new estrogen derivatives having steroid hormone inhibitor activity and pharmaceutical compositions comprising such derivatives
GB0306718D0 (en) * 2003-03-24 2003-04-30 Sterix Ltd Compound
TWI331154B (en) * 2003-11-12 2010-10-01 Solvay Pharm Gmbh Novel 17-hydroxysteroid dehydrogenase type i inhibitors

Also Published As

Publication number Publication date
KR101364412B1 (ko) 2014-02-21
KR20080012960A (ko) 2008-02-12
IL187620A0 (en) 2008-03-20
RU2412196C2 (ru) 2011-02-20
RU2007147416A (ru) 2009-07-10
BRPI0611623A2 (pt) 2010-09-21
AU2006251154A1 (en) 2006-11-30
JP2008545678A (ja) 2008-12-18
JP5268635B2 (ja) 2013-08-21
CA2609726A1 (en) 2006-11-30
MX2007014736A (es) 2008-02-15
CA2609726C (en) 2013-10-01
EP1888615B1 (en) 2012-05-16
NO20076616L (no) 2008-02-01
UA92348C2 (en) 2010-10-25
EP1888615A1 (en) 2008-02-20
IL187620A (en) 2014-03-31
WO2006125800A1 (en) 2006-11-30
CN102796160A (zh) 2012-11-28
AU2006251154B2 (en) 2012-06-28
ES2388297T3 (es) 2012-10-11
CN101189251B (zh) 2012-09-12
HK1117538A1 (zh) 2009-01-16
CN101189251A (zh) 2008-05-28

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