Publication number: 20240299334
Abstract: This invention relates to pharmaceutical chemistry and specifically to the pharmaceutical composition of the compounds, which show multi-targeted action on the cholinergic, glutamatergic and mitochondrial systems that are affected in Alzheimer's Disease (AD), whose general Formula (I) is I, wherein the substituents R1 and R2 are set out in the description and claims. The formulation of these compounds increases effectiveness and tolerance in oral, sublingual, parenteral, transdermal and nasal administration. They can be used on their own, as monotherapy, as a replacement of the multi-therapy currently used for AD. The formulation of these compounds, their salts, hydrates, enantiomers, isomers, metabolites, prodrugs for administration to humans, as active ingredients for the treatment of AD, increases bioavailability, residence time of the active ingredient and adequate excretion, which increases the effectiveness, biosafety, adherence and tolerance to the treatment.
Type:
Application
Filed:
November 18, 2021
Publication date:
September 12, 2024
Applicant:
CENTRO DE NEUROCIENCIAS DE CUBA, CNEURO
Inventors:
Chryslaine RODRÍGUEZ-TANTY, Marquiza SABLÓN CARRAZANA, Roberto MENÉNDEZ SOTO DEL VALLE, Alberto BENCOMO MARTÍNEZ, Suchitil RIVERA MARRERO, Laura GARCÍA PUPO, Leonora GONZÁLEZ MESA, Samila LEÓN CHAVIANO, Adriana ÁGUILA CORDOVA, Kathleen CASTRO-PALOMINO ANTELA, Giselle PENTÓN ROL, Laura OTAÑO TAMAYO, Rafaela PÉREZ PERERA, Majel CERVANTES LLANOS, Orestes de Jesús DÍAZ GARCÍA, Miriam DORESTE BROWN
Patent number: 10155053
Abstract: This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belong 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.
Type:
Grant
Filed:
March 3, 2015
Date of Patent:
December 18, 2018
Assignee:
CENTRO DE NEUROCIENCIAS DE CUBA
Inventors:
Marquiza Sablon Carrazana, Chryslaine Rodriguez-Tanty, Alejandro Perera Pintado, Suchitil Rivera Marrero, Rafaela Perez Perera, Rosa Maria Lopez Barroso, Anais Prats Capote, Herman Velez Castro, Carlos Serafin Perez Martinez, Pedro Valdes Sosa
Patent number: 9763900
Abstract: This invention relates to chemistry and biochemistry applied to the field of medicine and is referred to a new method of prevention and therapeutic treatment of conformational diseases (CD), in particular to amyloid origin diseases by administrating an effective amount of one or more compounds, salts, prodrugs or solvates, which are considered herein as chemical chaperonins, of Formula I, Where: R1: -alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4; R3: —COOH, —OH, —SH, —NH2, —NH-alkyl-, —NH-dithiocarbamate-alkyl, —N-alkyl-dithiocarbamate alkaline earth metal salts. R4: succinimidyl group. R2: —H, -alkyl; wherein the term “alkyl” is characterized by a linear or branched aliphatic chain, hydrogen and saturated carbon atoms, comprising a methyl, ethyl, n-propyl, iso-propyl, n-butyl or iso-butyl groups. Wherein, the term “alkylenyl” refers to a divalent analog of a linear or branched alkyl group, preferably ethylenyl (—CH2CH2—) or butylenyl (—CH2CH2CH2CH2—) radicals.
Type:
Grant
Filed:
December 30, 2013
Date of Patent:
September 19, 2017
Assignee:
CENTRO DE NEUROCIENCIAS DE CUBA
Inventors:
Marquiza Sablón Carrazana, Chryslaine Rodriguez-Tanty, Myriam Marlene Altamirano Bustamante, Fernand Vedrenne Gutiérrez, Suchitil Rivera Marrero, Isaac Fernández Gómez, Rosa María López Barroso, Lina Andrea Rivillas Acevedo, Reyna Lara Martinez, Rafaela Perez Perera, Alberto Bencomo Martínez, María Guadalupe Domínguez Macouzet, Luis Felipe Jiménez García, Massiel Díaz Miranda, Julio Morán Andrade, Pedro Valdés Sosa, Alejandro Perera Pintado, Anaís Prats Capote, Sergio Agustín Islas Andrade
Patent number: 9764047
Abstract: 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.
Type:
Grant
Filed:
April 17, 2010
Date of Patent:
September 19, 2017
Assignee:
CENTRO DE NEUROCIENCIAS DE CUBA
Inventors:
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
Publication number: 20160106691
Abstract: This invention relates to chemistry and biochemistry applied to the field of medicine and is referred to a new method of prevention and therapeutic treatment of conformational diseases (CD), in particular to amyloid origin diseases by administrating an effective amount of one or more compounds, salts, prodrugs or solvates, which are considered herein as chemical chaperonins, of Formula I, Where: R1: -alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4; R3: —COOH, —OH, —SH, —NH2, —NH-alkyl-, —NH-dithiocarbamate-alkyl, —N-alkyl-dithiocarbamate alkaline earth metal salts. R4: succinimidyl group. R2: —H, -alkyl; wherein the term “alkyl” is characterized by a linear or branched aliphatic chain, hydrogen and saturated carbon atoms, comprising a methyl, ethyl, n-propyl, iso-propyl, n-butyl or iso-butyl groups. Wherein, the term “alkylenyl” refers to a divalent analog of a linear or branched alkyl group, preferably ethylenyl (—CH2CH2—) or butylenyl (—CH2CH2CH2CH2—) radicals.
Type:
Application
Filed:
December 30, 2013
Publication date:
April 21, 2016
Inventors:
MARQUIZA SABLON CARRAZANA, Chrislayne RODRIGUEZ-TANTY, Myriam Marlene ALTAMIRANO BUSTAMANTE, Fernand Vedrenne GUTIERREZ, Suchitil RIVERA MARRERO, Isaac Gomez FERNANDEZ, Rosa Maria LOPEZ BARROSO, Lina Andrea RIVILLAS ACEVEDOº, Reyna LARA MARTINEZ, Rafaela PEREZ PERERA, Alberto Guadalupe BENCOMO MARTINEZ, Maria Guadalupe DOMINGUEZ MACOUZET, Luis Felipe JIMENEZ GARCIA, Massiel DIAZ MIRANDA, Andreade Julio MORAN, Pedro VALDES SOSA, Alejandro PERERA PINADO, Anais PRATS CAPOTE, Sergio Agustin ISLAS ANDRADE
Publication number: 20150217005
Abstract: This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belong 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.
Type:
Application
Filed:
March 3, 2015
Publication date:
August 6, 2015
Inventors:
Marquiza Sablon Carrazana, Chryslaine Rodriguez-Tanty, Alejandro Perera Pintado, Suchitil Rivera Marrero, Rafaela Perez Perera, Rosa Maria Lopez Barroso, Anais Prats Capote, Herman Velez Castro, Carlos Serafin Perez Martinez, Pedro Valdes Sosa
Publication number: 20120321560
Abstract: 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.
Type:
Application
Filed:
April 17, 2010
Publication date:
December 20, 2012
Inventors:
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