JP2016514102A5 - - Google Patents

Info

Publication number

JP2016514102A5

JP2016514102A5 JP2015559276A JP2015559276A JP2016514102A5 JP 2016514102 A5 JP2016514102 A5 JP 2016514102A5 JP 2015559276 A JP2015559276 A JP 2015559276A JP 2015559276 A JP2015559276 A JP 2015559276A JP 2016514102 A5 JP2016514102 A5 JP 2016514102A5

Authority

JP

Japan

Prior art keywords

composition

peptide

seq

effective amount

gcra

Prior art date

2014-02-25

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

• Espacenet
• Global Dossier
• Discuss

• 239000000203 mixture Substances 0.000 claims description 29
• 108090000765 processed proteins & peptides Proteins 0.000 claims description 26
• 239000008141 laxative Substances 0.000 claims description 8
• 230000002475 laxative effect Effects 0.000 claims description 8
• 230000000112 colonic effect Effects 0.000 claims description 7
• 238000009472 formulation Methods 0.000 claims description 7
• 230000003204 osmotic effect Effects 0.000 claims description 6
• 210000001072 colon Anatomy 0.000 claims description 5
• ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 claims description 4
• WQZGKKKJIJFFOK-ZZWDRFIYSA-N L-glucose Chemical compound OC[C@@H]1OC(O)[C@@H](O)[C@H](O)[C@H]1O WQZGKKKJIJFFOK-ZZWDRFIYSA-N 0.000 claims description 4
• 229940099471 Phosphodiesterase inhibitor Drugs 0.000 claims description 4
• 239000002702 enteric coating Substances 0.000 claims description 4
• 238000009505 enteric coating Methods 0.000 claims description 4
• WGFOBBZOWHGYQH-MXHNKVEKSA-N lubiprostone Chemical compound O1[C@](C(F)(F)CCCC)(O)CC[C@@H]2[C@@H](CCCCCCC(O)=O)C(=O)C[C@H]21 WGFOBBZOWHGYQH-MXHNKVEKSA-N 0.000 claims description 4
• 239000002571 phosphodiesterase inhibitor Substances 0.000 claims description 4
• BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 claims description 4
• 238000002360 preparation method Methods 0.000 claims description 3
• NPFVRBCDMFKOPY-UHFFFAOYSA-N 3-(4-imidazol-1-ylthiophen-2-yl)-4-methyl-4,5-dihydro-1h-pyridazin-6-one Chemical compound CC1CC(=O)NN=C1C1=CC(N2C=NC=C2)=CS1 NPFVRBCDMFKOPY-UHFFFAOYSA-N 0.000 claims description 2
• GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 2
• 206010010774 Constipation Diseases 0.000 claims description 2
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 2
• 241000588724 Escherichia coli Species 0.000 claims description 2
• 108010078321 Guanylate Cyclase Proteins 0.000 claims description 2
• 102000014469 Guanylate cyclase Human genes 0.000 claims description 2
• GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
• 229930195725 Mannitol Natural products 0.000 claims description 2
• 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 2
• 229910019142 PO4 Inorganic materials 0.000 claims description 2
• 229920002472 Starch Polymers 0.000 claims description 2
• SECKRCOLJRRGGV-UHFFFAOYSA-N Vardenafil Chemical compound CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 SECKRCOLJRRGGV-UHFFFAOYSA-N 0.000 claims description 2
• 229940040386 amitiza Drugs 0.000 claims description 2
• 125000002619 bicyclic group Chemical group 0.000 claims description 2
• 230000001684 chronic effect Effects 0.000 claims description 2
• 239000003814 drug Substances 0.000 claims description 2
• 239000008101 lactose Substances 0.000 claims description 2
• 108010024409 linaclotide Proteins 0.000 claims description 2
• KXGCNMMJRFDFNR-WDRJZQOASA-N linaclotide Chemical compound C([C@H](NC(=O)[C@@H]1CSSC[C@H]2C(=O)N[C@H]3CSSC[C@H](N)C(=O)N[C@H](C(N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=4C=CC(O)=CC=4)C(=O)N2)=O)CSSC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(N)=O)NC3=O)C(=O)N[C@H](C(NCC(=O)N1)=O)[C@H](O)C)C(O)=O)C1=CC=C(O)C=C1 KXGCNMMJRFDFNR-WDRJZQOASA-N 0.000 claims description 2
• 229960000812 linaclotide Drugs 0.000 claims description 2
• 229960000345 lubiprostone Drugs 0.000 claims description 2
• 229960005336 magnesium citrate Drugs 0.000 claims description 2
• 235000002538 magnesium citrate Nutrition 0.000 claims description 2
• 239000004337 magnesium citrate Substances 0.000 claims description 2
• 239000000594 mannitol Substances 0.000 claims description 2
• 235000010355 mannitol Nutrition 0.000 claims description 2
• 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 2
• 239000008108 microcrystalline cellulose Substances 0.000 claims description 2
• 229940016286 microcrystalline cellulose Drugs 0.000 claims description 2
• 229950002910 motapizone Drugs 0.000 claims description 2
• NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
• 239000010452 phosphate Substances 0.000 claims description 2
• 239000000018 receptor agonist Substances 0.000 claims description 2
• 229940044601 receptor agonist Drugs 0.000 claims description 2
• 229960003310 sildenafil Drugs 0.000 claims description 2
• 235000019698 starch Nutrition 0.000 claims description 2
• 239000008107 starch Substances 0.000 claims description 2
• MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical group CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 claims description 2
• 229940124597 therapeutic agent Drugs 0.000 claims description 2
• PLSARIKBYIPYPF-UHFFFAOYSA-H trimagnesium dicitrate Chemical group [Mg+2].[Mg+2].[Mg+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O PLSARIKBYIPYPF-UHFFFAOYSA-H 0.000 claims description 2
• 229960002381 vardenafil Drugs 0.000 claims description 2
• REZGGXNDEMKIQB-UHFFFAOYSA-N zaprinast Chemical compound CCCOC1=CC=CC=C1C1=NC(=O)C2=NNNC2=N1 REZGGXNDEMKIQB-UHFFFAOYSA-N 0.000 claims description 2
• 229950005371 zaprinast Drugs 0.000 claims description 2
• 238000000034 method Methods 0.000 description 12