JP2011502113A5 - - Google Patents

Info

Publication number

JP2011502113A5

JP2011502113A5 JP2010530588A JP2010530588A JP2011502113A5 JP 2011502113 A5 JP2011502113 A5 JP 2011502113A5 JP 2010530588 A JP2010530588 A JP 2010530588A JP 2010530588 A JP2010530588 A JP 2010530588A JP 2011502113 A5 JP2011502113 A5 JP 2011502113A5

Authority

JP

Japan

Prior art keywords

compound

group

administering

animal

human

Prior art date

2008-10-30

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
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• 150000001875 compounds Chemical class 0.000 claims 39
• 238000000034 method Methods 0.000 claims 17
• 241001465754 Metazoa Species 0.000 claims 9
• 239000008194 pharmaceutical composition Substances 0.000 claims 9
• 230000002265 prevention Effects 0.000 claims 7
• 125000003545 alkoxy group Chemical group 0.000 claims 5
• 125000000217 alkyl group Chemical group 0.000 claims 4
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
• 125000006701 (C1-C7) alkyl group Chemical group 0.000 claims 3
• PNLQMIOPVBCLRV-UHFFFAOYSA-N 2-ethyldocosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CCC=CCC=CCC=CCC=CCC=CCC=CCC(CC)C(O)=O PNLQMIOPVBCLRV-UHFFFAOYSA-N 0.000 claims 3
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
• 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 3
• CTKINSOISVBQLD-UHFFFAOYSA-N Glycidol Chemical compound OCC1CO1 CTKINSOISVBQLD-UHFFFAOYSA-N 0.000 claims 2
• 206010022489 Insulin Resistance Diseases 0.000 claims 2
• 208000008589 Obesity Diseases 0.000 claims 2
• 206010033307 Overweight Diseases 0.000 claims 2
• JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
• 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 2
• 239000003153 chemical reaction reagent Substances 0.000 claims 2
• 230000008878 coupling Effects 0.000 claims 2
• 238000010168 coupling process Methods 0.000 claims 2
• 238000005859 coupling reaction Methods 0.000 claims 2
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
• 208000006575 hypertriglyceridemia Diseases 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
• -1 methoxy, ethoxy, propoxy, isopropoxy, sec- butoxy, phenoxy, benzyloxy Chemical group 0.000 claims 2
• 235000020824 obesity Nutrition 0.000 claims 2
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
• QAEDZJGFFMLHHQ-UHFFFAOYSA-N trifluoroacetic anhydride Chemical compound FC(F)(F)C(=O)OC(=O)C(F)(F)F QAEDZJGFFMLHHQ-UHFFFAOYSA-N 0.000 claims 2
• 206010014486 Elevated triglycerides 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
• 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
• 102000004877 Insulin Human genes 0.000 claims 1
• 108090001061 Insulin Proteins 0.000 claims 1
• 108010028554 LDL Cholesterol Proteins 0.000 claims 1
• 238000008214 LDL Cholesterol Methods 0.000 claims 1
• 102000004882 Lipase Human genes 0.000 claims 1
• 108090001060 Lipase Proteins 0.000 claims 1
• 239000004367 Lipase Substances 0.000 claims 1
• 108010069201 VLDL Cholesterol Proteins 0.000 claims 1
• 239000002253 acid Substances 0.000 claims 1
• 125000002252 acyl group Chemical group 0.000 claims 1
• 125000004423 acyloxy group Chemical group 0.000 claims 1
• 125000003342 alkenyl group Chemical group 0.000 claims 1
• 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
• 125000003282 alkyl amino group Chemical group 0.000 claims 1
• 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 1
• 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
• 125000004414 alkyl thio group Chemical group 0.000 claims 1
• 125000000304 alkynyl group Chemical group 0.000 claims 1
• 125000003277 amino group Chemical group 0.000 claims 1
• 125000003118 aryl group Chemical group 0.000 claims 1
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
• 239000008280 blood Substances 0.000 claims 1
• 210000004369 blood Anatomy 0.000 claims 1
• 239000002775 capsule Substances 0.000 claims 1
• 206010012601 diabetes mellitus Diseases 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 239000012039 electrophile Substances 0.000 claims 1
• 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
• 239000008103 glucose Substances 0.000 claims 1
• 125000005843 halogen group Chemical group 0.000 claims 1
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
• 208000027866 inflammatory disease Diseases 0.000 claims 1
• 229940125396 insulin Drugs 0.000 claims 1
• 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
• 235000019421 lipase Nutrition 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
• 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
• 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims 1
• 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
• 230000000269 nucleophilic effect Effects 0.000 claims 1
• 230000002093 peripheral effect Effects 0.000 claims 1
• 239000000651 prodrug Substances 0.000 claims 1
• 229940002612 prodrug Drugs 0.000 claims 1
• 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 1
• UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
• 150000003839 salts Chemical class 0.000 claims 1
• 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
• 210000002966 serum Anatomy 0.000 claims 1
• 239000012453 solvate Substances 0.000 claims 1
• 208000024891 symptom Diseases 0.000 claims 1
• 150000003626 triacylglycerols Chemical class 0.000 claims 1
• 230000004584 weight gain Effects 0.000 claims 1
• 235000019786 weight gain Nutrition 0.000 claims 1
• 230000004580 weight loss Effects 0.000 claims 1