Substituted 6,7-Dihydro-5H-Benzo[7]Annulene Compounds and Their Derivatives, Processes for Their Preparation and Therapeutic Uses Thereof

Disclosed herein are compounds of the formula (I), or pharmaceutically acceptable salts thereof wherein R1 and R2 represent a hydrogen atom or a deuterium atom; R3 represents a hydrogen atom, a -COOH group or a -OH group; R3′ and R3″ represent a hydrogen atom, a methyl group, a methoxy group, a chlo...

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Hauptverfasser: El Ahmad, Youssef, Halley, Frank, Terrier, Corinne, De Bruin, Béatrice, Bernardelli, Patrick, Nicolai, Eric, Da Rocha, Alice, Slowinski, Franck, Bianciotto, Marc, Certal, Victor, Periers, Anne-Marie, Mougenot, Patrick, Petit, Frédéric
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creator El Ahmad, Youssef
Halley, Frank
Terrier, Corinne
De Bruin, Béatrice
Bernardelli, Patrick
Nicolai, Eric
Da Rocha, Alice
Slowinski, Franck
Bianciotto, Marc
Certal, Victor
Periers, Anne-Marie
Mougenot, Patrick
Petit, Frédéric
description Disclosed herein are compounds of the formula (I), or pharmaceutically acceptable salts thereof wherein R1 and R2 represent a hydrogen atom or a deuterium atom; R3 represents a hydrogen atom, a -COOH group or a -OH group; R3′ and R3″ represent a hydrogen atom, a methyl group, a methoxy group, a chlorine atom, a fluorine atom, or a cyano group; R4 and R5 represent a hydrogen atom, a halogen atom, a -IMH2 group, a (C1-C3)alkyl group, a (C1-C3)alkoxy group, or a -OH group; or R4 and R5 together form an oxo group or R4 and R5 together form a ═NOCH3 group or a (C3-C5)cycloalkyl group; R7 represents a hydrogen atom, a methyl group, a -OH group or a fluorine atom; R6 represents a phenyl group, a fused phenyl group, a bicyclic group comprising 5 to 12 carbon atoms, a heteroaryl group comprising 2 to 9 carbon atoms and comprising from 1 to 3 heteroatoms, a cycloalkyl group comprising 3 to 7 carbon atoms, a (C3-C6) cycloalkyl (C1-C3) alkyl group, a 3 to 8 membered-heterocycloalkyl group, a (C1-C6)alkyl group or a phenyl (C1-C2) alkyl group; X represents -CH2-, -O- or -S-; Y represents -CH═, -N═ or -CR″═; R8 represents a (C1-C3) alkyl group, a halogen atom, a cyano group, or a (C1-C3) fluoroalkyl group; R9 represents a hydrogen atom or a fluorine atom; RIO and RIO′ represent a hydrogen atom or a fluorine atom; Rll represents a hydrogen atom a (C1-C3)alkyl group or a cyclopropyl group; n is 0, 1 or 2, and m is 0 or 1. Further disclosed are process for preparing the same, pharmaceutical compositions comprising them as well as said compounds of formula (I) for use as an inhibitor and degrader of estrogen receptors, in particular in the treatment of ovulatory dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hypertrophy or inflammation.
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Further disclosed are process for preparing the same, pharmaceutical compositions comprising them as well as said compounds of formula (I) for use as an inhibitor and degrader of estrogen receptors, in particular in the treatment of ovulatory dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hypertrophy or inflammation.</description><language>eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2023</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20231130&amp;DB=EPODOC&amp;CC=US&amp;NR=2023382854A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20231130&amp;DB=EPODOC&amp;CC=US&amp;NR=2023382854A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>El Ahmad, Youssef</creatorcontrib><creatorcontrib>Halley, Frank</creatorcontrib><creatorcontrib>Terrier, Corinne</creatorcontrib><creatorcontrib>De Bruin, Béatrice</creatorcontrib><creatorcontrib>Bernardelli, Patrick</creatorcontrib><creatorcontrib>Nicolai, Eric</creatorcontrib><creatorcontrib>Da Rocha, Alice</creatorcontrib><creatorcontrib>Slowinski, Franck</creatorcontrib><creatorcontrib>Bianciotto, Marc</creatorcontrib><creatorcontrib>Certal, Victor</creatorcontrib><creatorcontrib>Periers, Anne-Marie</creatorcontrib><creatorcontrib>Mougenot, Patrick</creatorcontrib><creatorcontrib>Petit, Frédéric</creatorcontrib><title>Substituted 6,7-Dihydro-5H-Benzo[7]Annulene Compounds and Their Derivatives, Processes for Their Preparation and Therapeutic Uses Thereof</title><description>Disclosed herein are compounds of the formula (I), or pharmaceutically acceptable salts thereof wherein R1 and R2 represent a hydrogen atom or a deuterium atom; R3 represents a hydrogen atom, a -COOH group or a -OH group; R3′ and R3″ represent a hydrogen atom, a methyl group, a methoxy group, a chlorine atom, a fluorine atom, or a cyano group; R4 and R5 represent a hydrogen atom, a halogen atom, a -IMH2 group, a (C1-C3)alkyl group, a (C1-C3)alkoxy group, or a -OH group; or R4 and R5 together form an oxo group or R4 and R5 together form a ═NOCH3 group or a (C3-C5)cycloalkyl group; R7 represents a hydrogen atom, a methyl group, a -OH group or a fluorine atom; R6 represents a phenyl group, a fused phenyl group, a bicyclic group comprising 5 to 12 carbon atoms, a heteroaryl group comprising 2 to 9 carbon atoms and comprising from 1 to 3 heteroatoms, a cycloalkyl group comprising 3 to 7 carbon atoms, a (C3-C6) cycloalkyl (C1-C3) alkyl group, a 3 to 8 membered-heterocycloalkyl group, a (C1-C6)alkyl group or a phenyl (C1-C2) alkyl group; X represents -CH2-, -O- or -S-; Y represents -CH═, -N═ or -CR″═; R8 represents a (C1-C3) alkyl group, a halogen atom, a cyano group, or a (C1-C3) fluoroalkyl group; R9 represents a hydrogen atom or a fluorine atom; RIO and RIO′ represent a hydrogen atom or a fluorine atom; Rll represents a hydrogen atom a (C1-C3)alkyl group or a cyclopropyl group; n is 0, 1 or 2, and m is 0 or 1. 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Halley, Frank ; Terrier, Corinne ; De Bruin, Béatrice ; Bernardelli, Patrick ; Nicolai, Eric ; Da Rocha, Alice ; Slowinski, Franck ; Bianciotto, Marc ; Certal, Victor ; Periers, Anne-Marie ; Mougenot, Patrick ; Petit, Frédéric</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_US2023382854A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2023</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>El Ahmad, Youssef</creatorcontrib><creatorcontrib>Halley, Frank</creatorcontrib><creatorcontrib>Terrier, Corinne</creatorcontrib><creatorcontrib>De Bruin, Béatrice</creatorcontrib><creatorcontrib>Bernardelli, Patrick</creatorcontrib><creatorcontrib>Nicolai, Eric</creatorcontrib><creatorcontrib>Da Rocha, Alice</creatorcontrib><creatorcontrib>Slowinski, Franck</creatorcontrib><creatorcontrib>Bianciotto, Marc</creatorcontrib><creatorcontrib>Certal, Victor</creatorcontrib><creatorcontrib>Periers, Anne-Marie</creatorcontrib><creatorcontrib>Mougenot, Patrick</creatorcontrib><creatorcontrib>Petit, Frédéric</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>El Ahmad, Youssef</au><au>Halley, Frank</au><au>Terrier, Corinne</au><au>De Bruin, Béatrice</au><au>Bernardelli, Patrick</au><au>Nicolai, Eric</au><au>Da Rocha, Alice</au><au>Slowinski, Franck</au><au>Bianciotto, Marc</au><au>Certal, Victor</au><au>Periers, Anne-Marie</au><au>Mougenot, Patrick</au><au>Petit, Frédéric</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Substituted 6,7-Dihydro-5H-Benzo[7]Annulene Compounds and Their Derivatives, Processes for Their Preparation and Therapeutic Uses Thereof</title><date>2023-11-30</date><risdate>2023</risdate><abstract>Disclosed herein are compounds of the formula (I), or pharmaceutically acceptable salts thereof wherein R1 and R2 represent a hydrogen atom or a deuterium atom; R3 represents a hydrogen atom, a -COOH group or a -OH group; R3′ and R3″ represent a hydrogen atom, a methyl group, a methoxy group, a chlorine atom, a fluorine atom, or a cyano group; R4 and R5 represent a hydrogen atom, a halogen atom, a -IMH2 group, a (C1-C3)alkyl group, a (C1-C3)alkoxy group, or a -OH group; or R4 and R5 together form an oxo group or R4 and R5 together form a ═NOCH3 group or a (C3-C5)cycloalkyl group; R7 represents a hydrogen atom, a methyl group, a -OH group or a fluorine atom; R6 represents a phenyl group, a fused phenyl group, a bicyclic group comprising 5 to 12 carbon atoms, a heteroaryl group comprising 2 to 9 carbon atoms and comprising from 1 to 3 heteroatoms, a cycloalkyl group comprising 3 to 7 carbon atoms, a (C3-C6) cycloalkyl (C1-C3) alkyl group, a 3 to 8 membered-heterocycloalkyl group, a (C1-C6)alkyl group or a phenyl (C1-C2) alkyl group; X represents -CH2-, -O- or -S-; Y represents -CH═, -N═ or -CR″═; R8 represents a (C1-C3) alkyl group, a halogen atom, a cyano group, or a (C1-C3) fluoroalkyl group; R9 represents a hydrogen atom or a fluorine atom; RIO and RIO′ represent a hydrogen atom or a fluorine atom; Rll represents a hydrogen atom a (C1-C3)alkyl group or a cyclopropyl group; n is 0, 1 or 2, and m is 0 or 1. Further disclosed are process for preparing the same, pharmaceutical compositions comprising them as well as said compounds of formula (I) for use as an inhibitor and degrader of estrogen receptors, in particular in the treatment of ovulatory dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hypertrophy or inflammation.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Substituted 6,7-Dihydro-5H-Benzo[7]Annulene Compounds and Their Derivatives, Processes for Their Preparation and Therapeutic Uses Thereof
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