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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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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GIESE, Anja ; LIENAU, Philip ; PÜEHLER, Florian ; HÄGEBARTH, Andrea ; GOLZ, Stefan</creator><creatorcontrib>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</creatorcontrib><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.</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&date=20171227&DB=EPODOC&CC=EP&NR=3259251A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,309,782,887,25571,76555</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20171227&DB=EPODOC&CC=EP&NR=3259251A1$$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**; 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.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2017</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjLEOgjAUAFkcjPoPb9ShA6CD4xMe9CXQNm2F4EKIqZNREhz8fDHxA5xuuMsto7cSRpLqKrGttTVSV6zEXnQVaAuGDVm88Kx3mJHHmnOCnCw36LkhB6hy8JLYwtkRoANWkk_stXWgi6-CVnlwXCqs5nUJBr1ssXPraHEb7lPY_LiKoCCfSRHGZx-mcbiGR3j1ZNLkcEwOMcbpH8kHJm45nw</recordid><startdate>20171227</startdate><enddate>20171227</enddate><creator>MÖNNING, Ursula</creator><creator>SCOTT, William, J</creator><creator>ZORN, Ludwig</creator><creator>BASTING, Daniel</creator><creator>SIEGEL, Franziska</creator><creator>LIU, Ningshu</creator><creator>MÖWES, Manfred</creator><creator>SCHNEIDER, Dirk</creator><creator>THEDE, Kai</creator><creator>BENDER, Eckhard</creator><creator>GIESE, Anja</creator><creator>LIENAU, Philip</creator><creator>PÜEHLER, Florian</creator><creator>HÄGEBARTH, Andrea</creator><creator>GOLZ, Stefan</creator><scope>EVB</scope></search><sort><creationdate>20171227</creationdate><title>N-PHENYL-(MORPHOLIN-4-YL OR PIPERAZINYL)ACETAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE WNT SIGNALLING PATHWAYS</title><author>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</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_EP3259251A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fre ; ger</language><creationdate>2017</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>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><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><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>MÖNNING, Ursula</au><au>SCOTT, William, J</au><au>ZORN, Ludwig</au><au>BASTING, Daniel</au><au>SIEGEL, Franziska</au><au>LIU, Ningshu</au><au>MÖWES, Manfred</au><au>SCHNEIDER, Dirk</au><au>THEDE, Kai</au><au>BENDER, Eckhard</au><au>GIESE, Anja</au><au>LIENAU, Philip</au><au>PÜEHLER, Florian</au><au>HÄGEBARTH, Andrea</au><au>GOLZ, Stefan</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>N-PHENYL-(MORPHOLIN-4-YL OR PIPERAZINYL)ACETAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE WNT SIGNALLING PATHWAYS</title><date>2017-12-27</date><risdate>2017</risdate><abstract>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.</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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