G-protein-coupled receptor regulators and methods of use thereof
US-2024417378-A1 · Dec 19, 2024 · US
US2017143701A1 · US · A1
| Field | Value |
|---|---|
| Publication number | US-2017143701-A1 |
| Application number | US-201515320061-A |
| Country | US |
| Kind code | A1 |
| Filing date | Jun 11, 2015 |
| Priority date | Jun 20, 2014 |
| Publication date | May 25, 2017 |
| Grant date | — |
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Provided is a safe carbohydrate metabolism-ameliorating agent having an excellent carbohydrate metabolism-ameliorating action, and a safe GLP-1 secretion accelerator having an excellent GLP-1 secretion-accelerating action. The carbohydrate metabolism-ameliorating agent or GLP-1 secretion accelerator according to the present invention, which contains a specific cyclic dipeptide or a salt thereof as an active ingredient, is advantageous in that it has an excellent carbohydrate metabolism-ameliorating action, and that it is safe and can be ingested for a long period.
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1 . A carbohydrate metabolism-ameliorating agent comprising a cyclic dipeptide including amino acids as constituent units or a salt thereof as an active ingredient, wherein the cyclic dipeptide or salt thereof is one or two or more cyclic dipeptides selected from the group consisting of cyclo-threonyl-tyrosine, cyclo-valyl-tyrosine, cyclo-glutaminyl-tyrosine, cyclo-asparaginyl-isoleucine, cyclo-arginyl-proline, cyclo-asparaginyl-glycine, cyclo-methionyl-valine, cyclo-glutamyl-cysteine, cyclo-seryl-glutamic acid, cyclo-isoleucyl-lysine, cyclo-glutaminyl-leucine, cyclo-isoleucyl-threonine, cyclo-threonyl-threonine, cyclo-methionyl-threonine, cyclo-alanyl-cysteine, cyclo-glycyl-cysteine, cyclo-aspartyl-serine, cyclo-arginyl-aspartic acid, cyclo-glycyl-tryptophan, cyclo-histidyl-phenylalanine, cyclo-aspartyl-leucine, cyclo-isoleucyl-histidine, cyclo-seryl-leucine, cyclo-isoleucyl-aspartic acid, cyclo-seryl-cysteine, cyclo-phenylalanyl-tryptophan, cyclo-alanyl-leucine, cyclo-glutaminyl-histidine, cyclo-arginyl-valine, cyclo-glutamyl-leucine, cyclo-leucyl-tryptophan, cyclo-tryptophanyl-tryptophan, cyclo-L-alanyl-proline, cyclo-methionyl-arginine, cyclo-lysyl-phenylalanine, cyclo-phenylalanyl-phenylalanine, cyclo-tryptophanyl-tyrosine, cyclo-asparaginyl-valine, cyclo-glutaminyl-isoleucine, cyclo-alanyl-serine, cyclo-methionyl-histidine, cyclo-methionyl-proline, cyclo-arginyl-leucine, cyclo-methionyl-glutamic acid, cyclo-methionyl-alanine, cyclo-isoleucyl-glutamic acid, cyclo-isoleucyl-serine, cyclo-valyl-serine, cyclo-methionyl-glycine, cyclo-valyl-threonine, cyclo-valyl-aspartic acid, cyclo-glycyl-proline, cyclo-leucyl-proline, cyclo-glutaminyl-glycine, cyclo-tryptophanyl-lysine, cyclo-glutaminyl-phenylalanine, cyclo-lysyl-glycine, cyclo-seryl-lysine, cyclo-valyl-lysine, cyclo-asparaginyl-lysine, cyclo-histidyl-histidine, cyclo-threonyl-histidine, cyclo-aspartyl-histidine, cyclo-asparaginyl-histidine, cyclo-arginyl-serine, cyclo-asparaginyl-methionine, cyclo-glutaminyl-methionine, cyclo-tryptophanyl-arginine, cyclo-asparaginyl-arginine, cyclo-asparaginyl-proline, and cyclo-arginyl-arginine or salts thereof. 2 . The carbohydrate metabolism-ameliorating agent according to claim 1 , wherein the cyclic dipeptide or salt thereof is three or more cyclic dipeptides selected from the group defined in claim 1 or salts thereof. 3 . A GLP-1 secretion accelerator comprising a cyclic dipeptide including amino acids as constituent units or a salt thereof as an active ingredient, wherein the cyclic dipeptide or salt thereof is one or two or more cyclic dipeptides selected from the group consisting of cyclo-threonyl-tyrosine, cyclo-valyl-tyrosine, cyclo-glutaminyl-tyrosine, cyclo-asparaginyl-isoleucine, cyclo-arginyl-proline, cyclo-asparaginyl-glycine, cyclo-methionyl-valine, cyclo-glutamyl-cysteine, cyclo-seryl-glutamic acid, cyclo-isoleucyl-lysine, cyclo-glutaminyl-leucine, cyclo-isoleucyl-threonine, cyclo-threonyl-threonine, cyclo-methionyl-threonine, cyclo-alanyl-cysteine, cyclo-glycyl-cysteine, cyclo-aspartyl-serine, cyclo-arginyl-aspartic acid, cyclo-glycyl-tryptophan, cyclo-histidyl-phenylalanine, cyclo-aspartyl-leucine, cyclo-isoleucyl-histidine, cyclo-seryl-leucine, cyclo-isoleucyl-aspartic acid, cyclo-seryl-cysteine, cyclo-phenylalanyl-tryptophan, cyclo-alanyl-leucine, cyclo-glutaminyl-histidine, cyclo-arginyl-valine, cyclo-glutamyl-leucine, cyclo-leucyl-tryptophan, cyclo-tryptophanyl-tryptophan, cyclo-L-alanyl-proline, cyclo-methionyl-arginine, cyclo-lysyl-phenylalanine, cyclo-phenylalanyl-phenylalanine, cyclo-tryptophanyl-tyrosine, cyclo-asparaginyl-valine, cyclo-glutaminyl-isoleucine, cyclo-alanyl-serine, cyclo-methionyl-histidine, cyclo-methionyl-proline, cyclo-arginyl-leucine, cyclo-methionyl-glutamic acid, cyclo-methionyl-alanine, cyclo-isoleucyl-glutamic acid, cyclo-isoleucyl-serine, cyclo-valyl-serine, cyclo-methionyl-glycine, cyclo-valyl-threonine, and cyclo-valyl-aspartic acid, cyclo-glycyl-proline, cyclo-leucyl-proline, cyclo-glutaminyl-glycine, cyclo-tryptophanyl-lysine, cyclo-glutaminyl-phenylalanine, cyclo-lysyl-glycine, cyclo-seryl-lysine, cyclo-valyl-lysine, cyclo-asparaginyl-lysine, cyclo-histidyl-histidine, cyclo-threonyl-histidine, cyclo-aspartyl-histidine, cyclo-asparaginyl-histidine, cyclo-arginyl-serine, cyclo-asparaginyl-methionine, cyclo-glutaminyl-methionine, cyclo-tryptophanyl-arginine, cyclo-asparaginyl-arginine, cyclo-asparaginyl-proline, and cyclo-arginyl-arginine or salts thereof. 4 . The GLP-1 secretion accelerator according to claim 3 , wherein the cyclic dipeptide or salt thereof is three or more cyclic dipeptides selected from the group defined in claim 3 or salts thereof. 5 . The GLP-1 secretion accelerator according to claim 1 , wherein the cyclic dipeptide including amino acids as constituent units is derived from soybean. 6 . The GLP-1 secretion accelerator according to claim 1 , wherein the cyclic dipeptide including amino acids as constituent units is derived from tea. 7 . Use of a cyclic dipeptide including amino acids as constituent units or a salt thereof for ameliorating carbohydrate metabolism, wherein the cyclic dipeptide or salt thereof is one or two or more cyclic dipeptides selected from the group consisting of cyclo-threonyl-tyrosine, cyclo-valyl-tyrosine, cyclo-glutaminyl-tyrosine, cyclo-asparaginyl-isoleucine, cyclo-arginyl-proline, cyclo-asparaginyl-glycine, cyclo-methionyl-valine, cyclo-glutamyl-cysteine, cyclo-seryl-glutamic acid, cyclo-isoleucyl-lysine, cyclo-glutaminyl-leucine, cyclo-isoleucyl-threonine, cyclo-threonyl-threonine, cyclo-methionyl-threonine, cyclo-alanyl-cysteine, cyclo-glycyl-cysteine, cyclo-aspartyl-serine, cyclo-arginyl-aspartic acid, cyclo-glycyl-tryptophan, cyclo-histidyl-phenylalanine, cyclo-aspartyl-leucine, cyclo-isoleucyl-histidine, cyclo-seryl-leucine, cyclo-isoleucyl-aspartic acid, cyclo-seryl-cysteine, cyclo-phenylalanyl-tryptophan, cyclo-alanyl-leucine, cyclo-glutaminyl-histidine, cyclo-arginyl-valine, cyclo-glutamyl-leucine, cyclo-leucyl-tryptophan, cyclo-tryptophanyl-tryptophan, cyclo-L-alanyl-proline, cyclo-methionyl-arginine, cyclo-lysyl-phenylalanine, cyclo-phenylalanyl-phenylalanine, cyclo-tryptophanyl-tyrosine, cyclo-asparaginyl-valine, cyclo-glutaminyl-isoleucine, cyclo-alanyl-serine, cyclo-methionyl-histidine, cyclo-methionyl-proline, cyclo-arginyl-leucine, cyclo-methionyl-glutamic acid, cyclo-methionyl-alanine, cyclo-isoleucyl-glutamic acid, cyclo-isoleucyl-serine, cyclo-valyl-serine, cyclo-methionyl-glycine, cyclo-valyl-threonine, and cyclo-valyl-aspartic acid, cyclo-glycyl-proline, cyclo-leucyl-proline, cyclo-glutaminyl-glycine, cyclo-tryptophanyl-lysine, cyclo-glutaminyl-phenylalanine, cyclo-lysyl-glycine, cyclo-seryl-lysine, cyclo-valyl-lysine, cyclo-asparaginyl-lysine, cyclo-histidyl-histidine, cyclo-threonyl-histidine, cyclo-aspartyl-histidine, cyclo-asparaginyl-histidine, cyclo-arginyl-serine, cyclo-asparaginyl-methionine, cyclo-glutaminyl-methionine, cyclo-tryptophanyl-arginine, cyclo-asparaginyl-arginine, cyclo-asparaginyl-proline, and cyclo-arginyl-arginine or salts thereof. 8 . The use according to claim 7 , wherein the cyclic dipeptide or salt thereof is three or more cyclic dipeptides selected from the group defined in claim 7 or salts thereof. 9 . The use according to claim 7 , wherein the cyclic dipeptide including amino acids as constituent units is derived from soybean. 10 . The use according to claim 7 , wherein the cyclic dipeptide including amino acids as constituent units is derived from tea. 11 . The GLP-1 secretion accelerator according to claim 2 , wherein the cyclic dipeptide including amino acids as constituent units is derived from soybean. 12 . The GLP-1 secretion accelerator acc
for hyperglycaemia, e.g. antidiabetics · CPC title
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
for increasing or potentiating the activity of insulin · CPC title
Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae · CPC title
Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems · CPC title
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