CA2640080A1 - Compositions and methods for the treatment of ophthalmic disease - Google Patents
Compositions and methods for the treatment of ophthalmic disease Download PDFInfo
- Publication number
- CA2640080A1 CA2640080A1 CA002640080A CA2640080A CA2640080A1 CA 2640080 A1 CA2640080 A1 CA 2640080A1 CA 002640080 A CA002640080 A CA 002640080A CA 2640080 A CA2640080 A CA 2640080A CA 2640080 A1 CA2640080 A1 CA 2640080A1
- Authority
- CA
- Canada
- Prior art keywords
- seq
- azepanyl
- amino
- group
- cyclohexyl
- 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.)
- Abandoned
Links
- 238000000034 method Methods 0.000 title claims abstract 100
- 239000000203 mixture Substances 0.000 title claims abstract 27
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
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- 101000922348 Homo sapiens C-X-C chemokine receptor type 4 Proteins 0.000 claims abstract 20
- 230000002401 inhibitory effect Effects 0.000 claims abstract 4
- 125000003729 nucleotide group Chemical group 0.000 claims 30
- 125000004432 carbon atom Chemical group C* 0.000 claims 28
- 239000002773 nucleotide Substances 0.000 claims 28
- 125000001424 substituent group Chemical group 0.000 claims 24
- 239000003112 inhibitor Substances 0.000 claims 20
- 108020004707 nucleic acids Proteins 0.000 claims 19
- 102000039446 nucleic acids Human genes 0.000 claims 19
- 150000007523 nucleic acids Chemical group 0.000 claims 19
- 102100021669 Stromal cell-derived factor 1 Human genes 0.000 claims 16
- 101710088580 Stromal cell-derived factor 1 Proteins 0.000 claims 16
- 108020004459 Small interfering RNA Proteins 0.000 claims 15
- 239000004055 small Interfering RNA Substances 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 11
- 241000124008 Mammalia Species 0.000 claims 10
- 239000007943 implant Substances 0.000 claims 10
- 125000002950 monocyclic group Chemical group 0.000 claims 10
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 9
- 230000000694 effects Effects 0.000 claims 9
- 108091030071 RNAI Proteins 0.000 claims 8
- 230000009368 gene silencing by RNA Effects 0.000 claims 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 208000017442 Retinal disease Diseases 0.000 claims 7
- -1 heterocycle compound Chemical class 0.000 claims 7
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 7
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 6
- 230000000295 complement effect Effects 0.000 claims 6
- 125000006165 cyclic alkyl group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000003367 polycyclic group Chemical group 0.000 claims 6
- 229920001184 polypeptide Polymers 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 102000004196 processed proteins & peptides Human genes 0.000 claims 6
- 108090000765 processed proteins & peptides Proteins 0.000 claims 6
- 230000002207 retinal effect Effects 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 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 5
- 108091028043 Nucleic acid sequence Proteins 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 239000004005 microsphere Substances 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 239000007788 liquid Substances 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- 125000004450 alkenylene group Chemical group 0.000 claims 3
- 125000003275 alpha amino acid group Chemical group 0.000 claims 3
- 239000005557 antagonist Substances 0.000 claims 3
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- 125000005017 substituted alkenyl group Chemical group 0.000 claims 3
- 125000005156 substituted alkylene group Chemical group 0.000 claims 3
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- 102000001706 Immunoglobulin Fab Fragments Human genes 0.000 claims 2
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- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 125000004419 alkynylene group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 239000002576 chemokine receptor CXCR4 antagonist Substances 0.000 claims 2
- 229940121384 cxc chemokine receptor type 4 (cxcr4) antagonist Drugs 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 239000012634 fragment Substances 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 108020004999 messenger RNA Proteins 0.000 claims 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 239000003981 vehicle Substances 0.000 claims 2
- YNAQHHIFLRWASS-JDSVYEKJSA-N (2r)-2-amino-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-3-(1h-imidazol-5-yl)propanamide Chemical compound C([C@@H](N)C(=O)NCCC1N(CCCC1NC=1N=C(C=CN=1)N1CCCCCC1)C1CCCCC1)C1=CNC=N1 YNAQHHIFLRWASS-JDSVYEKJSA-N 0.000 claims 1
- LPPBSZCRUGORCI-JMYZALGVSA-N (2r)-2-amino-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-3-(4-hydroxyphenyl)propanamide Chemical compound C([C@@H](N)C(=O)NCCC1N(CCCC1NC=1N=C(C=CN=1)N1CCCCCC1)C1CCCCC1)C1=CC=C(O)C=C1 LPPBSZCRUGORCI-JMYZALGVSA-N 0.000 claims 1
- YNAQHHIFLRWASS-IHSPPPAMSA-N (2s)-2-amino-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-3-(1h-imidazol-5-yl)propanamide Chemical compound C([C@H](N)C(=O)NCCC1N(CCCC1NC=1N=C(C=CN=1)N1CCCCCC1)C1CCCCC1)C1=CNC=N1 YNAQHHIFLRWASS-IHSPPPAMSA-N 0.000 claims 1
- VSJZWDXZUNQTBO-BOMBAVFCSA-N (2s)-2-amino-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-4-hydroxybutanamide Chemical compound OCC[C@H](N)C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 VSJZWDXZUNQTBO-BOMBAVFCSA-N 0.000 claims 1
- HQGRTAMXYWZZOR-JNLGVIEDSA-N (2s)-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]piperidine-2-carboxamide Chemical compound O=C([C@H]1NCCCC1)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 HQGRTAMXYWZZOR-JNLGVIEDSA-N 0.000 claims 1
- SDFYFIRUYZGZPG-GMUMFXLYSA-N (3r)-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]piperidine-3-carboxamide Chemical compound O=C([C@H]1CNCCC1)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 SDFYFIRUYZGZPG-GMUMFXLYSA-N 0.000 claims 1
- VMVKHCSARBZILS-PBGLPUTKSA-N (3r)-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]pyrrolidine-3-carboxamide Chemical compound O=C([C@H]1CNCC1)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 VMVKHCSARBZILS-PBGLPUTKSA-N 0.000 claims 1
- SDFYFIRUYZGZPG-XPWZEYHZSA-N (3s)-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]piperidine-3-carboxamide Chemical compound O=C([C@@H]1CNCCC1)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 SDFYFIRUYZGZPG-XPWZEYHZSA-N 0.000 claims 1
- APQRNAUXFIHFMW-BSSNWTCHSA-N (3s)-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpyrrolidin-2-yl]ethyl]piperidine-3-carboxamide Chemical compound O=C([C@@H]1CNCCC1)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCN1C1CCCCC1 APQRNAUXFIHFMW-BSSNWTCHSA-N 0.000 claims 1
- CHRYTLTVYUCYQI-UHFFFAOYSA-N 2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]-n-[3-(dimethylamino)propyl]acetamide Chemical compound CN(C)CCCNC(=O)CC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 CHRYTLTVYUCYQI-UHFFFAOYSA-N 0.000 claims 1
- ZCLZWGUQQLPRRR-UHFFFAOYSA-N 2-amino-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-2-methylpropanamide Chemical compound CC(C)(N)C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 ZCLZWGUQQLPRRR-UHFFFAOYSA-N 0.000 claims 1
- ZJTGTOMHLFLFHX-FOPBOCKXSA-N 4-[(1h-imidazol-2-ylmethylamino)methyl]-n-[(2s)-5-[(2-methylphenyl)methylamino]-1-[[(1s)-1-naphthalen-1-ylethyl]amino]-1-oxopentan-2-yl]benzamide Chemical compound C([C@@H](C(=O)N[C@@H](C)C=1C2=CC=CC=C2C=CC=1)NC(=O)C=1C=CC(CNCC=2NC=CN=2)=CC=1)CCNCC1=CC=CC=C1C ZJTGTOMHLFLFHX-FOPBOCKXSA-N 0.000 claims 1
- 108010061299 CXCR4 Receptors Proteins 0.000 claims 1
- 102000012000 CXCR4 Receptors Human genes 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
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- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- HPXRVTGHNJAIIH-UHFFFAOYSA-N cyclohexanol Chemical compound OC1CCCCC1 HPXRVTGHNJAIIH-UHFFFAOYSA-N 0.000 claims 1
- 239000000539 dimer Substances 0.000 claims 1
- 239000013604 expression vector Substances 0.000 claims 1
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 150000002391 heterocyclic compounds Chemical class 0.000 claims 1
- 125000005113 hydroxyalkoxy group Chemical group 0.000 claims 1
- 238000011065 in-situ storage Methods 0.000 claims 1
- 230000002452 interceptive effect Effects 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- LRGPGXCWFGEZDS-UHFFFAOYSA-N n-(2-aminoethyl)-2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]acetamide Chemical compound NCCNC(=O)CC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 LRGPGXCWFGEZDS-UHFFFAOYSA-N 0.000 claims 1
- NICFYINMVCBKEL-UHFFFAOYSA-N n-(2-aminoethyl)-n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)N(CCN)CCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 NICFYINMVCBKEL-UHFFFAOYSA-N 0.000 claims 1
- ZXMJOQZMYUGRHP-UHFFFAOYSA-N n-(3-aminopropyl)-2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]acetamide Chemical compound NCCCNC(=O)CC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 ZXMJOQZMYUGRHP-UHFFFAOYSA-N 0.000 claims 1
- AUXZVEBWKFOFQU-UHFFFAOYSA-N n-(4-aminobutyl)-2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]acetamide Chemical compound NCCCCNC(=O)CC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 AUXZVEBWKFOFQU-UHFFFAOYSA-N 0.000 claims 1
- FYYOLKFRSBAUGY-LEWJYISDSA-N n-[(2r,3s)-2-(3-aminopropyl)-1-cyclohexylpyrrolidin-3-yl]-4-(azepan-1-yl)pyrimidin-2-amine Chemical compound C([C@@H]([C@H]1CCCN)NC=2N=C(C=CN=2)N2CCCCCC2)CN1C1CCCCC1 FYYOLKFRSBAUGY-LEWJYISDSA-N 0.000 claims 1
- FYYOLKFRSBAUGY-UHFFFAOYSA-N n-[2-(3-aminopropyl)-1-cyclohexylpyrrolidin-3-yl]-4-(azepan-1-yl)pyrimidin-2-amine Chemical compound NCCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCN1C1CCCCC1 FYYOLKFRSBAUGY-UHFFFAOYSA-N 0.000 claims 1
- OWMARXKWPWKPDH-UHFFFAOYSA-N n-[2-[1-cyclohexyl-3-[(4-pyrrolidin-1-ylpyrimidin-2-yl)amino]piperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCC2)CCCN1C1CCCCC1 OWMARXKWPWKPDH-UHFFFAOYSA-N 0.000 claims 1
- OYINMNOEWYITSF-UHFFFAOYSA-N n-[2-[1-ethyl-3-[(4-piperidin-1-ylpyrimidin-2-yl)amino]piperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)NCCC1N(CC)CCCC1NC(N=1)=NC=CC=1N1CCCCC1 OYINMNOEWYITSF-UHFFFAOYSA-N 0.000 claims 1
- DQJBSVNHNLGMNF-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-(1,1-dioxothian-4-yl)piperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCS(=O)(=O)CC1 DQJBSVNHNLGMNF-UHFFFAOYSA-N 0.000 claims 1
- OWIVCJDVGKSZCY-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-(1,3-dihydroxypropan-2-yl)piperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)NCCC1N(C(CO)CO)CCCC1NC(N=1)=NC=CC=1N1CCCCCC1 OWIVCJDVGKSZCY-UHFFFAOYSA-N 0.000 claims 1
- PMIQFCJSLZHMQB-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-(1-oxothian-4-yl)piperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCS(=O)CC1 PMIQFCJSLZHMQB-UHFFFAOYSA-N 0.000 claims 1
- WOXPRFMBRXGQGJ-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-(3-hydroxypropyl)piperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)NCCC1N(CCCO)CCCC1NC(N=1)=NC=CC=1N1CCCCCC1 WOXPRFMBRXGQGJ-UHFFFAOYSA-N 0.000 claims 1
- VNEOBUHJYVLPCF-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-(oxan-4-yl)piperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCOCC1 VNEOBUHJYVLPCF-UHFFFAOYSA-N 0.000 claims 1
- ZDPBLMOKKGUWQH-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-(thian-4-yl)piperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCSCC1 ZDPBLMOKKGUWQH-UHFFFAOYSA-N 0.000 claims 1
- ZKZWNYUCHLGVKF-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-1-ethylpiperidine-4-carboxamide Chemical compound C1CN(CC)CCC1C(=O)NCCC1N(C2CCCCC2)CCCC1NC1=NC=CC(N2CCCCCC2)=N1 ZKZWNYUCHLGVKF-UHFFFAOYSA-N 0.000 claims 1
- BUBGSYJHKADCHW-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-1-propan-2-ylpiperidine-4-carboxamide Chemical compound C1CN(C(C)C)CCC1C(=O)NCCC1N(C2CCCCC2)CCCC1NC1=NC=CC(N2CCCCCC2)=N1 BUBGSYJHKADCHW-UHFFFAOYSA-N 0.000 claims 1
- JLZJIEIBNPFFGX-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-4-hydroxypiperidine-4-carboxamide Chemical compound N=1C=CC(N2CCCCCC2)=NC=1NC1CCCN(C2CCCCC2)C1CCNC(=O)C1(O)CCNCC1 JLZJIEIBNPFFGX-UHFFFAOYSA-N 0.000 claims 1
- JABUACRJVFRTHC-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-n-(2-hydroxyethyl)piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)N(CCO)CCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 JABUACRJVFRTHC-UHFFFAOYSA-N 0.000 claims 1
- VEPFSNSLGIQZHX-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-n-(2-methoxyethyl)piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)N(CCOC)CCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 VEPFSNSLGIQZHX-UHFFFAOYSA-N 0.000 claims 1
- OIGBLWTTXQMBAH-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-n-(oxan-4-yl)morpholine-2-carboxamide Chemical compound N=1C=CC(N2CCCCCC2)=NC=1NC1CCCN(C2CCCCC2)C1CCN(C1CCOCC1)C(=O)C1CNCCO1 OIGBLWTTXQMBAH-UHFFFAOYSA-N 0.000 claims 1
- BDDIRWMLJIEXOE-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]-n-(oxan-4-yl)piperidine-4-carboxamide Chemical compound N=1C=CC(N2CCCCCC2)=NC=1NC1CCCN(C2CCCCC2)C1CCN(C1CCOCC1)C(=O)C1CCNCC1 BDDIRWMLJIEXOE-UHFFFAOYSA-N 0.000 claims 1
- PMQJRNHBTBEQND-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]morpholine-2-carboxamide Chemical compound C1NCCOC1C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 PMQJRNHBTBEQND-UHFFFAOYSA-N 0.000 claims 1
- GLQSEOUKPYZFPG-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]piperidine-4-carboxamide Chemical compound C1CNCCC1C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 GLQSEOUKPYZFPG-UHFFFAOYSA-N 0.000 claims 1
- MDCVPERZCWKACQ-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpiperidin-2-yl]ethyl]pyridine-3-carboxamide Chemical compound C=1C=CN=CC=1C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCCN1C1CCCCC1 MDCVPERZCWKACQ-UHFFFAOYSA-N 0.000 claims 1
- JXZWSVUUKPQGQK-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-cyclohexylpyrrolidin-2-yl]ethyl]morpholine-2-carboxamide Chemical compound C1NCCOC1C(=O)NCCC1C(NC=2N=C(C=CN=2)N2CCCCCC2)CCN1C1CCCCC1 JXZWSVUUKPQGQK-UHFFFAOYSA-N 0.000 claims 1
- UWYZNDFRDXEQHY-UHFFFAOYSA-N n-[2-[3-[[4-(azepan-1-yl)pyrimidin-2-yl]amino]-1-propan-2-ylpiperidin-2-yl]ethyl]-1-ethylpiperidine-4-carboxamide Chemical compound C1CN(CC)CCC1C(=O)NCCC1N(C(C)C)CCCC1NC1=NC=CC(N2CCCCCC2)=N1 UWYZNDFRDXEQHY-UHFFFAOYSA-N 0.000 claims 1
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- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- JSPCTNUQYWIIOT-UHFFFAOYSA-N piperidine-1-carboxamide Chemical compound NC(=O)N1CCCCC1 JSPCTNUQYWIIOT-UHFFFAOYSA-N 0.000 claims 1
- 125000001500 prolyl group Chemical group [H]N1C([H])(C(=O)[*])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
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- 239000002336 ribonucleotide Substances 0.000 claims 1
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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2866—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for cytokines, lymphokines, interferons
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- C12N15/1136—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against growth factors, growth regulators, cytokines, lymphokines or hormones
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- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
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- C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
- C12N15/1138—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against receptors or cell surface proteins
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- A61K48/00—Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
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| KR20060129246A (ko) | 2003-12-05 | 2006-12-15 | 컴파운드 쎄라퓨틱스, 인크. | 타입 2 혈관 내피 성장 인자 수용체의 억제제 |
| JP5272408B2 (ja) * | 2005-02-25 | 2013-08-28 | 小野薬品工業株式会社 | 含窒素複素環化合物およびその医薬用途 |
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| CA2670471A1 (en) | 2006-11-22 | 2008-06-05 | Adnexus, A Bristol-Myers Squibb R&D Company (A Delaware Corporation) | Targeted therapeutics based on engineered proteins for tyrosine kinases receptors, including igf-ir |
| US11078262B2 (en) * | 2007-04-30 | 2021-08-03 | Allergan, Inc. | High viscosity macromolecular compositions for treating ocular conditions |
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-
2007
- 2007-02-02 BR BRPI0707446-8A patent/BRPI0707446A2/pt not_active Application Discontinuation
- 2007-02-02 EP EP11177758A patent/EP2407171A3/en not_active Ceased
- 2007-02-02 AU AU2007293169A patent/AU2007293169A1/en not_active Abandoned
- 2007-02-02 EP EP11177757A patent/EP2397148A3/en not_active Withdrawn
- 2007-02-02 EP EP07848839A patent/EP1993584B1/en active Active
- 2007-02-02 JP JP2008552923A patent/JP2009531283A/ja active Pending
- 2007-02-02 ES ES07848839T patent/ES2385924T3/es active Active
- 2007-02-02 WO PCT/IB2007/003262 patent/WO2008029276A2/en not_active Ceased
- 2007-02-02 US US11/670,883 patent/US7964191B2/en active Active
- 2007-02-02 CA CA002640080A patent/CA2640080A1/en not_active Abandoned
-
2011
- 2011-06-10 US US13/158,084 patent/US20120003275A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2008029276A2 (en) | 2008-03-13 |
| JP2009531283A (ja) | 2009-09-03 |
| EP2397148A3 (en) | 2012-04-25 |
| US20120003275A1 (en) | 2012-01-05 |
| US7964191B2 (en) | 2011-06-21 |
| ES2385924T3 (es) | 2012-08-03 |
| EP1993584B1 (en) | 2012-05-30 |
| AU2007293169A1 (en) | 2008-03-13 |
| EP2407171A3 (en) | 2012-04-11 |
| WO2008029276A8 (en) | 2009-08-06 |
| WO2008029276A3 (en) | 2008-12-04 |
| EP2397148A2 (en) | 2011-12-21 |
| EP2407171A2 (en) | 2012-01-18 |
| EP1993584A2 (en) | 2008-11-26 |
| BRPI0707446A2 (pt) | 2011-05-03 |
| US20070203089A1 (en) | 2007-08-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Discontinued |
Effective date: 20140930 |