http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2187511-C2
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_ba045776bcd32d32e3100da8dfce4e28 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K7-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-725 |
filingDate | 1997-02-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2002-08-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_089c075be9aec9cfd9992cb2b320d211 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2a1ccd14eba42c93f3aafb69fd4dfbc5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_658132a5e9363922a45bff8ac2634ba5 |
publicationDate | 2002-08-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | RU-2187511-C2 |
titleOfInvention | Peptide derivatives |
abstract | FIELD: organic chemistry, peptides. SUBSTANCE: invention proposes peptide derivatives of the general formula (I): P-R 1 -R 2 -R 3 -R 4 or their pharmaceutically acceptable salts where P means an organic hydrophobic group comprising of from 5 to 20 carbon atoms of the formula RCO- where R means aryl(2-10 C)alkyl or heteroaryl(2-10 C)alkyl where aryl or heteroaryl group in R is substituted optionally with one or more (1-4 C)alkyl, halogen atom, cyano-group or (1-4 C)alkoxy-group; R 1 means a sequence of 5 L-amino acid presented as AA1-AA2-AA3-AA4-AA5 and R 3 means a single L-amino acid taken among Ala, Gly, azaalanine or azaglycine; or R 1 means a sequence of 3 L- amino acids presented as AA6-AA7-AA8 and R 3 means a sequence of 3 L-amino acids presented as AA9-AA10- -AA11 where AA1 is taken among Ala, Ile, Arg, Gap, GapMe4 and Lys(=C(NMe 2 ) 2 ); AA2 is taken among Ala, Lys, Ile and Arg; AA3 is taken among Ala and Asn; AA4 is taken among Ala, Asn, Lys, Arg and His; AA5 is taken among Val and Thr; AA6 is taken among Ala, Arg and Ile; AA7 is taken among Lys, Arg, Ala and Ile; AA8 means Ala; AA9 is taken among Ala and Leu; AA10 is taken among Ala and Arg; AA11 means Ala; R 2 means a group of the formula (II) or formula (III) where Ra and Rb are taken independently among hydrogen atom and (1-4 C)alkyl and A means methylene; and R 4 means OH, NH 2 or NRcRd where Rc is taken among (1-4 C)alkyl, 3-carbamoylphenyl, 4-carbamoylphenyl, 4-(carbamoylmethyl)phenyl, 4-(carboxymethyl)-phenyl, 4-(methoxycarbonylmethyl)phenyl, 2-morpholinoethyl and a group of the formula -A 1 -G 1 where A 1 means (3 C)alkylene or A 1 means a group of the formula -A 2 -B 2 - where A 2 means p-phenylene and B 2 means (1-4 C)alkylene; and G 1 means a group of the formula -N=C[N(Rp) 2 ] 2 where each Rp means hydrogen atom; or A 1 means a group of the formula -A 4 -B 4 - where A 4 means p-phenylene and B 4 means -CH 2 --CO-; and G 1 means 2-morpholinoethylamino-group or 4-[2-(2-hydroxyethoxy)ethyl] -piperazine-1-yl; and Rd means hydrogen atom or (1-4 C)alkyl; or R 4 means 4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl, 1-piperidyl or 4-substituted-1-piperidyl where this 4-substitute is taken among carboxy-group and carbamoyl-group. Invention proposes a method of synthesis of compounds of the formula (I) by claim 1and a pharmaceutical composition showing ability to inhibit T- cellular immune response mediated by molecule MHC of class II comprising the peptide derivative of the formula (I) or its pharmaceutically acceptable salt. Invention proposes a method of treatment of MHC- dependent of class II T-cellular mediated autoimmune or inflammatory disease. The described invention proposes peptides showing minimal losses associated with degradation in release from a medicinal preparation. EFFECT: improved method of treatment, valuable medicinal properties. 15 cl |
priorityDate | 1996-10-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 45.