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Amides of creatine, method of their preparation, and remedy possessing a neuroprotective activity (патент US № 8350077)

Официальная публикация
патента US № 8350077

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Классы МПК:C07C229/26 ...содержащие более чем одну аминогруппу, связанную с углеродным скелетом, например лизин
C07C231/00 Получение амидов карбоновых кислот
C07C237/20 ..углеродного скелета, содержащего шестичленные ароматические кольца
Автор(ы):Burov, Sergej Vladimirovich (Saint-Petersburg, RU)
Khromova, Natalia Vasilyevna (Saint-Petersburg, RU)
Khromova, Anna Alexandrovna (Saint-Petersburg, RU)
Khromov, Petr Alekseevich (Saint-Petersburg, RU)
Патентообладатель(и):VERTEX Closed Joint Stock Company (St. Petersburg, RU)
Приоритеты:
подача заявки
24.12.2008
публикация патента
08.01.2013

РЕФЕРАТ (Abstract)

The invention relates to pharmaceutical chemistry notably to new biologically active substances (BAS) and their properties. In particular, the invention relates to Creatine derivatives having a general formula: NH═C(NH2)—N(CH3)—CH2—CO—NH—R*X, wherein R—amino acid residue of aliphatic, aromatic or heteroaromatic L-amino acid or its derivative representing a salts of amino acid, amino acid esters, amino acid amides or peptides; X—lower organic or mineral acid or water. New substances are prepared by interaction of aforesaid amides of sarcosine having a general formula of HN(CH3)—CH2—CO—NH—R*X, wherein: R is amino acid residue or substituted amino acid residue; X is low-molecular-weight organic acid or mineral acid or water, with a guanidinylating agents with the in organic solvents at temperature not exceeding 50° C. New chemical compounds can be used as a remedy possessing a neuroprotective activity.

ФОРМУЛА ИЗОБРЕТЕНИЯ (CLAIMS)

The invention claimed is:

1. Amides of Creatine having a general formula: NH═C(NH2)-N(CH3)-CH2-CO—NH—R*X, wherein R is amino acid residue of aliphatic L-amino acid, or aromatic amino L-acid or heteroaromatic L-amino acid or derivatives of aliphatic L-amino acid, or aromatic L-amino acid or heteroaromatic L-amino acid representing at least one of the following: salts of amino acid, amino acid esters, amino acid amides, or amino acid peptides; and X is low-molecular-weight organic or mineral acid or water.

2. A method for preparation of said amides of Creatine according to claim 1, said method comprising: interaction of amides of sarcosine and amino acids or their derivatives with guanidinylating agents in an organic solvents at a temperature not exceeding 50° C.

3. A compound possessing neuroprotective activity, said compound consisting of: amides of Creatine having a general formula: NH═C(NH2)—N(CH3)—CH2—CO—NH—R*X; wherein R is amino acid residue of aliphatic L-amino acid, or aromatic amino L-acid or heteroaromatic L-amino acid, or derivatives of aliphatic L-amino acid, or aromatic L-amino acid, or heteroaromatic L-amino acid representing at least one of the following: salts of amino acid, amino acid esters, amino acid amides, or amino acid peptides; and X is low-molecular-weight organic or mineral acid or water as a remedy possessing a neuroprotective activity.


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