JP2008534601A5 - - Google Patents

Info

Publication number

JP2008534601A5

JP2008534601A5 JP2008504297A JP2008504297A JP2008534601A5 JP 2008534601 A5 JP2008534601 A5 JP 2008534601A5 JP 2008504297 A JP2008504297 A JP 2008504297A JP 2008504297 A JP2008504297 A JP 2008504297A JP 2008534601 A5 JP2008534601 A5 JP 2008534601A5

Authority

JP

Japan

Prior art keywords

amino

ribofuranosyl

deoxy

imidazole

salt

Prior art date

2006-03-28

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

• Espacenet
• Global Dossier
• Discuss

• ZBNZAJFNDPPMDT-UHFFFAOYSA-N 1h-imidazole-5-carboxamide Chemical compound NC(=O)C1=CNC=N1 ZBNZAJFNDPPMDT-UHFFFAOYSA-N 0.000 claims 34
• 239000008194 pharmaceutical composition Substances 0.000 claims 30
• 150000003839 salts Chemical class 0.000 claims 30
• 239000000651 prodrug Substances 0.000 claims 28
• 229940002612 prodrug Drugs 0.000 claims 28
• 238000007631 vascular surgery Methods 0.000 claims 28
• 239000000203 mixture Substances 0.000 claims 22
• 208000010125 myocardial infarction Diseases 0.000 claims 19
• WLLGXSLBOPFWQV-UHFFFAOYSA-N MGK 264 Chemical compound C1=CC2CC1C1C2C(=O)N(CC(CC)CCCC)C1=O WLLGXSLBOPFWQV-UHFFFAOYSA-N 0.000 claims 16
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 16
• 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 16
• 230000000694 effects Effects 0.000 claims 13
• 238000002271 resection Methods 0.000 claims 9
• -1 5-amino-5-deoxy-β-D-ribofuranosyl Chemical group 0.000 claims 8
• 229910052739 hydrogen Inorganic materials 0.000 claims 8
• 239000001257 hydrogen Substances 0.000 claims 8
• RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 6
• FLSNXUIOVZDMKE-XVFCMESISA-N (2R,3R,4S,5R)-2-(5-aminoimidazol-1-yl)-5-(aminomethyl)oxolane-3,4-diol Chemical compound NC1=CN=CN1[C@H]1[C@H](O)[C@H](O)[C@H](O1)CN FLSNXUIOVZDMKE-XVFCMESISA-N 0.000 claims 5
• RTRQQBHATOEIAF-UHFFFAOYSA-N AICA riboside Natural products NC1=C(C(=O)N)N=CN1C1C(O)C(O)C(CO)O1 RTRQQBHATOEIAF-UHFFFAOYSA-N 0.000 claims 5
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
• RTRQQBHATOEIAF-UUOKFMHZSA-N acadesine Chemical compound NC1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 RTRQQBHATOEIAF-UUOKFMHZSA-N 0.000 claims 5
• 229960003000 acadesine Drugs 0.000 claims 5
• 239000003085 diluting agent Substances 0.000 claims 4
• 239000003814 drug Substances 0.000 claims 4
• 238000009472 formulation Methods 0.000 claims 4
• 229910052736 halogen Inorganic materials 0.000 claims 4
• 150000002367 halogens Chemical class 0.000 claims 4
• 239000000546 pharmaceutical excipient Substances 0.000 claims 4
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
• 230000002861 ventricular Effects 0.000 claims 4
• 208000005016 Intestinal Neoplasms Diseases 0.000 claims 3
• 208000037062 Polyps Diseases 0.000 claims 3
• 230000003187 abdominal effect Effects 0.000 claims 3
• 238000007486 appendectomy Methods 0.000 claims 3
• 210000001072 colon Anatomy 0.000 claims 3
• 150000001875 compounds Chemical class 0.000 claims 3
• 239000003937 drug carrier Substances 0.000 claims 3
• 208000014617 hemorrhoid Diseases 0.000 claims 3
• 150000002431 hydrogen Chemical class 0.000 claims 3
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
• 238000009802 hysterectomy Methods 0.000 claims 3
• 210000002429 large intestine Anatomy 0.000 claims 3
• 238000007443 liposuction Methods 0.000 claims 3
• 239000000693 micelle Substances 0.000 claims 3
• 210000005036 nerve Anatomy 0.000 claims 3
• 238000009806 oophorectomy Methods 0.000 claims 3
• 230000000399 orthopedic effect Effects 0.000 claims 3
• 210000003101 oviduct Anatomy 0.000 claims 3
• 210000002307 prostate Anatomy 0.000 claims 3
• 201000010727 rectal prolapse Diseases 0.000 claims 3
• 210000000664 rectum Anatomy 0.000 claims 3
• 238000002435 rhinoplasty Methods 0.000 claims 3
• 210000000813 small intestine Anatomy 0.000 claims 3
• 229910052717 sulfur Inorganic materials 0.000 claims 3
• 238000007483 tonsillectomy Methods 0.000 claims 3
• 238000007879 vasectomy Methods 0.000 claims 3
• NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
• 125000003545 alkoxy group Chemical group 0.000 claims 2
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
• 150000005676 cyclic carbonates Chemical class 0.000 claims 2
• 238000000034 method Methods 0.000 claims 2
• 229910052760 oxygen Inorganic materials 0.000 claims 2
• 239000001301 oxygen Substances 0.000 claims 2
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
• 230000036470 plasma concentration Effects 0.000 claims 2
• 239000011593 sulfur Chemical group 0.000 claims 2
• BXDZOYLPNAIDOC-UHFFFAOYSA-N N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]-1-[2-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethylamino]-2-oxoethyl]piperidine-4-carboxamide Chemical compound CC(C)(C)c1cnc(CSc2cnc(NC(=O)C3CCN(CC(=O)NCCOCCOCCOCCNc4cccc5C(=O)N(C6CCC(=O)NC6=O)C(=O)c45)CC3)s2)o1 BXDZOYLPNAIDOC-UHFFFAOYSA-N 0.000 claims 1
• 229910019142 PO4 Inorganic materials 0.000 claims 1
• LZLREEUGSYITMX-JQWIXIFHSA-N Ser-Trp Chemical compound C1=CC=C2C(C[C@H](NC(=O)[C@H](CO)N)C(O)=O)=CNC2=C1 LZLREEUGSYITMX-JQWIXIFHSA-N 0.000 claims 1
• YKOWBJJOJNGCAD-SHYZEUOFSA-N [(2r,3s,5r)-3-hydroxy-5-[4-(hydroxyamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methyl dihydrogen phosphate Chemical group O=C1N=C(NO)C=CN1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)C1 YKOWBJJOJNGCAD-SHYZEUOFSA-N 0.000 claims 1
• 125000002252 acyl group Chemical group 0.000 claims 1
• 125000000217 alkyl group Chemical group 0.000 claims 1
• 125000003118 aryl group Chemical group 0.000 claims 1
• HMFHBZSHGGEWLO-TXICZTDVSA-N beta-D-ribose Chemical group OC[C@H]1O[C@@H](O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-TXICZTDVSA-N 0.000 claims 1
• 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
• 230000003247 decreasing effect Effects 0.000 claims 1
• 229940079593 drug Drugs 0.000 claims 1
• 125000000623 heterocyclic group Chemical group 0.000 claims 1
• 239000007788 liquid Substances 0.000 claims 1
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
• MPNNOLHYOHFJKL-UHFFFAOYSA-N peroxyphosphoric acid Chemical class OOP(O)(O)=O MPNNOLHYOHFJKL-UHFFFAOYSA-N 0.000 claims 1
• 239000008063 pharmaceutical solvent Substances 0.000 claims 1
• 239000010452 phosphate Substances 0.000 claims 1
• 230000002265 prevention Effects 0.000 claims 1
• 230000001698 pyrogenic effect Effects 0.000 claims 1
• 239000007909 solid dosage form Substances 0.000 claims 1
• 238000001356 surgical procedure Methods 0.000 claims 1
• 125000003396 thiol group Chemical group [H]S* 0.000 claims 1