ARYLPIPERAZUINE DERIVATIVES AS SELECTIVE LIGAND FOR THE DOPAMINE D3 RECEPTOR
Spoj formule (I): naznačen time da: R1 predstavlja heteroaril od pet ili šest lančanih veza, koji sadrži jedan ili više heteroatoma, izabran između 2-piridila, 2-pirimidinila, 2-piridazinila, 2-pirazinila, 2-imidazolila, 2-oksazolila, 2-tiazolila, 3-izoksazolila, 3-izotiazolila, 1,2,4-triazol-2-ila,...
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| creator | JEANNE-MARIE LECOMTE THIERRY CALMELS PHILIPPE ROBERT MARC CAPET ISABELLE BERREBI-BERTRAND JEANARLES SCHWARTZ MARCEL MORVAN DENIS DANVY NICOLAS LEVOIN |
| description | Spoj formule (I): naznačen time da: R1 predstavlja heteroaril od pet ili šest lančanih veza, koji sadrži jedan ili više heteroatoma, izabran između 2-piridila, 2-pirimidinila, 2-piridazinila, 2-pirazinila, 2-imidazolila, 2-oksazolila, 2-tiazolila, 3-izoksazolila, 3-izotiazolila, 1,2,4-triazol-2-ila, 1,3,4-oksadiazol-2-ila, 1,3,4-tiadiazol-2-ila, po želji supstituiran jednom ili više grupa, identičnih ili različitih, izabranih između halogenog atoma ili hidroksi-grupe, alkila, monofluoroalkila, polifluoroalkila, alkoksi, polifluoro-alkoksi, alkilsulfanila, polifluoroalkilsulfanila; Ar je aril ili heteroaril, po želji supstituiran jednim ili više identičnih ili različitih supstituenata, izabranih između halogenog atoma ili hidroksi-grupe, aklila, monofluoroalkila, polifluoroalkila, alkoksi,polifluoroalkoksi, alkilsulfanila, polifluoroalkilsulfanila, cijano, karbamoila, dialkilkarbamoila,alkil-C(=O)-, alkil-O-C(=O)-, HO-C(=O)-, (HO)alkil-, ili je Ar spojen s karbocikličkim ili heterocikličkim prstenom, odnosno zasićenim, nezasićenim ili aromatskim prstenom; a = 2, 3 ili 4; b i c su identični ili različiti i predstavljaju 1 ili 2; R2, R3, R4, R5 i R6 predstavljaju, svaki neovisno, atom vodika ili halogena ili hidroksi-grupu, alkil,monofluoroalkil, polifluoroalkil, alkoksi, polifluoroalkoksi, alkilsulfanil, polifluoroalkilsulfanil, cijano, -NRR', -COOR, -COR, -CONRR' ili su dva susjedna R2, R3, R4, R5 i R6 međusobno povezana i tvore karbociklički ili heterociklički prsten, zasićen ili nezasićen, spojen na fenilnu jezgru na koju su pričvršćeni; ili R i R', identični ili različiti, predstavljaju neovisno atom vodika ili alkilnu grupu; kao i njihovi stereoizomeri ili njihove smjese, tautomerni oblici, hidrati, solvati, farmaceutski prihvatljive soli i esteri. Patent sadrži još 22 patentna zahtjeva.
Arylpiperazine compounds (I) and their stereoisomers, tautomeric forms, hydrates, solvates, salts or esters are new. Arylpiperazine compounds of formula (I) and their stereoisomers, tautomeric forms, hydrates, solvates, salts or esters are new. R1 : heteroaryl with 5-6 chain links (optionally containing heteroatoms of 2-pyridyl, 2-pyrimidinyl, 2-pyridazinyl, 2-pyrazinyl, 2-imidazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl, 3-isothiazolyl, 1,2,4-triazol- 2-yl, 1,3,4-oxadiazol-2-yl or 1,3,4-thiadiazol-2-yl) (all optionally substituted by halo or OH), alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl or polyfluoroalkylsulfanyl group); Ar : (h |
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| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_HRP20070285TT3</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>HRP20070285TT3</sourcerecordid><originalsourceid>FETCH-epo_espacenet_HRP20070285TT33</originalsourceid><addsrcrecordid>eNrjZPBxDIr0CfAMcA1yjAr19HNVcHEN8gxzDPEMcw1WcAxWCHb1cXUG8RR8PN0d_VwU3PyDFEI8gOr8Axx9wRqMFYJcnV0DQvyDeBhY0xJzilN5oTQ3g7Kba4izh25qQX58anFBYnJqXmpJvEdQgJGBgbmBkYVpSIixMXGqAJNHL24</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>ARYLPIPERAZUINE DERIVATIVES AS SELECTIVE LIGAND FOR THE DOPAMINE D3 RECEPTOR</title><source>esp@cenet</source><creator>JEANNE-MARIE LECOMTE ; THIERRY CALMELS ; PHILIPPE ROBERT ; MARC CAPET ; ISABELLE BERREBI-BERTRAND ; JEANARLES SCHWARTZ ; MARCEL MORVAN ; DENIS DANVY ; NICOLAS LEVOIN</creator><creatorcontrib>JEANNE-MARIE LECOMTE ; THIERRY CALMELS ; PHILIPPE ROBERT ; MARC CAPET ; ISABELLE BERREBI-BERTRAND ; JEANARLES SCHWARTZ ; MARCEL MORVAN ; DENIS DANVY ; NICOLAS LEVOIN</creatorcontrib><description>Spoj formule (I): naznačen time da: R1 predstavlja heteroaril od pet ili šest lančanih veza, koji sadrži jedan ili više heteroatoma, izabran između 2-piridila, 2-pirimidinila, 2-piridazinila, 2-pirazinila, 2-imidazolila, 2-oksazolila, 2-tiazolila, 3-izoksazolila, 3-izotiazolila, 1,2,4-triazol-2-ila, 1,3,4-oksadiazol-2-ila, 1,3,4-tiadiazol-2-ila, po želji supstituiran jednom ili više grupa, identičnih ili različitih, izabranih između halogenog atoma ili hidroksi-grupe, alkila, monofluoroalkila, polifluoroalkila, alkoksi, polifluoro-alkoksi, alkilsulfanila, polifluoroalkilsulfanila; Ar je aril ili heteroaril, po želji supstituiran jednim ili više identičnih ili različitih supstituenata, izabranih između halogenog atoma ili hidroksi-grupe, aklila, monofluoroalkila, polifluoroalkila, alkoksi,polifluoroalkoksi, alkilsulfanila, polifluoroalkilsulfanila, cijano, karbamoila, dialkilkarbamoila,alkil-C(=O)-, alkil-O-C(=O)-, HO-C(=O)-, (HO)alkil-, ili je Ar spojen s karbocikličkim ili heterocikličkim prstenom, odnosno zasićenim, nezasićenim ili aromatskim prstenom; a = 2, 3 ili 4; b i c su identični ili različiti i predstavljaju 1 ili 2; R2, R3, R4, R5 i R6 predstavljaju, svaki neovisno, atom vodika ili halogena ili hidroksi-grupu, alkil,monofluoroalkil, polifluoroalkil, alkoksi, polifluoroalkoksi, alkilsulfanil, polifluoroalkilsulfanil, cijano, -NRR', -COOR, -COR, -CONRR' ili su dva susjedna R2, R3, R4, R5 i R6 međusobno povezana i tvore karbociklički ili heterociklički prsten, zasićen ili nezasićen, spojen na fenilnu jezgru na koju su pričvršćeni; ili R i R', identični ili različiti, predstavljaju neovisno atom vodika ili alkilnu grupu; kao i njihovi stereoizomeri ili njihove smjese, tautomerni oblici, hidrati, solvati, farmaceutski prihvatljive soli i esteri. Patent sadrži još 22 patentna zahtjeva.
Arylpiperazine compounds (I) and their stereoisomers, tautomeric forms, hydrates, solvates, salts or esters are new. Arylpiperazine compounds of formula (I) and their stereoisomers, tautomeric forms, hydrates, solvates, salts or esters are new. R1 : heteroaryl with 5-6 chain links (optionally containing heteroatoms of 2-pyridyl, 2-pyrimidinyl, 2-pyridazinyl, 2-pyrazinyl, 2-imidazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl, 3-isothiazolyl, 1,2,4-triazol- 2-yl, 1,3,4-oxadiazol-2-yl or 1,3,4-thiadiazol-2-yl) (all optionally substituted by halo or OH), alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl or polyfluoroalkylsulfanyl group); Ar : (hetero)aryl (optionally fused with R1 and optionally substituted by halo or OH), alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl, polyfluoroalkylsulfanyl, CN, carbamoyl, dialkylcarbamoyl, alkyl-C(=O)-, alkyl-O-C(=O)-, HO-C(=O)-, (HO)alkyl group or fused with optionally saturated or aromatic hydrocarbon cycle or heterocycle; a : 2-4; b, c : 1-2; either R2-R6 : H, halo, OH, alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl, polyfluoroalkylsulfanyl, CN, -NRR-a, COOR, COR or CONRR-a group; R2+R3+R4+R5+R6 : hydrocarbon cycle or optionally saturated heterocycle (both are fused to the phenyl nucleus to which they are attached); and R, R-a : H or alkyl. Provided that compounds for which R1 is 2-oxazolyl, 2-imidazolyl or 2-thiazolyl fused to the Ar group (optionally substituted phenyl), and compounds for which R1 is 2-pyridyl group, fused to the Ar group phenyl (optionally substituted by CH3 in position 4 of the resultant quinoline cycle, a is 2, b, c are 1, R2 is H, OCH3 and R3-R6 is H or R2, R3 are Me and R4-R6 is H; R1 is 2-pyrimidinyl group, fused to the Ar group is phenyl substituted by OCH3 in positions 6 and 7 and -OH in position 4 or 6 of the resultant quinazolinyl cycle, a is 2, b, c are 1, R2-R5 are H and R6 is OCH3. Independent claims are also included for the preparations of (I). [Image] ACTIVITY : Neuroleptic; Antiaddictive; Endocrine-Gen.; Vasotropic; CNS-Gen.; Muscular-Gen.; Antiparkinsonian; Antidepressant. MECHANISM OF ACTION : Dopamine D3 receptor ligand. (I) were tested for dopamine D3 receptor ligand activity in HEK 293 cells. The inhibitory constant value of 2-{4-[4-(2,3-dichlorophenyl)piperazin-1-y l]butyl}amino-4-phenylpyridine was 0.55 nM.</description><language>hrv ; eng</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>2007</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=20070831&DB=EPODOC&CC=HR&NR=P20070285T3$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76289</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20070831&DB=EPODOC&CC=HR&NR=P20070285T3$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>JEANNE-MARIE LECOMTE</creatorcontrib><creatorcontrib>THIERRY CALMELS</creatorcontrib><creatorcontrib>PHILIPPE ROBERT</creatorcontrib><creatorcontrib>MARC CAPET</creatorcontrib><creatorcontrib>ISABELLE BERREBI-BERTRAND</creatorcontrib><creatorcontrib>JEANARLES SCHWARTZ</creatorcontrib><creatorcontrib>MARCEL MORVAN</creatorcontrib><creatorcontrib>DENIS DANVY</creatorcontrib><creatorcontrib>NICOLAS LEVOIN</creatorcontrib><title>ARYLPIPERAZUINE DERIVATIVES AS SELECTIVE LIGAND FOR THE DOPAMINE D3 RECEPTOR</title><description>Spoj formule (I): naznačen time da: R1 predstavlja heteroaril od pet ili šest lančanih veza, koji sadrži jedan ili više heteroatoma, izabran između 2-piridila, 2-pirimidinila, 2-piridazinila, 2-pirazinila, 2-imidazolila, 2-oksazolila, 2-tiazolila, 3-izoksazolila, 3-izotiazolila, 1,2,4-triazol-2-ila, 1,3,4-oksadiazol-2-ila, 1,3,4-tiadiazol-2-ila, po želji supstituiran jednom ili više grupa, identičnih ili različitih, izabranih između halogenog atoma ili hidroksi-grupe, alkila, monofluoroalkila, polifluoroalkila, alkoksi, polifluoro-alkoksi, alkilsulfanila, polifluoroalkilsulfanila; Ar je aril ili heteroaril, po želji supstituiran jednim ili više identičnih ili različitih supstituenata, izabranih između halogenog atoma ili hidroksi-grupe, aklila, monofluoroalkila, polifluoroalkila, alkoksi,polifluoroalkoksi, alkilsulfanila, polifluoroalkilsulfanila, cijano, karbamoila, dialkilkarbamoila,alkil-C(=O)-, alkil-O-C(=O)-, HO-C(=O)-, (HO)alkil-, ili je Ar spojen s karbocikličkim ili heterocikličkim prstenom, odnosno zasićenim, nezasićenim ili aromatskim prstenom; a = 2, 3 ili 4; b i c su identični ili različiti i predstavljaju 1 ili 2; R2, R3, R4, R5 i R6 predstavljaju, svaki neovisno, atom vodika ili halogena ili hidroksi-grupu, alkil,monofluoroalkil, polifluoroalkil, alkoksi, polifluoroalkoksi, alkilsulfanil, polifluoroalkilsulfanil, cijano, -NRR', -COOR, -COR, -CONRR' ili su dva susjedna R2, R3, R4, R5 i R6 međusobno povezana i tvore karbociklički ili heterociklički prsten, zasićen ili nezasićen, spojen na fenilnu jezgru na koju su pričvršćeni; ili R i R', identični ili različiti, predstavljaju neovisno atom vodika ili alkilnu grupu; kao i njihovi stereoizomeri ili njihove smjese, tautomerni oblici, hidrati, solvati, farmaceutski prihvatljive soli i esteri. Patent sadrži još 22 patentna zahtjeva.
Arylpiperazine compounds (I) and their stereoisomers, tautomeric forms, hydrates, solvates, salts or esters are new. Arylpiperazine compounds of formula (I) and their stereoisomers, tautomeric forms, hydrates, solvates, salts or esters are new. R1 : heteroaryl with 5-6 chain links (optionally containing heteroatoms of 2-pyridyl, 2-pyrimidinyl, 2-pyridazinyl, 2-pyrazinyl, 2-imidazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl, 3-isothiazolyl, 1,2,4-triazol- 2-yl, 1,3,4-oxadiazol-2-yl or 1,3,4-thiadiazol-2-yl) (all optionally substituted by halo or OH), alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl or polyfluoroalkylsulfanyl group); Ar : (hetero)aryl (optionally fused with R1 and optionally substituted by halo or OH), alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl, polyfluoroalkylsulfanyl, CN, carbamoyl, dialkylcarbamoyl, alkyl-C(=O)-, alkyl-O-C(=O)-, HO-C(=O)-, (HO)alkyl group or fused with optionally saturated or aromatic hydrocarbon cycle or heterocycle; a : 2-4; b, c : 1-2; either R2-R6 : H, halo, OH, alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl, polyfluoroalkylsulfanyl, CN, -NRR-a, COOR, COR or CONRR-a group; R2+R3+R4+R5+R6 : hydrocarbon cycle or optionally saturated heterocycle (both are fused to the phenyl nucleus to which they are attached); and R, R-a : H or alkyl. Provided that compounds for which R1 is 2-oxazolyl, 2-imidazolyl or 2-thiazolyl fused to the Ar group (optionally substituted phenyl), and compounds for which R1 is 2-pyridyl group, fused to the Ar group phenyl (optionally substituted by CH3 in position 4 of the resultant quinoline cycle, a is 2, b, c are 1, R2 is H, OCH3 and R3-R6 is H or R2, R3 are Me and R4-R6 is H; R1 is 2-pyrimidinyl group, fused to the Ar group is phenyl substituted by OCH3 in positions 6 and 7 and -OH in position 4 or 6 of the resultant quinazolinyl cycle, a is 2, b, c are 1, R2-R5 are H and R6 is OCH3. Independent claims are also included for the preparations of (I). [Image] ACTIVITY : Neuroleptic; Antiaddictive; Endocrine-Gen.; Vasotropic; CNS-Gen.; Muscular-Gen.; Antiparkinsonian; Antidepressant. MECHANISM OF ACTION : Dopamine D3 receptor ligand. (I) were tested for dopamine D3 receptor ligand activity in HEK 293 cells. The inhibitory constant value of 2-{4-[4-(2,3-dichlorophenyl)piperazin-1-y l]butyl}amino-4-phenylpyridine was 0.55 nM.</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>2007</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZPBxDIr0CfAMcA1yjAr19HNVcHEN8gxzDPEMcw1WcAxWCHb1cXUG8RR8PN0d_VwU3PyDFEI8gOr8Axx9wRqMFYJcnV0DQvyDeBhY0xJzilN5oTQ3g7Kba4izh25qQX58anFBYnJqXmpJvEdQgJGBgbmBkYVpSIixMXGqAJNHL24</recordid><startdate>20070831</startdate><enddate>20070831</enddate><creator>JEANNE-MARIE LECOMTE</creator><creator>THIERRY CALMELS</creator><creator>PHILIPPE ROBERT</creator><creator>MARC CAPET</creator><creator>ISABELLE BERREBI-BERTRAND</creator><creator>JEANARLES SCHWARTZ</creator><creator>MARCEL MORVAN</creator><creator>DENIS DANVY</creator><creator>NICOLAS LEVOIN</creator><scope>EVB</scope></search><sort><creationdate>20070831</creationdate><title>ARYLPIPERAZUINE DERIVATIVES AS SELECTIVE LIGAND FOR THE DOPAMINE D3 RECEPTOR</title><author>JEANNE-MARIE LECOMTE ; THIERRY CALMELS ; PHILIPPE ROBERT ; MARC CAPET ; ISABELLE BERREBI-BERTRAND ; JEANARLES SCHWARTZ ; MARCEL MORVAN ; DENIS DANVY ; NICOLAS LEVOIN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_HRP20070285TT33</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>hrv ; eng</language><creationdate>2007</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>JEANNE-MARIE LECOMTE</creatorcontrib><creatorcontrib>THIERRY CALMELS</creatorcontrib><creatorcontrib>PHILIPPE ROBERT</creatorcontrib><creatorcontrib>MARC CAPET</creatorcontrib><creatorcontrib>ISABELLE BERREBI-BERTRAND</creatorcontrib><creatorcontrib>JEANARLES SCHWARTZ</creatorcontrib><creatorcontrib>MARCEL MORVAN</creatorcontrib><creatorcontrib>DENIS DANVY</creatorcontrib><creatorcontrib>NICOLAS LEVOIN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>JEANNE-MARIE LECOMTE</au><au>THIERRY CALMELS</au><au>PHILIPPE ROBERT</au><au>MARC CAPET</au><au>ISABELLE BERREBI-BERTRAND</au><au>JEANARLES SCHWARTZ</au><au>MARCEL MORVAN</au><au>DENIS DANVY</au><au>NICOLAS LEVOIN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>ARYLPIPERAZUINE DERIVATIVES AS SELECTIVE LIGAND FOR THE DOPAMINE D3 RECEPTOR</title><date>2007-08-31</date><risdate>2007</risdate><abstract>Spoj formule (I): naznačen time da: R1 predstavlja heteroaril od pet ili šest lančanih veza, koji sadrži jedan ili više heteroatoma, izabran između 2-piridila, 2-pirimidinila, 2-piridazinila, 2-pirazinila, 2-imidazolila, 2-oksazolila, 2-tiazolila, 3-izoksazolila, 3-izotiazolila, 1,2,4-triazol-2-ila, 1,3,4-oksadiazol-2-ila, 1,3,4-tiadiazol-2-ila, po želji supstituiran jednom ili više grupa, identičnih ili različitih, izabranih između halogenog atoma ili hidroksi-grupe, alkila, monofluoroalkila, polifluoroalkila, alkoksi, polifluoro-alkoksi, alkilsulfanila, polifluoroalkilsulfanila; Ar je aril ili heteroaril, po želji supstituiran jednim ili više identičnih ili različitih supstituenata, izabranih između halogenog atoma ili hidroksi-grupe, aklila, monofluoroalkila, polifluoroalkila, alkoksi,polifluoroalkoksi, alkilsulfanila, polifluoroalkilsulfanila, cijano, karbamoila, dialkilkarbamoila,alkil-C(=O)-, alkil-O-C(=O)-, HO-C(=O)-, (HO)alkil-, ili je Ar spojen s karbocikličkim ili heterocikličkim prstenom, odnosno zasićenim, nezasićenim ili aromatskim prstenom; a = 2, 3 ili 4; b i c su identični ili različiti i predstavljaju 1 ili 2; R2, R3, R4, R5 i R6 predstavljaju, svaki neovisno, atom vodika ili halogena ili hidroksi-grupu, alkil,monofluoroalkil, polifluoroalkil, alkoksi, polifluoroalkoksi, alkilsulfanil, polifluoroalkilsulfanil, cijano, -NRR', -COOR, -COR, -CONRR' ili su dva susjedna R2, R3, R4, R5 i R6 međusobno povezana i tvore karbociklički ili heterociklički prsten, zasićen ili nezasićen, spojen na fenilnu jezgru na koju su pričvršćeni; ili R i R', identični ili različiti, predstavljaju neovisno atom vodika ili alkilnu grupu; kao i njihovi stereoizomeri ili njihove smjese, tautomerni oblici, hidrati, solvati, farmaceutski prihvatljive soli i esteri. Patent sadrži još 22 patentna zahtjeva.
Arylpiperazine compounds (I) and their stereoisomers, tautomeric forms, hydrates, solvates, salts or esters are new. Arylpiperazine compounds of formula (I) and their stereoisomers, tautomeric forms, hydrates, solvates, salts or esters are new. R1 : heteroaryl with 5-6 chain links (optionally containing heteroatoms of 2-pyridyl, 2-pyrimidinyl, 2-pyridazinyl, 2-pyrazinyl, 2-imidazolyl, 2-oxazolyl, 2-thiazolyl, 3-isoxazolyl, 3-isothiazolyl, 1,2,4-triazol- 2-yl, 1,3,4-oxadiazol-2-yl or 1,3,4-thiadiazol-2-yl) (all optionally substituted by halo or OH), alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl or polyfluoroalkylsulfanyl group); Ar : (hetero)aryl (optionally fused with R1 and optionally substituted by halo or OH), alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl, polyfluoroalkylsulfanyl, CN, carbamoyl, dialkylcarbamoyl, alkyl-C(=O)-, alkyl-O-C(=O)-, HO-C(=O)-, (HO)alkyl group or fused with optionally saturated or aromatic hydrocarbon cycle or heterocycle; a : 2-4; b, c : 1-2; either R2-R6 : H, halo, OH, alkyl, monofluoroalkyl, polyfluoroalkyl, alkoxy, polyfluoroalkoxy, alkylsulfanyl, polyfluoroalkylsulfanyl, CN, -NRR-a, COOR, COR or CONRR-a group; R2+R3+R4+R5+R6 : hydrocarbon cycle or optionally saturated heterocycle (both are fused to the phenyl nucleus to which they are attached); and R, R-a : H or alkyl. Provided that compounds for which R1 is 2-oxazolyl, 2-imidazolyl or 2-thiazolyl fused to the Ar group (optionally substituted phenyl), and compounds for which R1 is 2-pyridyl group, fused to the Ar group phenyl (optionally substituted by CH3 in position 4 of the resultant quinoline cycle, a is 2, b, c are 1, R2 is H, OCH3 and R3-R6 is H or R2, R3 are Me and R4-R6 is H; R1 is 2-pyrimidinyl group, fused to the Ar group is phenyl substituted by OCH3 in positions 6 and 7 and -OH in position 4 or 6 of the resultant quinazolinyl cycle, a is 2, b, c are 1, R2-R5 are H and R6 is OCH3. Independent claims are also included for the preparations of (I). [Image] ACTIVITY : Neuroleptic; Antiaddictive; Endocrine-Gen.; Vasotropic; CNS-Gen.; Muscular-Gen.; Antiparkinsonian; Antidepressant. MECHANISM OF ACTION : Dopamine D3 receptor ligand. (I) were tested for dopamine D3 receptor ligand activity in HEK 293 cells. The inhibitory constant value of 2-{4-[4-(2,3-dichlorophenyl)piperazin-1-y l]butyl}amino-4-phenylpyridine was 0.55 nM.</abstract><oa>free_for_read</oa></addata></record> |
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| language | hrv ; eng |
| recordid | cdi_epo_espacenet_HRP20070285TT3 |
| source | esp@cenet |
| 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 | ARYLPIPERAZUINE DERIVATIVES AS SELECTIVE LIGAND FOR THE DOPAMINE D3 RECEPTOR |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-08T16%3A44%3A06IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-epo_EVB&rft_val_fmt=info:ofi/fmt:kev:mtx:patent&rft.genre=patent&rft.au=JEANNE-MARIE%20LECOMTE&rft.date=2007-08-31&rft_id=info:doi/&rft_dat=%3Cepo_EVB%3EHRP20070285TT3%3C/epo_EVB%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true |