METHOD FOR OBTAINING NOVEL DERIVATIVES OF NAPHTHALENE FOR THE IN VIVO DIAGNOSIS OF ALZHEIMER'S DISEASE
The invention relates to chemistry and in particular to the field involved in the organic synthesis of compounds belonging to the category of naphthalene or bicyclic aromatics, used in the detection of amyloid plaques. These novel naphthalene derivatives have general formula: (I), (II), wherein: R r...
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| creator | LOPEZ BARROSO, ROSA MARIA PEREZ MARTINEZ, CARLOS SERAFIN VALDES SOSA, PEDRO SABLON CARRAZANA, MARQUIZA PEREZ PERERA, RAFAELA VELEZ CASTRO, HERMAN PERERA PINTADO, ALEJANDRO RIVERA MARRERO, SUCHITIL RODRIGUEZ-TANTY, CHRYSLAINE PRATS CAPOTE, ANAIS |
| description | The invention relates to chemistry and in particular to the field involved in the organic synthesis of compounds belonging to the category of naphthalene or bicyclic aromatics, used in the detection of amyloid plaques. These novel naphthalene derivatives have general formula: (I), (II), wherein: R represents groups that are independent of one another. In formula (I), R1 represents -alkylenyl-C(O)NH- alkylenyl-R3, -alkylenyl-C(O)O-R4; R3 represents -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-/V- dithiocarbamate of salts of alkaline earth metals; R4 represents H, succinimide group; and R2 represents -H, - alkyl. In formula (II), R1 represents -alkyl, -alkylenyl-halide, -alkylenyl-hidroxyl, -alkylenyl-O- arylsulfonate, alkylenyl-O-alkylsulfonate; R2 represents-halide, -alkylenyl-O-arylsulfonate, - alkylenyl-O-alkylsulfonate, -alkylenyl-halide, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-?/-dithiocarbamate of alkaline salts. The terms "alkyl" and "alkylenyl" refer to linear or branched aliphatic chains, preferably with between 1 and 4 carbon atoms, and the term halide refers to fluorine, bromine or iodine. These compounds are neutral, lipophilic and of low molecular weight, allowing same to pass through the blood-brain barrier and adhere to amyloid plaques. The invention relates to methods for obtaining naphthalene derivatives in good yields, which are practical, economical and can be adapted to larger-scale manufacture. We are not aware of any reference in the prior art to the compounds presented in this application.
Esta invención se relaciona con la rama de la Química, en particular con el campo de la síntesis orgánica de compuestos que pertenecen a la categoría de aromáticos bicíclicos o naftalénicos, utilizados en la detección de placas amiloideas. Estos nuevos derivados de naftaleno tienen fórmula general: (I), (II). Donde R representa a grupos independientes entre sí. En I: R1: -alquilenil-C(O)NH- alquilenil-R3, -alquilenil-C(O)O-R4; R3: -COOH, -OH, -SH, -NH2, -alquil-NH, -alquil-/V- ditiocarbamato de sales de metales alcalino térreo; R4: H, grupo succinimido; R2: -H, - alquil. En II: R1: -alquilo, -alquilenil-haluro, -alquilenil-hidroxilo, -alquilenil-O- arilsulfonato, alquilenil-O-alquilsulfonato; R2:-haluro, -alquilenil-O-arilsulfonato, - alquilenil-O-alquilsulfonato, -alquilenil-haluro, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alquilenil-NH2, -alquilenil-NH-alquil, -alqu¡lenil-alquil-?/-ditiocarbamato de sales alcalina |
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| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_WO2010118706A3</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>WO2010118706A3</sourcerecordid><originalsourceid>FETCH-epo_espacenet_WO2010118706A33</originalsourceid><addsrcrecordid>eNqNyjEKwkAQQNE0FqLeYcDCSsgaUNvRTLIDyYxklxVsQpBNJRqI90cJHsDqF__Nk74mbzWHQhvQk0cWlhJEA1WQU8MBPQdyoAUIXqy3WJHQxL0lYIHAQSFnLEUdTxCrmyWuqdm473CEjpbJrO8eY1z9ukjWBfmz3cbh1cZx6O7xGd_tVXepSY05HtI9Ztl_6gNq8DWx</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>METHOD FOR OBTAINING NOVEL DERIVATIVES OF NAPHTHALENE FOR THE IN VIVO DIAGNOSIS OF ALZHEIMER'S DISEASE</title><source>esp@cenet</source><creator>LOPEZ BARROSO, ROSA MARIA ; PEREZ MARTINEZ, CARLOS SERAFIN ; VALDES SOSA, PEDRO ; SABLON CARRAZANA, MARQUIZA ; PEREZ PERERA, RAFAELA ; VELEZ CASTRO, HERMAN ; PERERA PINTADO, ALEJANDRO ; RIVERA MARRERO, SUCHITIL ; RODRIGUEZ-TANTY, CHRYSLAINE ; PRATS CAPOTE, ANAIS</creator><creatorcontrib>LOPEZ BARROSO, ROSA MARIA ; PEREZ MARTINEZ, CARLOS SERAFIN ; VALDES SOSA, PEDRO ; SABLON CARRAZANA, MARQUIZA ; PEREZ PERERA, RAFAELA ; VELEZ CASTRO, HERMAN ; PERERA PINTADO, ALEJANDRO ; RIVERA MARRERO, SUCHITIL ; RODRIGUEZ-TANTY, CHRYSLAINE ; PRATS CAPOTE, ANAIS</creatorcontrib><description>The invention relates to chemistry and in particular to the field involved in the organic synthesis of compounds belonging to the category of naphthalene or bicyclic aromatics, used in the detection of amyloid plaques. These novel naphthalene derivatives have general formula: (I), (II), wherein: R represents groups that are independent of one another. In formula (I), R1 represents -alkylenyl-C(O)NH- alkylenyl-R3, -alkylenyl-C(O)O-R4; R3 represents -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-/V- dithiocarbamate of salts of alkaline earth metals; R4 represents H, succinimide group; and R2 represents -H, - alkyl. In formula (II), R1 represents -alkyl, -alkylenyl-halide, -alkylenyl-hidroxyl, -alkylenyl-O- arylsulfonate, alkylenyl-O-alkylsulfonate; R2 represents-halide, -alkylenyl-O-arylsulfonate, - alkylenyl-O-alkylsulfonate, -alkylenyl-halide, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-?/-dithiocarbamate of alkaline salts. The terms "alkyl" and "alkylenyl" refer to linear or branched aliphatic chains, preferably with between 1 and 4 carbon atoms, and the term halide refers to fluorine, bromine or iodine. These compounds are neutral, lipophilic and of low molecular weight, allowing same to pass through the blood-brain barrier and adhere to amyloid plaques. The invention relates to methods for obtaining naphthalene derivatives in good yields, which are practical, economical and can be adapted to larger-scale manufacture. We are not aware of any reference in the prior art to the compounds presented in this application.
Esta invención se relaciona con la rama de la Química, en particular con el campo de la síntesis orgánica de compuestos que pertenecen a la categoría de aromáticos bicíclicos o naftalénicos, utilizados en la detección de placas amiloideas. Estos nuevos derivados de naftaleno tienen fórmula general: (I), (II). Donde R representa a grupos independientes entre sí. En I: R1: -alquilenil-C(O)NH- alquilenil-R3, -alquilenil-C(O)O-R4; R3: -COOH, -OH, -SH, -NH2, -alquil-NH, -alquil-/V- ditiocarbamato de sales de metales alcalino térreo; R4: H, grupo succinimido; R2: -H, - alquil. En II: R1: -alquilo, -alquilenil-haluro, -alquilenil-hidroxilo, -alquilenil-O- arilsulfonato, alquilenil-O-alquilsulfonato; R2:-haluro, -alquilenil-O-arilsulfonato, - alquilenil-O-alquilsulfonato, -alquilenil-haluro, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alquilenil-NH2, -alquilenil-NH-alquil, -alqu¡lenil-alquil-?/-ditiocarbamato de sales alcalinas. Los términos "alquil" y "alquilenil" se refieren a cadenas alifáticas lineales o ramificadas, preferentemente de 1 a 4 átomos de carbono y el término haluro a Flúor, Bromo o Yodo. Estos compuestos son neutros, lipofílicos y de bajo peso molecular por lo que atraviesan la barrera hematoencefálica y se adhieren a las placas amiloideas. La presente invención proporciona los procedimientos para la obtención de derivados de naftaleno con buenos rendimientos, que pueden ser prácticos, económicos y ser adaptados a una manufactura a mayor escala. No tenemos conocimiento de que los compuestos presentados en esta invención hayan sido reportados anteriormente.
L'invention concerne la branche de la chimie, et notamment le domaine de la synthèse organique de composés appartenant à la catégorie des composés aromatiques bicycliques ou naphtaléniques, utilisés dans la détection de plaques amyloïdes. Ces nouveaux dérivés de naphtalène sont représentés par les formules générales (I) et (II), dans lesquelles R représente des groupes mutuellement indépendants. Dans la formule (I): R1 est -alkylényl-C(O)NH-alkylényl-R3, -alkylényl-C(O))-R4; R3 est -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-N-dithiocarbamate de sels de métaux alcalino-terreux; R4 est H, un groupe succinimide; R2 est -H, -alkyle. Dans la formule (II): R1 est -alkyle, -alkylényl-haluro, -alkylényl-hydroxylo, -alkylényl-O-arylsulfonate, alkylényl-O-alkylsulfonate; R2 est -haluro, -alkylényl-O-arylsulfonate, -alkylényl-O-alkylsulfonate, -alkylényl-haluro, -CH(O), -HC=C(CN)2, -HC=CHNO2, -alkylényl-NH2, alkylényl-NH-alkyle, -alkylényl-alkyl-N-dithiocarbamate de sels alcalins. Les termes "alkyle" et alkylényle" font référence à des chaînes aliphatiques linéaires ou ramifiées, de préférence de 1 à 4 atomes de carbone, et le terme "haluro" à fluor, brome ou iode. Ces composés sont neutres, lipophiles et de faible poids moléculaire, et peuvent ainsi traverser la barrière hémato-encéphalique et se fixer sur les plaques amyloïdes. La présente invention concerne des procédés permettant d'obtenir des dérivés de naphtalène avec un rendement élevé, ces procédés pouvant être pratiques, économiques et adaptés à une fabrication à plus grande échelle. A notre connaissance, les composés présentés dans cette invention n'ont pas été décrits antérieurement.</description><language>eng ; fre ; spa</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; CHEMISTRY ; HUMAN NECESSITIES ; HYGIENE ; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES ; MEASURING ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PHYSICS ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; TESTING</subject><creationdate>2010</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=20101202&DB=EPODOC&CC=WO&NR=2010118706A3$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76289</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20101202&DB=EPODOC&CC=WO&NR=2010118706A3$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>LOPEZ BARROSO, ROSA MARIA</creatorcontrib><creatorcontrib>PEREZ MARTINEZ, CARLOS SERAFIN</creatorcontrib><creatorcontrib>VALDES SOSA, PEDRO</creatorcontrib><creatorcontrib>SABLON CARRAZANA, MARQUIZA</creatorcontrib><creatorcontrib>PEREZ PERERA, RAFAELA</creatorcontrib><creatorcontrib>VELEZ CASTRO, HERMAN</creatorcontrib><creatorcontrib>PERERA PINTADO, ALEJANDRO</creatorcontrib><creatorcontrib>RIVERA MARRERO, SUCHITIL</creatorcontrib><creatorcontrib>RODRIGUEZ-TANTY, CHRYSLAINE</creatorcontrib><creatorcontrib>PRATS CAPOTE, ANAIS</creatorcontrib><title>METHOD FOR OBTAINING NOVEL DERIVATIVES OF NAPHTHALENE FOR THE IN VIVO DIAGNOSIS OF ALZHEIMER'S DISEASE</title><description>The invention relates to chemistry and in particular to the field involved in the organic synthesis of compounds belonging to the category of naphthalene or bicyclic aromatics, used in the detection of amyloid plaques. These novel naphthalene derivatives have general formula: (I), (II), wherein: R represents groups that are independent of one another. In formula (I), R1 represents -alkylenyl-C(O)NH- alkylenyl-R3, -alkylenyl-C(O)O-R4; R3 represents -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-/V- dithiocarbamate of salts of alkaline earth metals; R4 represents H, succinimide group; and R2 represents -H, - alkyl. In formula (II), R1 represents -alkyl, -alkylenyl-halide, -alkylenyl-hidroxyl, -alkylenyl-O- arylsulfonate, alkylenyl-O-alkylsulfonate; R2 represents-halide, -alkylenyl-O-arylsulfonate, - alkylenyl-O-alkylsulfonate, -alkylenyl-halide, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-?/-dithiocarbamate of alkaline salts. The terms "alkyl" and "alkylenyl" refer to linear or branched aliphatic chains, preferably with between 1 and 4 carbon atoms, and the term halide refers to fluorine, bromine or iodine. These compounds are neutral, lipophilic and of low molecular weight, allowing same to pass through the blood-brain barrier and adhere to amyloid plaques. The invention relates to methods for obtaining naphthalene derivatives in good yields, which are practical, economical and can be adapted to larger-scale manufacture. We are not aware of any reference in the prior art to the compounds presented in this application.
Esta invención se relaciona con la rama de la Química, en particular con el campo de la síntesis orgánica de compuestos que pertenecen a la categoría de aromáticos bicíclicos o naftalénicos, utilizados en la detección de placas amiloideas. Estos nuevos derivados de naftaleno tienen fórmula general: (I), (II). Donde R representa a grupos independientes entre sí. En I: R1: -alquilenil-C(O)NH- alquilenil-R3, -alquilenil-C(O)O-R4; R3: -COOH, -OH, -SH, -NH2, -alquil-NH, -alquil-/V- ditiocarbamato de sales de metales alcalino térreo; R4: H, grupo succinimido; R2: -H, - alquil. En II: R1: -alquilo, -alquilenil-haluro, -alquilenil-hidroxilo, -alquilenil-O- arilsulfonato, alquilenil-O-alquilsulfonato; R2:-haluro, -alquilenil-O-arilsulfonato, - alquilenil-O-alquilsulfonato, -alquilenil-haluro, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alquilenil-NH2, -alquilenil-NH-alquil, -alqu¡lenil-alquil-?/-ditiocarbamato de sales alcalinas. Los términos "alquil" y "alquilenil" se refieren a cadenas alifáticas lineales o ramificadas, preferentemente de 1 a 4 átomos de carbono y el término haluro a Flúor, Bromo o Yodo. Estos compuestos son neutros, lipofílicos y de bajo peso molecular por lo que atraviesan la barrera hematoencefálica y se adhieren a las placas amiloideas. La presente invención proporciona los procedimientos para la obtención de derivados de naftaleno con buenos rendimientos, que pueden ser prácticos, económicos y ser adaptados a una manufactura a mayor escala. No tenemos conocimiento de que los compuestos presentados en esta invención hayan sido reportados anteriormente.
L'invention concerne la branche de la chimie, et notamment le domaine de la synthèse organique de composés appartenant à la catégorie des composés aromatiques bicycliques ou naphtaléniques, utilisés dans la détection de plaques amyloïdes. Ces nouveaux dérivés de naphtalène sont représentés par les formules générales (I) et (II), dans lesquelles R représente des groupes mutuellement indépendants. Dans la formule (I): R1 est -alkylényl-C(O)NH-alkylényl-R3, -alkylényl-C(O))-R4; R3 est -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-N-dithiocarbamate de sels de métaux alcalino-terreux; R4 est H, un groupe succinimide; R2 est -H, -alkyle. Dans la formule (II): R1 est -alkyle, -alkylényl-haluro, -alkylényl-hydroxylo, -alkylényl-O-arylsulfonate, alkylényl-O-alkylsulfonate; R2 est -haluro, -alkylényl-O-arylsulfonate, -alkylényl-O-alkylsulfonate, -alkylényl-haluro, -CH(O), -HC=C(CN)2, -HC=CHNO2, -alkylényl-NH2, alkylényl-NH-alkyle, -alkylényl-alkyl-N-dithiocarbamate de sels alcalins. Les termes "alkyle" et alkylényle" font référence à des chaînes aliphatiques linéaires ou ramifiées, de préférence de 1 à 4 atomes de carbone, et le terme "haluro" à fluor, brome ou iode. Ces composés sont neutres, lipophiles et de faible poids moléculaire, et peuvent ainsi traverser la barrière hémato-encéphalique et se fixer sur les plaques amyloïdes. La présente invention concerne des procédés permettant d'obtenir des dérivés de naphtalène avec un rendement élevé, ces procédés pouvant être pratiques, économiques et adaptés à une fabrication à plus grande échelle. A notre connaissance, les composés présentés dans cette invention n'ont pas été décrits antérieurement.</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</subject><subject>CHEMISTRY</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES</subject><subject>MEASURING</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PHYSICS</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>TESTING</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2010</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNyjEKwkAQQNE0FqLeYcDCSsgaUNvRTLIDyYxklxVsQpBNJRqI90cJHsDqF__Nk74mbzWHQhvQk0cWlhJEA1WQU8MBPQdyoAUIXqy3WJHQxL0lYIHAQSFnLEUdTxCrmyWuqdm473CEjpbJrO8eY1z9ukjWBfmz3cbh1cZx6O7xGd_tVXepSY05HtI9Ztl_6gNq8DWx</recordid><startdate>20101202</startdate><enddate>20101202</enddate><creator>LOPEZ BARROSO, ROSA MARIA</creator><creator>PEREZ MARTINEZ, CARLOS SERAFIN</creator><creator>VALDES SOSA, PEDRO</creator><creator>SABLON CARRAZANA, MARQUIZA</creator><creator>PEREZ PERERA, RAFAELA</creator><creator>VELEZ CASTRO, HERMAN</creator><creator>PERERA PINTADO, ALEJANDRO</creator><creator>RIVERA MARRERO, SUCHITIL</creator><creator>RODRIGUEZ-TANTY, CHRYSLAINE</creator><creator>PRATS CAPOTE, ANAIS</creator><scope>EVB</scope></search><sort><creationdate>20101202</creationdate><title>METHOD FOR OBTAINING NOVEL DERIVATIVES OF NAPHTHALENE FOR THE IN VIVO DIAGNOSIS OF ALZHEIMER'S DISEASE</title><author>LOPEZ BARROSO, ROSA MARIA ; PEREZ MARTINEZ, CARLOS SERAFIN ; VALDES SOSA, PEDRO ; SABLON CARRAZANA, MARQUIZA ; PEREZ PERERA, RAFAELA ; VELEZ CASTRO, HERMAN ; PERERA PINTADO, ALEJANDRO ; RIVERA MARRERO, SUCHITIL ; RODRIGUEZ-TANTY, CHRYSLAINE ; PRATS CAPOTE, ANAIS</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_WO2010118706A33</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fre ; spa</language><creationdate>2010</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</topic><topic>CHEMISTRY</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES</topic><topic>MEASURING</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PHYSICS</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>TESTING</topic><toplevel>online_resources</toplevel><creatorcontrib>LOPEZ BARROSO, ROSA MARIA</creatorcontrib><creatorcontrib>PEREZ MARTINEZ, CARLOS SERAFIN</creatorcontrib><creatorcontrib>VALDES SOSA, PEDRO</creatorcontrib><creatorcontrib>SABLON CARRAZANA, MARQUIZA</creatorcontrib><creatorcontrib>PEREZ PERERA, RAFAELA</creatorcontrib><creatorcontrib>VELEZ CASTRO, HERMAN</creatorcontrib><creatorcontrib>PERERA PINTADO, ALEJANDRO</creatorcontrib><creatorcontrib>RIVERA MARRERO, SUCHITIL</creatorcontrib><creatorcontrib>RODRIGUEZ-TANTY, CHRYSLAINE</creatorcontrib><creatorcontrib>PRATS CAPOTE, ANAIS</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>LOPEZ BARROSO, ROSA MARIA</au><au>PEREZ MARTINEZ, CARLOS SERAFIN</au><au>VALDES SOSA, PEDRO</au><au>SABLON CARRAZANA, MARQUIZA</au><au>PEREZ PERERA, RAFAELA</au><au>VELEZ CASTRO, HERMAN</au><au>PERERA PINTADO, ALEJANDRO</au><au>RIVERA MARRERO, SUCHITIL</au><au>RODRIGUEZ-TANTY, CHRYSLAINE</au><au>PRATS CAPOTE, ANAIS</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>METHOD FOR OBTAINING NOVEL DERIVATIVES OF NAPHTHALENE FOR THE IN VIVO DIAGNOSIS OF ALZHEIMER'S DISEASE</title><date>2010-12-02</date><risdate>2010</risdate><abstract>The invention relates to chemistry and in particular to the field involved in the organic synthesis of compounds belonging to the category of naphthalene or bicyclic aromatics, used in the detection of amyloid plaques. These novel naphthalene derivatives have general formula: (I), (II), wherein: R represents groups that are independent of one another. In formula (I), R1 represents -alkylenyl-C(O)NH- alkylenyl-R3, -alkylenyl-C(O)O-R4; R3 represents -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-/V- dithiocarbamate of salts of alkaline earth metals; R4 represents H, succinimide group; and R2 represents -H, - alkyl. In formula (II), R1 represents -alkyl, -alkylenyl-halide, -alkylenyl-hidroxyl, -alkylenyl-O- arylsulfonate, alkylenyl-O-alkylsulfonate; R2 represents-halide, -alkylenyl-O-arylsulfonate, - alkylenyl-O-alkylsulfonate, -alkylenyl-halide, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-?/-dithiocarbamate of alkaline salts. The terms "alkyl" and "alkylenyl" refer to linear or branched aliphatic chains, preferably with between 1 and 4 carbon atoms, and the term halide refers to fluorine, bromine or iodine. These compounds are neutral, lipophilic and of low molecular weight, allowing same to pass through the blood-brain barrier and adhere to amyloid plaques. The invention relates to methods for obtaining naphthalene derivatives in good yields, which are practical, economical and can be adapted to larger-scale manufacture. We are not aware of any reference in the prior art to the compounds presented in this application.
Esta invención se relaciona con la rama de la Química, en particular con el campo de la síntesis orgánica de compuestos que pertenecen a la categoría de aromáticos bicíclicos o naftalénicos, utilizados en la detección de placas amiloideas. Estos nuevos derivados de naftaleno tienen fórmula general: (I), (II). Donde R representa a grupos independientes entre sí. En I: R1: -alquilenil-C(O)NH- alquilenil-R3, -alquilenil-C(O)O-R4; R3: -COOH, -OH, -SH, -NH2, -alquil-NH, -alquil-/V- ditiocarbamato de sales de metales alcalino térreo; R4: H, grupo succinimido; R2: -H, - alquil. En II: R1: -alquilo, -alquilenil-haluro, -alquilenil-hidroxilo, -alquilenil-O- arilsulfonato, alquilenil-O-alquilsulfonato; R2:-haluro, -alquilenil-O-arilsulfonato, - alquilenil-O-alquilsulfonato, -alquilenil-haluro, -CH(O), -HC=C(CN)2, -HC=CHNO2, - alquilenil-NH2, -alquilenil-NH-alquil, -alqu¡lenil-alquil-?/-ditiocarbamato de sales alcalinas. Los términos "alquil" y "alquilenil" se refieren a cadenas alifáticas lineales o ramificadas, preferentemente de 1 a 4 átomos de carbono y el término haluro a Flúor, Bromo o Yodo. Estos compuestos son neutros, lipofílicos y de bajo peso molecular por lo que atraviesan la barrera hematoencefálica y se adhieren a las placas amiloideas. La presente invención proporciona los procedimientos para la obtención de derivados de naftaleno con buenos rendimientos, que pueden ser prácticos, económicos y ser adaptados a una manufactura a mayor escala. No tenemos conocimiento de que los compuestos presentados en esta invención hayan sido reportados anteriormente.
L'invention concerne la branche de la chimie, et notamment le domaine de la synthèse organique de composés appartenant à la catégorie des composés aromatiques bicycliques ou naphtaléniques, utilisés dans la détection de plaques amyloïdes. Ces nouveaux dérivés de naphtalène sont représentés par les formules générales (I) et (II), dans lesquelles R représente des groupes mutuellement indépendants. Dans la formule (I): R1 est -alkylényl-C(O)NH-alkylényl-R3, -alkylényl-C(O))-R4; R3 est -COOH, -OH, -SH, -NH2, -alkyl-NH, -alkyl-N-dithiocarbamate de sels de métaux alcalino-terreux; R4 est H, un groupe succinimide; R2 est -H, -alkyle. Dans la formule (II): R1 est -alkyle, -alkylényl-haluro, -alkylényl-hydroxylo, -alkylényl-O-arylsulfonate, alkylényl-O-alkylsulfonate; R2 est -haluro, -alkylényl-O-arylsulfonate, -alkylényl-O-alkylsulfonate, -alkylényl-haluro, -CH(O), -HC=C(CN)2, -HC=CHNO2, -alkylényl-NH2, alkylényl-NH-alkyle, -alkylényl-alkyl-N-dithiocarbamate de sels alcalins. Les termes "alkyle" et alkylényle" font référence à des chaînes aliphatiques linéaires ou ramifiées, de préférence de 1 à 4 atomes de carbone, et le terme "haluro" à fluor, brome ou iode. Ces composés sont neutres, lipophiles et de faible poids moléculaire, et peuvent ainsi traverser la barrière hémato-encéphalique et se fixer sur les plaques amyloïdes. La présente invention concerne des procédés permettant d'obtenir des dérivés de naphtalène avec un rendement élevé, ces procédés pouvant être pratiques, économiques et adaptés à une fabrication à plus grande échelle. A notre connaissance, les composés présentés dans cette invention n'ont pas été décrits antérieurement.</abstract><oa>free_for_read</oa></addata></record> |
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| language | eng ; fre ; spa |
| recordid | cdi_epo_espacenet_WO2010118706A3 |
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| subjects | ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY HUMAN NECESSITIES HYGIENE INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES MEASURING MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PHYSICS PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES TESTING |
| title | METHOD FOR OBTAINING NOVEL DERIVATIVES OF NAPHTHALENE FOR THE IN VIVO DIAGNOSIS OF ALZHEIMER'S DISEASE |
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