JP2017525744A5 - - Google Patents

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Publication number

JP2017525744A5

JP2017525744A5 JP2017512780A JP2017512780A JP2017525744A5 JP 2017525744 A5 JP2017525744 A5 JP 2017525744A5 JP 2017512780 A JP2017512780 A JP 2017512780A JP 2017512780 A JP2017512780 A JP 2017512780A JP 2017525744 A5 JP2017525744 A5 JP 2017525744A5

Authority

JP

Japan

Prior art keywords

alkyl

methyl

benzodiazacyclododecin

dioxo

nhco

Prior art date

2015-09-03

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

• Espacenet
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• 125000000217 alkyl group Chemical group 0.000 claims 96
• 229910052739 hydrogen Inorganic materials 0.000 claims 24
• 229910052799 carbon Inorganic materials 0.000 claims 17
• 229910052736 halogen Inorganic materials 0.000 claims 14
• 150000002367 halogens Chemical class 0.000 claims 14
• 229910052757 nitrogen Chemical group 0.000 claims 13
• -1 (±) -methyl Chemical group 0.000 claims 12
• 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 11
• 125000000623 heterocyclic group Chemical group 0.000 claims 11
• 150000003839 salts Chemical class 0.000 claims 9
• 150000001875 compounds Chemical class 0.000 claims 7
• 125000004432 carbon atom Chemical group C* 0.000 claims 6
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
• 208000035475 disorder Diseases 0.000 claims 6
• 125000005842 heteroatom Chemical group 0.000 claims 6
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
• 230000009424 thromboembolic effect Effects 0.000 claims 6
• 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
• 125000003545 alkoxy group Chemical group 0.000 claims 5
• 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
• KPPVNWGJXFMGAM-UUILKARUSA-N (e)-2-methyl-1-(6-methyl-3,4-dihydro-2h-quinolin-1-yl)but-2-en-1-one Chemical compound CC1=CC=C2N(C(=O)C(/C)=C/C)CCCC2=C1 KPPVNWGJXFMGAM-UUILKARUSA-N 0.000 claims 4
• 239000008194 pharmaceutical composition Substances 0.000 claims 4
• 125000004414 alkyl thio group Chemical group 0.000 claims 3
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
• 208000007536 Thrombosis Diseases 0.000 claims 2
• 206010047249 Venous thrombosis Diseases 0.000 claims 2
• 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
• 230000002526 effect on cardiovascular system Effects 0.000 claims 2
• MTDWONZHWZACQI-FQEVSTJZSA-N methyl N-[(9S)-9-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethylcarbamoyl]-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(12),13,15-trien-15-yl]carbamate Chemical compound COC(=O)Nc1ccc2c(NC(=O)CCCCC[C@H](NC2=O)C(=O)NCCc2cc(Cl)ccc2-n2cnnn2)c1 MTDWONZHWZACQI-FQEVSTJZSA-N 0.000 claims 2
• 229910052760 oxygen Inorganic materials 0.000 claims 2
• 229910052717 sulfur Inorganic materials 0.000 claims 2
• UDJKQCZYNZIIJX-IUINOXSKSA-N (6E,9R)-N-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethyl]-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(16),6,12,14-tetraene-9-carboxamide Chemical compound Clc1ccc(c(CCNC(=O)[C@H]2C\C=C\CCC(=O)Nc3ccccc3C(=O)N2)c1)-n1cnnn1 UDJKQCZYNZIIJX-IUINOXSKSA-N 0.000 claims 1
• 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
• 206010002388 Angina unstable Diseases 0.000 claims 1
• 201000001320 Atherosclerosis Diseases 0.000 claims 1
• 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
• QMLDERKCRDMXBF-OWOJBTEDSA-N C(N)(=N)N1CCC(CC1)NC(=O)C1C/C=C/CCC(NC2=C(C(N1)=O)C=CC=C2)=O Chemical compound C(N)(=N)N1CCC(CC1)NC(=O)C1C/C=C/CCC(NC2=C(C(N1)=O)C=CC=C2)=O QMLDERKCRDMXBF-OWOJBTEDSA-N 0.000 claims 1
• KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
• 206010008088 Cerebral artery embolism Diseases 0.000 claims 1
• 206010008092 Cerebral artery thrombosis Diseases 0.000 claims 1
• WMKDDDFZWIMAOE-UHFFFAOYSA-N ClC=1C=CC(=C(C=1)CCNC(=O)C1CCCCCC(NC2=C(C(N1)=O)C=CC=C2)=O)N1N=NN=C1 Chemical compound ClC=1C=CC(=C(C=1)CCNC(=O)C1CCCCCC(NC2=C(C(N1)=O)C=CC=C2)=O)N1N=NN=C1 WMKDDDFZWIMAOE-UHFFFAOYSA-N 0.000 claims 1
• 206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
• 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
• 206010014513 Embolism arterial Diseases 0.000 claims 1
• 208000032382 Ischaemic stroke Diseases 0.000 claims 1
• 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
• 206010037437 Pulmonary thrombosis Diseases 0.000 claims 1
• 206010063544 Renal embolism Diseases 0.000 claims 1
• 208000006011 Stroke Diseases 0.000 claims 1
• 208000007814 Unstable Angina Diseases 0.000 claims 1
• 125000003118 aryl group Chemical group 0.000 claims 1
• 125000004429 atom Chemical group 0.000 claims 1
• 230000015572 biosynthetic process Effects 0.000 claims 1
• 239000008280 blood Substances 0.000 claims 1
• 210000004369 blood Anatomy 0.000 claims 1
• 210000005242 cardiac chamber Anatomy 0.000 claims 1
• 208000002528 coronary thrombosis Diseases 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
• 201000010849 intracranial embolism Diseases 0.000 claims 1
• ZWOVUXOCMLKLQV-IIBYNOLFSA-N methyl N-[(4R,9R)-9-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethylcarbamoyl]-4-methyl-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(12),13,15-trien-15-yl]carbamate Chemical compound COC(=O)Nc1ccc2c(NC(=O)[C@H](C)CCCC[C@@H](NC2=O)C(=O)NCCc2cc(Cl)ccc2-n2cnnn2)c1 ZWOVUXOCMLKLQV-IIBYNOLFSA-N 0.000 claims 1
• INAKQOFTONZECB-KKSFZXQISA-N methyl N-[(5S,9S)-9-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethylcarbamoyl]-5-methyl-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(12),13,15-trien-15-yl]carbamate Chemical compound COC(=O)Nc1ccc2c(NC(=O)C[C@@H](C)CCC[C@H](NC2=O)C(=O)NCCc2cc(Cl)ccc2-n2cnnn2)c1 INAKQOFTONZECB-KKSFZXQISA-N 0.000 claims 1
• ZDNIPUHFPCOYDW-ZOXCZHJPSA-N methyl N-[(6E,9R)-9-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethylcarbamoyl]-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(12),6,13,15-tetraen-15-yl]carbamate Chemical compound COC(=O)Nc1ccc2c(NC(=O)CC\C=C\C[C@@H](NC2=O)C(=O)NCCc2cc(Cl)ccc2-n2cnnn2)c1 ZDNIPUHFPCOYDW-ZOXCZHJPSA-N 0.000 claims 1
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 239000000203 mixture Substances 0.000 claims 1
• 208000010125 myocardial infarction Diseases 0.000 claims 1
• 230000000414 obstructive effect Effects 0.000 claims 1
• 230000003836 peripheral circulation Effects 0.000 claims 1
• 230000002093 peripheral effect Effects 0.000 claims 1
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
• 230000002265 prevention Effects 0.000 claims 1
• 238000002560 therapeutic procedure Methods 0.000 claims 1
• 201000005060 thrombophlebitis Diseases 0.000 claims 1
• 230000001052 transient effect Effects 0.000 claims 1