JP2012509273A5 - - Google Patents

Info

Publication number

JP2012509273A5

JP2012509273A5 JP2011536585A JP2011536585A JP2012509273A5 JP 2012509273 A5 JP2012509273 A5 JP 2012509273A5 JP 2011536585 A JP2011536585 A JP 2011536585A JP 2011536585 A JP2011536585 A JP 2011536585A JP 2012509273 A5 JP2012509273 A5 JP 2012509273A5

Authority

JP

Japan

Prior art keywords

substituted

alkyl

nhc

independently

compound

Prior art date

2009-11-17

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.)

Ceased

Links

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• 125000000217 alkyl group Chemical group 0.000 claims 27
• 239000002105 nanoparticle Substances 0.000 claims 22
• 150000001875 compounds Chemical class 0.000 claims 19
• 108091034117 Oligonucleotide Proteins 0.000 claims 17
• 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 13
• 229910052739 hydrogen Inorganic materials 0.000 claims 13
• 125000003545 alkoxy group Chemical group 0.000 claims 10
• 239000001257 hydrogen Substances 0.000 claims 10
• 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 10
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 9
• 230000000692 anti-sense effect Effects 0.000 claims 9
• 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 9
• 125000003118 aryl group Chemical group 0.000 claims 8
• 108020004707 nucleic acids Proteins 0.000 claims 8
• 102000039446 nucleic acids Human genes 0.000 claims 8
• 150000007523 nucleic acids Chemical class 0.000 claims 8
• 125000000547 substituted alkyl group Chemical group 0.000 claims 8
• 150000001412 amines Chemical class 0.000 claims 6
• 125000004405 heteroalkoxy group Chemical group 0.000 claims 6
• 150000002632 lipids Chemical class 0.000 claims 6
• 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 6
• 125000003107 substituted aryl group Chemical group 0.000 claims 6
• 229920006395 saturated elastomer Polymers 0.000 claims 5
• 125000003710 aryl alkyl group Chemical group 0.000 claims 4
• 229910052799 carbon Inorganic materials 0.000 claims 4
• HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 4
• 125000001072 heteroaryl group Chemical group 0.000 claims 4
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
• -1 cationic lipid Chemical class 0.000 claims 3
• 229910052760 oxygen Inorganic materials 0.000 claims 3
• 229910052717 sulfur Inorganic materials 0.000 claims 3
• 108091023037 Aptamer Proteins 0.000 claims 2
• 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
• 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
• 108700011259 MicroRNAs Proteins 0.000 claims 2
• 108091093037 Peptide nucleic acid Proteins 0.000 claims 2
• NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
• 108020004459 Small interfering RNA Proteins 0.000 claims 2
• QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 2
• 239000002253 acid Substances 0.000 claims 2
• 230000001588 bifunctional effect Effects 0.000 claims 2
• 235000012000 cholesterol Nutrition 0.000 claims 2
• 125000004404 heteroalkyl group Chemical group 0.000 claims 2
• 239000002679 microRNA Substances 0.000 claims 2
• 239000002773 nucleotide Substances 0.000 claims 2
• 125000003729 nucleotide group Chemical group 0.000 claims 2
• 239000004055 small Interfering RNA Substances 0.000 claims 2
• 125000005017 substituted alkenyl group Chemical group 0.000 claims 2
• 125000004426 substituted alkynyl group Chemical group 0.000 claims 2
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 1
• 102100021569 Apoptosis regulator Bcl-2 Human genes 0.000 claims 1
• 102100021663 Baculoviral IAP repeat-containing protein 5 Human genes 0.000 claims 1
• 108060000903 Beta-catenin Proteins 0.000 claims 1
• 102000015735 Beta-catenin Human genes 0.000 claims 1
• 125000006539 C12 alkyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
• 102000053642 Catalytic RNA Human genes 0.000 claims 1
• 108090000994 Catalytic RNA Proteins 0.000 claims 1
• 108020004414 DNA Proteins 0.000 claims 1
• 108010045100 HSP27 Heat-Shock Proteins Proteins 0.000 claims 1
• 102100039165 Heat shock protein beta-1 Human genes 0.000 claims 1
• 101000971171 Homo sapiens Apoptosis regulator Bcl-2 Proteins 0.000 claims 1
• 101001046870 Homo sapiens Hypoxia-inducible factor 1-alpha Proteins 0.000 claims 1
• 101000605639 Homo sapiens Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Proteins 0.000 claims 1
• 102100022875 Hypoxia-inducible factor 1-alpha Human genes 0.000 claims 1
• 102100038332 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Human genes 0.000 claims 1
• 108091030071 RNAI Proteins 0.000 claims 1
• 108091028664 Ribonucleotide Proteins 0.000 claims 1
• 108091027076 Spiegelmer Proteins 0.000 claims 1
• 108010002687 Survivin Proteins 0.000 claims 1
• 108010088665 Zinc Finger Protein Gli2 Proteins 0.000 claims 1
• 230000002378 acidificating effect Effects 0.000 claims 1
• 125000003342 alkenyl group Chemical group 0.000 claims 1
• 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
• 150000001413 amino acids Chemical class 0.000 claims 1
• 102000001307 androgen receptors Human genes 0.000 claims 1
• 108010080146 androgen receptors Proteins 0.000 claims 1
• 239000000074 antisense oligonucleotide Substances 0.000 claims 1
• 238000012230 antisense oligonucleotides Methods 0.000 claims 1
• 125000004429 atom Chemical group 0.000 claims 1
• 150000001735 carboxylic acids Chemical class 0.000 claims 1
• 125000002091 cationic group Chemical group 0.000 claims 1
• 229940106189 ceramide Drugs 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
• 230000000799 fusogenic effect Effects 0.000 claims 1
• 230000009368 gene silencing by RNA Effects 0.000 claims 1
• 125000005842 heteroatom Chemical group 0.000 claims 1
• 150000002466 imines Chemical class 0.000 claims 1
• 125000000400 lauroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 125000001419 myristoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 230000007935 neutral effect Effects 0.000 claims 1
• 229910052757 nitrogen Inorganic materials 0.000 claims 1
• 125000002811 oleoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])/C([H])=C([H])\C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 229910052698 phosphorus Inorganic materials 0.000 claims 1
• 239000002336 ribonucleotide Substances 0.000 claims 1
• 125000002652 ribonucleotide group Chemical group 0.000 claims 1
• 108091092562 ribozyme Proteins 0.000 claims 1
• 125000006850 spacer group Chemical group 0.000 claims 1
• 125000003696 stearoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 0 *CC(C(*(CC*=C(C1)[*@]1C1C=CC(C(*(CCCCC(*)*)=C)=O)=CC1)=C)=O)=C Chemical compound *CC(C(*(CC*=C(C1)[*@]1C1C=CC(C(*(CCCCC(*)*)=C)=O)=CC1)=C)=O)=C 0.000 description 1