http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2624451-T3
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_30b12884bf7af9bb83635dc6a3b10e6a |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-1024 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K14-665 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K7-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-665 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-10 |
filingDate | 2010-08-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2017-07-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9da87cf95d1cca729e373ddd36aac0a2 |
publicationDate | 2017-07-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | ES-2624451-T3 |
titleOfInvention | Melanocortin stabilized ligands |
abstract | A non-naturally occurring melanocortin ligand which comprises a melanocortin analog coupled to a degradation-resistant C-terminal extension and an N-terminal extension, where the non-naturally occurring melanocortin ligand comprises the Formula I: Y1-Y2-Y3-R1-R2-R3-R4-5 R5-R6-R7-X1-X2-X3 (Formula I) where the melanocortin analog comprises R1 to R7, where: R1 is absent or selected from the group consisting of cysteine, norleucine, acetylated norleucine, acetylated cysteine, D-phenylalanine, D-phenylalanine acetylated, succinic acid, o-phthalic acid, tyrosine, aspartic acid, glutaric acid, CO-cis-CH> = CH-CO , an n-pentanoyl group, and an n-hexanoyl group; R2 is absent or selected from the group consisting of proline, aspartic acid, glutamic acid, glycine, cysteine, norleucine, arginine, succinic acid, glutaric acid, CO-cis-CH> = CH-CO, an n-pentanoyl group, and a nhexanoyl group; R3 is selected from the group consisting of histidine, 1 or 3-position methylated histidine, D-proline, L-proline, DNal (2 '), L-Nal (2'), succinic acid, tButGly, Hyp (Bzl), Mamb, Oic, norleucine, Aba, ß-alanine, and Tic; R4 is selected from the group consisting of histidine, D-phenylalanine, L-phenylalanine, D-Nal (2 '), pCl-D-Phe, and (o-Phe) Phe; R5 is selected from the group consisting of arginine, homoarginine, ornithine, alanine, proline, Pip, Nip, Tic, Phg, Sar, and Azt; R6 is selected from D-tryptophan, L-tryptophan, D-Nal (2 '), L-Nal (2'), Tic, and Bip; R7 is selected from the group consisting of cysteine, lysine, and 2,3-diamino-propionic acid; where if R3 is Aba, then R4 is selected from the group consisting of D-Phe, D-Nal (2 '), and pCl-D-Phe; and where if R2 is an n-pentanoyl group or an n-hexanoyl group, then R1, Y1, Y2, and Y3 are absent; where the N-terminal extension comprises Y1 to Y3: Y1 is absent or is selected from the group consisting of D-threonine, L-threonine, D-proline, and L-proline; Y2 is absent or selected from the group consisting of D-threonine, L-threonine, D-proline, L-proline, and a piperazin-2-one ring; Y3 is absent or selected from the group consisting of cysteine, D-threonine, L-threonine, D-proline, L-proline, and a piperazin-2-one ring; where the degradation resistant C-terminal extension comprises X1 to X3 and X1 is D-threonine; X2 is D-proline; X3 is D-threonine where the melanocortin ligand is cyclized by a unit selected from the group consisting of: when R2 is cysteine and R7 is cysteine a disulfide bond is formed between R2 and R7; when R2 is glutamic acid or aspartic acid and R7 is lysine, a side chain lactam bridge is formed between R2 and R7; and when R2 or R3 is succinic acid and R7 is 2,3-diamino-propionic acid, a lactam seal is formed between R2 or R3 and R7. |
priorityDate | 2009-08-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 196.