JP2015502918A5 - - Google Patents
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- JP2015502918A5 JP2015502918A5 JP2014539352A JP2014539352A JP2015502918A5 JP 2015502918 A5 JP2015502918 A5 JP 2015502918A5 JP 2014539352 A JP2014539352 A JP 2014539352A JP 2014539352 A JP2014539352 A JP 2014539352A JP 2015502918 A5 JP2015502918 A5 JP 2015502918A5
- Authority
- JP
- Japan
- Prior art keywords
- 8ado
- glu
- ygwldf
- leu
- lys
- 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.)
- Granted
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- 208000008589 Obesity Diseases 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 239000012453 solvate Substances 0.000 claims 14
- 235000020824 obesity Nutrition 0.000 claims 12
- 239000000863 peptide conjugate Substances 0.000 claims 12
- 108090000765 processed proteins & peptides Proteins 0.000 claims 12
- 239000000126 substance Substances 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 201000009104 prediabetes syndrome Diseases 0.000 claims 8
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims 6
- 208000032928 Dyslipidaemia Diseases 0.000 claims 6
- 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 6
- 206010020772 Hypertension Diseases 0.000 claims 6
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 6
- 206010012601 diabetes mellitus Diseases 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 239000008103 glucose Substances 0.000 claims 6
- 230000006698 induction Effects 0.000 claims 6
- 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 6
- 208000002705 Glucose Intolerance Diseases 0.000 claims 4
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 4
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 4
- 208000001280 Prediabetic State Diseases 0.000 claims 4
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 4
- 239000005557 antagonist Substances 0.000 claims 4
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 4
- 230000005764 inhibitory process Effects 0.000 claims 4
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 4
- 230000017074 necrotic cell death Effects 0.000 claims 4
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 4
- 229940126409 proton pump inhibitor Drugs 0.000 claims 4
- 239000000612 proton pump inhibitor Substances 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- 244000137850 Marrubium vulgare Species 0.000 claims 3
- 229960002685 biotin Drugs 0.000 claims 3
- 235000020958 biotin Nutrition 0.000 claims 3
- 239000011616 biotin Substances 0.000 claims 3
- 230000037396 body weight Effects 0.000 claims 3
- 239000005541 ACE inhibitor Substances 0.000 claims 2
- 241000024188 Andala Species 0.000 claims 2
- 102000008873 Angiotensin II receptor Human genes 0.000 claims 2
- 108050000824 Angiotensin II receptor Proteins 0.000 claims 2
- 101710129690 Angiotensin-converting enzyme inhibitor Proteins 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 2
- 101710086378 Bradykinin-potentiating and C-type natriuretic peptides Proteins 0.000 claims 2
- YNXLOPYTAAFMTN-SBUIBGKBSA-N C([C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(N)=O)C1=CC=C(O)C=C1 Chemical compound C([C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(N)=O)C1=CC=C(O)C=C1 YNXLOPYTAAFMTN-SBUIBGKBSA-N 0.000 claims 2
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 2
- 102100033868 Cannabinoid receptor 1 Human genes 0.000 claims 2
- 101710187010 Cannabinoid receptor 1 Proteins 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 2
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 2
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 2
- 229940097420 Diuretic Drugs 0.000 claims 2
- 208000012895 Gastric disease Diseases 0.000 claims 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 2
- 101000581402 Homo sapiens Melanin-concentrating hormone receptor 1 Proteins 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 208000031773 Insulin resistance syndrome Diseases 0.000 claims 2
- 229940086609 Lipase inhibitor Drugs 0.000 claims 2
- 102100027375 Melanin-concentrating hormone receptor 1 Human genes 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 2
- 108010088847 Peptide YY Proteins 0.000 claims 2
- 102100029909 Peptide YY Human genes 0.000 claims 2
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 2
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 2
- 208000001647 Renal Insufficiency Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 229940100389 Sulfonylurea Drugs 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 2
- 230000006907 apoptotic process Effects 0.000 claims 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 2
- 230000000923 atherogenic effect Effects 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 2
- 239000002876 beta blocker Substances 0.000 claims 2
- 229940097320 beta blocking agent Drugs 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 239000000480 calcium channel blocker Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000001906 cholesterol absorption Effects 0.000 claims 2
- 238000002648 combination therapy Methods 0.000 claims 2
- 208000012696 congenital leptin deficiency Diseases 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000002934 diuretic Substances 0.000 claims 2
- 230000001882 diuretic effect Effects 0.000 claims 2
- 229940125753 fibrate Drugs 0.000 claims 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 2
- 208000020694 gallbladder disease Diseases 0.000 claims 2
- -1 glitazones Substances 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 125000004857 imidazopyridinyl group Chemical class N1C(=NC2=C1C=CC=N2)* 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 239000004026 insulin derivative Substances 0.000 claims 2
- 201000006370 kidney failure Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 2
- 229960003105 metformin Drugs 0.000 claims 2
- 208000001022 morbid obesity Diseases 0.000 claims 2
- BPGXUIVWLQTVLZ-OFGSCBOVSA-N neuropeptide y(npy) Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=C(O)C=C1 BPGXUIVWLQTVLZ-OFGSCBOVSA-N 0.000 claims 2
- 229960003512 nicotinic acid Drugs 0.000 claims 2
- 235000001968 nicotinic acid Nutrition 0.000 claims 2
- 239000011664 nicotinic acid Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000035755 proliferation Effects 0.000 claims 2
- 230000001737 promoting effect Effects 0.000 claims 2
- 239000003087 receptor blocking agent Substances 0.000 claims 2
- 201000002859 sleep apnea Diseases 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 230000004083 survival effect Effects 0.000 claims 2
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 230000004584 weight gain Effects 0.000 claims 2
- 235000019786 weight gain Nutrition 0.000 claims 2
- 230000004580 weight loss Effects 0.000 claims 2
- DFZVZEMNPGABKO-ZETCQYMHSA-N (2s)-2-amino-3-pyridin-3-ylpropanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=CN=C1 DFZVZEMNPGABKO-ZETCQYMHSA-N 0.000 claims 1
- NKOHRVBBQISBSB-UHFFFAOYSA-N 5-[(4-hydroxyphenyl)methyl]-1,3-thiazolidine-2,4-dione Chemical compound C1=CC(O)=CC=C1CC1C(=O)NC(=O)S1 NKOHRVBBQISBSB-UHFFFAOYSA-N 0.000 claims 1
- 108010011459 Exenatide Proteins 0.000 claims 1
- 102400000921 Gastrin Human genes 0.000 claims 1
- 102400000922 Gastrin-6 Human genes 0.000 claims 1
- 101800002467 Gastrin-6 Proteins 0.000 claims 1
- 102400000322 Glucagon-like peptide 1 Human genes 0.000 claims 1
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 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(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 1
- 101800000224 Glucagon-like peptide 1 Proteins 0.000 claims 1
- 241000270431 Heloderma suspectum Species 0.000 claims 1
- 101001002317 Homo sapiens Gastrin Proteins 0.000 claims 1
- 102100023724 Melanocortin receptor 4 Human genes 0.000 claims 1
- 108010008364 Melanocortins Proteins 0.000 claims 1
- 108010021436 Type 4 Melanocortin Receptor Proteins 0.000 claims 1
- JUFFVKRROAPVBI-PVOYSMBESA-N chembl1210015 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N[C@H]1[C@@H]([C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@]3(O[C@@H](C[C@H](O)[C@H](O)CO)[C@H](NC(C)=O)[C@@H](O)C3)C(O)=O)O2)O)[C@@H](CO)O1)NC(C)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](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](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)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)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 JUFFVKRROAPVBI-PVOYSMBESA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960001519 exenatide Drugs 0.000 claims 1
- 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 1
- 239000003877 glucagon like peptide 1 receptor agonist Substances 0.000 claims 1
- 239000002865 melanocortin Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000005022 packaging material Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 238000010188 recombinant method Methods 0.000 claims 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 1
- 238000001308 synthesis method Methods 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161555435P | 2011-11-03 | 2011-11-03 | |
| US61/555,435 | 2011-11-03 | ||
| PCT/EP2012/071766 WO2013064669A1 (en) | 2011-11-03 | 2012-11-02 | Glp-1 receptor agonist peptide gastrin conjugates |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015502918A JP2015502918A (ja) | 2015-01-29 |
| JP2015502918A5 true JP2015502918A5 (enExample) | 2015-12-24 |
| JP6359972B2 JP6359972B2 (ja) | 2018-07-18 |
Family
ID=47146385
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014539352A Active JP6359972B2 (ja) | 2011-11-03 | 2012-11-02 | Ｇｌｐ−１受容体アゴニストペプチドガストリンコンジュゲート |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9259477B2 (enExample) |
| EP (1) | EP2773377B1 (enExample) |
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| TW201326194A (zh) | 2011-11-03 | 2013-07-01 | Zealand Pharma As | Ｇｌｐ－１胃泌素受體促效劑肽結合物 |
| WO2015067715A2 (en) | 2013-11-06 | 2015-05-14 | Zealand Pharma A/S | Gip-glp-1 dual agonist compounds and methods |
| CN105829339B (zh) | 2013-11-06 | 2021-03-12 | 西兰制药公司 | 胰高血糖素-glp-1-gip三重激动剂化合物 |
| KR102620911B1 (ko) | 2014-10-29 | 2024-01-05 | 질랜드 파마 에이/에스 | Gip 효능제 화합물 및 방법 |
| WO2016168388A2 (en) | 2015-04-14 | 2016-10-20 | Palatin Technologies, Inc. | Therapies for obesity, diabetes and related indications |
| EP3426678B1 (en) * | 2016-03-10 | 2025-07-02 | Shenzhen Hightide Biopharmaceutical, Ltd. | Conjugates of islet neogenesis peptides and analogs, and methods thereof |
| EP3551651B1 (en) | 2016-12-09 | 2024-03-06 | Zealand Pharma A/S | Acylated glp-1/glp-2 dual agonists |
| SG11201912433YA (en) * | 2017-06-29 | 2020-01-30 | Ureka Sarl | Pro-drug peptide with improved pharmaceutical properties |
| CN109248323B (zh) * | 2017-07-14 | 2023-09-08 | 杭州先为达生物科技有限公司 | 酰化的glp-1衍生物 |
| CN109331173B (zh) * | 2018-12-17 | 2021-05-07 | 中国医学科学院医学实验动物研究所 | 胃泌素-二氧化硅微球及其用途 |
| 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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2012
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- 2012-11-02 EA EA201490790A patent/EA028951B9/ru not_active IP Right Cessation
- 2012-11-02 CN CN201280060332.8A patent/CN104144704B/zh active Active
- 2012-11-02 US US14/355,906 patent/US9259477B2/en active Active
- 2012-11-02 BR BR112014010780A patent/BR112014010780A2/pt not_active Application Discontinuation
- 2012-11-02 MX MX2014005351A patent/MX2014005351A/es unknown
- 2012-11-02 EP EP12783582.5A patent/EP2773377B1/en active Active
- 2012-11-02 AR ARP120104123A patent/AR088636A1/es unknown
- 2012-11-02 JP JP2014539352A patent/JP6359972B2/ja active Active
- 2012-11-02 CA CA2853884A patent/CA2853884A1/en not_active Abandoned
- 2012-11-02 KR KR1020147015223A patent/KR20140100947A/ko not_active Withdrawn
- 2012-11-02 AU AU2012331053A patent/AU2012331053A1/en not_active Abandoned
- 2012-11-02 WO PCT/EP2012/071766 patent/WO2013064669A1/en not_active Ceased
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2015
- 2015-09-24 US US14/864,540 patent/US9861706B2/en active Active
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