JP2006522119A5 - - Google Patents
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- JP2006522119A5 JP2006522119A5 JP2006509028A JP2006509028A JP2006522119A5 JP 2006522119 A5 JP2006522119 A5 JP 2006522119A5 JP 2006509028 A JP2006509028 A JP 2006509028A JP 2006509028 A JP2006509028 A JP 2006509028A JP 2006522119 A5 JP2006522119 A5 JP 2006522119A5
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- Prior art keywords
- och
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- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 416
- 125000001931 aliphatic group Chemical group 0.000 claims 143
- 229910052757 nitrogen Inorganic materials 0.000 claims 109
- -1 2-methoxy-phenoxy Chemical group 0.000 claims 95
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 91
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 85
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 82
- 229910052731 fluorine Inorganic materials 0.000 claims 81
- 239000000203 mixture Substances 0.000 claims 80
- 229910052801 chlorine Inorganic materials 0.000 claims 75
- 125000003118 aryl group Chemical group 0.000 claims 74
- 229910052717 sulfur Inorganic materials 0.000 claims 63
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 62
- 125000005842 heteroatom Chemical group 0.000 claims 62
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 61
- 229910052794 bromium Inorganic materials 0.000 claims 61
- 229910052760 oxygen Chemical group 0.000 claims 61
- 239000001301 oxygen Chemical group 0.000 claims 61
- 239000011593 sulfur Substances 0.000 claims 59
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 58
- 125000002950 monocyclic group Chemical group 0.000 claims 55
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 51
- 229910052739 hydrogen Inorganic materials 0.000 claims 49
- 239000001257 hydrogen Substances 0.000 claims 49
- 125000001072 heteroaryl group Chemical group 0.000 claims 47
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 47
- 229910052736 halogen Inorganic materials 0.000 claims 45
- 150000002367 halogens Chemical class 0.000 claims 45
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 45
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 44
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 43
- 229910004013 NO 2 Inorganic materials 0.000 claims 42
- 125000003386 piperidinyl group Chemical group 0.000 claims 42
- 229920006395 saturated elastomer Polymers 0.000 claims 42
- 125000002619 bicyclic group Chemical group 0.000 claims 41
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 41
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 32
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 29
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 26
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 21
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 20
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 20
- 150000002431 hydrogen Chemical class 0.000 claims 19
- 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 18
- 125000003545 alkoxy group Chemical group 0.000 claims 17
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 17
- 125000004076 pyridyl group Chemical group 0.000 claims 17
- 125000000335 thiazolyl group Chemical group 0.000 claims 17
- 125000004434 sulfur atom Chemical group 0.000 claims 14
- 229910052799 carbon Inorganic materials 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 12
- 125000005322 morpholin-1-yl group Chemical group 0.000 claims 11
- 208000002193 Pain Diseases 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 10
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 9
- 125000004429 atom Chemical group 0.000 claims 9
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 9
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 9
- 125000004368 propenyl group Chemical group C(=CC)* 0.000 claims 9
- 101000687448 Homo sapiens REST corepressor 1 Proteins 0.000 claims 8
- 102100024864 REST corepressor 1 Human genes 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 8
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 7
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 6
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical group C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 5
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims 5
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 4
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 4
- KHBQMWCZKVMBLN-UHFFFAOYSA-N Benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1 KHBQMWCZKVMBLN-UHFFFAOYSA-N 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims 4
- 208000004296 neuralgia Diseases 0.000 claims 4
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims 3
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 3
- RAUWPNXIALNKQM-UHFFFAOYSA-N 4-nitro-1,2-phenylenediamine Chemical compound NC1=CC=C([N+]([O-])=O)C=C1N RAUWPNXIALNKQM-UHFFFAOYSA-N 0.000 claims 3
- 208000008035 Back Pain Diseases 0.000 claims 3
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 3
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 3
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- KZKRRZFCAYOXQE-UHFFFAOYSA-N 1$l^{2}-azinane Chemical group C1CC[N]CC1 KZKRRZFCAYOXQE-UHFFFAOYSA-N 0.000 claims 2
- IANQTJSKSUMEQM-UHFFFAOYSA-N 1-benzofuran Chemical compound C1=CC=C2OC=CC2=C1 IANQTJSKSUMEQM-UHFFFAOYSA-N 0.000 claims 2
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- VRJHQPZVIGNGMX-UHFFFAOYSA-N 4-piperidinone Chemical group O=C1CCNCC1 VRJHQPZVIGNGMX-UHFFFAOYSA-N 0.000 claims 2
- 206010058019 Cancer Pain Diseases 0.000 claims 2
- 208000000094 Chronic Pain Diseases 0.000 claims 2
- 206010019233 Headaches Diseases 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 206010065390 Inflammatory pain Diseases 0.000 claims 2
- 208000004404 Intractable Pain Diseases 0.000 claims 2
- 206010028836 Neck pain Diseases 0.000 claims 2
- 208000004550 Postoperative Pain Diseases 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- 208000008765 Sciatica Diseases 0.000 claims 2
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 claims 2
- 208000005298 acute pain Diseases 0.000 claims 2
- XTKDAFGWCDAMPY-UHFFFAOYSA-N azaperone Chemical compound C1=CC(F)=CC=C1C(=O)CCCN1CCN(C=2N=CC=CC=2)CC1 XTKDAFGWCDAMPY-UHFFFAOYSA-N 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- DIOQZVSQGTUSAI-UHFFFAOYSA-N decane Chemical compound CCCCCCCCCC DIOQZVSQGTUSAI-UHFFFAOYSA-N 0.000 claims 2
- 231100000869 headache Toxicity 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 2
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 claims 2
- NGXSWUFDCSEIOO-SCSAIBSYSA-N (3r)-pyrrolidin-3-amine Chemical compound N[C@@H]1CCNC1 NGXSWUFDCSEIOO-SCSAIBSYSA-N 0.000 claims 1
- FTNJQNQLEGKTGD-UHFFFAOYSA-N 1,3-benzodioxole Chemical compound C1=CC=C2OCOC2=C1 FTNJQNQLEGKTGD-UHFFFAOYSA-N 0.000 claims 1
- 125000001462 1-pyrrolyl group Chemical group [*]N1C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- ULUJSOKAYRGZQV-UHFFFAOYSA-N 2,5-diazabicyclo[2.2.1]heptane;2,2,2-trifluoroacetic acid Chemical compound C1NC2CNC1C2.OC(=O)C(F)(F)F.OC(=O)C(F)(F)F ULUJSOKAYRGZQV-UHFFFAOYSA-N 0.000 claims 1
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical group O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000005809 3,4,5-trimethoxyphenyl group Chemical group [H]C1=C(OC([H])([H])[H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims 1
- 125000003762 3,4-dimethoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims 1
- LCPAGOYFGIFJCL-UHFFFAOYSA-N 3,8-diazabicyclo[3.2.1]octane;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F.C1NCC2CCC1N2 LCPAGOYFGIFJCL-UHFFFAOYSA-N 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- IQFIFBLWZFRCCZ-UHFFFAOYSA-N 4-(3-benzyl-3,8-diazabicyclo[3.2.1]octan-8-yl)-2-phenylquinazoline Chemical compound C=1C=CC=CC=1CN(C1)CC2CCC1N2C(C1=CC=CC=C1N=1)=NC=1C1=CC=CC=C1 IQFIFBLWZFRCCZ-UHFFFAOYSA-N 0.000 claims 1
- 125000004939 6-pyridyl group Chemical group N1=CC=CC=C1* 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003591 Ataxia Diseases 0.000 claims 1
- 108090000312 Calcium Channels Proteins 0.000 claims 1
- 102000003922 Calcium Channels Human genes 0.000 claims 1
- 208000006561 Cluster Headache Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010021639 Incontinence Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 206010061533 Myotonia Diseases 0.000 claims 1
- 208000001294 Nociceptive Pain Diseases 0.000 claims 1
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 1
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims 1
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims 1
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 claims 1
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 208000018912 cluster headache syndrome Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- 208000014617 hemorrhoid Diseases 0.000 claims 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 206010022437 insomnia Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000015706 neuroendocrine disease Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- HDOWRFHMPULYOA-UHFFFAOYSA-N piperidin-4-ol Chemical group OC1CCNCC1 HDOWRFHMPULYOA-UHFFFAOYSA-N 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical group C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 1
- NGXSWUFDCSEIOO-UHFFFAOYSA-N pyrrolidin-3-amine Chemical compound NC1CCNC1 NGXSWUFDCSEIOO-UHFFFAOYSA-N 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000005505 thiomorpholino group Chemical group 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
- 0 CC(*)N1CCNCC1 Chemical compound CC(*)N1CCNCC1 0.000 description 11
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45145803P | 2003-03-03 | 2003-03-03 | |
| US60/451,458 | 2003-03-03 | ||
| US46379703P | 2003-04-18 | 2003-04-18 | |
| US60/463,797 | 2003-04-18 | ||
| PCT/US2004/006451 WO2004078733A1 (en) | 2003-03-03 | 2004-03-03 | Quinazolines useful as modulators of ion channels |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006522119A JP2006522119A (ja) | 2006-09-28 |
| JP2006522119A5 true JP2006522119A5 (enExample) | 2007-04-26 |
| JP5247027B2 JP5247027B2 (ja) | 2013-07-24 |
Family
ID=32965550
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006509028A Expired - Fee Related JP5247027B2 (ja) | 2003-03-03 | 2004-03-03 | イオンチャネルのモジュレーターとして有用なキナゾリン |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US7678802B2 (enExample) |
| EP (1) | EP1608632B1 (enExample) |
| JP (1) | JP5247027B2 (enExample) |
| KR (1) | KR20050108379A (enExample) |
| AR (1) | AR044502A1 (enExample) |
| AT (1) | ATE453629T1 (enExample) |
| AU (1) | AU2004217891B2 (enExample) |
| BR (1) | BRPI0408026A (enExample) |
| CA (1) | CA2517844A1 (enExample) |
| CL (1) | CL2004000409A1 (enExample) |
| DE (1) | DE602004024873D1 (enExample) |
| ES (1) | ES2338553T3 (enExample) |
| IL (1) | IL170636A (enExample) |
| NO (1) | NO20054546L (enExample) |
| NZ (1) | NZ542664A (enExample) |
| PE (1) | PE20041059A1 (enExample) |
| RU (1) | RU2378260C2 (enExample) |
| TW (1) | TW200426147A (enExample) |
| UY (1) | UY28215A1 (enExample) |
| WO (1) | WO2004078733A1 (enExample) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7713983B2 (en) * | 2003-03-03 | 2010-05-11 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| JP4895806B2 (ja) * | 2003-04-09 | 2012-03-14 | エクセリクシス， インク． | Ｔｉｅ−２モジュレータと使用方法 |
| EP1635846A4 (en) * | 2003-06-20 | 2009-01-28 | Coley Pharm Gmbh | SMALL MOLECULAR TLR (TOLL-LIKE RECEPTOR) ANTAGONISTS |
| AR045037A1 (es) * | 2003-07-10 | 2005-10-12 | Aventis Pharma Sa | Tetrahidro-1h-pirazolo [3,4-c] piridinas sustituidas, composiciones que las contienen y su utilizacion. |
| TWI344364B (en) * | 2003-11-10 | 2011-07-01 | Synta Pharmaceuticals Corp | Fused heterocyclic compounds |
| EP1784393B1 (en) * | 2004-09-02 | 2009-07-01 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| US7928107B2 (en) | 2004-09-02 | 2011-04-19 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| US8283354B2 (en) | 2004-09-02 | 2012-10-09 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| US7718658B2 (en) * | 2004-09-02 | 2010-05-18 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| ZA200704972B (en) * | 2004-12-17 | 2008-09-25 | Vertex Pharma | Processes for producing 4-aminoquinazolines |
| US8252806B2 (en) | 2005-03-14 | 2012-08-28 | Neurosearch A/S | Potassium channel modulating agents and their medical use |
| JP5112297B2 (ja) * | 2005-05-20 | 2013-01-09 | バーテックス ファーマシューティカルズ インコーポレイテッド | イオンチャネルのモジュレーターとして有用なキノリン誘導体 |
| FR2891829A1 (fr) * | 2005-10-12 | 2007-04-13 | Sanofi Aventis Sa | Derives de la 4-amino-quinazoline, leur preparation et leur application en therapeutique |
| GB0522715D0 (en) | 2005-11-08 | 2005-12-14 | Helperby Therapeutics Ltd | New use |
| ES2377988T3 (es) | 2005-11-14 | 2012-04-03 | Vertex Pharmaceuticals, Inc. | Quinazolinas útiles como moduladores de canales iónicos controlados por voltaje |
| KR20080070749A (ko) | 2005-11-23 | 2008-07-30 | 페인셉터 파마 코포레이션 | 개폐 이온 통로를 조절하기 위한 조성물 및 방법 |
| JP2009520700A (ja) * | 2005-12-21 | 2009-05-28 | ペインセプター ファーマ コーポレーション | 依存性イオンチャネルを調節するための組成物および方法 |
| WO2007115410A1 (en) * | 2006-04-10 | 2007-10-18 | Painceptor Pharma Corporation | Compositions and methods for modulating gated ion channels |
| EP2024333A2 (en) | 2006-04-26 | 2009-02-18 | Cancer Research Technology Limited | Amino-ethyl-amino-aryl (aeaa) compounds and their use |
| MX2008015908A (es) | 2006-06-12 | 2009-01-28 | Vertex Pharma | Tienopirimidinas utiles como moduladores de canales de iones. |
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- 2004-03-03 EP EP04716887A patent/EP1608632B1/en not_active Expired - Lifetime
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- 2004-03-03 PE PE2004000236A patent/PE20041059A1/es not_active Application Discontinuation
- 2004-03-03 AT AT04716887T patent/ATE453629T1/de active
- 2004-03-03 WO PCT/US2004/006451 patent/WO2004078733A1/en not_active Ceased
- 2004-03-03 RU RU2005130486/04A patent/RU2378260C2/ru not_active IP Right Cessation
- 2004-03-03 KR KR1020057016287A patent/KR20050108379A/ko not_active Ceased
- 2004-03-03 AU AU2004217891A patent/AU2004217891B2/en not_active Ceased
- 2004-03-03 BR BR0408026-2A patent/BRPI0408026A/pt not_active IP Right Cessation
- 2004-03-03 NZ NZ542664A patent/NZ542664A/en unknown
- 2004-03-03 UY UY28215A patent/UY28215A1/es not_active Application Discontinuation
- 2004-03-03 JP JP2006509028A patent/JP5247027B2/ja not_active Expired - Fee Related
- 2004-03-03 DE DE602004024873T patent/DE602004024873D1/de not_active Expired - Lifetime
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2005
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2010
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