JP2011513245A5

JP2011513245A5 -

Download PDF

Info

Publication number: JP2011513245A5
Authority: JP; Japan
Prior art keywords: methyl; oxo; diazepan; diphenylethyl; naphthoamide
Prior art date: 2009-02-27
Legal status : Granted

Application number

JP2010547918A

Other languages

English (en)

Japanese (ja)

Other versions

JP2011513245A (ja

JP5503558B2 (ja

Filing date

2009-02-27

Publication date

2014-02-20

2009-02-24 Priority claimed from US12/391,748 external-priority patent/US8377925B2/en

2009-02-27 Application filed filed Critical

2009-02-27 Priority claimed from PCT/AU2009/000231 external-priority patent/WO2009105824A1/en

2011-04-28 Publication of JP2011513245A publication Critical patent/JP2011513245A/ja

2014-02-20 Publication of JP2011513245A5 publication Critical patent/JP2011513245A5/ja

2014-05-28 Application granted granted Critical

2014-05-28 Publication of JP5503558B2 publication Critical patent/JP5503558B2/ja

Status Expired - Fee Related legal-status Critical Current

2029-02-27 Anticipated expiration legal-status Critical

Links

125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 236
-1 OR 20 Chemical compound 0.000 claims 134
KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 110
HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical compound NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 claims 31
125000000579 2,2-diphenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(C1=C([H])C([H])=C([H])C([H])=C1[H])C([H])([H])* 0.000 claims 25
125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 25
125000003118 aryl group Chemical group 0.000 claims 21
125000000217 alkyl group Chemical group 0.000 claims 20
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 19
125000001072 heteroaryl group Chemical group 0.000 claims 19
150000001875 compounds Chemical class 0.000 claims 18
239000008194 pharmaceutical composition Substances 0.000 claims 17
125000000592 heterocycloalkyl group Chemical group 0.000 claims 16
229910052799 carbon Inorganic materials 0.000 claims 15
DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 14
125000000753 cycloalkyl group Chemical group 0.000 claims 12
APEJMQOBVMLION-UHFFFAOYSA-N cinnamamide Chemical compound NC(=O)C=CC1=CC=CC=C1 APEJMQOBVMLION-UHFFFAOYSA-N 0.000 claims 10
125000004429 atom Chemical group 0.000 claims 8
125000004404 heteroalkyl group Chemical group 0.000 claims 8
125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 7
125000003974 3-carbamimidamidopropyl group Chemical group C(N)(=N)NCCC* 0.000 claims 7
229910052736 halogen Inorganic materials 0.000 claims 7
150000002367 halogens Chemical class 0.000 claims 7
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
150000003839 salts Chemical class 0.000 claims 7
125000003342 alkenyl group Chemical group 0.000 claims 6
239000000651 prodrug Substances 0.000 claims 5
229940002612 prodrug Drugs 0.000 claims 5
125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 4
125000000304 alkynyl group Chemical group 0.000 claims 4
LKYNGTHMKCTTQC-UHFFFAOYSA-N 1,2-oxazole-3-carboxamide Chemical compound NC(=O)C=1C=CON=1 LKYNGTHMKCTTQC-UHFFFAOYSA-N 0.000 claims 3
125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims 3
125000006176 2-ethylbutyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 claims 3
241000124008 Mammalia Species 0.000 claims 3
125000004122 cyclic group Chemical group 0.000 claims 3
PNZXMIKHJXIPEK-UHFFFAOYSA-N cyclohexanecarboxamide Chemical compound NC(=O)C1CCCCC1 PNZXMIKHJXIPEK-UHFFFAOYSA-N 0.000 claims 3
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
125000000623 heterocyclic group Chemical group 0.000 claims 3
RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
229910052757 nitrogen Inorganic materials 0.000 claims 3
125000004433 nitrogen atom Chemical group N* 0.000 claims 3
PWXPFYVNYKVJBW-ZZXKWVIFSA-N (e)-3-(4-chlorophenyl)prop-2-enamide Chemical compound NC(=O)\C=C\C1=CC=C(Cl)C=C1 PWXPFYVNYKVJBW-ZZXKWVIFSA-N 0.000 claims 2
125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 2
125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 2
208000002874 Acne Vulgaris Diseases 0.000 claims 2
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
102000030612 Melanocortin 5 receptor Human genes 0.000 claims 2
108010088565 Melanocortin 5 receptor Proteins 0.000 claims 2
KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 2
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
206010000496 acne Diseases 0.000 claims 2
125000003545 alkoxy group Chemical group 0.000 claims 2
125000005605 benzo 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
125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
150000001721 carbon Chemical group 0.000 claims 2
125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
230000000694 effects Effects 0.000 claims 2
239000012634 fragment Substances 0.000 claims 2
125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
HFJKZDDMHRPINP-WNJJXGMVSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1h-indole-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1NC2=CC=CC=C2C=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 HFJKZDDMHRPINP-WNJJXGMVSA-N 0.000 claims 2
WBKKFYBGSRVUDI-XCZPVHLTSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]benzamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCNC(=N)N)NC(=O)C1=CC=CC=C1 WBKKFYBGSRVUDI-XCZPVHLTSA-N 0.000 claims 2
RMHJJUOPOWPRBP-UHFFFAOYSA-N naphthalene-1-carboxamide Chemical compound C1=CC=C2C(C(=O)N)=CC=CC2=C1 RMHJJUOPOWPRBP-UHFFFAOYSA-N 0.000 claims 2
125000001624 naphthyl group Chemical group 0.000 claims 2
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
208000008742 seborrheic dermatitis Diseases 0.000 claims 2
125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
XAEJSKLIFZIGGW-RUHGTMQNSA-N (3r)-n-[[(3s,5s)-1-(2,2-diphenylethyl)-3-[3-[(n'-methylcarbamimidoyl)amino]propyl]-2-oxo-1,4-diazepan-5-yl]methyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide Chemical compound C([C@@H](CNC(=O)[C@@H]1NCC2=CC=CC=C2C1)N[C@H](C1=O)CCCNC(=N)NC)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 XAEJSKLIFZIGGW-RUHGTMQNSA-N 0.000 claims 1
VHRJTLUSJYUVEM-RUHGTMQNSA-N (3r)-n-[[(3s,5s)-3-(4-aminobutyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide Chemical compound C([C@@H](CNC(=O)[C@@H]1NCC2=CC=CC=C2C1)N[C@H](C1=O)CCCCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 VHRJTLUSJYUVEM-RUHGTMQNSA-N 0.000 claims 1
SELTWCXBYXUAHF-LHGWWSMPSA-N (3r)-n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide Chemical compound C([C@@H](CNC(=O)[C@@H]1NCC2=CC=CC=C2C1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 SELTWCXBYXUAHF-LHGWWSMPSA-N 0.000 claims 1
QHDPVOTZDXQHFB-OGXMWTIWSA-N (3r)-n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide Chemical compound C([C@@H](CNC(=O)[C@@H]1OC2=CC=CC=C2OC1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 QHDPVOTZDXQHFB-OGXMWTIWSA-N 0.000 claims 1
VHRJTLUSJYUVEM-GOBOWQCMSA-N (3s)-n-[[(3s,5s)-3-(4-aminobutyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide Chemical compound C([C@@H](CNC(=O)[C@H]1NCC2=CC=CC=C2C1)N[C@H](C1=O)CCCCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 VHRJTLUSJYUVEM-GOBOWQCMSA-N 0.000 claims 1
SELTWCXBYXUAHF-ASVWTAOFSA-N (3s)-n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide Chemical compound C([C@@H](CNC(=O)[C@H]1NCC2=CC=CC=C2C1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 SELTWCXBYXUAHF-ASVWTAOFSA-N 0.000 claims 1
DXEIOFDUNMIKQD-ZQAZVOLISA-N (3s,5s)-5-[[(3,4-dichlorophenyl)methylamino]methyl]-1-(2,2-diphenylethyl)-3-(2-piperidin-1-ylethyl)-1,4-diazepan-2-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC[C@H]1N[C@@H](CCN2CCCCC2)C(=O)N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 DXEIOFDUNMIKQD-ZQAZVOLISA-N 0.000 claims 1
AOIVVCOHGHEUTB-AZIXZEHSSA-N (3s,5s)-5-[[(3,4-dichlorophenyl)methylamino]methyl]-1-[(2s)-2-phenylbutyl]-3-(2-piperidin-1-ylethyl)-1,4-diazepan-2-one Chemical compound C([C@@H]1CCN(C([C@H](CCN2CCCCC2)N1)=O)C[C@@H](CC)C=1C=CC=CC=1)NCC1=CC=C(Cl)C(Cl)=C1 AOIVVCOHGHEUTB-AZIXZEHSSA-N 0.000 claims 1
125000004641 (C1-C12) haloalkyl group Chemical group 0.000 claims 1
JSFIMWWDJRWMHJ-VOTSOKGWSA-N (e)-3-(4-methylphenyl)prop-2-enamide Chemical compound CC1=CC=C(\C=C\C(N)=O)C=C1 JSFIMWWDJRWMHJ-VOTSOKGWSA-N 0.000 claims 1
ZCVUMSAODQOJOW-BGMRFITDSA-N (e)-n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3-(4-fluorophenyl)-n-methylprop-2-enamide Chemical compound C([C@H](N[C@@H](CCCN)C1=O)CN(C)C(=O)\C=C\C=2C=CC(F)=CC=2)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 ZCVUMSAODQOJOW-BGMRFITDSA-N 0.000 claims 1
PDMNGEJGQQMGAS-VQSCXVRDSA-N (e)-n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-methyl-3-phenylprop-2-enamide Chemical compound C([C@H]1N[C@@H](CCCNC(N)=N)C(=O)N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)NC(=O)C(/C)=C/C1=CC=CC=C1 PDMNGEJGQQMGAS-VQSCXVRDSA-N 0.000 claims 1
RDDLSTIRVULBOT-KKLGXJKSSA-N (e)-n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3-(2-methylphenyl)prop-2-enamide Chemical compound CC1=CC=CC=C1\C=C\C(=O)NC[C@H]1N[C@@H](CCCNC(N)=N)C(=O)N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RDDLSTIRVULBOT-KKLGXJKSSA-N 0.000 claims 1
HDDGFPOMMDMKBV-HCRUOQKOSA-N (z)-n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-fluoro-3-phenylprop-2-enamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCNC(=N)N)NC(=O)C(\F)=C\C1=CC=CC=C1 HDDGFPOMMDMKBV-HCRUOQKOSA-N 0.000 claims 1
KZKRRZFCAYOXQE-UHFFFAOYSA-N 1$l^{2}-azinane Chemical group C1CC[N]CC1 KZKRRZFCAYOXQE-UHFFFAOYSA-N 0.000 claims 1
KDWQLICBSFIDRM-UHFFFAOYSA-N 1,1,1-trifluoropropane Chemical compound CCC(F)(F)F KDWQLICBSFIDRM-UHFFFAOYSA-N 0.000 claims 1
LXYUSXFFUYVKOV-UHFFFAOYSA-N 1,3-dioxole-4-carboxamide Chemical compound NC(=O)C1=COCO1 LXYUSXFFUYVKOV-UHFFFAOYSA-N 0.000 claims 1
WHOZDLQKWBNXOC-UHFFFAOYSA-N 1,4-dioxine-2-carboxamide Chemical compound NC(=O)C1=COC=CO1 WHOZDLQKWBNXOC-UHFFFAOYSA-N 0.000 claims 1
125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 1
NAOPCNXRXLBSFV-NYDCQLBNSA-N 2-[3-[(2s,7s)-4-(2,2-diphenylethyl)-7-[(naphthalen-2-ylsulfonylamino)methyl]-3-oxo-1,4-diazepan-2-yl]propyl]guanidine Chemical compound C([C@@H](CNS(=O)(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 NAOPCNXRXLBSFV-NYDCQLBNSA-N 0.000 claims 1
125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
125000004493 2-methylbut-1-yl group Chemical group CC(C*)CC 0.000 claims 1
125000005916 2-methylpentyl group Chemical group 0.000 claims 1
GTKIGDZXPDCIKR-UHFFFAOYSA-N 2-phenylbenzamide Chemical compound NC(=O)C1=CC=CC=C1C1=CC=CC=C1 GTKIGDZXPDCIKR-UHFFFAOYSA-N 0.000 claims 1
125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
125000006512 3,4-dichlorobenzyl group Chemical group [H]C1=C(Cl)C(Cl)=C([H])C(=C1[H])C([H])([H])* 0.000 claims 1
125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 1
125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims 1
LUQVCHRDAGWYMG-UHFFFAOYSA-N 4-phenylbenzamide Chemical compound C1=CC(C(=O)N)=CC=C1C1=CC=CC=C1 LUQVCHRDAGWYMG-UHFFFAOYSA-N 0.000 claims 1
125000004539 5-benzimidazolyl group Chemical group N1=CNC2=C1C=CC(=C2)* 0.000 claims 1
AHZLHBIQAMKSTD-CDZUIXILSA-N 6-amino-n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(N)=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 AHZLHBIQAMKSTD-CDZUIXILSA-N 0.000 claims 1
CKRUBELSJRPQAA-CDZUIXILSA-N 6-bromo-n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(Br)=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 CKRUBELSJRPQAA-CDZUIXILSA-N 0.000 claims 1
JPDQABHVCKKMON-HTXOAEFJSA-N 6-chloro-n-[[(3s)-2-oxo-1-(2-phenylbutyl)-3-(1-propan-2-ylpiperidin-4-yl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1([C@@H]2NC(CNC(=O)C=3C=C4C=CC(Cl)=CC4=CC=3)CCN(C2=O)CC(CC)C=2C=CC=CC=2)CCN(C(C)C)CC1 JPDQABHVCKKMON-HTXOAEFJSA-N 0.000 claims 1
RAYWGUBSGQJFLB-GIWKVKTRSA-N 6-chloro-n-[[(3s,5s)-1-(2,2-diphenylethyl)-2-oxo-3-(2-piperidin-1-ylethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCN1CCCCC1)C1=O)CNC(=O)C2=CC3=CC=C(C=C3C=C2)Cl)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 RAYWGUBSGQJFLB-GIWKVKTRSA-N 0.000 claims 1
KTMMPQNVEBKYCG-LRHLLKFHSA-N 6-chloro-n-[[(3s,5s)-1-(2,2-diphenylethyl)-3-(2-morpholin-4-ylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCN1CCOCC1)C1=O)CNC(=O)C2=CC3=CC=C(C=C3C=C2)Cl)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 KTMMPQNVEBKYCG-LRHLLKFHSA-N 0.000 claims 1
XITCVVZMRPNABW-YTMVLYRLSA-N 6-chloro-n-[[(3s,5s)-1-[(2,4-dichlorophenyl)methyl]-2-oxo-3-(2-piperidin-1-ylethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound ClC1=CC(Cl)=CC=C1CN1C(=O)[C@H](CCN2CCCCC2)N[C@H](CNC(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CC1 XITCVVZMRPNABW-YTMVLYRLSA-N 0.000 claims 1
VECSQBGFYNJZBA-OIFPXGRLSA-N 6-chloro-n-[[(3s,5s)-1-[(2r)-2-ethyl-3-methylbutyl]-2-oxo-3-(2-piperidin-1-ylethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H]1N[C@H](CNC(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CCN(C1=O)C[C@H](CC)C(C)C)CN1CCCCC1 VECSQBGFYNJZBA-OIFPXGRLSA-N 0.000 claims 1
VECSQBGFYNJZBA-MGONOCMRSA-N 6-chloro-n-[[(3s,5s)-1-[(2s)-2-ethyl-3-methylbutyl]-2-oxo-3-(2-piperidin-1-ylethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H]1N[C@H](CNC(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CCN(C1=O)C[C@@H](CC)C(C)C)CN1CCCCC1 VECSQBGFYNJZBA-MGONOCMRSA-N 0.000 claims 1
DEPCHJKRPDKDGR-VMPREFPWSA-N 6-chloro-n-[[(3s,5s)-1-[(3,5-dichlorophenyl)methyl]-2-oxo-3-(2-piperidin-1-ylethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCN1CCCCC1)C1=O)CNC(=O)C2=CC3=CC=C(C=C3C=C2)Cl)CN1CC1=CC(Cl)=CC(Cl)=C1 DEPCHJKRPDKDGR-VMPREFPWSA-N 0.000 claims 1
KXPZUJMIXREJSZ-NSOVKSMOSA-N 6-chloro-n-[[(3s,5s)-1-[(3,5-dichlorophenyl)methyl]-3-(2-morpholin-4-ylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCN1CCOCC1)C1=O)CNC(=O)C2=CC3=CC=C(C=C3C=C2)Cl)CN1CC1=CC(Cl)=CC(Cl)=C1 KXPZUJMIXREJSZ-NSOVKSMOSA-N 0.000 claims 1
IXZQVROIFOTPNN-STQWGSIPSA-N 6-chloro-n-[[(3s,5s)-2-oxo-1-[(2s)-2-phenylbutyl]-3-[2-(propan-2-ylsulfonylamino)ethyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1([C@@H](CN2C([C@H](CCNS(=O)(=O)C(C)C)N[C@H](CNC(=O)C=3C=C4C=CC(Cl)=CC4=CC=3)CC2)=O)CC)=CC=CC=C1 IXZQVROIFOTPNN-STQWGSIPSA-N 0.000 claims 1
XKIDWGAOZSALDO-HDXYBINASA-N 6-chloro-n-[[(3s,5s)-2-oxo-3-(2-piperidin-1-ylethyl)-1-[(2r)-2-thiophen-3-ylbutyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H]1N[C@H](CNC(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CCN(C1=O)C[C@H](CC)C1=CSC=C1)CN1CCCCC1 XKIDWGAOZSALDO-HDXYBINASA-N 0.000 claims 1
XKIDWGAOZSALDO-STQWGSIPSA-N 6-chloro-n-[[(3s,5s)-2-oxo-3-(2-piperidin-1-ylethyl)-1-[(2s)-2-thiophen-3-ylbutyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H]1N[C@H](CNC(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CCN(C1=O)C[C@@H](CC)C1=CSC=C1)CN1CCCCC1 XKIDWGAOZSALDO-STQWGSIPSA-N 0.000 claims 1
UNIUHTXBGLCPAQ-DJDPXSJISA-N 6-chloro-n-[[(3s,5s)-3-(2-methyl-2-piperidin-1-ylpropyl)-2-oxo-1-[(2s)-2-phenylbutyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H]1N[C@H](CNC(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CCN(C1=O)C[C@@H](CC)C=1C=CC=CC=1)C(C)(C)N1CCCCC1 UNIUHTXBGLCPAQ-DJDPXSJISA-N 0.000 claims 1
MXQULUQGATWCNX-PBXQCXKZSA-N 6-chloro-n-[[(3s,5s)-3-[(diaminomethylideneamino)methyl]-2-oxo-1-[(2s)-2-phenylbutyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1([C@@H](CN2C([C@H](CNC(N)=N)N[C@H](CNC(=O)C=3C=C4C=CC(Cl)=CC4=CC=3)CC2)=O)CC)=CC=CC=C1 MXQULUQGATWCNX-PBXQCXKZSA-N 0.000 claims 1
ILSJFQAVPNGFPA-COWIPBKQSA-N 6-chloro-n-[[3-(1-ethylpiperidin-4-yl)-2-oxo-1-[(2s)-2-phenylbutyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CC)C=1C=CC=CC=1)N(C1=O)CCC(CNC(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)NC1C1CCN(CC)CC1 ILSJFQAVPNGFPA-COWIPBKQSA-N 0.000 claims 1
JOYRKODLDBILNP-UHFFFAOYSA-N Ethyl urethane Chemical compound CCOC(N)=O JOYRKODLDBILNP-UHFFFAOYSA-N 0.000 claims 1
LKJPYSCBVHEWIU-UHFFFAOYSA-N N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide Chemical compound C=1C=C(C#N)C(C(F)(F)F)=CC=1NC(=O)C(O)(C)CS(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-UHFFFAOYSA-N 0.000 claims 1
MSTAOBRZXXUMJU-TXIPYEPDSA-N N-[[(3S,5S)-3-[3-(diaminomethylideneamino)propyl]-1-(2-oxo-1-phenylethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound N(C(=N)N)CCC[C@H]1CN(CC[C@H](N1)CNC(=O)C1=CC2=CC=CC=C2C=C1)C(C=O)C1=CC=CC=C1 MSTAOBRZXXUMJU-TXIPYEPDSA-N 0.000 claims 1
PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 1
WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
206010039792 Seborrhoea Diseases 0.000 claims 1
206010039793 Seborrhoeic dermatitis Diseases 0.000 claims 1
XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 1
125000005336 allyloxy group Chemical group 0.000 claims 1
125000003275 alpha amino acid group Chemical group 0.000 claims 1
125000003725 azepanyl group Chemical group 0.000 claims 1
125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 1
125000002393 azetidinyl group Chemical group 0.000 claims 1
235000010290 biphenyl Nutrition 0.000 claims 1
239000004305 biphenyl Substances 0.000 claims 1
229910052794 bromium Inorganic materials 0.000 claims 1
GTCAXTIRRLKXRU-UHFFFAOYSA-N carbamic acid methyl ester Natural products COC(N)=O GTCAXTIRRLKXRU-UHFFFAOYSA-N 0.000 claims 1
239000004202 carbamide Substances 0.000 claims 1
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
229910052801 chlorine Inorganic materials 0.000 claims 1
125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
230000002222 downregulating effect Effects 0.000 claims 1
229910052731 fluorine Inorganic materials 0.000 claims 1
125000004438 haloalkoxy group Chemical group 0.000 claims 1
125000001188 haloalkyl group Chemical group 0.000 claims 1
125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
125000005842 heteroatom Chemical group 0.000 claims 1
125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
125000002249 indol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([*])=C([H])C2=C1[H] 0.000 claims 1
230000002401 inhibitory effect Effects 0.000 claims 1
229910052740 iodine Inorganic materials 0.000 claims 1
125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
SRJOCJYGOFTFLH-UHFFFAOYSA-N isonipecotic acid Chemical compound OC(=O)C1CCNCC1 SRJOCJYGOFTFLH-UHFFFAOYSA-N 0.000 claims 1
125000000555 isopropenyl group Chemical group [H]\C([H])=C(\*)C([H])([H])[H] 0.000 claims 1
125000004551 isoquinolin-3-yl group Chemical group C1=NC(=CC2=CC=CC=C12)* 0.000 claims 1
125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
125000002757 morpholinyl group Chemical group 0.000 claims 1
BQQWQJSSWRPXDB-PUPDPRJKSA-N n-[(1r)-1-[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]-2-naphthalen-2-ylethyl]acetamide Chemical compound C([C@H](N[C@@H](CCCNC(N)=N)C1=O)[C@@H](CC=2C=C3C=CC=CC3=CC=2)NC(=O)C)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 BQQWQJSSWRPXDB-PUPDPRJKSA-N 0.000 claims 1
DAZFBUPSURRZJX-IAPPQJPRSA-N n-[2-[(3s,5r)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]ethyl]benzamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCN)CNC(=O)C1=CC=CC=C1 DAZFBUPSURRZJX-IAPPQJPRSA-N 0.000 claims 1
PZKLIHADSFMOCW-BHYZAODMSA-N n-[2-[(3s,5r)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]ethyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CCNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 PZKLIHADSFMOCW-BHYZAODMSA-N 0.000 claims 1
QOIYHTMMIORSMO-PJJRWXIWSA-N n-[[(3s,5s)-1-(1-adamantylmethyl)-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1CN(CC23CC4CC(CC(C4)C2)C3)C(=O)[C@H](CCCNC(=N)N)N[C@@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 QOIYHTMMIORSMO-PJJRWXIWSA-N 0.000 claims 1
ANTSJPZYEYUKQW-LRHLLKFHSA-N n-[[(3s,5s)-1-(2,2-diphenylethyl)-2-oxo-3-(piperidin-1-ylmethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CN1CCCCC1)C1=O)CNC(=O)C=2C=C3C=CC=CC3=CC=2)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 ANTSJPZYEYUKQW-LRHLLKFHSA-N 0.000 claims 1
CSVKOBXXZWQJFH-TWJUONSBSA-N n-[[(3s,5s)-1-(2,2-diphenylethyl)-2-oxo-3-[2-(propan-2-ylamino)ethyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCNC(C)C)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 CSVKOBXXZWQJFH-TWJUONSBSA-N 0.000 claims 1
KBNVEJCZPFDCIH-LRHLLKFHSA-N n-[[(3s,5s)-1-(2,2-diphenylethyl)-2-oxo-3-[3-(propan-2-ylamino)propyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(C)C)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 KBNVEJCZPFDCIH-LRHLLKFHSA-N 0.000 claims 1
VLSQOCSIELJZCT-GIWKVKTRSA-N n-[[(3s,5s)-1-(2,2-diphenylethyl)-2-oxo-3-[4-(propan-2-ylamino)butyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCCNC(C)C)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 VLSQOCSIELJZCT-GIWKVKTRSA-N 0.000 claims 1
WUFPAWGDVHSNQX-WEZIJMHWSA-N n-[[(3s,5s)-1-(2,2-diphenylethyl)-3-[3-[(n'-methylcarbamimidoyl)amino]propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)NC)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 WUFPAWGDVHSNQX-WEZIJMHWSA-N 0.000 claims 1
KHSZVGIVMCAAEX-UIOOFZCWSA-N n-[[(3s,5s)-1-(2-cyclohexylethyl)-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CCC1CCCCC1 KHSZVGIVMCAAEX-UIOOFZCWSA-N 0.000 claims 1
BDLQPOKUIAQPOP-NSOVKSMOSA-N n-[[(3s,5s)-1-(2-ethylbutyl)-2-oxo-3-(2-piperidin-1-ylethyl)-1,4-diazepan-5-yl]methyl]-6-fluoronaphthalene-2-carboxamide Chemical compound C([C@@H]1N[C@H](CNC(=O)C=2C=C3C=CC(F)=CC3=CC=2)CCN(C1=O)CC(CC)CC)CN1CCCCC1 BDLQPOKUIAQPOP-NSOVKSMOSA-N 0.000 claims 1
DTOOUBDUVXWTKR-NSOVKSMOSA-N n-[[(3s,5s)-1-(2-ethylbutyl)-2-oxo-3-(2-piperidin-1-ylethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H]1N[C@H](CNC(=O)C=2C=C3C=CC=CC3=CC=2)CCN(C1=O)CC(CC)CC)CN1CCCCC1 DTOOUBDUVXWTKR-NSOVKSMOSA-N 0.000 claims 1
LXVAANGAZWTPKK-SVBPBHIXSA-N n-[[(3s,5s)-1-(cyclohexylmethyl)-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]-4-phenylbenzamide Chemical compound C([C@H]1N[C@H](C(N(CC2CCCCC2)CC1)=O)CCCNC(=N)N)NC(=O)C(C=C1)=CC=C1C1=CC=CC=C1 LXVAANGAZWTPKK-SVBPBHIXSA-N 0.000 claims 1
OHGAJPCQASYOGK-DQEYMECFSA-N n-[[(3s,5s)-1-(cyclohexylmethyl)-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC1CCCCC1 OHGAJPCQASYOGK-DQEYMECFSA-N 0.000 claims 1
ADKVQJADKHYOED-UPVQGACJSA-N n-[[(3s,5s)-1-(cyclohexylmethyl)-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]quinoline-3-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=NC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC1CCCCC1 ADKVQJADKHYOED-UPVQGACJSA-N 0.000 claims 1
IZBHZOBLFBQQPY-SVBPBHIXSA-N n-[[(3s,5s)-1-[(3,5-dichlorophenyl)methyl]-2-oxo-3-(pyrrolidin-1-ylmethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound ClC1=CC(Cl)=CC(CN2C([C@H](CN3CCCC3)N[C@H](CNC(=O)C=3C=C4C=CC=CC4=CC=3)CC2)=O)=C1 IZBHZOBLFBQQPY-SVBPBHIXSA-N 0.000 claims 1
VHKRXIDKQSHFJJ-DQEYMECFSA-N n-[[(3s,5s)-1-[(3-chloro-5-fluorophenyl)methyl]-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC1=CC(F)=CC(Cl)=C1 VHKRXIDKQSHFJJ-DQEYMECFSA-N 0.000 claims 1
ZLZLPEBYLQRVNZ-CDZUIXILSA-N n-[[(3s,5s)-1-[2,2-bis(4-fluorophenyl)ethyl]-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC(F)=CC=1)C1=CC=C(F)C=C1 ZLZLPEBYLQRVNZ-CDZUIXILSA-N 0.000 claims 1
UNHBDQDXOBLMTP-NHZFLZHXSA-N n-[[(3s,5s)-1-[2,2-bis(4-methoxyphenyl)ethyl]-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1=CC(OC)=CC=C1C(C=1C=CC(OC)=CC=1)CN1C(=O)[C@H](CCCNC(N)=N)N[C@H](CNC(=O)C=2C=C3C=CC=CC3=CC=2)CC1 UNHBDQDXOBLMTP-NHZFLZHXSA-N 0.000 claims 1
LLSPVLURZFRKQC-LIOFFLAUSA-N n-[[(3s,5s)-1-[2-(3-bicyclo[2.2.1]heptanyl)ethyl]-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1CN(CCC2C3CCC(C3)C2)C(=O)[C@H](CCCNC(=N)N)N[C@@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 LLSPVLURZFRKQC-LIOFFLAUSA-N 0.000 claims 1
WPCJZOUXSQEEEF-DQEYMECFSA-N n-[[(3s,5s)-1-benzyl-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC1=CC=CC=C1 WPCJZOUXSQEEEF-DQEYMECFSA-N 0.000 claims 1
RQAUICUAVHREBS-UPVQGACJSA-N n-[[(3s,5s)-1-cyclohexyl-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1C1CCCCC1 RQAUICUAVHREBS-UPVQGACJSA-N 0.000 claims 1
MQVWWDKVLLEGKD-VLIDNHJSSA-N n-[[(3s,5s)-2-oxo-1-(2-phenylbutyl)-3-(3-piperidin-1-ylpropyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H]1N[C@H](CNC(=O)C=2C=C3C=CC=CC3=CC=2)CCN(C1=O)CC(CC)C=1C=CC=CC=1)CCN1CCCCC1 MQVWWDKVLLEGKD-VLIDNHJSSA-N 0.000 claims 1
BWKKOIFSAZINTN-HOFKKMOUSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCN)NC(=O)C1=CC=C(Cl)C(Cl)=C1 BWKKOIFSAZINTN-HOFKKMOUSA-N 0.000 claims 1
BTIWBRIJMDPPKC-YTMVLYRLSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dimethylbenzamide Chemical compound C1=C(C)C(C)=CC=C1C(=O)NC[C@H]1N[C@@H](CCN)C(=O)N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 BTIWBRIJMDPPKC-YTMVLYRLSA-N 0.000 claims 1
HGIXWOZHCWCIOK-YTMVLYRLSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3-(4-chlorophenyl)propanamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCN)NC(=O)CCC1=CC=C(Cl)C=C1 HGIXWOZHCWCIOK-YTMVLYRLSA-N 0.000 claims 1
QDLJXAZKKOTFNI-BDYUSTAISA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3-(trifluoromethyl)benzamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCN)NC(=O)C1=CC=CC(C(F)(F)F)=C1 QDLJXAZKKOTFNI-BDYUSTAISA-N 0.000 claims 1
CBFIYCZMOUVLSR-BDYUSTAISA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-4-(trifluoromethyl)benzamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCN)NC(=O)C1=CC=C(C(F)(F)F)C=C1 CBFIYCZMOUVLSR-BDYUSTAISA-N 0.000 claims 1
SCRNPYIGTBTDKZ-SMCANUKXSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(Cl)=CC2=CC=1)N[C@H](C1=O)CCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 SCRNPYIGTBTDKZ-SMCANUKXSA-N 0.000 claims 1
IVQZHFPXELZMDW-SMCANUKXSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-fluoronaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(F)=CC2=CC=1)N[C@H](C1=O)CCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 IVQZHFPXELZMDW-SMCANUKXSA-N 0.000 claims 1
HUOQZTHEUHMEDW-SMCANUKXSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 HUOQZTHEUHMEDW-SMCANUKXSA-N 0.000 claims 1
HTBBNBWHLJVPTJ-BLFAFILHSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-cyclopropylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound O=C([C@H](CCN)N[C@H](CNC(=O)C=1C=C2C=CC(Cl)=CC2=CC=1)CC1)N1CC(CC)C1CC1 HTBBNBWHLJVPTJ-BLFAFILHSA-N 0.000 claims 1
CSVQQMRXTKTVBN-LPHOPBHVSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethyl-2-methylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(C)(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(Cl)C(Cl)=C1 CSVQQMRXTKTVBN-LPHOPBHVSA-N 0.000 claims 1
VFXJBQANOFFTLE-GOTSBHOMSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethyl-2-methylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(C)(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 VFXJBQANOFFTLE-GOTSBHOMSA-N 0.000 claims 1
NCOYGPIFNDMXCO-LXKGCQHHSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethyl-3-methylbut-3-enyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)C(C)=C)CC[C@H]1CNC(=O)C1=CC=C(Cl)C(Cl)=C1 NCOYGPIFNDMXCO-LXKGCQHHSA-N 0.000 claims 1
QJCVJUHQSMDVKK-JUQRWGLSSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethyl-3-methylbut-3-enyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)C(C)=C)CC[C@H]1CNC(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 QJCVJUHQSMDVKK-JUQRWGLSSA-N 0.000 claims 1
QGNFOMXXBDIGJR-LPHOPBHVSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(Cl)C(Cl)=C1 QGNFOMXXBDIGJR-LPHOPBHVSA-N 0.000 claims 1
IWXFBIJRILMYKC-LPHOPBHVSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3-chloro-4-fluorobenzamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(F)C(Cl)=C1 IWXFBIJRILMYKC-LPHOPBHVSA-N 0.000 claims 1
SFWBAROKYIEQQK-ICSRJNTNSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3-chloro-4-methylbenzamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(C)C(Cl)=C1 SFWBAROKYIEQQK-ICSRJNTNSA-N 0.000 claims 1
ZCQARZDWEORZBP-LPHOPBHVSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-4-chloro-3-fluorobenzamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(Cl)C(F)=C1 ZCQARZDWEORZBP-LPHOPBHVSA-N 0.000 claims 1
IZLQANWXAURBRV-ICSRJNTNSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-4-chloro-3-methylbenzamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(Cl)C(C)=C1 IZLQANWXAURBRV-ICSRJNTNSA-N 0.000 claims 1
IEKXJQVZGMJMCA-GOTSBHOMSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-bromonaphthalene-2-carboxamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(C=C(Br)C=C2)C2=C1 IEKXJQVZGMJMCA-GOTSBHOMSA-N 0.000 claims 1
CUXGFAFNHPUFBW-GOTSBHOMSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 CUXGFAFNHPUFBW-GOTSBHOMSA-N 0.000 claims 1
VRPPVWOIMJSSEJ-GOTSBHOMSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-fluoronaphthalene-2-carboxamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(C=C(F)C=C2)C2=C1 VRPPVWOIMJSSEJ-GOTSBHOMSA-N 0.000 claims 1
JCDGDLIWBJJHQP-GOTSBHOMSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound N1[C@@H](CCN)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 JCDGDLIWBJJHQP-GOTSBHOMSA-N 0.000 claims 1
HBKPZZFNAMXAOE-HSJPWVCISA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-(3-methyl-2-phenylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound O=C([C@H](CCN)N[C@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)CC1)N1CC(C(C)C)C1=CC=CC=C1 HBKPZZFNAMXAOE-HSJPWVCISA-N 0.000 claims 1
ZLMMRMFQYXKUTG-JXFKEZNVSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(2,4-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C([C@H]1N[C@H](C(N(CC=2C(=CC(Cl)=CC=2)Cl)CC1)=O)CCN)NC(=O)C1=CC=C(Cl)C(Cl)=C1 ZLMMRMFQYXKUTG-JXFKEZNVSA-N 0.000 claims 1
VXNONGPPOZEGEO-UPVQGACJSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(2,4-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(Cl)=CC2=CC=1)N[C@H](C1=O)CCN)CN1CC1=CC=C(Cl)C=C1Cl VXNONGPPOZEGEO-UPVQGACJSA-N 0.000 claims 1
SSKMMZGAMAHEJL-KNBMTAEXSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(2r)-2-ethyl-3-methylbutyl]-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound N1[C@@H](CCN)C(=O)N(C[C@H](CC)C(C)C)CC[C@H]1CNC(=O)C1=CC=C(Cl)C(Cl)=C1 SSKMMZGAMAHEJL-KNBMTAEXSA-N 0.000 claims 1
YNDUUKABKHQMSJ-NWVWQQAFSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(2r)-2-ethyl-3-methylbutyl]-2-oxo-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound N1[C@@H](CCN)C(=O)N(C[C@H](CC)C(C)C)CC[C@H]1CNC(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 YNDUUKABKHQMSJ-NWVWQQAFSA-N 0.000 claims 1
SSKMMZGAMAHEJL-SYNHAJSKSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(2s)-2-ethyl-3-methylbutyl]-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound N1[C@@H](CCN)C(=O)N(C[C@@H](CC)C(C)C)CC[C@H]1CNC(=O)C1=CC=C(Cl)C(Cl)=C1 SSKMMZGAMAHEJL-SYNHAJSKSA-N 0.000 claims 1
YNDUUKABKHQMSJ-DKLXNKCPSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(2s)-2-ethyl-3-methylbutyl]-2-oxo-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound N1[C@@H](CCN)C(=O)N(C[C@@H](CC)C(C)C)CC[C@H]1CNC(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 YNDUUKABKHQMSJ-DKLXNKCPSA-N 0.000 claims 1
LAOYIESGAAPHNK-PXNSSMCTSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(3,5-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C([C@H]1N[C@H](C(N(CC=2C=C(Cl)C=C(Cl)C=2)CC1)=O)CCN)NC(=O)C1=CC=C(Cl)C(Cl)=C1 LAOYIESGAAPHNK-PXNSSMCTSA-N 0.000 claims 1
SAZDPTSZGYBNIO-ZEQRLZLVSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(3,5-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(Cl)=CC2=CC=1)N[C@H](C1=O)CCN)CN1CC1=CC(Cl)=CC(Cl)=C1 SAZDPTSZGYBNIO-ZEQRLZLVSA-N 0.000 claims 1
QHOCHQYTGSIOPC-ZEQRLZLVSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(3,5-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCN)CN1CC1=CC(Cl)=CC(Cl)=C1 QHOCHQYTGSIOPC-ZEQRLZLVSA-N 0.000 claims 1
NKYAUCIDYPAKAP-ADNZQJBKSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(3,5-dimethylcyclohexyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C1C(C)CC(C)CC1CN1C(=O)[C@H](CCN)N[C@H](CNC(=O)C=2C=C(Cl)C(Cl)=CC=2)CC1 NKYAUCIDYPAKAP-ADNZQJBKSA-N 0.000 claims 1
GHTFXPGMMCNCPQ-OSTLVTSRSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[(3,5-dimethylcyclohexyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1C(C)CC(C)CC1CN1C(=O)[C@H](CCN)N[C@H](CNC(=O)C=2C=C3C=CC=CC3=CC=2)CC1 GHTFXPGMMCNCPQ-OSTLVTSRSA-N 0.000 claims 1
HKNGQTNXBWWWPO-AIKKUKTPSA-N n-[[(3s,5s)-3-(2-aminoethyl)-1-[2-(4-chlorophenyl)propyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound O=C([C@H](CCN)N[C@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)CC1)N1CC(C)C1=CC=C(Cl)C=C1 HKNGQTNXBWWWPO-AIKKUKTPSA-N 0.000 claims 1
WICUPIKXMHXENI-FOLYQGEWSA-N n-[[(3s,5s)-3-(2-aminoethyl)-2-oxo-1-(2-phenylbutyl)-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C([C@@H]1CCN(C([C@H](CCN)N1)=O)CC(CC)C=1C=CC=CC=1)NC(=O)C1=CC=C(Cl)C(Cl)=C1 WICUPIKXMHXENI-FOLYQGEWSA-N 0.000 claims 1
MPNJIEHJLOQRCL-KFTXQHHCSA-N n-[[(3s,5s)-3-(2-aminoethyl)-2-oxo-1-(2-phenylbutyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound O=C([C@H](CCN)N[C@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)CC1)N1CC(CC)C1=CC=CC=C1 MPNJIEHJLOQRCL-KFTXQHHCSA-N 0.000 claims 1
FGZDTSSBZOVZFL-MQTLACETSA-N n-[[(3s,5s)-3-(2-aminoethyl)-2-oxo-1-(2-thiophen-3-ylbutyl)-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound O=C([C@H](CCN)N[C@H](CNC(=O)C=1C=C2C=CC(Cl)=CC2=CC=1)CC1)N1CC(CC)C=1C=CSC=1 FGZDTSSBZOVZFL-MQTLACETSA-N 0.000 claims 1
WICUPIKXMHXENI-MONBJTKQSA-N n-[[(3s,5s)-3-(2-aminoethyl)-2-oxo-1-[(2s)-2-phenylbutyl]-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C([C@@H]1CCN(C([C@H](CCN)N1)=O)C[C@@H](CC)C=1C=CC=CC=1)NC(=O)C1=CC=C(Cl)C(Cl)=C1 WICUPIKXMHXENI-MONBJTKQSA-N 0.000 claims 1
KIYXBNPDQRSXPO-PHXCCWLDSA-N n-[[(3s,5s)-3-(2-aminoethyl)-2-oxo-1-[(2s)-2-phenylbutyl]-1,4-diazepan-5-yl]methyl]-6-chloronaphthalene-2-carboxamide Chemical compound C1([C@@H](CN2C([C@H](CCN)N[C@H](CNC(=O)C=3C=C4C=CC(Cl)=CC4=CC=3)CC2)=O)CC)=CC=CC=C1 KIYXBNPDQRSXPO-PHXCCWLDSA-N 0.000 claims 1
MPNJIEHJLOQRCL-AIGMYPEUSA-N n-[[(3s,5s)-3-(2-aminoethyl)-2-oxo-1-[(2s)-2-phenylbutyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1([C@@H](CN2C([C@H](CCN)N[C@H](CNC(=O)C=3C=C4C=CC=CC4=CC=3)CC2)=O)CC)=CC=CC=C1 MPNJIEHJLOQRCL-AIGMYPEUSA-N 0.000 claims 1
ZOJZPJKDVGKPAL-WNJJXGMVSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1h-indole-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1NC2=CC=CC=C2C=1)N[C@H](C1=O)CCCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 ZOJZPJKDVGKPAL-WNJJXGMVSA-N 0.000 claims 1
FYYVLUVZEXACBD-WNJJXGMVSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-(4-fluorophenoxy)acetamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCN)NC(=O)COC1=CC=C(F)C=C1 FYYVLUVZEXACBD-WNJJXGMVSA-N 0.000 claims 1
QCBUQTAEJQXPDH-TXJYOHDVSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-ethylhexanamide Chemical compound O=C1[C@H](CCCN)N[C@H](CNC(=O)C(CC)CCCC)CCN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 QCBUQTAEJQXPDH-TXJYOHDVSA-N 0.000 claims 1
XSOVPZBZTYQPSS-XTBGFXFQSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-oxo-1-phenylpyrrolidine-3-carboxamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCN)NC(=O)C(C1=O)CCN1C1=CC=CC=C1 XSOVPZBZTYQPSS-XTBGFXFQSA-N 0.000 claims 1
WZRHDCPARKBLRT-YTMVLYRLSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-phenyl-1,3-thiazole-4-carboxamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCN)NC(=O)C(N=1)=CSC=1C1=CC=CC=C1 WZRHDCPARKBLRT-YTMVLYRLSA-N 0.000 claims 1
XAHFMULGPKQPNU-CUBQBAPOSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCN)NC(=O)C1=CC=C(Cl)C(Cl)=C1 XAHFMULGPKQPNU-CUBQBAPOSA-N 0.000 claims 1
YRIJEWGEWVSBMX-JDXGNMNLSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dimethylbenzamide Chemical compound C1=C(C)C(C)=CC=C1C(=O)NC[C@H]1N[C@@H](CCCN)C(=O)N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 YRIJEWGEWVSBMX-JDXGNMNLSA-N 0.000 claims 1
BETBALQOLRCOSP-YTMVLYRLSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3-phenyl-1h-pyrazole-5-carboxamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCN)NC(=O)C(NN=1)=CC=1C1=CC=CC=C1 BETBALQOLRCOSP-YTMVLYRLSA-N 0.000 claims 1
RUDKYWWUECNFKN-TWJUONSBSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-4-phenylbenzamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCN)NC(=O)C(C=C1)=CC=C1C1=CC=CC=C1 RUDKYWWUECNFKN-TWJUONSBSA-N 0.000 claims 1
LRHDGJCOTTVMKL-JDXGNMNLSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-5-(4-chlorophenyl)furan-2-carboxamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCN)NC(=O)C(O1)=CC=C1C1=CC=C(Cl)C=C1 LRHDGJCOTTVMKL-JDXGNMNLSA-N 0.000 claims 1
UOABSESNZXNJQO-IUDBTDONSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-5-methyl-1-phenylpyrazole-4-carboxamide Chemical compound CC1=C(C(=O)NC[C@H]2N[C@@H](CCCN)C(=O)N(CC(C=3C=CC=CC=3)C=3C=CC=CC=3)CC2)C=NN1C1=CC=CC=C1 UOABSESNZXNJQO-IUDBTDONSA-N 0.000 claims 1
WPCLPNAHZOHTIW-WEZIJMHWSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-bromo-n-methylnaphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCN)C1=O)CN(C)C(=O)C=2C=C3C=CC(Br)=CC3=CC=2)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 WPCLPNAHZOHTIW-WEZIJMHWSA-N 0.000 claims 1
ZUIVKBAJDLMMDS-CDZUIXILSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-bromonaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(Br)=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 ZUIVKBAJDLMMDS-CDZUIXILSA-N 0.000 claims 1
SBIOEJXYDUVYQR-CDZUIXILSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-fluoronaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(F)=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 SBIOEJXYDUVYQR-CDZUIXILSA-N 0.000 claims 1
PWLOKCRKECNMCH-CDZUIXILSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 PWLOKCRKECNMCH-CDZUIXILSA-N 0.000 claims 1
GJDBJWUKDCFAPT-WEZIJMHWSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-(2,2-diphenylethyl)-4-methyl-2-oxo-1,4-diazepan-5-yl]methyl]-6-bromonaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(Br)=CC2=CC=1)N([C@H](C1=O)CCCN)C)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 GJDBJWUKDCFAPT-WEZIJMHWSA-N 0.000 claims 1
XRTIRNHZVUVWOJ-UPVQGACJSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(2,3-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC=CC(Cl)=C1Cl XRTIRNHZVUVWOJ-UPVQGACJSA-N 0.000 claims 1
XTKNLEWVDDEEIW-ZCYQVOJMSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(2,4-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC=C(Cl)C=C1Cl XTKNLEWVDDEEIW-ZCYQVOJMSA-N 0.000 claims 1
GNYPKRMHSTUXSC-ZCYQVOJMSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(2,5-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC(Cl)=CC=C1Cl GNYPKRMHSTUXSC-ZCYQVOJMSA-N 0.000 claims 1
PJUVKKCZPWFZRM-OFVILXPXSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(2,6-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=C(Cl)C=CC=C1Cl PJUVKKCZPWFZRM-OFVILXPXSA-N 0.000 claims 1
ALCHGVJBUISZGZ-ZAZPTELASA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(2,6-dimethylcyclohexyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound CC1CCCC(C)C1CN1C(=O)[C@H](CCCN)N[C@H](CNC(=O)C=2C=C3C=CC=CC3=CC=2)CC1 ALCHGVJBUISZGZ-ZAZPTELASA-N 0.000 claims 1
GXINBEVXEUIFAY-ZCYQVOJMSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(2-chlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC=CC=C1Cl GXINBEVXEUIFAY-ZCYQVOJMSA-N 0.000 claims 1
JKAROZVYTRWXET-DHLKQENFSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(3,4-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC=C(Cl)C(Cl)=C1 JKAROZVYTRWXET-DHLKQENFSA-N 0.000 claims 1
IWGHRQNJSJBQNT-VMPREFPWSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(3,5-diethynylphenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC(C#C)=CC(C#C)=C1 IWGHRQNJSJBQNT-VMPREFPWSA-N 0.000 claims 1
YFYIVHIAEHXMCH-DQEYMECFSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(3-chlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC=CC(Cl)=C1 YFYIVHIAEHXMCH-DQEYMECFSA-N 0.000 claims 1
PXFWVGFTDAQGCB-UIOOFZCWSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(3-fluoro-5-methylphenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound CC1=CC(F)=CC(CN2C([C@H](CCCN)N[C@H](CNC(=O)C=3C=C4C=CC=CC4=CC=3)CC2)=O)=C1 PXFWVGFTDAQGCB-UIOOFZCWSA-N 0.000 claims 1
FYYRJGXJJZHVBW-DQEYMECFSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[(4-chlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC=C(Cl)C=C1 FYYRJGXJJZHVBW-DQEYMECFSA-N 0.000 claims 1
NHAPQTWPUKDQDZ-DQEYMECFSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 NHAPQTWPUKDQDZ-DQEYMECFSA-N 0.000 claims 1
DPRPUEFBFUJOKZ-DQEYMECFSA-N n-[[(3s,5s)-3-(3-aminopropyl)-1-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1=CC(F)=CC(C(F)(F)F)=C1 DPRPUEFBFUJOKZ-DQEYMECFSA-N 0.000 claims 1
HIXSQRVONZIWDI-WLHBAFDUSA-N n-[[(3s,5s)-3-(3-aminopropyl)-2-oxo-1-(2-phenylbutyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound O=C([C@H](CCCN)N[C@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)CC1)N1CC(CC)C1=CC=CC=C1 HIXSQRVONZIWDI-WLHBAFDUSA-N 0.000 claims 1
BAKDCQAYDVMYLF-KYJUHHDHSA-N n-[[(3s,5s)-3-(3-aminopropyl)-2-oxo-1-[(1-phenylcyclohexyl)methyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCN)CN1CC1(C=2C=CC=CC=2)CCCCC1 BAKDCQAYDVMYLF-KYJUHHDHSA-N 0.000 claims 1
HIXSQRVONZIWDI-FAQZDJIUSA-N n-[[(3s,5s)-3-(3-aminopropyl)-2-oxo-1-[(2r)-2-phenylbutyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1([C@H](CN2C([C@H](CCCN)N[C@H](CNC(=O)C=3C=C4C=CC=CC4=CC=3)CC2)=O)CC)=CC=CC=C1 HIXSQRVONZIWDI-FAQZDJIUSA-N 0.000 claims 1
BQPYVCCPIGAKCW-PUUVEUEGSA-N n-[[(3s,5s)-3-(3-aminopropyl)-2-oxo-1-[(2r)-2-phenylpropyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1([C@H](CN2C([C@H](CCCN)N[C@H](CNC(=O)C=3C=C4C=CC=CC4=CC=3)CC2)=O)C)=CC=CC=C1 BQPYVCCPIGAKCW-PUUVEUEGSA-N 0.000 claims 1
HIXSQRVONZIWDI-WWEDSPNTSA-N n-[[(3s,5s)-3-(3-aminopropyl)-2-oxo-1-[(2s)-2-phenylbutyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1([C@@H](CN2C([C@H](CCCN)N[C@H](CNC(=O)C=3C=C4C=CC=CC4=CC=3)CC2)=O)CC)=CC=CC=C1 HIXSQRVONZIWDI-WWEDSPNTSA-N 0.000 claims 1
BQPYVCCPIGAKCW-AIGMYPEUSA-N n-[[(3s,5s)-3-(3-aminopropyl)-2-oxo-1-[(2s)-2-phenylpropyl]-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1([C@@H](CN2C([C@H](CCCN)N[C@H](CNC(=O)C=3C=C4C=CC=CC4=CC=3)CC2)=O)C)=CC=CC=C1 BQPYVCCPIGAKCW-AIGMYPEUSA-N 0.000 claims 1
NMLHHLNZWBDJJX-YTMVLYRLSA-N n-[[(3s,5s)-3-(4-aminobutyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1-benzofuran-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1OC2=CC=CC=C2C=1)N[C@H](C1=O)CCCCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 NMLHHLNZWBDJJX-YTMVLYRLSA-N 0.000 claims 1
ZEMZLZWYFQYUMY-WEZIJMHWSA-N n-[[(3s,5s)-3-(4-aminobutyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCCN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 ZEMZLZWYFQYUMY-WEZIJMHWSA-N 0.000 claims 1
YISLVKWGIZADMO-SVEHJYQDSA-N n-[[(3s,5s)-3-(4-aminobutyl)-1-(naphthalen-1-ylmethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-(1h-indol-3-yl)acetamide Chemical compound C1CN(CC=2C3=CC=CC=C3C=CC=2)C(=O)[C@H](CCCCN)N[C@@H]1CNC(=O)CC1=CNC2=CC=CC=C12 YISLVKWGIZADMO-SVEHJYQDSA-N 0.000 claims 1
PDOBGZCNSXLOEM-YZNIXAGQSA-N n-[[(3s,5s)-3-(4-aminobutyl)-1-(naphthalen-1-ylmethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-1-carboxamide Chemical compound C1CN(CC=2C3=CC=CC=C3C=CC=2)C(=O)[C@H](CCCCN)N[C@@H]1CNC(=O)C1=CC=CC2=CC=CC=C12 PDOBGZCNSXLOEM-YZNIXAGQSA-N 0.000 claims 1
MVRXLHCLTQPYTR-JDXGNMNLSA-N n-[[(3s,5s)-3-(4-aminobutyl)-1-(naphthalen-1-ylmethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1CN(CC=2C3=CC=CC=C3C=CC=2)C(=O)[C@H](CCCCN)N[C@@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 MVRXLHCLTQPYTR-JDXGNMNLSA-N 0.000 claims 1
SDVSRNPMIZLVKX-FIBWVYCGSA-N n-[[(3s,5s)-3-(4-aminobutyl)-1-(naphthalen-2-ylmethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-1-carboxamide Chemical compound C1CN(CC=2C=C3C=CC=CC3=CC=2)C(=O)[C@H](CCCCN)N[C@@H]1CNC(=O)C1=CC=CC2=CC=CC=C12 SDVSRNPMIZLVKX-FIBWVYCGSA-N 0.000 claims 1
VCMTYQKPHKCMBO-KYJUHHDHSA-N n-[[(3s,5s)-3-(4-aminobutyl)-1-(naphthalen-2-ylmethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1CN(CC=2C=C3C=CC=CC3=CC=2)C(=O)[C@H](CCCCN)N[C@@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 VCMTYQKPHKCMBO-KYJUHHDHSA-N 0.000 claims 1
SPIZUXNPIGYOQI-JDXGNMNLSA-N n-[[(3s,5s)-3-(aminomethyl)-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CN)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 SPIZUXNPIGYOQI-JDXGNMNLSA-N 0.000 claims 1
PCFLAUAVIGOSHR-LPHOPBHVSA-N n-[[(3s,5s)-3-(aminomethyl)-1-[(3,5-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C([C@H]1N[C@H](C(N(CC=2C=C(Cl)C=C(Cl)C=2)CC1)=O)CN)NC(=O)C1=CC=C(Cl)C(Cl)=C1 PCFLAUAVIGOSHR-LPHOPBHVSA-N 0.000 claims 1
JOKUOPPJNZPFEZ-GOTSBHOMSA-N n-[[(3s,5s)-3-(aminomethyl)-1-[(3,5-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CN)CN1CC1=CC(Cl)=CC(Cl)=C1 JOKUOPPJNZPFEZ-GOTSBHOMSA-N 0.000 claims 1
DHCFNRRGYVCRJE-XWJWOQKWSA-N n-[[(3s,5s)-3-[2-(benzylamino)ethyl]-2-oxo-1-[(2s)-2-phenylbutyl]-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C([C@@H]1CCN(C([C@H](CCNCC=2C=CC=CC=2)N1)=O)C[C@@H](CC)C=1C=CC=CC=1)NC(=O)C1=CC=C(Cl)C(Cl)=C1 DHCFNRRGYVCRJE-XWJWOQKWSA-N 0.000 claims 1
OGICFAGGMUMKDU-LRHLLKFHSA-N n-[[(3s,5s)-3-[2-(diethylamino)ethyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-fluoronaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(F)=CC2=CC=1)N[C@H](C1=O)CCN(CC)CC)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 OGICFAGGMUMKDU-LRHLLKFHSA-N 0.000 claims 1
UWQQSOAJJGLAJJ-LRHLLKFHSA-N n-[[(3s,5s)-3-[2-(diethylamino)ethyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCN(CC)CC)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 UWQQSOAJJGLAJJ-LRHLLKFHSA-N 0.000 claims 1
DIVJZDICYXIBKA-WEZIJMHWSA-N n-[[(3s,5s)-3-[2-(dimethylamino)ethyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCN(C)C)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 DIVJZDICYXIBKA-WEZIJMHWSA-N 0.000 claims 1
SUTJQAQQNRADEC-IGKWTDBASA-N n-[[(3s,5s)-3-[2-[[(2s)-2-amino-3-methylbutanoyl]amino]ethyl]-1-[(2,4-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]-3,4-dichlorobenzamide Chemical compound C([C@H]1N[C@H](C(N(CC=2C(=CC(Cl)=CC=2)Cl)CC1)=O)CCNC(=O)[C@@H](N)C(C)C)NC(=O)C1=CC=C(Cl)C(Cl)=C1 SUTJQAQQNRADEC-IGKWTDBASA-N 0.000 claims 1
JGMYRBOXTPCJCO-LRHLLKFHSA-N n-[[(3s,5s)-3-[3-(azetidin-1-yl)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCN1CCC1)C1=O)CNC(=O)C=2C=C3C=CC=CC3=CC=2)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 JGMYRBOXTPCJCO-LRHLLKFHSA-N 0.000 claims 1
FVFAEOHHVAXJJV-QARUCVQPSA-N n-[[(3s,5s)-3-[3-(benzylamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCNCC=1C=CC=CC=1)C1=O)CNC(=O)C=2C=C3C=CC=CC3=CC=2)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 FVFAEOHHVAXJJV-QARUCVQPSA-N 0.000 claims 1
WBJLUKAHTWVGIC-GIWKVKTRSA-N n-[[(3s,5s)-3-[3-(cyclobutylamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCNC1CCC1)C1=O)CNC(=O)C=2C=C3C=CC=CC3=CC=2)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 WBJLUKAHTWVGIC-GIWKVKTRSA-N 0.000 claims 1
IKEACBIJKWZQNF-BAEGBANDSA-N n-[[(3s,5s)-3-[3-(cyclohexylamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCNC1CCCCC1)C1=O)CNC(=O)C=2C=C3C=CC=CC3=CC=2)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 IKEACBIJKWZQNF-BAEGBANDSA-N 0.000 claims 1
DOKVYAMBTPOVNF-JSXFGMRASA-N n-[[(3s,5s)-3-[3-(cyclopentylamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCNC1CCCC1)C1=O)CNC(=O)C=2C=C3C=CC=CC3=CC=2)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 DOKVYAMBTPOVNF-JSXFGMRASA-N 0.000 claims 1
XFTYVIHDMVCKHS-XMASUTJCSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1,2,3,4-tetrahydronaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C1CC2=CC=CC=C2CC1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 XFTYVIHDMVCKHS-XMASUTJCSA-N 0.000 claims 1
OYYQWIXOFRMTOX-LSYYVWMOSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1,3-benzothiazole-6-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2SC=NC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 OYYQWIXOFRMTOX-LSYYVWMOSA-N 0.000 claims 1
VPHOQWUKPMTLBC-UCGGBYDDSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1,4-dimethoxynaphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCNC(N)=N)C1=O)CNC(=O)C=2C=C(C3=CC=CC=C3C=2OC)OC)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 VPHOQWUKPMTLBC-UCGGBYDDSA-N 0.000 claims 1
RJGLNXBOEGFWTK-XCZPVHLTSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1-benzofuran-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1OC2=CC=CC=C2C=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 RJGLNXBOEGFWTK-XCZPVHLTSA-N 0.000 claims 1
QATWEZXRMWFGTE-XCZPVHLTSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1-benzothiophene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1SC2=CC=CC=C2C=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 QATWEZXRMWFGTE-XCZPVHLTSA-N 0.000 claims 1
LPMORJOHMZFEIK-YTMVLYRLSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1-benzothiophene-5-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CSC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 LPMORJOHMZFEIK-YTMVLYRLSA-N 0.000 claims 1
HDAGSQJWWKSPBM-IUDBTDONSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-1-methoxynaphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCNC(N)=N)C1=O)CNC(=O)C2=C(C3=CC=CC=C3C=C2)OC)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 HDAGSQJWWKSPBM-IUDBTDONSA-N 0.000 claims 1
BHYXUUNNKRKTBD-SMCANUKXSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2,3-dihydro-1h-indene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C1CC2=CC=CC=C2C1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 BHYXUUNNKRKTBD-SMCANUKXSA-N 0.000 claims 1
OJOHMJHTJUYUDU-SVEHJYQDSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2,4-dimethoxybenzamide Chemical compound COC1=CC(OC)=CC=C1C(=O)NC[C@H]1N[C@@H](CCCNC(N)=N)C(=O)N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 OJOHMJHTJUYUDU-SVEHJYQDSA-N 0.000 claims 1
UFCYHRZLFHTIGL-TXJYOHDVSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-ethylhexanamide Chemical compound O=C1[C@H](CCCNC(N)=N)N[C@H](CNC(=O)C(CC)CCCC)CCN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 UFCYHRZLFHTIGL-TXJYOHDVSA-N 0.000 claims 1
ICTHKJGARPGKGX-WNJJXGMVSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-phenoxyacetamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCNC(=N)N)NC(=O)COC1=CC=CC=C1 ICTHKJGARPGKGX-WNJJXGMVSA-N 0.000 claims 1
JPYWMTFCLCNPPY-RSNGWFSUSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2-phenylcyclopropane-1-carboxamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCNC(=N)N)NC(=O)C1CC1C1=CC=CC=C1 JPYWMTFCLCNPPY-RSNGWFSUSA-N 0.000 claims 1
GPEJAIVLVVLFTF-IGKIAQTJSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-2h-benzotriazole-5-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2N=NNC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 GPEJAIVLVVLFTF-IGKIAQTJSA-N 0.000 claims 1
PKRYJKIJRNTLIG-NYDCQLBNSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3-methoxynaphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCNC(N)=N)C1=O)CNC(=O)C2=CC3=CC=CC=C3C=C2OC)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 PKRYJKIJRNTLIG-NYDCQLBNSA-N 0.000 claims 1
HSWYIFVAUMCGPT-JDXGNMNLSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3-phenylpropanamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCNC(=N)N)NC(=O)CCC1=CC=CC=C1 HSWYIFVAUMCGPT-JDXGNMNLSA-N 0.000 claims 1
MGALBVBSAKGKNO-LSYYVWMOSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-3h-benzimidazole-5-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2N=CNC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 MGALBVBSAKGKNO-LSYYVWMOSA-N 0.000 claims 1
ZOFQWNXCEGKDES-IUDBTDONSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-5-methyl-1-phenylpyrazole-4-carboxamide Chemical compound CC1=C(C(=O)NC[C@H]2N[C@@H](CCCNC(N)=N)C(=O)N(CC(C=3C=CC=CC=3)C=3C=CC=CC=3)CC2)C=NN1C1=CC=CC=C1 ZOFQWNXCEGKDES-IUDBTDONSA-N 0.000 claims 1
LHQIFXQXKCPIAN-JDXGNMNLSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-5-phenylfuran-2-carboxamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCNC(=N)N)NC(=O)C(O1)=CC=C1C1=CC=CC=C1 LHQIFXQXKCPIAN-JDXGNMNLSA-N 0.000 claims 1
LUHXUGOQYLKEAQ-CDZUIXILSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-fluoronaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(F)=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 LUHXUGOQYLKEAQ-CDZUIXILSA-N 0.000 claims 1
FFXCJBHZYBVAQZ-NYDCQLBNSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-hydroxynaphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC(O)=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 FFXCJBHZYBVAQZ-NYDCQLBNSA-N 0.000 claims 1
QWZOMDZWJNKNEN-DITALETJSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]-6-methoxynaphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCNC(N)=N)C1=O)CNC(=O)C2=CC3=CC=C(C=C3C=C2)OC)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 QWZOMDZWJNKNEN-DITALETJSA-N 0.000 claims 1
LVLRCGQAMVAAFS-QPQPGPPRSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]adamantane-1-carboxamide Chemical compound C([C@@H](CNC(=O)C12CC3CC(CC(C3)C1)C2)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 LVLRCGQAMVAAFS-QPQPGPPRSA-N 0.000 claims 1
SZIKENIAXDBLSZ-XCZPVHLTSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]cyclohexanecarboxamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCNC(=N)N)NC(=O)C1CCCCC1 SZIKENIAXDBLSZ-XCZPVHLTSA-N 0.000 claims 1
IAFLAYKZFOVGIP-BDYUSTAISA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]cyclopentanecarboxamide Chemical compound C([C@H]1N[C@H](C(N(CC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1)=O)CCCNC(=N)N)NC(=O)C1CCCC1 IAFLAYKZFOVGIP-BDYUSTAISA-N 0.000 claims 1
XBQSFLUOEFLRMW-JDXGNMNLSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]isoquinoline-3-carboxamide Chemical compound C([C@@H](CNC(=O)C=1N=CC2=CC=CC=C2C=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 XBQSFLUOEFLRMW-JDXGNMNLSA-N 0.000 claims 1
DKFQXTHTGAKMJQ-CDZUIXILSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 DKFQXTHTGAKMJQ-CDZUIXILSA-N 0.000 claims 1
JHNKBSKIHRSONS-DHIFEGFHSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]quinoline-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1N=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 JHNKBSKIHRSONS-DHIFEGFHSA-N 0.000 claims 1
DGSLZNRWLKTSPO-IZEXYCQBSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]quinoline-3-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=NC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 DGSLZNRWLKTSPO-IZEXYCQBSA-N 0.000 claims 1
NLQZQYYRZWYWMJ-SVEHJYQDSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]quinoxaline-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1N=C2C=CC=CC2=NC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 NLQZQYYRZWYWMJ-SVEHJYQDSA-N 0.000 claims 1
ORGUBOVABKKYFO-ACHIHNKUSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2,2-diphenylpropyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound O=C([C@H](CCCNC(N)=N)N[C@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)CC1)N1CC(C)(C=1C=CC=CC=1)C1=CC=CC=C1 ORGUBOVABKKYFO-ACHIHNKUSA-N 0.000 claims 1
MVQZRJYURGRTIW-ZEQRLZLVSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2-ethylbutyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound N1[C@@H](CCCNC(N)=N)C(=O)N(CC(CC)CC)CC[C@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 MVQZRJYURGRTIW-ZEQRLZLVSA-N 0.000 claims 1
CBJRTXOFLNIBPS-TXIPYEPDSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2-methoxy-2-phenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound O=C([C@H](CCCNC(N)=N)N[C@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)CC1)N1CC(OC)C1=CC=CC=C1 CBJRTXOFLNIBPS-TXIPYEPDSA-N 0.000 claims 1
WKXADWDUHHIJAQ-KYJUHHDHSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(2-naphthalen-2-ylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1CN(CCC=2C=C3C=CC=CC3=CC=2)C(=O)[C@H](CCCNC(=N)N)N[C@@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 WKXADWDUHHIJAQ-KYJUHHDHSA-N 0.000 claims 1
JKHAMWNJJHWPQL-IEWVHIKDSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(9h-fluoren-9-ylmethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1CN(CC2C3=CC=CC=C3C3=CC=CC=C32)C(=O)[C@H](CCCNC(=N)N)N[C@@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 JKHAMWNJJHWPQL-IEWVHIKDSA-N 0.000 claims 1
RUAUGPCLNGSTAG-YTMVLYRLSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(naphthalen-1-ylmethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1CN(CC=2C3=CC=CC=C3C=CC=2)C(=O)[C@H](CCCNC(=N)N)N[C@@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 RUAUGPCLNGSTAG-YTMVLYRLSA-N 0.000 claims 1
YUDDAXQRMZKAPF-VMPREFPWSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-(naphthalen-2-ylmethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1CN(CC=2C=C3C=CC=CC3=CC=2)C(=O)[C@H](CCCNC(=N)N)N[C@@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 YUDDAXQRMZKAPF-VMPREFPWSA-N 0.000 claims 1
JNPSAMRJNQMYOH-DQEYMECFSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-[(3,5-dichlorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC1=CC(Cl)=CC(Cl)=C1 JNPSAMRJNQMYOH-DQEYMECFSA-N 0.000 claims 1
SMUSSXMLUFUAPZ-DQEYMECFSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-[(3,5-difluorophenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC1=CC(F)=CC(F)=C1 SMUSSXMLUFUAPZ-DQEYMECFSA-N 0.000 claims 1
VCQJMRSDQYAODK-HDYFOKATSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-[(3,5-dimethylcyclohexyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1C(C)CC(C)CC1CN1C(=O)[C@H](CCCNC(N)=N)N[C@H](CNC(=O)C=2C=C3C=CC=CC3=CC=2)CC1 VCQJMRSDQYAODK-HDYFOKATSA-N 0.000 claims 1
QUXFTJDVAXLSOB-SVBPBHIXSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-[(3,5-dimethylphenyl)methyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound CC1=CC(C)=CC(CN2C([C@H](CCCNC(N)=N)N[C@H](CNC(=O)C=3C=C4C=CC=CC4=CC=3)CC2)=O)=C1 QUXFTJDVAXLSOB-SVBPBHIXSA-N 0.000 claims 1
DVRZIZBUPVOICY-AHWVRZQESA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-[2-(2,4-dichlorophenyl)ethyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CCC1=CC=C(Cl)C=C1Cl DVRZIZBUPVOICY-AHWVRZQESA-N 0.000 claims 1
XEECERRNBOAODP-OZXSUGGESA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-[2-(3,4-dichlorophenyl)ethyl]-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CCC1=CC=C(Cl)C(Cl)=C1 XEECERRNBOAODP-OZXSUGGESA-N 0.000 claims 1
OGFAWJRTQSHKDV-XCZPVHLTSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-1-naphthalen-2-yl-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C1CN(C=2C=C3C=CC=CC3=CC=2)C(=O)[C@H](CCCNC(=N)N)N[C@@H]1CNC(=O)C1=CC=C(C=CC=C2)C2=C1 OGFAWJRTQSHKDV-XCZPVHLTSA-N 0.000 claims 1
FQJPIRCJJADUTL-AQBAIUPUSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1-(2-phenoxy-2-phenylethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)OC1=CC=CC=C1 FQJPIRCJJADUTL-AQBAIUPUSA-N 0.000 claims 1
QSTKPYSOOVYKHW-KOPQTXDBSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1-(2-phenyl-2-phenylmethoxyethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)N[C@H](C1=O)CCCNC(=N)N)CN1CC(C=1C=CC=CC=1)OCC1=CC=CC=C1 QSTKPYSOOVYKHW-KOPQTXDBSA-N 0.000 claims 1
YJVUOLOUFSCBHJ-ASYYUYISSA-N n-[[(3s,5s)-3-[3-(diaminomethylideneamino)propyl]-2-oxo-1-(2-phenyl-2-propoxyethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound O=C([C@H](CCCNC(N)=N)N[C@H](CNC(=O)C=1C=C2C=CC=CC2=CC=1)CC1)N1CC(OCCC)C1=CC=CC=C1 YJVUOLOUFSCBHJ-ASYYUYISSA-N 0.000 claims 1
XHLLZJNFKOIUFF-PUAPYOPTSA-N n-[[(3s,5s)-3-[3-[di(cyclobutyl)amino]propyl]-1-(2,2-diphenylethyl)-2-oxo-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C([C@H](N[C@@H](CCCN(C1CCC1)C1CCC1)C1=O)CNC(=O)C=2C=C3C=CC=CC3=CC=2)CN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 XHLLZJNFKOIUFF-PUAPYOPTSA-N 0.000 claims 1
PNITVXIZXUWQET-UHFFFAOYSA-N n-[[1-(2,2-diphenylethyl)-2-oxo-3-(piperidin-4-ylmethyl)-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C=1C=C2C=CC=CC2=CC=1C(=O)NCC(NC(CC1CCNCC1)C1=O)CCN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 PNITVXIZXUWQET-UHFFFAOYSA-N 0.000 claims 1
YTNMWQMBKAZCMS-UHFFFAOYSA-N n-[[1-(2,2-diphenylethyl)-2-oxo-3-piperidin-4-yl-1,4-diazepan-5-yl]methyl]naphthalene-2-carboxamide Chemical compound C=1C=C2C=CC=CC2=CC=1C(=O)NCC(NC(C1=O)C2CCNCC2)CCN1CC(C=1C=CC=CC=1)C1=CC=CC=C1 YTNMWQMBKAZCMS-UHFFFAOYSA-N 0.000 claims 1
125000002347 octyl group Chemical group [H]C([*])([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
UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 claims 1
IBBMAWULFFBRKK-UHFFFAOYSA-N picolinamide Chemical compound NC(=O)C1=CC=CC=N1 IBBMAWULFFBRKK-UHFFFAOYSA-N 0.000 claims 1
125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
125000004193 piperazinyl group Chemical group 0.000 claims 1
125000003386 piperidinyl group Chemical group 0.000 claims 1
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims 1
UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
125000004262 quinoxalin-2-yl group Chemical group [H]C1=NC2=C([H])C([H])=C([H])C([H])=C2N=C1* 0.000 claims 1
210000002374 sebum Anatomy 0.000 claims 1
230000028327 secretion Effects 0.000 claims 1
125000001424 substituent group Chemical group 0.000 claims 1
125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
125000000446 sulfanediyl group Chemical group *S* 0.000 claims 1
208000024891 symptom Diseases 0.000 claims 1
150000003536 tetrazoles Chemical class 0.000 claims 1
125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 claims 1
229930192474 thiophene Natural products 0.000 claims 1
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1

JP2010547918A 2008-02-29 2009-02-27 Ｍｃ５受容体の活性を調節する方法およびこの受容体と関連する症状の治療 Expired - Fee Related JP5503558B2 (ja)