HRP20100603T1 - Derivati pirimidina koji se koriste kao inhibitori pi-3 kinaze - Google Patents
Derivati pirimidina koji se koriste kao inhibitori pi-3 kinaze Download PDFInfo
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- HRP20100603T1 HRP20100603T1 HR20100603T HRP20100603T HRP20100603T1 HR P20100603 T1 HRP20100603 T1 HR P20100603T1 HR 20100603 T HR20100603 T HR 20100603T HR P20100603 T HRP20100603 T HR P20100603T HR P20100603 T1 HRP20100603 T1 HR P20100603T1
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- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 title 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 49
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 36
- 239000001257 hydrogen Substances 0.000 claims abstract 36
- 229910052736 halogen Inorganic materials 0.000 claims abstract 25
- 150000002367 halogens Chemical class 0.000 claims abstract 25
- 125000000217 alkyl group Chemical group 0.000 claims abstract 22
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 21
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 15
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 14
- 125000003118 aryl group Chemical group 0.000 claims abstract 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 13
- 150000002431 hydrogen Chemical class 0.000 claims abstract 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 13
- 150000003839 salts Chemical class 0.000 claims abstract 11
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 9
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 7
- 125000000304 alkynyl group Chemical group 0.000 claims abstract 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 7
- -1 hydroxy, amino Chemical group 0.000 claims abstract 6
- 229940124530 sulfonamide Drugs 0.000 claims abstract 4
- 150000003456 sulfonamides Chemical class 0.000 claims abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 20
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 241001465754 Metazoa Species 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 3
- CWHUFRVAEUJCEF-UHFFFAOYSA-N BKM120 Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2CCOCC2)=NC(N2CCOCC2)=N1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 claims 2
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 2
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical class C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 2
- 229960002584 gefitinib Drugs 0.000 claims 2
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 2
- 229960002411 imatinib Drugs 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- YCOYDOIWSSHVCK-UHFFFAOYSA-N vatalanib Chemical group C1=CC(Cl)=CC=C1NC(C1=CC=CC=C11)=NN=C1CC1=CC=NC=C1 YCOYDOIWSSHVCK-UHFFFAOYSA-N 0.000 claims 2
- 229950000578 vatalanib Drugs 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- XKVODZRJCXLQCY-CYBMUJFWSA-N 1-[(3r)-3-[6-(2,4-diaminopyrimidin-5-yl)-2-morpholin-4-ylpyrimidin-4-yl]oxypiperidin-1-yl]ethanone Chemical compound C1N(C(=O)C)CCC[C@H]1OC1=CC(C=2C(=NC(N)=NC=2)N)=NC(N2CCOCC2)=N1 XKVODZRJCXLQCY-CYBMUJFWSA-N 0.000 claims 1
- WJKGLEPYSVEMMR-CYBMUJFWSA-N 1-[(3r)-3-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]oxypyrrolidin-1-yl]ethanone Chemical compound C1N(C(=O)C)CC[C@H]1OC1=CC(C=2C(=CC(N)=NC=2)C(F)(F)F)=NC(N2CCOCC2)=N1 WJKGLEPYSVEMMR-CYBMUJFWSA-N 0.000 claims 1
- WJKGLEPYSVEMMR-ZDUSSCGKSA-N 1-[(3s)-3-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]oxypyrrolidin-1-yl]ethanone Chemical compound C1N(C(=O)C)CC[C@@H]1OC1=CC(C=2C(=CC(N)=NC=2)C(F)(F)F)=NC(N2CCOCC2)=N1 WJKGLEPYSVEMMR-ZDUSSCGKSA-N 0.000 claims 1
- IRGQATMSWNBAAN-UHFFFAOYSA-N 1-[2-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-6-morpholin-4-ylpyrimidin-4-yl]piperidin-2-one Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=NC(N2CCOCC2)=CC(N2C(CCCC2)=O)=N1 IRGQATMSWNBAAN-UHFFFAOYSA-N 0.000 claims 1
- DAVMGHKVRIVQHK-UHFFFAOYSA-N 1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-3-phenylimidazolidin-2-one Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2C(N(CC2)C=2C=CC=CC=2)=O)=NC(N2CCOCC2)=N1 DAVMGHKVRIVQHK-UHFFFAOYSA-N 0.000 claims 1
- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 claims 1
- HLWTXVAXGWFIGD-UHFFFAOYSA-N 2-amino-5-[2-morpholin-4-yl-6-(quinolin-3-ylamino)pyrimidin-4-yl]pyridine-4-carbonitrile Chemical compound C1=NC(N)=CC(C#N)=C1C1=CC(NC=2C=C3C=CC=CC3=NC=2)=NC(N2CCOCC2)=N1 HLWTXVAXGWFIGD-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004487 4-tetrahydropyranyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- GPSNQTAHWLFUMS-UHFFFAOYSA-N 5-(2-morpholin-4-yl-6-piperidin-4-yloxypyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(OC2CCNCC2)=NC(N2CCOCC2)=N1 GPSNQTAHWLFUMS-UHFFFAOYSA-N 0.000 claims 1
- QJJOWBBWAJMFKV-UHFFFAOYSA-N 5-(2-morpholin-4-yl-6-piperidin-4-yloxypyrimidin-4-yl)pyrimidine-2,4-diamine Chemical compound NC1=NC(N)=NC=C1C1=CC(OC2CCNCC2)=NC(N2CCOCC2)=N1 QJJOWBBWAJMFKV-UHFFFAOYSA-N 0.000 claims 1
- ZCLGMFVGVKWRBN-UHFFFAOYSA-N 5-(2-morpholin-4-yl-6-pyridin-3-yloxypyrimidin-4-yl)pyrimidin-2-amine Chemical compound C1=NC(N)=NC=C1C1=CC(OC=2C=NC=CC=2)=NC(N2CCOCC2)=N1 ZCLGMFVGVKWRBN-UHFFFAOYSA-N 0.000 claims 1
- BVDFIHKEDFXZGJ-UHFFFAOYSA-N 5-[2-morpholin-4-yl-6-(2-phenylmorpholin-4-yl)pyrimidin-4-yl]pyrimidin-2-amine Chemical compound C1=NC(N)=NC=C1C1=CC(N2CC(OCC2)C=2C=CC=CC=2)=NC(N2CCOCC2)=N1 BVDFIHKEDFXZGJ-UHFFFAOYSA-N 0.000 claims 1
- CXHHDYIDOQJRSB-UHFFFAOYSA-N 5-[2-morpholin-4-yl-6-(oxan-4-yloxy)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(OC2CCOCC2)=NC(N2CCOCC2)=N1 CXHHDYIDOQJRSB-UHFFFAOYSA-N 0.000 claims 1
- USBKPGIHJDOWOB-LLVKDONJSA-N 5-[2-morpholin-4-yl-6-[(3r)-oxolan-3-yl]oxypyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(O[C@H]2COCC2)=NC(N2CCOCC2)=N1 USBKPGIHJDOWOB-LLVKDONJSA-N 0.000 claims 1
- SSUDJOSHFSFMEP-GFCCVEGCSA-N 5-[2-morpholin-4-yl-6-[(3r)-piperidin-3-yl]oxypyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(O[C@H]2CNCCC2)=NC(N2CCOCC2)=N1 SSUDJOSHFSFMEP-GFCCVEGCSA-N 0.000 claims 1
- USBKPGIHJDOWOB-NSHDSACASA-N 5-[2-morpholin-4-yl-6-[(3s)-oxolan-3-yl]oxypyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(O[C@@H]2COCC2)=NC(N2CCOCC2)=N1 USBKPGIHJDOWOB-NSHDSACASA-N 0.000 claims 1
- SSUDJOSHFSFMEP-LBPRGKRZSA-N 5-[2-morpholin-4-yl-6-[(3s)-piperidin-3-yl]oxypyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(O[C@@H]2CNCCC2)=NC(N2CCOCC2)=N1 SSUDJOSHFSFMEP-LBPRGKRZSA-N 0.000 claims 1
- VNVTYBPKOXYXRR-UHFFFAOYSA-N 6-(2-aminopyrimidin-5-yl)-n-(2-methoxyethyl)-2-morpholin-4-ylpyrimidin-4-amine Chemical compound N=1C(NCCOC)=CC(C=2C=NC(N)=NC=2)=NC=1N1CCOCC1 VNVTYBPKOXYXRR-UHFFFAOYSA-N 0.000 claims 1
- WZUWBEVLBFHSDB-UHFFFAOYSA-N 6-(2-aminopyrimidin-5-yl)-n-methyl-2-morpholin-4-yl-n-(oxan-4-yl)pyrimidin-4-amine Chemical compound C=1C(C=2C=NC(N)=NC=2)=NC(N2CCOCC2)=NC=1N(C)C1CCOCC1 WZUWBEVLBFHSDB-UHFFFAOYSA-N 0.000 claims 1
- DWXBYTYWBANFCB-UHFFFAOYSA-N 6-(2-aminopyrimidin-5-yl)-n-tert-butyl-2-morpholin-4-ylpyrimidin-4-amine Chemical compound N=1C(NC(C)(C)C)=CC(C=2C=NC(N)=NC=2)=NC=1N1CCOCC1 DWXBYTYWBANFCB-UHFFFAOYSA-N 0.000 claims 1
- VROANLXOBIMUFA-UHFFFAOYSA-N 6-(6-aminopyridin-3-yl)-n-(6-methoxypyridin-3-yl)-2-morpholin-4-ylpyrimidin-4-amine Chemical compound C1=NC(OC)=CC=C1NC1=CC(C=2C=NC(N)=CC=2)=NC(N2CCOCC2)=N1 VROANLXOBIMUFA-UHFFFAOYSA-N 0.000 claims 1
- ONFWLFUSCUBPIH-UHFFFAOYSA-N 6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-yl-n-[4-(1-propan-2-ylpiperidin-4-yl)oxyphenyl]pyrimidin-4-amine Chemical compound C1CN(C(C)C)CCC1OC(C=C1)=CC=C1NC1=CC(C=2C(=CC(N)=NC=2)C(F)(F)F)=NC(N2CCOCC2)=N1 ONFWLFUSCUBPIH-UHFFFAOYSA-N 0.000 claims 1
- QFLIOAOFLZFXMC-UHFFFAOYSA-N 6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-yl-n-[6-(1-propan-2-ylpiperidin-4-yl)oxypyridin-3-yl]pyrimidin-4-amine Chemical compound C1CN(C(C)C)CCC1OC(N=C1)=CC=C1NC1=CC(C=2C(=CC(N)=NC=2)C(F)(F)F)=NC(N2CCOCC2)=N1 QFLIOAOFLZFXMC-UHFFFAOYSA-N 0.000 claims 1
- JRTWKORVIFDHNA-UHFFFAOYSA-N 6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-n-[3-methoxy-4-(1-propan-2-ylpiperidin-4-yl)oxyphenyl]-2-morpholin-4-ylpyrimidin-4-amine Chemical compound C=1C=C(OC2CCN(CC2)C(C)C)C(OC)=CC=1NC(N=1)=CC(C=2C(=CC(N)=NC=2)C(F)(F)F)=NC=1N1CCOCC1 JRTWKORVIFDHNA-UHFFFAOYSA-N 0.000 claims 1
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 238000002372 labelling Methods 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- OLEQMKFFMNHBSI-UHFFFAOYSA-N methyl 4-[6-(2-amino-6-oxo-1h-pyrimidin-5-yl)-2-morpholin-4-ylpyrimidin-4-yl]oxypiperidine-1-carboxylate Chemical compound C1CN(C(=O)OC)CCC1OC1=CC(C=2C(NC(N)=NC=2)=O)=NC(N2CCOCC2)=N1 OLEQMKFFMNHBSI-UHFFFAOYSA-N 0.000 claims 1
- GJOPPYUMRDERJE-UHFFFAOYSA-N n-[3-[6-(6-aminopyridin-3-yl)-2-morpholin-4-ylpyrimidin-4-yl]pyridin-2-yl]methanesulfonamide Chemical compound CS(=O)(=O)NC1=NC=CC=C1C1=CC(C=2C=NC(N)=CC=2)=NC(N2CCOCC2)=N1 GJOPPYUMRDERJE-UHFFFAOYSA-N 0.000 claims 1
- SYPNVSVTWDNXJU-UHFFFAOYSA-N n-[6-(2-aminopyrimidin-5-yl)-2-morpholin-4-ylpyrimidin-4-yl]-5-methoxyquinolin-3-amine Chemical compound C1=C2C(OC)=CC=CC2=NC=C1NC(N=1)=CC(C=2C=NC(N)=NC=2)=NC=1N1CCOCC1 SYPNVSVTWDNXJU-UHFFFAOYSA-N 0.000 claims 1
- LICCCQJZOPRJSR-UHFFFAOYSA-N n-[6-(2-aminopyrimidin-5-yl)-2-morpholin-4-ylpyrimidin-4-yl]quinolin-3-amine Chemical compound C1=NC(N)=NC=C1C1=CC(NC=2C=C3C=CC=CC3=NC=2)=NC(N2CCOCC2)=N1 LICCCQJZOPRJSR-UHFFFAOYSA-N 0.000 claims 1
- AAGMAOVYPSOAOX-UHFFFAOYSA-N n-[6-(6-amino-4-fluoropyridin-3-yl)-2-morpholin-4-ylpyrimidin-4-yl]quinolin-3-amine Chemical compound C1=NC(N)=CC(F)=C1C1=CC(NC=2C=C3C=CC=CC3=NC=2)=NC(N2CCOCC2)=N1 AAGMAOVYPSOAOX-UHFFFAOYSA-N 0.000 claims 1
- NHIATJMNLHUPCB-UHFFFAOYSA-N n-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-4-[2-(diethylamino)ethyl]-1,3-thiazol-2-amine Chemical compound CCN(CC)CCC1=CSC(NC=2N=C(N=C(C=2)C=2C(=CC(N)=NC=2)C(F)(F)F)N2CCOCC2)=N1 NHIATJMNLHUPCB-UHFFFAOYSA-N 0.000 claims 1
- HRKLHXAWCDUDFO-UHFFFAOYSA-N n-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-4-phenyl-1,3-thiazol-2-amine Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(NC=2SC=C(N=2)C=2C=CC=CC=2)=NC(N2CCOCC2)=N1 HRKLHXAWCDUDFO-UHFFFAOYSA-N 0.000 claims 1
- PLVUFUDHSFMSTP-UHFFFAOYSA-N n-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-5-(diethylaminomethyl)-1,3-thiazol-2-amine Chemical compound S1C(CN(CC)CC)=CN=C1NC1=CC(C=2C(=CC(N)=NC=2)C(F)(F)F)=NC(N2CCOCC2)=N1 PLVUFUDHSFMSTP-UHFFFAOYSA-N 0.000 claims 1
- MFWHRPHYUREIFE-UHFFFAOYSA-N n-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-5-methyl-2-morpholin-4-ylpyrimidin-4-yl]-4-phenyl-1,3-thiazol-2-amine Chemical compound N1=C(N2CCOCC2)N=C(C=2C(=CC(N)=NC=2)C(F)(F)F)C(C)=C1NC(SC=1)=NC=1C1=CC=CC=C1 MFWHRPHYUREIFE-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- OYRRZWATULMEPF-UHFFFAOYSA-N pyrimidin-4-amine Chemical compound NC1=CC=NC=N1 OYRRZWATULMEPF-UHFFFAOYSA-N 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 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 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 150000003527 tetrahydropyrans Chemical class 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
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- 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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- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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US76078906P | 2006-01-20 | 2006-01-20 | |
PCT/US2007/001708 WO2007084786A1 (en) | 2006-01-20 | 2007-01-22 | Pyrimidine derivatives used as pi-3 kinase inhibitors |
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HR20100603T HRP20100603T1 (hr) | 2006-01-20 | 2010-11-09 | Derivati pirimidina koji se koriste kao inhibitori pi-3 kinaze |
HRP20130796TT HRP20130796T1 (en) | 2006-01-20 | 2013-08-22 | Pyrimidine derivatives used as pi-3 kinase inhibitors |
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