Tetrahydroquinazoline-2,4-diones and therapeutic uses thereof
The present invention relates to tetrahydroquinazoline-2,4-diones derivatives of the formula (I): pharmaceutically acceptable salts thereof, wherein A is (CH2)n where n is equal to 0, 1 or 2; U is CH2, NH, or NR3, R1 and R2 are selected independently from H, (C1-C6)alkyl, Cl, F, CN, nitro, CF3, -NHC...
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creator | GALLASCHUN RANDAL JAMES JONES BRIAN PATRICK RAGAN JOHN ANTHONY FLIRI ANTON FRANZ JOSEPH BUTLER TODD WILLIAM |
description | The present invention relates to tetrahydroquinazoline-2,4-diones derivatives of the formula (I): pharmaceutically acceptable salts thereof, wherein A is (CH2)n where n is equal to 0, 1 or 2; U is CH2, NH, or NR3, R1 and R2 are selected independently from H, (C1-C6)alkyl, Cl, F, CN, nitro, CF3, -NHC(O)R6 and -OR7, or R1 and R2, together with the atoms to which they are attached, form a carbocyclic or heterocyclic five- or six-membered ring, R3 is selected from the group consisting of H, (C1-C6)malkyl, C(=O)-(C1-C6)alkyl, where m=1 or 2; R4 and R5 are selected from H, (C1-C6)alkyl, Cl, F, -CF3, -CN, -NHC(=O)R6, -OR7, a 5-to 7-membered aryl or heteroaryl ring, where m, R6 and R7 are as defined above; and R6 and R7 are selected independently from H, (C1-C6)alkyl or a 5- to 7-membered aryl or heteroaryl ring; V is CH, CR3, or N; W is CH2, C(O), or S(O)2; X is C or N; and Y is CH, CR1, CR2, or N. The invention also relates to pharmaceutical compositions containing the same and to methods of use thereof, including in the inhibition of serotonin reuptake, the inhibition of the binding of 5-HT2A serotonin receptors and the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to methods for the preparation of 4-(4-phenyl-1,2,3,6-tetrahydropyridin-1-yl)-propyl-1,2,3,4-tetrahydroquinazoline-2,4-dione compounds and intermediates useful therefor. |
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The invention also relates to pharmaceutical compositions containing the same and to methods of use thereof, including in the inhibition of serotonin reuptake, the inhibition of the binding of 5-HT2A serotonin receptors and the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to methods for the preparation of 4-(4-phenyl-1,2,3,6-tetrahydropyridin-1-yl)-propyl-1,2,3,4-tetrahydroquinazoline-2,4-dione compounds and intermediates useful therefor.</description><edition>7</edition><language>eng</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; 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>2003</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=20030612&DB=EPODOC&CC=US&NR=2003109516A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,309,781,886,25569,76552</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20030612&DB=EPODOC&CC=US&NR=2003109516A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>GALLASCHUN RANDAL JAMES</creatorcontrib><creatorcontrib>JONES BRIAN PATRICK</creatorcontrib><creatorcontrib>RAGAN JOHN ANTHONY</creatorcontrib><creatorcontrib>FLIRI ANTON FRANZ JOSEPH</creatorcontrib><creatorcontrib>BUTLER TODD WILLIAM</creatorcontrib><title>Tetrahydroquinazoline-2,4-diones and therapeutic uses thereof</title><description>The present invention relates to tetrahydroquinazoline-2,4-diones derivatives of the formula (I): pharmaceutically acceptable salts thereof, wherein A is (CH2)n where n is equal to 0, 1 or 2; U is CH2, NH, or NR3, R1 and R2 are selected independently from H, (C1-C6)alkyl, Cl, F, CN, nitro, CF3, -NHC(O)R6 and -OR7, or R1 and R2, together with the atoms to which they are attached, form a carbocyclic or heterocyclic five- or six-membered ring, R3 is selected from the group consisting of H, (C1-C6)malkyl, C(=O)-(C1-C6)alkyl, where m=1 or 2; R4 and R5 are selected from H, (C1-C6)alkyl, Cl, F, -CF3, -CN, -NHC(=O)R6, -OR7, a 5-to 7-membered aryl or heteroaryl ring, where m, R6 and R7 are as defined above; and R6 and R7 are selected independently from H, (C1-C6)alkyl or a 5- to 7-membered aryl or heteroaryl ring; V is CH, CR3, or N; W is CH2, C(O), or S(O)2; X is C or N; and Y is CH, CR1, CR2, or N. The invention also relates to pharmaceutical compositions containing the same and to methods of use thereof, including in the inhibition of serotonin reuptake, the inhibition of the binding of 5-HT2A serotonin receptors and the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to methods for the preparation of 4-(4-phenyl-1,2,3,6-tetrahydropyridin-1-yl)-propyl-1,2,3,4-tetrahydroquinazoline-2,4-dione compounds and intermediates useful therefor.</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</subject><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>2003</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZLANSS0pSsyoTCnKLyzNzEusys_JzEvVNdIx0U3JzM9LLVZIzEtRKMlILUosSC0tyUxWKC0GCoIEUvPTeBhY0xJzilN5oTQ3g7Kba4izh25qQX58anFBYnJqXmpJfGiwkYGBsaGBpamhmaOhMXGqAANoMU8</recordid><startdate>20030612</startdate><enddate>20030612</enddate><creator>GALLASCHUN RANDAL JAMES</creator><creator>JONES BRIAN PATRICK</creator><creator>RAGAN JOHN ANTHONY</creator><creator>FLIRI ANTON FRANZ JOSEPH</creator><creator>BUTLER TODD WILLIAM</creator><scope>EVB</scope></search><sort><creationdate>20030612</creationdate><title>Tetrahydroquinazoline-2,4-diones and therapeutic uses thereof</title><author>GALLASCHUN RANDAL JAMES ; JONES BRIAN PATRICK ; RAGAN JOHN ANTHONY ; FLIRI ANTON FRANZ JOSEPH ; BUTLER TODD WILLIAM</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_US2003109516A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2003</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</topic><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>GALLASCHUN RANDAL JAMES</creatorcontrib><creatorcontrib>JONES BRIAN PATRICK</creatorcontrib><creatorcontrib>RAGAN JOHN ANTHONY</creatorcontrib><creatorcontrib>FLIRI ANTON FRANZ JOSEPH</creatorcontrib><creatorcontrib>BUTLER TODD WILLIAM</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>GALLASCHUN RANDAL JAMES</au><au>JONES BRIAN PATRICK</au><au>RAGAN JOHN ANTHONY</au><au>FLIRI ANTON FRANZ JOSEPH</au><au>BUTLER TODD WILLIAM</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Tetrahydroquinazoline-2,4-diones and therapeutic uses thereof</title><date>2003-06-12</date><risdate>2003</risdate><abstract>The present invention relates to tetrahydroquinazoline-2,4-diones derivatives of the formula (I): pharmaceutically acceptable salts thereof, wherein A is (CH2)n where n is equal to 0, 1 or 2; U is CH2, NH, or NR3, R1 and R2 are selected independently from H, (C1-C6)alkyl, Cl, F, CN, nitro, CF3, -NHC(O)R6 and -OR7, or R1 and R2, together with the atoms to which they are attached, form a carbocyclic or heterocyclic five- or six-membered ring, R3 is selected from the group consisting of H, (C1-C6)malkyl, C(=O)-(C1-C6)alkyl, where m=1 or 2; R4 and R5 are selected from H, (C1-C6)alkyl, Cl, F, -CF3, -CN, -NHC(=O)R6, -OR7, a 5-to 7-membered aryl or heteroaryl ring, where m, R6 and R7 are as defined above; and R6 and R7 are selected independently from H, (C1-C6)alkyl or a 5- to 7-membered aryl or heteroaryl ring; V is CH, CR3, or N; W is CH2, C(O), or S(O)2; X is C or N; and Y is CH, CR1, CR2, or N. The invention also relates to pharmaceutical compositions containing the same and to methods of use thereof, including in the inhibition of serotonin reuptake, the inhibition of the binding of 5-HT2A serotonin receptors and the treatment of diseases, conditions or disorders of the central nervous system. Further, the present invention is also directed to methods for the preparation of 4-(4-phenyl-1,2,3,6-tetrahydropyridin-1-yl)-propyl-1,2,3,4-tetrahydroquinazoline-2,4-dione compounds and intermediates useful therefor.</abstract><edition>7</edition><oa>free_for_read</oa></addata></record> |
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subjects | ACYCLIC OR CARBOCYCLIC COMPOUNDS 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 | Tetrahydroquinazoline-2,4-diones and therapeutic uses thereof |
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