http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2674946-T3

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3120ae9cab5bb4831f0cc16288966367
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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-435
filingDate 2013-06-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2018-07-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7e47a333daaf818894877f87c9d72dc0
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9f7775ccbc8fef610ad72a2002d9ec48
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publicationDate 2018-07-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2674946-T3
titleOfInvention Glucagon analogs showing GIP receptor activity
abstract Peptide comprising the sequence of X1X2X3GTFTSDX10SKYLX15X16X17X18X19X20X21FVQWLX27X28X29X30PSSGX35PPPS (SEQ ID NO: 140), in which: i) X1 corresponds to position 1 of the 5 natural glucagon and X1 is Ace from D-group: , Acetyl D-Phe, Desamino Tyr, D-His and D-Tyr; X2 is Ala, Gly, Pro, sarcosine, Ser and Val, X3 is Gln, an amino acid comprising a side chain of structure I, II, or III, a hydrophobic amino acid, an acidic amino acid or a basic amino acid or is a selected amino acid from the group consisting of: Glu, Ala, Leu, Ile, Nle, Val, Norval, homoserine, Met, methionine sulfoxide, methionine sulfone, acetyl-Orn, acetyldiaminobutanoic acid and acetyl-Lys; wherein structure I, II, and III are: ** Formula ** in which R1 is C0-3 alkyl or C0-3 heteroalkyl; R2 is NHR4 or C1-3 alkyl; R3 is C1-3 alkyl; R4 is H or C1-3 alkyl; X is NH, O, or S; and Y is NHR4, SR3 or OR3; X10 is Tyr or an amino acid covalently linked to a C12 to C18 acyl or alkyl group; X15 is an acidic amino acid, optionally, Glu or Asp; X16 is any amino acid, optionally, any amino acid other than Gly, Pro, and Ser; for example, Glu, Ala, alpha amino acid, alpha-disubstituted (for example, AIB), His, Lys X17 is Arg, His, Gln; X18 is Arg or Ala; X19 is Ala or alpha amino acid, disubstituted alpha; X20 is selected from the group consisting of: alpha amino acid, disubstituted alpha (for example, AIB) or Gln or His, Lys, or Ala; X21 is an acidic amino acid, optionally, Asp or Glu; X27 is Leu, Ala, Nle, or Met; X28 is Ala or an acidic amino acid (optionally, Asp or Glu); X29 is aliphatic, for example, Ala or Leu or Gly or AIB or Val; X30 is a small aliphatic amino acid, for example, Ala or Gly X35 is Ala or a basic amino acid (optionally, Arg or Lys); wherein, when X28 is an acidic amino acid, X35 is a basic amino acid; wherein, optionally, when X28 is Asp, then X29 is not Gly in which, when X10 is Tyr, the peptide comprises at position 40 an amino acid covalently linked to an acyl group or C12 to C18 alkyl, and, in the that, optionally, the peptide comprises Gly at position 41, wherein the C-terminal amino acid of the peptide is amidated; or ii) X1 corresponds to position 1 of natural glucagon and X1 is selected from the group consisting of: Acetyl D-His, Acetyl D-Tyr, Acetyl D-Phe, deamino Tyr, D-His and D-Tyr; X2 is Ala or Gly, X3 is Gln; X10 is an amino acid covalently linked to an acyl or C12-C18 alkyl group; X15 is Asp; X16 is Glu; X17 is Arg, His or Gln; X18 is Ala; X19 is Ala; X20 is Gln; X21 is Asp; X27 is Leu; X28 is Glu; X29 is Gly; X30 is Gly X35 is Ala; wherein the peptide shows agonist activity in the human GIP receptor and the human GLP-1 receptor and / or the human glucagon receptor, optionally, in which the glucagon analogue has a selectivity less than 100 times for the receptor of human GLP-1 against the GIP receptor.
priorityDate 2012-06-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 1448.