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WO2004091488A3 - Estrogen receptor modulators - Google Patents

Estrogen receptor modulators Download PDF

Info

Publication number
WO2004091488A3
WO2004091488A3 PCT/US2004/010853 US2004010853W WO2004091488A3 WO 2004091488 A3 WO2004091488 A3 WO 2004091488A3 US 2004010853 W US2004010853 W US 2004010853W WO 2004091488 A3 WO2004091488 A3 WO 2004091488A3
Authority
WO
WIPO (PCT)
Prior art keywords
estrogen
receptor modulators
compounds
estrogen receptor
functioning
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2004/010853
Other languages
French (fr)
Other versions
WO2004091488A2 (en
Inventor
Frank P Dininno
Helen Y Chen
Qiang Tan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
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 and Co Inc filed Critical Merck and Co Inc
Publication of WO2004091488A2 publication Critical patent/WO2004091488A2/en
Publication of WO2004091488A3 publication Critical patent/WO2004091488A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/60—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with aryl radicals attached in position 2

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
PCT/US2004/010853 2003-04-14 2004-04-09 Estrogen receptor modulators Ceased WO2004091488A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US46263503P 2003-04-14 2003-04-14
US60/462,635 2003-04-14

Publications (2)

Publication Number Publication Date
WO2004091488A2 WO2004091488A2 (en) 2004-10-28
WO2004091488A3 true WO2004091488A3 (en) 2005-04-07

Family

ID=33299962

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/010853 Ceased WO2004091488A2 (en) 2003-04-14 2004-04-09 Estrogen receptor modulators

Country Status (1)

Country Link
WO (1) WO2004091488A2 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011021167A1 (en) * 2009-08-19 2011-02-24 University Of The Free State Synthesis of c-3 coupled biflavonoids and c-3 coupled biflavonoid analogues
DK2580210T5 (en) * 2010-06-10 2017-06-19 Seragon Pharmaceuticals Inc ESTROGEN RECEPTOR MODULATORS AND APPLICATIONS THEREOF
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
WO2013090829A1 (en) 2011-12-14 2013-06-20 Aragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
CA2857061A1 (en) 2011-12-16 2013-06-20 Olema Pharmaceuticals, Inc. Novel benzopyran compounds, compositions and uses thereof
WO2014203132A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Substituted benzopyran compounds, compositions and uses thereof
JP6576916B2 (en) * 2013-06-19 2019-09-18 セラゴン ファーマシューティカルズ， インク． Estrogen receptor modulators and uses thereof
WO2014203129A1 (en) 2013-06-19 2014-12-24 Olema Pharmaceuticals, Inc. Combinations of benzopyran compounds, compositions and uses thereof
JP6389517B2 (en) * 2013-06-19 2018-09-12 セラゴン ファーマシューティカルズ， インク． Azetidine estrogen receptor modulator and use thereof
CN107531722B (en) 2015-05-26 2020-07-17 豪夫迈·罗氏有限公司 Heterocyclic estrogen receptor modulators and uses thereof
SI3368519T1 (en) * 2015-10-27 2022-07-29 Sun Pharma Advanced Research Company Limited Novel heterocyclic antiestrogens
CA3012078C (en) * 2016-02-05 2024-01-30 Inventisbio Inc. Selective estrogen receptor degraders and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5395842A (en) * 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
US20010025028A1 (en) * 1998-03-13 2001-09-27 Merck & Co., Inc. Methods of inhibiting bone resorption

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5395842A (en) * 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
US20010025028A1 (en) * 1998-03-13 2001-09-27 Merck & Co., Inc. Methods of inhibiting bone resorption

Also Published As

Publication number Publication date
WO2004091488A2 (en) 2004-10-28

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