WO2008057309A3 - Modulateurs de récepteur d'oestrogène - Google Patents

Modulateurs de récepteur d'oestrogène Download PDF

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Publication number
WO2008057309A3
WO2008057309A3 PCT/US2007/022798 US2007022798W WO2008057309A3 WO 2008057309 A3 WO2008057309 A3 WO 2008057309A3 US 2007022798 W US2007022798 W US 2007022798W WO 2008057309 A3 WO2008057309 A3 WO 2008057309A3
Authority
WO
WIPO (PCT)
Prior art keywords
disease
estrogen
compounds
bone
receptor modulators
Prior art date
Application number
PCT/US2007/022798
Other languages
English (en)
Other versions
WO2008057309A2 (fr
Inventor
Zhoupeng Zhang
Robert R Wilkening
Mark L Greenlee
Amy Kathleen Fried
Original Assignee
Merck & Co Inc
Zhoupeng Zhang
Robert R Wilkening
Mark L Greenlee
Amy Kathleen Fried
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 Merck & Co Inc, Zhoupeng Zhang, Robert R Wilkening, Mark L Greenlee, Amy Kathleen Fried filed Critical Merck & Co Inc
Publication of WO2008057309A2 publication Critical patent/WO2008057309A2/fr
Publication of WO2008057309A3 publication Critical patent/WO2008057309A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C62/00—Compounds having carboxyl groups bound to carbon atoms of rings other than six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C62/30—Unsaturated compounds
    • C07C62/38—Unsaturated compounds containing keto groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C305/00—Esters of sulfuric acids
    • C07C305/22—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/63—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/65—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by splitting-off hydrogen atoms or functional groups; by hydrogenolysis of functional groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/65—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by splitting-off hydrogen atoms or functional groups; by hydrogenolysis of functional groups
    • C07C45/66—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by splitting-off hydrogen atoms or functional groups; by hydrogenolysis of functional groups by dehydration
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/673—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/673—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton
    • C07C45/676—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton by elimination of carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/78—Separation; Purification; Stabilisation; Use of additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/703—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups
    • C07C49/747—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/753—Unsaturated compounds containing a keto groups being part of a ring containing ether groups, groups, groups, or groups
    • C07C49/755—Unsaturated compounds containing a keto groups being part of a ring containing ether groups, groups, groups, or groups a keto group being part of a condensed ring system with two or three rings, at least one ring being a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/16—Benz[e]indenes; Hydrogenated benz[e]indenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/56—Ring systems containing bridged rings
    • C07C2603/86—Ring systems containing bridged rings containing four rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La présente invention concerne des composés et leurs dérivés, leur synthèse, et leur utilisation en tant que modulateurs de récepteur d'oestrogène. Les composés de la présente invention sont des ligands des récepteurs d'oestrogène qui, comme tels, peuvent être utiles pour le traitement ou la prévention d'une variété de troubles associés au fonctionnement de l'oestrogène comprenant : la perte de la masse osseuse, les fractures osseuses, l'ostéoporose, les troubles osseux métastatiques, la maladie de Paget, les troubles parodontaux, la dégénération cartilagineuse, l'endométriose, le fibrome utérin, les bouffées de chaleur, l'augmentation des niveaux de cholestérol LDL, les maladies cardio-vasculaires, l'affaiblissement des fonctions cognitives, l'affaiblissement bénin des fonctions cognitives liées à l'âge, les troubles dégénératifs cérébraux, la resténose, la gynécomastie, la prolifération des cellules musculaires lisses vasculaires, l'obésité, l'incontinence, l'inflammation, l'affection abdominale inflammatoire, le syndrome du colon irritable, les troubles sexuels, l'hypertension, la dégénération rétinienne et le cancer, en particulier du sein, de l'utérus et de la prostate.
PCT/US2007/022798 2006-11-02 2007-10-29 Modulateurs de récepteur d'oestrogène WO2008057309A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US85614206P 2006-11-02 2006-11-02
US60/856,142 2006-11-02

Publications (2)

Publication Number Publication Date
WO2008057309A2 WO2008057309A2 (fr) 2008-05-15
WO2008057309A3 true WO2008057309A3 (fr) 2008-08-07

Family

ID=39365014

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2007/022798 WO2008057309A2 (fr) 2006-11-02 2007-10-29 Modulateurs de récepteur d'oestrogène

Country Status (1)

Country Link
WO (1) WO2008057309A2 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9359315B2 (en) 2013-09-10 2016-06-07 Arrien Pharmaceuticals Llc Substituted 2,3-dihydro-1H-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis
CN113197893A (zh) * 2021-05-31 2021-08-03 福建医科大学附属第一医院 赤霉素及其衍生物在制备预防和/或治疗中枢神经系统疾病的用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001082923A1 (fr) * 2000-02-14 2001-11-08 Merck & Co., Inc. Modulateurs de recepteurs d'oestrogene
WO2006026316A2 (fr) * 2004-08-26 2006-03-09 Wyeth Promedicament derive de benzoxazoles substitues en tant qu'agent oestrogenique

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001082923A1 (fr) * 2000-02-14 2001-11-08 Merck & Co., Inc. Modulateurs de recepteurs d'oestrogene
WO2006026316A2 (fr) * 2004-08-26 2006-03-09 Wyeth Promedicament derive de benzoxazoles substitues en tant qu'agent oestrogenique

Also Published As

Publication number Publication date
WO2008057309A2 (fr) 2008-05-15

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