JP2014514323A5 - - Google Patents
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- Publication number
- JP2014514323A5 JP2014514323A5 JP2014506609A JP2014506609A JP2014514323A5 JP 2014514323 A5 JP2014514323 A5 JP 2014514323A5 JP 2014506609 A JP2014506609 A JP 2014506609A JP 2014506609 A JP2014506609 A JP 2014506609A JP 2014514323 A5 JP2014514323 A5 JP 2014514323A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heterocycle
- heteroaryl
- aryl
- carbocycle
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims description 244
- 125000000623 heterocyclic group Chemical group 0.000 claims description 178
- 125000001072 heteroaryl group Chemical group 0.000 claims description 164
- 125000003118 aryl group Chemical group 0.000 claims description 153
- 125000001188 haloalkyl group Chemical group 0.000 claims description 99
- 125000000304 alkynyl group Chemical group 0.000 claims description 82
- 150000001875 compounds Chemical class 0.000 claims description 69
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 61
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 39
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 26
- 125000005843 halogen group Chemical group 0.000 claims description 25
- 125000002837 carbocyclic group Chemical group 0.000 claims description 15
- 239000003112 inhibitor Substances 0.000 claims description 14
- 208000031886 HIV Infections Diseases 0.000 claims description 10
- 208000037357 HIV infectious disease Diseases 0.000 claims description 10
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims description 10
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- 239000001301 oxygen Substances 0.000 claims description 5
- 239000002777 nucleoside Substances 0.000 claims description 4
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 4
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims description 3
- 102100035875 C-C chemokine receptor type 5 Human genes 0.000 claims description 2
- 101710149870 C-C chemokine receptor type 5 Proteins 0.000 claims description 2
- 102100031650 C-X-C chemokine receptor type 4 Human genes 0.000 claims description 2
- 229940099797 HIV integrase inhibitor Drugs 0.000 claims description 2
- 229940122440 HIV protease inhibitor Drugs 0.000 claims description 2
- 101000922348 Homo sapiens C-X-C chemokine receptor type 4 Proteins 0.000 claims description 2
- 210000000234 capsid Anatomy 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 229940124784 gp41 inhibitor Drugs 0.000 claims description 2
- 239000003084 hiv integrase inhibitor Substances 0.000 claims description 2
- 239000004030 hiv protease inhibitor Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 238000013160 medical therapy Methods 0.000 claims description 2
- 239000002773 nucleotide Substances 0.000 claims description 2
- 125000003729 nucleotide group Chemical group 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 238000006116 polymerization reaction Methods 0.000 claims description 2
- 230000000069 prophylactic effect Effects 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 7
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 7
- 125000006736 (C6-C20) aryl group Chemical group 0.000 claims 4
- 102100034343 Integrase Human genes 0.000 claims 3
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 229910052717 sulfur Chemical group 0.000 claims 3
- 239000011593 sulfur Chemical group 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 description 90
- 0 *C(*)(C(O)=O)c1c(*)c(*)c2nc(*)[s]c2c1* Chemical compound *C(*)(C(O)=O)c1c(*)c(*)c2nc(*)[s]c2c1* 0.000 description 22
- 125000002619 bicyclic group Chemical group 0.000 description 17
- 125000004429 atom Chemical group 0.000 description 12
- 229910052736 halogen Inorganic materials 0.000 description 11
- 150000003254 radicals Chemical class 0.000 description 10
- 125000004043 oxo group Chemical group O=* 0.000 description 8
- 125000002877 alkyl aryl group Chemical group 0.000 description 7
- 150000002367 halogens Chemical class 0.000 description 7
- 238000000034 method Methods 0.000 description 7
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- 241000124008 Mammalia Species 0.000 description 6
- 125000005213 alkyl heteroaryl group Chemical group 0.000 description 6
- 125000005024 alkenyl aryl group Chemical group 0.000 description 5
- 125000005217 alkenylheteroaryl group Chemical group 0.000 description 5
- 125000005025 alkynylaryl group Chemical group 0.000 description 5
- 125000000464 thioxo group Chemical group S=* 0.000 description 5
- -1 -OH Chemical group 0.000 description 4
- 125000001054 5 membered carbocyclic group Chemical group 0.000 description 4
- 125000004008 6 membered carbocyclic group Chemical group 0.000 description 4
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- XKCBCFFAQVLJPP-VWLOTQADSA-N CC(C)N(C)c1nc(cc(C)c([C@@H](C(O)=O)OC(C)(C)C)c2-c(cc3)c4nccc5c4c3OCC5)c2[s]1 Chemical compound CC(C)N(C)c1nc(cc(C)c([C@@H](C(O)=O)OC(C)(C)C)c2-c(cc3)c4nccc5c4c3OCC5)c2[s]1 XKCBCFFAQVLJPP-VWLOTQADSA-N 0.000 description 4
- FKSKUTHBADGXQV-UHFFFAOYSA-N CCCc(cc1)c2nccc3c2c1OCC3 Chemical compound CCCc(cc1)c2nccc3c2c1OCC3 FKSKUTHBADGXQV-UHFFFAOYSA-N 0.000 description 4
- QEPFWYGLFVVATF-UHFFFAOYSA-N CCc(ccc1c2NCCO1)c2Cl Chemical compound CCc(ccc1c2NCCO1)c2Cl QEPFWYGLFVVATF-UHFFFAOYSA-N 0.000 description 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 4
- WGFNXGPBPIJYLI-UHFFFAOYSA-N 2,6-difluoro-3-[(3-fluorophenyl)sulfonylamino]-n-(3-methoxy-1h-pyrazolo[3,4-b]pyridin-5-yl)benzamide Chemical compound C1=C2C(OC)=NNC2=NC=C1NC(=O)C(C=1F)=C(F)C=CC=1NS(=O)(=O)C1=CC=CC(F)=C1 WGFNXGPBPIJYLI-UHFFFAOYSA-N 0.000 description 3
- 125000001963 4 membered heterocyclic group Chemical group 0.000 description 3
- 125000002373 5 membered heterocyclic group Chemical group 0.000 description 3
- 125000004070 6 membered heterocyclic group Chemical group 0.000 description 3
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- 108010078851 HIV Reverse Transcriptase Proteins 0.000 description 3
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