TW200621795A - 15β-substituted steroids having selective estrogenic activity - Google Patents

15β-substituted steroids having selective estrogenic activity

Info

Publication number
TW200621795A
TW200621795A TW094130148A TW94130148A TW200621795A TW 200621795 A TW200621795 A TW 200621795A TW 094130148 A TW094130148 A TW 094130148A TW 94130148 A TW94130148 A TW 94130148A TW 200621795 A TW200621795 A TW 200621795A
Authority
TW
Taiwan
Prior art keywords
estrogenic activity
substituted steroids
5alkyl
selective estrogenic
substituted
Prior art date
Application number
TW094130148A
Other languages
English (en)
Chinese (zh)
Inventor
Hubert Jan Jozef Loozen
Antonius Gerardus Hendrikus Ederveen
Fredericus Antonius Dijcks
Original Assignee
Akzo Nobel Nv
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 Akzo Nobel Nv filed Critical Akzo Nobel Nv
Publication of TW200621795A publication Critical patent/TW200621795A/zh

Links

Classifications

    • 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
    • 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
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P15/18—Feminine contraceptives
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW094130148A 2004-09-08 2005-09-02 15β-substituted steroids having selective estrogenic activity TW200621795A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP04104334 2004-09-08

Publications (1)

Publication Number Publication Date
TW200621795A true TW200621795A (en) 2006-07-01

Family

ID=34929554

Family Applications (1)

Application Number Title Priority Date Filing Date
TW094130148A TW200621795A (en) 2004-09-08 2005-09-02 15β-substituted steroids having selective estrogenic activity

Country Status (20)

Country Link
US (1) US7838516B2 (enExample)
EP (1) EP1805201B1 (enExample)
JP (1) JP4889644B2 (enExample)
AR (1) AR050732A1 (enExample)
AT (1) ATE414710T1 (enExample)
AU (1) AU2005281705B2 (enExample)
BR (1) BRPI0514976A (enExample)
CA (1) CA2577497C (enExample)
DK (1) DK1805201T3 (enExample)
ES (1) ES2317312T3 (enExample)
NZ (1) NZ553266A (enExample)
PE (1) PE20060590A1 (enExample)
PL (1) PL1805201T3 (enExample)
PT (1) PT1805201E (enExample)
RS (1) RS51640B (enExample)
RU (1) RU2386637C2 (enExample)
SI (1) SI1805201T1 (enExample)
TW (1) TW200621795A (enExample)
UA (1) UA89964C2 (enExample)
WO (1) WO2006027347A1 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8030298B2 (en) 2005-05-26 2011-10-04 Abbott Products Gmbh 17β-HSD1 and STS inhibitors
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
EP2448901A1 (en) * 2009-06-29 2012-05-09 Merz Pharma GmbH & Co. KGaA Method of preparing 3,3,5,5-tetramethylcyclohexanone
ES2416462T3 (es) * 2009-06-29 2013-08-01 Merz Pharma Gmbh & Co. Kgaa Método de preparación de neramexane.
EP2448908B1 (en) * 2009-06-29 2013-09-18 Merz Pharma GmbH & Co. KGaA Method of preparing neramexane
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
AU2012320423C1 (en) * 2011-10-07 2018-01-25 Estetra Srl Process for the production of estetrol
TW201512215A (zh) 2013-06-25 2015-04-01 Forendo Pharma Ltd 治療活性雌三烯噻唑衍生物
JP6456373B2 (ja) 2013-06-25 2019-01-23 フォレンド ファーマ リミテッド １７β−ヒドロキシステロイドデヒドロゲナーゼ タイプ１の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体
AU2014300894A1 (en) 2013-06-25 2016-01-28 Forendo Pharma Ltd Therapeutically active 17-nitrogen substituted estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxysteroid dehydrogenase
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
MA44206B1 (fr) 2015-06-18 2021-04-30 Estetra Sprl Comprimé orodispersible comprenant estetrol
CU24523B1 (es) 2015-06-18 2021-06-08 Estetra Sprl Unidad de dosificación orodispersable que contiene un componente estetrol
LT3310345T (lt) 2015-06-18 2021-06-25 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio
EP3701944B1 (en) 2015-06-18 2021-12-08 Estetra SRL Orodispersible dosage unit containing an estetrol component
CA3178291A1 (en) 2016-08-05 2018-04-12 Estetra Srl Method for the management of dysmenorrhea and menstrual pain
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
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
EP3781171B1 (en) 2018-04-19 2022-02-09 Estetra SRL Compounds and their uses for alleviating menopause-associated symptoms
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
TWI893101B (zh) 2020-04-16 2025-08-11 比利時商埃斯特拉有限責任公司 具有降低之副作用之避孕組成物

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL226738A (enExample) 1957-04-11
DE1084261B (de) 1957-04-11 1960-06-30 Syntex Sa Verfahren zur Herstellung neuer Cyclopentanophenanthrenderivate
US3257429A (en) * 1957-11-12 1966-06-21 Syntex Corp 16-methylene derivatives of estrone and estradiol
US3007946A (en) 1958-11-06 1961-11-07 Searle & Co 3-alkoxy-16-methylene-1, 3, 5(10)-estratrien-17-ones
US3049555A (en) 1959-12-22 1962-08-14 Searle & Co 3-alkoxy-16-methyl-1, 3, 5 (10)-estratrien-17-ones
US3092645A (en) 1961-12-28 1963-06-04 Searle & Co Esters of 17alpha-alkynylester-5(10)-ene-3beta, 17beta-diols
GB1110792A (en) 1964-04-07 1968-04-24 Res Inst Medicine Chem Novel 5(10)-dehydro-steroids
US3299108A (en) 1965-10-18 1967-01-17 Searle & Co 17alpha-alkynyl/alkenyl-13beta-alkyl-11-alkylgona-1, 3, 5 (10)-triene-3, 17beta-diols, ethers and esters thereof and intermediates thereto
US3465010A (en) 1966-11-22 1969-09-02 Searle & Co 17 - (unsaturated hydrocarbon - substituted) 11,13beta - dialkylgon -4 - ene - 3,17beta-diols and esters thereof
US3377366A (en) 1966-12-02 1968-04-09 Searle & Co 17alpha-alkynyl/alkenyl-11, 13beta-dialkylgon-5(10)-en-3-ones and esters thereof
US3642992A (en) * 1967-09-08 1972-02-15 Upjohn Co Organic compounds
ZA712312B (en) 1970-04-28 1972-01-26 Ochsner Med Found Alton 4,14-estradiene compounds
US3652606A (en) 1970-08-07 1972-03-28 Searle & Co 3-oxygenated 11beta-methylestr-4-en-17beta-ol and esters thereof
US3704253A (en) 1970-09-23 1972-11-28 American Home Prod 13 - polycarbonalkyl - 16 - methylgona-1,3,5(10)-trienes and 13-polycarbonalkyl-16-methylgon - 4 - en-3-ones and intermediates for their production
US3766224A (en) * 1971-06-03 1973-10-16 Sandoz Ag 15-methyl-substituted steroids
FR2377419A1 (fr) 1977-01-13 1978-08-11 Roussel Uclaf Nouveaux derives steroides 11b-substitues 1,3,5 (10) trieniques, leur procede de preparation et leur application comme medicament
DE2757157C3 (de) 1977-12-19 1980-10-09 Schering Ag, 1000 Berlin Und 4619 Bergkamen Verfahren zur Herstellung von 16 a -alkylierten Steroiden
AU572589B2 (en) 1983-12-14 1988-05-12 Upjohn Company, The 11(alpha)-difluoromethyl and (e)-and (z)-11-fluoromethylene steroids
US5116830A (en) 1984-08-17 1992-05-26 Sri International Stereoisomerically pure 17α-ethynyl-estra-2-en-17β-ol and the 17β esters thereof, methods of preparation and uses
US5204337A (en) * 1988-10-31 1993-04-20 Endorecherche Inc. Estrogen nucleus derivatives for use in inhibition of sex steroid activity
ZA94715B (en) 1993-02-08 1994-10-24 Akzo Nv Steroids for treating menopausal complaints
EP0613687B1 (en) 1993-03-05 1999-06-02 Akzo Nobel N.V. Use of a pregnane derivatives for the treatment of tumours
CA2200423C (en) 1996-03-26 2006-12-19 Sietse Mosselman Novel estrogen receptor
TW403736B (en) 1997-02-21 2000-09-01 Akzo Nobel Nv Steroid compounds having contraceptive and anti-osteoporosis activity
CA2319765A1 (en) 1998-03-09 1999-09-16 Akzo Nobel Nv New contraceptive kit
TR200003743T2 (tr) 1998-06-19 2001-07-23 Akzo Nobel N.V. Testosteron türevi.
WO2000031112A1 (en) 1998-11-20 2000-06-02 Akzo Nobel N.V. Estrogenic estra-1,3,5(10)-trienes with differential effects on the alpha and beta estrogen receptors, having a linear hydrocarbon chain of from 5-9 carbon atoms in position 11
TW548277B (en) 1999-07-16 2003-08-21 Akzo Nobel Nv Orally active androgens
NZ517281A (en) 1999-09-06 2003-09-26 Akzo Nobel Nv Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11
PT1226155E (pt) * 1999-11-02 2007-07-26 Bayer Schering Pharma Ag 18-nor-esteróides como estrogénios selectivamente activos
US7696190B2 (en) * 2000-07-28 2010-04-13 N.V. Organon 16Alpha-methyl or ethyl substituted estrogens

Also Published As

Publication number Publication date
WO2006027347A1 (en) 2006-03-16
PT1805201E (pt) 2008-12-31
AU2005281705B2 (en) 2011-03-10
US20070254860A1 (en) 2007-11-01
US7838516B2 (en) 2010-11-23
SI1805201T1 (sl) 2009-04-30
BRPI0514976A (pt) 2008-07-01
AR050732A1 (es) 2006-11-15
RS51640B (sr) 2011-10-31
RU2007112939A (ru) 2008-11-10
PL1805201T3 (pl) 2009-04-30
AU2005281705A1 (en) 2006-03-16
RU2386637C2 (ru) 2010-04-20
RS20070075A (sr) 2008-09-29
JP4889644B2 (ja) 2012-03-07
ES2317312T3 (es) 2009-04-16
EP1805201A1 (en) 2007-07-11
NZ553266A (en) 2009-06-26
PE20060590A1 (es) 2006-07-14
UA89964C2 (ru) 2010-03-25
EP1805201B1 (en) 2008-11-19
ATE414710T1 (de) 2008-12-15
CA2577497A1 (en) 2006-03-16
JP2008512426A (ja) 2008-04-24
DK1805201T3 (da) 2009-01-12
CA2577497C (en) 2012-03-20

Similar Documents

Publication Publication Date Title
AR050732A1 (es) 15 beta-sustituidos esteroides con actividad estrogenica selectiva
MXPA06001592A (es) Derivados de (4-hidroxifenil)-1h-indol-3-carbaldehido oxima como agentes estrogenicos.
NZ561747A (en) (Pyrrol-2-ylmethyl)-indol-1-yl-acetic acid derivatives with PGD2 antagonist activity
WO2005070893A3 (en) Azadecalin glucocorticoid receptor modulators
BR0214023A (pt) Derivados de 1,2,4-tiadiazólio como moduladores de receptor de melanocortina
WO2006072599A3 (en) Androstane 17-alpha carbonate derivatives for use in the treatment of allergic and inflammatory conditions
IL175949A0 (en) Benzenesulfonylamino-pyridin-2-yl derivatives and related compounds as inhibitors of 11-beta-hydroxy steroid dehydrogenase type1 (11-beta-hsd-1) for the treatment of diabetes and obesity
GEP20146124B (en) Novel ccr2 receptor antagonists and usage thereof
WO2009002802A3 (en) Liquiritigenin and derivatives as selective estrogen receptor beta agonists
NO20071922L (no) Indazoler, benzisokazoler og benzinsotiazoler og anvendelse derav som ostrogene midler
IL183064A0 (en) Phenylpiperazine derivatives with a combination of partial dopamine-d2 receptor agonism and serotonin reuptake inhibition
WO2008111632A1 (ja) ２，２，４－トリメチル－６－フェニル－１，２－ジヒドロキノリン誘導体からなるグルココルチコイド受容体アゴニスト
SG151331A1 (en) Crystalline polymorph of a bazedoxifene acetate
WO2008147144A3 (en) Upper body support apparatus for toilets
CY1111128T1 (el) Στεροειδη παραγωγα 17-φωσφορου χρησιμα ως τροποποιητες υποδοχεων προγεστερονης
UA86055C2 (ru) Кристаллическая форма в базедоксифена ацетата
EP1655291A4 (en) COMPOUNDS WITH THROMBOPOIETIN RECEPTOR AGONISM
MX2010012303A (es) Agonista de receptor de glucocorticoide compuesto de derivado de 2,2,4-trimetil-6-fenil-1,2-dihidroquinolina que tiene un grupo oxi sustituido.
WO2003082894A3 (en) C-17 spirolactonization and 6,7 oxidation of steroids
TW200611909A (en) Process for the preparation 2-substituted-derivatives of estrone and estradiol
MY143679A (en) 15b-subsitituded streoids having selective estrogenic activity
NO20021079D0 (no) Ikke-aromatiske östrogene steroider med en hydrogensubstituent i posisjon 11
NO20065885L (no) Steroide prolegemidler med androgen virkning
CY1109412T1 (el) Στεροειδη που υποκαθιστανται στο 15 βητα τα οποια εχουν μια εκλεκτικη οιστρογονικη δραστηριοτητα
AU5209600A (en) Orally active androgens