公开(公告)号：US09764047B2

公开(公告)日：2017-09-19

申请号：US13574050

申请日：2010-04-17

申请人： Marquiza Sablón Carrazana ,  Chryslaine Rodriguez-Tanty ,  Alejandro Perera Pintado ,  Suchitil Rivera Marrero ,  Rafaela Perez Perera ,  Rosa Maria López Barroso ,  Anais Prats Capote ,  Hermán Vélez Castro ,  Carlos Serafin Pérez Martínez ,  Pedro Valdés Sosa

发明人： Marquiza Sablón Carrazana ,  Chryslaine Rodriguez-Tanty ,  Alejandro Perera Pintado ,  Suchitil Rivera Marrero ,  Rafaela Perez Perera ,  Rosa Maria López Barroso ,  Anais Prats Capote ,  Hermán Vélez Castro ,  Carlos Serafin Pérez Martínez ,  Pedro Valdés Sosa

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  C07C43/225 ,  C07C233/07 ,  C07C233/36 ,  C07C233/47 ,  C07C323/25 ,  C07D207/06 ,  C07D207/46

CPC分类号： A61K51/0446 ,  A61K51/0402 ,  A61K51/0482 ,  C07B2200/05 ,  C07C43/225 ,  C07C233/07 ,  C07C233/36 ,  C07C233/47 ,  C07C323/25 ,  C07D207/06 ,  C07D207/46

摘要： This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R1:-alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4, R3:—COOH, —OH, —SH, —NH2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R4: H, succinimidyl group, R2: —H,-alkyl. In II: R1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN)2, —HC═CHNO2, -alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.

公开(公告)号：US20120321560A1

公开(公告)日：2012-12-20

申请号：US13574050

申请日：2010-04-17

申请人： Marquiza Sablón Carrazana ,  Chryslaine Rodriguez-Tanty ,  Alejandro Perera Pintado ,  Suchitil Rivera Marrero ,  Rafaela Perez Perera ,  Rosa Maria López Barroso ,  Anais Prats Capote ,  Hermán Vélez Castro ,  Carlos Serafin Pérez Martínez ,  Pedro Valdés Sosa

发明人： Marquiza Sablón Carrazana ,  Chryslaine Rodriguez-Tanty ,  Alejandro Perera Pintado ,  Suchitil Rivera Marrero ,  Rafaela Perez Perera ,  Rosa Maria López Barroso ,  Anais Prats Capote ,  Hermán Vélez Castro ,  Carlos Serafin Pérez Martínez ,  Pedro Valdés Sosa

IPC分类号： A61K51/04 ,  C07C43/20 ,  C07D207/46 ,  C07C237/20 ,  C07D207/40 ,  C07C229/34

CPC分类号： A61K51/0446 ,  A61K51/0402 ,  A61K51/0482 ,  C07B2200/05 ,  C07C43/225 ,  C07C233/07 ,  C07C233/36 ,  C07C233/47 ,  C07C323/25 ,  C07D207/06 ,  C07D207/46

摘要： This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R1:-alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4, R3:—COOH, —OH, —SH, —NH2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R4: H, succinimidyl group, R2: —H,-alkyl. In II: R1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN)2, —HC═CHNO2, -alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.

摘要翻译： 本发明涉及用于检测淀粉样蛋白片的化学分支，特别是涉及属于芳族双环或萘类的化合物有机合成领域。 这些新的萘衍生物具有通式：其中R表示相互独立的基团。 在I中：R 1： - 亚烷基-C（O）NH-亚烷基-R 3， - 亚烷基-C（O）O-R 4，R 3：-COOH，-OH，-SH，-NH 2， - 烷基-N-烷基 - N-二硫代氨基甲酸碱土金属盐，R4：H，琥珀酰亚胺基，R2：-H， - 烷基。 在II中：R 1：烷基， - 亚烷基 - 卤化物 - 亚烷基 - 羟基 - 亚烷基基 - O-芳基， - O-烷基磺酸酯亚烷基基团，R 2：卤化 - 亚烷基基 - O-芳基， - 亚烷基基-O-烷基磺酸酯， 卤化物，-CH（O），-HC = C（CN）2，-HC = CHNO2， - 亚烷基-NH2， - 亚烷基-NH-烷基， - 亚烷基 - 烷基-N-二硫代氨基甲酸盐碱性盐。 术语烷基和亚烷基指的是直链或支链脂族链，优选1至4个碳原子，术语卤化物为氟，溴或碘。 这些化合物是中性的，亲脂性的并且具有低分子量，因此它们穿过血脑屏障并附着于淀粉样蛋白片。 本发明提供了以高产率获得萘衍生物的方法，其可以实用，经济并适应于大规模制造。 我们不知道以前是否报告了本发明中呈现的化合物。