Neuroprotective agents

 

The invention relates to a group of compounds of General formula (I) high degree of purification.

where Q represents a group of positive charge selected from a number of amido groups or groups with the formula XYN-, where X and Y are the same or different and each may represent a hydrogen atom, a C1-C6-alkyl, or a simple group containing a heteroatom, or together with the nitrogen atom to which they are attached, form a heterocyclic group with the nitrogen; Rais a straight or branched chain alkylene or alkilinity group having from 1 to 6 carbon atoms, and each of which may be optionally substituted by 1 to 4 alkyl groups with the number of carbon atoms from 1 to 3; Rband Rcboth are alkylene or alkilinity group containing 3 or 4 carbon atoms in a straight chain, each of which may be optionally substituted 1 or 2 the two alkyl groups each containing 1 to 3 carbon atoms, with the total number of carbon atoms in said straight chain Rband Rcequal to 7; R2and R3the same or different from each other and each represents a hydrogen atom or a group with the formula R is substituted by one or more substituentsdefined below; chiral carbon atom marked with an asterisk in- configuration; Z is an aromatic amino acid residue; n is 0 or 1; R1represents a hydrogen atom or a lower alkyl group which may be optionally substituted by one or more substituentsdefined below, and
W represents a hydrogen atom or an alkyl or aryl group; and
deputiesselected from: halogen atoms, amino groups, alkylamino, dialkylamino, cyano groups, hydroxyl, alkyl groups (except substitution alkyl), aryl groups, karbonilnyh, alkyl - and dialkylanilines groups and carboxyl groups and derivatives of the latter esters, and pharmaceutically acceptable salts of the compounds, despite the fact that the length of the longest link chain means the number of atoms excluding hydrogen from 14 to 25 who have a neuroprotective effect; and to a method of treatment of mammals in order to protect them from neural lesions. 3 S. p. and 15 C.p. f-crystals, 7 tab., 4 Il.

Description text in facsimile form (see graphic part). Those



where Q represents a group of positive charge selected from a number of aminogroup or groups with the formula XYN-, where X and Y are the same or different and each may represent a hydrogen atom, a C1-C6-alkyl, or a simple group containing a heteroatom, or together with the nitrogen atom to which they are attached, form a heterocyclic group with the nitrogen;
Rais a straight or branched chain alkylene or alkilinity group having from 1 to 6 carbon atoms and each of which may be optionally substituted by 1 to 4 alkyl groups with the number of carbon atoms from 1 to 3.

Rband Rcboth are alkylene or alkilinity group containing 3 or 4 carbon atoms in a straight chain, each of which may be optionally substituted 1 or 2 the two alkyl groups each containing 1 to 3 carbon atoms, with the total number of carbon atoms in said straight chain Rband Rcequal to 7;
R2and R3the same or different from each other, and each represents a hydrogen atom or a group with the formula R, RCO-, ROCO or RNHCO-, where R is an alkyl or aryl group, these groups can be optionally substituted is marked with an asterisk inconfiguration;
Z is an aromatic amino acid residue;
n is 0 or 1;
R1represents a hydrogen atom or a lower alkyl group which may be optionally substituted by one or more substituentsdefined below, and
W represents a hydrogen atom or an alkyl or aryl group; and the substituentsare selected from halogen atoms, amino groups, alkylamino, dialkylamino, cyano groups, hydroxyl, alkyl groups (except substitution alkyl), aryl groups, karbonilnyh, alkyl - and dialkylanilines groups and carboxyl groups and derivatives of the latter ester,
and pharmaceutically acceptable salts of the compounds, despite the fact that the length of the longest link chain means the number of atoms excluding hydrogen from 14 to 25.

2. Connection on p. 1, corresponding to formula (Ia)

where Q, Ra, Rb, Rc, R2, R3, Z, n and R1defined in paragraph 1.

3. Connection on p. 1, corresponding to formula (Ib)

where X, Y, Z, n and R1defined above;
x is an integer from 1 to 5;
y is 3 or 4;
R4, R5, Rconfiguration;
4. Compounds according to any of the preceding paragraphs, in which Z is an aromatic amino acid residue inconfiguration.

5. Non-toxic salts of the compounds of formula (I) under item 1.

6. Non-toxic salts of the compounds of the formula Iandunder item 2.

7. Non-toxic salts of the compounds of the formula Ibunder item 3.

8. Connection on p. 1, which is a

9. Connection on p. 1, which is a

10. Connection on p. 1, which is a

11. Connection on p. 1, which is a

12. Connection on p. 1, which is a

13. Connection on p. 1, which is a

14. Connection on p. 1, which is a

15. Connection on p. 1, which is a

16. Connection on p. 1, which is a
treatment of mammals in order to protect them from neural lesions by introducing them to, after or during ischemic exposure to an effective amount of toxic compounds, the corresponding PP. 1-16.

 

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< / BR>
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< / BR>
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< / BR>
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< / BR>
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< / BR>
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