JP2005525378A5 - - Google Patents
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- JP2005525378A5 JP2005525378A5 JP2003574195A JP2003574195A JP2005525378A5 JP 2005525378 A5 JP2005525378 A5 JP 2005525378A5 JP 2003574195 A JP2003574195 A JP 2003574195A JP 2003574195 A JP2003574195 A JP 2003574195A JP 2005525378 A5 JP2005525378 A5 JP 2005525378A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- aryl
- phenyl
- alkyl
- group
- 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 heterocyclylene Chemical group 0.000 claims 71
- 150000001875 compounds Chemical class 0.000 claims 49
- 125000003118 aryl group Chemical group 0.000 claims 45
- 125000000217 alkyl group Chemical group 0.000 claims 40
- 239000008194 pharmaceutical composition Substances 0.000 claims 35
- 229910052739 hydrogen Inorganic materials 0.000 claims 31
- 239000001257 hydrogen Substances 0.000 claims 31
- 150000003839 salts Chemical class 0.000 claims 27
- 229910052757 nitrogen Inorganic materials 0.000 claims 26
- 150000002431 hydrogen Chemical class 0.000 claims 19
- CYJJEZFPSTZBQU-UHFFFAOYSA-N 3-[4-[2-butyl-4-[4-[2-(4-chlorophenyl)ethoxy]phenyl]imidazol-1-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OCCC=3C=CC(Cl)=CC=3)=CC=2)=CN1C1=CC=C(OCCCN(CC)CC)C=C1 CYJJEZFPSTZBQU-UHFFFAOYSA-N 0.000 claims 17
- 125000001424 substituent group Chemical group 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 125000002947 alkylene group Chemical group 0.000 claims 14
- 239000003085 diluting agent Substances 0.000 claims 14
- 239000003937 drug carrier Substances 0.000 claims 14
- 239000000546 pharmaceutical excipient Substances 0.000 claims 14
- XLLKIRLDIQLCCE-UHFFFAOYSA-N 3-[4-[4-[4-[2-(4-chlorophenyl)ethoxy]phenyl]-2-pentan-3-ylimidazol-1-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCC(CC)C1=NC(C=2C=CC(OCCC=3C=CC(Cl)=CC=3)=CC=2)=CN1C1=CC=C(OCCCN(CC)CC)C=C1 XLLKIRLDIQLCCE-UHFFFAOYSA-N 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 9
- KJNNWYBAOPXVJY-UHFFFAOYSA-N 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]imidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OCCCN(CC)CC)=CC=2)=CN1C(C=C1)=CC=C1OC1=CC=C(Cl)C=C1 KJNNWYBAOPXVJY-UHFFFAOYSA-N 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 6
- 125000004367 cycloalkylaryl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000004104 aryloxy group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000004450 alkenylene group Chemical group 0.000 claims 4
- 125000004419 alkynylene group Chemical group 0.000 claims 4
- 125000000732 arylene group Chemical group 0.000 claims 4
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 4
- 125000002993 cycloalkylene group Chemical group 0.000 claims 4
- 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 4
- 239000000203 mixture Substances 0.000 claims 4
- CLVACVUEXJMIOJ-UHFFFAOYSA-N 3-[4-[2-butyl-1-[4-(4-methylphenoxy)phenyl]imidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OCCCN(CC)CC)=CC=2)=CN1C(C=C1)=CC=C1OC1=CC=C(C)C=C1 CLVACVUEXJMIOJ-UHFFFAOYSA-N 0.000 claims 3
- PWGADFKSBNBILW-UHFFFAOYSA-N 3-[4-[2-butyl-4-[4-(4-chlorophenoxy)phenyl]imidazol-1-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OC=3C=CC(Cl)=CC=3)=CC=2)=CN1C1=CC=C(OCCCN(CC)CC)C=C1 PWGADFKSBNBILW-UHFFFAOYSA-N 0.000 claims 3
- ORUAKMCVNKXWMV-UHFFFAOYSA-N 3-[4-[4-[4-[2-(4-chlorophenyl)ethoxy]phenyl]-2-(2-methylpropyl)imidazol-1-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound C1=CC(OCCCN(CC)CC)=CC=C1N1C(CC(C)C)=NC(C=2C=CC(OCCC=3C=CC(Cl)=CC=3)=CC=2)=C1 ORUAKMCVNKXWMV-UHFFFAOYSA-N 0.000 claims 3
- 239000002671 adjuvant Substances 0.000 claims 3
- 230000037396 body weight Effects 0.000 claims 3
- 230000001684 chronic effect Effects 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000004975 3-butenyl group Chemical group C(CC=C)* 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 229940123208 Biguanide Drugs 0.000 claims 2
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 206010027476 Metastases Diseases 0.000 claims 2
- 208000017442 Retinal disease Diseases 0.000 claims 2
- 206010038923 Retinopathy Diseases 0.000 claims 2
- 229940100389 Sulfonylurea Drugs 0.000 claims 2
- 206010064390 Tumour invasion Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 229930013930 alkaloid Natural products 0.000 claims 2
- 150000003797 alkaloid derivatives Chemical class 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 229940100198 alkylating agent Drugs 0.000 claims 2
- 239000002168 alkylating agent Substances 0.000 claims 2
- 125000005275 alkylenearyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 230000000202 analgesic effect Effects 0.000 claims 2
- 230000000340 anti-metabolite Effects 0.000 claims 2
- 229940125681 anticonvulsant agent Drugs 0.000 claims 2
- 239000001961 anticonvulsive agent Substances 0.000 claims 2
- 229940100197 antimetabolite Drugs 0.000 claims 2
- 239000002256 antimetabolite Substances 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 230000003115 biocidal effect Effects 0.000 claims 2
- 230000008512 biological response Effects 0.000 claims 2
- 230000009400 cancer invasion Effects 0.000 claims 2
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000005215 cycloalkylheteroaryl group Chemical group 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 238000009472 formulation Methods 0.000 claims 2
- 239000003862 glucocorticoid Substances 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000005549 heteroarylene group Chemical group 0.000 claims 2
- 239000005556 hormone Substances 0.000 claims 2
- 229940088597 hormone Drugs 0.000 claims 2
- 201000001881 impotence Diseases 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 230000009401 metastasis Effects 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000003607 modifier Substances 0.000 claims 2
- SDMMXCCXSAOATE-UHFFFAOYSA-N n,n-diethyl-3-[4-[1-[4-[4-fluoro-3-(trifluoromethyl)phenoxy]phenyl]-2-methylimidazol-4-yl]phenoxy]propan-1-amine Chemical compound C1=CC(OCCCN(CC)CC)=CC=C1C1=CN(C=2C=CC(OC=3C=C(C(F)=CC=3)C(F)(F)F)=CC=2)C(C)=N1 SDMMXCCXSAOATE-UHFFFAOYSA-N 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
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 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
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 230000008728 vascular permeability Effects 0.000 claims 2
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims 1
- JJLKXBIUMBGNNY-UHFFFAOYSA-N 2-(4-phenylphenyl)acetamide Chemical compound C1=CC(CC(=O)N)=CC=C1C1=CC=CC=C1 JJLKXBIUMBGNNY-UHFFFAOYSA-N 0.000 claims 1
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- AZIGXQSARFVFQL-UHFFFAOYSA-N 2-butyl-1-[4-(4-chlorophenoxy)phenyl]-4-[4-(2-pyrrolidin-1-ylethoxy)phenyl]imidazole Chemical compound CCCCC1=NC(C=2C=CC(OCCN3CCCC3)=CC=2)=CN1C(C=C1)=CC=C1OC1=CC=C(Cl)C=C1 AZIGXQSARFVFQL-UHFFFAOYSA-N 0.000 claims 1
- 125000005806 3,4,5-trimethoxybenzyl group Chemical group [H]C1=C(OC([H])([H])[H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1C([H])([H])* 0.000 claims 1
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 1
- KMMKMFFKTIARRO-UHFFFAOYSA-N 3-[4-[1-[4-(4-chlorophenoxy)phenyl]-2-(2-methylpropyl)imidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound C1=CC(OCCCN(CC)CC)=CC=C1C1=CN(C=2C=CC(OC=3C=CC(Cl)=CC=3)=CC=2)C(CC(C)C)=N1 KMMKMFFKTIARRO-UHFFFAOYSA-N 0.000 claims 1
- UPCYIFFPBGKRRP-UHFFFAOYSA-N 3-[4-[2,5-dibutyl-1-[4-(4-chlorophenoxy)phenyl]imidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OCCCN(CC)CC)=CC=2)=C(CCCC)N1C(C=C1)=CC=C1OC1=CC=C(Cl)C=C1 UPCYIFFPBGKRRP-UHFFFAOYSA-N 0.000 claims 1
- QVSUTSZHMYGEHS-UHFFFAOYSA-N 3-[4-[2-butyl-1-[4-(3-tert-butylphenoxy)phenyl]imidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OCCCN(CC)CC)=CC=2)=CN1C(C=C1)=CC=C1OC1=CC=CC(C(C)(C)C)=C1 QVSUTSZHMYGEHS-UHFFFAOYSA-N 0.000 claims 1
- GOKMRUDQKCCPKA-UHFFFAOYSA-N 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]-5-methylimidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OCCCN(CC)CC)=CC=2)=C(C)N1C(C=C1)=CC=C1OC1=CC=C(Cl)C=C1 GOKMRUDQKCCPKA-UHFFFAOYSA-N 0.000 claims 1
- PFTVDTSWWSHXGX-UHFFFAOYSA-N 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]-5-propylimidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OCCCN(CC)CC)=CC=2)=C(CCC)N1C(C=C1)=CC=C1OC1=CC=C(Cl)C=C1 PFTVDTSWWSHXGX-UHFFFAOYSA-N 0.000 claims 1
- JPHOJYZQKOQQRY-UHFFFAOYSA-N 3-[4-[2-butyl-1-[4-(4-fluorophenoxy)phenyl]imidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=NC(C=2C=CC(OCCCN(CC)CC)=CC=2)=CN1C(C=C1)=CC=C1OC1=CC=C(F)C=C1 JPHOJYZQKOQQRY-UHFFFAOYSA-N 0.000 claims 1
- KWQOOVPYNKDBSV-UHFFFAOYSA-N 3-[4-[2-butyl-1-[4-(4-methoxynaphthalen-1-yl)oxyphenyl]imidazol-4-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound C=1N(C=2C=CC(OC=3C4=CC=CC=C4C(OC)=CC=3)=CC=2)C(CCCC)=NC=1C1=CC=C(OCCCN(CC)CC)C=C1 KWQOOVPYNKDBSV-UHFFFAOYSA-N 0.000 claims 1
- CQTPANQYQUZPSJ-UHFFFAOYSA-N 3-[4-[4-[4-(3,3-diphenylpropoxy)phenyl]-2-(2-methylpropyl)imidazol-1-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound C1=CC(OCCCN(CC)CC)=CC=C1N1C(CC(C)C)=NC(C=2C=CC(OCCC(C=3C=CC=CC=3)C=3C=CC=CC=3)=CC=2)=C1 CQTPANQYQUZPSJ-UHFFFAOYSA-N 0.000 claims 1
- WAIZZRJKONWWLS-UHFFFAOYSA-N 3-[4-[4-[4-[2-(4-chlorophenyl)ethoxy]phenyl]-2-(2-methylpropyl)-5-propylimidazol-1-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCC1=C(C=2C=CC(OCCC=3C=CC(Cl)=CC=3)=CC=2)N=C(CC(C)C)N1C1=CC=C(OCCCN(CC)CC)C=C1 WAIZZRJKONWWLS-UHFFFAOYSA-N 0.000 claims 1
- KGJQQXDIGYEZJU-UHFFFAOYSA-N 3-[4-[5-butyl-4-[4-[2-(4-chlorophenyl)ethoxy]phenyl]-2-(2-methylpropyl)imidazol-1-yl]phenoxy]-n,n-diethylpropan-1-amine Chemical compound CCCCC1=C(C=2C=CC(OCCC=3C=CC(Cl)=CC=3)=CC=2)N=C(CC(C)C)N1C1=CC=C(OCCCN(CC)CC)C=C1 KGJQQXDIGYEZJU-UHFFFAOYSA-N 0.000 claims 1
- 125000006281 4-bromobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Br)C([H])([H])* 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 125000001318 4-trifluoromethylbenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])*)C(F)(F)F 0.000 claims 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 1
- 229940122041 Cholinesterase inhibitor Drugs 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 102100037907 High mobility group protein B1 Human genes 0.000 claims 1
- 101710168537 High mobility group protein B1 Proteins 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 102000001109 Leukocyte L1 Antigen Complex Human genes 0.000 claims 1
- 108010069316 Leukocyte L1 Antigen Complex Proteins 0.000 claims 1
- 208000011623 Obstructive Lung disease Diseases 0.000 claims 1
- 102100029812 Protein S100-A12 Human genes 0.000 claims 1
- 101710110949 Protein S100-A12 Proteins 0.000 claims 1
- 208000038016 acute inflammation Diseases 0.000 claims 1
- 230000006022 acute inflammation Effects 0.000 claims 1
- 239000000443 aerosol Substances 0.000 claims 1
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 230000000561 anti-psychotic effect Effects 0.000 claims 1
- 239000000935 antidepressant agent Substances 0.000 claims 1
- 229940005513 antidepressants 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
- 150000004283 biguanides Chemical class 0.000 claims 1
- 239000007795 chemical reaction product Substances 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 230000006020 chronic inflammation Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 230000036252 glycation Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 239000006208 topical dosage form Substances 0.000 claims 1
- 239000008009 topical excipient Substances 0.000 claims 1
- 0 CN(C)C(N(C)*)=O Chemical compound CN(C)C(N(C)*)=O 0.000 description 2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36198302P | 2002-03-05 | 2002-03-05 | |
| PCT/US2003/006749 WO2003075921A2 (en) | 2002-03-05 | 2003-03-05 | Mono- and bicyclic azole derivatives that inhibit the interaction of ligands with rage |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008271566A Division JP2009096806A (ja) | 2002-03-05 | 2008-10-22 | リガンドのｒａｇｅとの相互作用を阻害する単環式および二環式アゾール誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005525378A JP2005525378A (ja) | 2005-08-25 |
| JP2005525378A5 true JP2005525378A5 (https=) | 2007-12-06 |
| JP4481011B2 JP4481011B2 (ja) | 2010-06-16 |
Family
ID=27805104
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003574195A Expired - Lifetime JP4481011B2 (ja) | 2002-03-05 | 2003-03-05 | リガンドのｒａｇｅとの相互作用を阻害する単環式および二環式アゾール誘導体 |
| JP2008271566A Pending JP2009096806A (ja) | 2002-03-05 | 2008-10-22 | リガンドのｒａｇｅとの相互作用を阻害する単環式および二環式アゾール誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008271566A Pending JP2009096806A (ja) | 2002-03-05 | 2008-10-22 | リガンドのｒａｇｅとの相互作用を阻害する単環式および二環式アゾール誘導体 |
Country Status (10)
| Country | Link |
|---|---|
| US (5) | US7361678B2 (https=) |
| EP (2) | EP2324830A1 (https=) |
| JP (2) | JP4481011B2 (https=) |
| CN (3) | CN101597262A (https=) |
| AT (1) | ATE529110T1 (https=) |
| AU (2) | AU2007202350B2 (https=) |
| CA (1) | CA2476594C (https=) |
| DK (1) | DK1482931T3 (https=) |
| ES (1) | ES2373875T3 (https=) |
| WO (1) | WO2003075921A2 (https=) |
Families Citing this family (84)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6303321B1 (en) | 1999-02-11 | 2001-10-16 | North Shore-Long Island Jewish Research Institute | Methods for diagnosing sepsis |
| CN1235583C (zh) * | 2001-03-05 | 2006-01-11 | 特兰斯泰克制药公司 | 用作治疗剂的苯并咪唑衍生物 |
| US7304034B2 (en) | 2001-05-15 | 2007-12-04 | The Feinstein Institute For Medical Research | Use of HMGB fragments as anti-inflammatory agents |
| JP4120586B2 (ja) | 2002-01-18 | 2008-07-16 | アステラス製薬株式会社 | ２−アシルアミノチアゾール誘導体又はその塩 |
| DK1482931T3 (da) * | 2002-03-05 | 2011-12-19 | Transtech Pharma Inc | Mono- og bicycliske azolderivater der inhiberer interaktionen af ligander med RAGE |
| CA2514363A1 (en) * | 2003-02-12 | 2004-08-26 | Transtech Pharma, Inc. | Substituted azole derivatives as therapeutic agents |
| WO2005000295A1 (en) * | 2003-05-20 | 2005-01-06 | Transtech Pharma, Inc. | Rage antagonists as agents to reverse amyloidosis and diseases associated therewith |
| US7696169B2 (en) | 2003-06-06 | 2010-04-13 | The Feinstein Institute For Medical Research | Inhibitors of the interaction between HMGB polypeptides and toll-like receptor 2 as anti-inflammatory agents |
| AU2004272607B2 (en) | 2003-09-11 | 2008-11-06 | Cornerstone Therapeutics Inc. | Monoclonal antibodies against HMGB1 |
| CA2551909C (en) * | 2004-02-12 | 2011-10-11 | Transtech Pharma, Inc. | Substituted azole derivatives, compositions, and methods of use |
| JP2007527920A (ja) * | 2004-03-08 | 2007-10-04 | ワイス | イオンチャンネルモジュレーター |
| EP1723120A4 (en) * | 2004-03-08 | 2007-09-26 | Wyeth Corp | MODULATORS OF THE ION CHANNEL FUNCTION |
| JP4607950B2 (ja) * | 2004-03-18 | 2011-01-05 | トランス テック ファーマ，インコーポレイテッド | 蛍光偏光アッセイ |
| KR20060133084A (ko) | 2004-04-03 | 2006-12-22 | 아스트라제네카 아베 | 치료제 |
| EP1771565B1 (en) * | 2004-07-20 | 2012-09-05 | The Feinstein Institute for Medical Research | Rage protein derivatives |
| SG161242A1 (en) * | 2004-08-03 | 2010-05-27 | Transtech Pharma Inc | Rage fusion proteins and methods of use |
| US20060223849A1 (en) | 2005-03-14 | 2006-10-05 | Mjalli Adnan M | Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors |
| WO2006119510A2 (en) * | 2005-05-04 | 2006-11-09 | Receptor Biologix, Inc. | Isoforms of receptor for advanced glycation end products (rage) and methods of identifying and using same |
| BRPI0612287A8 (pt) * | 2005-06-27 | 2019-01-22 | Exelixis Inc | composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear |
| WO2007008942A2 (en) * | 2005-07-11 | 2007-01-18 | Aerie Pharmaceuticals, Inc. | Phenylamino-acetic acid [1-(pyridin-4-yl)-methylidene]-hydrazide derivatives and related compounds as modulators of g protein-coupled receptor kinases for the treatment of eye diseases |
| US7470787B2 (en) * | 2005-07-11 | 2008-12-30 | Aerie Pharmaceuticals, Inc. | Isoquinoline compounds |
| JP5133889B2 (ja) * | 2005-09-21 | 2013-01-30 | デコード ジェネティクス イーエイチエフ | 炎症治療のためのビアリール基置換複素環ｌｔａ４ｈ阻害剤 |
| JP5301999B2 (ja) * | 2005-10-31 | 2013-09-25 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｃｅｔｐ阻害薬 |
| NZ569329A (en) | 2006-01-30 | 2011-09-30 | Transtech Pharma Inc | Substituted imidazole derivatives and their use as PTPase inhibitors |
| CA2641880C (en) | 2006-02-10 | 2014-09-09 | Summit Corporation Plc | Treatment of duchenne muscular dystrophy |
| FR2900404B1 (fr) * | 2006-04-27 | 2008-07-18 | Sod Conseils Rech Applic | Nouveaux derives d'imidazoles, leur preparation et leur utilisation en tant que medicament |
| WO2008130368A2 (en) * | 2006-06-23 | 2008-10-30 | Paratek Pharmaceuticals, Inc. | Transcription factor modulating compounds and methods of use thereof |
| TWI386405B (zh) | 2006-09-05 | 2013-02-21 | 咪唑衍生物 | |
| ES2729424T3 (es) | 2006-09-20 | 2019-11-04 | Aerie Pharmaceuticals Inc | Inhibidores de Rho cinasa |
| US8012955B2 (en) * | 2006-12-28 | 2011-09-06 | Rigel Pharmaceuticals, Inc. | N-substituted-heterocycloalkyloxybenzamide compounds and methods of use |
| US8455513B2 (en) * | 2007-01-10 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-aminoisoquinoline compounds |
| US20080186971A1 (en) * | 2007-02-02 | 2008-08-07 | Tarari, Inc. | Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic |
| CA2681864A1 (en) * | 2007-04-05 | 2008-10-16 | Transtech Pharma, Inc. | Crystalline forms i and ii of [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1h-imidazol-4-yl}-phenoxy)-propyl]-diethyl-amine |
| US20100254983A1 (en) * | 2007-06-07 | 2010-10-07 | Ann Marie Schmidt | Uses of rage antagonists for treating obesity and related diseases |
| CA2685540C (en) * | 2007-08-03 | 2018-10-16 | Graham Michael Wynne | Drug combinations for the treatment of duchenne muscular dystrophy |
| GB0715937D0 (en) * | 2007-08-15 | 2007-09-26 | Vastox Plc | Method of treatment og duchenne muscular dystrophy |
| US8138168B1 (en) | 2007-09-26 | 2012-03-20 | Takeda Pharmaceutical Company Limited | Renin inhibitors |
| CA2709203A1 (en) * | 2007-12-13 | 2009-06-18 | Siena Biotech S.P.A. | Hedgehog pathway antagonists and therapeutic applications thereof |
| US8455514B2 (en) * | 2008-01-17 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-and 7-amino isoquinoline compounds and methods for making and using the same |
| CN101932306A (zh) * | 2008-02-05 | 2010-12-29 | 阿特维斯集团公司 | 阿仑膦酸盐制剂、其制备方法和使用方法 |
| WO2009099736A2 (en) * | 2008-02-06 | 2009-08-13 | Lead Therapeutics, Inc. | Benzoxazole carboxamide inhibitors of poly(adp-ribose)polymerase (parp) |
| US8188131B2 (en) | 2008-02-07 | 2012-05-29 | Massachusetts Eye & Ear Infirmary | Compounds that enhance Atoh1 expression |
| US8450344B2 (en) | 2008-07-25 | 2013-05-28 | Aerie Pharmaceuticals, Inc. | Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds |
| US8436025B2 (en) * | 2008-09-19 | 2013-05-07 | CompleGen Partners, Inc. | Compounds and methods for PKC theta inhibition |
| WO2010040661A1 (en) * | 2008-10-09 | 2010-04-15 | F. Hoffmann-La Roche Ag | Modulators for amyloid beta |
| WO2010050445A1 (ja) * | 2008-10-27 | 2010-05-06 | 武田薬品工業株式会社 | 二環性化合物 |
| US20100278835A1 (en) * | 2009-03-10 | 2010-11-04 | Astrazeneca Uk Limited | Novel compounds 660 |
| JP2012525389A (ja) | 2009-04-27 | 2012-10-22 | ハイ ポイント ファーマシューティカルズ，リミティド ライアビリティ カンパニー | 置換イソキノリン誘導体、医薬組成物、及びβ−セクレターゼ阻害剤としての使用方法 |
| EP3828172A1 (en) | 2009-05-01 | 2021-06-02 | Aerie Pharmaceuticals, Inc. | Dual mechanism inhibitors for the treatment of disease |
| JP5805646B2 (ja) * | 2009-09-30 | 2015-11-04 | ブイティーブイ・セラピューティクス・エルエルシー | アルツハイマー病の治療のための置換イミダゾール誘導体 |
| WO2011103091A1 (en) | 2010-02-18 | 2011-08-25 | Transtech Pharma, Inc. | Phenyl-heteroaryl derivatives and methods of use thereof |
| EP2549874A4 (en) | 2010-03-23 | 2013-10-02 | High Point Pharmaceuticals Llc | SUBSTITUTED IMIDAZOLE [1,2-B] PYRIDAZINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS |
| WO2013074820A1 (en) | 2011-11-16 | 2013-05-23 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Immunogenic tumor associated stromal cell antigen peptides and methods of their use |
| KR101415174B1 (ko) * | 2012-04-26 | 2014-07-04 | (주) 메디프론디비티 | 신규한 벤조옥사졸계 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 ｒａｇｅ 수용체 관련 질환의 예방 또는 치료용 약학적 조성물 |
| NZ705813A (en) * | 2012-10-05 | 2018-02-23 | Vtv Therapeutics Llc | Treatment of mild and moderate alzheimer’s disease |
| US9717710B2 (en) | 2012-10-05 | 2017-08-01 | Vtv Therapeutics Llc | Treatment of mild and moderate Alzheimer's disease |
| ES2852377T3 (es) | 2013-03-15 | 2021-09-13 | Aerie Pharmaceuticals Inc | Sales dimesilato de 4-(3-amino-1-(isoquinolin-6-ilamino)-1-oxopropan-2-il)bencilo, sus combinaciones con prostaglandinas y el uso de las mismas en el tratamiento de trastornos oculares |
| US9353078B2 (en) | 2013-10-01 | 2016-05-31 | New York University | Amino, amido and heterocyclic compounds as modulators of rage activity and uses thereof |
| WO2015175845A1 (en) * | 2014-05-15 | 2015-11-19 | Peloton Therapeutics, Inc. | Benzimidazole derivatives and uses thereof |
| EP2991990B1 (en) * | 2014-05-23 | 2017-02-01 | Active Biotech AB | Novel compounds useful as s100-inhibitors |
| EP3015459A1 (en) * | 2014-10-30 | 2016-05-04 | Sanofi | Benzylhydroxyde derivatives, preparation thereof and therapeutic use thereof |
| EP3822291A1 (en) | 2015-06-10 | 2021-05-19 | The Broad Institute Inc. | Antibodies, compounds and screens for identifying and treating cachexia or pre-cachexia |
| KR102579582B1 (ko) | 2015-11-17 | 2023-09-15 | 에어리 파마슈티컬즈, 인코포레이티드 | 키나아제 억제제 및 이의 중간체의 제조 방법 |
| US9643927B1 (en) | 2015-11-17 | 2017-05-09 | Aerie Pharmaceuticals, Inc. | Process for the preparation of kinase inhibitors and intermediates thereof |
| AU2017225537B2 (en) * | 2016-03-01 | 2020-07-30 | Vtv Therapeutics Llc | Piperidine derivative and methods of use thereof |
| WO2017184547A1 (en) | 2016-04-18 | 2017-10-26 | New York University | Quinoline compounds as modulators of rage activity and uses thereof |
| KR102568079B1 (ko) | 2016-08-31 | 2023-08-17 | 에어리 파마슈티컬즈, 인코포레이티드 | 안과용 조성물 |
| AU2018243687C1 (en) | 2017-03-31 | 2020-12-24 | Alcon Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
| CN109896986B (zh) * | 2017-12-07 | 2022-03-15 | 中国医学科学院药物研究所 | 木脂素类天然产物4-o-甲基三白草醇的结构简化物，其制法和其药物组合物与用途 |
| WO2019190822A1 (en) | 2018-03-28 | 2019-10-03 | Vtv Therapeutics Llc | Crystalline forms of [3-(4- {2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1h-imidazol-4-yl} -phenoxy)-propyl]-diethyl-amine |
| WO2019190823A1 (en) | 2018-03-28 | 2019-10-03 | Vtv Therapeutics Llc | Pharmaceutically acceptable salts of [3-(4- {2-butyl-1-[4-(4-chlorophenoxy)-phenyl]-1h-imidazol-4-yl} -phenoxy)-propyl]-diethyl-amine |
| CA3112391A1 (en) | 2018-09-14 | 2020-03-19 | Aerie Pharmaceuticals, Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
| WO2020076668A1 (en) | 2018-10-10 | 2020-04-16 | Vtv Therapeutics Llc | Metabolites of [3-(4-{2-butyl-l-[4-(4-chloro-phenoxy)-phenyl]-lh-imidazol-4-yl } -phen ox y)-prop yl] -diethyl-amine |
| WO2020086388A1 (en) | 2018-10-22 | 2020-04-30 | Vtv Therapeutics Llc | Glucokinase activator compositions for the treatment of cognitive impairment |
| US20220296604A1 (en) * | 2019-08-08 | 2022-09-22 | New York University | Indole compounds as modulators of rage activity and uses thereof |
| KR102532692B1 (ko) * | 2021-03-15 | 2023-05-16 | (주)피알지에스앤텍 | 신경섬유종증 2형 증후군 예방 또는 치료용 조성물 |
| CN115594642B (zh) * | 2021-06-28 | 2024-12-27 | 广西医科大学 | 阿齐瑞格三氮唑衍生物及其抗乳腺癌用途 |
| EP4558141A4 (en) * | 2022-07-20 | 2025-08-06 | Hadasit Medical Res Services&Development Ltd | COMBINATION FOR THE TREATMENT OF RETINAL DISEASE |
| KR102896914B1 (ko) * | 2022-12-27 | 2025-12-09 | (주)피알지에스앤텍 | 신규 화합물 제조방법 |
| US11648235B1 (en) * | 2022-12-30 | 2023-05-16 | Cantex Pharmaceuticals, Inc. | Treatment of glioblastoma |
| EP4676453A1 (en) | 2023-03-08 | 2026-01-14 | Institut National de la Santé et de la Recherche Médicale | Methods for the treatment of food allergy |
| CN116785311A (zh) * | 2023-07-17 | 2023-09-22 | 华中科技大学同济医学院附属梨园医院 | Rage基因表达拮抗剂的应用及包含该拮抗剂的药物 |
| WO2025146850A1 (ko) * | 2024-01-05 | 2025-07-10 | (주)피알지에스앤텍 | 신규 화합물 제조방법 |
| CN118615283A (zh) * | 2024-05-31 | 2024-09-10 | 中南大学湘雅三医院 | Ttp488在制备抑制淋巴细胞耗竭的药物中的应用 |
Family Cites Families (106)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US552317A (en) * | 1895-12-31 | Cigar-mold | ||
| US361983A (en) | 1887-04-26 | Edwin f | ||
| NL7017486A (https=) * | 1969-12-15 | 1971-06-17 | ||
| US3708598A (en) * | 1970-07-10 | 1973-01-02 | Sandoz Ag | Substituted 2,4-(omega-aminoalkoxy)phenyl imidazoles as cholesterol reducing agents |
| US4024271A (en) * | 1971-03-09 | 1977-05-17 | Smith Kline & French Laboratories Limited | Pharmacologically active guanidine compounds |
| IL55573A0 (en) | 1977-10-03 | 1978-12-17 | Erba Carlo Spa | Substituted n-(ss-alkoxy-ethyl)-n-(4-phenoxybenzyl)-dichloroacetamides and process for their preparation |
| US4356108A (en) * | 1979-12-20 | 1982-10-26 | The Mead Corporation | Encapsulation process |
| US4265874A (en) * | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
| US4356106A (en) * | 1980-05-09 | 1982-10-26 | United Kingdom Atomic Energy Authority | Cerium compounds |
| US5202424A (en) * | 1984-03-19 | 1993-04-13 | The Rockefeller University | Mesangial cell-derived receptors for advanced glycosylation endproducts and uses thereof |
| US5585344A (en) * | 1984-03-19 | 1996-12-17 | The Rockefeller University | Liver-derived receptors for advanced glycosylation endproducts and uses thereof |
| US5358960A (en) * | 1984-03-19 | 1994-10-25 | The Rockefeller University | Method for inhibiting advanced glycosylation of proteins using aminosubstituted imidazoles |
| US4873313A (en) * | 1985-01-18 | 1989-10-10 | Beckman Research Institute Of City Of Hope | Specific hybridoma cell line and monocolonal antibodies produced from such specific hybridoma cell line and method of using such monoclonal antibodies to detect carcinoembryonic antigens |
| US4963539A (en) * | 1987-09-10 | 1990-10-16 | E. R. Squibb & Sons, Inc. | Phosphonate and phosphonamide endopeptidase inhibitors |
| US4963422A (en) * | 1987-10-28 | 1990-10-16 | National Starch And Chemical Investment Holding Corporation | Ethylene vinyl acetate alkyl acrylate compositions for flocking adhesives |
| DE3815234A1 (de) * | 1988-05-05 | 1989-11-16 | Sueddeutsche Kalkstickstoff | Beschleuniger fuer cyanamid enthaltende epoxidhaerter |
| EP0352581A3 (de) * | 1988-07-28 | 1990-07-04 | F. Hoffmann-La Roche Ag | Aethylendiaminmonoamid-Derivate |
| US5166214A (en) * | 1988-12-05 | 1992-11-24 | Du Pont Merck Pharmaceutical Company | Use of imidazoles for the treatment of atherosclerosis |
| US5318984A (en) * | 1988-12-05 | 1994-06-07 | The Du Pont Merck Pharmaceutical Company | Imidazoles for the treatment of atherosclerosis |
| US5153226A (en) * | 1989-08-31 | 1992-10-06 | Warner-Lambert Company | Acat inhibitors for treating hypocholesterolemia |
| US5192785A (en) * | 1989-09-03 | 1993-03-09 | A. H. Robins Company, Incorporated | Sulfamates as antiglaucoma agents |
| DE4015535A1 (de) * | 1990-05-15 | 1991-11-21 | Basf Ag | Verfahren zur herstellung von n-substituierten imidazolen |
| US5192789A (en) | 1991-01-18 | 1993-03-09 | Hoechst-Roussel Pharmaceuticals Incorporated | Substituted 1,2,3,4-tetrahydrocyclopent[b]indoles, 1,2,3,3a,4,8a-hexahydrocyclopent[b]indoles and related compounds |
| US5500463A (en) * | 1991-03-11 | 1996-03-19 | Nippon Paint Co., Ltd. | Aqueous resin composition and method for forming coating film on can body |
| MX9205392A (es) | 1991-10-29 | 1993-04-01 | Du Pont | Triazolcarbozamidas herbicidas y procedimiento para su obtencion. |
| CA2085844A1 (en) * | 1991-12-27 | 1993-06-28 | Nobuyuki Hamanaka | Fused benzeneoxyacetic acid derivatives |
| DE4222980A1 (de) * | 1992-07-13 | 1994-01-20 | Cassella Ag | Verwendung von 2-(N-(2-Aminoethyl)amino)-essigsäure-derivaten |
| JPH0656665A (ja) | 1992-08-03 | 1994-03-01 | Nippon Chemiphar Co Ltd | イミダゾール誘導体を含有する胃溶性抗潰瘍剤 |
| JPH0680656A (ja) | 1992-09-03 | 1994-03-22 | Mitsui Petrochem Ind Ltd | 光学活性エポキシドの製造方法 |
| JPH07304748A (ja) | 1993-06-29 | 1995-11-21 | Nissan Chem Ind Ltd | アルドキシム誘導体および農園芸用殺菌剤 |
| US5523317A (en) * | 1993-07-05 | 1996-06-04 | Nippon Chemiphar Co., Ltd. | Method of reducing blood pressure |
| JPH0770083A (ja) | 1993-07-05 | 1995-03-14 | Nippon Chemiphar Co Ltd | イミダゾール誘導体を有効成分とする血圧降下剤 |
| IL110296A (en) * | 1993-07-16 | 1999-12-31 | Smithkline Beecham Corp | Imidazole compounds process for their preparation and pharmaceutical compositions containing them |
| NZ274074A (en) | 1993-10-01 | 1997-11-24 | Merrell Pharma Inc | Various dipeptide derivatives having a reduced carboxy group, the aldehyde being optionally substituted; pharmaceutical compositions |
| CA2186606A1 (en) * | 1994-03-29 | 1995-10-05 | Edward B. Nelson | Treatment of atherosclerosis with angiotensin ii receptor blocking imidazoles |
| GB9406573D0 (en) * | 1994-03-31 | 1994-05-25 | Merck Sharp & Dohme | Medicaments |
| GB9409150D0 (en) | 1994-05-09 | 1994-06-29 | Black James Foundation | Cck and gastrin receptor ligands |
| US5597845A (en) | 1994-06-20 | 1997-01-28 | Merrell Pharmaceuticals Inc. | Substituted alkyldiamine derivatives |
| US5939526A (en) * | 1995-03-21 | 1999-08-17 | Ludwig Institute For Cancer Research | Isolated RAGE-1 derived peptides which complex with HLA-B7 molecules and uses thereof |
| JP3950170B2 (ja) | 1995-04-13 | 2007-07-25 | アベンティス・ファーマスーティカルズ・インコーポレイテッド | タキキニン受容体アンタゴニスト活性を有する新規な置換されたピペラジン誘導体 |
| JP3849157B2 (ja) | 1995-08-01 | 2006-11-22 | 東ソー株式会社 | ２−イミダゾリン類の製造法 |
| US6228858B1 (en) | 1995-09-12 | 2001-05-08 | University Of Kansas Medical Center | Advanced glycation end-product intermediaries and post-amadori inhibition |
| US5843904A (en) | 1995-12-20 | 1998-12-01 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1βconverting enzyme |
| AU1832797A (en) | 1996-01-26 | 1997-08-20 | Trustees Of Columbia University In The City Of New York, The | A polypeptide from lung extract which binds amyloid-beta peptide |
| US6673927B2 (en) * | 1996-02-16 | 2004-01-06 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | Farnesyl transferase inhibitors |
| WO1997039121A1 (en) | 1996-04-16 | 1997-10-23 | Schering Aktiengesellschaft | Advanced glycosylation end-product receptor peptides and uses therefor |
| US5864018A (en) * | 1996-04-16 | 1999-01-26 | Schering Aktiengesellschaft | Antibodies to advanced glycosylation end-product receptor polypeptides and uses therefor |
| US5688653A (en) * | 1996-06-27 | 1997-11-18 | The Picower Institute For Medical Research | 3-alkylamino-2-hydroxy-4-hydroxymethyl-2-cyclopenten-1-one advanced glycosylation endproducts and methods of use therefor |
| US6416733B1 (en) * | 1996-10-07 | 2002-07-09 | Bristol-Myers Squibb Pharma Company | Radiopharmaceuticals for imaging infection and inflammation |
| US6790443B2 (en) | 1996-11-22 | 2004-09-14 | The Trustees Of Columbia University In The City Of New York | Method for treating symptoms of diabetes |
| US7258857B2 (en) * | 1996-11-22 | 2007-08-21 | The Trustees Of Columbia University In The City Of New York | Rage-related methods for treating inflammation |
| US6555651B2 (en) | 1997-10-09 | 2003-04-29 | The Trustees Of Columbia University In The City Of New York | Ligand binding site of rage and uses thereof |
| US6201002B1 (en) * | 1997-01-10 | 2001-03-13 | Merck & Co., Inc. | Method for reducing mortality with an angiotensin II antagonist |
| US5962535A (en) * | 1997-01-17 | 1999-10-05 | Takeda Chemical Industries, Ltd. | Composition for alzheimer's disease |
| US6004958A (en) | 1997-02-05 | 1999-12-21 | Fox Chase Cancer Center | Compounds and methods for therapeutic intervention in preventing diabetic complications and procedures for assessing a diabetic's risk of developing complications and determining the efficacy of therapeutic intervention |
| JP2001509814A (ja) * | 1997-02-18 | 2001-07-24 | アメリカン・ホーム・プロダクツ・コーポレイション | ４−アミノアルコキシ−１ｈ−ベンゾイミダゾール誘導体、それらの調製およびそれらのドパミン自己受容体（ｄ▲下２▼）作動薬としての使用 |
| US6100098A (en) * | 1997-02-18 | 2000-08-08 | Mcgill University | Anti-AGE IgG and uses thereof for the diagnosis of severe disease |
| US6197791B1 (en) * | 1997-02-27 | 2001-03-06 | American Cyanamid Company | N-hdroxy-2-(alkyl, aryl, or heteroaryl, sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors |
| YU40999A (sh) | 1997-02-27 | 2002-06-19 | American Cyanamid Company | N-hidroksi-2-(alkil,aril ili heteroaril sulfanil,sulfinil ili sulfonil)-3-supstituisani alkil,aril ili heteroarilamidi, kao inhibitori za matrične metaloproteinaze |
| US5817823A (en) * | 1997-04-17 | 1998-10-06 | Sepracor Inc. | Method for synthesizing 2-substituted imidazoles |
| US7101838B2 (en) | 1997-08-05 | 2006-09-05 | The Trustees Of Columbia University In The City Of New York | Method to prevent accelerated atherosclerosis using (sRAGE) soluble receptor for advanced glycation endproducts |
| FR2767527B1 (fr) * | 1997-08-25 | 1999-11-12 | Pf Medicament | Derives de piperazines indoliques, utiles comme medicaments et procede de preparation |
| AU744939B2 (en) | 1997-09-26 | 2002-03-07 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| HUP9902721A2 (hu) * | 1997-11-25 | 1999-12-28 | The Procter & Gamble Co. | Tömény textillágyító készítmény és ehhez alkalmazható magas telítetlenségű textillágyító vegyület |
| FR2773800B1 (fr) * | 1998-01-20 | 2000-02-18 | Synthelabo | Derives de benzimidazole, leur procede de preparation et leur application en therapeutique |
| CA2318778A1 (en) * | 1998-02-25 | 1999-09-02 | Merck & Co., Inc. | Method for decreasing qt dispersion or inhibiting the progression of qt dispersion with an angiotensin ii receptor antagonist |
| ATE346035T1 (de) | 1998-03-31 | 2006-12-15 | Vertex Pharma | Inhibitoren von serin proteasen, insbesondere von hepatitis c virus ns3 protease |
| US6465422B1 (en) | 1998-04-17 | 2002-10-15 | The Trustees Of Columbia University In The City Of New York | Method for inhibiting tumor invasion or spreading in a subject |
| FR2780404B1 (fr) * | 1998-06-26 | 2001-04-13 | Adir | Nouveaux derives de nitrone, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| AU1199600A (en) * | 1998-10-02 | 2000-04-26 | Board Of Trustees Of The University Of Illinois, The | Estrogen receptor ligands |
| US6753150B2 (en) | 1998-10-05 | 2004-06-22 | The Trustees Of Columbia University In The City Of New York | Method for determining whether a compound is capable of inhibiting the interaction of a peptide with rage |
| AU765719B2 (en) | 1998-10-06 | 2003-09-25 | Trustees Of Columbia University In The City Of New York, The | Extracellular novel rage binding protein (EN-RAGE) and uses thereof |
| CO5210925A1 (es) * | 1998-11-17 | 2002-10-30 | Novartis Ag | Derivados de diamino nitroguanidina tetrasustituidos |
| DE19859809A1 (de) | 1998-12-23 | 2000-06-29 | Henkel Kgaa | Mittel zum Färben von keratinhaltigen Fasern |
| NZ511674A (en) * | 1998-12-23 | 2003-11-28 | Du Pont Pharm Co | Nitrogen containing heterobicycles as factor Xa inhibitors |
| EP1210087A2 (en) | 1999-04-29 | 2002-06-05 | City of Hope | Pentoxifylline, pioglitazone and metformin are inhibitors of formation of advanced glycation endproducts (age's) |
| IT1313601B1 (it) * | 1999-08-05 | 2002-09-09 | Isagro Ricerca Srl | Fenilpirazoli ad attivita' erbicida |
| EP1237849A1 (en) | 1999-11-05 | 2002-09-11 | University College London | Activators of soluble guanylate cyclase |
| US7423177B2 (en) | 2001-03-05 | 2008-09-09 | Transtech Pharma, Inc. | Carboxamide derivatives as therapeutic agents |
| US6613801B2 (en) * | 2000-05-30 | 2003-09-02 | Transtech Pharma, Inc. | Method for the synthesis of compounds of formula I and their uses thereof |
| IL153246A0 (en) * | 2000-06-28 | 2003-07-06 | Astrazeneca Ab | Substituted quinazoline derivatives and their use as inhibitors |
| WO2002000648A1 (en) * | 2000-06-28 | 2002-01-03 | Ssp Co., Ltd. | Imidazole derivatives or salts thereof and drugs containing the derivatives or the salts |
| US6541639B2 (en) * | 2000-07-26 | 2003-04-01 | Bristol-Myers Squibb Pharma Company | Efficient ligand-mediated Ullmann coupling of anilines and azoles |
| US6825164B1 (en) * | 2000-08-14 | 2004-11-30 | The Trustees Of Columbia University In The City Of New York | Method to increase cerebral blood flow in amyloid angiopathy |
| AU2002213477A1 (en) * | 2000-10-16 | 2002-04-29 | Chugai Seiyaku Kabushiki Kaisha | Process for preparation of n-substituted 2-sulfanylimidazoles |
| US6441064B1 (en) * | 2000-11-01 | 2002-08-27 | Air Products And Chemicals, Inc. | Imidazole-phosphoric acid salts as accelerators for dicyandiamide in one-component epoxy compositions |
| CN1235583C (zh) | 2001-03-05 | 2006-01-11 | 特兰斯泰克制药公司 | 用作治疗剂的苯并咪唑衍生物 |
| JP2003012690A (ja) | 2001-07-03 | 2003-01-15 | Mitsui Chemicals Inc | 置換イミダゾール誘導体又は置換ベンズイミダゾール誘導体を用いたヌクレオチドの製造法 |
| JP2003040888A (ja) | 2001-07-30 | 2003-02-13 | Sankyo Co Ltd | イミダゾール誘導体 |
| FR2829765A1 (fr) | 2001-09-14 | 2003-03-21 | Lipha | Derives imidazolylalkoxylarylalcanoiques leurs applications en therapeutique |
| WO2003053922A2 (en) | 2001-12-19 | 2003-07-03 | Merck & Co., Inc. | Heteroaryl substituted imidazole modulators of metabotropic glutamate receptor-5 |
| DK1482931T3 (da) * | 2002-03-05 | 2011-12-19 | Transtech Pharma Inc | Mono- og bicycliske azolderivater der inhiberer interaktionen af ligander med RAGE |
| US7026312B2 (en) | 2002-03-14 | 2006-04-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof |
| AU2003216579A1 (en) | 2002-04-12 | 2003-10-27 | Pfizer Inc. | Imidazole compounds as anti-inflammatory and analgesic agents |
| JP2003313172A (ja) | 2002-04-23 | 2003-11-06 | Tosoh Corp | Ｎ−置換イミダゾール化合物の製造方法 |
| JP4529342B2 (ja) | 2002-04-23 | 2010-08-25 | 東ソー株式会社 | 環状アミジニウム有機酸塩の製造方法 |
| US7077873B2 (en) | 2002-09-10 | 2006-07-18 | L'Oréal, SA | Composition for the dyeing of human keratinous fibres comprising a monocationic monoazo dye |
| TW200410701A (en) | 2002-10-15 | 2004-07-01 | Novartis Ag | Method of administering bisphosphonates |
| AU2003302106A1 (en) | 2002-11-21 | 2004-06-15 | Vicore Pharma Ab | New tricyclic angiotensin ii agonists |
| JP2004221557A (ja) | 2002-12-25 | 2004-08-05 | Sanyo Chem Ind Ltd | 電解液 |
| WO2004077711A2 (en) * | 2003-02-24 | 2004-09-10 | Hawe William R | System, method and apparatus for ascertaining a dynamic attribute of a system |
| CA2520863A1 (en) | 2003-04-03 | 2004-10-14 | Merck & Co., Inc. | 4-ring imidazole derivatives as modulators of metabotropic glutamate receptor-5 |
| WO2005000295A1 (en) * | 2003-05-20 | 2005-01-06 | Transtech Pharma, Inc. | Rage antagonists as agents to reverse amyloidosis and diseases associated therewith |
| ATE526314T1 (de) | 2003-08-26 | 2011-10-15 | Ecole Polytech | Ionische flüssigkeiten basierend auf imidazoliumsalzen mit einer nitrilfunktionalität |
| DE102004050176A1 (de) * | 2004-09-20 | 2006-03-23 | Universität Duisburg-Essen | Optoelektronisches Bauelement und Verfahren zum Steuern von Tunnelelektronenströmen durch Photonen |
| CA2484381C (en) * | 2004-10-08 | 2013-03-19 | Anne Marie Sedgwick | Supporting device |
-
2003
- 2003-03-05 DK DK03713918.5T patent/DK1482931T3/da active
- 2003-03-05 JP JP2003574195A patent/JP4481011B2/ja not_active Expired - Lifetime
- 2003-03-05 AT AT03713918T patent/ATE529110T1/de active
- 2003-03-05 WO PCT/US2003/006749 patent/WO2003075921A2/en not_active Ceased
- 2003-03-05 CN CNA2009101508570A patent/CN101597262A/zh active Pending
- 2003-03-05 CN CN200910150500A patent/CN101613321A/zh active Pending
- 2003-03-05 EP EP10179011A patent/EP2324830A1/en not_active Withdrawn
- 2003-03-05 CA CA2476594A patent/CA2476594C/en not_active Expired - Fee Related
- 2003-03-05 CN CNB038052040A patent/CN100525763C/zh not_active Expired - Fee Related
- 2003-03-05 ES ES03713918T patent/ES2373875T3/es not_active Expired - Lifetime
- 2003-03-05 US US10/382,203 patent/US7361678B2/en not_active Expired - Lifetime
- 2003-03-05 EP EP03713918A patent/EP1482931B1/en not_active Expired - Lifetime
-
2006
- 2006-08-28 US US11/511,163 patent/US7714013B2/en not_active Expired - Lifetime
-
2007
- 2007-05-03 US US11/800,085 patent/US7737285B2/en not_active Expired - Lifetime
- 2007-05-24 AU AU2007202350A patent/AU2007202350B2/en not_active Ceased
-
2008
- 2008-10-22 JP JP2008271566A patent/JP2009096806A/ja active Pending
-
2009
- 2009-07-13 AU AU2009202814A patent/AU2009202814B2/en not_active Ceased
-
2010
- 2010-05-05 US US12/799,971 patent/US20100256119A1/en not_active Abandoned
-
2011
- 2011-10-10 US US13/270,208 patent/US20120088778A1/en not_active Abandoned
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