JP2008526824A5 - - Google Patents
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- JP2008526824A5 JP2008526824A5 JP2007549955A JP2007549955A JP2008526824A5 JP 2008526824 A5 JP2008526824 A5 JP 2008526824A5 JP 2007549955 A JP2007549955 A JP 2007549955A JP 2007549955 A JP2007549955 A JP 2007549955A JP 2008526824 A5 JP2008526824 A5 JP 2008526824A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- indol
- pyrimidin
- amine
- formula
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 52
- -1 CF 3 Inorganic materials 0.000 claims 28
- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 14
- 239000003085 diluting agent Substances 0.000 claims 12
- 239000000546 pharmaceutical excipient Substances 0.000 claims 12
- 125000002723 alicyclic group Chemical group 0.000 claims 9
- 125000004122 cyclic group Chemical group 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims 5
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical compound NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 230000001419 dependent effect Effects 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 125000004193 piperazinyl group Chemical group 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 230000003796 beauty Effects 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000005549 heteroarylene group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 3
- QNMZWFNNJMGJPU-UHFFFAOYSA-N 4-(1h-indol-3-yl)pyrimidin-2-amine Chemical compound NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 QNMZWFNNJMGJPU-UHFFFAOYSA-N 0.000 claims 2
- 241000700588 Human alphaherpesvirus 1 Species 0.000 claims 2
- 241000701085 Human alphaherpesvirus 3 Species 0.000 claims 2
- 241000701024 Human betaherpesvirus 5 Species 0.000 claims 2
- 241000713772 Human immunodeficiency virus 1 Species 0.000 claims 2
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 208000015114 central nervous system disease Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- JIAARYAFYJHUJI-UHFFFAOYSA-L zinc dichloride Chemical compound [Cl-].[Cl-].[Zn+2] JIAARYAFYJHUJI-UHFFFAOYSA-L 0.000 claims 2
- MFJBGNAKQQZROG-UHFFFAOYSA-N 1-[3-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]indol-1-yl]ethanone Chemical compound C12=CC=CC=C2N(C(=O)C)C=C1C(N=1)=CC=NC=1NC(C=C1)=CC=C1N1CCOCC1 MFJBGNAKQQZROG-UHFFFAOYSA-N 0.000 claims 1
- ORYJIEHLXNBUDO-UHFFFAOYSA-N 1-[4-[2-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C1=CC=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3N(C)C=2)=N1 ORYJIEHLXNBUDO-UHFFFAOYSA-N 0.000 claims 1
- QTEDNMKQFCBAAX-UHFFFAOYSA-N 1-[4-[2-[[4-(1h-indol-3-yl)pyrimidin-2-yl]amino]-6-methylphenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C1=C(C)C=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 QTEDNMKQFCBAAX-UHFFFAOYSA-N 0.000 claims 1
- ALVHKDFSUMXMAM-UHFFFAOYSA-N 1-[4-[2-[[4-(1h-indol-3-yl)pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1C1=CC=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 ALVHKDFSUMXMAM-UHFFFAOYSA-N 0.000 claims 1
- OHSNNALNCJKABP-UHFFFAOYSA-N 1-[4-[2-[[4-(7-methoxy-1h-indol-3-yl)pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone Chemical compound C=1NC=2C(OC)=CC=CC=2C=1C(N=1)=CC=NC=1NC1=CC=CC=C1N1CCN(C(C)=O)CC1 OHSNNALNCJKABP-UHFFFAOYSA-N 0.000 claims 1
- GEHZQYLPZVLSBQ-UHFFFAOYSA-N 1-n-[4-(1h-indol-3-yl)pyrimidin-2-yl]-4-n,4-n-dimethylbenzene-1,4-diamine Chemical compound C1=CC(N(C)C)=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 GEHZQYLPZVLSBQ-UHFFFAOYSA-N 0.000 claims 1
- XCCVIORCKHCUBO-UHFFFAOYSA-N 3-[6-(4-bromophenyl)-2-piperazin-1-ylpyrimidin-4-yl]-1h-indole Chemical compound C1=CC(Br)=CC=C1C1=CC(C=2C3=CC=CC=C3NC=2)=NC(N2CCNCC2)=N1 XCCVIORCKHCUBO-UHFFFAOYSA-N 0.000 claims 1
- BSYRLFVDLLFKHN-UHFFFAOYSA-N 3-[6-(4-bromophenyl)-2-pyrrolidin-1-ylpyrimidin-4-yl]-1h-indole Chemical compound C1=CC(Br)=CC=C1C1=CC(C=2C3=CC=CC=C3NC=2)=NC(N2CCCC2)=N1 BSYRLFVDLLFKHN-UHFFFAOYSA-N 0.000 claims 1
- GCNIRIHGOROKHE-UHFFFAOYSA-N 4-(1-methylindol-3-yl)-n-(4-morpholin-4-ylphenyl)pyrimidin-2-amine Chemical compound C12=CC=CC=C2N(C)C=C1C(N=1)=CC=NC=1NC(C=C1)=CC=C1N1CCOCC1 GCNIRIHGOROKHE-UHFFFAOYSA-N 0.000 claims 1
- IGBOLHKYTYGQHA-UHFFFAOYSA-N 4-(1h-indol-3-yl)-n-(2-methyl-4-morpholin-4-ylphenyl)pyrimidin-2-amine Chemical compound C=1C=C(NC=2N=C(C=CN=2)C=2C3=CC=CC=C3NC=2)C(C)=CC=1N1CCOCC1 IGBOLHKYTYGQHA-UHFFFAOYSA-N 0.000 claims 1
- KAOVBKLGTDLFFF-UHFFFAOYSA-N 4-(1h-indol-3-yl)-n-(3,4,5-trimethoxyphenyl)pyrimidin-2-amine Chemical compound COC1=C(OC)C(OC)=CC(NC=2N=C(C=CN=2)C=2C3=CC=CC=C3NC=2)=C1 KAOVBKLGTDLFFF-UHFFFAOYSA-N 0.000 claims 1
- NSGNJVMFDJRZTQ-UHFFFAOYSA-N 4-(1h-indol-3-yl)-n-(3-methoxy-4-morpholin-4-ylphenyl)pyrimidin-2-amine Chemical compound COC1=CC(NC=2N=C(C=CN=2)C=2C3=CC=CC=C3NC=2)=CC=C1N1CCOCC1 NSGNJVMFDJRZTQ-UHFFFAOYSA-N 0.000 claims 1
- IFZZRTFWXXWCAG-UHFFFAOYSA-N 4-(1h-indol-3-yl)-n-(3-methyl-4-thiomorpholin-4-ylphenyl)pyrimidin-2-amine Chemical compound CC1=CC(NC=2N=C(C=CN=2)C=2C3=CC=CC=C3NC=2)=CC=C1N1CCSCC1 IFZZRTFWXXWCAG-UHFFFAOYSA-N 0.000 claims 1
- YREMHFSLEPPRKL-UHFFFAOYSA-N 4-(1h-indol-3-yl)-n-(3-nitrophenyl)pyrimidin-2-amine Chemical compound [O-][N+](=O)C1=CC=CC(NC=2N=C(C=CN=2)C=2C3=CC=CC=C3NC=2)=C1 YREMHFSLEPPRKL-UHFFFAOYSA-N 0.000 claims 1
- UFJLSLOQYSZPMI-UHFFFAOYSA-N 4-(1h-indol-3-yl)-n-(4-morpholin-4-ylphenyl)pyrimidin-2-amine Chemical compound C1COCCN1C(C=C1)=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 UFJLSLOQYSZPMI-UHFFFAOYSA-N 0.000 claims 1
- PXGRGKDEILVGHC-UHFFFAOYSA-N 4-(1h-indol-3-yl)-n-(4-piperazin-1-ylphenyl)pyrimidin-2-amine Chemical compound C1CNCCN1C(C=C1)=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 PXGRGKDEILVGHC-UHFFFAOYSA-N 0.000 claims 1
- OJHMIXITQDAWHE-UHFFFAOYSA-N 4-(1h-indol-3-yl)-n-(6-methoxypyridin-3-yl)pyrimidin-2-amine Chemical compound C1=NC(OC)=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 OJHMIXITQDAWHE-UHFFFAOYSA-N 0.000 claims 1
- LINLHBQPNYMQFJ-UHFFFAOYSA-N 4-(1h-indol-3-yl)-n-[2-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine Chemical compound C1CN(C)CCN1C1=CC=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 LINLHBQPNYMQFJ-UHFFFAOYSA-N 0.000 claims 1
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 102000003989 Aurora kinases Human genes 0.000 claims 1
- 108090000433 Aurora kinases Proteins 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000030852 Parasitic disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- WETWJCDKMRHUPV-UHFFFAOYSA-N acetyl chloride Chemical compound CC(Cl)=O WETWJCDKMRHUPV-UHFFFAOYSA-N 0.000 claims 1
- 239000012346 acetyl chloride Substances 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000008065 acid anhydrides Chemical class 0.000 claims 1
- 231100000360 alopecia Toxicity 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 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
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- JAZZHCIYTHOJIC-UHFFFAOYSA-N cyclopropyl-[3-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]indol-1-yl]methanone Chemical compound C1=C(C=2N=C(NC=3C=CC(=CC=3)N3CCOCC3)N=CC=2)C2=CC=CC=C2N1C(=O)C1CC1 JAZZHCIYTHOJIC-UHFFFAOYSA-N 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- FRIJBUGBVQZNTB-UHFFFAOYSA-M magnesium;ethane;bromide Chemical compound [Mg+2].[Br-].[CH2-]C FRIJBUGBVQZNTB-UHFFFAOYSA-M 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000000813 microbial effect Effects 0.000 claims 1
- LUFWSVASWTXJRR-UHFFFAOYSA-N n-(1,3-benzodioxol-5-yl)-4-(1h-indol-3-yl)pyrimidin-2-amine Chemical compound C1=CC=C2C(C=3C=CN=C(N=3)NC3=CC=C4OCOC4=C3)=CNC2=C1 LUFWSVASWTXJRR-UHFFFAOYSA-N 0.000 claims 1
- BOQFTUSRPOGVOO-UHFFFAOYSA-N n-(3,5-dimethoxyphenyl)-4-(1h-indol-3-yl)pyrimidin-2-amine Chemical compound COC1=CC(OC)=CC(NC=2N=C(C=CN=2)C=2C3=CC=CC=C3NC=2)=C1 BOQFTUSRPOGVOO-UHFFFAOYSA-N 0.000 claims 1
- XQOMWIBDIAWJPS-UHFFFAOYSA-N n-(4-fluorophenyl)-4-(1h-indol-3-yl)pyrimidin-2-amine Chemical compound C1=CC(F)=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 XQOMWIBDIAWJPS-UHFFFAOYSA-N 0.000 claims 1
- UHXXXKOMOCSVKR-UHFFFAOYSA-N n-[2-(2,6-dimethylmorpholin-4-yl)phenyl]-4-(1h-indol-3-yl)pyrimidin-2-amine Chemical compound C1C(C)OC(C)CN1C1=CC=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 UHXXXKOMOCSVKR-UHFFFAOYSA-N 0.000 claims 1
- ZPCJDYUHELRFHH-UHFFFAOYSA-N n-[2-(3,5-dimethylpiperidin-1-yl)phenyl]-4-(1h-indol-3-yl)pyrimidin-2-amine Chemical compound C1C(C)CC(C)CN1C1=CC=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 ZPCJDYUHELRFHH-UHFFFAOYSA-N 0.000 claims 1
- UZQPYJFQWWIAML-UHFFFAOYSA-N n-[2-(4-benzylpiperazin-1-yl)phenyl]-4-(1h-indol-3-yl)pyrimidin-2-amine Chemical compound C1CN(C=2C(=CC=CC=2)NC=2N=C(C=CN=2)C=2C3=CC=CC=C3NC=2)CCN1CC1=CC=CC=C1 UZQPYJFQWWIAML-UHFFFAOYSA-N 0.000 claims 1
- UHXXXKOMOCSVKR-CALCHBBNSA-N n-[2-[(2s,6r)-2,6-dimethylmorpholin-4-yl]phenyl]-4-(1h-indol-3-yl)pyrimidin-2-amine Chemical compound C1[C@@H](C)O[C@@H](C)CN1C1=CC=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 UHXXXKOMOCSVKR-CALCHBBNSA-N 0.000 claims 1
- UHXXXKOMOCSVKR-IRXDYDNUSA-N n-[2-[(2s,6s)-2,6-dimethylmorpholin-4-yl]phenyl]-4-(1h-indol-3-yl)pyrimidin-2-amine Chemical compound C1[C@H](C)O[C@@H](C)CN1C1=CC=CC=C1NC1=NC=CC(C=2C3=CC=CC=C3NC=2)=N1 UHXXXKOMOCSVKR-IRXDYDNUSA-N 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 235000005074 zinc chloride Nutrition 0.000 claims 1
- 239000011592 zinc chloride Substances 0.000 claims 1
- 0 Cc1c(C(C*)=O)c(c(*)c(*)c(*)c2*)c2[n]1 Chemical compound Cc1c(C(C*)=O)c(c(*)c(*)c(*)c2*)c2[n]1 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0500492.4A GB0500492D0 (en) | 2005-01-11 | 2005-01-11 | Compound |
| PCT/GB2006/000087 WO2006075152A1 (en) | 2005-01-11 | 2006-01-11 | 4- (1h-indol-3-yl) -pyrimidin-2-ylamine derivates and their use in therapy |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008526824A JP2008526824A (ja) | 2008-07-24 |
| JP2008526824A5 true JP2008526824A5 (enExample) | 2009-02-19 |
Family
ID=34203901
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007549955A Pending JP2008526824A (ja) | 2005-01-11 | 2006-01-11 | 4−(1h−インドール−3−イル)−ピリミジン−2−イルアミン誘導体及び治療におけるこれらの使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20090318446A1 (enExample) |
| EP (1) | EP1836194A1 (enExample) |
| JP (1) | JP2008526824A (enExample) |
| CN (1) | CN101111490A (enExample) |
| AU (1) | AU2006205710A1 (enExample) |
| BR (1) | BRPI0606313A2 (enExample) |
| CA (1) | CA2592723A1 (enExample) |
| GB (1) | GB0500492D0 (enExample) |
| IL (1) | IL184313A0 (enExample) |
| MX (1) | MX2007008373A (enExample) |
| WO (1) | WO2006075152A1 (enExample) |
Families Citing this family (89)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0205693D0 (en) | 2002-03-09 | 2002-04-24 | Astrazeneca Ab | Chemical compounds |
| GB0205688D0 (en) | 2002-03-09 | 2002-04-24 | Astrazeneca Ab | Chemical compounds |
| GB0205690D0 (en) | 2002-03-09 | 2002-04-24 | Astrazeneca Ab | Chemical compounds |
| AU2003208479A1 (en) | 2002-03-09 | 2003-09-22 | Astrazeneca Ab | 4- imidazolyl substuited pyrimidine derivatives with cdk inhibitiory activity |
| GB0311276D0 (en) | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| GB0311274D0 (en) | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| FR2878849B1 (fr) | 2004-12-06 | 2008-09-12 | Aventis Pharma Sa | Indoles substitues, compositions les contenant, procede de fabrication et utilisation |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| US20100267707A1 (en) * | 2006-06-22 | 2010-10-21 | Merck Sharp & Dohme Corp. | Tyrosine Kinase Inhibitors |
| JP5325783B2 (ja) * | 2006-09-08 | 2013-10-23 | エフ.ホフマン−ラ ロシュ アーゲー | ベンゾトリアゾールキナーゼモジュレーター |
| BRPI0719883A2 (pt) | 2006-10-09 | 2015-05-05 | Takeda Pharmaceutical | Inibidores de quinase |
| EP2283009B1 (en) * | 2008-05-16 | 2012-08-29 | F. Hoffmann-La Roche AG | Inhibitors of jnk |
| CN101723936B (zh) * | 2008-10-27 | 2014-01-15 | 上海睿星基因技术有限公司 | 激酶抑制剂及其在药学中的用途 |
| EP2370424A1 (en) | 2008-11-10 | 2011-10-05 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2376485B1 (en) | 2008-12-19 | 2017-12-06 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of atr kinase |
| CN102458402B (zh) | 2009-06-12 | 2013-10-02 | 百时美施贵宝公司 | 用作激酶调节剂的烟酰胺化合物 |
| RU2012136451A (ru) | 2010-01-28 | 2014-03-10 | Президент Энд Феллоуз Оф Гарвард Колледж | Композиции и способы улучшения активности протеасомы |
| BR112012024380A2 (pt) | 2010-03-25 | 2015-09-15 | Glaxosmithkline Llc | compostos químicos |
| MY159995A (en) | 2010-04-27 | 2017-02-15 | Hutchison Medipharma Ltd | Pyrimidinyl indole compounds |
| KR20130066633A (ko) | 2010-05-12 | 2013-06-20 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 억제제로서 유용한 화합물 |
| US8962631B2 (en) | 2010-05-12 | 2015-02-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2011143399A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2569284B1 (en) | 2010-05-12 | 2015-07-08 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as inhibitors of atr kinase |
| EP2569286B1 (en) | 2010-05-12 | 2014-08-20 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| JP2013526540A (ja) | 2010-05-12 | 2013-06-24 | 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 | Atrキナーゼ阻害剤として有用な化合物 |
| WO2011163527A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| AU2011338389A1 (en) | 2010-12-09 | 2013-06-13 | Amgen Inc. | Bicyclic compounds as Pim inhibitors |
| CZ305457B6 (cs) | 2011-02-28 | 2015-09-30 | Ústav organické chemie a biochemie, Akademie věd ČR v. v. i. | Pyrimidinové sloučeniny inhibující tvorbu oxidu dusnatého a prostaglandinu E2, způsob výroby a použití |
| AU2012230890A1 (en) | 2011-03-22 | 2013-09-26 | Amgen Inc. | Azole compounds as Pim inhibitors |
| WO2012138938A1 (en) | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
| JP6208122B2 (ja) | 2011-05-12 | 2017-10-04 | プロテオステイシス セラピューティクス,インコーポレイテッド | プロテオスタシス調節因子 |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| US8822469B2 (en) | 2011-06-22 | 2014-09-02 | Vertex Pharmaceuticals Incorporated | Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase |
| US9096602B2 (en) | 2011-06-22 | 2015-08-04 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors |
| EP3333161B1 (en) | 2011-07-27 | 2020-02-19 | Astrazeneca AB | 2-(2,4,5-substituted-anilino)pyrimidine derivatives as egfr modulators useful for treating cancer |
| KR101283895B1 (ko) * | 2011-08-04 | 2013-07-16 | 한국해양과학기술원 | 5-하이드록시인돌 화합물 또는 해면동물 스칼라리스폰지아 추출물을 유효성분으로 함유하는 암 질환의 예방 및 치료를 위한 조성물 |
| BR112014007690B1 (pt) | 2011-09-30 | 2022-10-04 | Vertex Pharmaceuticals Incorporated | Usos de inibidores de atr no tratamento de câncer pancreático e câncer de pulmão de células não pequenas |
| CN103987709B (zh) | 2011-09-30 | 2016-09-28 | 沃泰克斯药物股份有限公司 | 用于制备可用作atr激酶抑制剂的化合物的方法 |
| IN2014KN00943A (enExample) | 2011-09-30 | 2015-08-21 | Vertex Pharma | |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP2751088B1 (en) | 2011-09-30 | 2016-04-13 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013059634A1 (en) | 2011-10-20 | 2013-04-25 | The Regents Of The University Of California | Use of cdk9 inhibitors to reduce cartilage degradation |
| WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2013071093A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| US8841449B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2013071090A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP3311816A1 (en) | 2012-04-05 | 2018-04-25 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase for the treatment of cancer |
| US8999632B2 (en) | 2012-10-04 | 2015-04-07 | Vertex Pharmaceuticals Incorporated | Method for measuring ATR inhibition mediated increases in DNA damage |
| EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| PL3808749T3 (pl) | 2012-12-07 | 2023-07-10 | Vertex Pharmaceuticals Incorporated | Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych |
| US9849135B2 (en) | 2013-01-25 | 2017-12-26 | President And Fellows Of Harvard College | USP14 inhibitors for treating or preventing viral infections |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | 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Vertex Pharmaceuticals Incorporated | Atrキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体 |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| PL3077397T3 (pl) | 2013-12-06 | 2020-04-30 | Vertex Pharmaceuticals Inc. | Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne |
| CN104876914B (zh) * | 2014-02-28 | 2017-04-19 | 山东轩竹医药科技有限公司 | 嘧啶衍生物类间变性淋巴瘤激酶抑制剂 |
| CN108558842B (zh) * | 2014-03-06 | 2021-06-04 | 山东轩竹医药科技有限公司 | 嘧啶衍生物类间变性淋巴瘤激酶抑制剂 |
| SG10201902206QA (en) | 2014-06-05 | 2019-04-29 | Vertex Pharma | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
| PT3157566T (pt) | 2014-06-17 | 2019-07-11 | Vertex Pharma | Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr |
| EP3206749B1 (en) | 2014-10-14 | 2021-09-08 | The Regents of the University of California | The cdk9 and brd4 inhibitors flavopiridol and jq1 to inhibit cartilage inflammation |
| KR20250035597A (ko) * | 2015-09-25 | 2025-03-12 | 디잘 (지앙수) 파마슈티칼 씨오., 리미티드 | Jak를 억제하기 위한 화합물 및 방법 |
| RU2768621C1 (ru) | 2015-09-30 | 2022-03-24 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr |
| US10513509B2 (en) | 2016-05-26 | 2019-12-24 | Recurium Ip Holdings, Llc | EGFR inhibitor compounds |
| WO2018064465A1 (en) | 2016-09-29 | 2018-04-05 | The Regents Of The University Of California | Compounds for increasing neural plasticity |
| JP6608565B2 (ja) * | 2017-01-26 | 2019-11-20 | ハンミ ファーマシューティカルズ カンパニー リミテッド | ピリミジン化合物及びその医薬用途 |
| CN107987054B (zh) * | 2017-11-28 | 2020-05-19 | 四川大学 | 一种cdk2抑制剂 |
| CA3088529A1 (en) | 2018-01-16 | 2019-07-25 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| EP3740207A4 (en) * | 2018-01-16 | 2021-10-13 | Syros Pharmaceuticals, Inc. | CYCLINE-DEPENDENT KINASE 7 (CDK7) INHIBITORS |
| CN111683976B (zh) | 2018-02-05 | 2022-11-18 | 生物辐射实验室股份有限公司 | 具有阴离子交换-疏水混合模式配体的色谱树脂 |
| WO2019154177A1 (zh) * | 2018-02-12 | 2019-08-15 | 恩瑞生物医药科技(上海)有限公司 | 嘧啶类化合物、其制备方法及其医药用途 |
| AU2019203034B1 (en) * | 2018-07-25 | 2019-09-26 | Hanmi Pharm. Co., Ltd. | Pyrimidine compounds and pharmaceutical compositions for preventing or treating cancers including the same |
| KR101954370B1 (ko) * | 2018-07-25 | 2019-03-05 | 한미약품 주식회사 | 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물 |
| WO2020071550A1 (ja) * | 2018-10-04 | 2020-04-09 | 京都薬品工業株式会社 | Cdk8阻害剤およびその用途 |
| JP2020070270A (ja) * | 2018-11-01 | 2020-05-07 | 御木本製薬株式会社 | フィブロネクチン遺伝子発現促進剤 |
| MX2021005007A (es) * | 2018-11-01 | 2021-07-21 | Syros Pharmaceuticals Inc | Inhibidores de cinasa 7 dependiente de ciclina (cdk7). |
| US11633399B2 (en) | 2018-12-25 | 2023-04-25 | Sol-Gel Technologies Ltd. | Treatment of skin disorders with compositions comprising an EGFR inhibitor |
| BR112021016522A2 (pt) | 2019-02-22 | 2021-10-26 | Hanmi Pharm. Co., Ltd. | Composição farmacêutica para o tratamento da leucemia mieloide aguda |
| WO2020171649A1 (ko) * | 2019-02-22 | 2020-08-27 | 한미약품 주식회사 | Flt3 저해제 및 iap 길항제를 포함하는 급성 골수성 백혈병의 치료를 위한 약학적 조합물 |
| CA3130770A1 (en) | 2019-02-27 | 2020-09-03 | The Regents Of The University Of California | Azepino-indoles and other heterocycles for treating brain disorders |
| CN113645976A (zh) | 2019-03-29 | 2021-11-12 | 阿斯利康(瑞典)有限公司 | 用于治疗非小细胞肺癌的奧希替尼 |
| CN114364675A (zh) | 2019-05-05 | 2022-04-15 | 上海齐鲁锐格医药研发有限公司 | Cdk抑制剂 |
| AU2020277541A1 (en) * | 2019-05-22 | 2022-01-06 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Indole derivative-containing inhibitor, preparation method therefor and application thereof |
| AU2020308814A1 (en) | 2019-06-27 | 2022-02-03 | Hanmi Pharm. Co., Ltd. | Pharmaceutical composition for treating acute myeloid leukemia, containing FLT3 inhibitor and chemotherapeutic agents |
| CN114269742B (zh) * | 2019-07-10 | 2024-07-16 | 常州千红生化制药股份有限公司 | 作为治疗剂的4-(咪唑并[1,2-a]吡啶-3-基)-N-(吡啶基)嘧啶-2-胺的衍生物 |
| US12233064B1 (en) * | 2019-07-12 | 2025-02-25 | University Of South Florida | Antarctic tunicate Synoicum species-derived alkaloids and methods of treatment |
| KR20210038366A (ko) * | 2019-09-30 | 2021-04-07 | 한미약품 주식회사 | Flt3 저해제 및 mdm2 저해제를 포함하는 급성 골수성 백혈병 치료용 약학적 조성물 |
| WO2021084541A1 (en) * | 2019-10-31 | 2021-05-06 | Sol-Gel Technologies Ltd. | Treatment of hair loss disorders with a topical egfr inhibitor |
| CN116583284A (zh) * | 2020-11-05 | 2023-08-11 | 韩美药品株式会社 | 用于治疗髓性白血病的包括flt3抑制剂的药物组合物 |
| TW202333668A (zh) | 2021-12-15 | 2023-09-01 | 美商德利克斯醫療公司 | 經苯氧基及苄氧基取代之精神成形素(psychoplastogen)及其用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3751742T3 (de) * | 1986-01-13 | 2002-11-21 | American Cyanamid Co., Wayne | 4,5,6-Substituierte 2-Pyrimidinamine |
| GB9523675D0 (en) * | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| TW440563B (en) * | 1996-05-23 | 2001-06-16 | Hoffmann La Roche | Aryl pyrimidine derivatives and a pharmaceutical composition thereof |
| GB9914258D0 (en) * | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| WO2002102783A1 (en) * | 2001-06-19 | 2002-12-27 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| GB0308466D0 (en) * | 2003-04-11 | 2003-05-21 | Novartis Ag | Organic compounds |
-
2005
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