JP2021138740A5 - - Google Patents

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Publication number

JP2021138740A5

JP2021138740A5 JP2021096014A JP2021096014A JP2021138740A5 JP 2021138740 A5 JP2021138740 A5 JP 2021138740A5 JP 2021096014 A JP2021096014 A JP 2021096014A JP 2021096014 A JP2021096014 A JP 2021096014A JP 2021138740 A5 JP2021138740 A5 JP 2021138740A5

Authority

JP

Japan

Prior art keywords

peg3

aib

carboxy

egtfisdysieldk

pharmaceutically acceptable

Prior art date

2021-06-08

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

Links

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• 150000003839 salts Chemical class 0.000 claims 23
• 239000012453 solvate Substances 0.000 claims 23
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
• 208000035475 disorder Diseases 0.000 claims 9
• 101100505076 Caenorhabditis elegans gly-2 gene Proteins 0.000 claims 8
• YMAWOPBAYDPSLA-UHFFFAOYSA-N glycylglycine Chemical compound [NH3+]CC(=O)NCC([O-])=O YMAWOPBAYDPSLA-UHFFFAOYSA-N 0.000 claims 8
• 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 7
• 208000008589 Obesity Diseases 0.000 claims 6
• 239000008280 blood Substances 0.000 claims 6
• 210000004369 blood Anatomy 0.000 claims 6
• 235000020824 obesity Nutrition 0.000 claims 6
• 206010020772 Hypertension Diseases 0.000 claims 5
• 206010012601 diabetes mellitus Diseases 0.000 claims 5
• -1 17-carboxy-Heptadecanoyl Chemical group 0.000 claims 4
• 125000002947 alkylene group Chemical group 0.000 claims 4
• 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 4
• 150000002632 lipids Chemical class 0.000 claims 4
• 125000004432 carbon atom Chemical group C* 0.000 claims 3
• 239000008194 pharmaceutical composition Substances 0.000 claims 3
• 229920006395 saturated elastomer Polymers 0.000 claims 3
• 125000001424 substituent group Chemical group 0.000 claims 3
• 201000001320 Atherosclerosis Diseases 0.000 claims 2
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
• ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical compound OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 2
• 125000002252 acyl group Chemical group 0.000 claims 2
• 230000036772 blood pressure Effects 0.000 claims 2
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
• 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 2
• 238000002648 combination therapy Methods 0.000 claims 2
• 230000001631 hypertensive effect Effects 0.000 claims 2
• 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 2
• 208000030159 metabolic disease Diseases 0.000 claims 2
• 201000009104 prediabetes syndrome Diseases 0.000 claims 2
• 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 2
• 125000000542 sulfonic acid group Chemical group 0.000 claims 2
• 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
• 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
• ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical compound OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 claims 1
• 206010003210 Arteriosclerosis Diseases 0.000 claims 1
• 208000010392 Bone Fractures Diseases 0.000 claims 1
• 108010074051 C-Reactive Protein Proteins 0.000 claims 1
• 102100032752 C-reactive protein Human genes 0.000 claims 1
• QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 claims 1
• MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
• 208000032928 Dyslipidaemia Diseases 0.000 claims 1
• 108010049003 Fibrinogen Proteins 0.000 claims 1
• 102000008946 Fibrinogen Human genes 0.000 claims 1
• 206010017076 Fracture Diseases 0.000 claims 1
• 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 1
• 208000002705 Glucose Intolerance Diseases 0.000 claims 1
• 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
• 208000013016 Hypoglycemia Diseases 0.000 claims 1
• 206010061218 Inflammation Diseases 0.000 claims 1
• 102000004877 Insulin Human genes 0.000 claims 1
• 108090001061 Insulin Proteins 0.000 claims 1
• 206010022489 Insulin Resistance Diseases 0.000 claims 1
• 238000008214 LDL Cholesterol Methods 0.000 claims 1
• 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
• HGNRJCINZYHNOU-LURJTMIESA-N Lys-Gly Chemical group NCCCC[C@H](N)C(=O)NCC(O)=O HGNRJCINZYHNOU-LURJTMIESA-N 0.000 claims 1
• 208000001132 Osteoporosis Diseases 0.000 claims 1
• 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 1
• 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
• 108010022233 Plasminogen Activator Inhibitor 1 Proteins 0.000 claims 1
• 102100039418 Plasminogen activator inhibitor 1 Human genes 0.000 claims 1
• 208000001280 Prediabetic State Diseases 0.000 claims 1
• MKGIILKDUGDRRO-FXQIFTODSA-N Pro-Ser-Ser Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1 MKGIILKDUGDRRO-FXQIFTODSA-N 0.000 claims 1
• 208000006011 Stroke Diseases 0.000 claims 1
• 208000007536 Thrombosis Diseases 0.000 claims 1
• 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
• 239000003472 antidiabetic agent Substances 0.000 claims 1
• 229940125708 antidiabetic agent Drugs 0.000 claims 1
• 125000001124 arachidoyl 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])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
• 230000003143 atherosclerotic effect Effects 0.000 claims 1
• 235000012000 cholesterol Nutrition 0.000 claims 1
• 238000013270 controlled release Methods 0.000 claims 1
• 208000029078 coronary artery disease Diseases 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 230000004064 dysfunction Effects 0.000 claims 1
• 229940012952 fibrinogen Drugs 0.000 claims 1
• 208000004104 gestational diabetes Diseases 0.000 claims 1
• 239000003877 glucagon like peptide 1 receptor agonist Substances 0.000 claims 1
• 239000008103 glucose Substances 0.000 claims 1
• 229910052739 hydrogen Inorganic materials 0.000 claims 1
• 239000001257 hydrogen Substances 0.000 claims 1
• 206010020718 hyperplasia Diseases 0.000 claims 1
• 230000002390 hyperplastic effect Effects 0.000 claims 1
• 230000002218 hypoglycaemic effect Effects 0.000 claims 1
• 230000004054 inflammatory process Effects 0.000 claims 1
• 238000001802 infusion Methods 0.000 claims 1
• 238000002347 injection Methods 0.000 claims 1
• 239000007924 injection Substances 0.000 claims 1
• 229940125396 insulin Drugs 0.000 claims 1
• 125000005647 linker group Chemical group 0.000 claims 1
• 239000007788 liquid Substances 0.000 claims 1
• 108010064235 lysylglycine Proteins 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 229910052757 nitrogen Inorganic materials 0.000 claims 1
• 229910052760 oxygen Inorganic materials 0.000 claims 1
• 239000001301 oxygen Substances 0.000 claims 1
• 230000007406 plaque accumulation Effects 0.000 claims 1
• 201000002859 sleep apnea Diseases 0.000 claims 1
• 125000006850 spacer group Chemical group 0.000 claims 1
• 125000003696 stearoyl 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])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 229910052717 sulfur Inorganic materials 0.000 claims 1
• 125000004434 sulfur atom Chemical group 0.000 claims 1
• UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 1