JP2008501776A5 - - Google Patents

Info

Publication number

JP2008501776A5

JP2008501776A5 JP2007526593A JP2007526593A JP2008501776A5 JP 2008501776 A5 JP2008501776 A5 JP 2008501776A5 JP 2007526593 A JP2007526593 A JP 2007526593A JP 2007526593 A JP2007526593 A JP 2007526593A JP 2008501776 A5 JP2008501776 A5 JP 2008501776A5

Authority

JP

Japan

Prior art keywords

pde10

antagonist

subject

pharmaceutical composition

quinazoline

Prior art date

2005-05-30

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.)

Withdrawn

Links

• Espacenet
• Global Dossier
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• 239000005557 antagonist Substances 0.000 claims 17
• 239000008194 pharmaceutical composition Substances 0.000 claims 11
• 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 5
• KWGRBVOPPLSCSI-WPRPVWTQSA-N (-)-ephedrine Chemical compound CN[C@@H](C)[C@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WPRPVWTQSA-N 0.000 claims 4
• 208000002705 Glucose Intolerance Diseases 0.000 claims 4
• 208000001145 Metabolic Syndrome Diseases 0.000 claims 4
• 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 4
• 210000000577 adipose tissue Anatomy 0.000 claims 4
• 239000000883 anti-obesity agent Substances 0.000 claims 4
• 229940125710 antiobesity agent Drugs 0.000 claims 4
• KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 claims 4
• 239000003814 drug Substances 0.000 claims 4
• 201000009104 prediabetes syndrome Diseases 0.000 claims 4
• 150000003839 salts Chemical class 0.000 claims 4
• 229940124597 therapeutic agent Drugs 0.000 claims 4
• 238000000034 method Methods 0.000 claims 3
• AZEXWHKOMMASPA-UHFFFAOYSA-N 2-{[4-(1-methyl-4-pyridin-4-yl-1h-pyrazol-3-yl)phenoxy]methyl}quinoline Chemical compound C=1C=C(OCC=2N=C3C=CC=CC3=CC=2)C=CC=1C1=NN(C)C=C1C1=CC=NC=C1 AZEXWHKOMMASPA-UHFFFAOYSA-N 0.000 claims 2
• VRWJZGHUCOFGPZ-UHFFFAOYSA-N 2-{[4-(4-pyridin-4-yl-1h-pyrazol-3-yl)phenoxy]methyl}quinoline Chemical compound C=1C=C2C=CC=CC2=NC=1COC(C=C1)=CC=C1C1=NNC=C1C1=CC=NC=C1 VRWJZGHUCOFGPZ-UHFFFAOYSA-N 0.000 claims 2
• PBAXECCRMPYTKV-UHFFFAOYSA-N 4-(2-fluorophenyl)-6,7-dimethoxy-2-piperazin-1-ylquinazoline Chemical compound C=12C=C(OC)C(OC)=CC2=NC(N2CCNCC2)=NC=1C1=CC=CC=C1F PBAXECCRMPYTKV-UHFFFAOYSA-N 0.000 claims 2
• MUOKUOYNTHTOBU-UHFFFAOYSA-N 4-[[2-(6,7-dimethoxyquinazolin-4-yl)-3,4-dihydro-1h-isoquinolin-8-yl]sulfonyl]morpholine Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1N(CC1=2)CCC1=CC=CC=2S(=O)(=O)N1CCOCC1 MUOKUOYNTHTOBU-UHFFFAOYSA-N 0.000 claims 2
• UBIIFKJMNRPNMT-UHFFFAOYSA-N 6,7-dimethoxy-4-(3-quinoxalin-2-yloxypyrrolidin-1-yl)quinazoline Chemical compound C1=CC=CC2=NC(OC3CCN(C3)C=3N=CN=C4C=C(C(=CC4=3)OC)OC)=CN=C21 UBIIFKJMNRPNMT-UHFFFAOYSA-N 0.000 claims 2
• 102000016267 Leptin Human genes 0.000 claims 2
• 108010092277 Leptin Proteins 0.000 claims 2
• 230000037396 body weight Effects 0.000 claims 2
• OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 claims 2
• 229960002802 bromocriptine Drugs 0.000 claims 2
• 150000001875 compounds Chemical class 0.000 claims 2
• 229960002179 ephedrine Drugs 0.000 claims 2
• 150000004677 hydrates Chemical class 0.000 claims 2
• 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 2
• 229940039781 leptin Drugs 0.000 claims 2
• AHLBNYSZXLDEJQ-FWEHEUNISA-N orlistat Chemical compound CCCCCCCCCCC[C@H](OC(=O)[C@H](CC(C)C)NC=O)C[C@@H]1OC(=O)[C@H]1CCCCCC AHLBNYSZXLDEJQ-FWEHEUNISA-N 0.000 claims 2
• 229960001243 orlistat Drugs 0.000 claims 2
• 108090000765 processed proteins & peptides Proteins 0.000 claims 2
• KWGRBVOPPLSCSI-WCBMZHEXSA-N pseudoephedrine Chemical compound CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WCBMZHEXSA-N 0.000 claims 2
• 229960003908 pseudoephedrine Drugs 0.000 claims 2
• JZCPYUJPEARBJL-UHFFFAOYSA-N rimonabant Chemical compound CC=1C(C(=O)NN2CCCCC2)=NN(C=2C(=CC(Cl)=CC=2)Cl)C=1C1=CC=C(Cl)C=C1 JZCPYUJPEARBJL-UHFFFAOYSA-N 0.000 claims 2
• 229960003015 rimonabant Drugs 0.000 claims 2
• UNAANXDKBXWMLN-UHFFFAOYSA-N sibutramine Chemical compound C=1C=C(Cl)C=CC=1C1(C(N(C)C)CC(C)C)CCC1 UNAANXDKBXWMLN-UHFFFAOYSA-N 0.000 claims 2
• 229960004425 sibutramine Drugs 0.000 claims 2
• 239000002904 solvent Substances 0.000 claims 2
• 238000012360 testing method Methods 0.000 claims 2
• 206010033307 Overweight Diseases 0.000 claims 1
• 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 claims 1
• 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 claims 1
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 230000000694 effects Effects 0.000 claims 1
• 238000000338 in vitro Methods 0.000 claims 1