JP2010514689A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010514689A5 JP2010514689A5 JP2009543209A JP2009543209A JP2010514689A5 JP 2010514689 A5 JP2010514689 A5 JP 2010514689A5 JP 2009543209 A JP2009543209 A JP 2009543209A JP 2009543209 A JP2009543209 A JP 2009543209A JP 2010514689 A5 JP2010514689 A5 JP 2010514689A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- group
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 57
- 229910052739 hydrogen Inorganic materials 0.000 claims 48
- 239000001257 hydrogen Substances 0.000 claims 43
- 229910052736 halogen Inorganic materials 0.000 claims 34
- 150000002367 halogens Chemical class 0.000 claims 34
- 125000000217 alkyl group Chemical group 0.000 claims 33
- 150000002431 hydrogen Chemical class 0.000 claims 29
- 239000003814 drug Substances 0.000 claims 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 25
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 23
- 125000003118 aryl group Chemical group 0.000 claims 22
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 22
- 102000001253 Protein Kinase Human genes 0.000 claims 16
- 108060006633 protein kinase Proteins 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 13
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 12
- -1 nitro, hydroxy Chemical group 0.000 claims 12
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 11
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 11
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 9
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 8
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 208000035475 disorder Diseases 0.000 claims 8
- 150000002148 esters Chemical class 0.000 claims 8
- 150000002825 nitriles Chemical class 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims 6
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 6
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims 6
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 6
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 6
- 239000004480 active ingredient Substances 0.000 claims 6
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 6
- NAROVGXVMKGQLH-UHFFFAOYSA-N 4-(1h-imidazol-2-yl)morpholine Chemical compound C1COCCN1C1=NC=CN1 NAROVGXVMKGQLH-UHFFFAOYSA-N 0.000 claims 5
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 5
- 239000003112 inhibitor Substances 0.000 claims 5
- 206010009944 Colon cancer Diseases 0.000 claims 4
- 206010061218 Inflammation Diseases 0.000 claims 4
- 206010033128 Ovarian cancer Diseases 0.000 claims 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 4
- 208000036142 Viral infection Diseases 0.000 claims 4
- 150000001408 amides Chemical group 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 206010017758 gastric cancer Diseases 0.000 claims 4
- 230000004054 inflammatory process Effects 0.000 claims 4
- SBOJXQVPLKSXOG-UHFFFAOYSA-N o-amino-hydroxylamine Chemical class NON SBOJXQVPLKSXOG-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 201000011549 stomach cancer Diseases 0.000 claims 4
- 229940124530 sulfonamide Drugs 0.000 claims 4
- 150000003456 sulfonamides Chemical class 0.000 claims 4
- 150000003457 sulfones Chemical class 0.000 claims 4
- 150000003852 triazoles Chemical class 0.000 claims 4
- 230000009385 viral infection Effects 0.000 claims 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 claims 3
- 102100032857 Cyclin-dependent kinase 1 Human genes 0.000 claims 3
- 101710106279 Cyclin-dependent kinase 1 Proteins 0.000 claims 3
- 102100036239 Cyclin-dependent kinase 2 Human genes 0.000 claims 3
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 claims 3
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 3
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 229940127089 cytotoxic agent Drugs 0.000 claims 3
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 3
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 3
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 3
- 150000003536 tetrazoles Chemical class 0.000 claims 3
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010005949 Bone cancer Diseases 0.000 claims 2
- 208000018084 Bone neoplasm Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 101150013553 CD40 gene Proteins 0.000 claims 2
- 102100032937 CD40 ligand Human genes 0.000 claims 2
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 2
- 208000006029 Cardiomegaly Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 claims 2
- 108010025454 Cyclin-Dependent Kinase 5 Proteins 0.000 claims 2
- 108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 claims 2
- 102100036252 Cyclin-dependent kinase 4 Human genes 0.000 claims 2
- 102100026804 Cyclin-dependent kinase 6 Human genes 0.000 claims 2
- 102100026810 Cyclin-dependent kinase 7 Human genes 0.000 claims 2
- 102100024456 Cyclin-dependent kinase 8 Human genes 0.000 claims 2
- 102100026805 Cyclin-dependent-like kinase 5 Human genes 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 2
- 101000759376 Escherichia phage Mu Tail sheath protein Proteins 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims 2
- 101000868215 Homo sapiens CD40 ligand Proteins 0.000 claims 2
- 101000911952 Homo sapiens Cyclin-dependent kinase 7 Proteins 0.000 claims 2
- 101000980937 Homo sapiens Cyclin-dependent kinase 8 Proteins 0.000 claims 2
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims 2
- 241000725303 Human immunodeficiency virus Species 0.000 claims 2
- 241000701806 Human papillomavirus Species 0.000 claims 2
- 206010023825 Laryngeal cancer Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 241000710960 Sindbis virus Species 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 102100040245 Tumor necrosis factor receptor superfamily member 5 Human genes 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims 2
- 241000700605 Viruses Species 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 208000037976 chronic inflammation Diseases 0.000 claims 2
- 230000006020 chronic inflammation Effects 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 claims 2
- 239000002254 cytotoxic agent Substances 0.000 claims 2
- 231100000599 cytotoxic agent Toxicity 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 125000006575 electron-withdrawing group Chemical group 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 2
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 150000003568 thioethers Chemical class 0.000 claims 2
- JSPLKZUTYZBBKA-UHFFFAOYSA-N trioxidane Chemical compound OOO JSPLKZUTYZBBKA-UHFFFAOYSA-N 0.000 claims 2
- 241000701161 unidentified adenovirus Species 0.000 claims 2
- 241001529453 unidentified herpesvirus Species 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 1
- NQVIIUBWMBHLOZ-UHFFFAOYSA-N 2-[2-hydroxyethyl-[6-[(4-methoxyphenyl)methylamino]-9-propan-2-ylpurin-2-yl]amino]ethanol Chemical compound C1=CC(OC)=CC=C1CNC1=NC(N(CCO)CCO)=NC2=C1N=CN2C(C)C NQVIIUBWMBHLOZ-UHFFFAOYSA-N 0.000 claims 1
- NDMPLJNOPCLANR-UHFFFAOYSA-N 3,4-dihydroxy-15-(4-hydroxy-18-methoxycarbonyl-5,18-seco-ibogamin-18-yl)-16-methoxy-1-methyl-6,7-didehydro-aspidospermidine-3-carboxylic acid methyl ester Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 NDMPLJNOPCLANR-UHFFFAOYSA-N 0.000 claims 1
- TVZGACDUOSZQKY-LBPRGKRZSA-N 4-aminofolic acid Chemical compound C1=NC2=NC(N)=NC(N)=C2N=C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 TVZGACDUOSZQKY-LBPRGKRZSA-N 0.000 claims 1
- WNWVKZTYMQWFHE-UHFFFAOYSA-N 4-ethylmorpholine Chemical compound [CH2]CN1CCOCC1 WNWVKZTYMQWFHE-UHFFFAOYSA-N 0.000 claims 1
- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims 1
- 102100036329 Cyclin-dependent kinase 3 Human genes 0.000 claims 1
- 229930105110 Cyclosporin A Natural products 0.000 claims 1
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims 1
- 108010036949 Cyclosporine Proteins 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- 101000715946 Homo sapiens Cyclin-dependent kinase 3 Proteins 0.000 claims 1
- 101000979342 Homo sapiens Nuclear factor NF-kappa-B p105 subunit Proteins 0.000 claims 1
- 101100369992 Homo sapiens TNFSF10 gene Proteins 0.000 claims 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 1
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 1
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 1
- JXLYSJRDGCGARV-PJXZDTQASA-N Leurosidine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-PJXZDTQASA-N 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 102100023050 Nuclear factor NF-kappa-B p105 subunit Human genes 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- HRHKSTOGXBBQCB-UHFFFAOYSA-N Porfiromycine Chemical compound O=C1C(N)=C(C)C(=O)C2=C1C(COC(N)=O)C1(OC)C3N(C)C3CN12 HRHKSTOGXBBQCB-UHFFFAOYSA-N 0.000 claims 1
- 102000046283 TNF-Related Apoptosis-Inducing Ligand Human genes 0.000 claims 1
- 108700012411 TNFSF10 Proteins 0.000 claims 1
- QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 claims 1
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 1
- 108060008683 Tumor Necrosis Factor Receptor Proteins 0.000 claims 1
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 1
- JXLYSJRDGCGARV-KSNABSRWSA-N ac1l29ym Chemical compound C([C@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-KSNABSRWSA-N 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 229960003896 aminopterin Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims 1
- 230000033228 biological regulation Effects 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229960004562 carboplatin Drugs 0.000 claims 1
- 229930188550 carminomycin Natural products 0.000 claims 1
- XREUEWVEMYWFFA-CSKJXFQVSA-N carminomycin Chemical compound C1[C@H](N)[C@H](O)[C@H](C)O[C@H]1O[C@@H]1C2=C(O)C(C(=O)C3=C(O)C=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XREUEWVEMYWFFA-CSKJXFQVSA-N 0.000 claims 1
- XREUEWVEMYWFFA-UHFFFAOYSA-N carminomycin I Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=C(O)C=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XREUEWVEMYWFFA-UHFFFAOYSA-N 0.000 claims 1
- 229950001725 carubicin Drugs 0.000 claims 1
- 238000004113 cell culture Methods 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 230000036755 cellular response Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229960001265 ciclosporin Drugs 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229940104302 cytosine Drugs 0.000 claims 1
- STQGQHZAVUOBTE-VGBVRHCVSA-N daunorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(C)=O)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 STQGQHZAVUOBTE-VGBVRHCVSA-N 0.000 claims 1
- 229960000975 daunorubicin Drugs 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- YJGVMLPVUAXIQN-UHFFFAOYSA-N epipodophyllotoxin Natural products COC1=C(OC)C(OC)=CC(C2C3=CC=4OCOC=4C=C3C(O)C3C2C(OC3)=O)=C1 YJGVMLPVUAXIQN-UHFFFAOYSA-N 0.000 claims 1
- 229930013356 epothilone Natural products 0.000 claims 1
- 150000003883 epothilone derivatives Chemical class 0.000 claims 1
- 229960005420 etoposide Drugs 0.000 claims 1
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims 1
- 229960000752 etoposide phosphate Drugs 0.000 claims 1
- LIQODXNTTZAGID-OCBXBXKTSA-N etoposide phosphate Chemical compound COC1=C(OP(O)(O)=O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 LIQODXNTTZAGID-OCBXBXKTSA-N 0.000 claims 1
- 229960002949 fluorouracil Drugs 0.000 claims 1
- 102000037865 fusion proteins Human genes 0.000 claims 1
- 108020001507 fusion proteins Proteins 0.000 claims 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- 229940080856 gleevec Drugs 0.000 claims 1
- 150000002344 gold compounds Chemical class 0.000 claims 1
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 1
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 1
- 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 1
- 150000002460 imidazoles Chemical class 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 229940125721 immunosuppressive agent Drugs 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 229960000681 leflunomide Drugs 0.000 claims 1
- VHOGYURTWQBHIL-UHFFFAOYSA-N leflunomide Chemical compound O1N=CC(C(=O)NC=2C=CC(=CC=2)C(F)(F)F)=C1C VHOGYURTWQBHIL-UHFFFAOYSA-N 0.000 claims 1
- 230000001926 lymphatic effect Effects 0.000 claims 1
- SGDBTWWWUNNDEQ-LBPRGKRZSA-N melphalan Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N(CCCl)CCCl)C=C1 SGDBTWWWUNNDEQ-LBPRGKRZSA-N 0.000 claims 1
- 229960001924 melphalan Drugs 0.000 claims 1
- 229960001428 mercaptopurine Drugs 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229960004857 mitomycin Drugs 0.000 claims 1
- 229950007856 mofetil Drugs 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 150000007965 phenolic acids Chemical class 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 150000003053 piperidines Chemical group 0.000 claims 1
- YJGVMLPVUAXIQN-XVVDYKMHSA-N podophyllotoxin Chemical compound COC1=C(OC)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@H](O)[C@@H]3[C@@H]2C(OC3)=O)=C1 YJGVMLPVUAXIQN-XVVDYKMHSA-N 0.000 claims 1
- 229960001237 podophyllotoxin Drugs 0.000 claims 1
- YVCVYCSAAZQOJI-UHFFFAOYSA-N podophyllotoxin Natural products COC1=C(O)C(OC)=CC(C2C3=CC=4OCOC=4C=C3C(O)C3C2C(OC3)=O)=C1 YVCVYCSAAZQOJI-UHFFFAOYSA-N 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 1
- 229960002930 sirolimus Drugs 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 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
- NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 claims 1
- 229960001278 teniposide Drugs 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 229940046728 tumor necrosis factor alpha inhibitor Drugs 0.000 claims 1
- 239000002452 tumor necrosis factor alpha inhibitor Substances 0.000 claims 1
- 102000003298 tumor necrosis factor receptor Human genes 0.000 claims 1
- 229960003048 vinblastine Drugs 0.000 claims 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
- 229960004528 vincristine Drugs 0.000 claims 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims 1
- 229960004355 vindesine Drugs 0.000 claims 1
- UGGWPQSBPIFKDZ-KOTLKJBCSA-N vindesine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(N)=O)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1N=C1[C]2C=CC=C1 UGGWPQSBPIFKDZ-KOTLKJBCSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87147106P | 2006-12-22 | 2006-12-22 | |
| PCT/US2007/088292 WO2008079933A2 (en) | 2006-12-22 | 2007-12-20 | Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010514689A JP2010514689A (ja) | 2010-05-06 |
| JP2010514689A5 true JP2010514689A5 (enExample) | 2011-02-17 |
Family
ID=39367530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009543209A Pending JP2010514689A (ja) | 2006-12-22 | 2007-12-20 | 癌、炎症およびウイルス感染症の処置のためのｃｄｋ阻害剤としてのヘテロアリール−ヘテロアリール化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20100048597A1 (enExample) |
| EP (1) | EP2094682A2 (enExample) |
| JP (1) | JP2010514689A (enExample) |
| KR (1) | KR20090091306A (enExample) |
| CN (1) | CN101568529A (enExample) |
| AU (1) | AU2007336933A1 (enExample) |
| BR (1) | BRPI0720635A2 (enExample) |
| CA (1) | CA2672518A1 (enExample) |
| EA (1) | EA200900799A1 (enExample) |
| MX (1) | MX2009006536A (enExample) |
| WO (1) | WO2008079933A2 (enExample) |
Families Citing this family (115)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2686382C (en) * | 2007-05-04 | 2013-09-17 | Irm Llc | Phenylaminopyrimidine derivatives and compositions thereof as c-kit and pdgfr kinase inhibitors |
| PT2200436E (pt) | 2007-09-04 | 2015-04-29 | Scripps Research Inst | Pirimidinilaminas substituídas como inibidoras da proteína quinase |
| EP2341911A4 (en) * | 2008-10-01 | 2012-10-24 | Univ North Carolina | HEMATOPOIETIC PROTECTION AGAINST CHEMOTHERAPEUTIC COMPOUNDS USING SELECTIVE INHIBITORS OF KINASES DEPENDENT ON CYCLINES 4/6 |
| AR074339A1 (es) * | 2008-11-14 | 2011-01-12 | Bayer Cropscience Sa | Derivados de (piridil) -azinilamida sustituidos como agentes de proteccion de plantas |
| AU2010248886A1 (en) | 2009-05-13 | 2011-12-01 | The University Of North Carolina At Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
| US8415381B2 (en) * | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
| CA2771563A1 (en) * | 2009-09-04 | 2011-03-10 | Novartis Ag | Bipyridines useful for the treatment of proliferative diseases |
| US20120165306A1 (en) * | 2009-09-04 | 2012-06-28 | Barsanti Paul A | Pyrazinylpyridines useful for the treatment of proliferative diseases |
| BR112012015916A2 (pt) * | 2009-12-31 | 2017-04-25 | Novartis Ag | derivados de pirazina e seu uso no tratamento de distúrbios neurológicos |
| EA026917B1 (ru) * | 2010-03-22 | 2017-05-31 | Лид Дискавери Сентр Гмбх | Фармацевтически активные производные двузамещенного триазина |
| JP2013542967A (ja) * | 2010-11-17 | 2013-11-28 | ノバルティス アーゲー | ３−（アミノアリール）−ピリジン化合物 |
| US9808461B2 (en) | 2010-11-17 | 2017-11-07 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6 |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| WO2012101065A2 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | Pyrimidine biaryl amine compounds and their uses |
| WO2012101013A1 (en) * | 2011-01-28 | 2012-08-02 | Boehringer Ingelheim International Gmbh | Substituted pyridinyl-pyrimidines and their use as medicaments |
| WO2012101063A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyridine biaryl compounds and their uses |
| WO2012101066A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | Pyridine biaryl amine compounds and their uses |
| WO2012101064A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyrimidine biaryl compounds as protein kinase inhibitors |
| EP2668162A1 (en) * | 2011-01-28 | 2013-12-04 | Novartis AG | Substituted bi-heteroaryl compounds as cdk9 inhibitors and their uses |
| WO2012118850A1 (en) | 2011-02-28 | 2012-09-07 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
| CN103562184B (zh) * | 2011-03-02 | 2016-04-27 | 利德探索中心有限公司 | 药学活性的二取代的吡啶衍生物 |
| US9226929B2 (en) | 2011-03-02 | 2016-01-05 | Bayer Intellectual Property Gmbh | Pharmaceutically active disubstituted triazine derivatives |
| KR20140019381A (ko) * | 2011-04-19 | 2014-02-14 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 치환된 4-아릴-n-페닐-1,3,5-트리아진-2-아민 |
| TWI555737B (zh) * | 2011-05-24 | 2016-11-01 | 拜耳知識產權公司 | 含有硫醯亞胺基團之４－芳基－ｎ－苯基－１，３，５－三氮雜苯－２－胺 |
| EP2527332A1 (en) | 2011-05-24 | 2012-11-28 | Bayer Intellectual Property GmbH | 4-Aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group as CDK9 inhibitors |
| ES2552989T3 (es) | 2011-08-04 | 2015-12-03 | Array Biopharma, Inc. | Compuestos de quinazolina como inhibidores de la cinasa de serina / treonina |
| EP2561867A1 (en) | 2011-08-22 | 2013-02-27 | Lead Discovery Center GmbH | CDK9 inhibitors in the treatment of midline carcinoma |
| EP2562265A1 (en) | 2011-08-22 | 2013-02-27 | Lead Discovery Center GmbH | Susceptibility to selective CDK9 inhibitors |
| WO2013037894A1 (en) | 2011-09-16 | 2013-03-21 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group |
| US9108926B2 (en) * | 2011-09-16 | 2015-08-18 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro-pyrimidines |
| WO2013059634A1 (en) | 2011-10-20 | 2013-04-25 | The Regents Of The University Of California | Use of cdk9 inhibitors to reduce cartilage degradation |
| CN106349217B (zh) | 2012-03-01 | 2020-08-28 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| EP3176170B1 (en) | 2012-06-13 | 2018-11-14 | Incyte Holdings Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| US8901305B2 (en) * | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| MX2015002310A (es) | 2012-08-23 | 2015-06-05 | Hoffmann La Roche | Nuevas amidas de fenil-piridina/pirazina para el tratamiento de cancer. |
| HK1210174A1 (en) | 2012-08-27 | 2016-04-15 | Array Biopharma, Inc. | Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases |
| EP2900665B1 (en) * | 2012-09-28 | 2018-01-03 | Merck Sharp & Dohme Corp. | Triazolyl derivatives as syk inhibitors |
| JP2015536311A (ja) | 2012-10-18 | 2015-12-21 | バイエル ファーマ アクチエンゲゼルシャフト | スルホン基を含有する４−（オルト）−フルオロフェニル−５−フルオロピリミジン−２−イルアミン |
| CA2888383A1 (en) | 2012-10-18 | 2014-04-24 | Bayer Pharma Aktiengesellschaft | N-(pyridin-2-yl)pyrimidin-4-amine derivatives containing a sulfone group |
| CN104854091B (zh) | 2012-10-18 | 2018-04-03 | 拜耳药业股份公司 | 含砜基团的5‑氟‑n‑(吡啶‑2‑基)吡啶‑2‑胺衍生物 |
| TW201418243A (zh) | 2012-11-15 | 2014-05-16 | Bayer Pharma AG | 含有磺醯亞胺基團之ｎ－（吡啶－２－基）嘧啶－４－胺衍生物 |
| JP6263193B2 (ja) | 2012-11-15 | 2018-01-17 | バイエル ファーマ アクチエンゲゼルシャフト | スルホキシイミン基を含んでいる５−フルオロ−ｎ−（ピリジン−２−イル）ピリジン−２−アミン誘導体 |
| UA118094C2 (uk) | 2012-11-21 | 2018-11-26 | Пітісі Терап'Ютикс, Інк. | Заміщені зворотні піримідинові інгібітори bmi-1 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| CA2906166C (en) | 2013-03-15 | 2023-03-14 | G1 Therapeutics, Inc. | Hspc-sparing treatments for rb-positive abnormal cellular proliferation |
| JP6435315B2 (ja) | 2013-03-15 | 2018-12-05 | ジー１、セラピューティクス、インコーポレイテッドＧ１ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | 高活性抗新生物薬及び抗増殖剤 |
| SG10201708520YA (en) | 2013-04-19 | 2017-12-28 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| JP6371385B2 (ja) | 2013-07-04 | 2018-08-08 | バイエル ファーマ アクチエンゲゼルシャフト | スルホキシイミン置換５−フルオロ−ｎ−（ピリジン−２−イル）ピリジン−２−アミン誘導体およびそのｃｄｋ９キナーゼ阻害薬としての使用 |
| WO2015030847A1 (en) * | 2013-08-30 | 2015-03-05 | Ptc Therapeutics, Inc. | Substituted pyrimidine bmi-1 inhibitors |
| WO2015049325A1 (en) * | 2013-10-03 | 2015-04-09 | F. Hoffmann-La Roche Ag | Therapeutic inhibitors of cdk8 and uses thereof |
| EP3071553A4 (en) | 2013-11-21 | 2017-08-02 | PTC Therapeutics, Inc. | Substituted pyridine and pyrazine bmi-1 inhibitors |
| EP3091008B1 (en) | 2013-12-31 | 2018-06-27 | Xuanzhu Pharma Co., Ltd. | Kinase inhibitor and use thereof |
| US9949976B2 (en) | 2013-12-31 | 2018-04-24 | Xuanzhu Pharma Co., Ltd. | Kinase inhibitor and use thereof |
| CA2935867C (en) | 2014-01-14 | 2023-04-04 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| JP2017508757A (ja) | 2014-03-13 | 2017-03-30 | バイエル ファーマ アクチエンゲゼルシャフト | スルホン基を含有する５−フルオロ−ｎ−（ピリジン−２−イル）ピリジン−２−アミン誘導体 |
| EP3126338B1 (en) | 2014-04-01 | 2019-09-04 | Bayer Pharma Aktiengesellschaft | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfondiimine group |
| EP3129387B1 (en) | 2014-04-11 | 2019-06-26 | Bayer Pharma Aktiengesellschaft | Novel macrocyclic compounds |
| US20150297606A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic Lactams for Use in the Protection of Hematopoietic Stem and Progenitor Cells Against Ionizing Radiation |
| EP3191098A4 (en) | 2014-09-12 | 2018-04-25 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| WO2016061144A1 (en) | 2014-10-14 | 2016-04-21 | The Regents Of The University Of California | Use of cdk9 and brd4 inhibitors to inhibit inflammation |
| WO2016059086A1 (en) | 2014-10-16 | 2016-04-21 | Bayer Pharma Aktiengesellschaft | Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group |
| CN107207475A (zh) | 2014-10-16 | 2017-09-26 | 拜耳医药股份有限公司 | 含有砜基团的氟化苯并呋喃基‑嘧啶衍生物 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CN111170998B (zh) * | 2014-11-05 | 2023-04-11 | 益方生物科技(上海)股份有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| JP2018509439A (ja) | 2015-03-24 | 2018-04-05 | バイエル ファーマ アクチエンゲゼルシャフト | 多発性骨髄腫を治療するための４−（４−フルオロ−２−メトキシフェニル）−ｎ−｛３−［（ｓ−メチルスルホンイミドイル）メチル］フェニル｝−１，３，５−トリアジン−２−アミンの使用 |
| JP2018509440A (ja) | 2015-03-24 | 2018-04-05 | バイエル ファーマ アクチエンゲゼルシャフト | リンパ腫の治療のための４−（４−フルオロ−２−メトキシフェニル）−ｎ−｛３−［（ｓ−メチルスルホンイミドイル）メチル］フェニル｝−１，３，５−トリアジン−２−アミンの使用 |
| WO2016150902A1 (en) | 2015-03-24 | 2016-09-29 | Bayer Pharma Aktiengesellschaft | Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating gastric cancers |
| CN106188029B (zh) * | 2015-05-05 | 2018-09-18 | 山东轩竹医药科技有限公司 | 二并环类间变性淋巴瘤激酶抑制剂 |
| CN106699785A (zh) * | 2015-07-13 | 2017-05-24 | 南开大学 | 作为CDK4/6抑制剂的2-(N-氧化吡啶-2基氨基)-吡啶并[2,3-d]嘧啶-7-酮类化合物 |
| ES2786552T3 (es) | 2015-09-29 | 2020-10-13 | Bayer Pharma AG | Compuestos de sulfondiimina macrocíclicos nuevos |
| ES2819869T3 (es) | 2015-10-08 | 2021-04-19 | Bayer Pharma AG | Nuevos compuestos macrocíclicos modificados |
| WO2017060322A2 (en) | 2015-10-10 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Ptefb-inhibitor-adc |
| IL311265A (en) | 2016-12-05 | 2024-05-01 | G1 Therapeutics Inc | Preservation of immune response during chemotherapy regimens |
| WO2018177889A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| US11254690B2 (en) | 2017-03-28 | 2022-02-22 | Bayer Pharma Aktiengesellschaft | PTEFb inhibiting macrocyclic compounds |
| GB201705263D0 (en) * | 2017-03-31 | 2017-05-17 | Probiodrug Ag | Novel inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CN109985241B (zh) * | 2017-12-29 | 2024-10-18 | 广州威溶特医药科技有限公司 | Cdk抑制剂和溶瘤病毒在制备抗肿瘤药物的应用 |
| CN111837146B (zh) | 2018-01-08 | 2024-10-15 | G1治疗公司 | G1t38优异剂量方案 |
| CN110041253B (zh) * | 2018-01-17 | 2022-03-29 | 上海翰森生物医药科技有限公司 | 吡啶类n-氧化衍生物及其制备方法和应用 |
| KR102764122B1 (ko) | 2018-02-13 | 2025-02-05 | 바이엘 악티엔게젤샤프트 | 미만성 거대 b-세포 림프종을 치료하기 위한 5-플루오로-4-(4-플루오로-2-메톡시페닐)-n-[4-[(s-메틸술폰이미도일)메틸]피리딘-2-일]피리딘-2-아민의 용도 |
| CR20240498A (es) | 2018-05-04 | 2025-01-08 | Incyte Corp | FORMAS SÓLIDAS DE UN INHIBIDOR DE FGFR Y PROCESOS PARA PREPARARLAS (Divisional EXP. 2020-0590) |
| BR112020022373A2 (pt) | 2018-05-04 | 2021-02-02 | Incyte Corporation | sais de um inibidor de fgfr |
| CN113164479A (zh) | 2018-08-17 | 2021-07-23 | Ptc医疗公司 | 用于治疗胰腺癌的方法 |
| JP7098826B2 (ja) * | 2018-09-12 | 2022-07-11 | ジェネンテック， インコーポレイテッド | ピリミジニル－ヘテロアリールオキシ－ナフチル化合物および使用方法 |
| TWI831829B (zh) | 2018-09-12 | 2024-02-11 | 美商建南德克公司 | 苯氧基-吡啶基-嘧啶化合物及使用方法 |
| US20220017520A1 (en) | 2018-12-19 | 2022-01-20 | Keythera (Suzhou) Pharmaceuticals Co. Ltd. | Macrocyclic compound as cdk inhibitor, preparation method therefor, and use thereof in medicine |
| WO2020142612A1 (en) | 2019-01-03 | 2020-07-09 | Genentech, Inc. | Pyrido-pyrimidinone and pteridinone compounds as inhibitors of endoribonuclease inositol requiring enzyme i (ire i alpha) for the treatment of cancer diseases. |
| CN109678962B (zh) * | 2019-01-22 | 2020-05-08 | 山西农业大学 | 一种Cdk5纳米抗体和筛选方法 |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| CN109836385B (zh) * | 2019-04-04 | 2021-12-17 | 上海翰森生物医药科技有限公司 | 四氢喹啉类n-氧化衍生物及其制备方法和应用 |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN110511211B (zh) * | 2019-08-30 | 2020-10-16 | 武汉工程大学 | 一种吲唑哌啶嘧啶类化合物的应用 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JOP20220083A1 (ar) | 2019-10-14 | 2023-01-30 | Incyte Corp | حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| PE20221504A1 (es) | 2019-12-04 | 2022-09-30 | Incyte Corp | Derivados de un inhibidor de fgfr |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN111349624A (zh) * | 2020-03-20 | 2020-06-30 | 深圳大学 | 核酸、多肽偶联组合物、多肽组合物及其制备方法和应用 |
| US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
| KR20230038740A (ko) * | 2020-08-07 | 2023-03-21 | 파마블럭 사이언시스 (난징), 인코포레이티드 | Cdk9 억제제 및 이의 용도 |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| KR102693170B1 (ko) * | 2021-04-27 | 2024-08-08 | 재단법인 아산사회복지재단 | 사이클린 의존성 키나아제 억제용 조성물 및 이의 의학적 용도 |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| JP2024522188A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式ヘテロ環 |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CN117384135A (zh) * | 2022-07-04 | 2024-01-12 | 浙江同源康医药股份有限公司 | 用作cdk7激酶抑制剂的化合物及其应用 |
| CN119841771A (zh) * | 2025-01-08 | 2025-04-18 | 华中农业大学 | 一种猪链球菌丝氨酸蛋白激酶抑制剂的筛选方法及其应用 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4788195A (en) * | 1986-01-13 | 1988-11-29 | American Cyanamid Company | 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines |
| EP0233461B2 (en) * | 1986-01-13 | 2002-05-29 | American Cyanamid Company | 4,5,6-Substituted-2-pyrimidinamines |
| US5521184A (en) * | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| GB9523675D0 (en) * | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| US5744460A (en) * | 1996-03-07 | 1998-04-28 | Novartis Corporation | Combination for treatment of proliferative diseases |
| US6057329A (en) * | 1996-12-23 | 2000-05-02 | Celltech Therapeutics Limited | Fused polycyclic 2-aminopyrimidine derivatives |
| JP2002534385A (ja) * | 1999-01-08 | 2002-10-15 | スミスクライン・ビーチャム・コーポレイション | 新規化合物 |
| US7122544B2 (en) * | 2000-12-06 | 2006-10-17 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto |
| US6949544B2 (en) * | 2001-03-29 | 2005-09-27 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases |
| DK1533304T3 (da) * | 2002-06-28 | 2010-03-22 | Nippon Shinyaku Co Ltd | Amidderivat |
| GB0226724D0 (en) * | 2002-11-15 | 2002-12-24 | Merck Sharp & Dohme | Therapeutic agents |
| SE0203654D0 (sv) * | 2002-12-09 | 2002-12-09 | Astrazeneca Ab | New compounds |
| WO2004078682A2 (en) * | 2003-03-05 | 2004-09-16 | Irm Llc | Cyclic compounds and compositions as protein kinase inhibitors |
| GB0307268D0 (en) * | 2003-03-28 | 2003-05-07 | Syngenta Ltd | Organic compounds |
| WO2005065074A2 (en) * | 2003-09-09 | 2005-07-21 | Temple University Of The Commonwealth System Of Higher Education | Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors |
| BRPI0418074B8 (pt) * | 2003-12-25 | 2021-05-25 | Nippon Shinyaku Co Ltd | derivado de amida, composição farmacêutica, inibidor da tirosina cinase bcr-abl e agentes terapêuticos |
| CA2564355C (en) * | 2004-05-07 | 2012-07-03 | Amgen Inc. | Protein kinase modulators and method of use |
| CA2578122A1 (en) * | 2004-08-27 | 2006-03-02 | Gpc Biotech Ag | Pyrimidine derivatives |
| EP2364702A3 (en) * | 2006-09-05 | 2012-01-25 | Emory University | Kinase inhibitors for preventing or treating pathogen infection and method of use thereof |
-
2007
- 2007-12-20 WO PCT/US2007/088292 patent/WO2008079933A2/en not_active Ceased
- 2007-12-20 EP EP07869607A patent/EP2094682A2/en not_active Withdrawn
- 2007-12-20 CA CA002672518A patent/CA2672518A1/en not_active Abandoned
- 2007-12-20 US US12/520,755 patent/US20100048597A1/en not_active Abandoned
- 2007-12-20 AU AU2007336933A patent/AU2007336933A1/en not_active Abandoned
- 2007-12-20 BR BRPI0720635-6A patent/BRPI0720635A2/pt not_active Application Discontinuation
- 2007-12-20 EA EA200900799A patent/EA200900799A1/ru unknown
- 2007-12-20 KR KR1020097012787A patent/KR20090091306A/ko not_active Withdrawn
- 2007-12-20 CN CNA2007800476340A patent/CN101568529A/zh active Pending
- 2007-12-20 MX MX2009006536A patent/MX2009006536A/es not_active Application Discontinuation
- 2007-12-20 JP JP2009543209A patent/JP2010514689A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2010514689A5 (enExample) | ||
| JP5815558B2 (ja) | キナーゼ調節のための化合物及び方法ならびにそれらの適応症 | |
| JP6506779B2 (ja) | 医薬化合物 | |
| CN107108637B (zh) | 三唑并嘧啶化合物及其用途 | |
| JP6277198B2 (ja) | 置換インドール−５−オール誘導体及びそれらの治療適用 | |
| RU2686323C2 (ru) | Новые соединения и композиции для ингибирования fasn | |
| JP2022501431A (ja) | Ｓｒｃホモロジー−２ホスファターゼ阻害剤としての縮合三環式環誘導体 | |
| CN111201223A (zh) | SHP2的八氢环戊二烯并[c]吡咯别构抑制剂 | |
| ME00486B (me) | Jedinjenja pirolopirimidina i njihova upotreba | |
| JP2018510857A5 (enExample) | ||
| TW201701879A (zh) | Ｉｒａｋ４抑制劑組合 | |
| KR20120062839A (ko) | 단백질 키나제 억제제로서의 화합물 및 조성물 | |
| JP6885629B2 (ja) | インドリノン化合物の使用 | |
| US11529350B2 (en) | Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof | |
| US20070185013A1 (en) | Use of chk1 inhibitors to control cell proliferation | |
| JP2018509442A (ja) | Ｆｇｆｒ４阻害剤としてのホルミル化ｎ−複素環式誘導体 | |
| JP2018087200A (ja) | 置換インドール−５−オール誘導体及びそれらの治療適用 | |
| CN112739345A (zh) | Pim激酶抑制剂组合物，方法和其用途 | |
| US20230106032A1 (en) | Imidazotriazines acting on cancer via inhibition of cdk12 | |
| JP2024542984A (ja) | がんを治療および予防するためのピペリジニルピラジン－カルボキサミド化合物、およびｂｔｋを分解するためのピペリジニルピラジン－カルボキサミド化合物 | |
| RU2011105059A (ru) | Применение производных пиримидиламинобензамида для лечения фиброза | |
| US20240336592A1 (en) | Phenyl- and pyridopyrazole derivatives as inhibitors of ddr1 | |
| US20230339939A1 (en) | Substituted 1h-pyrrolo[3,2-b]pyridine compounds and methods of use thereof | |
| JP2022531230A (ja) | Ｐｉｍキナーゼインヒビター組成物及びその使用 | |
| US20250127790A1 (en) | Combination therapy using vps34 inhibitors |