JP2016516756A5 - - Google Patents

Info

Publication number

JP2016516756A5

JP2016516756A5 JP2016506681A JP2016506681A JP2016516756A5 JP 2016516756 A5 JP2016516756 A5 JP 2016516756A5 JP 2016506681 A JP2016506681 A JP 2016506681A JP 2016506681 A JP2016506681 A JP 2016506681A JP 2016516756 A5 JP2016516756 A5 JP 2016516756A5

Authority

JP

Japan

Prior art keywords

seq

myristoyl

pharmaceutical composition

peptide

composition according

Prior art date

2014-04-07

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

Links

• Espacenet
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• 239000008194 pharmaceutical composition Substances 0.000 claims 32
• 108090000765 processed proteins & peptides Proteins 0.000 claims 29
• 206010028980 Neoplasm Diseases 0.000 claims 19
• 102000015695 Myristoylated Alanine-Rich C Kinase Substrate Human genes 0.000 claims 15
• 108010063737 Myristoylated Alanine-Rich C Kinase Substrate Proteins 0.000 claims 15
• 201000011510 cancer Diseases 0.000 claims 14
• 230000002401 inhibitory effect Effects 0.000 claims 12
• 150000001875 compounds Chemical class 0.000 claims 11
• 150000001408 amides Chemical class 0.000 claims 9
• 210000004027 cell Anatomy 0.000 claims 9
• 238000009472 formulation Methods 0.000 claims 8
• 239000000203 mixture Substances 0.000 claims 8
• 206010027476 Metastases Diseases 0.000 claims 6
• 230000009401 metastasis Effects 0.000 claims 6
• 102000004196 processed proteins & peptides Human genes 0.000 claims 6
• 125000001429 N-terminal alpha-amino-acid group Chemical group 0.000 claims 5
• 230000002265 prevention Effects 0.000 claims 5
• 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 4
• -1 aliphatic alkyl sulfonic acids Chemical class 0.000 claims 4
• 239000003112 inhibitor Substances 0.000 claims 4
• 239000007924 injection Substances 0.000 claims 4
• 238000002347 injection Methods 0.000 claims 4
• 238000013508 migration Methods 0.000 claims 4
• 230000005012 migration Effects 0.000 claims 4
• 125000003275 alpha amino acid group Chemical group 0.000 claims 3
• 108020004707 nucleic acids Proteins 0.000 claims 3
• 102000039446 nucleic acids Human genes 0.000 claims 3
• 150000007523 nucleic acids Chemical class 0.000 claims 3
• 108091033319 polynucleotide Proteins 0.000 claims 3
• 102000040430 polynucleotide Human genes 0.000 claims 3
• 239000002157 polynucleotide Substances 0.000 claims 3
• 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 2
• 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 2
• 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 2
• 241000124008 Mammalia Species 0.000 claims 2
• 108020004459 Small interfering RNA Proteins 0.000 claims 2
• DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims 2
• 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 2
• WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
• 230000001747 exhibiting effect Effects 0.000 claims 2
• 239000012669 liquid formulation Substances 0.000 claims 2
• 239000006193 liquid solution Substances 0.000 claims 2
• 239000006194 liquid suspension Substances 0.000 claims 2
• 108091070501 miRNA Proteins 0.000 claims 2
• 239000002679 microRNA Substances 0.000 claims 2
• 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
• 239000000843 powder Substances 0.000 claims 2
• KCSNGWMKFYVMKF-HGYIIGRXSA-N (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-acetamidoacetyl)amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-6-aminohexanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]propanoyl]amino]-6-aminohexanoic acid Chemical compound NCCCC[C@@H](C(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](O)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)CNC(C)=O)CC1=CC=CC=C1 KCSNGWMKFYVMKF-HGYIIGRXSA-N 0.000 claims 1
• 108020005544 Antisense RNA Proteins 0.000 claims 1
• 239000005711 Benzoic acid Substances 0.000 claims 1
• 108091027967 Small hairpin RNA Proteins 0.000 claims 1
• 230000010933 acylation Effects 0.000 claims 1
• 238000005917 acylation reaction Methods 0.000 claims 1
• 150000007933 aliphatic carboxylic acids Chemical class 0.000 claims 1
• 125000001931 aliphatic group Chemical group 0.000 claims 1
• 125000000217 alkyl group Chemical group 0.000 claims 1
• 238000010640 amide synthesis reaction Methods 0.000 claims 1
• 125000003277 amino group Chemical group 0.000 claims 1
• 229910021529 ammonia Inorganic materials 0.000 claims 1
• QGZKDVFQNNGYKY-UHFFFAOYSA-N ammonia Natural products N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims 1
• 235000010233 benzoic acid Nutrition 0.000 claims 1
• 210000004899 c-terminal region Anatomy 0.000 claims 1
• 230000009702 cancer cell proliferation Effects 0.000 claims 1
• 125000002843 carboxylic acid group Chemical group 0.000 claims 1
• 239000003184 complementary RNA Substances 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 229940079593 drug Drugs 0.000 claims 1
• 238000007918 intramuscular administration Methods 0.000 claims 1
• 239000007927 intramuscular injection Substances 0.000 claims 1
• 239000007928 intraperitoneal injection Substances 0.000 claims 1
• 238000001990 intravenous administration Methods 0.000 claims 1
• 238000012423 maintenance Methods 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
• 230000035755 proliferation Effects 0.000 claims 1
• 229920006395 saturated elastomer Polymers 0.000 claims 1
• 239000002924 silencing RNA Substances 0.000 claims 1
• 239000004055 small Interfering RNA Substances 0.000 claims 1
• 238000006467 substitution reaction Methods 0.000 claims 1
• 239000000829 suppository Substances 0.000 claims 1
• 230000009885 systemic effect Effects 0.000 claims 1
• 230000005747 tumor angiogenesis Effects 0.000 claims 1
• 230000004614 tumor growth Effects 0.000 claims 1