JP2016531156A5 - - Google Patents
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- Publication number
- JP2016531156A5 JP2016531156A5 JP2016542823A JP2016542823A JP2016531156A5 JP 2016531156 A5 JP2016531156 A5 JP 2016531156A5 JP 2016542823 A JP2016542823 A JP 2016542823A JP 2016542823 A JP2016542823 A JP 2016542823A JP 2016531156 A5 JP2016531156 A5 JP 2016531156A5
- Authority
- JP
- Japan
- Prior art keywords
- therapeutic agent
- peptide
- group
- amino acid
- relaxin
- 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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- 239000003814 drug Substances 0.000 claims 55
- 229940124597 therapeutic agent Drugs 0.000 claims 55
- 108090000765 processed proteins & peptides Proteins 0.000 claims 23
- 108090000103 Relaxin Proteins 0.000 claims 17
- 102000003743 Relaxin Human genes 0.000 claims 17
- 125000003275 alpha amino acid group Chemical group 0.000 claims 14
- 150000002632 lipids Chemical class 0.000 claims 11
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 10
- 235000001014 amino acid Nutrition 0.000 claims 9
- 150000001413 amino acids Chemical class 0.000 claims 8
- -1 fatty diacids Chemical class 0.000 claims 7
- 238000006467 substitution reaction Methods 0.000 claims 7
- 230000006229 amino acid addition Effects 0.000 claims 5
- 229920000151 polyglycol Polymers 0.000 claims 5
- 239000010695 polyglycol Substances 0.000 claims 5
- 208000002193 Pain Diseases 0.000 claims 4
- MBMBGCFOFBJSGT-KUBAVDMBSA-N all-cis-docosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 claims 4
- 238000012217 deletion Methods 0.000 claims 4
- 230000037430 deletion Effects 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 claims 4
- BNJOQKFENDDGSC-UHFFFAOYSA-N octadecanedioic acid Chemical compound OC(=O)CCCCCCCCCCCCCCCCC(O)=O BNJOQKFENDDGSC-UHFFFAOYSA-N 0.000 claims 4
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 3
- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 claims 3
- 229930182558 Sterol Natural products 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000003827 glycol group Chemical group 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 229920001223 polyethylene glycol Polymers 0.000 claims 3
- 150000003432 sterols Chemical class 0.000 claims 3
- 235000003702 sterols Nutrition 0.000 claims 3
- BHQCQFFYRZLCQQ-UHFFFAOYSA-N (3alpha,5alpha,7alpha,12alpha)-3,7,12-trihydroxy-cholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 BHQCQFFYRZLCQQ-UHFFFAOYSA-N 0.000 claims 2
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims 2
- 239000005541 ACE inhibitor Substances 0.000 claims 2
- 102000008873 Angiotensin II receptor Human genes 0.000 claims 2
- 108050000824 Angiotensin II receptor Proteins 0.000 claims 2
- 206010007556 Cardiac failure acute Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 239000004380 Cholic acid Substances 0.000 claims 2
- 108010011459 Exenatide Proteins 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 102100039997 Gastric inhibitory polypeptide receptor Human genes 0.000 claims 2
- 102400000321 Glucagon Human genes 0.000 claims 2
- 108060003199 Glucagon Proteins 0.000 claims 2
- 102100040890 Glucagon receptor Human genes 0.000 claims 2
- 102400000326 Glucagon-like peptide 2 Human genes 0.000 claims 2
- 101800000221 Glucagon-like peptide 2 Proteins 0.000 claims 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 2
- 101000886866 Homo sapiens Gastric inhibitory polypeptide receptor Proteins 0.000 claims 2
- 101001040075 Homo sapiens Glucagon receptor Proteins 0.000 claims 2
- 101000668058 Infectious salmon anemia virus (isolate Atlantic salmon/Norway/810/9/99) RNA-directed RNA polymerase catalytic subunit Proteins 0.000 claims 2
- 206010065390 Inflammatory pain Diseases 0.000 claims 2
- SMEROWZSTRWXGI-UHFFFAOYSA-N Lithocholsaeure Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)CC2 SMEROWZSTRWXGI-UHFFFAOYSA-N 0.000 claims 2
- 235000021314 Palmitic acid Nutrition 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 235000021355 Stearic acid Nutrition 0.000 claims 2
- PLZVEHJLHYMBBY-UHFFFAOYSA-N Tetradecylamine Chemical compound CCCCCCCCCCCCCCN PLZVEHJLHYMBBY-UHFFFAOYSA-N 0.000 claims 2
- 238000007792 addition Methods 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 150000008431 aliphatic amides Chemical class 0.000 claims 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 2
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 239000002876 beta blocker Substances 0.000 claims 2
- 229940097320 beta blocking agent Drugs 0.000 claims 2
- 239000003613 bile acid Substances 0.000 claims 2
- BHQCQFFYRZLCQQ-OELDTZBJSA-N cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 claims 2
- 229960002471 cholic acid Drugs 0.000 claims 2
- 235000019416 cholic acid Nutrition 0.000 claims 2
- KXGVEGMKQFWNSR-UHFFFAOYSA-N deoxycholic acid Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 KXGVEGMKQFWNSR-UHFFFAOYSA-N 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- 239000002934 diuretic Substances 0.000 claims 2
- 229940030606 diuretics Drugs 0.000 claims 2
- 229940090949 docosahexaenoic acid Drugs 0.000 claims 2
- 235000020669 docosahexaenoic acid Nutrition 0.000 claims 2
- 229940125542 dual agonist Drugs 0.000 claims 2
- 230000009977 dual effect Effects 0.000 claims 2
- 229960001519 exenatide Drugs 0.000 claims 2
- 229930195729 fatty acid Natural products 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 150000004665 fatty acids Chemical class 0.000 claims 2
- 150000002191 fatty alcohols Chemical class 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 2
- 229960004666 glucagon Drugs 0.000 claims 2
- TWSALRJGPBVBQU-PKQQPRCHSA-N glucagon-like peptide 2 Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CC(N)=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]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(O)=O)[C@@H](C)CC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=CC=C1 TWSALRJGPBVBQU-PKQQPRCHSA-N 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 claims 2
- 208000004296 neuralgia Diseases 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229920001184 polypeptide Polymers 0.000 claims 2
- 102000004196 processed proteins & peptides Human genes 0.000 claims 2
- 239000008117 stearic acid Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 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
- 108700041144 Angiopoietin-Like Protein 8 Proteins 0.000 claims 1
- 102100034604 Angiopoietin-like protein 8 Human genes 0.000 claims 1
- 102100025668 Angiopoietin-related protein 3 Human genes 0.000 claims 1
- HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide 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(N)=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 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 claims 1
- 102000003973 Fibroblast growth factor 21 Human genes 0.000 claims 1
- 108090000376 Fibroblast growth factor 21 Proteins 0.000 claims 1
- 102100034120 Golgin subfamily A member 6A Human genes 0.000 claims 1
- 102100040898 Growth/differentiation factor 11 Human genes 0.000 claims 1
- 108091016366 Histone-lysine N-methyltransferase EHMT1 Proteins 0.000 claims 1
- 101000693085 Homo sapiens Angiopoietin-related protein 3 Proteins 0.000 claims 1
- 101000998777 Homo sapiens Early placenta insulin-like peptide Proteins 0.000 claims 1
- 101000893545 Homo sapiens Growth/differentiation factor 11 Proteins 0.000 claims 1
- 101100397008 Homo sapiens INSL3 gene Proteins 0.000 claims 1
- 101000976075 Homo sapiens Insulin Proteins 0.000 claims 1
- 101000599951 Homo sapiens Insulin-like growth factor I Proteins 0.000 claims 1
- 101000998810 Homo sapiens Insulin-like peptide INSL6 Proteins 0.000 claims 1
- 108700012441 IGF2 Proteins 0.000 claims 1
- 108010092277 Leptin Proteins 0.000 claims 1
- 102000016267 Leptin Human genes 0.000 claims 1
- 108700014400 Leydig insulin-like Proteins 0.000 claims 1
- TUNFSRHWOTWDNC-UHFFFAOYSA-N Myristic acid Natural products CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 claims 1
- 102400000319 Oxyntomodulin Human genes 0.000 claims 1
- 101800001388 Oxyntomodulin Proteins 0.000 claims 1
- 229930003427 Vitamin E Natural products 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
- 125000003636 chemical group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 102000044162 human IGF1 Human genes 0.000 claims 1
- 102000055043 human INSL4 Human genes 0.000 claims 1
- 102000050306 human INSL6 Human genes 0.000 claims 1
- PBGKTOXHQIOBKM-FHFVDXKLSA-N insulin (human) Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=3C=CC(O)=CC=3)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3C=CC(O)=CC=3)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=3NC=NC=3)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(=O)N[C@@H](CC(N)=O)C(O)=O)=O)CSSC[C@@H](C(N2)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC=1C=CC=CC=1)C(C)C)C1=CN=CN1 PBGKTOXHQIOBKM-FHFVDXKLSA-N 0.000 claims 1
- NRYBAZVQPHGZNS-ZSOCWYAHSA-N leptin Chemical compound O=C([C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(C)C)CCSC)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CS)C(O)=O NRYBAZVQPHGZNS-ZSOCWYAHSA-N 0.000 claims 1
- 229940039781 leptin Drugs 0.000 claims 1
- PXZWGQLGAKCNKD-DPNMSELWSA-N molport-023-276-326 Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 PXZWGQLGAKCNKD-DPNMSELWSA-N 0.000 claims 1
- 229920001748 polybutylene Polymers 0.000 claims 1
- 229920001451 polypropylene glycol Polymers 0.000 claims 1
- 108010087851 prorelaxin Proteins 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 108700012359 toxins Proteins 0.000 claims 1
- 235000019165 vitamin E Nutrition 0.000 claims 1
- 229940046009 vitamin E Drugs 0.000 claims 1
- 239000011709 vitamin E Substances 0.000 claims 1
- 150000003712 vitamin E derivatives Chemical class 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361877799P | 2013-09-13 | 2013-09-13 | |
| US61/877,799 | 2013-09-13 | ||
| US201361917816P | 2013-12-18 | 2013-12-18 | |
| US61/917,816 | 2013-12-18 | ||
| PCT/US2014/055457 WO2015038938A1 (en) | 2013-09-13 | 2014-09-12 | Modified therapeutic agents and compositions thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
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| CN104039342A (zh) | 2011-10-18 | 2014-09-10 | 爱勒让治疗公司 | 拟肽大环化合物 |
| HK1205454A1 (en) | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| CN104302408B (zh) * | 2012-02-27 | 2016-12-14 | 阿穆尼克斯运营公司 | Xten缀合组合物和制造其的方法 |
| US9273093B2 (en) | 2012-10-11 | 2016-03-01 | Protagonist Therapeutics, Inc. | α4β7 peptide dimer antagonists |
| SG11201503052RA (en) | 2012-11-01 | 2015-05-28 | Aileron Therapeutics Inc | Disubstituted amino acids and methods of preparation and use thereof |
| US10286078B2 (en) * | 2013-09-13 | 2019-05-14 | The California Institute For Biomedical Research | Modified therapeutic agents and compositions thereof |
| CA2933701C (en) | 2013-12-18 | 2022-05-31 | The California Institute For Biomedical Research | Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof |
| MA41794A (fr) | 2015-03-18 | 2018-01-23 | The California Institute For Biomedical Res | Agents thérapeutiques modifiés et compositions associées |
-
2014
- 2014-09-12 US US14/917,689 patent/US10286078B2/en active Active
- 2014-09-12 JP JP2016542823A patent/JP6822839B2/ja active Active
- 2014-09-12 KR KR1020167009482A patent/KR102302634B1/ko active Active
- 2014-09-12 WO PCT/US2014/055457 patent/WO2015038938A1/en not_active Ceased
- 2014-09-12 CN CN201480062386.7A patent/CN105792851B/zh active Active
- 2014-09-12 CA CA2924109A patent/CA2924109A1/en not_active Abandoned
- 2014-09-12 ES ES14843357T patent/ES2927607T3/es active Active
- 2014-09-12 EP EP14843357.6A patent/EP3043824B1/en active Active
- 2014-09-12 AU AU2014318579A patent/AU2014318579A1/en not_active Abandoned
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2019
- 2019-05-07 US US16/405,594 patent/US10987427B2/en active Active
- 2019-10-30 JP JP2019197971A patent/JP2020063249A/ja active Pending
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