JP2012527475A5 - - Google Patents

Info

Publication number

JP2012527475A5

JP2012527475A5 JP2012512030A JP2012512030A JP2012527475A5 JP 2012527475 A5 JP2012527475 A5 JP 2012527475A5 JP 2012512030 A JP2012512030 A JP 2012512030A JP 2012512030 A JP2012512030 A JP 2012512030A JP 2012527475 A5 JP2012527475 A5 JP 2012527475A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

disease

uric acid

compound

viii

Prior art date

2010-05-20

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Withdrawn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

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• 239000008194 pharmaceutical composition Substances 0.000 claims 21
• 150000001875 compounds Chemical class 0.000 claims 16
• LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 claims 12
• TVWHNULVHGKJHS-UHFFFAOYSA-N Uric acid Natural products N1C(=O)NC(=O)C2NC(=O)NC21 TVWHNULVHGKJHS-UHFFFAOYSA-N 0.000 claims 12
• 229940116269 uric acid Drugs 0.000 claims 12
• 201000010099 disease Diseases 0.000 claims 9
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
• 201000005569 Gout Diseases 0.000 claims 8
• 210000001519 tissue Anatomy 0.000 claims 7
• 229940079593 drug Drugs 0.000 claims 5
• 239000003814 drug Substances 0.000 claims 5
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 5
• 210000000056 organ Anatomy 0.000 claims 5
• IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 claims 4
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
• 229910052739 hydrogen Inorganic materials 0.000 claims 4
• 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 4
• 229960003459 allopurinol Drugs 0.000 claims 3
• OFCNXPDARWKPPY-UHFFFAOYSA-N allopurinol Chemical compound OC1=NC=NC2=C1C=NN2 OFCNXPDARWKPPY-UHFFFAOYSA-N 0.000 claims 3
• 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
• 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
• 239000003937 drug carrier Substances 0.000 claims 3
• 229960005101 febuxostat Drugs 0.000 claims 3
• BQSJTQLCZDPROO-UHFFFAOYSA-N febuxostat Chemical compound C1=C(C#N)C(OCC(C)C)=CC=C1C1=NC(C)=C(C(O)=O)S1 BQSJTQLCZDPROO-UHFFFAOYSA-N 0.000 claims 3
• RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
• 229910052760 oxygen Inorganic materials 0.000 claims 3
• 229910052717 sulfur Inorganic materials 0.000 claims 3
• 239000000275 Adrenocorticotropic Hormone Substances 0.000 claims 2
• 101800000414 Corticotropin Proteins 0.000 claims 2
• 206010020772 Hypertension Diseases 0.000 claims 2
• 201000001431 Hyperuricemia Diseases 0.000 claims 2
• 102000018251 Hypoxanthine Phosphoribosyltransferase Human genes 0.000 claims 2
• 108010091358 Hypoxanthine Phosphoribosyltransferase Proteins 0.000 claims 2
• ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 2
• 102100027467 Pro-opiomelanocortin Human genes 0.000 claims 2
• KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
• FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
• 230000002159 abnormal effect Effects 0.000 claims 2
• 206010003246 arthritis Diseases 0.000 claims 2
• 125000003118 aryl group Chemical group 0.000 claims 2
• 229910052799 carbon Inorganic materials 0.000 claims 2
• 125000004432 carbon atom Chemical group C* 0.000 claims 2
• 150000001768 cations Chemical class 0.000 claims 2
• 229960001338 colchicine Drugs 0.000 claims 2
• IDLFZVILOHSSID-OVLDLUHVSA-N corticotropin Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@@H](N)CO)C1=CC=C(O)C=C1 IDLFZVILOHSSID-OVLDLUHVSA-N 0.000 claims 2
• 229960000258 corticotropin Drugs 0.000 claims 2
• 230000029142 excretion Effects 0.000 claims 2
• 125000005842 heteroatom Chemical group 0.000 claims 2
• ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims 2
• CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 2
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
• 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
• 229910052757 nitrogen Inorganic materials 0.000 claims 2
• DBABZHXKTCFAPX-UHFFFAOYSA-N probenecid Chemical compound CCCN(CCC)S(=O)(=O)C1=CC=C(C(O)=O)C=C1 DBABZHXKTCFAPX-UHFFFAOYSA-N 0.000 claims 2
• 229960003081 probenecid Drugs 0.000 claims 2
• 229920006395 saturated elastomer Polymers 0.000 claims 2
• 229960003329 sulfinpyrazone Drugs 0.000 claims 2
• MBGGBVCUIVRRBF-UHFFFAOYSA-N sulfinpyrazone Chemical compound O=C1N(C=2C=CC=CC=2)N(C=2C=CC=CC=2)C(=O)C1CCS(=O)C1=CC=CC=C1 MBGGBVCUIVRRBF-UHFFFAOYSA-N 0.000 claims 2
• 230000001629 suppression Effects 0.000 claims 2
• 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
• 208000019838 Blood disease Diseases 0.000 claims 1
• 206010007027 Calculus urinary Diseases 0.000 claims 1
• 208000024172 Cardiovascular disease Diseases 0.000 claims 1
• 102100039259 Cytochrome c oxidase subunit 8A, mitochondrial Human genes 0.000 claims 1
• 206010018634 Gouty Arthritis Diseases 0.000 claims 1
• 101000745956 Homo sapiens Cytochrome c oxidase subunit 8A, mitochondrial Proteins 0.000 claims 1
• 201000002980 Hyperparathyroidism Diseases 0.000 claims 1
• HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims 1
• 206010061218 Inflammation Diseases 0.000 claims 1
• 208000000913 Kidney Calculi Diseases 0.000 claims 1
• 208000009625 Lesch-Nyhan syndrome Diseases 0.000 claims 1
• 206010027439 Metal poisoning Diseases 0.000 claims 1
• CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims 1
• 206010029148 Nephrolithiasis Diseases 0.000 claims 1
• 201000004681 Psoriasis Diseases 0.000 claims 1
• WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
• 208000001647 Renal Insufficiency Diseases 0.000 claims 1
• 208000035317 Total hypoxanthine-guanine phosphoribosyl transferase deficiency Diseases 0.000 claims 1
• 125000000217 alkyl group Chemical group 0.000 claims 1
• 239000002220 antihypertensive agent Substances 0.000 claims 1
• 229940127088 antihypertensive drug Drugs 0.000 claims 1
• 239000002246 antineoplastic agent Substances 0.000 claims 1
• 229940041181 antineoplastic drug Drugs 0.000 claims 1
• -1 aromatic ring compound Chemical class 0.000 claims 1
• 230000015572 biosynthetic process Effects 0.000 claims 1
• 210000004369 blood Anatomy 0.000 claims 1
• 239000008280 blood Substances 0.000 claims 1
• 230000007211 cardiovascular event Effects 0.000 claims 1
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 208000029078 coronary artery disease Diseases 0.000 claims 1
• 239000003246 corticosteroid Substances 0.000 claims 1
• 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
• 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
• 230000003247 decreasing effect Effects 0.000 claims 1
• 230000007812 deficiency Effects 0.000 claims 1
• 208000014951 hematologic disease Diseases 0.000 claims 1
• 208000018706 hematopoietic system disease Diseases 0.000 claims 1
• 125000001072 heteroaryl group Chemical group 0.000 claims 1
• 229960001680 ibuprofen Drugs 0.000 claims 1
• 230000004054 inflammatory process Effects 0.000 claims 1
• 208000018937 joint inflammation Diseases 0.000 claims 1
• 208000017169 kidney disease Diseases 0.000 claims 1
• 201000006370 kidney failure Diseases 0.000 claims 1
• 208000008127 lead poisoning Diseases 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 229960002009 naproxen Drugs 0.000 claims 1
• CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims 1
• 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
• 238000012261 overproduction Methods 0.000 claims 1
• WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical group C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 1
• 210000002381 plasma Anatomy 0.000 claims 1
• 239000000651 prodrug Chemical group 0.000 claims 1
• 229940002612 prodrug Drugs 0.000 claims 1
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 230000000306 recurrent effect Effects 0.000 claims 1
• 201000000306 sarcoidosis Diseases 0.000 claims 1
• 210000002966 serum Anatomy 0.000 claims 1
• 208000011580 syndromic disease Diseases 0.000 claims 1
• VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims 1
• 150000003852 triazoles Chemical class 0.000 claims 1
• 208000008281 urolithiasis Diseases 0.000 claims 1
• 0 CC1=C(*C=C)[C@@](*)*C=C1* Chemical compound CC1=C(*C=C)[C@@](*)*C=C1* 0.000 description 1