JP2010540648A5 - - Google Patents

Info

Publication number

JP2010540648A5

JP2010540648A5 JP2010528062A JP2010528062A JP2010540648A5 JP 2010540648 A5 JP2010540648 A5 JP 2010540648A5 JP 2010528062 A JP2010528062 A JP 2010528062A JP 2010528062 A JP2010528062 A JP 2010528062A JP 2010540648 A5 JP2010540648 A5 JP 2010540648A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

composition according

opioid antagonist

constipation

gastrointestinal

Prior art date

2008-09-30

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

• 239000008194 pharmaceutical composition Substances 0.000 claims 38
• 239000003401 opiate antagonist Substances 0.000 claims 16
• 206010010774 Constipation Diseases 0.000 claims 8
• 230000000694 effects Effects 0.000 claims 7
• 230000002496 gastric effect Effects 0.000 claims 6
• 206010028813 Nausea Diseases 0.000 claims 5
• -1 morphinan compound Chemical class 0.000 claims 5
• 230000008693 nausea Effects 0.000 claims 5
• 208000018522 Gastrointestinal disease Diseases 0.000 claims 4
• 206010047700 Vomiting Diseases 0.000 claims 4
• 230000002093 peripheral effect Effects 0.000 claims 4
• 230000008673 vomiting Effects 0.000 claims 4
• JVLBPIPGETUEET-WIXLDOGYSA-O (3r,4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-3-ium-7-one Chemical group C([N@+]1(C)[C@@H]2CC=3C4=C(C(=CC=3)O)O[C@@H]3[C@]4([C@@]2(O)CCC3=O)CC1)C1CC1 JVLBPIPGETUEET-WIXLDOGYSA-O 0.000 claims 3
• 230000037396 body weight Effects 0.000 claims 3
• 239000003467 chloride channel stimulating agent Substances 0.000 claims 3
• 208000002551 irritable bowel syndrome Diseases 0.000 claims 3
• 230000011987 methylation Effects 0.000 claims 3
• 238000007069 methylation reaction Methods 0.000 claims 3
• JVLBPIPGETUEET-GAAHOAFPSA-O methylnaltrexone Chemical compound C[N+]1([C@@H]2CC=3C4=C(C(=CC=3)O)O[C@@H]3[C@]4([C@@]2(O)CCC3=O)CC1)CC1CC1 JVLBPIPGETUEET-GAAHOAFPSA-O 0.000 claims 3
• 229960002921 methylnaltrexone Drugs 0.000 claims 3
• DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 claims 3
• 229960003086 naltrexone Drugs 0.000 claims 3
• 150000003839 salts Chemical group 0.000 claims 3
• PCSQOABIHJXZMR-MGQKVWQSSA-O (4r,4as,7ar,12bs)-4a,9-dihydroxy-3-methyl-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-3-ium-7-one Chemical compound O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CC[N+](C)(CC=C)[C@@H]3CC5=CC=C4O PCSQOABIHJXZMR-MGQKVWQSSA-O 0.000 claims 2
• HJDWPCLBBHHTIG-NNJWZEOZSA-O (4r,7s,7ar,12bs)-3-methyl-3-prop-2-enyl-2,4,4a,7,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-3-ium-7,9-diol Chemical compound O([C@H]1[C@H](C=CC23)O)C4=C5[C@@]12CC[N+](C)(CC=C)[C@@H]3CC5=CC=C4O HJDWPCLBBHHTIG-NNJWZEOZSA-O 0.000 claims 2
• 208000004998 Abdominal Pain Diseases 0.000 claims 2
• 206010000060 Abdominal distension Diseases 0.000 claims 2
• 206010012735 Diarrhoea Diseases 0.000 claims 2
• 208000030053 Opioid-Induced Constipation Diseases 0.000 claims 2
• 150000001875 compounds Chemical class 0.000 claims 2
• 201000006549 dyspepsia Diseases 0.000 claims 2
• 239000003112 inhibitor Substances 0.000 claims 2
• 239000002618 kappa opiate receptor antagonist Substances 0.000 claims 2
• 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 2
• 229960000345 lubiprostone Drugs 0.000 claims 2
• 239000002623 mu opiate receptor antagonist Substances 0.000 claims 2
• VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
• 208000014540 Functional gastrointestinal disease Diseases 0.000 claims 1
• 208000017228 Gastrointestinal motility disease Diseases 0.000 claims 1
• 108090000862 Ion Channels Proteins 0.000 claims 1
• 102000004310 Ion Channels Human genes 0.000 claims 1
• 206010054048 Postoperative ileus Diseases 0.000 claims 1
• 239000012190 activator Substances 0.000 claims 1
• 230000002411 adverse Effects 0.000 claims 1
• 230000001684 chronic effect Effects 0.000 claims 1
• 208000014797 chronic intestinal pseudoobstruction Diseases 0.000 claims 1
• 210000001072 colon Anatomy 0.000 claims 1
• 208000010643 digestive system disease Diseases 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 230000002183 duodenal effect Effects 0.000 claims 1
• 208000021302 gastroesophageal reflux disease Diseases 0.000 claims 1
• 208000018685 gastrointestinal system disease Diseases 0.000 claims 1
• 208000024798 heartburn Diseases 0.000 claims 1
• 238000007918 intramuscular administration Methods 0.000 claims 1
• 238000001990 intravenous administration Methods 0.000 claims 1
• UZHSEJADLWPNLE-GRGSLBFTSA-N naloxone Chemical group O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(O)C2=C5[C@@]13CCN4CC=C UZHSEJADLWPNLE-GRGSLBFTSA-N 0.000 claims 1
• 229960004127 naloxone Drugs 0.000 claims 1
• 230000003405 preventing effect Effects 0.000 claims 1
• 238000010992 reflux Methods 0.000 claims 1
• 238000007920 subcutaneous administration Methods 0.000 claims 1