N-PHENYL-(MORPHOLIN-4-YL OR PIPERAZINYL)ACETAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE WNT SIGNALLING PATHWAYS

The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) wherein LA represents *CH2** or *Δ**; wherein indicates the point of attachment to the carbonyl group, and ** indicates the point of attachment to R1; LB represents *N(H)-C(=O)** or *C(=O)-N(H)**; where...

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Hauptverfasser: MÖNNING, Ursula, SCOTT, William, J, ZORN, Ludwig, BASTING, Daniel, SIEGEL, Franziska, LIU, Ningshu, MÖWES, Manfred, SCHNEIDER, Dirk, THEDE, Kai, BENDER, Eckhard, GIESE, Anja, LIENAU, Philip, PÜEHLER, Florian, HÄGEBARTH, Andrea, GOLZ, Stefan
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creator MÖNNING, Ursula
SCOTT, William, J
ZORN, Ludwig
BASTING, Daniel
SIEGEL, Franziska
LIU, Ningshu
MÖWES, Manfred
SCHNEIDER, Dirk
THEDE, Kai
BENDER, Eckhard
GIESE, Anja
LIENAU, Philip
PÜEHLER, Florian
HÄGEBARTH, Andrea
GOLZ, Stefan
description The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) wherein LA represents *CH2** or *Δ**; wherein indicates the point of attachment to the carbonyl group, and ** indicates the point of attachment to R1; LB represents *N(H)-C(=O)** or *C(=O)-N(H)**; wherein * indicates the point of attachment to R2, and ** indicates the point of attachment to the phenyl group; R1 represents a group selected from: (AA); wherein * indicates the point of attachment to LA, R2 represents: (BB) wherein * indicates the point of attachment to R3, and ** indicates the point of attachment to LB R3 represents a group selected from: (CC); wherein * indicates the point of attachment to R2; R4 and R5 represent a hydrogen atom; and R6 represents a halogen atom or group selected from: -CH3, -O-CH3, -O-CHF2, -O-CF3, and -O-cyclopropyl; to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular, of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.
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wherein * indicates the point of attachment to R2; R4 and R5 represent a hydrogen atom; and R6 represents a halogen atom or group selected from: -CH3, -O-CH3, -O-CHF2, -O-CF3, and -O-cyclopropyl; to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular, of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.</description><language>eng ; fre ; ger</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2017</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=20171227&amp;DB=EPODOC&amp;CC=EP&amp;NR=3259251A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,309,782,887,25571,76555</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20171227&amp;DB=EPODOC&amp;CC=EP&amp;NR=3259251A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>MÖNNING, Ursula</creatorcontrib><creatorcontrib>SCOTT, William, J</creatorcontrib><creatorcontrib>ZORN, Ludwig</creatorcontrib><creatorcontrib>BASTING, Daniel</creatorcontrib><creatorcontrib>SIEGEL, Franziska</creatorcontrib><creatorcontrib>LIU, Ningshu</creatorcontrib><creatorcontrib>MÖWES, Manfred</creatorcontrib><creatorcontrib>SCHNEIDER, Dirk</creatorcontrib><creatorcontrib>THEDE, Kai</creatorcontrib><creatorcontrib>BENDER, Eckhard</creatorcontrib><creatorcontrib>GIESE, Anja</creatorcontrib><creatorcontrib>LIENAU, Philip</creatorcontrib><creatorcontrib>PÜEHLER, Florian</creatorcontrib><creatorcontrib>HÄGEBARTH, Andrea</creatorcontrib><creatorcontrib>GOLZ, Stefan</creatorcontrib><title>N-PHENYL-(MORPHOLIN-4-YL OR PIPERAZINYL)ACETAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE WNT SIGNALLING PATHWAYS</title><description>The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) wherein LA represents *CH2** or *Δ**; 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wherein indicates the point of attachment to the carbonyl group, and ** indicates the point of attachment to R1; LB represents *N(H)-C(=O)** or *C(=O)-N(H)**; wherein * indicates the point of attachment to R2, and ** indicates the point of attachment to the phenyl group; R1 represents a group selected from: (AA); wherein * indicates the point of attachment to LA, R2 represents: (BB) wherein * indicates the point of attachment to R3, and ** indicates the point of attachment to LB R3 represents a group selected from: (CC); wherein * indicates the point of attachment to R2; R4 and R5 represent a hydrogen atom; and R6 represents a halogen atom or group selected from: -CH3, -O-CH3, -O-CHF2, -O-CF3, and -O-cyclopropyl; to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular, of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.</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
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title N-PHENYL-(MORPHOLIN-4-YL OR PIPERAZINYL)ACETAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE WNT SIGNALLING PATHWAYS
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