JP2007519642A5 - - Google Patents
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- JP2007519642A5 JP2007519642A5 JP2006549818A JP2006549818A JP2007519642A5 JP 2007519642 A5 JP2007519642 A5 JP 2007519642A5 JP 2006549818 A JP2006549818 A JP 2006549818A JP 2006549818 A JP2006549818 A JP 2006549818A JP 2007519642 A5 JP2007519642 A5 JP 2007519642A5
- Authority
- JP
- Japan
- Prior art keywords
- glp
- seq
- gastrin
- agonist
- weeks
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 102400000921 Gastrin Human genes 0.000 claims 41
- 108010052343 Gastrins Proteins 0.000 claims 36
- 239000003877 glucagon like peptide 1 receptor agonist Substances 0.000 claims 35
- -1 gastrin compound Chemical class 0.000 claims 31
- 239000008194 pharmaceutical composition Substances 0.000 claims 28
- 239000000203 mixture Substances 0.000 claims 27
- 230000009286 beneficial effect Effects 0.000 claims 21
- 150000001408 amides Chemical class 0.000 claims 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 201000010099 disease Diseases 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 9
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 8
- AOXOCDRNSPFDPE-UKEONUMOSA-N chembl413654 Chemical compound C([C@H](C(=O)NCC(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@@H](N)CCC(O)=O)C1=CC=C(O)C=C1 AOXOCDRNSPFDPE-UKEONUMOSA-N 0.000 claims 7
- 230000002459 sustained effect Effects 0.000 claims 7
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 6
- 102400000322 Glucagon-like peptide 1 Human genes 0.000 claims 6
- 206010012601 diabetes mellitus Diseases 0.000 claims 6
- GKDWRERMBNGKCZ-RNXBIMIWSA-N gastrin-17 Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 GKDWRERMBNGKCZ-RNXBIMIWSA-N 0.000 claims 6
- 238000011282 treatment Methods 0.000 claims 6
- 108010066264 gastrin 17 Proteins 0.000 claims 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims 5
- 239000003981 vehicle Substances 0.000 claims 5
- 101800000285 Big gastrin Proteins 0.000 claims 4
- 108700006605 Val(8)- glucagon-like peptide 1 (7-36) Proteins 0.000 claims 4
- 239000000556 agonist Substances 0.000 claims 4
- 201000001421 hyperglycemia Diseases 0.000 claims 4
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 4
- 102000004506 Blood Proteins Human genes 0.000 claims 3
- 108010017384 Blood Proteins Proteins 0.000 claims 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 3
- 210000004369 blood Anatomy 0.000 claims 3
- 239000008280 blood Substances 0.000 claims 3
- 230000003247 decreasing effect Effects 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 239000008103 glucose Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000031729 Bacteremia Diseases 0.000 claims 2
- 102400000948 Big gastrin Human genes 0.000 claims 2
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 208000002705 Glucose Intolerance Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000013016 Hypoglycemia Diseases 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 208000007177 Left Ventricular Hypertrophy Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 208000007107 Stomach Ulcer Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 230000006793 arrhythmia Effects 0.000 claims 2
- 206010003119 arrhythmia Diseases 0.000 claims 2
- 230000001925 catabolic effect Effects 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 201000005917 gastric ulcer Diseases 0.000 claims 2
- FMIHGWZLPSIAFY-WGFKALLTSA-N gastrin-34 Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1N(CCC1)C(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCC(N)=O)C(C)C)C1=CC=C(O)C=C1 FMIHGWZLPSIAFY-WGFKALLTSA-N 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 210000004153 islets of langerhan Anatomy 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000010125 myocardial infarction Diseases 0.000 claims 2
- 230000009707 neogenesis Effects 0.000 claims 2
- 230000000626 neurodegenerative effect Effects 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 230000002093 peripheral effect Effects 0.000 claims 2
- 230000002980 postoperative effect Effects 0.000 claims 2
- 201000009104 prediabetes syndrome Diseases 0.000 claims 2
- RZIMNEGTIDYAGZ-HNSJZBNRSA-N pro-gastrin Chemical compound N([C@@H](CC(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CC(O)=O)C(=O)NCC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)C(=O)[C@@H]1CCC(=O)N1 RZIMNEGTIDYAGZ-HNSJZBNRSA-N 0.000 claims 2
- NGJOFQZEYQGZMB-KTKZVXAJSA-N (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 NGJOFQZEYQGZMB-KTKZVXAJSA-N 0.000 claims 1
- VOUAQYXWVJDEQY-QENPJCQMSA-N 33017-11-7 Chemical compound OC(=O)CC[C@H](N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(O)=O)CCC1 VOUAQYXWVJDEQY-QENPJCQMSA-N 0.000 claims 1
- 108010075254 C-Peptide Proteins 0.000 claims 1
- 206010061818 Disease progression Diseases 0.000 claims 1
- 102400000920 Gastrin-14 Human genes 0.000 claims 1
- 102400000949 Gastrin-52 Human genes 0.000 claims 1
- 101800004422 Gastrin-52 Proteins 0.000 claims 1
- 102400000922 Gastrin-6 Human genes 0.000 claims 1
- 101800002467 Gastrin-6 Proteins 0.000 claims 1
- 102400000947 Gastrin-71 Human genes 0.000 claims 1
- 101800001254 Gastrin-71 Proteins 0.000 claims 1
- 101800004295 Glucagon-like peptide 1(7-36) Proteins 0.000 claims 1
- 102000008100 Human Serum Albumin Human genes 0.000 claims 1
- 108091006905 Human Serum Albumin Proteins 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 1
- JQSXWJXBASFONF-KKUMJFAQSA-N Leu-Asp-Phe Chemical group [H]N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(O)=O JQSXWJXBASFONF-KKUMJFAQSA-N 0.000 claims 1
- PNDCUTDWYVKBHX-IHRRRGAJSA-N Met-Asp-Tyr Chemical compound CSCC[C@H](N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(O)=O)CC1=CC=C(O)C=C1 PNDCUTDWYVKBHX-IHRRRGAJSA-N 0.000 claims 1
- 108010079943 Pentagastrin Proteins 0.000 claims 1
- 206010039897 Sedation Diseases 0.000 claims 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 1
- 108010012944 Tetragastrin Proteins 0.000 claims 1
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- UKVFVQPAANCXIL-FJVFSOETSA-N glp-1 (1-37) amide Chemical group C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 UKVFVQPAANCXIL-FJVFSOETSA-N 0.000 claims 1
- 108010063245 glucagon-like peptide 1 (7-36)amide Proteins 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 210000002660 insulin-secreting cell Anatomy 0.000 claims 1
- 230000002045 lasting effect Effects 0.000 claims 1
- 238000012153 long-term therapy Methods 0.000 claims 1
- 230000007774 longterm Effects 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 108010076432 minigastrin Proteins 0.000 claims 1
- 230000007935 neutral effect Effects 0.000 claims 1
- 230000001019 normoglycemic effect Effects 0.000 claims 1
- ANRIQLNBZQLTFV-DZUOILHNSA-N pentagastrin Chemical compound C([C@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1[C]2C=CC=CC2=NC=1)NC(=O)CCNC(=O)OC(C)(C)C)CCSC)C(N)=O)C1=CC=CC=C1 ANRIQLNBZQLTFV-DZUOILHNSA-N 0.000 claims 1
- 229960000444 pentagastrin Drugs 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 229920001184 polypeptide Polymers 0.000 claims 1
- 239000002243 precursor Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
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- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
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- 238000012154 short term therapy Methods 0.000 claims 1
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- 210000000130 stem cell Anatomy 0.000 claims 1
- 230000004083 survival effect Effects 0.000 claims 1
- RGYLYUZOGHTBRF-BIHRQFPBSA-N tetragastrin Chemical compound C([C@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C2=CC=CC=C2NC=1)CCSC)C(N)=O)C1=CC=CC=C1 RGYLYUZOGHTBRF-BIHRQFPBSA-N 0.000 claims 1
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| PCT/CA2005/000099 WO2005072045A2 (en) | 2004-01-30 | 2005-01-28 | The combined use of glp-1 agonists and gastrin for regulating blood glucose levels |
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| JP2007519642A JP2007519642A (ja) | 2007-07-19 |
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| EP (1) | EP1711532A4 (https=) |
| JP (1) | JP2007519642A (https=) |
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| IL (1) | IL177066A0 (https=) |
| RU (1) | RU2006131046A (https=) |
| WO (1) | WO2005072045A2 (https=) |
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| IL156828A0 (en) | 2001-01-12 | 2004-02-08 | Waratah Pharmaceuticals Inc | Prolonged efficacy of islet neogenesis therapy methods with a gastrin/cck receptor ligand and an egf receptor ligand composition in subjects with preexisting diabetes |
| US7560425B2 (en) | 2002-06-07 | 2009-07-14 | Waratah Pharmaceuticals Inc. | Pharmaceutical composition consisting of rapamycine and gastrin 17(LEU15) and a method for treating diabetes |
| EP1837031B1 (en) | 2002-06-07 | 2009-10-14 | Waratah Pharmaceuticals, Inc. | Compositions and methods for treating diabetes |
| WO2006000567A2 (en) * | 2004-06-28 | 2006-01-05 | Novo Nordisk A/S | Use of glp-1 receptor agonists and / or dpp-iv inhibitors in combination with proton pump inhibitors and ppar agonists for the preparation of a medicament for the treatment of diabetes type i i and impaired pancreatic beta-cell function |
| EP1951286A4 (en) * | 2005-10-07 | 2009-11-04 | Waratah Pharmaceuticals Inc | COMBINED USE OF INHIBITORS OF DPP-IV AND GASTRIN COMPOUNDS |
| EP1971363A1 (en) * | 2005-12-02 | 2008-09-24 | Waratah Pharmaceuticals, Inc. | Combination treatments with gastrin agonists for diabetes and related diseases |
| WO2007095737A1 (en) * | 2006-02-21 | 2007-08-30 | Waratah Pharmaceuticals Inc. | Combination therapy for the treatment of diabetes comprising an exendin agonist and a gastrin compound |
| WO2008071010A1 (en) * | 2006-12-12 | 2008-06-19 | Waratah Pharmaceuticals Inc. | Combination treatments with selected growth/hormone regulatory factors for diabetes and related diseases |
| WO2008106779A1 (en) * | 2007-03-02 | 2008-09-12 | Waratah Pharmaceuticals Inc. | Gastrin compound for diabetes treatment |
| JP2010539017A (ja) * | 2007-09-11 | 2010-12-16 | モンドバイオテック ラボラトリーズ アクチエンゲゼルシャフト | 単独でまたはニューロキニン−ｂと組み合わせて用いる、治療剤としてのｒｆｒｐの使用 |
| US9168288B2 (en) * | 2010-04-09 | 2015-10-27 | Mount Sinai Hospital | Methods for treating disorders of the gastrointestinal tract using a GLP-1 agonist |
| EA023925B1 (ru) | 2010-04-27 | 2016-07-29 | Зилэнд Фарма А/С | Пептидные конъюгаты агонистов рецептора glp-1 и их применение |
| JP2014504588A (ja) * | 2010-12-22 | 2014-02-24 | アミリン・ファーマシューティカルズ，リミテッド・ライアビリティ・カンパニー | 膵島細胞移植のためのｇｌｐ−１受容体アゴニスト |
| MX2014005351A (es) | 2011-11-03 | 2014-05-28 | Zealand Pharma As | Conjugados de gastrina peptidicos de agonistas de receptor glp-1. |
| AU2013295035B2 (en) | 2012-07-23 | 2017-08-03 | Zealand Pharma A/S | Glucagon analogues |
| TWI608013B (zh) | 2012-09-17 | 2017-12-11 | 西蘭製藥公司 | 升糖素類似物 |
| US9988429B2 (en) | 2013-10-17 | 2018-06-05 | Zealand Pharma A/S | Glucagon analogues |
| WO2015055801A1 (en) | 2013-10-17 | 2015-04-23 | Zealand Pharma A/S | Acylated glucagon analogues |
| AU2014345570B2 (en) | 2013-11-06 | 2019-01-24 | Zealand Pharma A/S | Glucagon-GLP-1-GIP triple agonist compounds |
| MX2016005556A (es) | 2013-11-06 | 2016-07-15 | Zealand Pharma As | Compuestos agonistas duales de gip-glp-1 y procedimientos. |
| US10253078B2 (en) | 2014-10-29 | 2019-04-09 | Zealand Pharma A/S | GIP agonist compounds and methods |
| WO2016168388A2 (en) * | 2015-04-14 | 2016-10-20 | Palatin Technologies, Inc. | Therapies for obesity, diabetes and related indications |
| US10336802B2 (en) | 2015-04-16 | 2019-07-02 | Zealand Pharma A/S | Acylated glucagon analogue |
| AU2017371516C1 (en) | 2016-12-09 | 2021-09-02 | Zealand Pharma A/S | Acylated GLP-1/GLP-2 dual agonists |
| WO2019200594A1 (zh) | 2018-04-19 | 2019-10-24 | 杭州先为达生物科技有限公司 | 酰化的glp-1衍生物 |
| CN112759640B (zh) * | 2020-12-09 | 2023-09-08 | 江苏师范大学 | 一类glp-1/胃泌素受体双重激动剂及其应用 |
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| US5545618A (en) * | 1990-01-24 | 1996-08-13 | Buckley; Douglas I. | GLP-1 analogs useful for diabetes treatment |
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| US5424286A (en) * | 1993-05-24 | 1995-06-13 | Eng; John | Exendin-3 and exendin-4 polypeptides, and pharmaceutical compositions comprising same |
| US5705483A (en) * | 1993-12-09 | 1998-01-06 | Eli Lilly And Company | Glucagon-like insulinotropic peptides, compositions and methods |
| GB9409496D0 (en) * | 1994-05-12 | 1994-06-29 | London Health Ass | Method for improving glycaemic control in diabetes |
| US5512549A (en) * | 1994-10-18 | 1996-04-30 | Eli Lilly And Company | Glucagon-like insulinotropic peptide analogs, compositions, and methods of use |
| US20010006943A1 (en) * | 1994-12-23 | 2001-07-05 | Ejvind Jensen | Protracted GLP-1 compositions |
| DE19514087A1 (de) * | 1995-04-13 | 1996-10-17 | Deutsches Krebsforsch | Konjugat aus einem Wirkstoff, einem Polyether und ggfs. einem nicht als körperfremd angesehenen, nativen Protein |
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| US5981488A (en) * | 1997-03-31 | 1999-11-09 | Eli Lillly And Company | Glucagon-like peptide-1 analogs |
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| AU5027299A (en) * | 1998-07-31 | 2000-02-28 | Novo Nordisk A/S | Use of glp-1 and analogues for preventing type ii diabetes |
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| KR20050074492A (ko) * | 2002-10-22 | 2005-07-18 | 와라타 파마수티컬즈, 인크. | 당뇨병의 치료 |
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-
2005
- 2005-01-28 US US10/587,529 patent/US20090202494A1/en not_active Abandoned
- 2005-01-28 BR BRPI0507189-5A patent/BRPI0507189A/pt not_active IP Right Cessation
- 2005-01-28 AU AU2005207870A patent/AU2005207870B2/en not_active Ceased
- 2005-01-28 EP EP05706425A patent/EP1711532A4/en not_active Withdrawn
- 2005-01-28 CA CA002554458A patent/CA2554458A1/en not_active Abandoned
- 2005-01-28 RU RU2006131046/15A patent/RU2006131046A/ru not_active Application Discontinuation
- 2005-01-28 WO PCT/CA2005/000099 patent/WO2005072045A2/en not_active Ceased
- 2005-01-28 JP JP2006549818A patent/JP2007519642A/ja not_active Withdrawn
-
2006
- 2006-07-25 IL IL177066A patent/IL177066A0/en unknown
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