发明申请
- 专利标题: Method for Obtaining Novel Derivatives of Naphthalene for the In Vivo Diagnosis of Alzheimer's Disease
- 专利标题(中): 获得萘衍生物用于体内诊断阿尔茨海默病的方法
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申请号: US13574050申请日: 2010-04-17
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公开(公告)号: US20120321560A1公开(公告)日: 2012-12-20
- 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
- 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
- 优先权: CUPCT/CU2009/000057 20090417
- 国际申请: PCT/CU2010/000001 WO 20100417
- 主分类号: A61K51/04
- IPC分类号: A61K51/04 ; C07C43/20 ; C07D207/46 ; C07C237/20 ; C07D207/40 ; C07C229/34
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.