JP2017512183A5 - - Google Patents

Info

Publication number

JP2017512183A5

JP2017512183A5 JP2016547558A JP2016547558A JP2017512183A5 JP 2017512183 A5 JP2017512183 A5 JP 2017512183A5 JP 2016547558 A JP2016547558 A JP 2016547558A JP 2016547558 A JP2016547558 A JP 2016547558A JP 2017512183 A5 JP2017512183 A5 JP 2017512183A5

Authority

JP

Japan

Prior art keywords

optionally substituted

group

alkyl

heteroalkyl

substituted

Prior art date

2015-02-11

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.)

Pending

Links

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• 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims description 66
• 239000003124 biologic agent Substances 0.000 claims description 66
• 150000001875 compounds Chemical class 0.000 claims description 52
• 229910052739 hydrogen Inorganic materials 0.000 claims description 38
• 125000001072 heteroaryl group Chemical group 0.000 claims description 28
• 229910052760 oxygen Inorganic materials 0.000 claims description 28
• 238000000034 method Methods 0.000 claims description 26
• 229910052799 carbon Inorganic materials 0.000 claims description 24
• 150000003839 salts Chemical class 0.000 claims description 24
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 22
• 229940002612 prodrug Drugs 0.000 claims description 22
• 239000000651 prodrug Substances 0.000 claims description 22
• 125000003107 substituted aryl group Chemical group 0.000 claims description 20
• 210000004027 cell Anatomy 0.000 claims description 19
• 125000003545 alkoxy group Chemical group 0.000 claims description 18
• 239000008194 pharmaceutical composition Substances 0.000 claims description 16
• 229940075993 receptor modulator Drugs 0.000 claims description 14
• 125000003118 aryl group Chemical group 0.000 claims description 13
• 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 12
• OBOXTJCIIVUZEN-UHFFFAOYSA-N [C].[O] Chemical compound [C].[O] OBOXTJCIIVUZEN-UHFFFAOYSA-N 0.000 claims description 12
• 125000004432 carbon atom Chemical group C* 0.000 claims description 12
• 201000010099 disease Diseases 0.000 claims description 12
• 208000035475 disorder Diseases 0.000 claims description 10
• 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 10
• PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims description 8
• 229910019142 PO4 Inorganic materials 0.000 claims description 8
• 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims description 8
• 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims description 8
• 125000004404 heteroalkyl group Chemical group 0.000 claims description 8
• 235000021317 phosphate Nutrition 0.000 claims description 8
• 150000003013 phosphoric acid derivatives Chemical class 0.000 claims description 8
• 125000004423 acyloxy group Chemical group 0.000 claims description 7
• 230000003054 hormonal effect Effects 0.000 claims description 6
• 208000019423 liver disease Diseases 0.000 claims description 6
• 229910052757 nitrogen Inorganic materials 0.000 claims description 6
• 239000010452 phosphate Substances 0.000 claims description 6
• UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical class [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims description 6
• 229940124213 Dipeptidyl peptidase 4 (DPP IV) inhibitor Drugs 0.000 claims description 4
• 208000032928 Dyslipidaemia Diseases 0.000 claims description 4
• 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 description 4
• 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 4
• 208000017170 Lipid metabolism disease Diseases 0.000 claims description 4
• 102000007399 Nuclear hormone receptor Human genes 0.000 claims description 4
• 108020005497 Nuclear hormone receptor Proteins 0.000 claims description 4
• 230000000840 anti-viral effect Effects 0.000 claims description 4
• 239000002246 antineoplastic agent Substances 0.000 claims description 4
• 239000003443 antiviral agent Substances 0.000 claims description 4
• 239000003613 bile acid Substances 0.000 claims description 4
• 239000003603 dipeptidyl peptidase IV inhibitor Substances 0.000 claims description 4
• 229940125753 fibrate Drugs 0.000 claims description 4
• 239000008103 glucose Substances 0.000 claims description 4
• 230000009229 glucose formation Effects 0.000 claims description 4
• 125000000623 heterocyclic group Chemical group 0.000 claims description 4
• 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims description 4
• 239000003112 inhibitor Substances 0.000 claims description 4
• 150000002632 lipids Chemical class 0.000 claims description 4
• 210000004185 liver Anatomy 0.000 claims description 4
• 229960003512 nicotinic acid Drugs 0.000 claims description 4
• 235000001968 nicotinic acid Nutrition 0.000 claims description 4
• 239000011664 nicotinic acid Substances 0.000 claims description 4
• 239000002777 nucleoside Substances 0.000 claims description 4
• 150000003833 nucleoside derivatives Chemical class 0.000 claims description 4
• 235000020660 omega-3 fatty acid Nutrition 0.000 claims description 4
• 229940012843 omega-3 fatty acid Drugs 0.000 claims description 4
• 108090000721 thyroid hormone receptors Proteins 0.000 claims description 4
• 102000004217 thyroid hormone receptors Human genes 0.000 claims description 4
• 210000005260 human cell Anatomy 0.000 claims description 3
• HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims description 2
• 125000006823 (C1-C6) acyl group Chemical group 0.000 claims description 2
• 201000001320 Atherosclerosis Diseases 0.000 claims description 2
• 208000004930 Fatty Liver Diseases 0.000 claims description 2
• 206010019708 Hepatic steatosis Diseases 0.000 claims description 2
• 208000031226 Hyperlipidaemia Diseases 0.000 claims description 2
• 241000124008 Mammalia Species 0.000 claims description 2
• 208000008589 Obesity Diseases 0.000 claims description 2
• 208000030852 Parasitic disease Diseases 0.000 claims description 2
• ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical class OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims description 2
• 208000036142 Viral infection Diseases 0.000 claims description 2
• 229940041181 antineoplastic drug Drugs 0.000 claims description 2
• 125000004104 aryloxy group Chemical group 0.000 claims description 2
• 239000007795 chemical reaction product Substances 0.000 claims description 2
• 208000019425 cirrhosis of liver Diseases 0.000 claims description 2
• CYQFCXCEBYINGO-IAGOWNOFSA-N delta1-THC Chemical compound C1=C(C)CC[C@H]2C(C)(C)OC3=CC(CCCCC)=CC(O)=C3[C@@H]21 CYQFCXCEBYINGO-IAGOWNOFSA-N 0.000 claims description 2
• 206010012601 diabetes mellitus Diseases 0.000 claims description 2
• 239000003814 drug Substances 0.000 claims description 2
• 230000002526 effect on cardiovascular system Effects 0.000 claims description 2
• 208000010706 fatty liver disease Diseases 0.000 claims description 2
• 208000006454 hepatitis Diseases 0.000 claims description 2
• 231100000283 hepatitis Toxicity 0.000 claims description 2
• 210000003494 hepatocyte Anatomy 0.000 claims description 2
• 125000005553 heteroaryloxy group Chemical group 0.000 claims description 2
• 230000013632 homeostatic process Effects 0.000 claims description 2
• 201000001421 hyperglycemia Diseases 0.000 claims description 2
• 230000002401 inhibitory effect Effects 0.000 claims description 2
• 201000007270 liver cancer Diseases 0.000 claims description 2
• 208000014018 liver neoplasm Diseases 0.000 claims description 2
• 201000004792 malaria Diseases 0.000 claims description 2
• 210000004962 mammalian cell Anatomy 0.000 claims description 2
• 230000002503 metabolic effect Effects 0.000 claims description 2
• 230000003990 molecular pathway Effects 0.000 claims description 2
• 235000020824 obesity Nutrition 0.000 claims description 2
• 239000006014 omega-3 oil Substances 0.000 claims description 2
• 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
• PTMHPRAIXMAOOB-UHFFFAOYSA-L phosphoramidate Chemical compound NP([O-])([O-])=O PTMHPRAIXMAOOB-UHFFFAOYSA-L 0.000 claims description 2
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
• 231100000240 steatosis hepatitis Toxicity 0.000 claims description 2
• 229910052717 sulfur Inorganic materials 0.000 claims description 2
• 229940124597 therapeutic agent Drugs 0.000 claims description 2
• 230000029812 viral genome replication Effects 0.000 claims description 2
• 230000009385 viral infection Effects 0.000 claims description 2
• 238000002059 diagnostic imaging Methods 0.000 claims 1
• 239000012216 imaging agent Substances 0.000 claims 1
• 125000000217 alkyl group Chemical group 0.000 description 56
• 125000002252 acyl group Chemical group 0.000 description 4
• 125000004442 acylamino group Chemical group 0.000 description 3
• 239000002872 contrast media Substances 0.000 description 1
• 238000001727 in vivo Methods 0.000 description 1
• 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 description 1