JP2015514804A5 - - Google Patents
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- JP2015514804A5 JP2015514804A5 JP2015509082A JP2015509082A JP2015514804A5 JP 2015514804 A5 JP2015514804 A5 JP 2015514804A5 JP 2015509082 A JP2015509082 A JP 2015509082A JP 2015509082 A JP2015509082 A JP 2015509082A JP 2015514804 A5 JP2015514804 A5 JP 2015514804A5
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- 125000000217 alkyl group Chemical group 0.000 claims description 318
- 150000001875 compounds Chemical class 0.000 claims description 92
- 229910052739 hydrogen Inorganic materials 0.000 claims description 68
- 125000000623 heterocyclic group Chemical group 0.000 claims description 58
- 239000001257 hydrogen Substances 0.000 claims description 56
- 125000001153 fluoro group Chemical group F* 0.000 claims description 52
- 150000002431 hydrogen Chemical class 0.000 claims description 48
- -1 pyrrolidinonyl Chemical group 0.000 claims description 39
- 229910052799 carbon Inorganic materials 0.000 claims description 34
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 32
- 125000002757 morpholinyl group Chemical group 0.000 claims description 26
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 24
- 125000003566 oxetanyl group Chemical group 0.000 claims description 20
- 125000003386 piperidinyl group Chemical group 0.000 claims description 20
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 18
- 229910052731 fluorine Inorganic materials 0.000 claims description 18
- 229910052736 halogen Inorganic materials 0.000 claims description 18
- 150000002367 halogens Chemical class 0.000 claims description 18
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 18
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 18
- 125000001072 heteroaryl group Chemical group 0.000 claims description 17
- 125000002393 azetidinyl group Chemical group 0.000 claims description 16
- 125000004193 piperazinyl group Chemical group 0.000 claims description 16
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 14
- 125000004069 aziridinyl group Chemical group 0.000 claims description 14
- 125000002883 imidazolyl group Chemical group 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 10
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 229910052805 deuterium Inorganic materials 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000001544 thienyl group Chemical group 0.000 claims description 8
- 125000004122 cyclic group Chemical group 0.000 claims description 7
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims description 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 125000000532 dioxanyl group Chemical group 0.000 claims description 6
- 125000005879 dioxolanyl group Chemical group 0.000 claims description 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 6
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 6
- 125000000335 thiazolyl group Chemical group 0.000 claims description 6
- 125000001425 triazolyl group Chemical group 0.000 claims description 6
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims description 4
- 125000004273 azetidin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])C1([H])* 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 125000002541 furyl group Chemical group 0.000 claims description 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 4
- 125000004274 oxetan-2-yl group Chemical group [H]C1([H])OC([H])(*)C1([H])[H] 0.000 claims description 4
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 3
- 239000000203 mixture Substances 0.000 claims description 3
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims description 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 230000005778 DNA damage Effects 0.000 claims description 2
- 231100000277 DNA damage Toxicity 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 238000011285 therapeutic regimen Methods 0.000 claims description 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 2
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 1
- 238000005728 strengthening Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 6
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- 230000001235 sensitizing effect Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261637512P | 2012-04-24 | 2012-04-24 | |
| US61/637,512 | 2012-04-24 | ||
| US201261725652P | 2012-11-13 | 2012-11-13 | |
| US61/725,652 | 2012-11-13 | ||
| US201361777806P | 2013-03-12 | 2013-03-12 | |
| US61/777,806 | 2013-03-12 | ||
| PCT/US2013/037811 WO2013163190A1 (en) | 2012-04-24 | 2013-04-23 | Dna-pk inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017131233A Division JP2017165788A (ja) | 2012-04-24 | 2017-07-04 | Ｄｎａ−ｐｋ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015514804A JP2015514804A (ja) | 2015-05-21 |
| JP2015514804A5 true JP2015514804A5 (cg-RX-API-DMAC7.html) | 2016-06-09 |
| JP6378171B2 JP6378171B2 (ja) | 2018-08-22 |
Family
ID=48225150
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015509082A Active JP6378171B2 (ja) | 2012-04-24 | 2013-04-23 | Ｄｎａ−ｐｋ阻害剤 |
| JP2017131233A Withdrawn JP2017165788A (ja) | 2012-04-24 | 2017-07-04 | Ｄｎａ−ｐｋ阻害剤 |
| JP2019094453A Active JP6741825B2 (ja) | 2012-04-24 | 2019-05-20 | Ｄｎａ−ｐｋ阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017131233A Withdrawn JP2017165788A (ja) | 2012-04-24 | 2017-07-04 | Ｄｎａ−ｐｋ阻害剤 |
| JP2019094453A Active JP6741825B2 (ja) | 2012-04-24 | 2019-05-20 | Ｄｎａ−ｐｋ阻害剤 |
Country Status (30)
Families Citing this family (69)
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| MX361488B (es) | 2013-10-17 | 2018-12-07 | Vertex Pharma | Cocristales de (s)-n-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il ) amino)propan-2-il)quinolina-4-carboxamida y sus derivados deuterados como inhibidores de proteínas cinasa dependientes de adn (adn-pk). |
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