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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Abstract
Spoj, naznačen time, da ima formulu I: ili njegov stereoizomer, tautomer ili farmaceutski prihvatljiva sol, gdje W je CRW ili N, gdje RW je odabran iz skupine koja sadrživodik, cijano, halogen, metil, trifluorometil, sulfonamid; R1 je odabran iz skupine koja sadrživodik, cijano, nitro, halogen, supstituirani i nesupstituirani alkil, supstituirani i nesupstituirani alkenil, supstituirani i nesupstituirani alkinil, supstituirani i nesupstituirani aril, supstituirani i nesupstituirani heteroaril, supstituirani i nesupstituirani heterociklil, supstituirani i nesupstituirani cikloalkil,-COR1a,-CO2R1a,-CONR1aR1b,-NR1aR1b,-NR1aCOR1b,-NR1aSO2R1b,-OCOR1a,-OR1a,-SR1a,-SOR1a,-SO2R1a, i-SO2NR1aR1b,gdje R1a i R1b su neovisno odabrani iz skupine koja sadrži vodik, supstituirani ili nesupstituirani alkil, supstituirani i nesupstituirani aril, supstituirani i nesupstituirani heteroaril, supstituirani i nesupstituirani heterociklil, isupstituirani i nesupstituirani cikloalkil; R2 je odabran iz skupine koja sadrživodik, cijano, nitro, halogen, hidroksi, amino, supstituirani i nesupstituirani alkil,-COR2a, i-NR2aCOR2b,gdje R2a i R2b su neovisno odabrani iz skupine koja sadrživodik, isupstituirani ili nesupstituirani alkil; R3 je odabran iz skupine koja sadrživodik, cijano, nitro, halogen, supstituirani i nesupstituirani alkil, supstituirani i nesupstituirani alkenil, supstituirani i nesupstituirani alkinil, supstituirani i nesupstituirani aril, supstituirani i nesupstituirani heteroaril, supstituirani i nesupstituirani heterociklil, supstituirani i nesupstituirani cikloalkil,-COR3a,-NR3aR3b,-NR3aCOR3b,-NR3aSO2R3b,-OR3a,-SR3a,-SOR3a,-SO2R3a, i-SO2NR3aR3b,gdje R3a i R3b su neovisno odabrani iz skupine koja sadrživodik, supstituirani ili nesupstituirani alkil, supstituirani i nesupstituirani aril, supstituirani i nesupstituirani heteroaril, supstituirani i nesupstituirani heterociklil, isupstituirani i nesupstituirani cikloalkil; iR4 je odabran iz skupine koja sadrživodik, ihalogen. Patent sadrži još 52 patentna zahtjeva.
Claims (53)
1. Spoj, naznačen time, da ima formulu I:
[image]
ili njegov stereoizomer, tautomer ili farmaceutski prihvatljiva sol, gdje W je CRW ili N, gdje RWje odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) halogen,
(4) metil,
(5) rifluorometil,
(6) sulfonamid;
R1 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) nitro,
(4) halogen,
(5) supstituirani i nesupstituirani alkil,
(6) supstituirani i nesupstituirani alkenil,
(7) supstituirani i nesupstituirani alkinil,
(8) supstituirani i nesupstituirani aril,
(9) supstituirani i nesupstituirani heteroaril,
(10) supstituirani i nesupstituirani heterociklil,
(11) supstituirani i nesupstituirani cikloalkil,
(12) –COR1a,
(13) –CO2R1a,
(14) –CONR1aR1b,
(15) –NR1aR1b,
(16) –NR1aCOR1b,
(17) –NR1aSO2R1b,
(18) –OCOR1a,
(19) –OR1a,
(20) –SR1a,
(21) –SOR1a,
(22) –SO2R1a, i
(23) –SO2NR1aR1b,
gdje R1a i R1b su neovisno odabrani iz skupine koja sadrži
(a) vodik,
(b) supstituirani ili nesupstituirani alkil,
(c) supstituirani i nesupstituirani aril,
(d) supstituirani i nesupstituirani heteroaril,
(e) supstituirani i nesupstituirani heterociklil, i
(f) supstituirani i nesupstituirani cikloalkil;
R2 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) nitro,
(4) halogen,
(5) hidroksi,
(6) amino,
(7) supstituirani i nesupstituirani alkil,
(8) –COR2a, i
(9) –NR2aCOR2b,
gdje R2a i R2b su neovisno odabrani iz skupine koja sadrži
(a) vodik, i
(b) supstituirani ili nesupstituirani alkil;
R3 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) nitro,
(4) halogen,
(5) supstituirani i nesupstituirani alkil,
(6) supstituirani i nesupstituirani alkenil,
(7) supstituirani i nesupstituirani alkinil,
(8) supstituirani i nesupstituirani aril,
(9) supstituirani i nesupstituirani heteroaril,
(10) supstituirani i nesupstituirani heterociklil,
(11) supstituirani i nesupstituirani cikloalkil,
(12) –COR3a,
(13) –NR3aR3b,
(14) –NR3aCOR3b,
(15) –NR3aSO2R3b,
(16) –OR3a,
(17) –SR3a,
(18) –SOR3a,
(19) –SO2R3a, i
(20) –SO2NR3aR3b,
gdje R3a i R3b su neovisno odabrani iz skupine koja sadrži
(a) vodik,
(b) supstituirani ili nesupstituirani alkil,
(c) supstituirani i nesupstituirani aril,
(d) supstituirani i nesupstituirani heteroaril,
(e) supstituirani i nesupstituirani heterociklil, i
(f) supstituirani i nesupstituirani cikloalkil;
i
R4 je odabran iz skupine koja sadrži
(1) vodik, i
(2) halogen.
2. Spoj prema Zahtjevu 1, naznačen time, da W je N.
3. Spoj prema Zahtjevu 1, naznačen time, da W je CH.
4. Spoj prema Zahtjevu 1, naznačen time, da R1 je odabran iz skupine koja sadrži
(1) supstituirani i nesupstituirani alkil,
(2) supstituirani i nesupstituirani aril,
(3) supstituirani i nesupstituirani heteroaril,
(4) supstituirani i nesupstituirani heterociklil,
(5) supstituirani i nesupstituirani cikloalkil,
(6) –OR1a, i
(7) –NR1aR1b,
gdje R1a i R1b su neovisno odabrani iz skupine koja sadrži
(a) supstituirani i nesupstituirani heteroaril, i
(b) supstituirani i nesupstituirani heterociklil.
5. Spoj prema Zahtjevu 4, naznačen time, da R1 je supstituirani ili nesupstituirani heterociklil, ili supstituirani ili nesupstituirani –O-heterociklil.
6. Spoj prema Zahtjevu 4, naznačen time, da R1 je supstituirani ili nesupstituirani morfolinil.
7. Spoj prema Zahtjevu 6, naznačen time, da R1 je nesupstituirani N-povezan morfolinil.
8. Spoj prema Zahtjevu 4, naznačen time, da R1 je supstituirani ili nesupstituirani tetrahidropiran ili supstituirani ili nesupstituirani tetrahidropiraniloksi.
9. Spoj prema Zahtjevu 8, naznačen time, da R1 je nesupstituirani 4-tetrahidropiraniloksi.
10. Spoj prema Zahtjevu 4, naznačen time, da R1 je supstituirani ili nesupstituirani tetrahidrofuran ili supstituirani ili nesupstituirani tetrahidrofuraniloksi.
11. Spoj prema Zahtjevu 10, naznačen time, da R1 je nesupstituirani 3-tetrahidrofuraniloksi.
12. Spoj prema Zahtjevu 1, naznačen time, da R2 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) hidroksi,
(4) halogen,
(5) amino,
(6) metil, i
(7) trifluorometil.
13. Spoj prema Zahtjevu 1, naznačen time, da R2 je vodik ili halogen.
14. Spoj prema Zahtjevu 1, naznačen time, da R2 je vodik.
15. Spoj prema Zahtjevu 1, naznačen time, da R3 je odabran iz skupine koja sadrži
(1) cijano,
(2) nitro,
(3) halogen,
(4) hidroksi,
(5) amino, i
(6) trifluorometil.
16. Spoj prema Zahtjevu 1, naznačen time, da R3 je trifluorometil.
17. Spoj prema Zahtjevu 1, naznačen time, da R3 je cijano.
18. Spoj prema Zahtjevu 2, naznačen time, da R3 je =O.
19. Spoj, naznačen time, da ima formulu II:
[image]
ili njegov stereoizomer, tautomer ili farmaceutski prihvatljiva sol, gdje W je CRW ili N, gdje je RW odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) halogen,
(4) metil,
(5) trifluorometil, i
(6) sulfonamid;
X je O, S, NH, ili direktna veza;
R2 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) nitro,
(4) halogen,
(5) hidroksi,
(6) amino,
(7) supstituirani i nesupstituirani alkil,
(8) –COR2a, i
(9) –NR2aCOR2b,
gdje R2a i R2bsu neovisno odabrani iz skupine koja sadrži
(a) vodik, i
(b) supstituirani ili nesupstituirani alkil;
R3 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) nitro,
(4) halogen,
(5) supstituirani i nesupstituirani alkil,
(6) supstituirani i nesupstituirani alkenil,
(7) supstituirani i nesupstituirani alkinil,
(8) supstituirani i nesupstituirani aril,
(9) supstituirani i nesupstituirani heteroaril,
(10) supstituirani i nesupstituirani heterociklil,
(11) supstituirani i nesupstituirani cikloalkil,
(12) –COR3a,
(13) –NR3aR3b,
(14) –NR3aCOR3b,
(15) –NR3aSO2R3b,
(16) –OR3a,
(17) –SR3a,
(18) –SOR3a,
(19) –SO2R3a, i
(20) –SO2NR3aR3b,
gdje R3ai R3bsu neovisno odabrani iz skupine koja sadrži
(a) vodik,
(b) supstituirani ili nesupstituirani alkil,
(c) supstituirani i nesupstituirani aril,
(d) supstituirani i nesupstituirani heteroaril,
(e) supstituirani i nesupstituirani heterociklil, i
(f) supstituirani i nesupstituirani cikloalkil;
R4jeodabran iz skupine koja sadrži
(1) vodik, i
(2) halogen; i
R5jeodabran iz skupine koja sadrži
(1) supstituirani i nesupstituirani cikloalkil,
(2) supstituirani i nesupstituirani heterociklil,
(3) supstituirani i nesupstituirani aril, i
(4) supstituirani i nesupstituirani heteroaril.
20. Spoj prema Zahtjevu 19, naznačen time, da R2 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) hidroksi,
(4) amino,
(5) halogen, i
(6) supstituirani i nesupstituirani C1-3alkil.
21. Spoj prema Zahtjevu 19, naznačen time, da R3 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) tio,
(4) halogen,
(5) nitro,
(6) supstituirani i nesupstituirani alkil,
(7) supstituirani i nesupstituirani alkenil,
(8) supstituirani i nesupstituirani alkinil,
(9) –OR3a,
(10) –NR3aR3b,
(11) –COR3a, i
(12) –NR3aCOR3b,
gdje R3ai R3bsu neovisno odabrani iz skupine koja sadrži
(a) vodik, i
(b) supstituirani ili nesupstituirani alkil.
22. Spoj prema Zahtjevu 19, naznačen time, da R3 je trifluorometil.
23. Spoj prema Zahtjevu 19, naznačen time, da W je CH.
24. Spoj prema Zahtjevu 19, naznačen time, da R2 je H.
25. Spoj prema Zahtjevu 19, naznačen time, da R5 je odabran iz skupine koja sadrži
(1) supstituirani ili nesupstituirani morfolinil,
(2) supstituirani ili nesupstituirani tetrahidropiranil, i
(3) supstituirani ili nesupstituirani tetrahidrofuranil.
26. Spoj prema Zahtjevu 19, naznačen time, da X je direktni spoj, a R5 je nesupstituirani N-povezan morfolinil.
27. Spoj prema Zahtjevu 19, naznačen time, da X je O, a R5 je 4-tetrahidropiranil.
28. Spoj prema Zahtjevu 19, naznačen time, da X je O, a R5 je 3-tetrahidrofuranil.
29. Spoj prema Zahtjevu 19, naznačen time, da W je N.
30. Spoj prema Zahtjevu 19, naznačen time, da R3 je =O.
31. Spoj, naznačen time, da ima formulu III:
[image]
ili njegov stereoizomer, tautomer ili farmaceutski prihvatljiva sol, gdje, W je CRW ili N, gdje RW je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) halogen,
(4) metil,
(5) trifluorometil, i
(6) sulfonamid;
R2 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) nitro,
(4) halogen,
(5) hidroksi,
(6) amino,
(7) supstituirani i nesupstituirani alkil,
(8) –COR2a, i
(9) –NR2aCOR2b,
gdje R2a i R2b su neovisno odabrani iz skupine koja sadrži
(a) vodik, i
(b)supstituirani ili nesupstituirani alkil;
R3 je odabran iz skupine koja sadrži
(1) vodik,
(2) cijano,
(3) nitro,
(4) halogen,
(5) supstituirani i nesupstituirani alkil,
(6) supstituirani i nesupstituirani alkenil,
(7) supstituirani i nesupstituirani alkinil,
(8) supstituirani i nesupstituirani aril,
(9) supstituirani i nesupstituirani heteroaril,
(10) supstituirani i nesupstituirani heterociklil,
(11) supstituirani i nesupstituirani cikloalkil,
(12) –COR3a,
(13) –NR3aR3b,
(14) –NR3aCOR3b,
(15) –NR3aSO2R3b,
(16) –OR3a,
(17) –SR3a,
(18) –SOR3a,
(19) –SO2R3a, i
(20) –SO2NR3aR3b,
gdje R3a, i R3b su neovisno odabrani iz skupine koja sadrži
(1) vodik,
(2) supstituirani ili nesupstituirani alkil,
(3) supstituirani i nesupstituirani aril,
(4) supstituirani i nesupstituirani heteroaril,
(5) supstituirani i nesupstituirani heterociklil, i
(6) supstituirani i nesupstituirani cikloalkil;
R4 je odabran iz skupine koja sadrži
(1) vodik, i
(2) halogen; i
R6 je odabran iz skupine koja sadrži
(1) vodik,
(2) supstituirani i nesupstituirani akil, i
(3) supstituirani i nesupstituirani cikloalkil.
32. Spoj prema Zahtjevu 31, naznačen time, da je R2 odabran iz grupe koja sadrži
(1) vodik,
(2) cijano,
(3) hidroksi,
(4) halogen,
(5) amino,
(6) metil, i
(7) trifluorometil.
33. Spoj prema Zahtjevu 31, naznačen time, da je R3 odabran iz grupe koja sadrži
(1) cijano,
(2) nitro,
(3) halogen,
(4) hidroksi,
(5) amino, i
(6) trifluorometil.
34. Spoj prema Zahtjevu 31, naznačen time, da je R6 odabran iz grupe koja sadrži
(1) vodik,
(2) metil, i
(3) etil.
35. Spoj, naznačen time, da je odabran od:
N-(6-(2-aminopirimidin-5-il)-2-morfolinopirimidin-4-il)kinolin-3-amin;
[6-(6-amino-piridin-3-il)-2-morfolin-4-il-pirimidin-4-il]-(6-metoksi-piridin-3-il)-amin;
N-{3-[6-(6-amino-piridin-3-il)-2-morfolin-4-il-pirimidin-4-il]piridin-2-il}-metansulfonamid;
N-(6-(6-amino-4-fluoropiridin-3-il)-2-morfolinopirimidin-4-il)kinolin-3-amin;
2-amino-5-[2-morfolin-4-il-6-(kinolin-3-ilamino)-pirimidin-4-il]-izonikotinonitril;
N6-metil-2-morfolino- N6-(tetrahidro-2H-piran-4-il)-4,5'-bipirimidin-2',6-diamin;
N-(6-(2-aminopirimidin-5-il)-2-morfolinopirimidin-4-il)-5-metoksikinolin-3-amin;
5-(2-morfolino-6-(piridin-3-iloksi)pirimidin-4-il)pirimidin-2-amin;
6-(2-aminopirimidin-5-il)-2-morfolino-N-(6-piperazin-1-il)piridin-3-il)pirimidin-4-amin;
4-(trifluorometil)-5-(2,6-dimorfolinopirimidin-4-il)piridin-2-amin;
N-(6-(1-izopropilpiperidin-4-iloksi)piridin-3-il)-6-(6-amino-4-(trifluorometil)piridin-3-il)-2-morfolinopirimidin-4-amin;
N-(5-((dietilamino)metil)tiazol-2-il)-6-(6-amino-4-(trifluorometil)piridin-3-il)-2-morfolinopirimidin-4-amin;
6-(6-amino-4-(trifluorometil)piridin-3-il)-N-(4-(2-(dietilamino)etil)tiazol-2-il)-2-morfolinopirimidin-4-amin;
N6-(2-metoksietil)-2-morfolino-4,5'-bipirimidin-2',6-diamin;
2-morfolino-6-(2-fenilmorfolino)-4,5'-bipirimidin-2'-amin;
N6-tert-butil-2-morfolino-4,5'-bipirimidin-2',6-diamin;
1-(2-(6-amino-4-(trifluorometil)piridin-3-il)-6-morfolino-pirimidin-4-il)piperidin-2-on;
1-(6-(6-amino-4-(trifluorometil)piridin-3-il)-2-morfolinopirimidin-4-il)-3-fenilimidazolin-2-on;
1-(4-(6-amino-4-(trifluorometil)piridin-3-il)-2-morfolinopirimidin-4-iloksi)piperidin-1-il)etanon;
5-(6-((S)-piperidin-3-iloksi)-2-morfolinopirimidin-4-il)-4-(trifluorometil)piridin-2-amin;
5-(6-((R)-piperidin-3-iloksi)-2-morfolinopirimidin-4-il)-4-(trifluorometil)piridin-2-amin;
1-((R)-3-(6-(6-amino-4-(trifluorometil)piridin-3-il)-2-morfolinopirimidin-4-iloksi)pirolidin-1-il)etanon;
1-((S)-3-(6-(6-amino-4-(trifluorometil)piridin-3-il)-2-morfolinopirimidin-4-iloksi)pirolidin-1-il)etanon;
4-(trifluorometil)-5-(2-morfolino-6-(tetrahidro-2H-piran-4-iloksi)pirimidin-4-il)piridin-2-amin;
5-(6-((R)-tetrahidrofuran-3-iloksi)-2-morfolinopirimidin-4-il)-4-(trifluorometil)piridin-2-amin;
5-(6-((S)-tetrahidrofuran-3-iloksi)-2-morfolinopirimidin-4-il)-4-(trifluorometil)piridin-2-amin;
4-(trifluorometil)-5-(2-morfolino-6-(piperidin-4-iloksi)pirimidin-4-il)piridin-2-amin;
5-(2-morfolino-6-(piperidin-4-iloksi)pirimidin-4-il)pirimidin-2,4-diamin;
1-((R)-3-(6-(2,4-diaminopirimidin-5-il)-2-morfolinopirimidin-4-iloksi)piperidin-1-il)etanon;
2-amino-5-(2-morfolino-6-(N-acil-piperidin-4-iloksi)pirimidin-4-il)pirimidin-4(3H)-on;
2-amino-5-(2-morfolino-6-(N-metoksikarbonil-piperidin-4-iloksi)pirimidin-4-il)pirimidin-4(3H)-on;
6-[6-amino-4-(trifluorometil)piridin-3-il]-N-[4-(1-izopropilpiperidin-4-iloksi)fenil]-2-morfolinopirimidin-4-amin;
6-[6-amino-4-(trifluorometil)piridin-3-il]-N-[4-(1-izopropilpiperidin-4-iloksi)-3-metoksifenil]-2-morfolinopirimidin-4-amin;
N-(6-(6-amino-4-(trifluorometil)piridin-3-il)-2-morfolinopirimidin-4-il)-4-feniltiazol-2-amin;
N-(6-(6-amino-4-(trifluorometil)piridin-3-il)-5-metil-2-morfolinopirimidin-4-il)-4-feniltiazol-2-amin;
ili njegova farmaceutski prihvatljiva sol.
36. Spoj, naznačen time, da ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol.
37. Spoj, naznačen time, da ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol.
38. Spoj, naznačen time, da ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol.
39. Spoj, naznačen time, da je to
4-(trifluorometil)-5-(2,6-dimorfolinopirimidin-4-il)piridin-2-amin, ili njegova farmaceutski prihvatljiva sol.
40. Sastav, naznačen time, da se sastoji od farmaceutski prihvatljivog nosača i određene količine spoja prema bilo kojem od Zahtjeva 1 do 39, učinkovitog za inhibiranje aktivnosti PI3-K u ljudskom ili životinjskom subjektu kada se na njega primjenjuje.
41. Sastav prema Zahtjevu 40, naznačen time, da selektivno inhibira PI3-K alfa aktivnost kada se primjenjuje na ljudskom ili životinjskom subjektu.
42. Sastav prema Zahtjevu 40, naznačen time, da nadalje sadrži barem jedan dodatni agens za liječenje raka.
43. Sastav prema Zahtjevu 42, naznačen time, da barem jedan dodatni agens za liječenje raka je vatalanib, imatinib ili gefitinib.
44. Uporaba spoja prema bilo kojem od Zahtjeva 1 do 39, naznačena time, da se koristi za proizvodnju lijeka za inhibiranje PI3-K aktivnosti za liječenje raka kod ljudskog ili životinjskog subjekta.
45. Uporaba prema Zahtjevu 44, naznačena time, da se nadalje primjenjuje na ljudskom ili životinjskom subjektu davanjem barem jednog dodatnog agensa za liječenje raka.
46. Uporaba prema Zahtjevu 45, naznačena time, da barem jedan dodatni agens za liječenje raka je vatalanib, imatinib ili gefitinib.
47. Uporaba prema Zahtjevu 44, naznačena time, da rak je rak dojke, rak mjehura, rak crijeva, gliom, glioblastom, rak pluća, hepatocelularni rak, rak želudca, melanom, rak tiroidne žlijezde, endometrijski rak, rak bubrega, rak cerviksa, rak pankreasa, rak jednjaka, rak prostate, rak mozga, ili rak jajnika.
48. Spoj prema bilo kojem od Zahtjeva 1 do 39, naznačen time, da se koristi u liječenju raka.
49. Uporaba spoja prema bilo kojem od Zahtjeva 1 do 39, naznačena time, da se koristi u proizvodnji lijeka za liječenje raka.
50. Oprema, naznačena time, da sadrži spoj prema bilo kojem od Zahtjeva 1 do 39 i pakirni umetak ili drugo etiketiranje uključujući upute za liječenje celularne proliferativne bolesti davanjem PI3-K inhibirajuće količine spoja.
51. Uporaba prema Zahtjevu 44, naznačena time, da spoj ima vrijednost IC50 od manje od oko 1μM u odnosu na inhibiciju PI3-K.
52. Sastav, naznačen time, da sadrži farmaceutski prihvatljiv nosač i određenu količinu spoja prema bilo kojem od Zahtjeva 1 do 39 ili njegovu farmaceutski prihvatljivu sol.
53. Spoj prema bilo kojem od Zahtjeva 1 do 39 ili njegova farmaceutski prihvatljiva sol, naznačen time, da se koristi kao farmaceutsko sredstvo.
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Families Citing this family (333)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
AR060358A1 (es) | 2006-04-06 | 2008-06-11 | Novartis Vaccines & Diagnostic | Quinazolinas para la inhibicion de pdk 1 |
JP5534811B2 (ja) | 2006-08-24 | 2014-07-02 | アストラゼネカ アクチボラグ | 増殖性疾患の治療に有用なモルホリノピリミジン誘導体 |
NZ578162A (en) | 2006-12-07 | 2011-12-22 | Genentech Inc | Phosphoinositide 3-kinase inhibitor compounds and methods of use |
KR20090108124A (ko) * | 2007-02-06 | 2009-10-14 | 노파르티스 아게 | Pi 3-키나제 억제제 및 그의 사용 방법 |
JP5676249B2 (ja) * | 2007-04-20 | 2015-02-25 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体 |
JP5603770B2 (ja) | 2007-05-31 | 2014-10-08 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ccr2受容体拮抗薬およびその使用 |
AU2008273891B2 (en) | 2007-07-09 | 2012-01-12 | Astrazeneca Ab | Morpholino pyrimidine derivatives used in diseases linked to mTOR kinase and/or PI3K |
WO2009017838A2 (en) * | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
US20100311736A1 (en) * | 2007-10-22 | 2010-12-09 | Glaxosmithkline Llc | Pyridosulfonamide derivatives as p13 kinase inhibitors |
WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
WO2009093981A1 (en) * | 2008-01-23 | 2009-07-30 | S Bio Pte Ltd | Triazine compounds as kinase inhibitors |
AU2009221164B2 (en) * | 2008-03-05 | 2012-07-26 | Novartis Ag | Use of pyrimidine derivatives for the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members |
AU2012203914C1 (en) * | 2008-03-26 | 2013-11-28 | Novartis Ag | 5imidazoquinolines and pyrimidine derivatives as potent modulators of VEGF-driven angiogenic processes |
US20110020338A1 (en) * | 2008-03-26 | 2011-01-27 | Carlos Garcia-Echeverria | 5Imidazoquinolines and Pyrimidine Derivatives as Potent Modulators of VEGF-Driven Angiogenic Processes |
US20110053907A1 (en) * | 2008-03-27 | 2011-03-03 | Auckland Uniservices Limited | Substituted pyrimidines and triazines and their use in cancer therapy |
US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
MX353308B (es) | 2008-05-21 | 2018-01-08 | Ariad Pharma Inc | Derivados fosforosos como inhibidores de cinasa. |
WO2009157880A1 (en) * | 2008-06-27 | 2009-12-30 | S*Bio Pte Ltd | Pyrazine substituted purines |
MX336723B (es) * | 2008-07-11 | 2016-01-28 | Novartis Ag | Combinacion de (a) un inhibidor de fosfoinositido 3-cinasa y (b) un modulador de la ruta de ras/raf/mek. |
EP2323992B1 (en) * | 2008-07-29 | 2016-07-20 | Boehringer Ingelheim International GmbH | 5-alkynyl-pyrimidines |
WO2010030967A1 (en) * | 2008-09-12 | 2010-03-18 | Wyeth Llc | 4-aryloxyquinolin-2(1h)-ones as mtor kinase and pi3 kinase inhibitors, for use as anti-cancer agents |
EP2617414A3 (en) * | 2008-10-01 | 2013-11-06 | Novartis AG | Smoothened antagonism for the treatment of hedgehog pathway-related disorders |
TWI378933B (en) | 2008-10-14 | 2012-12-11 | Daiichi Sankyo Co Ltd | Morpholinopurine derivatives |
KR20110090911A (ko) * | 2008-10-31 | 2011-08-10 | 노파르티스 아게 | 포스파티딜이노시톨-3-키나아제 (pi3k) 억제제 및 mtor 억제제의 조합물 |
EP2356117B1 (en) * | 2008-11-20 | 2012-09-26 | Genentech, Inc. | Pyrazolopyridine pi3k inhibitor compounds and methods of use |
PE20120061A1 (es) | 2008-12-19 | 2012-02-19 | Boehringer Ingelheim Int | Derivados de pirimidina como antagonistas del receptor ccr2 |
SG172469A1 (en) | 2009-03-05 | 2011-08-29 | Daiichi Sankyo Co Ltd | Pyridine derivative |
WO2010110685A2 (en) | 2009-03-27 | 2010-09-30 | Pathway Therapeutics Limited | Pyrimddinyl and 1,3,5-triazinyl benzimtoazole sulfonamides and their use in cancer therapy |
KR20120018761A (ko) * | 2009-04-09 | 2012-03-05 | 온코타이레온, 인코포레이티드 | 섬유증을 치료하기 위한 방법 및 pi-3 키나제 억제제의 조성물 |
UY32582A (es) | 2009-04-28 | 2010-11-30 | Amgen Inc | Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero |
JP2012526772A (ja) * | 2009-05-15 | 2012-11-01 | ノバルティス アーゲー | ホスホイノシチド3−キナーゼ阻害剤および抗糖尿病性化合物の組合せ剤 |
EP2435438A1 (en) * | 2009-05-27 | 2012-04-04 | Genentech, Inc. | Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use |
EP2451802A1 (en) | 2009-07-07 | 2012-05-16 | Pathway Therapeutics, Inc. | Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy |
US20120065166A1 (en) * | 2009-08-12 | 2012-03-15 | Virginia Espina | Bone Modulators And Methods Therewith |
CN101993416B (zh) * | 2009-08-27 | 2013-09-11 | 中国科学院上海药物研究所 | 喹啉类化合物、其制备方法、包含该化合物的药物组合物及该化合物的用途 |
BR112012008385A2 (pt) * | 2009-09-09 | 2019-09-24 | Avila Therapeutics Inc | inibidores de p13 cinase e uso dos mesmos. |
ES2683311T3 (es) | 2009-10-16 | 2018-09-26 | Melinta Therapeutics, Inc. | Compuestos antimicrobianos y métodos para fabricar y usar los mismos |
EA023350B1 (ru) * | 2009-10-16 | 2016-05-31 | Мелинта Терапьютикс, Инк. | Противомикробные соединения, способы их получения и применение |
BR112012015873B1 (pt) | 2009-12-17 | 2021-06-01 | Centrexion Therapeutics Corporation | Antagonistas de receptores ccr2 |
GB201004200D0 (en) | 2010-03-15 | 2010-04-28 | Univ Basel | Spirocyclic compounds and their use as therapeutic agents and diagnostic probes |
EP2569295B1 (en) | 2010-05-12 | 2014-11-19 | Boehringer Ingelheim International GmbH | New ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments |
US8877745B2 (en) | 2010-05-12 | 2014-11-04 | Boehringer Ingelheim International Gmbh | CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments |
JP5647339B2 (ja) | 2010-05-17 | 2014-12-24 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ccr2アンタゴニスト及びこれらの使用 |
EP2576542B1 (en) | 2010-05-25 | 2015-04-22 | Boehringer Ingelheim International GmbH | Cyclic amide derivatives of pyridazine-3-carboxylic acids and their use in the treatment of pulmonary, pain, immune related and cardiovascular diseases |
US8962656B2 (en) | 2010-06-01 | 2015-02-24 | Boehringer Ingelheim International Gmbh | CCR2 antagonists |
SA111320519B1 (ar) | 2010-06-11 | 2014-07-02 | Astrazeneca Ab | مركبات بيريميدينيل للاستخدام كمثبطات atr |
CN103209955A (zh) | 2010-09-07 | 2013-07-17 | 第一三共株式会社 | 制备安息香酸酯的方法 |
ES2699951T3 (es) * | 2010-10-01 | 2019-02-13 | Novartis Ag | Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3 |
MX2013004086A (es) * | 2010-10-14 | 2013-07-05 | Ariad Pharma Inc | Metodos para inhibir proliferacion celular en cancers accionados por egfr. |
BR112013011728A2 (pt) | 2010-11-12 | 2016-08-16 | Univ Texas | terapia de combinação com dexametasona |
MX2013005041A (es) * | 2010-11-12 | 2013-06-03 | Bayer Ip Gmbh | Procedimiento para la preparacion de 2,2-difluoroetilamina partiendo de prop-2-en-1-amina. |
JP2014500308A (ja) * | 2010-12-21 | 2014-01-09 | ノバルティス アーゲー | Vps34阻害剤としてのビヘテロアリール化合物 |
RU2013141559A (ru) * | 2011-02-11 | 2015-03-20 | Дана-Фарбер Кэнсер Инститьют, Инк. | Способ ингибирования клеток опухоли гамартомы |
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 |
JP6042406B2 (ja) | 2011-03-28 | 2016-12-14 | メイ プハルマ,インコーポレーテッド | (α−置換アラルキルアミノ及びヘテロアリールアルキルアミノ)ピリミジニル及び1,3,5−トリアジニルベンズイミダゾール、それらを含む医薬組成物、並びに増殖性疾患の治療で使用するためのこれらの化合物 |
CA2832504C (en) | 2011-05-04 | 2019-10-01 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
KR20140040770A (ko) * | 2011-07-01 | 2014-04-03 | 노파르티스 아게 | 암 치료에 사용하기 위한 cdk4/6 억제제 및 pi3k 억제제를 포함하는 조합 요법 |
EP2731941B1 (en) | 2011-07-15 | 2019-05-08 | Boehringer Ingelheim International GmbH | Novel and selective ccr2 antagonists |
PL3409278T3 (pl) | 2011-07-21 | 2021-02-22 | Sumitomo Pharma Oncology, Inc. | Heterocykliczne inhibitory kinazy białkowej |
KR20140072028A (ko) | 2011-08-31 | 2014-06-12 | 노파르티스 아게 | Pi3k- 및 mek-억제제의 상승작용적 조합물 |
US20140213583A1 (en) * | 2011-09-01 | 2014-07-31 | Novartis Ag | PI3K Inhibitor for Use in the Treatment of Bone Cancer or for Preventing Metastatic Dissemination Primary Cancer Cells into the Bone |
CU24269B1 (es) | 2011-09-27 | 2017-08-08 | Novartis Ag | 3- pirimidin- 4-il- oxazolidin- 2- onas inhibidores de la idh mutante |
WO2013049581A1 (en) * | 2011-09-30 | 2013-04-04 | Beth Israel Deaconess Medical Center Inc. | Compositions and methods for the treatment of proliferative diseases |
BR112014009993A2 (pt) | 2011-10-28 | 2017-04-25 | Novartis Ag | método para o tratamento de tumores do estroma gastrointestinal |
RU2014124184A (ru) * | 2011-11-15 | 2015-12-27 | Новартис Аг | Комбинация ингибитора фосфоинозитид-3-киназы и модулятора пути янус-киназы 2 - проводника сигнала и активатора транскрипции 5 |
UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
DK3459942T3 (da) | 2012-04-24 | 2021-03-08 | Vertex Pharma | DNA-PK-hæmmere |
JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Egfr発動性がんの細胞増殖阻害用化合物 |
BR112014028420A2 (pt) * | 2012-05-16 | 2017-09-19 | Novartis Ag | regime de dosagem para um inibidor de quinase pi-3 |
EP2852661A1 (en) | 2012-05-23 | 2015-04-01 | F. Hoffmann-La Roche AG | Compositions and methods of obtaining and using endoderm and hepatocyte cells |
EP2858631A1 (en) | 2012-06-06 | 2015-04-15 | Novartis AG | Combination of a 17 -alpha -hydroxylase (c17, 20 - lyase) inhibitor and a specific pi-3k inhibitor for treating a tumor disease |
WO2013192367A1 (en) | 2012-06-22 | 2013-12-27 | Novartis Ag | Neuroendocrine tumor treatment |
EP2869818A1 (en) | 2012-07-06 | 2015-05-13 | Novartis AG | Combination of a phosphoinositide 3-kinase inhibitor and an inhibitor of the il-8/cxcr interaction |
WO2014016849A2 (en) | 2012-07-23 | 2014-01-30 | Sphaera Pharma Pvt. Ltd. | Novel triazine compounds |
EP2885003B1 (en) * | 2012-08-16 | 2021-09-29 | Novartis AG | Combination of pi3k inhibitor and c-met inhibitor |
CN102952086B (zh) * | 2012-09-28 | 2013-08-28 | 天津科创医药中间体技术生产力促进有限公司 | 一种2-吗啉基取代嘧啶类化合物的制备方法 |
WO2014062838A2 (en) | 2012-10-16 | 2014-04-24 | Tolero Pharmaceuticals, Inc. | Pkm2 modulators and methods for their use |
CA2885471C (en) * | 2012-10-23 | 2021-02-23 | Dietmar Flubacher | Improved process for manufacturing 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-trifluoromethylpyridin-2-amine |
US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
BR112015011147A8 (pt) | 2012-11-16 | 2019-10-01 | Merck Sharp & Dohme | composto, composição farmacêutica, e, uso do referido composto |
WO2014093230A2 (en) * | 2012-12-10 | 2014-06-19 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
EP3251673A1 (en) | 2012-12-13 | 2017-12-06 | IP Gesellschaft für Management mbH | Combination therapy comprising a cdk4/6 inhibitor and a pi3k inhibitor for use in the treatment of cancer |
CN104245693B (zh) * | 2012-12-14 | 2016-08-24 | 上海恒瑞医药有限公司 | 嘧啶类衍生物及其可药用盐、其制备方法及其在医药上的应用 |
WO2014130657A1 (en) | 2013-02-20 | 2014-08-28 | The Trustees Of The University Of Pennsylvania | Treatment of cancer using humanized anti-egfrviii chimeric antigen receptor |
GB201303109D0 (en) * | 2013-02-21 | 2013-04-10 | Domainex Ltd | Novel pyrimidine compounds |
PE20151607A1 (es) | 2013-03-06 | 2015-11-26 | Novartis Ag | Formulaciones de compuestos organicos |
EP3985003B1 (en) | 2013-03-12 | 2023-08-09 | Vertex Pharmaceuticals Incorporated | Dna-pk inhibitors |
US9498532B2 (en) | 2013-03-13 | 2016-11-22 | Novartis Ag | Antibody drug conjugates |
EA028033B1 (ru) | 2013-03-14 | 2017-09-29 | Новартис Аг | 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантного idh |
PL2970205T3 (pl) | 2013-03-14 | 2019-10-31 | Tolero Pharmaceuticals Inc | Inhibitory jak2 i alk2 oraz sposoby ich zastosowania |
US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
EP3514178A1 (en) | 2013-03-15 | 2019-07-24 | Novartis AG | Antibody drug conjugates |
PL2976106T3 (pl) * | 2013-03-21 | 2021-10-25 | Array Biopharma Inc. | Terapia kombinowana obejmująca inhibitor B-Raf i drugi inhibitor |
US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
MY182082A (en) * | 2013-05-01 | 2021-01-18 | Hoffmann La Roche | Biheteroaryl compounds and uses thereof |
CN105164114B (zh) * | 2013-05-01 | 2018-03-23 | 豪夫迈·罗氏有限公司 | C‑连接的杂环烷基取代的嘧啶类和它们的用途 |
PT2994126T (pt) | 2013-05-07 | 2018-10-22 | Novartis Ag | Combinação de um inibidor de pi3 quinase com paclitaxel para utilização no tratamento ou prevenção de um cancro da cabeça e do pescoço |
BR112015030664A2 (pt) | 2013-06-11 | 2017-07-25 | Novartis Ag | combinação farmacêutica de um inibidor de pi3k e um agente desestabilizador de microtúbulos |
KR20160020502A (ko) | 2013-06-18 | 2016-02-23 | 노파르티스 아게 | 제약 조합물 |
RU2016107813A (ru) | 2013-08-08 | 2017-09-14 | Новартис Аг | Комбинации ингибиторов киназы pim |
EP3033086B1 (en) | 2013-08-14 | 2021-09-22 | Novartis AG | Combination therapy for the treatment of cancer |
WO2015022657A1 (en) | 2013-08-16 | 2015-02-19 | Novartis Ag | Pharmaceutical combinations |
JP2016529325A (ja) | 2013-09-09 | 2016-09-23 | メリンタ セラピューティクス,インコーポレイテッド | 抗微生物化合物ならびにそれの製造方法および使用方法 |
EP3039025A4 (en) | 2013-09-09 | 2017-05-31 | Melinta Therapeutics, Inc. | Antimicrobial compounds and methods of making and using the same |
CN103483345B (zh) * | 2013-09-25 | 2016-07-06 | 中山大学 | Pi3k激酶抑制剂、包含其的药物组合物及其应用 |
US10570204B2 (en) | 2013-09-26 | 2020-02-25 | The Medical College Of Wisconsin, Inc. | Methods for treating hematologic cancers |
SI3424920T1 (sl) | 2013-10-17 | 2020-08-31 | Vertex Pharmaceuticals Incorporated | Kokristali (s)-n-metil-8-(1-((2'-metil-(4,5'-bipirimidin)-6-il)amino)propan-2-il) kinolin-4-karboksamida in devterirani derivati le-teh kot inhibitorji dna-pk |
CN105916515A (zh) | 2014-01-15 | 2016-08-31 | 诺华股份有限公司 | 药物组合 |
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 |
CN106661039B (zh) | 2014-02-28 | 2019-09-13 | 林伯士拉克许米公司 | 酪氨酸蛋白质激酶2(tyk2)抑制剂和其用途 |
AU2015229103C9 (en) | 2014-03-14 | 2020-11-26 | Immutep S.A.S | Antibody molecules to LAG-3 and uses thereof |
KR102472711B1 (ko) * | 2014-04-22 | 2022-12-01 | 우니페르시테트 바젤 | 트리아진, 피리미딘 및 피리딘 유도체의 신규한 제조방법 |
WO2016001789A1 (en) * | 2014-06-30 | 2016-01-07 | Pfizer Inc. | Pyrimidine derivatives as pi3k inhibitors for use in the treatment of cancer |
WO2016001341A1 (en) * | 2014-07-03 | 2016-01-07 | F. Hoffmann-La Roche Ag | Sulfonylaminopyridine compounds, compositions and methods of use |
US10786578B2 (en) | 2014-08-05 | 2020-09-29 | Novartis Ag | CKIT antibody drug conjugates |
JP6749890B2 (ja) | 2014-08-12 | 2020-09-02 | モナッシュ ユニバーシティ | リンパ指向プロドラッグ |
CA2954599A1 (en) | 2014-08-12 | 2016-02-18 | Novartis Ag | Anti-cdh6 antibody drug conjugates |
CN105330699B (zh) * | 2014-08-13 | 2018-12-04 | 山东汇睿迪生物技术有限公司 | 一种含磷吡啶并[2,3-d]嘧啶-7-酮类化合物或其药学上可接受的盐、药物组合物及其应用 |
CN104151256B (zh) * | 2014-08-14 | 2016-08-24 | 西安交通大学 | 二取代苯甲酰胺类化合物及其合成方法和应用 |
US11344620B2 (en) | 2014-09-13 | 2022-05-31 | Novartis Ag | Combination therapies |
CN105461714B (zh) * | 2014-09-29 | 2017-11-28 | 山东轩竹医药科技有限公司 | 并环类pi3k抑制剂 |
CN107106687A (zh) | 2014-10-03 | 2017-08-29 | 诺华股份有限公司 | 组合治疗 |
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 |
MA40035A (fr) | 2014-10-14 | 2016-04-21 | Dana Farber Cancer Inst Inc | Molécules d'anticorps de pd-l1 et leurs utilisations |
MA40933A (fr) | 2014-11-11 | 2017-09-19 | Piqur Therapeutics Ag | Difluorométhyl-aminopyridines et difluorométhyl-aminopyrimidines |
EA201791050A1 (ru) | 2014-11-14 | 2017-09-29 | Новартис Аг | Конъюгаты антител и лекарственных средств |
CN105085476B (zh) * | 2014-11-24 | 2018-03-09 | 苏州晶云药物科技有限公司 | 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺二盐酸盐的晶型及其制备方法 |
EP3229803B1 (en) * | 2014-12-12 | 2020-01-29 | Massachusetts General Hospital | Treatment of breast cancer brain metastases |
CA2971118C (en) * | 2014-12-17 | 2020-07-14 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | 2-morpholin-4,6-disubstituted pyrimidine derivative, and preparation method and pharmaceutical use thereof |
EP3233918A1 (en) | 2014-12-19 | 2017-10-25 | Novartis AG | Combination therapies |
EP3237418B1 (en) | 2014-12-23 | 2019-01-30 | Novartis AG | Triazolopyrimidine compounds and uses thereof |
CN105832741A (zh) * | 2015-01-16 | 2016-08-10 | 复旦大学 | Pi3k抑制剂与紫杉醇的药物组合物及其在制备抗肿瘤药物中的应用 |
TWI744225B (zh) | 2015-02-27 | 2021-11-01 | 美商林伯士拉克許米公司 | 酪胺酸蛋白質激酶2(tyk2)抑制劑及其用途 |
CN107530304A (zh) | 2015-02-27 | 2018-01-02 | 科泰纳制药公司 | Olig2活性的抑制 |
US10449211B2 (en) | 2015-03-10 | 2019-10-22 | Aduro Biotech, Inc. | Compositions and methods for activating “stimulator of interferon gene”—dependent signalling |
AU2016228584A1 (en) | 2015-03-11 | 2017-10-05 | Melinta Therapeutics, Inc. | Antimicrobial compounds and methods of making and using the same |
US9481665B2 (en) * | 2015-03-13 | 2016-11-01 | Yong Xu | Process for preparing PI3K inhibitor buparsilib |
US10130629B2 (en) | 2015-03-25 | 2018-11-20 | Novartis Ag | Pharmaceutical combinations |
CN107667092B (zh) | 2015-03-25 | 2021-05-28 | 诺华股份有限公司 | 作为fgfr4抑制剂的甲酰化n-杂环衍生物 |
EP3310813A1 (en) | 2015-06-17 | 2018-04-25 | Novartis AG | Antibody drug conjugates |
WO2017004134A1 (en) | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
JP6917910B2 (ja) | 2015-07-02 | 2021-08-11 | セントレクシオン セラピューティクス コーポレイション | (4−((3r,4r)−3−メトキシテトラヒドロ−ピラン−4−イルアミノ)ピペリジン−1−イル)(5−メチル−6−(((2r,6s)−6−(p−トリル)テトラヒドロ−2h−ピラン−2−イル)メチルアミノ)ピリミジン−4イル)メタノンクエン酸塩 |
WO2017009751A1 (en) | 2015-07-15 | 2017-01-19 | Pfizer Inc. | Pyrimidine derivatives |
EP3964528A1 (en) | 2015-07-29 | 2022-03-09 | Novartis AG | Combination therapies comprising antibody molecules to lag-3 |
US20180207273A1 (en) | 2015-07-29 | 2018-07-26 | Novartis Ag | Combination therapies comprising antibody molecules to tim-3 |
EP3328418A1 (en) | 2015-07-29 | 2018-06-06 | Novartis AG | Combination therapies comprising antibody molecules to pd-1 |
CA2992221C (en) | 2015-08-28 | 2023-06-27 | Novartis Ag | Mdm2 inhibitors and combinations thereof |
CN105001151B (zh) * | 2015-08-28 | 2017-07-14 | 苏州明锐医药科技有限公司 | 布帕尼西中间体及其制备方法 |
TWI707852B (zh) | 2015-09-02 | 2020-10-21 | 美商林伯士拉克許米公司 | Tyk2 抑制劑及其用途 |
CN114031658A (zh) | 2015-09-08 | 2022-02-11 | 莫纳什大学 | 定向淋巴的前药 |
US10683308B2 (en) | 2015-09-11 | 2020-06-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
EP3364958B1 (en) | 2015-10-23 | 2023-01-04 | Navitor Pharmaceuticals, Inc. | Modulators of sestrin-gator2 interaction and uses thereof |
MA44334A (fr) | 2015-10-29 | 2018-09-05 | Novartis Ag | Conjugués d'anticorps comprenant un agoniste du récepteur de type toll |
RU2018119085A (ru) | 2015-11-02 | 2019-12-04 | Новартис Аг | Схема введения ингибитора фосфатидилинозитол-3-киназы |
BR112018008867A8 (pt) | 2015-11-03 | 2019-02-26 | Janssen Biotech Inc | anticorpos que se ligam especificamente a pd-1 e seus usos |
US20180353515A1 (en) | 2015-12-03 | 2018-12-13 | Novartis Ag | Treatment of cancer with a pi3k inhibitor in a patient presselected for having a pik3ca mutation in the ctdna |
WO2017106352A1 (en) | 2015-12-14 | 2017-06-22 | Raze Therapeutics, Inc. | Caffeine inhibitors of mthfd2 and uses thereof |
CN106883185B (zh) * | 2015-12-15 | 2021-07-09 | 重庆博腾制药科技股份有限公司 | 一种4-氯-2-三氟甲基嘧啶的制备方法 |
AU2016369537B2 (en) | 2015-12-17 | 2024-03-14 | Novartis Ag | Antibody molecules to PD-1 and uses thereof |
LT3426243T (lt) | 2016-03-09 | 2021-08-10 | Raze Therapeutics, Inc. | 3-fosfogliceratdehidrogenazės inhibitoriai ir jų panaudojimas |
US11014882B2 (en) * | 2016-03-09 | 2021-05-25 | Raze Therapeutics, Inc. | 3-phosphoglycerate dehydrogenase inhibitors and uses thereof |
JP2019510785A (ja) | 2016-04-08 | 2019-04-18 | エックス4 ファーマシューティカルズ, インコーポレイテッド | 癌を処置する方法 |
EP3231799A1 (en) * | 2016-04-14 | 2017-10-18 | Universität Basel | 4-(azetidin-1-yl)pyrimidine derivatives with anti-mitotic and anti-proliferative activity |
EP3452479A1 (en) | 2016-05-06 | 2019-03-13 | Melinta Therapeutics, Inc. | Antimicrobials and methods of making and using same |
EP3458067B1 (en) * | 2016-05-18 | 2020-12-30 | PIQUR Therapeutics AG | Treatment of neurological disorders |
KR102483630B1 (ko) | 2016-05-18 | 2023-01-02 | 토르쿠르 아게 | 피부 병변의 치료 |
CN108430987B (zh) * | 2016-06-02 | 2021-06-18 | 上海海雁医药科技有限公司 | Pi3k抑制剂及其药学上可接受的盐和多晶型物及其应用 |
WO2017221092A1 (en) | 2016-06-20 | 2017-12-28 | Novartis Ag | Triazolopyridine compounds and uses thereof |
CN109790166A (zh) | 2016-06-20 | 2019-05-21 | 诺华股份有限公司 | 咪唑并吡啶化合物用于治疗癌症 |
CA3027246A1 (en) | 2016-06-20 | 2017-12-28 | Novartis Ag | Crystalline forms of triazolopyrimidine compound |
CA3027498A1 (en) | 2016-06-21 | 2017-12-28 | X4 Pharmaceuticals, Inc. | Cxcr4 inhibitors and uses thereof |
CN109641838A (zh) | 2016-06-21 | 2019-04-16 | X4 制药有限公司 | Cxcr4抑制剂及其用途 |
JP7084624B2 (ja) | 2016-06-21 | 2022-06-15 | エックス4 ファーマシューティカルズ, インコーポレイテッド | Cxcr4阻害剤およびその使用 |
WO2018009466A1 (en) | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
CN106905294A (zh) * | 2016-07-08 | 2017-06-30 | 苏州科睿思制药有限公司 | 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法 |
CN110036033B (zh) | 2016-09-27 | 2023-12-08 | 森罗治疗公司 | 嵌合吞噬受体分子 |
MX2019003317A (es) | 2016-09-27 | 2019-08-05 | Vertex Pharma | Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk). |
TWI763722B (zh) | 2016-10-14 | 2022-05-11 | 美商林伯士拉克許米公司 | Tyk2抑制劑及其用途 |
CA3040286A1 (en) | 2016-10-21 | 2018-04-26 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
WO2018089499A1 (en) | 2016-11-08 | 2018-05-17 | Navitor Pharmaceuticals, Inc. | PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF |
WO2018092064A1 (en) | 2016-11-18 | 2018-05-24 | Novartis Ag | Combinations of mdm2 inhibitors and bcl-xl inhibitors |
EP4035659A1 (en) | 2016-11-29 | 2022-08-03 | PureTech LYT, Inc. | Exosomes for delivery of therapeutic agents |
WO2018106636A1 (en) | 2016-12-05 | 2018-06-14 | Raze Therapeutics, Inc. | Shmt inhibitors and uses thereof |
CN110603261A (zh) | 2016-12-23 | 2019-12-20 | 拜斯科阿迪有限公司 | 具有新型键结构的肽衍生物 |
US10624968B2 (en) | 2017-01-06 | 2020-04-21 | Bicyclerd Limited | Compounds for treating cancer |
JOP20190187A1 (ar) | 2017-02-03 | 2019-08-01 | Novartis Ag | مترافقات عقار جسم مضاد لـ ccr7 |
WO2018163051A1 (en) | 2017-03-06 | 2018-09-13 | Novartis Ag | Methods of treatment of cancer with reduced ubb expression |
EP3592746B1 (en) | 2017-03-08 | 2024-01-24 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors, uses, and methods for production thereof |
EP3375778A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aryl-piperidine derivatives |
EP3375784A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aza-dihydro-acridone derivatives |
GB201705263D0 (en) * | 2017-03-31 | 2017-05-17 | Probiodrug Ag | Novel inhibitors |
WO2018185618A1 (en) | 2017-04-03 | 2018-10-11 | Novartis Ag | Anti-cdh6 antibody drug conjugates and anti-gitr antibody combinations and methods of treatment |
US11339144B2 (en) | 2017-04-10 | 2022-05-24 | Navitor Pharmaceuticals, Inc. | Heteroaryl Rheb inhibitors and uses thereof |
AU2018258355B2 (en) | 2017-04-26 | 2024-05-30 | Navitor Pharmaceuticals, Inc. | Modulators of sestrin-gator2 interaction and uses thereof |
EP3615550A1 (en) | 2017-04-27 | 2020-03-04 | BicycleTx Limited | Bicyclic peptide ligands and uses thereof |
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 |
CA3063976A1 (en) | 2017-05-23 | 2018-11-29 | Mei Pharma, Inc. | Combination therapy |
CN111107868A (zh) | 2017-05-24 | 2020-05-05 | 诺华股份有限公司 | 抗体细胞因子移植蛋白及使用方法 |
WO2018215937A1 (en) | 2017-05-24 | 2018-11-29 | Novartis Ag | Interleukin-7 antibody cytokine engrafted proteins and methods of use in the treatment of cancer |
BR112019024556A2 (pt) | 2017-05-24 | 2020-06-23 | Novartis Ag | Proteínas enxertadas com citocina de anticorpo e métodos para uso no tratamento de câncer |
JP7433910B2 (ja) | 2017-06-22 | 2024-02-20 | ノバルティス アーゲー | Cd73に対する抗体分子及びその使用 |
WO2018237173A1 (en) | 2017-06-22 | 2018-12-27 | Novartis Ag | ANTIBODY MOLECULES DIRECTED AGAINST CD73 AND CORRESPONDING USES |
EP3645549A1 (en) | 2017-06-26 | 2020-05-06 | BicycleRD Limited | Bicyclic peptide ligands with detectable moieties and uses thereof |
AU2018306444B2 (en) | 2017-07-28 | 2022-11-17 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
ES2926195T3 (es) | 2017-08-04 | 2022-10-24 | Bicycletx Ltd | Ligandos peptídicos bicíclicos específicos de CD137 |
EP3668550A1 (en) | 2017-08-14 | 2020-06-24 | Bicyclerd Limited | Bicyclic peptide ligand prr-a conjugates and uses thereof |
WO2019034866A1 (en) | 2017-08-14 | 2019-02-21 | Bicyclerd Limited | BICYCLIC PEPTIDE LIGANDS CONJUGATES AND USES THEREOF |
AU2018318129A1 (en) | 2017-08-14 | 2020-03-26 | Mei Pharma, Inc. | Combination therapy |
EP3668839B1 (en) * | 2017-08-17 | 2023-04-12 | Board of Regents, The University of Texas System | Heterocyclic inhibitors of atr kinase |
US11883497B2 (en) | 2017-08-29 | 2024-01-30 | Puretech Lyt, Inc. | Lymphatic system-directing lipid prodrugs |
WO2019046491A1 (en) | 2017-08-29 | 2019-03-07 | Ariya Therapeutics, Inc. | LIPIDIC PRODRUGS DIRECTING TO THE LYMPHATIC SYSTEM |
CN111373055B (zh) | 2017-09-08 | 2024-07-23 | 豪夫迈·罗氏有限公司 | 用于癌症的诊断和治疗方法 |
US11358948B2 (en) | 2017-09-22 | 2022-06-14 | Kymera Therapeutics, Inc. | CRBN ligands and uses thereof |
WO2019060742A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc | AGENTS FOR DEGRADING PROTEINS AND USES THEREOF |
JP7286658B2 (ja) | 2017-09-26 | 2023-06-05 | セロ・セラピューティクス・インコーポレイテッド | キメラエンガルフメント受容体分子および使用方法 |
CN109651341A (zh) * | 2017-10-11 | 2019-04-19 | 上海医药工业研究院 | 二吗啉氰基嘧(吡)啶类衍生物及作为抗肿瘤药物应用 |
EP3694511A1 (en) | 2017-10-13 | 2020-08-19 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Combination treatment of pancreatic cancer |
WO2019101871A1 (en) | 2017-11-23 | 2019-05-31 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | A new marker for predicting the sensitivity to pi3k inhibitors |
US11608345B1 (en) | 2017-12-19 | 2023-03-21 | Puretech Lyt, Inc. | Lipid prodrugs of rapamycin and its analogs and uses thereof |
GB201721265D0 (en) | 2017-12-19 | 2018-01-31 | Bicyclerd Ltd | Bicyclic peptide ligands specific for EphA2 |
EP3727362A4 (en) | 2017-12-19 | 2021-10-06 | PureTech LYT, Inc. | MYCOPHENOLIC ACID LIPID MEDICINAL PRODUCTS AND THEIR USES |
US11304954B2 (en) | 2017-12-19 | 2022-04-19 | Puretech Lyt, Inc. | Lipid prodrugs of mycophenolic acid and uses thereof |
TWI825046B (zh) | 2017-12-19 | 2023-12-11 | 英商拜西可泰克斯有限公司 | Epha2特用之雙環胜肽配位基 |
BR112020012635A2 (pt) | 2017-12-22 | 2020-12-01 | Ravenna Pharmaceuticals, Inc. | derivados de aminopiridina como inibidores de fosfatidilinositol fosfato quinase |
IL275522B2 (en) | 2017-12-22 | 2024-02-01 | Petra Pharma Corp | Amine derivatives of ARYL–BIPYRIDINE as phosphatidylinositol phosphate kinase inhibitors |
BR112020012997A2 (pt) | 2017-12-26 | 2020-12-01 | Kymera Therapeutics, Inc. | degradadores de irak e usos dos mesmos |
WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
WO2019140387A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
AU2019211485A1 (en) | 2018-01-29 | 2020-08-06 | Merck Patent Gmbh | GCN2 inhibitors and uses thereof |
CA3089769A1 (en) | 2018-01-29 | 2019-08-01 | Merck Patent Gmbh | Gcn2 inhibitors and uses thereof |
KR20200140262A (ko) | 2018-02-27 | 2020-12-15 | 아텍스 바이오파마 인코포레이티드 | Tcr-nck 상호 작용의 억제제로서의 크로멘 유도체 |
CN112218887A (zh) | 2018-03-28 | 2021-01-12 | 森罗治疗公司 | 细胞免疫疗法组合物及其用途 |
JP7549533B2 (ja) | 2018-03-28 | 2024-09-11 | セロ・セラピューティクス・インコーポレイテッド | キメラ貪食受容体のための発現ベクター、遺伝子改変宿主細胞およびそれらの使用 |
EP3774906A1 (en) | 2018-03-28 | 2021-02-17 | Cero Therapeutics, Inc. | Chimeric tim4 receptors and uses thereof |
WO2019195753A1 (en) | 2018-04-05 | 2019-10-10 | Tolero Pharmaceuticals, Inc. | Axl kinase inhibitors and use of the same |
BR112020019732A2 (pt) * | 2018-04-06 | 2021-02-17 | Nippon Soda Co., Ltd. | composto, formulações para controlar organismos nocivos e para controlar ou exterminar endoparasitas, e, formulações inseticida ou acaricida e nematicida. |
SG11202008851UA (en) | 2018-04-10 | 2020-10-29 | Neuropore Therapies Inc | Morpholine derivates as inhibitors of vps34 |
CA3094714A1 (en) | 2018-04-10 | 2019-10-17 | Neuropore Therapies, Inc. | Tri-substituted aryl and heteroaryl derivatives as modulators of pi3-kinase and autophagy pathways |
AR114828A1 (es) | 2018-04-24 | 2020-10-21 | Vertex Pharma | Compuestos de pteridinona y sus usos |
HUE058746T2 (hu) | 2018-04-24 | 2022-09-28 | Merck Patent Gmbh | Antiproliferációs vegyületek és felhasználásuk |
UY38247A (es) | 2018-05-30 | 2019-12-31 | Novartis Ag | Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación |
WO2019232244A2 (en) | 2018-05-31 | 2019-12-05 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
IL314362A (en) | 2018-06-15 | 2024-09-01 | Janssen Pharmaceutica Nv | Rapamycin analogs and their uses |
CN108864067B (zh) * | 2018-06-20 | 2020-05-12 | 郑州大学 | 一种2-炔丙巯基-5-氰基嘧啶类衍生物及其制备方法和应用 |
GB201810316D0 (en) | 2018-06-22 | 2018-08-08 | Bicyclerd Ltd | Peptide ligands for binding to EphA2 |
US11180531B2 (en) | 2018-06-22 | 2021-11-23 | Bicycletx Limited | Bicyclic peptide ligands specific for Nectin-4 |
EP3817748A4 (en) | 2018-07-06 | 2022-08-24 | Kymera Therapeutics, Inc. | TRICYCLIC CRBN LIGANDS AND USES THEREOF |
EP3826684A4 (en) | 2018-07-26 | 2022-04-06 | Sumitomo Dainippon Pharma Oncology, Inc. | METHODS FOR TREATING DISEASES ASSOCIATED WITH ABNORMAL ACVR1 EXPRESSION AND ACVR1 INHIBITORS FOR USE THEREOF |
KR20210047313A (ko) | 2018-08-17 | 2021-04-29 | 노파르티스 아게 | Smarca2/brm atp분해효소 저해제로서의 우레아 화합물 및 조성물 |
US10548889B1 (en) | 2018-08-31 | 2020-02-04 | X4 Pharmaceuticals, Inc. | Compositions of CXCR4 inhibitors and methods of preparation and use |
CN113164419A (zh) | 2018-09-07 | 2021-07-23 | 皮克医疗公司 | Eif4e抑制剂和其用途 |
EP3866789A4 (en) | 2018-10-15 | 2022-07-06 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND USES THEREOF |
CN112955459A (zh) | 2018-10-23 | 2021-06-11 | 拜斯科技术开发有限公司 | 双环肽配体和其用途 |
CN113164414A (zh) | 2018-10-24 | 2021-07-23 | 纳维托制药有限公司 | 多晶型化合物和其用途 |
EP3873532A1 (en) | 2018-10-31 | 2021-09-08 | Novartis AG | Dc-sign antibody drug conjugates |
JP7530360B2 (ja) | 2018-11-30 | 2024-08-07 | 武田薬品工業株式会社 | Tyk2阻害剤およびその使用 |
BR112021010484A2 (pt) | 2018-11-30 | 2021-08-24 | Kymera Therapeutics, Inc. | Degradadores de irak e usos dos mesmos |
EP3670659A1 (en) | 2018-12-20 | 2020-06-24 | Abivax | Biomarkers, and uses in treatment of viral infections, inflammations, or cancer |
WO2020130125A1 (ja) | 2018-12-21 | 2020-06-25 | 第一三共株式会社 | 抗体-薬物コンジュゲートとキナーゼ阻害剤の組み合わせ |
PE20211296A1 (es) | 2018-12-21 | 2021-07-20 | Novartis Ag | Anticuerpos anti-pmel17 y conjugados de los mismos |
CN109705033B (zh) * | 2019-01-22 | 2021-03-30 | 杭州壹瑞医药科技有限公司 | N-杂芳基磺酰胺类衍生物及制备和应用 |
CN109651297B (zh) * | 2019-01-22 | 2022-05-27 | 杭州壹瑞医药科技有限公司 | 一种n-苄基-n-芳基磺酰胺类衍生物及制备和应用 |
EP3914357A4 (en) | 2019-01-23 | 2022-10-12 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND THEIR USES |
CN113412262A (zh) | 2019-02-12 | 2021-09-17 | 大日本住友制药肿瘤公司 | 包含杂环蛋白激酶抑制剂的制剂 |
WO2020165600A1 (en) | 2019-02-14 | 2020-08-20 | Bicycletx Limited | Bicyclic peptide ligand sting conjugates and uses thereof |
WO2020198077A1 (en) | 2019-03-22 | 2020-10-01 | Sumitomo Dainippon Pharma Oncology, Inc. | Compositions comprising pkm2 modulators and methods of treatment using the same |
US20220184222A1 (en) | 2019-04-02 | 2022-06-16 | Bicycletx Limited | Bicycle toxin conjugates and uses thereof |
AU2020253633A1 (en) | 2019-04-05 | 2021-11-04 | Kymera Therapeutics, Inc. | STAT degraders and uses thereof |
CN114502540A (zh) | 2019-05-31 | 2022-05-13 | 医肯纳肿瘤学公司 | Tead抑制剂和其用途 |
TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
EP3993786A1 (en) | 2019-07-02 | 2022-05-11 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the prophylactic treatment of cancer in patients suffering from pancreatitis |
WO2021001431A1 (en) | 2019-07-02 | 2021-01-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of pi3ka-selective inhibitors for treating metastatic disease in patients suffering from pancreatic cancer |
WO2021001426A1 (en) | 2019-07-02 | 2021-01-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of ultrafast elasticity imaging for detecting pancreatic cancers |
AU2020300619A1 (en) | 2019-07-03 | 2022-01-27 | Sumitomo Pharma Oncology, Inc. | Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof |
TW202110485A (zh) | 2019-07-30 | 2021-03-16 | 英商拜西可泰克斯有限公司 | 異質雙環肽複合物 |
AU2020345962A1 (en) | 2019-09-11 | 2022-03-31 | Vincere Biosciences, Inc. | USP30 inhibitors and uses thereof |
AU2020347274A1 (en) | 2019-09-13 | 2022-03-31 | Nimbus Saturn, Inc. | HPK1 antagonists and uses thereof |
JP2022548881A (ja) | 2019-09-18 | 2022-11-22 | ノバルティス アーゲー | Entpd2抗体、組合せ療法並びに抗体及び組合せ療法を使用する方法 |
US20220280509A1 (en) | 2019-09-26 | 2022-09-08 | Novartis Ag | Aza-quinoline compounds and uses thereof |
US20240058446A1 (en) | 2019-10-03 | 2024-02-22 | Cero Therapeutics, Inc. | Chimeric tim4 receptors and uses thereof |
IL292612A (en) | 2019-11-01 | 2022-07-01 | Navitor Pharm Inc | Treatment methods using mtorc1 modulator |
EP4069223A4 (en) | 2019-12-05 | 2023-12-20 | Janssen Pharmaceutica NV | RAPAMYCIN ANALOGS AND THEIR USES |
MX2022007576A (es) | 2019-12-17 | 2022-09-23 | Kymera Therapeutics Inc | Degradadores de cinasas asociadas al receptor de interleucina-1 (irak) y usos de los mismos. |
US11591332B2 (en) | 2019-12-17 | 2023-02-28 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
CA3162502A1 (en) | 2019-12-23 | 2021-07-01 | Yi Zhang | Smarca degraders and uses thereof |
AU2021217172A1 (en) | 2020-02-05 | 2022-09-22 | Monash University | Lipid prodrugs of neurosteroids |
CN115151534B (zh) * | 2020-02-14 | 2024-02-06 | 南京药石科技股份有限公司 | 白细胞介素-1受体相关激酶(irak)/fms样受体酪氨酸激酶(flt3)的抑制剂、其药物产品及其方法 |
CN115515685A (zh) | 2020-03-03 | 2022-12-23 | 皮克医疗公司 | Eif4e抑制剂及其用途 |
KR20230005160A (ko) | 2020-03-19 | 2023-01-09 | 카이메라 쎄라퓨틱스 인코포레이티드 | Mdm2 분해제 및 이의 용도 |
KR20230005844A (ko) * | 2020-03-27 | 2023-01-10 | 동아에스티 주식회사 | 아미노피리미딘 유도체 및 이의 아릴 탄화수소 수용체 조절제로서의 용도 |
US20230181756A1 (en) | 2020-04-30 | 2023-06-15 | Novartis Ag | Ccr7 antibody drug conjugates for treating cancer |
TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
KR20210158019A (ko) | 2020-06-23 | 2021-12-30 | 주식회사 온코빅스 | 포스파티딜이노시톨 3-키나제(pi3k) 억제제로써 pten 과오종 증후군에 의한 종양 세포의 성장 또는 증식을 억제하는데 유용한 신규한 피리미딘 유도체 및 이의 약제학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 약제학적 조성물 |
AR123185A1 (es) | 2020-08-10 | 2022-11-09 | Novartis Ag | Compuestos y composiciones para inhibir ezh2 |
WO2022036285A1 (en) | 2020-08-14 | 2022-02-17 | Cero Therapeutics, Inc. | Compositions and methods for treating cancer with chimeric tim receptors in combination with inhibitors of poly (adp-ribose) polymerase |
WO2022036265A1 (en) | 2020-08-14 | 2022-02-17 | Cero Therapeutics, Inc. | Chimeric tim receptors and uses thereof |
WO2022036287A1 (en) | 2020-08-14 | 2022-02-17 | Cero Therapeutics, Inc. | Anti-cd72 chimeric receptors and uses thereof |
MX2023001588A (es) | 2020-08-17 | 2023-05-03 | Bicycletx Ltd | Conjugados biciclo específicos para nectina-4 y usos de estos. |
WO2022043556A1 (en) | 2020-08-31 | 2022-03-03 | Novartis Ag | Stable radiopharmaceutical composition |
WO2022043557A1 (en) | 2020-08-31 | 2022-03-03 | Advanced Accelerator Applications International Sa | Method of treating psma-expressing cancers |
US20230338587A1 (en) | 2020-08-31 | 2023-10-26 | Advanced Accelerator Applications International Sa | Method of treating psma-expressing cancers |
TW202227089A (zh) | 2020-11-30 | 2022-07-16 | 大陸商杭州阿諾生物醫藥科技有限公司 | 用於治療pik3ca突變癌症的組合療法 |
WO2022120353A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
EP4255895A1 (en) | 2020-12-02 | 2023-10-11 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
TW202237119A (zh) | 2020-12-10 | 2022-10-01 | 美商住友製藥腫瘤公司 | Alk﹘5抑制劑和彼之用途 |
US20230113202A1 (en) | 2021-02-02 | 2023-04-13 | Liminal Biosciences Limited | Gpr84 antagonists and uses thereof |
MX2023009059A (es) | 2021-02-02 | 2023-09-15 | Liminal Biosciences Ltd | Antagonistas de gpr84 y usos de estos. |
CA3207380A1 (en) | 2021-02-15 | 2022-08-18 | Haojing RONG | Irak4 degraders and uses thereof |
BR112023017213A2 (pt) | 2021-02-26 | 2023-11-21 | Kelonia Therapeutics Inc | Vetores lentivirais direcionados a linfócitos |
US11926625B2 (en) | 2021-03-05 | 2024-03-12 | Nimbus Saturn, Inc. | HPK1 antagonists and uses thereof |
EP4310081A1 (en) * | 2021-03-18 | 2024-01-24 | Suzhou Guokuang Pharmtech. Co., Ltd. | Ctla-4 small molecule degradation agent and application thereof |
US12071442B2 (en) | 2021-03-29 | 2024-08-27 | Nimbus Saturn, Inc. | Substituted pyrrolo[3,4-c]pyridines as HPK1 antagonists |
MX2023012060A (es) | 2021-04-13 | 2024-01-22 | Nuvalent Inc | Heterociclos con sustitucion amino para tratar canceres con mutaciones de egfr. |
KR20230170738A (ko) | 2021-04-16 | 2023-12-19 | 노파르티스 아게 | 항체 약물 접합체 및 이의 제조 방법 |
WO2022221866A1 (en) | 2021-04-16 | 2022-10-20 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
WO2023010097A1 (en) | 2021-07-28 | 2023-02-02 | Cero Therapeutics, Inc. | Chimeric tim4 receptors and uses thereof |
US20230150997A1 (en) | 2021-08-25 | 2023-05-18 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
WO2023028238A1 (en) | 2021-08-25 | 2023-03-02 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
AU2022407039A1 (en) * | 2021-12-08 | 2024-07-25 | Kineta, Inc. | Pyrimidines and methods of their use |
WO2023114984A1 (en) | 2021-12-17 | 2023-06-22 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
US12091411B2 (en) | 2022-01-31 | 2024-09-17 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
CN114213340B (zh) | 2022-02-22 | 2022-06-07 | 北京蓝晶微生物科技有限公司 | 2,4-二氨基嘧啶氧化物的制备方法 |
CN114591326B (zh) * | 2022-02-28 | 2024-02-27 | 上海筛杰生物医药有限公司 | Cct-251921的中间体及其制备方法 |
WO2023173057A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
WO2023173053A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
WO2023211889A1 (en) | 2022-04-25 | 2023-11-02 | Ikena Oncology, Inc. | Polymorphic compounds and uses thereof |
TW202404581A (zh) | 2022-05-25 | 2024-02-01 | 美商醫肯納腫瘤學公司 | Mek抑制劑及其用途 |
TW202416972A (zh) | 2022-08-02 | 2024-05-01 | 英商利米那生物科技有限公司 | 經取代之吡啶酮gpr84拮抗劑及其用途 |
TW202416950A (zh) | 2022-08-02 | 2024-05-01 | 英商利米那生物科技有限公司 | 雜芳基甲醯胺及相關gpr84拮抗劑及其用途 |
WO2024028364A1 (en) | 2022-08-02 | 2024-02-08 | Liminal Biosciences Limited | Aryl-triazolyl and related gpr84 antagonists and uses thereof |
WO2024112894A1 (en) | 2022-11-22 | 2024-05-30 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
Family Cites Families (121)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB581334A (en) | 1943-09-29 | 1946-10-09 | Francis Henry Swinden Curd | New pyrimidine compounds |
AT340933B (de) * | 1973-08-20 | 1978-01-10 | Thomae Gmbh Dr K | Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze |
DE2341925A1 (de) | 1973-08-20 | 1975-03-06 | Thomae Gmbh Dr K | Neue pyrimidinderivate und verfahren zu ihrer herstellung |
JPS6041077B2 (ja) | 1976-09-06 | 1985-09-13 | 喜徳 喜谷 | 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体 |
US4323581A (en) | 1978-07-31 | 1982-04-06 | Johnson & Johnson | Method of treating carcinogenesis |
US4329726A (en) * | 1978-12-01 | 1982-05-11 | Raychem Corporation | Circuit protection devices comprising PTC elements |
IL73534A (en) | 1983-11-18 | 1990-12-23 | Riker Laboratories Inc | 1h-imidazo(4,5-c)quinoline-4-amines,their preparation and pharmaceutical compositions containing certain such compounds |
WO1988007045A1 (en) | 1987-03-09 | 1988-09-22 | Kyowa Hakko Kogyo Co., Ltd. | Derivatives of physiologically active substance k-252 |
US4994386A (en) | 1987-07-13 | 1991-02-19 | Pharmacia Diagnostics, Inc. | Production of HBLV virus in the HSB-2 cell line |
US4904768A (en) | 1987-08-04 | 1990-02-27 | Bristol-Myers Company | Epipodophyllotoxin glucoside 4'-phosphate derivatives |
WO1989007105A1 (en) | 1988-02-04 | 1989-08-10 | Kyowa Hakko Kogyo Co., Ltd. | Staurosporin derivatives |
US4929726A (en) | 1988-02-09 | 1990-05-29 | Georgia State University Foundation, Inc. | Novel diazines and their method of preparation |
US5238944A (en) | 1988-12-15 | 1993-08-24 | Riker Laboratories, Inc. | Topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine |
US4929624A (en) | 1989-03-23 | 1990-05-29 | Minnesota Mining And Manufacturing Company | Olefinic 1H-imidazo(4,5-c)quinolin-4-amines |
GB9012311D0 (en) | 1990-06-01 | 1990-07-18 | Wellcome Found | Pharmacologically active cns compounds |
US5389640A (en) | 1991-03-01 | 1995-02-14 | Minnesota Mining And Manufacturing Company | 1-substituted, 2-substituted 1H-imidazo[4,5-c]quinolin-4-amines |
US6410010B1 (en) | 1992-10-13 | 2002-06-25 | Board Of Regents, The University Of Texas System | Recombinant P53 adenovirus compositions |
US5451700A (en) | 1991-06-11 | 1995-09-19 | Ciba-Geigy Corporation | Amidino compounds, their manufacture and methods of treatment |
US5268376A (en) | 1991-09-04 | 1993-12-07 | Minnesota Mining And Manufacturing Company | 1-substituted 1H-imidazo[4,5-c]quinolin-4-amines |
WO1993007153A1 (en) | 1991-10-10 | 1993-04-15 | Schering Corporation | 4'-(n-substituted-n-oxide)staurosporine derivatives |
US5266575A (en) | 1991-11-06 | 1993-11-30 | Minnesota Mining And Manufacturing Company | 2-ethyl 1H-imidazo[4,5-ciquinolin-4-amines |
WO1993008809A1 (en) | 1991-11-08 | 1993-05-13 | The University Of Southern California | Compositions containing k-252 compounds for potentiation of neurotrophin activity |
GB9300059D0 (en) | 1992-01-20 | 1993-03-03 | Zeneca Ltd | Quinazoline derivatives |
US5948898A (en) | 1992-03-16 | 1999-09-07 | Isis Pharmaceuticals, Inc. | Methoxyethoxy oligonucleotides for modulation of protein kinase C expression |
US5756494A (en) | 1992-07-24 | 1998-05-26 | Cephalon, Inc. | Protein kinase inhibitors for treatment of neurological disorders |
US5621100A (en) | 1992-07-24 | 1997-04-15 | Cephalon, Inc. | K-252a derivatives for treatment of neurological disorders |
AU668772B2 (en) | 1992-08-31 | 1996-05-16 | Ludwig Institute For Cancer Research | Isolated nonapeptide derived from mage-3 gene and presented by HLA-A1, and uses thereof |
CA2123895A1 (en) | 1992-09-21 | 1994-03-31 | Tatsuya Tamaoki | A therapeutic agent for thrombocytopenia |
HU225646B1 (en) | 1992-10-28 | 2007-05-29 | Genentech Inc | Hvegf receptors as vascular endothelial cell growth factor antagonists |
US5395937A (en) | 1993-01-29 | 1995-03-07 | Minnesota Mining And Manufacturing Company | Process for preparing quinoline amines |
EP0708772B1 (en) | 1993-07-15 | 2000-08-23 | Minnesota Mining And Manufacturing Company | IMIDAZO [4,5-c]PYRIDIN-4-AMINES |
US5352784A (en) | 1993-07-15 | 1994-10-04 | Minnesota Mining And Manufacturing Company | Fused cycloalkylimidazopyridines |
US5478932A (en) | 1993-12-02 | 1995-12-26 | The Board Of Trustees Of The University Of Illinois | Ecteinascidins |
DK0817627T3 (da) | 1993-12-23 | 2005-06-06 | Lilly Co Eli | Inhibitorer af proteinkinase C |
US5587459A (en) | 1994-08-19 | 1996-12-24 | Regents Of The University Of Minnesota | Immunoconjugates comprising tyrosine kinase inhibitors |
US6083903A (en) | 1994-10-28 | 2000-07-04 | Leukosite, Inc. | Boronic ester and acid compounds, synthesis and uses |
US5482936A (en) | 1995-01-12 | 1996-01-09 | Minnesota Mining And Manufacturing Company | Imidazo[4,5-C]quinoline amines |
ES2332984T3 (es) | 1995-03-30 | 2010-02-16 | Pfizer Products Inc. | Derivados de quinazolinas. |
CA2190973C (en) * | 1995-04-13 | 2001-06-19 | Yasuo Konno | Novel 4,6-diarylpyrimidine derivatives and salts thereof |
GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
US6331555B1 (en) | 1995-06-01 | 2001-12-18 | University Of California | Treatment of platelet derived growth factor related disorders such as cancers |
US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
WO1997007081A2 (en) | 1995-08-11 | 1997-02-27 | Yale University | Glycosylated indolocarbazole synthesis |
FR2741881B1 (fr) | 1995-12-01 | 1999-07-30 | Centre Nat Rech Scient | Nouveaux derives de purine possedant notamment des prorietes anti-proliferatives et leurs applications biologiques |
EP1162201B1 (en) | 1995-12-08 | 2006-03-29 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibiting (imidazol-5-yl)methyl-2-quinolinone derivatives |
KR100447918B1 (ko) | 1996-07-25 | 2005-09-28 | 동아제약주식회사 | 대장을포함한위장관보호작용을갖는플라본및플라바논화합물 |
CA2262776C (en) | 1996-08-02 | 2005-03-08 | Jim A. Wright | Antitumor antisense sequences directed against r1 and r2 components of ribonucleotide reductase |
JP3734907B2 (ja) * | 1996-12-19 | 2006-01-11 | 富士写真フイルム株式会社 | 現像処理方法 |
CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
US6126965A (en) | 1997-03-21 | 2000-10-03 | Georgetown University School Of Medicine | Liposomes containing oligonucleotides |
CA2294244A1 (en) | 1997-07-12 | 1999-01-21 | Cancer Research Campaign Technology Limited | Cyclin dependent kinase inhibiting purine derivatives |
ES2213286T3 (es) * | 1997-07-24 | 2004-08-16 | Zenyaku Kogyo Kabushiki Kaisha | Compuestos heterociclicos y agente antitumoral que los contiene como ingredientes activos. |
US6166037A (en) | 1997-08-28 | 2000-12-26 | Merck & Co., Inc. | Pyrrolidine and piperidine modulators of chemokine receptor activity |
US6150362A (en) * | 1997-12-12 | 2000-11-21 | Henkin; Jack | Triazine angiogenesis inhibitors |
RS49779B (sr) | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
ES2193607T3 (es) * | 1998-01-16 | 2003-11-01 | Hoffmann La Roche | Derivados de benzosulfona . |
CO5031249A1 (es) | 1998-05-29 | 2001-04-27 | Sugen Inc | Pirrol substituido-2-indolinonas inhibidoras de proteinci-nasas |
WO1999065897A1 (en) | 1998-06-19 | 1999-12-23 | Chiron Corporation | Inhibitors of glycogen synthase kinase 3 |
US7045519B2 (en) | 1998-06-19 | 2006-05-16 | Chiron Corporation | Inhibitors of glycogen synthase kinase 3 |
US20030083242A1 (en) | 1998-11-06 | 2003-05-01 | Alphonse Galdes | Methods and compositions for treating or preventing peripheral neuropathies |
US6495558B1 (en) * | 1999-01-22 | 2002-12-17 | Amgen Inc. | Kinase inhibitors |
EP1144390A2 (en) | 1999-01-22 | 2001-10-17 | Amgen Inc., | Kinase inhibitors |
GB9913083D0 (en) | 1999-06-04 | 1999-08-04 | Novartis Ag | Organic compounds |
PL203116B1 (pl) | 1999-05-04 | 2009-08-31 | Schering Corp | Piperazynopiperydynowa pochodna użyteczna jako antagonista CCR5, zawierająca ją kompozycja farmaceutyczna i jej zastosowanie |
PL203117B1 (pl) | 1999-05-04 | 2009-08-31 | Schering Corp | Piperydynopiperydynowa pochodna użyteczna jako antagonista CCR5, zawierająca ją kompozycja farmaceutyczna i jej zastosowanie |
BRPI0012198B8 (pt) | 1999-06-25 | 2021-05-25 | Genentech Inc | anticorpos humanizados, composição e imunoconjugado |
EP1194152A4 (en) | 1999-06-30 | 2002-11-06 | Merck & Co Inc | SIN KINASE INHIBITOR COMPOUNDS |
EP1206260A4 (en) | 1999-06-30 | 2002-10-30 | Merck & Co Inc | SRC-KINASE INHIBITING COMPOUNDS |
CA2383546A1 (en) | 1999-06-30 | 2001-01-04 | William H. Parsons | Src kinase inhibitor compounds |
AU6014900A (en) | 1999-07-13 | 2001-01-30 | Kyowa Hakko Kogyo Co. Ltd. | Staurosporin derivatives |
JP2003505384A (ja) | 1999-07-15 | 2003-02-12 | ファーマコピーア,インコーポレーティッド | ブラジキニンb1受容体アンタゴニスト |
ES2265998T3 (es) | 1999-11-05 | 2007-03-01 | Astrazeneca Ab | Derivados de quizazolina como inhibidores de vegf. |
EA005996B1 (ru) | 2000-02-15 | 2005-08-25 | Сьюджен, Инк. | Пирролзамещенный 2-индолинон, фармацевтическая композиция (варианты), способ модулирования каталитической активности протеинкиназы, способ лечения или профилактики нарушения в организме, связанного с протеинкиназой |
NZ521068A (en) | 2000-03-29 | 2005-04-29 | Cyclacel Ltd | 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of proliferative disorders |
CA2406847C (en) | 2000-04-12 | 2009-11-17 | Genaera Corporation | Regioselective and stereoselective oxidation of fused ring systems useful for the preparation of aminosterols |
AU5261001A (en) | 2000-04-27 | 2001-11-12 | Imperial Cancer Research Technology Ltd | Condensed heteroaryl derivatives |
NZ522217A (en) | 2000-04-28 | 2004-04-30 | Tanabe Seiyaku Co | Cyclic compounds |
WO2002000647A1 (en) * | 2000-06-23 | 2002-01-03 | Bristol-Myers Squibb Pharma Company | Heteroaryl-phenyl substituted factor xa inhibitors |
DE60126611T2 (de) | 2000-06-30 | 2007-11-22 | Glaxo Group Ltd., Greenford | Ditosylatsalze von chinazolinverbindungen |
KR100816769B1 (ko) | 2000-09-06 | 2008-03-26 | 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 | 글리코겐 합성효소 키나아제 3의 억제제 |
SG129306A1 (en) | 2000-09-11 | 2007-02-26 | Chiron Corp | Quinolinone derivatives as tyrosine kinase inhibitors |
ATE326458T1 (de) | 2000-09-15 | 2006-06-15 | Vertex Pharma | Pyrazolverbindungen als protein-kinasehemmer |
US6677450B2 (en) | 2000-10-06 | 2004-01-13 | Bristol-Myers Squibb Company | Topoisomerase inhibitors |
SE0004053D0 (sv) | 2000-11-06 | 2000-11-06 | Astrazeneca Ab | N-type calcium channel antagonists for the treatment of pain |
DK1353916T3 (da) | 2000-12-21 | 2007-01-29 | Vertex Pharma | Pyrazolforbindelser der er egnede som proteinkinaseinhibitorer |
JP4323167B2 (ja) | 2001-01-16 | 2009-09-02 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | 分泌タンパク質を発現する細胞の単離 |
WO2002062766A2 (en) | 2001-02-07 | 2002-08-15 | Millennium Pharmaceuticals, Inc. | Melanocortin-4 receptor binding compounds and methods of use thereof |
WO2002062826A1 (fr) | 2001-02-07 | 2002-08-15 | Vadim Viktorovich Novikov | Procede de fabrication des peptides |
EP1395561A1 (en) * | 2001-05-25 | 2004-03-10 | Boehringer Ingelheim Pharmaceuticals Inc. | Carbamate and oxamide compounds as inhibitors of cytokine production |
WO2002102313A2 (en) | 2001-06-19 | 2002-12-27 | Bristol-Myers Squibb Company | Pyrimidine inhibitors of phosphodiesterase (pde) 7 |
US20040186172A1 (en) | 2001-07-02 | 2004-09-23 | Houssam Ibrahim | Oxaliplatin active substance with a very low content of oxalic acid |
US6603000B2 (en) * | 2001-07-11 | 2003-08-05 | Boehringer Ingelheim Pharmaceuticals, Inc. | Synthesis for heteroarylamine compounds |
KR100484504B1 (ko) | 2001-09-18 | 2005-04-20 | 학교법인 포항공과대학교 | 쿠커비투릴 유도체를 주인 분자로서 포함하고 있는 내포화합물 및 이를 포함한 약제학적 조성물 |
WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
US20030134846A1 (en) | 2001-10-09 | 2003-07-17 | Schering Corporation | Treatment of trypanosoma brucei with farnesyl protein transferase inhibitors |
AU2002316231A1 (en) | 2002-02-19 | 2003-09-29 | Xenoport, Inc. | Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof |
EP1485100B1 (en) * | 2002-03-15 | 2010-05-05 | Vertex Pharmaceuticals Incorporated | Azinylaminoazoles as inhibitors of protein kinases |
ATE433973T1 (de) * | 2002-03-15 | 2009-07-15 | Vertex Pharma | Azolylaminoazine als inhibitoren von proteinkinasen |
AU2003220300A1 (en) * | 2002-03-15 | 2003-09-29 | Binch, Hayley | Compositions useful as inhibitors of protein kinases |
US20040009981A1 (en) * | 2002-03-15 | 2004-01-15 | David Bebbington | Compositions useful as inhibitors of protein kinases |
AU2003226211B2 (en) | 2002-03-29 | 2008-05-29 | Novartis Vaccines And Diagnostics, Inc. | Substituted benzazoles and use thereof as RAF kinase inhibitors |
US6900342B2 (en) | 2002-05-10 | 2005-05-31 | Dabur India Limited | Anticancer taxanes such as paclitaxel, docetaxel and their structural analogs, and a method for the preparation thereof |
US6727272B1 (en) | 2002-07-15 | 2004-04-27 | Unitech Pharmaceuticals, Inc. | Leflunomide analogs for treating rheumatoid arthritis |
US7148342B2 (en) | 2002-07-24 | 2006-12-12 | The Trustees Of The University Of Pennyslvania | Compositions and methods for sirna inhibition of angiogenesis |
EP1562605A4 (en) | 2002-10-08 | 2006-07-12 | Massachusetts Inst Technology | COMPOUNDS FOR MODULATING CHOLESTER INTRANSPORT |
PL377821A1 (pl) * | 2002-11-21 | 2006-02-20 | Chiron Corporation | 2,4,6-tripodstawione pirymidyny jako inhibitory kinazy fosfatydyloinozytolu (PI) 3 i ich zastosowanie w leczeniu nowotworu |
WO2004060308A2 (en) | 2002-12-27 | 2004-07-22 | Chiron Corporation | Thiosemicarbazones as anti-virals and immunopotentiators |
ES2391770T3 (es) | 2003-01-21 | 2012-11-29 | Novartis Vaccines And Diagnostics, Inc. | Uso de compuestos de triptantrina para la potenciación inmune |
WO2004084824A2 (en) | 2003-03-24 | 2004-10-07 | Merck & Co., Inc. | Biaryl substituted 6-membered heterocyles as sodium channel blockers |
EP1608369B1 (en) | 2003-03-28 | 2013-06-26 | Novartis Vaccines and Diagnostics, Inc. | Use of organic compounds for immunopotentiation |
US20050014753A1 (en) * | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
WO2005009977A1 (en) | 2003-07-15 | 2005-02-03 | Neurogen Corporation | Substituted pyrimidin-4-ylamina analogues as vanilloid receptor ligands |
CA2531619A1 (en) | 2003-07-16 | 2005-01-27 | Neurogen Corporation | Biaryl piperazinyl-pyridine analogues |
PE20050952A1 (es) * | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
GB0415364D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
GB0415365D0 (en) * | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
CA2635997A1 (en) | 2006-01-11 | 2007-07-19 | Astrazeneca Ab | Morpholino pyrimidine derivatives and their use in therapy |
JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
KR20090108124A (ko) * | 2007-02-06 | 2009-10-14 | 노파르티스 아게 | Pi 3-키나제 억제제 및 그의 사용 방법 |
RU2013141559A (ru) | 2011-02-11 | 2015-03-20 | Дана-Фарбер Кэнсер Инститьют, Инк. | Способ ингибирования клеток опухоли гамартомы |
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