RU2016141566A - Производные пиразина, используемые в качестве ингибиторов киназы atr - Google Patents
Производные пиразина, используемые в качестве ингибиторов киназы atr Download PDFInfo
- Publication number
- RU2016141566A RU2016141566A RU2016141566A RU2016141566A RU2016141566A RU 2016141566 A RU2016141566 A RU 2016141566A RU 2016141566 A RU2016141566 A RU 2016141566A RU 2016141566 A RU2016141566 A RU 2016141566A RU 2016141566 A RU2016141566 A RU 2016141566A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- aliphatic group
- compound
- optionally substituted
- halogen
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 125000001931 aliphatic group Chemical group 0.000 claims 218
- 125000000217 alkyl group Chemical group 0.000 claims 199
- 150000001875 compounds Chemical class 0.000 claims 192
- 229910052736 halogen Inorganic materials 0.000 claims 97
- 150000002367 halogens Chemical class 0.000 claims 97
- 229910052799 carbon Inorganic materials 0.000 claims 95
- 229910052717 sulfur Inorganic materials 0.000 claims 95
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 82
- 229910052760 oxygen Inorganic materials 0.000 claims 82
- 229910052739 hydrogen Inorganic materials 0.000 claims 76
- 125000005842 heteroatom Chemical group 0.000 claims 70
- 238000000034 method Methods 0.000 claims 69
- 229910052757 nitrogen Inorganic materials 0.000 claims 69
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 65
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 62
- 239000001301 oxygen Chemical group 0.000 claims 62
- 125000000623 heterocyclic group Chemical group 0.000 claims 61
- 239000011593 sulfur Chemical group 0.000 claims 61
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 46
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 46
- 125000004429 atom Chemical group 0.000 claims 44
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 37
- 229910002091 carbon monoxide Inorganic materials 0.000 claims 35
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 35
- 125000003386 piperidinyl group Chemical group 0.000 claims 33
- 125000004193 piperazinyl group Chemical group 0.000 claims 28
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 27
- 206010028980 Neoplasm Diseases 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 21
- 125000004076 pyridyl group Chemical group 0.000 claims 21
- 210000004027 cell Anatomy 0.000 claims 20
- 125000005960 1,4-diazepanyl group Chemical group 0.000 claims 18
- 201000011510 cancer Diseases 0.000 claims 18
- 229910052731 fluorine Inorganic materials 0.000 claims 17
- 125000005843 halogen group Chemical group 0.000 claims 17
- 229920006395 saturated elastomer Polymers 0.000 claims 16
- 239000003112 inhibitor Substances 0.000 claims 14
- -1 2 -piperidinyl Chemical group 0.000 claims 13
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 12
- 239000011737 fluorine Substances 0.000 claims 12
- 239000012623 DNA damaging agent Substances 0.000 claims 11
- 208000009956 adenocarcinoma Diseases 0.000 claims 11
- 239000003795 chemical substances by application Substances 0.000 claims 11
- 125000004122 cyclic group Chemical group 0.000 claims 11
- 125000002950 monocyclic group Chemical group 0.000 claims 11
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 9
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 8
- 201000009030 Carcinoma Diseases 0.000 claims 8
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 8
- 125000002619 bicyclic group Chemical group 0.000 claims 8
- 230000007547 defect Effects 0.000 claims 8
- 125000002757 morpholinyl group Chemical group 0.000 claims 8
- 230000000340 anti-metabolite Effects 0.000 claims 7
- 229940100197 antimetabolite Drugs 0.000 claims 7
- 239000002256 antimetabolite Substances 0.000 claims 7
- 125000002393 azetidinyl group Chemical group 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 125000001544 thienyl group Chemical group 0.000 claims 7
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 6
- 206010025323 Lymphomas Diseases 0.000 claims 6
- 206010039491 Sarcoma Diseases 0.000 claims 6
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 6
- 230000003115 biocidal effect Effects 0.000 claims 6
- 239000012472 biological sample Substances 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 229940100198 alkylating agent Drugs 0.000 claims 5
- 239000002168 alkylating agent Substances 0.000 claims 5
- 125000003725 azepanyl group Chemical group 0.000 claims 5
- 230000005865 ionizing radiation Effects 0.000 claims 5
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 claims 5
- 125000002971 oxazolyl group Chemical group 0.000 claims 5
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 4
- 102000000872 ATM Human genes 0.000 claims 4
- 108010004586 Ataxia Telangiectasia Mutated Proteins Proteins 0.000 claims 4
- 102100025064 Cellular tumor antigen p53 Human genes 0.000 claims 4
- 102100039116 DNA repair protein RAD50 Human genes 0.000 claims 4
- 102100033996 Double-strand break repair protein MRE11 Human genes 0.000 claims 4
- 102100034533 Histone H2AX Human genes 0.000 claims 4
- 101000721661 Homo sapiens Cellular tumor antigen p53 Proteins 0.000 claims 4
- 101000743929 Homo sapiens DNA repair protein RAD50 Proteins 0.000 claims 4
- 101000591400 Homo sapiens Double-strand break repair protein MRE11 Proteins 0.000 claims 4
- 101001067891 Homo sapiens Histone H2AX Proteins 0.000 claims 4
- 101000581326 Homo sapiens Mediator of DNA damage checkpoint protein 1 Proteins 0.000 claims 4
- 101001128138 Homo sapiens NACHT, LRR and PYD domains-containing protein 2 Proteins 0.000 claims 4
- 101000981336 Homo sapiens Nibrin Proteins 0.000 claims 4
- 101000777277 Homo sapiens Serine/threonine-protein kinase Chk2 Proteins 0.000 claims 4
- 206010024612 Lipoma Diseases 0.000 claims 4
- 102100027643 Mediator of DNA damage checkpoint protein 1 Human genes 0.000 claims 4
- 102100024403 Nibrin Human genes 0.000 claims 4
- 102100031075 Serine/threonine-protein kinase Chk2 Human genes 0.000 claims 4
- 102000000504 Tumor Suppressor p53-Binding Protein 1 Human genes 0.000 claims 4
- 108010041385 Tumor Suppressor p53-Binding Protein 1 Proteins 0.000 claims 4
- 208000025865 Ulcer Diseases 0.000 claims 4
- 229940045714 alkyl sulfonate alkylating agent Drugs 0.000 claims 4
- 150000008052 alkyl sulfonates Chemical class 0.000 claims 4
- 239000002552 dosage form Substances 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 125000002541 furyl group Chemical group 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 4
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 150000003852 triazoles Chemical class 0.000 claims 4
- 231100000397 ulcer Toxicity 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 3
- WYWHKKSPHMUBEB-UHFFFAOYSA-N 6-Mercaptoguanine Natural products N1C(N)=NC(=S)C2=C1N=CN2 WYWHKKSPHMUBEB-UHFFFAOYSA-N 0.000 claims 3
- FJHBVJOVLFPMQE-QFIPXVFZSA-N 7-Ethyl-10-Hydroxy-Camptothecin Chemical compound C1=C(O)C=C2C(CC)=C(CN3C(C4=C([C@@](C(=O)OC4)(O)CC)C=C33)=O)C3=NC2=C1 FJHBVJOVLFPMQE-QFIPXVFZSA-N 0.000 claims 3
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 3
- PTOAARAWEBMLNO-KVQBGUIXSA-N Cladribine Chemical compound C1=NC=2C(N)=NC(Cl)=NC=2N1[C@H]1C[C@H](O)[C@@H](CO)O1 PTOAARAWEBMLNO-KVQBGUIXSA-N 0.000 claims 3
- 201000008808 Fibrosarcoma Diseases 0.000 claims 3
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 3
- 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 3
- 190014017285 Satraplatin Chemical compound 0.000 claims 3
- KLNFSAOEKUDMFA-UHFFFAOYSA-N azanide;2-hydroxyacetic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OCC(O)=O KLNFSAOEKUDMFA-UHFFFAOYSA-N 0.000 claims 3
- 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 3
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 3
- 229940127093 camptothecin Drugs 0.000 claims 3
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical group C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 3
- 229960004562 carboplatin Drugs 0.000 claims 3
- 229960004316 cisplatin Drugs 0.000 claims 3
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 3
- 229960002436 cladribine Drugs 0.000 claims 3
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims 3
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical group 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 3
- 229960005420 etoposide Drugs 0.000 claims 3
- 206010016629 fibroma Diseases 0.000 claims 3
- 229960000390 fludarabine Drugs 0.000 claims 3
- GIUYCYHIANZCFB-FJFJXFQQSA-N fludarabine phosphate Chemical compound C1=NC=2C(N)=NC(F)=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@@H]1O GIUYCYHIANZCFB-FJFJXFQQSA-N 0.000 claims 3
- 229960002949 fluorouracil Drugs 0.000 claims 3
- 201000011066 hemangioma Diseases 0.000 claims 3
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 3
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 3
- 125000001041 indolyl group Chemical group 0.000 claims 3
- 229960004768 irinotecan Drugs 0.000 claims 3
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 3
- 229960000485 methotrexate Drugs 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 229950007221 nedaplatin Drugs 0.000 claims 3
- 229960001756 oxaliplatin Drugs 0.000 claims 3
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims 3
- CPTBDICYNRMXFX-UHFFFAOYSA-N procarbazine Chemical compound CNNCC1=CC=C(C(=O)NC(C)C)C=C1 CPTBDICYNRMXFX-UHFFFAOYSA-N 0.000 claims 3
- 229960000624 procarbazine Drugs 0.000 claims 3
- VHXNKPBCCMUMSW-FQEVSTJZSA-N rubitecan Chemical compound C1=CC([N+]([O-])=O)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VHXNKPBCCMUMSW-FQEVSTJZSA-N 0.000 claims 3
- 229950009213 rubitecan Drugs 0.000 claims 3
- 229960005399 satraplatin Drugs 0.000 claims 3
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 229930192474 thiophene Natural products 0.000 claims 3
- 229960003087 tioguanine Drugs 0.000 claims 3
- MNRILEROXIRVNJ-UHFFFAOYSA-N tioguanine Chemical compound N1C(N)=NC(=S)C2=NC=N[C]21 MNRILEROXIRVNJ-UHFFFAOYSA-N 0.000 claims 3
- 229960000303 topotecan Drugs 0.000 claims 3
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 3
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 2
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims 2
- VSNHCAURESNICA-NJFSPNSNSA-N 1-oxidanylurea Chemical compound N[14C](=O)NO VSNHCAURESNICA-NJFSPNSNSA-N 0.000 claims 2
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims 2
- 206010001233 Adenoma benign Diseases 0.000 claims 2
- 201000003076 Angiosarcoma Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 102000002554 Cyclin A Human genes 0.000 claims 2
- 108010068192 Cyclin A Proteins 0.000 claims 2
- 102000003909 Cyclin E Human genes 0.000 claims 2
- 108090000257 Cyclin E Proteins 0.000 claims 2
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 claims 2
- 102100036239 Cyclin-dependent kinase 2 Human genes 0.000 claims 2
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims 2
- 230000005778 DNA damage Effects 0.000 claims 2
- 231100000277 DNA damage Toxicity 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
- 102100028138 F-box/WD repeat-containing protein 7 Human genes 0.000 claims 2
- 101710113436 GTPase KRas Proteins 0.000 claims 2
- 102100039788 GTPase NRas Human genes 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 2
- 101001060231 Homo sapiens F-box/WD repeat-containing protein 7 Proteins 0.000 claims 2
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 2
- 208000018142 Leiomyosarcoma Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 102000043276 Oncogene Human genes 0.000 claims 2
- 108700020796 Oncogene Proteins 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 2
- 241001655322 Streptomycetales Species 0.000 claims 2
- 206010043276 Teratoma Diseases 0.000 claims 2
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 2
- 208000008383 Wilms tumor Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 2
- 239000003242 anti bacterial agent Substances 0.000 claims 2
- 150000001541 aziridines Chemical class 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 230000003034 chemosensitisation Effects 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 210000001072 colon Anatomy 0.000 claims 2
- 208000002445 cystadenocarcinoma Diseases 0.000 claims 2
- 229960000684 cytarabine Drugs 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 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 2
- 229960005277 gemcitabine Drugs 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 210000000936 intestine Anatomy 0.000 claims 2
- 201000010260 leiomyoma Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 206010027191 meningioma Diseases 0.000 claims 2
- 229960001428 mercaptopurine Drugs 0.000 claims 2
- 210000000214 mouth Anatomy 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- JMVPFKZRJBWAEK-UHFFFAOYSA-N n,n-dimethyloxan-2-amine Chemical group CN(C)C1CCCCO1 JMVPFKZRJBWAEK-UHFFFAOYSA-N 0.000 claims 2
- 230000017074 necrotic cell death Effects 0.000 claims 2
- QZGIWPZCWHMVQL-UIYAJPBUSA-N neocarzinostatin chromophore Chemical compound O1[C@H](C)[C@H](O)[C@H](O)[C@@H](NC)[C@H]1O[C@@H]1C/2=C/C#C[C@H]3O[C@@]3([C@@H]3OC(=O)OC3)C#CC\2=C[C@H]1OC(=O)C1=C(O)C=CC2=C(C)C=C(OC)C=C12 QZGIWPZCWHMVQL-UIYAJPBUSA-N 0.000 claims 2
- 201000008026 nephroblastoma Diseases 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 229960005079 pemetrexed Drugs 0.000 claims 2
- QOFFJEBXNKRSPX-ZDUSSCGKSA-N pemetrexed Chemical compound C1=N[C]2NC(N)=NC(=O)C2=C1CCC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QOFFJEBXNKRSPX-ZDUSSCGKSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229960005235 piperonyl butoxide Drugs 0.000 claims 2
- 125000004591 piperonyl group Chemical group C(C1=CC=2OCOC2C=C1)* 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 239000002534 radiation-sensitizing agent Substances 0.000 claims 2
- 230000000113 radiomimetic effect Effects 0.000 claims 2
- 238000001959 radiotherapy Methods 0.000 claims 2
- 230000028617 response to DNA damage stimulus Effects 0.000 claims 2
- 230000035945 sensitivity Effects 0.000 claims 2
- 238000009097 single-agent therapy Methods 0.000 claims 2
- 230000004936 stimulating effect Effects 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 150000004654 triazenes Chemical class 0.000 claims 2
- 229950009268 zinostatin Drugs 0.000 claims 2
- FPVKHBSQESCIEP-UHFFFAOYSA-N (8S)-3-(2-deoxy-beta-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol Natural products C1C(O)C(CO)OC1N1C(NC=NCC2O)=C2N=C1 FPVKHBSQESCIEP-UHFFFAOYSA-N 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims 1
- POXWDTQUDZUOGP-UHFFFAOYSA-N 1h-1,4-diazepine Chemical compound N1C=CC=NC=C1 POXWDTQUDZUOGP-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
- AOJJSUZBOXZQNB-VTZDEGQISA-N 4'-epidoxorubicin 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-VTZDEGQISA-N 0.000 claims 1
- TVZGACDUOSZQKY-LBPRGKRZSA-N 4-aminofolic acid Chemical group 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
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- IDPUKCWIGUEADI-UHFFFAOYSA-N 5-[bis(2-chloroethyl)amino]uracil Chemical compound ClCCN(CCCl)C1=CNC(=O)NC1=O IDPUKCWIGUEADI-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
- 208000003200 Adenoma Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 108010006654 Bleomycin Proteins 0.000 claims 1
- 208000008720 Bone Marrow Neoplasms Diseases 0.000 claims 1
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims 1
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims 1
- 208000009458 Carcinoma in Situ Diseases 0.000 claims 1
- 206010008263 Cervical dysplasia Diseases 0.000 claims 1
- 208000010126 Chondromatosis Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 201000009047 Chordoma Diseases 0.000 claims 1
- 208000006332 Choriocarcinoma Diseases 0.000 claims 1
- 206010048832 Colon adenoma Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims 1
- 108010092160 Dactinomycin Proteins 0.000 claims 1
- 208000000471 Dysplastic Nevus Syndrome Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 206010014967 Ependymoma Diseases 0.000 claims 1
- HTIJFSOGRVMCQR-UHFFFAOYSA-N Epirubicin Natural products COc1cccc2C(=O)c3c(O)c4CC(O)(CC(OC5CC(N)C(=O)C(C)O5)c4c(O)c3C(=O)c12)C(=O)CO HTIJFSOGRVMCQR-UHFFFAOYSA-N 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 1
- 206010073153 Familial medullary thyroid cancer Diseases 0.000 claims 1
- 208000007659 Fibroadenoma Diseases 0.000 claims 1
- 206010053717 Fibrous histiocytoma Diseases 0.000 claims 1
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 1
- 208000000527 Germinoma Diseases 0.000 claims 1
- 208000007569 Giant Cell Tumors Diseases 0.000 claims 1
- 201000005409 Gliomatosis cerebri Diseases 0.000 claims 1
- 206010018691 Granuloma Diseases 0.000 claims 1
- 208000005234 Granulosa Cell Tumor Diseases 0.000 claims 1
- 208000002927 Hamartoma Diseases 0.000 claims 1
- 206010019629 Hepatic adenoma Diseases 0.000 claims 1
- XDXDZDZNSLXDNA-TZNDIEGXSA-N Idarubicin 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=CC=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XDXDZDZNSLXDNA-TZNDIEGXSA-N 0.000 claims 1
- XDXDZDZNSLXDNA-UHFFFAOYSA-N Idarubicin Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XDXDZDZNSLXDNA-UHFFFAOYSA-N 0.000 claims 1
- 208000002260 Keloid Diseases 0.000 claims 1
- 206010023347 Keratoacanthoma Diseases 0.000 claims 1
- 208000002404 Liver Cell Adenoma Diseases 0.000 claims 1
- GQYIWUVLTXOXAJ-UHFFFAOYSA-N Lomustine Chemical compound ClCCN(N=O)C(=O)NC1CCCCC1 GQYIWUVLTXOXAJ-UHFFFAOYSA-N 0.000 claims 1
- 208000006644 Malignant Fibrous Histiocytoma Diseases 0.000 claims 1
- 208000037196 Medullary thyroid carcinoma Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- VFKZTMPDYBFSTM-KVTDHHQDSA-N Mitobronitol Chemical compound BrC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CBr VFKZTMPDYBFSTM-KVTDHHQDSA-N 0.000 claims 1
- 229930192392 Mitomycin Natural products 0.000 claims 1
- 206010073148 Multiple endocrine neoplasia type 2A Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 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 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 201000004404 Neurofibroma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010031149 Osteitis Diseases 0.000 claims 1
- 208000000035 Osteochondroma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 1
- 206010061332 Paraganglion neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 208000005678 Rhabdomyoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
- IVTVGDXNLFLDRM-HNNXBMFYSA-N Tomudex Chemical compound C=1C=C2NC(C)=NC(=O)C2=CC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)S1 IVTVGDXNLFLDRM-HNNXBMFYSA-N 0.000 claims 1
- 190014017283 Triplatin Tetranitrate Chemical compound 0.000 claims 1
- 208000015778 Undifferentiated pleomorphic sarcoma Diseases 0.000 claims 1
- 206010048214 Xanthoma Diseases 0.000 claims 1
- 206010048215 Xanthomatosis Diseases 0.000 claims 1
- XSMVECZRZBFTIZ-UHFFFAOYSA-M [2-(aminomethyl)cyclobutyl]methanamine;2-oxidopropanoate;platinum(4+) Chemical compound [Pt+4].CC([O-])C([O-])=O.NCC1CCC1CN XSMVECZRZBFTIZ-UHFFFAOYSA-M 0.000 claims 1
- 229930183665 actinomycin Natural products 0.000 claims 1
- 208000002718 adenomatoid tumor Diseases 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 229960000473 altretamine Drugs 0.000 claims 1
- 229960003896 aminopterin Drugs 0.000 claims 1
- 229940045719 antineoplastic alkylating agent nitrosoureas Drugs 0.000 claims 1
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 claims 1
- LNHWXBUNXOXMRL-VWLOTQADSA-N belotecan Chemical compound C1=CC=C2C(CCNC(C)C)=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 LNHWXBUNXOXMRL-VWLOTQADSA-N 0.000 claims 1
- 229950011276 belotecan Drugs 0.000 claims 1
- 229960002707 bendamustine Drugs 0.000 claims 1
- YTKUWDBFDASYHO-UHFFFAOYSA-N bendamustine Chemical compound ClCCN(CCCl)C1=CC=C2N(C)C(CCCC(O)=O)=NC2=C1 YTKUWDBFDASYHO-UHFFFAOYSA-N 0.000 claims 1
- 208000001119 benign fibrous histiocytoma Diseases 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 210000000013 bile duct Anatomy 0.000 claims 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 1
- 229960001561 bleomycin Drugs 0.000 claims 1
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 208000018339 bone inflammation disease Diseases 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 201000006491 bone marrow cancer Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 201000003149 breast fibroadenoma Diseases 0.000 claims 1
- 208000003362 bronchogenic carcinoma Diseases 0.000 claims 1
- 201000002143 bronchus adenoma Diseases 0.000 claims 1
- 229960004117 capecitabine Drugs 0.000 claims 1
- 208000002458 carcinoid tumor Diseases 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 208000019065 cervical carcinoma Diseases 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 229960004630 chlorambucil Drugs 0.000 claims 1
- JCKYGMPEJWAADB-UHFFFAOYSA-N chlorambucil Chemical compound OC(=O)CCCC1=CC=C(N(CCCl)CCCl)C=C1 JCKYGMPEJWAADB-UHFFFAOYSA-N 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 229960000928 clofarabine Drugs 0.000 claims 1
- WDDPHFBMKLOVOX-AYQXTPAHSA-N clofarabine Chemical compound C1=NC=2C(N)=NC(Cl)=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@@H]1F WDDPHFBMKLOVOX-AYQXTPAHSA-N 0.000 claims 1
- 201000010305 cutaneous fibrous histiocytoma Diseases 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 208000035255 cutaneous malignant susceptibility to 2 melanoma Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- PZAQDVNYNJBUTM-UHFFFAOYSA-L cyclohexane-1,2-diamine;7,7-dimethyloctanoate;platinum(2+) Chemical compound [Pt+2].NC1CCCCC1N.CC(C)(C)CCCCCC([O-])=O.CC(C)(C)CCCCCC([O-])=O PZAQDVNYNJBUTM-UHFFFAOYSA-L 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 229960004397 cyclophosphamide Drugs 0.000 claims 1
- 229960003901 dacarbazine Drugs 0.000 claims 1
- 229960000975 daunorubicin 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
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 201000009409 embryonal rhabdomyosarcoma Diseases 0.000 claims 1
- 229960001904 epirubicin Drugs 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 201000003115 germ cell cancer Diseases 0.000 claims 1
- 208000006359 hepatoblastoma Diseases 0.000 claims 1
- 201000002735 hepatocellular adenoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- UUVWYPNAQBNQJQ-UHFFFAOYSA-N hexamethylmelamine Chemical compound CN(C)C1=NC(N(C)C)=NC(N(C)C)=N1 UUVWYPNAQBNQJQ-UHFFFAOYSA-N 0.000 claims 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims 1
- 229960000908 idarubicin Drugs 0.000 claims 1
- 229960001101 ifosfamide Drugs 0.000 claims 1
- HOMGKSMUEGBAAB-UHFFFAOYSA-N ifosfamide Chemical compound ClCCNP1(=O)OCCCN1CCCl HOMGKSMUEGBAAB-UHFFFAOYSA-N 0.000 claims 1
- 201000004933 in situ carcinoma Diseases 0.000 claims 1
- 206010022498 insulinoma Diseases 0.000 claims 1
- 210000001117 keloid Anatomy 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000022013 kidney Wilms tumor Diseases 0.000 claims 1
- 201000003445 large cell neuroendocrine carcinoma Diseases 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 210000002332 leydig cell Anatomy 0.000 claims 1
- 210000000088 lip Anatomy 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 229950008991 lobaplatin Drugs 0.000 claims 1
- 229960002247 lomustine Drugs 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 229960004961 mechlorethamine Drugs 0.000 claims 1
- HAWPXGHAZFHHAD-UHFFFAOYSA-N mechlorethamine Chemical group ClCCN(C)CCCl HAWPXGHAZFHHAD-UHFFFAOYSA-N 0.000 claims 1
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims 1
- 229960001924 melphalan Drugs 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
- 210000002418 meninge Anatomy 0.000 claims 1
- 229960005485 mitobronitol Drugs 0.000 claims 1
- 229960004857 mitomycin Drugs 0.000 claims 1
- 206010051747 multiple endocrine neoplasia Diseases 0.000 claims 1
- 208000009091 myxoma Diseases 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 201000004662 neurofibroma of spinal cord Diseases 0.000 claims 1
- 208000008798 osteoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000003101 oviduct Anatomy 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 208000021255 pancreatic insulinoma Diseases 0.000 claims 1
- 208000007312 paraganglioma Diseases 0.000 claims 1
- FPVKHBSQESCIEP-JQCXWYLXSA-N pentostatin Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(N=CNC[C@H]2O)=C2N=C1 FPVKHBSQESCIEP-JQCXWYLXSA-N 0.000 claims 1
- 229960002340 pentostatin Drugs 0.000 claims 1
- 210000003800 pharynx Anatomy 0.000 claims 1
- 208000028591 pheochromocytoma Diseases 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 229950005566 picoplatin Drugs 0.000 claims 1
- IIMIOEBMYPRQGU-UHFFFAOYSA-L picoplatin Chemical compound N.[Cl-].[Cl-].[Pt+2].CC1=CC=CC=N1 IIMIOEBMYPRQGU-UHFFFAOYSA-L 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 229960004432 raltitrexed Drugs 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 201000010174 renal carcinoma Diseases 0.000 claims 1
- 201000006845 reticulosarcoma Diseases 0.000 claims 1
- 208000029922 reticulum cell sarcoma Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 210000003625 skull Anatomy 0.000 claims 1
- 208000000649 small cell carcinoma Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 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
- 229960004964 temozolomide Drugs 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
- 208000001608 teratocarcinoma Diseases 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
- 210000001550 testis Anatomy 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 208000013818 thyroid gland medullary carcinoma Diseases 0.000 claims 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 1
- 210000002105 tongue Anatomy 0.000 claims 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 229950001353 tretamine Drugs 0.000 claims 1
- IUCJMVBFZDHPDX-UHFFFAOYSA-N tretamine Chemical compound C1CN1C1=NC(N2CC2)=NC(N2CC2)=N1 IUCJMVBFZDHPDX-UHFFFAOYSA-N 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 229950002860 triplatin tetranitrate Drugs 0.000 claims 1
- 229960000875 trofosfamide Drugs 0.000 claims 1
- UMKFEPPTGMDVMI-UHFFFAOYSA-N trofosfamide Chemical compound ClCCN(CCCl)P1(=O)OCCCN1CCCl UMKFEPPTGMDVMI-UHFFFAOYSA-N 0.000 claims 1
- 208000022271 tubular adenoma Diseases 0.000 claims 1
- 210000004881 tumor cell Anatomy 0.000 claims 1
- 229960001055 uracil mustard Drugs 0.000 claims 1
- 210000003708 urethra Anatomy 0.000 claims 1
- 210000002229 urogenital system Anatomy 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
- 210000001215 vagina Anatomy 0.000 claims 1
- 210000003905 vulva Anatomy 0.000 claims 1
- 229960000641 zorubicin Drugs 0.000 claims 1
- FBTUMDXHSRTGRV-ALTNURHMSA-N zorubicin 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)=N\NC(=O)C=1C=CC=CC=1)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 FBTUMDXHSRTGRV-ALTNURHMSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/4965—Non-condensed pyrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
- C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
-
- 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
-
- 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
- C07D401/10—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 linked by a carbon chain containing aromatic rings
-
- 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
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S507/00—Earth boring, well treating, and oil field chemistry
- Y10S507/939—Corrosion inhibitor
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (12)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13942008P | 2008-12-19 | 2008-12-19 | |
US13942608P | 2008-12-19 | 2008-12-19 | |
US13942408P | 2008-12-19 | 2008-12-19 | |
US13942908P | 2008-12-19 | 2008-12-19 | |
US61/139,424 | 2008-12-19 | ||
US61/139,426 | 2008-12-19 | ||
US61/139,420 | 2008-12-19 | ||
US61/139,429 | 2008-12-19 | ||
US18179409P | 2009-05-28 | 2009-05-28 | |
US61/181,794 | 2009-05-28 | ||
US21910009P | 2009-06-22 | 2009-06-22 | |
US61/219,100 | 2009-06-22 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2011129761/04A Division RU2604066C2 (ru) | 2008-12-19 | 2009-12-18 | Производные пиразина, используемые в качестве ингибиторов киназы atr |
Publications (2)
Publication Number | Publication Date |
---|---|
RU2016141566A true RU2016141566A (ru) | 2018-12-20 |
RU2016141566A3 RU2016141566A3 (forum.php) | 2020-02-17 |
Family
ID=41683104
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2016141566A RU2016141566A (ru) | 2008-12-19 | 2009-12-18 | Производные пиразина, используемые в качестве ингибиторов киназы atr |
RU2011129761/04A RU2604066C2 (ru) | 2008-12-19 | 2009-12-18 | Производные пиразина, используемые в качестве ингибиторов киназы atr |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2011129761/04A RU2604066C2 (ru) | 2008-12-19 | 2009-12-18 | Производные пиразина, используемые в качестве ингибиторов киназы atr |
Country Status (29)
Country | Link |
---|---|
US (7) | US8841308B2 (forum.php) |
EP (3) | EP2376485B1 (forum.php) |
JP (5) | JP5753093B2 (forum.php) |
KR (3) | KR101958632B1 (forum.php) |
CN (4) | CN106518856B (forum.php) |
AR (1) | AR074822A1 (forum.php) |
AU (3) | AU2009327357C1 (forum.php) |
BR (1) | BRPI0924084B1 (forum.php) |
CA (2) | CA2747252C (forum.php) |
CY (1) | CY1120002T1 (forum.php) |
DK (2) | DK3354650T3 (forum.php) |
ES (2) | ES2921576T3 (forum.php) |
HR (2) | HRP20180385T1 (forum.php) |
HU (1) | HUE036068T2 (forum.php) |
IL (3) | IL213613A (forum.php) |
LT (2) | LT2376485T (forum.php) |
MX (1) | MX2011006503A (forum.php) |
NO (1) | NO2376485T3 (forum.php) |
NZ (1) | NZ593969A (forum.php) |
PL (2) | PL2376485T3 (forum.php) |
PT (2) | PT3354650T (forum.php) |
RS (1) | RS56995B1 (forum.php) |
RU (2) | RU2016141566A (forum.php) |
SG (2) | SG10201607592PA (forum.php) |
SI (2) | SI2376485T1 (forum.php) |
SM (1) | SMT201800181T1 (forum.php) |
TW (3) | TWI478918B (forum.php) |
WO (1) | WO2010071837A1 (forum.php) |
ZA (1) | ZA201104498B (forum.php) |
Families Citing this family (92)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102264721B (zh) | 2008-11-10 | 2015-12-09 | 沃泰克斯药物股份有限公司 | 用作atr激酶抑制剂的化合物 |
PL2376485T3 (pl) | 2008-12-19 | 2018-05-30 | Vertex Pharmaceuticals Incorporated | Pochodne pirazyny użyteczne jako inhibitory kinazy ATR |
US8415381B2 (en) | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
JP2011057661A (ja) * | 2009-08-14 | 2011-03-24 | Bayer Cropscience Ag | 殺虫性カルボキサミド類 |
JP2013526538A (ja) | 2010-05-12 | 2013-06-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ阻害剤として有用な化合物 |
CA2798760A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as inhibitors of atr kinase |
WO2011143425A2 (en) * | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8962631B2 (en) | 2010-05-12 | 2015-02-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
WO2011143426A1 (en) * | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US9062008B2 (en) | 2010-05-12 | 2015-06-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
CA2803802A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
US8962623B2 (en) | 2011-03-04 | 2015-02-24 | Locus Pharmaceuticals, Inc. | Aminopyrazine compounds |
EP2686314A1 (en) | 2011-03-16 | 2014-01-22 | F.Hoffmann-La Roche Ag | 6,5-heterocyclic propargylic alcohol compounds and uses therefor |
JP2014510151A (ja) | 2011-04-05 | 2014-04-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ(trakinase)阻害剤として有用なアミノピラジン化合物 |
EA023364B1 (ru) * | 2011-05-23 | 2016-05-31 | Мерк Патент Гмбх | Производные пиридина и пиразина |
WO2012178125A1 (en) * | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
EP2723747A1 (en) * | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
WO2012178123A1 (en) * | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
WO2013038386A1 (en) * | 2011-09-16 | 2013-03-21 | Novartis Ag | Heterocyclic compounds for the treatment of cystic fibrosis |
EP2755652B1 (en) | 2011-09-16 | 2021-06-02 | Novartis AG | N-substituted heterocyclyl carboxamides |
CN103958507A (zh) * | 2011-09-30 | 2014-07-30 | 沃泰克斯药物股份有限公司 | 可用作atr激酶抑制剂的化合物 |
US8853217B2 (en) * | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
JP6162126B2 (ja) * | 2011-09-30 | 2017-08-23 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atr阻害剤による膵臓癌及び非小細胞肺癌の治療 |
EP2751097A2 (en) * | 2011-09-30 | 2014-07-09 | Vertex Pharmaceuticals Incorporated | Processes for making compounds useful as inhibitors of atr kinase |
US8765751B2 (en) | 2011-09-30 | 2014-07-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EP2776421A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
WO2013071090A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8846918B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
WO2013071085A1 (en) * | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
ES2654670T3 (es) | 2012-04-05 | 2018-02-14 | Vertex Pharmaceuticals Incorporated | Compuestos útiles como inhibidores de la cinasa ATR y terapias de combinación de los mismos |
UA115983C2 (uk) | 2012-04-24 | 2018-01-25 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори днк-пк |
US8999632B2 (en) | 2012-10-04 | 2015-04-07 | Vertex Pharmaceuticals Incorporated | Method for measuring ATR inhibition mediated increases in DNA damage |
EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
DK3486245T3 (da) | 2012-12-07 | 2021-07-19 | Vertex Pharma | 2-amino-n-(piperidin-1-yl-pyridin-3-yl) pyrazolo[1,5alpha]pyrimidin-3-carboxamid som hæmmer for atr kinase |
ES2637170T3 (es) * | 2013-01-02 | 2017-10-11 | H. Lundbeck A/S | Compuestos derivados de aminopiridina como inhibidores de LRRK2 |
MX361136B (es) | 2013-01-23 | 2018-11-28 | Astrazeneca Ab | Compuestos quimicos. |
SG11201507203RA (en) | 2013-03-12 | 2015-10-29 | Vertex Pharma | Dna-pk inhibitors |
US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
WO2014143240A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
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 |
SG11201604519PA (en) | 2013-12-06 | 2016-07-28 | Vertex Pharma | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
CN103804312B (zh) * | 2014-02-17 | 2016-04-20 | 四川百利药业有限责任公司 | 一类氮杂环化合物及其制备方法和用途 |
PL3134396T3 (pl) | 2014-04-24 | 2020-04-30 | Novartis Ag | Pochodne aminopirydyny jako inhibitory 3-kinazy fosfatydyloinozytolu |
US9862711B2 (en) | 2014-04-24 | 2018-01-09 | Novartis Ag | Pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors |
BR112016024533A8 (pt) * | 2014-04-24 | 2021-03-30 | Novartis Ag | derivados de amino pirazina como inibidores de fosfatidilinositol 3-cinase ou sal, seu uso, e composição e combinação farmacêuticas |
WO2015187451A1 (en) | 2014-06-05 | 2015-12-10 | Vertex Pharmacetucals Incorporated | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
SG10201811175WA (en) | 2014-06-17 | 2019-01-30 | Vertex Pharma | Method for treating cancer using a combination of chk1 and atr inhibitors |
TWI656121B (zh) | 2014-08-04 | 2019-04-11 | 德商拜耳製藥公司 | 2-(嗎啉-4-基)-1,7-萘啶 |
JO3589B1 (ar) | 2014-08-06 | 2020-07-05 | Novartis Ag | مثبطات كيناز البروتين c وطرق استخداماتها |
UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
KR102569226B1 (ko) * | 2014-10-13 | 2023-08-22 | 아트린 파마슈티컬스 엘엘씨 | 운동실조 모세혈관확장증 및 Rad3-관련 (ATR) 단백질 키나제 억제제 |
KR102678021B1 (ko) | 2015-09-30 | 2024-06-26 | 버텍스 파마슈티칼스 인코포레이티드 | Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물 |
EP3936153B1 (en) | 2016-01-11 | 2024-08-21 | Celator Pharmaceuticals, Inc. | Inhibiting ataxia telangiectasia and rad3-related protein (atr) |
WO2018029117A1 (en) | 2016-08-10 | 2018-02-15 | Rheinisch-Westfälische Technische Hochschule Aachen (RWTH) | New atr inhibitors for the use in cancer therapy |
US11730734B2 (en) * | 2016-09-12 | 2023-08-22 | University Of Florida Research Foundation, Incorporated | Use of ATR and Chk1 inhibitor compounds |
CN109715163B (zh) | 2016-09-19 | 2022-11-22 | 诺华股份有限公司 | 包含raf抑制剂和erk抑制剂的治疗组合 |
TW201815418A (zh) | 2016-09-27 | 2018-05-01 | Vertex Pharma | 使用dna破壞劑及dna-pk抑制劑之組合治療癌症的方法 |
EA039513B1 (ru) * | 2017-01-09 | 2022-02-04 | Селатор Фармасьютикалз, Инк. | Ингибитор атаксии-телеангиэкстазии и rad3-родственного белка (atr) и содержащие его липосомные композиции |
JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
WO2018153969A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with radium-223 salt |
WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
WO2018187479A1 (en) | 2017-04-04 | 2018-10-11 | Case Western Reserve University | Method of modulating ribonucleotide reductase |
RS64364B1 (sr) | 2017-04-27 | 2023-08-31 | Ishihara Sangyo Kaisha | Jedinjenje n-(4-piridil) nikotinamida ili njegova so |
IL270224B1 (en) | 2017-05-02 | 2024-04-01 | Novartis Ag | Combination therapy employing trametinib and a defined raf inhibitor |
WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
EP3661560B1 (en) | 2017-08-04 | 2025-02-26 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and pd-1/pd-l1 inhibitors |
GB201715410D0 (en) | 2017-09-22 | 2017-11-08 | Syngenta Participations Ag | Improvements in or relating to organic compounds |
EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
US11712440B2 (en) | 2017-12-08 | 2023-08-01 | Bayer Aktiengesellschaft | Predictive markers for ATR kinase inhibitors |
US11306079B2 (en) | 2017-12-21 | 2022-04-19 | Incyte Corporation | 3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as PI3K-gamma kinase inhibitors |
AU2018397736A1 (en) * | 2017-12-29 | 2020-07-09 | Vertex Pharmaceuticals Incorporated | Methods of cancer treatment using an ATR inhibitor |
CA3093445A1 (en) | 2018-03-08 | 2019-11-28 | Incyte Corporation | Aminopyrazine diol compounds as pi3k-.gamma. inhibitors |
US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
KR20210066837A (ko) | 2018-09-26 | 2021-06-07 | 메르크 파텐트 게엠베하 | 암 치료를 위한 pd-1 안타고니스트, atr 억제제 및 백금화제의 조합 |
US20210369705A1 (en) | 2018-10-15 | 2021-12-02 | Merck Patent Gmbh | Combination therapy utilizing dna alkylating agents and atr inhibitors |
EP3866805A1 (en) | 2018-10-16 | 2021-08-25 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
CA3118218A1 (en) | 2018-10-30 | 2020-05-07 | Repare Therapeutics Inc. | Compounds, pharmaceutical compositions, and methods of preparing compounds and of their use as atr kinase inhibitors |
CA3138123A1 (en) | 2019-05-13 | 2020-11-19 | Novartis Ag | New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer |
CN115916966A (zh) * | 2020-01-30 | 2023-04-04 | 加利福尼亚大学董事会 | Strad结合剂及其用途 |
WO2022063869A2 (en) * | 2020-09-24 | 2022-03-31 | Merck Patent Gmbh | Compounds for the treatment of viral infections |
WO2022090063A1 (en) | 2020-10-26 | 2022-05-05 | Merck Patent Gmbh | Atr inhibitors for use in the treatment of viral infections |
US20250026742A1 (en) * | 2021-08-13 | 2025-01-23 | Suzhou Ark Biopharmaceutical Co., Ltd. | Compound as atr kinase inhibitor |
CN115703768B (zh) * | 2021-08-13 | 2024-12-17 | 苏州爱科百发生物医药技术有限公司 | 用作atr激酶抑制剂的化合物 |
CA3181279A1 (en) * | 2022-03-24 | 2023-09-24 | Bloom Energy Corporation | Fuel cell stack assembly including heat sink inserts |
KR20250023494A (ko) | 2022-06-15 | 2025-02-18 | 아스트라제네카 아베 | 암 치료를 위한 병용 요법 |
CN118255760A (zh) * | 2022-12-27 | 2024-06-28 | 江苏亚虹医药科技股份有限公司 | 一种嘧啶类化合物及其制备方法和医药用途 |
AR131690A1 (es) * | 2023-01-30 | 2025-04-23 | Eurofarma Laboratorios S A | COMPUESTOS FENÓLICOS BLOQUEADORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, SUS COMPOSICIONES, SUS USOS, LOS MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y LOS KITS |
CN116655619A (zh) * | 2023-06-05 | 2023-08-29 | 南京康立凯医药科技有限公司 | 一种2h-吲唑类化合物及其制备方法和应用 |
CN117024413B (zh) * | 2023-10-07 | 2024-01-09 | 天津匠新致成科技有限公司 | 3-氨基吡嗪-2-甲酰胺类靶向蛋白水解嵌合体及其制备方法、药物组合物和应用 |
WO2025181153A1 (en) | 2024-03-01 | 2025-09-04 | F. Hoffmann-La Roche Ag | Use of atr inhibitors in combination with pi3k alpha inhibitors |
CN120097926A (zh) * | 2025-03-07 | 2025-06-06 | 杭州师范大学 | 一种选择性hpk1抑制剂及其制备方法和应用 |
Family Cites Families (226)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4309430A (en) | 1980-06-27 | 1982-01-05 | Merck & Co., Inc. | Pyrazinyl-1,2,4-oxadiazole-5-ones, for treatment of edema, and processes for preparing same |
JPS62270623A (ja) | 1985-12-07 | 1987-11-25 | Daicel Chem Ind Ltd | ビス(4−アミノフエニル)ピラジンおよびその製法、ならびにポリイミドおよびその製法 |
JPS63208520A (ja) | 1987-02-26 | 1988-08-30 | Terumo Corp | ピラジン誘導体を含有する血小板凝集抑制剤 |
US5329012A (en) | 1987-10-29 | 1994-07-12 | The Research Foundation Of State University Of New York | Bis(acyloxmethyl)imidazole compounds |
JPH0272372A (ja) | 1988-09-07 | 1990-03-12 | Konica Corp | 電子写真感光体 |
JPH0272370A (ja) | 1988-09-07 | 1990-03-12 | Konica Corp | 電子写真感光体 |
JPH0374370A (ja) | 1989-08-16 | 1991-03-28 | Terumo Corp | ピラジン誘導体およびこれを含有する血小板凝集抑制剤または抗炎症剤 |
JP2597917B2 (ja) | 1990-04-26 | 1997-04-09 | 富士写真フイルム株式会社 | 新規な色素形成カプラー及びそれを用いたハロゲン化銀カラー写真感光材料 |
US5572248A (en) | 1994-09-19 | 1996-11-05 | Teleport Corporation | Teleconferencing method and system for providing face-to-face, non-animated teleconference environment |
CA2253910A1 (en) | 1996-05-11 | 1997-11-20 | King's College London | Pyrazines |
JP4026876B2 (ja) | 1996-09-05 | 2007-12-26 | 日本食品化工株式会社 | 発光性シクロデキストリン誘導体及びその製造方法 |
JP2002241379A (ja) | 1997-03-21 | 2002-08-28 | Dainippon Pharmaceut Co Ltd | 3−オキサジアゾリルキノキサリン誘導体 |
WO1999044609A1 (en) | 1998-03-03 | 1999-09-10 | Merck & Co., Inc. | FUSED PIPERIDINE SUBSTITUTED ARYLSULFONAMIDES AS β3-AGONISTS |
DE19826671A1 (de) | 1998-06-16 | 1999-12-23 | Hoechst Schering Agrevo Gmbh | 1,3-Oxazolin- und 1,3-Thiazolin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel |
EP1097933A4 (en) | 1998-07-16 | 2001-11-07 | Shionogi & Co | PYRIMIDINE DERIVATIVES HAVING ANTI-TUMOR ACTIVITY |
US7023913B1 (en) | 2000-06-14 | 2006-04-04 | Monroe David A | Digital security multimedia sensor |
PT1150999E (pt) | 1999-02-05 | 2006-10-31 | Debiopharm Sa | Derivados da ciclosporina em que a sequencia peptidica contem pelo menos um aminoacido nao natural do tipo pseudo-prolina e metodo para preparacao dos mesmos |
US6738073B2 (en) | 1999-05-12 | 2004-05-18 | Imove, Inc. | Camera system with both a wide angle view and a high resolution view |
CA2412345A1 (en) | 1999-06-16 | 2000-12-21 | University Of Iowa Research Foundation | Antagonism of immunostimulatory cpg-oligonucleotides by 4-aminoquinolines and other weak bases |
US7015954B1 (en) | 1999-08-09 | 2006-03-21 | Fuji Xerox Co., Ltd. | Automatic video system using multiple cameras |
US6660753B2 (en) | 1999-08-19 | 2003-12-09 | Nps Pharmaceuticals, Inc. | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
EP1237880B1 (en) | 1999-12-17 | 2008-01-23 | Novartis Vaccines and Diagnostics, Inc. | Pyrazine based inhibitors of glycogen synthase kinase 3 |
AR029489A1 (es) | 2000-03-10 | 2003-07-02 | Euro Celtique Sa | Piridinas, pirimidinas, pirazinas, triazinas sustituidas por arilo, composiciones farmaceuticas y el uso de las mismas para la manufactura de un medicamento |
US6849660B1 (en) | 2000-08-01 | 2005-02-01 | Isis Pharmaceuticals, Inc. | Antimicrobial biaryl compounds |
JP2002072370A (ja) | 2000-08-29 | 2002-03-12 | Fuji Photo Optical Co Ltd | ペーパーマガジン及び写真焼付装置 |
JP2002072372A (ja) | 2000-09-04 | 2002-03-12 | Fuji Photo Film Co Ltd | 画像形成用シート体の切断装置 |
US6829391B2 (en) | 2000-09-08 | 2004-12-07 | Siemens Corporate Research, Inc. | Adaptive resolution system and method for providing efficient low bit rate transmission of image data for distributed applications |
EP1217000A1 (en) | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
KR100884877B1 (ko) | 2000-12-28 | 2009-02-23 | 다이이찌 세이야꾸 가부시기가이샤 | Vla-4 저해제 |
US8085293B2 (en) | 2001-03-14 | 2011-12-27 | Koninklijke Philips Electronics N.V. | Self adjusting stereo camera system |
US6759657B2 (en) | 2001-03-27 | 2004-07-06 | Kabushiki Kaisha Toshiba | Infrared sensor |
JPWO2002080899A1 (ja) | 2001-03-30 | 2005-01-06 | エーザイ株式会社 | 消化器疾患治療剤 |
US6469002B1 (en) | 2001-04-19 | 2002-10-22 | Millennium Pharmaceuticals, Inc. | Imidazolidine compounds |
DE60229059D1 (de) | 2001-05-08 | 2008-11-06 | Univ Yale | Proteomimetische verbindungen und verfahren |
SE0102438D0 (sv) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
SE0102439D0 (sv) * | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
JP2003074370A (ja) | 2001-09-05 | 2003-03-12 | Suzuki Motor Corp | エンジンのベルト保護装置 |
WO2003026572A2 (en) | 2001-09-26 | 2003-04-03 | Merck & Co., Inc. | Crystalline forms of ertapenem sodium |
GB0124939D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
US6992087B2 (en) | 2001-11-21 | 2006-01-31 | Pfizer Inc | Substituted aryl 1,4-pyrazine derivatives |
WO2003045924A1 (en) | 2001-11-21 | 2003-06-05 | Pharmacia & Upjohn Company | Substituted aryl 1,4-pyrazine derivatives |
US6693097B2 (en) | 2001-11-30 | 2004-02-17 | Synta Pharmaceuticals Corp. | Pyrimidine compounds |
US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
RU2004126671A (ru) | 2002-02-06 | 2005-04-10 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Гетероарилсоединения, полезные в качестве ингибиторов gsk-3 |
DE60320957D1 (en) | 2002-03-13 | 2008-06-26 | Janssen Pharmaceutica Nv | Sulfonylderivate als histone-deacetylase-inhibitoren |
GB0206860D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
US7043079B2 (en) | 2002-04-25 | 2006-05-09 | Microsoft Corporation | “Don't care” pixel interpolation |
GB0209715D0 (en) | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
US7704995B2 (en) * | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
EP1501514B1 (en) | 2002-05-03 | 2012-12-19 | Exelixis, Inc. | Protein kinase modulators and methods of use |
CN1656079A (zh) | 2002-05-31 | 2005-08-17 | 卫材株式会社 | 吡唑化合物和含有该化合物的药物组合物 |
WO2004000318A2 (en) | 2002-06-21 | 2003-12-31 | Cellular Genomics, Inc. | Certain amino-substituted monocycles as kinase modulators |
WO2004000820A2 (en) | 2002-06-21 | 2003-12-31 | Cellular Genomics, Inc. | Certain aromatic monocycles as kinase modulators |
AU2003282679A1 (en) | 2002-10-04 | 2004-05-04 | Arena Pharmaceuticals, Inc. | Hydroxypyrazoles for use against metabolic-related disorders |
US20040075741A1 (en) | 2002-10-17 | 2004-04-22 | Berkey Thomas F. | Multiple camera image multiplexer |
US7385626B2 (en) | 2002-10-21 | 2008-06-10 | Sarnoff Corporation | Method and system for performing surveillance |
US20040100560A1 (en) | 2002-11-22 | 2004-05-27 | Stavely Donald J. | Tracking digital zoom in a digital video camera |
SE0203754D0 (sv) | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
SE0203752D0 (sv) * | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
DK2476667T3 (da) | 2003-02-26 | 2014-09-15 | Sugen Inc | Aminoheteroaryl-forbindelser som proteinkinase-inhibitorer |
US7684624B2 (en) | 2003-03-03 | 2010-03-23 | Smart Technologies Ulc | System and method for capturing images of a target area on which information is recorded |
ES2308151T3 (es) | 2003-03-11 | 2008-12-01 | Pfizer Products Inc. | Compuestos de pirazina como inhibidores del factor de crecimiento transformante (tgf). |
EP1606266A4 (en) | 2003-03-21 | 2008-06-25 | Smithkline Beecham Corp | CHEMICAL COMPOUNDS |
AU2004224392A1 (en) | 2003-03-24 | 2004-10-07 | Merck & Co., Inc. | Biaryl substituted 6-membered heterocyles as sodium channel blockers |
GB2400101A (en) | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
GB2400514B (en) | 2003-04-11 | 2006-07-26 | Hewlett Packard Development Co | Image capture method |
EP1625123A4 (en) | 2003-05-15 | 2007-08-29 | Merck & Co Inc | 3- (2-AMINO-1-AZACYCLYL) -5-ARYL-1,2,4-OXADIAZOLE AS S1P RECEPTOR AGONISTS |
WO2004103991A1 (fr) | 2003-05-20 | 2004-12-02 | 'chemical Diversity Research Institute', Ltd. | Piperidines 2-substituees, bibliotheque focalisee et composition pharmaceutique |
US20050123902A1 (en) | 2003-05-21 | 2005-06-09 | President And Fellows Of Harvard College | Human papillomavirus inhibitors |
PE20050206A1 (es) | 2003-05-26 | 2005-03-26 | Schering Ag | Composicion farmaceutica que contiene un inhibidor de histona deacetilasa |
US7986339B2 (en) | 2003-06-12 | 2011-07-26 | Redflex Traffic Systems Pty Ltd | Automated traffic violation monitoring and reporting system with combined video and still-image data |
JP2005020227A (ja) | 2003-06-25 | 2005-01-20 | Pfu Ltd | 画像圧縮装置 |
AR045595A1 (es) | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
WO2005034952A2 (en) | 2003-10-07 | 2005-04-21 | The Feinstein Institute For Medical Research | Isoxazole and isothiazole compounds useful in the treatment of inflammation |
US20050116968A1 (en) | 2003-12-02 | 2005-06-02 | John Barrus | Multi-capability display |
WO2005058876A1 (en) | 2003-12-16 | 2005-06-30 | Gpc Biotech Ag | Pyrazine derivatives as effective compounds against infectious diseases |
AU2005215379A1 (en) | 2004-02-12 | 2005-09-01 | Merck & Co., Inc. | Bipyridyl amides as modulators of metabotropic glutamate receptor-5 |
US20050276765A1 (en) | 2004-06-10 | 2005-12-15 | Paul Nghiem | Preventing skin damage |
JP2008502687A (ja) | 2004-06-14 | 2008-01-31 | タケダ サン ディエゴ インコーポレイテッド | キナーゼ阻害剤 |
SG156685A1 (en) | 2004-07-27 | 2009-11-26 | Sgx Pharmaceuticals Inc | Fused ring heterocycle kinase modulators |
US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
ATE463486T1 (de) | 2004-08-26 | 2010-04-15 | Pfizer | Enantiomerenreine aminoheteroaryl-verbindungen als proteinkinasehemmer |
CA2578075A1 (en) * | 2004-08-26 | 2006-03-02 | Pfizer Inc. | Aminoheteroaryl compounds as protein tyrosine kinase inhibitors |
US7730406B2 (en) | 2004-10-20 | 2010-06-01 | Hewlett-Packard Development Company, L.P. | Image processing system and method |
CN101084208A (zh) | 2004-10-22 | 2007-12-05 | 詹森药业有限公司 | 作为c-fms激酶抑制剂的芳族酰胺 |
EP1828144A2 (en) | 2004-11-12 | 2007-09-05 | OSI Pharmaceuticals, Inc. | Integrin antagonists useful as anticancer agents |
CN101098872B (zh) | 2004-11-22 | 2012-09-05 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的吡咯并吡嗪和吡唑并吡嗪 |
JP4810669B2 (ja) | 2004-11-25 | 2011-11-09 | コニカミノルタホールディングス株式会社 | 有機エレクトロルミネッセンス素子、表示装置及び照明装置 |
GB0428235D0 (en) | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Novel compounds |
ZA200704959B (en) | 2004-12-27 | 2009-04-29 | Alcon Inc | Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases |
GB0500492D0 (en) | 2005-01-11 | 2005-02-16 | Cyclacel Ltd | Compound |
US7622583B2 (en) | 2005-01-14 | 2009-11-24 | Chemocentryx, Inc. | Heteroaryl sulfonamides and CCR2 |
GB0501999D0 (en) * | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
MX2007009945A (es) | 2005-02-16 | 2007-09-26 | Schering Corp | Piperazinas sustituidas con heterociclicos con actividad antagonista de cxcr3. |
AU2006239632B2 (en) | 2005-04-25 | 2012-03-15 | Merck Patent Gmbh | Novel AZA- heterocycles serving as kinase inhibitors |
WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
CA2610884A1 (en) | 2005-06-09 | 2006-12-21 | Merck & Co., Inc. | Inhibitors of checkpoint kinases |
US8153804B2 (en) | 2005-08-02 | 2012-04-10 | Lexicon Pharmaceuticals, Inc. | Aryl pyridines and methods of their use |
WO2007015632A1 (en) * | 2005-08-04 | 2007-02-08 | Cgk Co., Ltd. | Atm and atr inhibitor |
US7394926B2 (en) | 2005-09-30 | 2008-07-01 | Mitutoyo Corporation | Magnified machine vision user interface |
US7806604B2 (en) | 2005-10-20 | 2010-10-05 | Honeywell International Inc. | Face detection and tracking in a wide field of view |
TW200736260A (en) | 2005-11-10 | 2007-10-01 | Smithkline Beecham Corp | Inhibitors of Akt activity |
CA2630460C (en) | 2005-12-01 | 2013-01-08 | F. Hoffmann-La Roche Ag | Heteroaryl substituted piperidine derivatives as l-cpt1 inhibitors |
US7871982B2 (en) | 2005-12-09 | 2011-01-18 | Meiji Seika Kaisha, Ltd. | Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient |
EP1965645A2 (en) | 2005-12-14 | 2008-09-10 | E.I. Du Pont De Nemours And Company | Isoxazolines for controlling invertebrate pests |
CN101340912A (zh) | 2005-12-22 | 2009-01-07 | 爱尔康研究有限公司 | 用于治疗rho激酶介导的疾病和病状的(吲唑-5-基)-吡嗪和(1,3-二氢-吲哚-2-酮)-吡嗪 |
PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
ITMI20060311A1 (it) | 2006-02-21 | 2007-08-22 | Btsr Int Spa | Dispositivo perfezionato di alimentazione di filo o filatio ad una macchina tessile e metodo per attuare tale alimentazione |
GB0603684D0 (en) | 2006-02-23 | 2006-04-05 | Novartis Ag | Organic compounds |
WO2007096764A2 (en) | 2006-02-27 | 2007-08-30 | Glenmark Pharmaceuticals S.A. | Bicyclic heteroaryl derivatives as cannabinoid receptor modulators |
TW200800203A (en) | 2006-03-08 | 2008-01-01 | Astrazeneca Ab | New use |
CA2646701A1 (en) | 2006-03-22 | 2007-10-04 | Vertex Pharmaceuticals Incorporated | C-met protein kinase inhibitors for the treatment of proliferative disorders |
US7574131B2 (en) | 2006-03-29 | 2009-08-11 | Sunvision Scientific Inc. | Object detection system and method |
MX2008012658A (es) | 2006-03-31 | 2008-12-16 | Schering Corp | Inhibidores de cinasa. |
US7629346B2 (en) | 2006-06-19 | 2009-12-08 | Hoffmann-La Roche Inc. | Pyrazinecarboxamide derivatives as CB1 antagonists |
JP2009541323A (ja) | 2006-06-22 | 2009-11-26 | マリンクロット インコーポレイテッド | 拡張された共役を有するピラジン誘導体およびその使用 |
CA2654358A1 (en) | 2006-06-22 | 2007-12-27 | Biovitrum Ab (Publ) | Pyridine and pyrazine derivatives as mnk kinase inhibitors |
EP1900727A1 (en) | 2006-08-30 | 2008-03-19 | Cellzome Ag | Aminopyridine derivatives as kinase inhibitors |
EP2081933B1 (en) | 2006-09-29 | 2011-03-23 | Novartis AG | Pyrazolopyrimidines as pi3k lipid kinase inhibitors |
GB0619342D0 (en) | 2006-09-30 | 2006-11-08 | Vernalis R&D Ltd | New chemical compounds |
EP2074096B1 (en) | 2006-10-04 | 2012-06-27 | F. Hoffmann-La Roche AG | 3-pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as hdl-cholesterol raising agents |
ES2631003T3 (es) | 2006-10-19 | 2017-08-25 | Signal Pharmaceuticals, Llc | Compuestos heteroarilo, sus composiciones y métodos de tratamiento con ellos |
US8148361B2 (en) | 2006-11-10 | 2012-04-03 | Bristol-Myers Squibb Company | Kinase inhibitors |
US20080132698A1 (en) | 2006-11-30 | 2008-06-05 | University Of Ottawa | Use of N-oxide compounds in coupling reactions |
AR064348A1 (es) | 2006-12-15 | 2009-04-01 | Bayer Schering Pharma Ag | 3-h-pirazolopiridinas y sales de estas, composiciones farmaceuticas que las comprenden, metodos para prepararlas y sus usos |
US7687522B2 (en) | 2006-12-20 | 2010-03-30 | Amgen Inc. | Substituted pyridines and pyrimidines and their use in treatment of cancer |
PE20081581A1 (es) | 2006-12-21 | 2008-11-12 | Plexxikon Inc | COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA |
GB0625659D0 (en) | 2006-12-21 | 2007-01-31 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
WO2008103277A2 (en) | 2007-02-16 | 2008-08-28 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors |
AU2008221263B2 (en) | 2007-03-01 | 2012-02-23 | Novartis Ag | Pim kinase inhibitors and methods of their use |
JP2008260691A (ja) | 2007-04-10 | 2008-10-30 | Bayer Cropscience Ag | 殺虫性アリールイソオキサゾリン誘導体 |
US8372867B2 (en) | 2007-04-10 | 2013-02-12 | Bayer Cropscience Ag | Insecticidal aryl isoxazoline derivatives |
JP2010526823A (ja) | 2007-05-10 | 2010-08-05 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Pi3キナーゼ阻害物質としてのキノキサリン誘導体 |
PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
UY31137A1 (es) | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
JP2009027904A (ja) | 2007-06-19 | 2009-02-05 | Hitachi Ltd | 回転電機 |
EP2012409A2 (en) | 2007-06-19 | 2009-01-07 | Hitachi, Ltd. | Rotating electrical machine |
WO2008156174A1 (ja) | 2007-06-21 | 2008-12-24 | Taisho Pharmaceutical Co., Ltd. | ピラジンアミド化合物 |
WO2009002964A1 (en) | 2007-06-26 | 2008-12-31 | Lexicon Pharmaceuticals, Inc. | Methods of treating serotonin-mediated diseases and disorders |
JP2010531358A (ja) | 2007-06-27 | 2010-09-24 | メルク・シャープ・エンド・ドーム・コーポレイション | ヒストン脱アセチル化酵素阻害剤としてのピリジル及びピリミジニル誘導体 |
GB0713259D0 (en) * | 2007-07-09 | 2007-08-15 | Astrazeneca Ab | Pyrazine derivatives 954 |
ES2551095T3 (es) | 2007-07-19 | 2015-11-16 | Lundbeck, H., A/S | Amidas heterocíclicas de 5 miembros y compuestos relacionados |
CN101801958B (zh) | 2007-07-19 | 2014-01-29 | 默沙东公司 | 作为蛋白质激酶抑制剂的杂环酰胺化合物 |
KR20100038119A (ko) | 2007-08-01 | 2010-04-12 | 화이자 인코포레이티드 | 피라졸 화합물 및 raf 억제제로서 이의 용도 |
WO2009024825A1 (en) | 2007-08-21 | 2009-02-26 | Astrazeneca Ab | 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors |
US8415358B2 (en) | 2007-09-17 | 2013-04-09 | Neurosearch A/S | Pyrazine derivatives and their use as potassium channel modulators |
KR20100089090A (ko) | 2007-10-25 | 2010-08-11 | 아스트라제네카 아베 | 세포 증식 장애의 치료에 유용한 피리딘 및 피라진 유도체 |
WO2009099982A1 (en) | 2008-02-04 | 2009-08-13 | Osi Pharmaceuticals, Inc. | 2-aminopyridine kinase inhibitors |
PL2250172T3 (pl) | 2008-02-25 | 2012-01-31 | Hoffmann La Roche | Pirolopirazynowe inhibitory kinazy |
JP5485178B2 (ja) | 2008-02-25 | 2014-05-07 | エフ.ホフマン−ラ ロシュ アーゲー | ピロロピラジンキナーゼ阻害剤 |
CN101939324B (zh) | 2008-02-25 | 2014-10-15 | 霍夫曼-拉罗奇有限公司 | 吡咯并吡嗪激酶抑制剂 |
MX2010009023A (es) | 2008-02-25 | 2010-09-07 | Hoffmann La Roche | Inhibidores de cinasas de pirrolopirazina. |
TW200940537A (en) | 2008-02-26 | 2009-10-01 | Astrazeneca Ab | Heterocyclic urea derivatives and methods of use thereof |
WO2009111280A1 (en) | 2008-02-29 | 2009-09-11 | Array Biopharma Inc. | N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer |
US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
WO2009152087A1 (en) | 2008-06-10 | 2009-12-17 | Plexxikon, Inc. | Bicyclic heteroaryl compounds and methods for kinase modulation, and indications therefor |
GB0814364D0 (en) | 2008-08-05 | 2008-09-10 | Eisai London Res Lab Ltd | Diazaindole derivatives and their use in the inhibition of c-Jun N-terminal kinase |
CA2731368C (en) | 2008-08-06 | 2013-05-14 | Pfizer Inc. | 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors |
CN104478875B (zh) | 2008-08-06 | 2017-04-12 | 麦迪韦逊科技有限公司 | 聚(adp‑核糖)聚合酶(parp)的二氢吡啶并酞嗪酮抑制剂 |
JP2010077286A (ja) | 2008-09-26 | 2010-04-08 | Aica Kogyo Co Ltd | シリコーン樹脂組成物および粘着フィルム |
JP2012506381A (ja) | 2008-10-21 | 2012-03-15 | バーテックス ファーマシューティカルズ インコーポレイテッド | c−METタンパク質キナーゼ阻害剤 |
CN102264721B (zh) | 2008-11-10 | 2015-12-09 | 沃泰克斯药物股份有限公司 | 用作atr激酶抑制剂的化合物 |
WO2010068483A2 (en) | 2008-11-25 | 2010-06-17 | University Of Rochester | Mlk inhibitors and methods of use |
SG171956A1 (en) | 2008-12-05 | 2011-07-28 | Hoffmann La Roche | Pyrrolopyrazinyl urea kinase inhibitors |
PL2376485T3 (pl) | 2008-12-19 | 2018-05-30 | Vertex Pharmaceuticals Incorporated | Pochodne pirazyny użyteczne jako inhibitory kinazy ATR |
JP5575799B2 (ja) | 2008-12-22 | 2014-08-20 | アレイ バイオファーマ、インコーポレイテッド | 7−フェノキシクロマンカルボン酸誘導体 |
TW201028410A (en) | 2008-12-22 | 2010-08-01 | Astrazeneca Ab | Chemical compounds 610 |
ES2567047T3 (es) | 2008-12-23 | 2016-04-19 | Abbvie Inc. | Derivados de pirimidina anti-virales |
US8492582B2 (en) | 2009-01-30 | 2013-07-23 | Toyama Chemical Co., Ltd. | N-acyl anthranilic acid derivative or salt thereof |
JP5353279B2 (ja) | 2009-02-06 | 2013-11-27 | Jnc株式会社 | セレンテラミド又はその類縁体の製造方法 |
US8063032B2 (en) | 2009-02-11 | 2011-11-22 | Sunovion Pharmaceuticals Inc. | Histamine H3 inverse agonists and antagonists and methods of use thereof |
CN101537007A (zh) | 2009-03-18 | 2009-09-23 | 中国医学科学院血液病医院(血液学研究所) | N-(噻吩-2)吡唑并[1,5-a]嘧啶-3-甲酰胺类化合物在制备抗恶性肿瘤药物方面的应用 |
US20120065247A1 (en) | 2009-03-27 | 2012-03-15 | Discoverybiomed, Inc. | Modulating ires-mediated translation |
AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
CA2768424C (en) | 2009-07-13 | 2015-04-28 | Widex A/S | A hearing aid adapted for detecting brain waves and a method for adapting such a hearing aid |
MX2012000711A (es) | 2009-07-15 | 2012-03-16 | Abbott Lab | Inhibidores de pirrolopirazina de cinasas. |
NZ597597A (en) | 2009-08-07 | 2014-01-31 | Dow Agrosciences Llc | Pesticidal compositions containing heteroaryl-n-aryl carbamate compounds |
JP2011042639A (ja) | 2009-08-24 | 2011-03-03 | Kowa Co | ビフェニルピラジン化合物及びこれを有効成分として含有するエリスロポエチン産生促進剤 |
CN101671336B (zh) | 2009-09-23 | 2013-11-13 | 辽宁利锋科技开发有限公司 | 芳杂环并嘧啶衍生物和类似物及其制备方法和用途 |
DE102009043260A1 (de) | 2009-09-28 | 2011-04-28 | Merck Patent Gmbh | Pyridinyl-imidazolonderivate |
IL302896A (en) | 2009-10-06 | 2023-07-01 | Millennium Pharm Inc | Heterocyclic compounds useful as pdk1 inhibitors |
CA2780633C (en) | 2009-11-13 | 2019-06-11 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Diazeniumdiolated compounds, pharmaceutical compositions, and method of treating cancer |
ME02315B (me) | 2010-01-18 | 2016-06-20 | Medicines For Malaria Venture Mmv | Novi antimalarijski agensi |
US8518945B2 (en) | 2010-03-22 | 2013-08-27 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
EP2556060A1 (en) | 2010-04-08 | 2013-02-13 | Ah Usa 42 Llc | Substituted 3,5- diphenyl-isoxazoline derivatives as insecticides and acaricides |
ES2602475T3 (es) | 2010-04-15 | 2017-02-21 | Tracon Pharmaceuticals, Inc. | Potenciación de la actividad anticáncer por terapia de combinación con inhibidores de la vía BER |
EP2566858A2 (en) | 2010-05-04 | 2013-03-13 | Pfizer Inc. | Heterocyclic derivatives as alk inhibitors |
US9062008B2 (en) | 2010-05-12 | 2015-06-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
JP2013526538A (ja) | 2010-05-12 | 2013-06-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ阻害剤として有用な化合物 |
WO2011143425A2 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
CA2798760A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as inhibitors of atr kinase |
US8962631B2 (en) | 2010-05-12 | 2015-02-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
WO2011143426A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
TWI496785B (zh) | 2010-05-20 | 2015-08-21 | Hoffmann La Roche | 吡咯并吡激酶抑制劑 |
WO2011144585A1 (en) | 2010-05-20 | 2011-11-24 | F. Hoffmann-La Roche Ag | Pyrrolo [2, 3 - b] pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors |
CA2803802A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
CN102311396B (zh) | 2010-07-05 | 2015-01-07 | 暨南大学 | 一种吡嗪类衍生物和其制备方法及在制药中的应用 |
EP2407478A1 (en) | 2010-07-14 | 2012-01-18 | GENETADI Biotech, S.L. | New cyclotetrapeptides with pro-angiogenic properties |
JP5782238B2 (ja) | 2010-07-30 | 2015-09-24 | ルネサスエレクトロニクス株式会社 | 電圧検出回路及びその制御方法 |
EP2681206B1 (en) | 2011-03-04 | 2017-06-14 | Lexicon Pharmaceuticals, Inc. | Mst1 kinase inhibitors and methods of their use |
US8962623B2 (en) | 2011-03-04 | 2015-02-24 | Locus Pharmaceuticals, Inc. | Aminopyrazine compounds |
JP2014510151A (ja) | 2011-04-05 | 2014-04-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ(trakinase)阻害剤として有用なアミノピラジン化合物 |
JP2014513728A (ja) | 2011-05-17 | 2014-06-05 | プリンシピア バイオファーマ インコーポレイテッド | チロシンキナーゼ阻害剤としてのアザインドール誘導体 |
EP2723747A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
WO2012178125A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
WO2012178123A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
JP6162126B2 (ja) | 2011-09-30 | 2017-08-23 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atr阻害剤による膵臓癌及び非小細胞肺癌の治療 |
CN103958507A (zh) | 2011-09-30 | 2014-07-30 | 沃泰克斯药物股份有限公司 | 可用作atr激酶抑制剂的化合物 |
US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
US8765751B2 (en) | 2011-09-30 | 2014-07-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EP2751097A2 (en) | 2011-09-30 | 2014-07-09 | Vertex Pharmaceuticals Incorporated | Processes for making compounds useful as inhibitors of atr kinase |
WO2013071085A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
WO2013071090A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8846918B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EP2776421A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
ES2654670T3 (es) | 2012-04-05 | 2018-02-14 | Vertex Pharmaceuticals Incorporated | Compuestos útiles como inhibidores de la cinasa ATR y terapias de combinación de los mismos |
CN103373996A (zh) | 2012-04-20 | 2013-10-30 | 山东亨利医药科技有限责任公司 | 作为crth2受体拮抗剂的二并环衍生物 |
US8999632B2 (en) | 2012-10-04 | 2015-04-07 | Vertex Pharmaceuticals Incorporated | Method for measuring ATR inhibition mediated increases in DNA damage |
EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
DK3486245T3 (da) | 2012-12-07 | 2021-07-19 | Vertex Pharma | 2-amino-n-(piperidin-1-yl-pyridin-3-yl) pyrazolo[1,5alpha]pyrimidin-3-carboxamid som hæmmer for atr kinase |
JP6096005B2 (ja) | 2013-02-26 | 2017-03-15 | リンテック株式会社 | シート剥離装置および剥離方法 |
SG11201604519PA (en) | 2013-12-06 | 2016-07-28 | Vertex Pharma | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
WO2015187451A1 (en) | 2014-06-05 | 2015-12-10 | Vertex Pharmacetucals Incorporated | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
SG10201811175WA (en) | 2014-06-17 | 2019-01-30 | Vertex Pharma | Method for treating cancer using a combination of chk1 and atr inhibitors |
-
2009
- 2009-12-18 PL PL09798991T patent/PL2376485T3/pl unknown
- 2009-12-18 CA CA2747252A patent/CA2747252C/en active Active
- 2009-12-18 CN CN201610960262.1A patent/CN106518856B/zh active Active
- 2009-12-18 DK DK17205270.6T patent/DK3354650T3/da active
- 2009-12-18 SI SI200931816T patent/SI2376485T1/en unknown
- 2009-12-18 ES ES17205270T patent/ES2921576T3/es active Active
- 2009-12-18 EP EP09798991.7A patent/EP2376485B1/en active Active
- 2009-12-18 HR HRP20180385TT patent/HRP20180385T1/hr unknown
- 2009-12-18 PL PL17205270T patent/PL3354650T3/pl unknown
- 2009-12-18 KR KR1020177018220A patent/KR101958632B1/ko active Active
- 2009-12-18 CN CN201610960222.7A patent/CN106496210B/zh active Active
- 2009-12-18 US US12/642,447 patent/US8841308B2/en active Active
- 2009-12-18 LT LTEP09798991.7T patent/LT2376485T/lt unknown
- 2009-12-18 NO NO09798991A patent/NO2376485T3/no unknown
- 2009-12-18 SG SG10201607592PA patent/SG10201607592PA/en unknown
- 2009-12-18 NZ NZ593969A patent/NZ593969A/xx unknown
- 2009-12-18 DK DK09798991.7T patent/DK2376485T3/en active
- 2009-12-18 BR BRPI0924084-5A patent/BRPI0924084B1/pt active IP Right Grant
- 2009-12-18 HR HRP20220581TT patent/HRP20220581T1/hr unknown
- 2009-12-18 SG SG2011044724A patent/SG172248A1/en unknown
- 2009-12-18 AU AU2009327357A patent/AU2009327357C1/en active Active
- 2009-12-18 SM SM20180181T patent/SMT201800181T1/it unknown
- 2009-12-18 RU RU2016141566A patent/RU2016141566A/ru unknown
- 2009-12-18 PT PT172052706T patent/PT3354650T/pt unknown
- 2009-12-18 RU RU2011129761/04A patent/RU2604066C2/ru active
- 2009-12-18 SI SI200932162T patent/SI3354650T1/sl unknown
- 2009-12-18 LT LTEP17205270.6T patent/LT3354650T/lt unknown
- 2009-12-18 PT PT97989917T patent/PT2376485T/pt unknown
- 2009-12-18 MX MX2011006503A patent/MX2011006503A/es active IP Right Grant
- 2009-12-18 CA CA3013000A patent/CA3013000C/en active Active
- 2009-12-18 ES ES09798991.7T patent/ES2663222T3/es active Active
- 2009-12-18 EP EP22156312.5A patent/EP4059932A1/en active Pending
- 2009-12-18 WO PCT/US2009/068827 patent/WO2010071837A1/en active Application Filing
- 2009-12-18 CN CN201610956094.9A patent/CN106496209B/zh active Active
- 2009-12-18 KR KR1020117016218A patent/KR101745331B1/ko active Active
- 2009-12-18 KR KR1020147035688A patent/KR101755216B1/ko active Active
- 2009-12-18 CN CN200980155778.7A patent/CN102300862B/zh active Active
- 2009-12-18 JP JP2011542506A patent/JP5753093B2/ja active Active
- 2009-12-18 RS RS20180262A patent/RS56995B1/sr unknown
- 2009-12-18 EP EP17205270.6A patent/EP3354650B1/en active Active
- 2009-12-18 HU HUE09798991A patent/HUE036068T2/hu unknown
- 2009-12-21 TW TW098143971A patent/TWI478918B/zh active
- 2009-12-21 TW TW105117426A patent/TWI643854B/zh active
- 2009-12-21 AR ARP090105005A patent/AR074822A1/es active IP Right Grant
- 2009-12-21 TW TW103134778A patent/TWI543979B/zh active
-
2011
- 2011-06-16 IL IL213613A patent/IL213613A/en active IP Right Grant
- 2011-06-17 ZA ZA2011/04498A patent/ZA201104498B/en unknown
-
2014
- 2014-03-24 US US14/223,109 patent/US9365557B2/en active Active
- 2014-08-25 US US14/467,175 patent/US9701674B2/en active Active
- 2014-08-26 JP JP2014171200A patent/JP5894643B2/ja active Active
-
2015
- 2015-01-06 IL IL236602A patent/IL236602B/en active IP Right Grant
- 2015-10-06 JP JP2015198400A patent/JP6212527B2/ja active Active
-
2016
- 2016-04-29 US US15/142,286 patent/US20160311809A1/en not_active Abandoned
- 2016-08-31 AU AU2016222396A patent/AU2016222396B2/en active Active
-
2017
- 2017-05-30 US US15/608,630 patent/US10961232B2/en active Active
- 2017-08-16 JP JP2017157105A patent/JP6577537B2/ja active Active
-
2018
- 2018-02-26 AU AU2018201363A patent/AU2018201363C1/en active Active
- 2018-03-02 CY CY20181100268T patent/CY1120002T1/el unknown
- 2018-04-30 US US15/967,110 patent/US10479784B2/en active Active
- 2018-06-19 IL IL260158A patent/IL260158B/en active IP Right Grant
-
2019
- 2019-07-12 JP JP2019130031A patent/JP2019194250A/ja not_active Withdrawn
-
2021
- 2021-02-25 US US17/184,813 patent/US20230030414A1/en not_active Abandoned
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
RU2016141566A (ru) | Производные пиразина, используемые в качестве ингибиторов киназы atr | |
JP2012512906A5 (forum.php) | ||
JP2012508260A5 (forum.php) | ||
JP2013529643A5 (forum.php) | ||
CA2774046E (en) | Compositions comprising n-benzyl or n-sulfonylaryl-3-hydroxypyridin-2-(1h)-ones and their use for treating colitis | |
JP6027662B2 (ja) | 前立腺癌およびアンドロゲン受容体関連病態の治療のためのアンドロゲン受容体の調節剤 | |
RU2011123647A (ru) | Соединения, полезные в качестве ингибиторов atr киназы | |
ES2802296T3 (es) | Co-cristales de (S)-N-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il)quinolin-4-carboxamida y derivados deuterados de la misma como inhibidores de DNA-PK | |
JP2013526540A5 (forum.php) | ||
RU2686323C2 (ru) | Новые соединения и композиции для ингибирования fasn | |
TWI469970B (zh) | 調節hsp90活性之咪唑化合物 | |
TWI446910B (zh) | 調節hsp90活性的三唑化合物 | |
ES2733847T3 (es) | Método para tratar cáncer usando una combinación de inhibidores de CHK1 y ATR | |
JP2013526538A5 (forum.php) | ||
CN102438452B (zh) | 包含cdk抑制剂的化合物和组合物以及用于癌症治疗的方法 | |
BR112019018991A2 (pt) | compostos e composições para tratar distúrbios hematológicos | |
JP2013526539A5 (forum.php) | ||
JP2014510151A5 (forum.php) | ||
CN110105340B (zh) | 苯甲酰胺和烟酰胺化合物及其使用方法 | |
CN105254624B (zh) | 异噻唑衍生物pim激酶抑制剂及其制备方法与在制药中的应用 | |
CN105130959B (zh) | 嘧啶衍生物pim激酶抑制剂及其制备方法与在制药中的应用 | |
TW202317532A (zh) | Aak1抑制劑及其用途 | |
BR112021012138A2 (pt) | Análogos de pentamidina e seus usos | |
KR20060130681A (ko) | 테트라사이클릭 락탐 유도체 및 이것의 용도 | |
US7388016B2 (en) | Dibenzonaphthyridine derivatives and methods of use thereof |