WO2002022645A3 - Procede de preparation de d'utilisation de 7alpha-methyl-11beta-methoxy estradiol - Google Patents

Procede de preparation de d'utilisation de 7alpha-methyl-11beta-methoxy estradiol Download PDF

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Publication number
WO2002022645A3
WO2002022645A3 PCT/US2001/042154 US0142154W WO0222645A3 WO 2002022645 A3 WO2002022645 A3 WO 2002022645A3 US 0142154 W US0142154 W US 0142154W WO 0222645 A3 WO0222645 A3 WO 0222645A3
Authority
WO
WIPO (PCT)
Prior art keywords
estrogenic
7alpha
11beta
methyl
making
Prior art date
Application number
PCT/US2001/042154
Other languages
English (en)
Other versions
WO2002022645A2 (fr
Inventor
Lawrence B Hendry
Lewis W Roach Jr
Marc W Andersen
Original Assignee
Accelerated Pharmaceuticals In
Lawrence B Hendry
Lewis W Roach Jr
Marc W Andersen
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 Accelerated Pharmaceuticals In, Lawrence B Hendry, Lewis W Roach Jr, Marc W Andersen filed Critical Accelerated Pharmaceuticals In
Priority to AU2001296872A priority Critical patent/AU2001296872A1/en
Publication of WO2002022645A2 publication Critical patent/WO2002022645A2/fr
Publication of WO2002022645A3 publication Critical patent/WO2002022645A3/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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
    • 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
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified

Landscapes

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

Abstract

L'invention concerne des molécules conçues au moyen du pharmacophore d'oestrogène et possédant une activité biologique prédite et démontrée oestrogénique et/ou de modulation oestrogénique. Elle concerne également un procédé de synthèse chimique de 11β-méthoxy-7α-méthylestra-1,3,5(10)-triène-3,17β-diol et de molécules apparentées. Elle concerne également de nouvelles utilisations de 11β-méthoxy-7α-méthylestra-1,3,5(10)-triène-3,17β-diol afin d'exercer une bioactivité oestrogénique ou une activité biologique de modulation oestrogénique, quand on administre ces molécules avec un véhicule acceptable sur le plan pharmaceutique ou cosmétique. On peut utiliser ces molécules afin de traiter des états nécessitant une modulation de l'activité biologique oestrogénique.
PCT/US2001/042154 2000-09-14 2001-09-14 Procede de preparation de d'utilisation de 7alpha-methyl-11beta-methoxy estradiol WO2002022645A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001296872A AU2001296872A1 (en) 2000-09-14 2001-09-14 Method of making 7alpha-methyl-11beta-methoxy estradiol and related compounds with estrogenic activity

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US66194100A 2000-09-14 2000-09-14
US09/661,941 2000-09-14
US26575901P 2001-02-01 2001-02-01
US60/265,759 2001-02-01

Publications (2)

Publication Number Publication Date
WO2002022645A2 WO2002022645A2 (fr) 2002-03-21
WO2002022645A3 true WO2002022645A3 (fr) 2002-09-26

Family

ID=26951413

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/042154 WO2002022645A2 (fr) 2000-09-14 2001-09-14 Procede de preparation de d'utilisation de 7alpha-methyl-11beta-methoxy estradiol

Country Status (2)

Country Link
AU (1) AU2001296872A1 (fr)
WO (1) WO2002022645A2 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10174070B2 (en) 2005-09-30 2019-01-08 Endece Llc 6-substituted estradiol derivatives and methods of use
US8168621B2 (en) 2005-09-30 2012-05-01 Endece, Llc 6-substituted estradiol derivatives and methods of use

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3526648A (en) * 1966-06-07 1970-09-01 Roussel Uclaf Novel 11beta-alkoxy-delta**1,3,5(10)-gonatrienes
DE2752695A1 (de) * 1976-11-26 1978-06-01 Akzo Nv Steroidester
WO1987000175A1 (fr) * 1985-06-25 1987-01-15 Sri International OESTRONES 9alpha, 11beta SUBSTITUEES ET 11beta-SUBSTITUEES

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3526648A (en) * 1966-06-07 1970-09-01 Roussel Uclaf Novel 11beta-alkoxy-delta**1,3,5(10)-gonatrienes
DE2752695A1 (de) * 1976-11-26 1978-06-01 Akzo Nv Steroidester
WO1987000175A1 (fr) * 1985-06-25 1987-01-15 Sri International OESTRONES 9alpha, 11beta SUBSTITUEES ET 11beta-SUBSTITUEES

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
HENDRY, L. B. ET AL: "Multidimensional screening and design of pharmaceuticals by using endocrine pharmacophores", STEROIDS (1999), 64(9), 570-575, XP002203333 *
PETERS ET AL: "11.beta.-Nitrate estrane analogs: potent estrogens", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 32, no. 10, October 1989 (1989-10-01), pages 2306 - 2310, XP002109822, ISSN: 0022-2623 *
POMPER M G ET AL: "11 beta-methoxy-, 11 beta-ethyl- and 17 alpha-ethynyl-substituted 16 alpha-fluoroestradiols: receptor-based imaging agents with enhanced uptake efficiency and selectivity.", JOURNAL OF MEDICINAL CHEMISTRY. UNITED STATES DEC 1990, vol. 33, no. 12, December 1990 (1990-12-01), pages 3143 - 3155, XP002203336, ISSN: 0022-2623 *
SEGALOFF, ALBERT ET AL: "Structure-activity relationships of estrogens: effects of esterfication of the 11.beta.-hydroxyl group", STEROIDS (1984), 43(1), 111-23, XP002203334 *
TEDESCO R ET AL: "7alpha,11beta-disubstituted estrogens: probes for the shape of the ligand binding pocket in the estrogen receptor", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 7, no. 22, 18 November 1997 (1997-11-18), pages 2919 - 2924, XP004136557, ISSN: 0960-894X *
UBEROI, NARINDER K. ET AL: "Structure-activity relationships of some unique estrogens related to estradiol are predicted by fit into DNA", STEROIDS (1985), 45(3-4), 325-40, XP002203335 *

Also Published As

Publication number Publication date
WO2002022645A2 (fr) 2002-03-21
AU2001296872A1 (en) 2002-03-26

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