JP2005532331A5 - - Google Patents

Info

Publication number

JP2005532331A5

JP2005532331A5 JP2004506805A JP2004506805A JP2005532331A5 JP 2005532331 A5 JP2005532331 A5 JP 2005532331A5 JP 2004506805 A JP2004506805 A JP 2004506805A JP 2004506805 A JP2004506805 A JP 2004506805A JP 2005532331 A5 JP2005532331 A5 JP 2005532331A5

Authority

JP

Japan

Prior art keywords

optionally substituted

pharmaceutical composition

lower alkyl

fatty acid

acid oxidation

Prior art date

2003-05-21

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

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• 125000000217 alkyl group Chemical group 0.000 claims 56
• 229910052739 hydrogen Inorganic materials 0.000 claims 56
• 239000001257 hydrogen Substances 0.000 claims 56
• 239000008194 pharmaceutical composition Substances 0.000 claims 52
• 235000014113 dietary fatty acids Nutrition 0.000 claims 36
• 229930195729 fatty acid Natural products 0.000 claims 36
• 239000000194 fatty acid Substances 0.000 claims 36
• 150000004665 fatty acids Chemical class 0.000 claims 36
• 230000003647 oxidation Effects 0.000 claims 36
• 238000007254 oxidation reaction Methods 0.000 claims 36
• 239000003112 inhibitor Substances 0.000 claims 35
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 28
• 150000002431 hydrogen Chemical class 0.000 claims 28
• 239000000203 mixture Substances 0.000 claims 17
• XKLMZUWKNUAPSZ-UHFFFAOYSA-N N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide Chemical compound COC1=CC=CC=C1OCC(O)CN1CCN(CC(=O)NC=2C(=CC=CC=2C)C)CC1 XKLMZUWKNUAPSZ-UHFFFAOYSA-N 0.000 claims 16
• 150000003839 salts Chemical class 0.000 claims 15
• NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 14
• 125000003545 alkoxy group Chemical group 0.000 claims 14
• 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 14
• 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 14
• 125000004414 alkyl thio group Chemical group 0.000 claims 14
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 14
• 125000004093 cyano group Chemical group *C#N 0.000 claims 14
• 125000001475 halogen functional group Chemical group 0.000 claims 14
• 125000001072 heteroaryl group Chemical group 0.000 claims 14
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 14
• 229910052760 oxygen Inorganic materials 0.000 claims 14
• 239000001301 oxygen Substances 0.000 claims 14
• 125000003107 substituted aryl group Chemical group 0.000 claims 14
• 229910052717 sulfur Chemical group 0.000 claims 14
• 239000011593 sulfur Chemical group 0.000 claims 14
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 14
• 241000124008 Mammalia Species 0.000 claims 13
• 206010012601 diabetes mellitus Diseases 0.000 claims 13
• 229960000213 ranolazine Drugs 0.000 claims 9
• MNOULQLXILYKNV-UHFFFAOYSA-N 5-[4-(trifluoromethyl)phenyl]-1h-pyrazole Chemical group C1=CC(C(F)(F)F)=CC=C1C1=CC=NN1 MNOULQLXILYKNV-UHFFFAOYSA-N 0.000 claims 7
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 7
• 239000004480 active ingredient Substances 0.000 claims 7
• 125000002252 acyl group Chemical group 0.000 claims 7
• 125000003282 alkyl amino group Chemical group 0.000 claims 7
• 125000002947 alkylene group Chemical group 0.000 claims 7
• -1 aminocarbonylmethyl Chemical group 0.000 claims 7
• 229910052799 carbon Inorganic materials 0.000 claims 7
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 7
• 150000002148 esters Chemical class 0.000 claims 7
• 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 7
• 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
• 206010018429 Glucose tolerance impaired Diseases 0.000 claims 6
• 230000036470 plasma concentration Effects 0.000 claims 6
• HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 4
• 150000001875 compounds Chemical class 0.000 claims 4
• 238000013268 sustained release Methods 0.000 claims 4
• 239000012730 sustained-release form Substances 0.000 claims 4
• 229940081730 Partial fatty acid oxidation inhibitor Drugs 0.000 claims 3
• 238000009472 formulation Methods 0.000 claims 3
• 235000012000 cholesterol Nutrition 0.000 claims 2
• 239000012729 immediate-release (IR) formulation Substances 0.000 claims 2
• 206010012689 Diabetic retinopathy 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
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 238000004132 cross linking Methods 0.000 claims 1
• 239000003405 delayed action preparation Substances 0.000 claims 1
• 239000008103 glucose Substances 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 0 BC(C)(*(**)C(*)(*)C(*)(*)N1CC(**)O)C1(*)S Chemical compound BC(C)(*(**)C(*)(*)C(*)(*)N1CC(**)O)C1(*)S 0.000 description 1