JP2005533807A5 - - Google Patents

Info

Publication number

JP2005533807A5

JP2005533807A5 JP2004515868A JP2004515868A JP2005533807A5 JP 2005533807 A5 JP2005533807 A5 JP 2005533807A5 JP 2004515868 A JP2004515868 A JP 2004515868A JP 2004515868 A JP2004515868 A JP 2004515868A JP 2005533807 A5 JP2005533807 A5 JP 2005533807A5

Authority

JP

Japan

Prior art keywords

hydroxy

hydrogen

prop

oxo

ethoxy

Prior art date

2003-06-17

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

• 125000000217 alkyl group Chemical group 0.000 claims description 30
• 229910052739 hydrogen Inorganic materials 0.000 claims description 30
• 239000001257 hydrogen Substances 0.000 claims description 30
• 150000001875 compounds Chemical class 0.000 claims description 17
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 15
• 125000003545 alkoxy group Chemical group 0.000 claims description 15
• 150000002431 hydrogen Chemical class 0.000 claims description 15
• -1 cyano, hydroxy Chemical group 0.000 claims description 14
• 238000000034 method Methods 0.000 claims description 11
• 125000003342 alkenyl group Chemical group 0.000 claims description 10
• 125000000304 alkynyl group Chemical group 0.000 claims description 10
• 229910052736 halogen Inorganic materials 0.000 claims description 10
• 150000002367 halogens Chemical class 0.000 claims description 10
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
• 239000000651 prodrug Substances 0.000 claims description 7
• 229940002612 prodrug Drugs 0.000 claims description 7
• 125000004432 carbon atom Chemical group C* 0.000 claims description 5
• 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 5
• 238000001727 in vivo Methods 0.000 claims description 4
• 125000004093 cyano group Chemical group *C#N 0.000 claims description 3
• 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 22
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 20
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 20
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 18
• RPKLZQLYODPWTM-UHFFFAOYSA-N methyl 15-acetoxy(10),13E-ent-halimadien-18-oate Natural products C1CC2CCCCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)CC2 RPKLZQLYODPWTM-UHFFFAOYSA-N 0.000 claims 11
• RPKLZQLYODPWTM-KBMWBBLPSA-N cholanoic acid Chemical compound C1CC2CCCC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@@H](CCC(O)=O)C)[C@@]1(C)CC2 RPKLZQLYODPWTM-KBMWBBLPSA-N 0.000 claims 8
• LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 7
• 102000003676 Glucocorticoid Receptors Human genes 0.000 claims 4
• 108090000079 Glucocorticoid Receptors Proteins 0.000 claims 4
• 241000124008 Mammalia Species 0.000 claims 4
• 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 claims 4
• 230000003042 antagnostic effect Effects 0.000 claims 3
• UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 3
• 150000003839 salts Chemical class 0.000 claims 3
• 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 2
• 206010060378 Hyperinsulinaemia Diseases 0.000 claims 2
• 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
• 206010020772 Hypertension Diseases 0.000 claims 2
• 208000008589 Obesity Diseases 0.000 claims 2
• 206010012601 diabetes mellitus Diseases 0.000 claims 2
• 239000003862 glucocorticoid Substances 0.000 claims 2
• 239000008103 glucose Substances 0.000 claims 2
• 230000002440 hepatic effect Effects 0.000 claims 2
• 201000001421 hyperglycemia Diseases 0.000 claims 2
• 230000003451 hyperinsulinaemic effect Effects 0.000 claims 2
• 201000008980 hyperinsulinism Diseases 0.000 claims 2
• 210000004185 liver Anatomy 0.000 claims 2
• 235000020824 obesity Nutrition 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 239000000546 pharmaceutical excipient Substances 0.000 claims 2
• 208000011580 syndromic disease Diseases 0.000 claims 2
• 150000001345 alkine derivatives Chemical class 0.000 claims 1
• 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
• RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
• 0 C*C=C(*CCOC(CC1)CC2C1(C)C(C[C@](*)C1(C)C3CCC1C(C)CCC(O)=O)C3C(*I)C2)C(*)=CC(C(CC(C)(C(*)C(*)C1*)C1C1C(*)C2*)C1=C(CC1*I)C2=CC1=O)=* Chemical compound C*C=C(*CCOC(CC1)CC2C1(C)C(C[C@](*)C1(C)C3CCC1C(C)CCC(O)=O)C3C(*I)C2)C(*)=CC(C(CC(C)(C(*)C(*)C1*)C1C1C(*)C2*)C1=C(CC1*I)C2=CC1=O)=* 0.000 description 1
• KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 1
• 206010020751 Hypersensitivity Diseases 0.000 description 1
• 229910019142 PO4 Inorganic materials 0.000 description 1
• 208000030961 allergic reaction Diseases 0.000 description 1
• 238000013270 controlled release Methods 0.000 description 1
• 150000002148 esters Chemical class 0.000 description 1
• 230000007794 irritation Effects 0.000 description 1
• 235000021317 phosphate Nutrition 0.000 description 1
• 150000003013 phosphoric acid derivatives Chemical class 0.000 description 1
• 230000001988 toxicity Effects 0.000 description 1
• 231100000419 toxicity Toxicity 0.000 description 1