JP2007523903A5 - - Google Patents
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- JP2007523903A5 JP2007523903A5 JP2006553310A JP2006553310A JP2007523903A5 JP 2007523903 A5 JP2007523903 A5 JP 2007523903A5 JP 2006553310 A JP2006553310 A JP 2006553310A JP 2006553310 A JP2006553310 A JP 2006553310A JP 2007523903 A5 JP2007523903 A5 JP 2007523903A5
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- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- arylene
- group
- phenyl
- Prior art date
- 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
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- -1 isoxazol-3-ol-5-yl Chemical group 0.000 claims 68
- 150000001875 compounds Chemical class 0.000 claims 46
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 30
- 239000002253 acid Substances 0.000 claims 20
- 229920002554 vinyl polymer Polymers 0.000 claims 18
- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 239000003937 drug carrier Substances 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000001424 substituent group Chemical group 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 9
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 claims 4
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 4
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 4
- 102000004877 Insulin Human genes 0.000 claims 4
- 108090001061 Insulin Proteins 0.000 claims 4
- 230000015572 biosynthetic process Effects 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 229940125396 insulin Drugs 0.000 claims 4
- 238000003786 synthesis reaction Methods 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 102000018997 Growth Hormone Human genes 0.000 claims 3
- 108010051696 Growth Hormone Proteins 0.000 claims 3
- 102000002727 Protein Tyrosine Phosphatase Human genes 0.000 claims 3
- 125000004419 alkynylene group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 239000000122 growth hormone Substances 0.000 claims 3
- 108020000494 protein-tyrosine phosphatase Proteins 0.000 claims 3
- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical compound O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 claims 2
- 208000030507 AIDS Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 2
- 229940123208 Biguanide Drugs 0.000 claims 2
- 229920001268 Cholestyramine Polymers 0.000 claims 2
- 208000035473 Communicable disease Diseases 0.000 claims 2
- 102000004127 Cytokines Human genes 0.000 claims 2
- 108090000695 Cytokines Proteins 0.000 claims 2
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 2
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 2
- 208000002705 Glucose Intolerance Diseases 0.000 claims 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 2
- 229940122199 Insulin secretagogue Drugs 0.000 claims 2
- 229940122355 Insulin sensitizer Drugs 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 229940126033 PPAR agonist Drugs 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 229940100389 Sulfonylurea Drugs 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 229960002632 acarbose Drugs 0.000 claims 2
- XUFXOAAUWZOOIT-UHFFFAOYSA-N acarviostatin I01 Natural products OC1C(O)C(NC2C(C(O)C(O)C(CO)=C2)O)C(C)OC1OC(C(C1O)O)C(CO)OC1OC1C(CO)OC(O)C(O)C1O XUFXOAAUWZOOIT-UHFFFAOYSA-N 0.000 claims 2
- 239000012190 activator Substances 0.000 claims 2
- 229930013930 alkaloid Natural products 0.000 claims 2
- 150000003797 alkaloid derivatives Chemical class 0.000 claims 2
- 229940100198 alkylating agent Drugs 0.000 claims 2
- 239000002168 alkylating agent Substances 0.000 claims 2
- 230000000202 analgesic effect Effects 0.000 claims 2
- 230000000340 anti-metabolite Effects 0.000 claims 2
- 239000001961 anticonvulsive agent Substances 0.000 claims 2
- 239000000935 antidepressant agent Substances 0.000 claims 2
- 229940005513 antidepressants Drugs 0.000 claims 2
- 239000002256 antimetabolite Substances 0.000 claims 2
- 229940100197 antimetabolite Drugs 0.000 claims 2
- 125000000732 arylene group Chemical group 0.000 claims 2
- 230000003115 biocidal effect Effects 0.000 claims 2
- 230000008512 biological response Effects 0.000 claims 2
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 229940125753 fibrate Drugs 0.000 claims 2
- 239000003862 glucocorticoid Substances 0.000 claims 2
- 239000003102 growth factor Substances 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 239000005556 hormone Substances 0.000 claims 2
- 229940088597 hormone Drugs 0.000 claims 2
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000003607 modifier Substances 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000002307 peroxisome proliferator activated receptor agonist Substances 0.000 claims 2
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- WXRWCAWGXBJYOV-UHFFFAOYSA-N 1-phenoxybiphenylene Chemical group C=1C=CC=2C3=CC=CC=C3C=2C=1OC1=CC=CC=C1 WXRWCAWGXBJYOV-UHFFFAOYSA-N 0.000 claims 1
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims 1
- OMYPBNALFFVYNN-UHFFFAOYSA-N 3-[4-[4-[[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]methyl]phenyl]phenoxy]-5-(trifluoromethylsulfonylamino)benzoic acid Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1CC(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC(NS(=O)(=O)C(F)(F)F)=CC(C(O)=O)=C1 OMYPBNALFFVYNN-UHFFFAOYSA-N 0.000 claims 1
- FMKAUZHQCBRMGD-UHFFFAOYSA-N 4-[4-[4-[[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]methyl]phenyl]phenoxy]-2-(methanesulfonamido)benzoic acid Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1CC(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC=C(C(O)=O)C(NS(C)(=O)=O)=C1 FMKAUZHQCBRMGD-UHFFFAOYSA-N 0.000 claims 1
- AYUPLIAGKSMVNQ-UHFFFAOYSA-N 4-[4-[4-[[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]methyl]phenyl]phenoxy]-2-(trifluoromethyl)benzoic acid Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1CC(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC=C(C(O)=O)C(C(F)(F)F)=C1 AYUPLIAGKSMVNQ-UHFFFAOYSA-N 0.000 claims 1
- CJOXUXZCFXVZTE-UHFFFAOYSA-N 4-[4-[4-[[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]methyl]phenyl]phenoxy]-2-(trifluoromethylsulfonylamino)benzoic acid Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1CC(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC=C(C(O)=O)C(NS(=O)(=O)C(F)(F)F)=C1 CJOXUXZCFXVZTE-UHFFFAOYSA-N 0.000 claims 1
- FZFLAYDNACRQAC-UHFFFAOYSA-N 4-[4-[4-[[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]methyl]phenyl]phenoxy]-3-(trifluoromethylsulfonylamino)benzoic acid Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1CC(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC=C(C(O)=O)C=C1NS(=O)(=O)C(F)(F)F FZFLAYDNACRQAC-UHFFFAOYSA-N 0.000 claims 1
- BFFVUNKIOAATDZ-UHFFFAOYSA-N 4-[4-[4-[[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]methyl]phenyl]phenoxy]-n-methylsulfonyl-2-(trifluoromethyl)benzamide Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1CC(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC=C(C(=O)NS(C)(=O)=O)C(C(F)(F)F)=C1 BFFVUNKIOAATDZ-UHFFFAOYSA-N 0.000 claims 1
- KOEQTENTJFSOHT-CXUHLZMHSA-N 4-[[4-(2,4-dichlorophenyl)-2-[(e)-2-[4-(3-methylsulfonylphenyl)phenyl]ethenyl]imidazol-1-yl]methyl]benzoic acid Chemical compound CS(=O)(=O)C1=CC=CC(C=2C=CC(\C=C\C=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)C(O)=O)=CC=2)=C1 KOEQTENTJFSOHT-CXUHLZMHSA-N 0.000 claims 1
- RFCMTZCEQXJBBI-LICLKQGHSA-N 4-[[4-(2,4-dichlorophenyl)-2-[(e)-2-[4-[3-(propan-2-yloxycarbonylamino)phenyl]phenyl]ethenyl]imidazol-1-yl]methyl]benzoic acid Chemical compound CC(C)OC(=O)NC1=CC=CC(C=2C=CC(\C=C\C=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)C(O)=O)=CC=2)=C1 RFCMTZCEQXJBBI-LICLKQGHSA-N 0.000 claims 1
- FJCUPPUXPIERFU-LICLKQGHSA-N 4-[[4-(2,4-dichlorophenyl)-2-[(e)-2-[4-[3-(propan-2-ylsulfonylamino)phenyl]phenyl]ethenyl]imidazol-1-yl]methyl]benzoic acid Chemical compound CC(C)S(=O)(=O)NC1=CC=CC(C=2C=CC(\C=C\C=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)C(O)=O)=CC=2)=C1 FJCUPPUXPIERFU-LICLKQGHSA-N 0.000 claims 1
- BYCCHCPRJOMUHP-GIDUJCDVSA-N 4-[[4-(2,4-dichlorophenyl)-2-[(e)-2-[4-[3-methoxy-4-(2,2,2-trifluoroethylsulfonylamino)phenyl]phenyl]ethenyl]imidazol-1-yl]methyl]benzoic acid Chemical compound C1=C(NS(=O)(=O)CC(F)(F)F)C(OC)=CC(C=2C=CC(\C=C\C=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)C(O)=O)=CC=2)=C1 BYCCHCPRJOMUHP-GIDUJCDVSA-N 0.000 claims 1
- AIPGWGLUPVDFAB-CAOOACKPSA-N 4-[[4-(2,4-dichlorophenyl)-2-[(e)-2-[4-[3-methoxy-4-(propan-2-yloxycarbonylamino)phenyl]phenyl]ethenyl]imidazol-1-yl]methyl]benzoic acid Chemical compound C1=C(NC(=O)OC(C)C)C(OC)=CC(C=2C=CC(\C=C\C=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)C(O)=O)=CC=2)=C1 AIPGWGLUPVDFAB-CAOOACKPSA-N 0.000 claims 1
- NZPHXMPNKCCODX-FRKPEAEDSA-N 4-[[4-(2,4-dichlorophenyl)-2-[(e)-2-[4-[4-(methanesulfonamido)-3-methoxyphenyl]phenyl]ethenyl]imidazol-1-yl]methyl]benzoic acid Chemical compound C1=C(NS(C)(=O)=O)C(OC)=CC(C=2C=CC(\C=C\C=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)C(O)=O)=CC=2)=C1 NZPHXMPNKCCODX-FRKPEAEDSA-N 0.000 claims 1
- KEUDKNLMUYZCBX-UHFFFAOYSA-N 4-[[4-(2,4-dichlorophenyl)-2-[[4-[3-(ethylsulfonylamino)phenyl]phenyl]methyl]imidazol-1-yl]methyl]benzoic acid Chemical compound CCS(=O)(=O)NC1=CC=CC(C=2C=CC(CC=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)C(O)=O)=CC=2)=C1 KEUDKNLMUYZCBX-UHFFFAOYSA-N 0.000 claims 1
- YSZVNQRRMBCAJG-UHFFFAOYSA-N 4-[[4-(2,4-dichlorophenyl)-2-[[4-[3-(propylsulfonylamino)phenyl]phenyl]methyl]imidazol-1-yl]methyl]benzoic acid Chemical compound CCCS(=O)(=O)NC1=CC=CC(C=2C=CC(CC=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)C(O)=O)=CC=2)=C1 YSZVNQRRMBCAJG-UHFFFAOYSA-N 0.000 claims 1
- DRRQZPCPLOOBHT-FZSIALSZSA-N 5-[4-[4-[(e)-2-[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]ethenyl]phenyl]phenoxy]-2-(trifluoromethyl)benzoic acid Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1\C=C\C(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC=C(C(F)(F)F)C(C(O)=O)=C1 DRRQZPCPLOOBHT-FZSIALSZSA-N 0.000 claims 1
- QSAXTKLNHYNJBP-UHFFFAOYSA-N 5-[4-[4-[[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]methyl]phenyl]phenoxy]-2-(methanesulfonamido)benzoic acid Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1CC(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC=C(NS(C)(=O)=O)C(C(O)=O)=C1 QSAXTKLNHYNJBP-UHFFFAOYSA-N 0.000 claims 1
- CMFNPQVFMAPHRV-UHFFFAOYSA-N 5-[4-[4-[[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]methyl]phenyl]phenoxy]-2-(trifluoromethyl)benzoic acid Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1CC(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC=C(C(F)(F)F)C(C(O)=O)=C1 CMFNPQVFMAPHRV-UHFFFAOYSA-N 0.000 claims 1
- MDDZSCXZLBAAFQ-UHFFFAOYSA-N 5-[4-[4-[[4-(2,4-dichlorophenyl)-1-ethylimidazol-2-yl]methyl]phenyl]phenoxy]-2-(trifluoromethylsulfonylamino)benzoic acid Chemical compound CCN1C=C(C=2C(=CC(Cl)=CC=2)Cl)N=C1CC(C=C1)=CC=C1C(C=C1)=CC=C1OC1=CC=C(NS(=O)(=O)C(F)(F)F)C(C(O)=O)=C1 MDDZSCXZLBAAFQ-UHFFFAOYSA-N 0.000 claims 1
- MCSKNIHMZIZLGC-OVCLIPMQSA-N 5-[4-[[2-[(e)-2-[4-(3-chlorophenyl)phenyl]ethenyl]-4-(2,4-dichlorophenyl)imidazol-1-yl]methyl]phenyl]-1,1-dioxo-1,2,5-thiadiazolidin-3-one Chemical compound ClC1=CC=CC(C=2C=CC(\C=C\C=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)N3S(NC(=O)C3)(=O)=O)=CC=2)=C1 MCSKNIHMZIZLGC-OVCLIPMQSA-N 0.000 claims 1
- FGZQDCVRVQZMRR-CXUHLZMHSA-N 5-[4-[[2-[(e)-2-[4-(3-tert-butyl-5-methylphenyl)phenyl]ethenyl]-4-(2,4-dichlorophenyl)imidazol-1-yl]methyl]phenyl]-1,1-dioxo-1,2,5-thiadiazolidin-3-one Chemical compound CC(C)(C)C1=CC(C)=CC(C=2C=CC(\C=C\C=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)N3S(NC(=O)C3)(=O)=O)=CC=2)=C1 FGZQDCVRVQZMRR-CXUHLZMHSA-N 0.000 claims 1
- OPRYSFSZMDOOSW-UFWORHAWSA-N 5-[4-[[2-[(e)-2-[4-(4-tert-butylphenyl)phenyl]ethenyl]-4-(2,4-dichlorophenyl)imidazol-1-yl]methyl]phenyl]-1,1-dioxo-1,2,5-thiadiazolidin-3-one Chemical compound C1=CC(C(C)(C)C)=CC=C1C(C=C1)=CC=C1\C=C\C1=NC(C=2C(=CC(Cl)=CC=2)Cl)=CN1CC1=CC=C(N2S(NC(=O)C2)(=O)=O)C=C1 OPRYSFSZMDOOSW-UFWORHAWSA-N 0.000 claims 1
- XRGBZMXBRQMFQS-OVCLIPMQSA-N 5-[4-[[4-(2,4-dichlorophenyl)-2-[(e)-2-[4-[3-(trifluoromethyl)phenyl]phenyl]ethenyl]imidazol-1-yl]methyl]phenyl]-1,1-dioxo-1,2,5-thiadiazolidin-3-one Chemical compound FC(F)(F)C1=CC=CC(C=2C=CC(\C=C\C=3N(C=C(N=3)C=3C(=CC(Cl)=CC=3)Cl)CC=3C=CC(=CC=3)N3S(NC(=O)C3)(=O)=O)=CC=2)=C1 XRGBZMXBRQMFQS-OVCLIPMQSA-N 0.000 claims 1
- 229940122041 Cholinesterase inhibitor Drugs 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- 101000642591 Xenopus laevis Somatotropin-A Proteins 0.000 claims 1
- 208000038016 acute inflammation Diseases 0.000 claims 1
- 230000006022 acute inflammation Effects 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 230000001773 anti-convulsant effect Effects 0.000 claims 1
- 230000001430 anti-depressive effect Effects 0.000 claims 1
- 230000000561 anti-psychotic effect Effects 0.000 claims 1
- 229940125681 anticonvulsant agent Drugs 0.000 claims 1
- 229960003965 antiepileptics Drugs 0.000 claims 1
- 239000000164 antipsychotic agent Substances 0.000 claims 1
- 229940005529 antipsychotics Drugs 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
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| BR0309305A (pt) * | 2002-04-12 | 2005-02-15 | Pfizer | Compostos de imidazol como agentes antiinflamatórios e analgésicos |
| US20040009956A1 (en) * | 2002-04-29 | 2004-01-15 | Dehua Pei | Inhibition of protein tyrosine phosphatases and SH2 domains by a neutral phosphotyrosine mimetic |
| EP1499608A1 (en) * | 2002-05-02 | 2005-01-26 | Neurogen Corporation | Substituted imidazole derivatives: gaba a receptor ligands |
| AU2003239897A1 (en) * | 2002-05-23 | 2003-12-12 | Ceptyr, Inc. | Modulation of ptp1b signal transduction by rna interference |
| DE60304718T2 (de) * | 2002-08-06 | 2007-04-26 | Astrazeneca Ab | Kondensierte pyridine und pyrimidine mit tie2 (tek) aktivität |
| US6849761B2 (en) * | 2002-09-05 | 2005-02-01 | Wyeth | Substituted naphthoic acid derivatives useful in the treatment of insulin resistance and hyperglycemia |
| WO2004062664A1 (en) * | 2002-12-30 | 2004-07-29 | Vertex Pharmaceuticals Incorporated | Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders |
| US7279576B2 (en) * | 2002-12-31 | 2007-10-09 | Deciphera Pharmaceuticals, Llc | Anti-cancer medicaments |
| US7144911B2 (en) * | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| US7135493B2 (en) * | 2003-01-13 | 2006-11-14 | Astellas Pharma Inc. | HDAC inhibitor |
| JP2006518738A (ja) * | 2003-02-12 | 2006-08-17 | トランス テック ファーマ，インコーポレイテッド | 治療薬としての置換アゾール誘導体 |
| WO2004071448A2 (en) * | 2003-02-12 | 2004-08-26 | Transtech Pharma Inc. | Substituted azole derivatives as inhibitors of protein tyrosine phosphatases |
| US20040167188A1 (en) * | 2003-02-14 | 2004-08-26 | Zhili Xin | Protein-tyrosine phosphatase inhibitors and uses thereof |
| WO2005035551A2 (en) * | 2003-10-08 | 2005-04-21 | Incyte Corporation | Inhibitors of proteins that bind phosphorylated molecules |
| US7723369B2 (en) * | 2006-01-30 | 2010-05-25 | Transtech Pharma, Inc. | Substituted imidazole derivatives, compositions, and methods of use as PTPase inhibitors |
-
2005
- 2005-02-11 CA CA2551909A patent/CA2551909C/en not_active Expired - Fee Related
- 2005-02-11 EP EP05723026A patent/EP1730118A1/en not_active Withdrawn
- 2005-02-11 AU AU2005214349A patent/AU2005214349B2/en not_active Ceased
- 2005-02-11 WO PCT/US2005/004590 patent/WO2005080346A1/en not_active Ceased
- 2005-02-11 JP JP2006553310A patent/JP4898458B2/ja not_active Expired - Fee Related
- 2005-02-11 CN CNA2005800048601A patent/CN1922151A/zh active Pending
- 2005-02-11 US US11/056,498 patent/US20050187277A1/en not_active Abandoned
- 2005-02-11 ZA ZA200605526A patent/ZA200605526B/en unknown
- 2005-02-11 NZ NZ548208A patent/NZ548208A/en not_active IP Right Cessation
-
2006
- 2006-06-26 IL IL176571A patent/IL176571A0/en unknown
-
2010
- 2010-11-19 US US12/950,967 patent/US20110092553A1/en not_active Abandoned
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