ME02684B - Jedinjenja i preparati protein kinaznih inhibitora - Google Patents
Jedinjenja i preparati protein kinaznih inhibitoraInfo
- Publication number
- ME02684B ME02684B MEP-2017-6A MEP617A ME02684B ME 02684 B ME02684 B ME 02684B ME P617 A MEP617 A ME P617A ME 02684 B ME02684 B ME 02684B
- Authority
- ME
- Montenegro
- Prior art keywords
- compound
- alkyl
- halo
- fluoro
- substituted
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 26
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- 238000000034 method Methods 0.000 claims 11
- 239000003814 drug Substances 0.000 claims 9
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 229940124597 therapeutic agent Drugs 0.000 claims 8
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 5
- 206010009944 Colon cancer Diseases 0.000 claims 4
- 125000001309 chloro group Chemical group Cl* 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- -1 cyano, hydroxyl Chemical group 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- 108090000744 Mitogen-Activated Protein Kinase Kinases Proteins 0.000 claims 2
- 102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 claims 2
- VIUAUNHCRHHYNE-JTQLQIEISA-N N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)-4-pyridinecarboxamide Chemical compound OC[C@@H](O)CNC(=O)C1=CC=NC=C1NC1=CC=C(I)C=C1F VIUAUNHCRHHYNE-JTQLQIEISA-N 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims 2
- 229920002472 Starch Polymers 0.000 claims 2
- 230000003474 anti-emetic effect Effects 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 239000000935 antidepressant agent Substances 0.000 claims 2
- 229940005513 antidepressants Drugs 0.000 claims 2
- 239000002111 antiemetic agent Substances 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 102000009929 raf Kinases Human genes 0.000 claims 2
- 108010077182 raf Kinases Proteins 0.000 claims 2
- 239000000600 sorbitol Substances 0.000 claims 2
- 235000010356 sorbitol Nutrition 0.000 claims 2
- 229940032147 starch Drugs 0.000 claims 2
- 235000019698 starch Nutrition 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims 1
- KKVYYGGCHJGEFJ-UHFFFAOYSA-N 1-n-(4-chlorophenyl)-6-methyl-5-n-[3-(7h-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine Chemical compound N=1C=CC2=C(NC=3C(=CC=CN=3)C=3C=4N=CNC=4N=CN=3)C(C)=CC=C2C=1NC1=CC=C(Cl)C=C1 KKVYYGGCHJGEFJ-UHFFFAOYSA-N 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
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- 201000009030 Carcinoma Diseases 0.000 claims 1
- 229920002261 Corn starch Polymers 0.000 claims 1
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 claims 1
- 239000001856 Ethyl cellulose Substances 0.000 claims 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 1
- 102000007665 Extracellular Signal-Regulated MAP Kinases Human genes 0.000 claims 1
- 108010007457 Extracellular Signal-Regulated MAP Kinases Proteins 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- 241000206672 Gelidium Species 0.000 claims 1
- 229920002907 Guar gum Polymers 0.000 claims 1
- 101710113864 Heat shock protein 90 Proteins 0.000 claims 1
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 claims 1
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 101710176178 Kidney androgen-regulated protein Proteins 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 108091054455 MAP kinase family Proteins 0.000 claims 1
- 102000043136 MAP kinase family Human genes 0.000 claims 1
- 229940124647 MEK inhibitor Drugs 0.000 claims 1
- 240000003183 Manihot esculenta Species 0.000 claims 1
- 235000016735 Manihot esculenta subsp esculenta Nutrition 0.000 claims 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- 229920000881 Modified starch Polymers 0.000 claims 1
- 101100381978 Mus musculus Braf gene Proteins 0.000 claims 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 102100027343 Napsin-A Human genes 0.000 claims 1
- 101710088428 Napsin-A Proteins 0.000 claims 1
- 108091007960 PI3Ks Proteins 0.000 claims 1
- 102000038030 PI3Ks Human genes 0.000 claims 1
- 235000019483 Peanut oil Nutrition 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 108091008611 Protein Kinase B Proteins 0.000 claims 1
- 108090000315 Protein Kinase C Proteins 0.000 claims 1
- 102000003923 Protein Kinase C Human genes 0.000 claims 1
- 102100033810 RAC-alpha serine/threonine-protein kinase Human genes 0.000 claims 1
- 229940123690 Raf kinase inhibitor Drugs 0.000 claims 1
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical compound [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 claims 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
- BCKXLBQYZLBQEK-KVVVOXFISA-M Sodium oleate Chemical compound [Na+].CCCCCCCC\C=C/CCCCCCCC([O-])=O BCKXLBQYZLBQEK-KVVVOXFISA-M 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- 235000019486 Sunflower oil Nutrition 0.000 claims 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 229920001615 Tragacanth Polymers 0.000 claims 1
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 235000010419 agar Nutrition 0.000 claims 1
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- 150000004781 alginic acids Chemical class 0.000 claims 1
- 235000012211 aluminium silicate Nutrition 0.000 claims 1
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 claims 1
- 229940035676 analgesics Drugs 0.000 claims 1
- 239000000730 antalgic agent Substances 0.000 claims 1
- 230000001093 anti-cancer Effects 0.000 claims 1
- 230000001430 anti-depressive effect Effects 0.000 claims 1
- 229940125683 antiemetic agent Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940041181 antineoplastic drug Drugs 0.000 claims 1
- 210000003445 biliary tract Anatomy 0.000 claims 1
- 201000001531 bladder carcinoma Diseases 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 235000010216 calcium carbonate Nutrition 0.000 claims 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims 1
- 235000013539 calcium stearate Nutrition 0.000 claims 1
- 239000008116 calcium stearate Substances 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 claims 1
- 235000010980 cellulose Nutrition 0.000 claims 1
- 229920002678 cellulose Polymers 0.000 claims 1
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- 229920002301 cellulose acetate Polymers 0.000 claims 1
- 239000004927 clay Substances 0.000 claims 1
- BSMCAPRUBJMWDF-KRWDZBQOSA-N cobimetinib Chemical compound C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F BSMCAPRUBJMWDF-KRWDZBQOSA-N 0.000 claims 1
- 229960002271 cobimetinib Drugs 0.000 claims 1
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- 235000005687 corn oil Nutrition 0.000 claims 1
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- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 claims 1
- 229940096516 dextrates Drugs 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 235000019325 ethyl cellulose Nutrition 0.000 claims 1
- 229920001249 ethyl cellulose Polymers 0.000 claims 1
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 claims 1
- 229940093471 ethyl oleate Drugs 0.000 claims 1
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 claims 1
- 210000001508 eye Anatomy 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 0.000 claims 1
- 235000011187 glycerol Nutrition 0.000 claims 1
- 150000002334 glycols Chemical class 0.000 claims 1
- 235000010417 guar gum Nutrition 0.000 claims 1
- 239000000665 guar gum Substances 0.000 claims 1
- 229960002154 guar gum Drugs 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 claims 1
- 229940059904 light mineral oil Drugs 0.000 claims 1
- 239000000944 linseed oil Substances 0.000 claims 1
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- 229920000609 methyl cellulose Polymers 0.000 claims 1
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- 235000010446 mineral oil Nutrition 0.000 claims 1
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- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 1
- RDSACQWTXKSHJT-NSHDSACASA-N n-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2s)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 claims 1
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- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
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- 102000051624 phosphatidylethanolamine binding protein Human genes 0.000 claims 1
- 108700021017 phosphatidylethanolamine binding protein Proteins 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- LHNIIDJUOCFXAP-UHFFFAOYSA-N pictrelisib Chemical compound C1CN(S(=O)(=O)C)CCN1CC1=CC2=NC(C=3C=4C=NNC=4C=CC=3)=NC(N3CCOCC3)=C2S1 LHNIIDJUOCFXAP-UHFFFAOYSA-N 0.000 claims 1
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- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- WVWZXTJUCNEUAE-UHFFFAOYSA-M potassium;1,2-bis(ethenyl)benzene;2-methylprop-2-enoate Chemical compound [K+].CC(=C)C([O-])=O.C=CC1=CC=CC=C1C=C WVWZXTJUCNEUAE-UHFFFAOYSA-M 0.000 claims 1
- 229920001592 potato starch Polymers 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- CYOHGALHFOKKQC-UHFFFAOYSA-N selumetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1Cl CYOHGALHFOKKQC-UHFFFAOYSA-N 0.000 claims 1
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- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 1
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims 1
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- 229940116362 tragacanth Drugs 0.000 claims 1
- 229960004066 trametinib Drugs 0.000 claims 1
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical compound CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 claims 1
- 208000010570 urinary bladder carcinoma Diseases 0.000 claims 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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| US31303910P | 2010-03-11 | 2010-03-11 | |
| EP14152945.3A EP2727918B1 (en) | 2009-08-28 | 2010-08-27 | Compounds and Compositions as Protein Kinase Inhibitors |
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| MEP-2014-94A ME01860B (me) | 2009-08-28 | 2010-08-27 | Jedinjenja i preparati protein kinaznih inhibitora |
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Country Status (49)
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077975A1 (es) * | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| CA2789696C (en) | 2010-02-25 | 2017-11-07 | Dana-Farber Cancer Institute, Inc. | Braf mutations conferring resistance to braf inhibitors |
| US8907270B2 (en) | 2010-06-30 | 2014-12-09 | Schlumberger Technology Corporation | Method and apparatus for gain regulation in a gamma detector |
| WO2013070996A1 (en) | 2011-11-11 | 2013-05-16 | Novartis Ag | Method of treating a proliferative disease |
| AU2012340759C1 (en) * | 2011-11-23 | 2019-11-28 | Array Biopharma Inc. | Pharmaceutical formulations |
| US9408885B2 (en) | 2011-12-01 | 2016-08-09 | Vib Vzw | Combinations of therapeutic agents for treating melanoma |
| CN103159736B (zh) * | 2011-12-10 | 2015-05-13 | 通化济达医药有限公司 | 取代的吡唑激酶抑制剂 |
| UY34540A (es) * | 2011-12-23 | 2013-06-28 | Millennium Pharm Inc | Heteroarilos y usos de los mismos |
| ES2908078T3 (es) | 2012-03-28 | 2022-04-27 | Dana Farber Cancer Inst Inc | Usos médicos que implican mutantes C-RAF que confieren resistencia a los inhibidores de RAF |
| AU2013292580B2 (en) | 2012-07-18 | 2017-07-20 | Saint Louis University | Beta amino acid derivatives as integrin antagonists |
| US8716226B2 (en) | 2012-07-18 | 2014-05-06 | Saint Louis University | 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists |
| AR091876A1 (es) * | 2012-07-26 | 2015-03-04 | Novartis Ag | Combinaciones farmaceuticas para el tratamiento de enfermedades proliferativas |
| IN2015DN00450A (instruction) * | 2012-08-07 | 2015-06-26 | Novartis Ag | |
| LT2884979T (lt) | 2012-08-17 | 2019-09-10 | F. Hoffmann-La Roche Ag | Kombinuoti melanomos gydymo būdai, apimantys kobimetinibo ir vemurafenibo skyrimą |
| US20150232452A1 (en) * | 2012-09-19 | 2015-08-20 | Ruga Corporation | Novel raf kinase inhibitors |
| JP2015536964A (ja) * | 2012-11-08 | 2015-12-24 | ノバルティス アーゲー | Ｂ−ｒａｆ阻害剤とヒストン脱アセチル化酵素阻害剤を含む医薬組合せおよび増殖性疾患の治療におけるそれらの使用 |
| CN112641787A (zh) | 2013-03-21 | 2021-04-13 | 诺华股份有限公司 | 包含B-Raf抑制剂和第二抑制剂的组合疗法 |
| TWI634114B (zh) | 2013-05-08 | 2018-09-01 | 永恒生物科技公司 | 作為激酶抑制劑之呋喃酮化合物 |
| BR112015028845A2 (pt) | 2013-05-30 | 2017-07-25 | Plexxikon Inc | compostos para a modulação da quinase e indicações da mesma |
| EP3049442A4 (en) | 2013-09-26 | 2017-06-28 | Costim Pharmaceuticals Inc. | Methods for treating hematologic cancers |
| WO2015084804A1 (en) | 2013-12-03 | 2015-06-11 | Novartis Ag | Combination of mdm2 inhibitor and braf inhibitor and their use |
| ES2909910T3 (es) * | 2013-12-20 | 2022-05-10 | Biomed Valley Discoveries Inc | Tratamiento contra el cáncer usando combinaciones de inhibidores de ERK y RAF |
| MX2016008362A (es) * | 2013-12-23 | 2016-09-08 | Novartis Ag | Combinaciones farmaceuticas. |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
| DE102015103158A1 (de) | 2014-03-04 | 2015-09-10 | Bergische Universität Wuppertal | Verbindungen für die Behandlung des Melanoms |
| DK3116909T3 (da) | 2014-03-14 | 2020-01-20 | Novartis Ag | Antistofmolekyler til lag-3 og anvendelser deraf |
| WO2015145388A2 (en) | 2014-03-27 | 2015-10-01 | Novartis Ag | Methods of treating colorectal cancers harboring upstream wnt pathway mutations |
| US10428387B2 (en) | 2014-05-16 | 2019-10-01 | University Of Massachusetts | Treating chronic myelogenous leukemia (CML) |
| WO2015196072A2 (en) | 2014-06-19 | 2015-12-23 | Whitehead Institute For Biomedical Research | Uses of kinase inhibitors for inducing and maintaining pluripotency |
| US10167279B2 (en) * | 2014-09-12 | 2019-01-01 | Novartis Ag | Compounds and compositions as RAF kinase inhibitors |
| US11344620B2 (en) | 2014-09-13 | 2022-05-31 | Novartis Ag | Combination therapies |
| EP3200775B1 (en) | 2014-10-03 | 2019-11-20 | Novartis AG | Combination therapies |
| MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
| KR102513870B1 (ko) | 2014-10-14 | 2023-03-23 | 노파르티스 아게 | Pd-l1에 대한 항체 분자 및 그의 용도 |
| MX2017011597A (es) | 2015-03-10 | 2018-05-11 | Aduro Biotech Inc | Composiciones y metodos para activar la señalizacion dependiente del "estimulador del gen de interferon". |
| CN108025051B (zh) | 2015-07-29 | 2021-12-24 | 诺华股份有限公司 | 包含抗pd-1抗体分子的联合疗法 |
| WO2017019897A1 (en) | 2015-07-29 | 2017-02-02 | Novartis Ag | Combination therapies comprising antibody molecules to tim-3 |
| DK3317301T3 (da) | 2015-07-29 | 2021-06-28 | Immutep Sas | Kombinationsterapier omfattende antistofmolekyler mod lag-3 |
| MA43186B1 (fr) | 2015-11-03 | 2022-03-31 | Janssen Biotech Inc | Anticorps se liant spécifiquement à pd-1 et leurs utilisations |
| JP2019503349A (ja) | 2015-12-17 | 2019-02-07 | ノバルティス アーゲー | Ｐｄ−１に対する抗体分子およびその使用 |
| EP3738953A1 (en) | 2015-12-30 | 2020-11-18 | Saint Louis University | Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists with improved pharmacokinetic properties and methods for their manufacture |
| RU2615986C1 (ru) * | 2016-02-25 | 2017-04-12 | Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") | Замещенные метил (2-{ 4-[3-(3-метансульфониламино-2-фтор-5-хлор-фенил)-1Н-пиразол-4-ил]пиримидин-2-иламино} -этил)карбаматы, способ их получения и применения |
| SI3463345T1 (sl) | 2016-06-03 | 2023-02-28 | Array Biopharma Inc. | Farmacevtski sestavki |
| WO2018009466A1 (en) | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
| JP7076741B2 (ja) | 2016-12-27 | 2022-05-30 | 国立研究開発法人理化学研究所 | Ｂｍｐシグナル阻害化合物 |
| WO2018146253A1 (en) | 2017-02-10 | 2018-08-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway |
| UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
| CN107540699A (zh) * | 2017-10-16 | 2018-01-05 | 康化（上海）新药研发有限公司 | 一种2‑氨基‑3‑氟吡啶‑4‑硼酸盐酸盐的合成方法 |
| WO2019133810A1 (en) | 2017-12-28 | 2019-07-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
| US12398209B2 (en) | 2018-01-22 | 2025-08-26 | Janssen Biotech, Inc. | Methods of treating cancers with antagonistic anti-PD-1 antibodies |
| JP7262843B2 (ja) * | 2018-07-12 | 2023-04-24 | 深▲チェン▼市塔吉瑞生物医薬有限公司 | ジアリールピラゾール化合物、該化合物を含む組成物およびその使用 |
| WO2020124397A1 (en) * | 2018-12-19 | 2020-06-25 | Inventisbio Shanghai Ltd. | C-terminal src kinase inhibitors |
| SG11202106635WA (en) | 2018-12-21 | 2021-07-29 | Daiichi Sankyo Co Ltd | Combination of antibody-drug conjugate and kinase inhibitor |
| WO2020231976A1 (en) | 2019-05-16 | 2020-11-19 | Eli Lilly And Company | Triple combination of an erk1/2 inhibitor with a braf inhibitor and an egfr inhibitor for use in the treatment of brafv600e colorectal cancer |
| EP4069692A1 (en) | 2019-12-05 | 2022-10-12 | Institut National de la Santé et de la Recherche Médicale (INSERM) | N-(3-(5-(pyrimidin-4-yl)thiazol-4-yl)phenyl)sulfonamide compounds and their uses as braf inhibitors |
| PE20231651A1 (es) | 2020-06-09 | 2023-10-17 | Array Biopharma Inc | Compuestos para el tratamiento de enfermedades y trastornos asociados a braf |
| EP4196228A1 (en) | 2020-08-13 | 2023-06-21 | Albert Einstein College of Medicine | N-cyclyl-sulfonamides useful for inhibiting raf |
| WO2022074011A1 (en) | 2020-10-05 | 2022-04-14 | Pierre Fabre Medicament | Combination of encorafenib and binimetinib as adjuvant treatment for resected stage ii melanoma |
| CN117321418A (zh) | 2021-03-18 | 2023-12-29 | 诺华股份有限公司 | 癌症生物标志物及其使用方法 |
| US12371667B2 (en) | 2021-05-13 | 2025-07-29 | Washington University | Enhanced methods for inducing and maintaining naive human pluripotent stem cells |
| WO2022258612A1 (en) | 2021-06-09 | 2022-12-15 | F. Hoffmann-La Roche Ag | Combination therapy for cancer treatment |
| CN114181197B (zh) * | 2022-02-16 | 2022-05-06 | 北京康立生医药技术开发有限公司 | 一种治疗肠癌的药物的制备方法、制剂及纯度分析方法 |
| WO2023230554A1 (en) | 2022-05-25 | 2023-11-30 | Pfizer Inc. | Combination of a braf inhibitor, an egfr inhibitor, and a pd-1 antagonist for the treatment of braf v600e-mutant, msi-h/dmmr colorectal cancer |
| WO2024163166A1 (en) * | 2023-01-30 | 2024-08-08 | 5Metis, Inc. | Boron containing compounds and their uses |
| CN116396222A (zh) * | 2023-04-10 | 2023-07-07 | 上海睿腾医药科技有限公司 | 一种康奈非尼中间体1-（3-氨基-1-异丙基-1h-吡唑-4-基）乙-1-酮的合成方法 |
| WO2025003956A1 (en) | 2023-06-30 | 2025-01-02 | Pfizer Inc. | High drug loading formulations of encorafenib |
Family Cites Families (72)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4104250A (en) * | 1976-08-11 | 1978-08-01 | Borg-Warner Corporation | Flame-retardant polymers with 1,3,5-triazines having halo- and halo-aryl substitutents |
| JPS5475888A (en) | 1977-11-29 | 1979-06-18 | Jiyasuko Kk | Surgical laser |
| DE3571974D1 (en) | 1984-12-06 | 1989-09-07 | Pfizer | Substituted dihydroquinolone carboxylic acids, anti-bacterial compositions containing them |
| US6358932B1 (en) | 1994-05-31 | 2002-03-19 | Isis Pharmaceticals, Inc. | Antisense oligonucleotide inhibition of raf gene expression |
| US6391636B1 (en) | 1994-05-31 | 2002-05-21 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation of raf gene expression |
| US6037136A (en) | 1994-10-24 | 2000-03-14 | Cold Spring Harbor Laboratory | Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto |
| JPH11514979A (ja) | 1995-09-07 | 1999-12-21 | フイズ テクノロジーズ リミテッド | 実質的に非溶解性の生体作用薬剤をバイオ・アベイラブルにするシステム |
| US5717100A (en) | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
| WO1997044058A1 (en) | 1996-05-23 | 1997-11-27 | Applied Research Systems Ars Holding N.V. | Compounds that inhibit the binding of raf-1 or 14-3-3 proteins to the beta chain of il-2 receptor, and pharmaceutical compositions containing same |
| AR012634A1 (es) | 1997-05-02 | 2000-11-08 | Sugen Inc | Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| EP1000055A1 (en) | 1997-05-22 | 2000-05-17 | G.D. Searle & Co. | SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS |
| US6187799B1 (en) | 1997-05-23 | 2001-02-13 | Onyx Pharmaceuticals | Inhibition of raf kinase activity using aryl ureas |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| US6022884A (en) | 1997-11-07 | 2000-02-08 | Amgen Inc. | Substituted pyridine compounds and methods of use |
| US6204467B1 (en) | 1998-03-24 | 2001-03-20 | Ford Global Technologies, Inc. | Method and apparatus for resistive welding |
| ME00275B (me) | 1999-01-13 | 2011-02-10 | Bayer Corp | ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE |
| US6316435B2 (en) | 1999-02-24 | 2001-11-13 | Supergen, Inc. | Combination therapy for lymphoproliferative diseases |
| AU782469B2 (en) | 1999-12-23 | 2005-08-04 | Mayne Pharma International Pty Ltd | Improved pharmaceutical compositions for poorly soluble drugs |
| WO2002018654A1 (en) | 2000-08-30 | 2002-03-07 | The Board Of Trustees Of The University Of Arkansas | Induction of ldl receptor expression by extracellular-signal regulated kinase, erk-1/2 |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| DK1441714T3 (da) | 2001-10-25 | 2008-03-31 | Novartis Ag | Kombinationer omfattende en selektiv cyclooxygenase-2-inhibitor |
| AU2002356301A1 (en) | 2001-12-21 | 2003-07-15 | Cancer Research Technology Ltd. | 3,4-diarylpyrazoles and their use in the therapy of cancer |
| PL401637A1 (pl) | 2002-03-13 | 2013-05-27 | Array Biopharma Inc. | N3 alkilowane pochodne benzimidazolu jako inhibitory MEK |
| EA200600495A1 (ru) | 2003-09-23 | 2006-10-27 | Новартис Аг | Комбинация ингибитора vegf рецептора с химиотерапевтическим агентом |
| DK1692113T3 (en) | 2003-11-14 | 2018-01-08 | Lorus Therapeutics Inc | ARYLIMIDAZOLES AND USE THEREOF AS ANTICANCES |
| CN1906188A (zh) | 2004-01-09 | 2007-01-31 | 诺瓦提斯公司 | 作为igf－1r抑制剂的苯基－[4－(3－苯基－1h－吡唑－4－基)－嘧啶－2－基]－胺衍生物 |
| CA2567662C (en) | 2004-06-10 | 2012-11-27 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| US20060058311A1 (en) | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| BRPI0606281A2 (pt) | 2005-03-17 | 2009-06-09 | Novartis Ag | compostos orgánicos |
| US20070099856A1 (en) | 2005-05-13 | 2007-05-03 | Gumerlock Paul H | Combined treatment with docetaxel and an epidermal growth factor receptor kinase inhibitor using an intermittent dosing regimen |
| EP1934185A1 (en) | 2005-08-12 | 2008-06-25 | Synta Pharmaceuticals Corporation | Pyrazole compounds that modulate hsp90 activity |
| CA2619035A1 (en) | 2005-08-22 | 2007-03-01 | Novartis Ag | Pharmaceutical compositions |
| US20080242667A1 (en) | 2005-08-26 | 2008-10-02 | Smithkline Beecham Corporation | Pyrimidinyl-Pyrazole Inhibitors of Aurora Kinases |
| PE20070335A1 (es) | 2005-08-30 | 2007-04-21 | Novartis Ag | Benzimidazoles sustituidos y metodos para su preparacion |
| EP2024353A2 (en) * | 2006-03-16 | 2009-02-18 | Pfizer Products Inc. | Pyrazole compounds |
| KR20080108516A (ko) | 2006-04-05 | 2008-12-15 | 노파르티스 아게 | 암을 치료하기 위한 치료제의 조합물 |
| WO2007123892A2 (en) * | 2006-04-17 | 2007-11-01 | Arqule Inc. | Raf inhibitors and their uses |
| EP2061772A4 (en) | 2006-09-11 | 2011-06-29 | Curis Inc | MULTIFUNCTIONAL SMALL MOLECULES AS PROLIFERATION-ACTIVE ACTIVE SUBSTANCES |
| WO2008034776A1 (en) | 2006-09-18 | 2008-03-27 | Boehringer Ingelheim International Gmbh | Method for treating cancer harboring egfr mutations |
| MX2009003456A (es) | 2006-10-02 | 2009-04-14 | Irm Llc | Compuestos y composiciones como inhibidores de proteina cinasa. |
| CN101522026A (zh) * | 2006-10-06 | 2009-09-02 | Irm责任有限公司 | 蛋白激酶抑制剂及其应用方法 |
| WO2008100985A2 (en) | 2007-02-15 | 2008-08-21 | Novartis Ag | Combination of lbh589 with other therapeutic agents for treating cancer |
| US20090022789A1 (en) | 2007-07-18 | 2009-01-22 | Supernus Pharmaceuticals, Inc. | Enhanced formulations of lamotrigine |
| EA201000113A1 (ru) * | 2007-08-01 | 2010-08-30 | Пфайзер Инк. | Пиразольные соединения |
| EP2197425A2 (en) | 2007-10-19 | 2010-06-23 | Abbott GmbH & Co. KG | Solid dispersion product of n-aryl urea-based drugs |
| WO2009062676A2 (en) * | 2007-11-14 | 2009-05-22 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| BRPI0908906A2 (pt) * | 2008-03-21 | 2019-09-24 | Novartis Ag | compostos heterocíclicos e usos dos mesmos |
| UA103319C2 (en) * | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| EA019722B1 (ru) * | 2008-07-24 | 2014-05-30 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | 3,4-диарилпиразолы в качестве ингибиторов протеинкиназ |
| KR20110038159A (ko) | 2008-07-28 | 2011-04-13 | 길리애드 사이언시즈, 인코포레이티드 | 사이클로알킬리덴 및 헤테로사이클로알킬리덴 히스톤 데아세틸라아제 억제제 화합물 |
| AR073700A1 (es) | 2008-09-29 | 2010-11-24 | Boehringer Ingelheim Int | Heterociclos y composiciones farmaceuticas para usarse en el tratamiento de cancer, infecciones y enfermedades autoinmunitarias |
| CA2737400C (en) | 2008-10-07 | 2016-11-22 | Astrazeneca Uk Limited | Pharmaceutical formulation 514 |
| US20110293750A1 (en) * | 2008-11-11 | 2011-12-01 | Yale University | Activated wnt-beta-catenin signaling in melanoma |
| WO2010070060A1 (en) | 2008-12-19 | 2010-06-24 | Nerviano Medical Sciences S.R.L. | Bicyclic pyrazoles as protein kinase inhibitors |
| AR075180A1 (es) | 2009-01-29 | 2011-03-16 | Novartis Ag | Formulaciones orales solidas de una pirido-pirimidinona |
| RU2402602C1 (ru) | 2009-02-12 | 2010-10-27 | Государственное учреждение Российский онкологический научный центр им. Н.Н. Блохина РАМН | КЛЕТОЧНАЯ ЛИНИЯ МЕЛАНОМЫ ЧЕЛОВЕКА mel Rac, ИСПОЛЬЗУЕМАЯ ДЛЯ ПОЛУЧЕНИЯ ПРОТИВООПУХОЛЕВЫХ ВАКЦИН |
| WO2010100127A1 (en) | 2009-03-04 | 2010-09-10 | Novartis Ag | Disubstituted imidazole derivatives as modulators of raf kinase |
| TWI532484B (zh) | 2009-06-08 | 2016-05-11 | 艾伯維有限公司 | 包含凋亡促進劑之固態分散劑 |
| JP5789602B2 (ja) * | 2009-06-15 | 2015-10-07 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | 置換ピリミジニルピロロピリジノン誘導体、これらの製造のための方法およびキナーゼ阻害剤としてのこれらの使用 |
| KR101256018B1 (ko) * | 2009-08-20 | 2013-04-18 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물 |
| AR077975A1 (es) | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| US8242260B2 (en) | 2009-08-28 | 2012-08-14 | Novartis Ag | Compounds and compositions as protein kinase inhibitors |
| EA023942B1 (ru) | 2010-01-27 | 2016-07-29 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Сульфонамидные производные 3,4-диарилпиразолов в качестве ингибиторов протеинкиназы |
| SG10201502484SA (en) | 2010-03-30 | 2015-05-28 | Verseon Corp | Multisubstituted aromatic compounds as inhibitors of thrombin |
| JP5938038B2 (ja) | 2010-08-03 | 2016-06-22 | ネルヴィアーノ・メディカル・サイエンシズ・ソチエタ・ア・レスポンサビリタ・リミタータ | ピラゾロフェニル−ベンゼンスルホンアミド化合物の誘導体及びその抗腫瘍薬としての使用 |
| HUE032100T2 (en) | 2011-03-21 | 2017-08-28 | Valcuria Ab | A pharmaceutical composition comprising an HDAC inhibitor and a steroid and its use |
| JP6200884B2 (ja) | 2011-06-14 | 2017-09-20 | ノバルティス アーゲー | 骨髄増殖性腫瘍などの癌の治療におけるパノビノスタットおよびルキソリチニブの組合せ |
| WO2013070996A1 (en) | 2011-11-11 | 2013-05-16 | Novartis Ag | Method of treating a proliferative disease |
| AU2012340759C1 (en) | 2011-11-23 | 2019-11-28 | Array Biopharma Inc. | Pharmaceutical formulations |
| JP2015536964A (ja) | 2012-11-08 | 2015-12-24 | ノバルティス アーゲー | Ｂ−ｒａｆ阻害剤とヒストン脱アセチル化酵素阻害剤を含む医薬組合せおよび増殖性疾患の治療におけるそれらの使用 |
| US10576680B2 (en) | 2015-11-19 | 2020-03-03 | The Boeing Company | Modular thermoforming system |
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