JP2014534270A5 - - Google Patents

Info

Publication number

JP2014534270A5

JP2014534270A5 JP2014544857A JP2014544857A JP2014534270A5 JP 2014534270 A5 JP2014534270 A5 JP 2014534270A5 JP 2014544857 A JP2014544857 A JP 2014544857A JP 2014544857 A JP2014544857 A JP 2014544857A JP 2014534270 A5 JP2014534270 A5 JP 2014534270A5

Authority

JP

Japan

Prior art keywords

compound

pharmaceutically acceptable

acceptable salt

pharmaceutical composition

composition

Prior art date

2012-11-29

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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• 150000001875 compounds Chemical class 0.000 claims description 33
• 150000003839 salts Chemical class 0.000 claims description 25
• 239000008194 pharmaceutical composition Substances 0.000 claims description 16
• 239000000203 mixture Substances 0.000 claims description 12
• 239000003146 anticoagulant agent Substances 0.000 claims description 8
• 229940127219 anticoagulant drug Drugs 0.000 claims description 8
• 125000005647 linker group Chemical group 0.000 claims description 8
• 239000003130 blood coagulation factor inhibitor Substances 0.000 claims description 5
• 230000002429 anti-coagulating effect Effects 0.000 claims description 3
• 238000009007 Diagnostic Kit Methods 0.000 claims description 2
• 125000002947 alkylene group Chemical group 0.000 claims description 2
• 230000003042 antagnostic effect Effects 0.000 claims description 2
• 239000008280 blood Substances 0.000 claims description 2
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• 125000002091 cationic group Chemical group 0.000 claims description 2
• 239000003937 drug carrier Substances 0.000 claims description 2
• 238000001990 intravenous administration Methods 0.000 claims description 2
• 238000007911 parenteral administration Methods 0.000 claims description 2
• 230000004962 physiological condition Effects 0.000 claims description 2
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
• 238000007920 subcutaneous administration Methods 0.000 claims description 2
• 230000037396 body weight Effects 0.000 claims 2
• 239000007864 aqueous solution Substances 0.000 claims 1
• 239000002775 capsule Substances 0.000 claims 1
• 238000000034 method Methods 0.000 description 16
• HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical group OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 description 8
• 0 C[N+](*(N*(CC1)CC*1N)=C)[O-] Chemical compound C[N+](*(N*(CC1)CC*1N)=C)[O-] 0.000 description 4
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• 125000000524 functional group Chemical group 0.000 description 4
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• 229940127215 low-molecular weight heparin Drugs 0.000 description 4
• 229940123583 Factor Xa inhibitor Drugs 0.000 description 3
• GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 3
• 230000010100 anticoagulation Effects 0.000 description 3
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• 229960001148 rivaroxaban Drugs 0.000 description 3
• KGFYHTZWPPHNLQ-AWEZNQCLSA-N rivaroxaban Chemical compound S1C(Cl)=CC=C1C(=O)NC[C@@H]1OC(=O)N(C=2C=CC(=CC=2)N2C(COCC2)=O)C1 KGFYHTZWPPHNLQ-AWEZNQCLSA-N 0.000 description 3
• 206010051055 Deep vein thrombosis Diseases 0.000 description 2
• 208000032843 Hemorrhage Diseases 0.000 description 2
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• QNZCBYKSOIHPEH-UHFFFAOYSA-N Apixaban Chemical compound C1=CC(OC)=CC=C1N1C(C(=O)N(CC2)C=3C=CC(=CC=3)N3C(CCCC3)=O)=C2C(C(N)=O)=N1 QNZCBYKSOIHPEH-UHFFFAOYSA-N 0.000 description 1
• HGVDHZBSSITLCT-JLJPHGGASA-N Edoxaban Chemical compound N([C@H]1CC[C@@H](C[C@H]1NC(=O)C=1SC=2CN(C)CCC=2N=1)C(=O)N(C)C)C(=O)C(=O)NC1=CC=C(Cl)C=N1 HGVDHZBSSITLCT-JLJPHGGASA-N 0.000 description 1
• 108010029144 Factor IIa Proteins 0.000 description 1
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• 241000124008 Mammalia Species 0.000 description 1
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• 150000001408 amides Chemical class 0.000 description 1
• 229960003886 apixaban Drugs 0.000 description 1
• 125000006615 aromatic heterocyclic group Chemical group 0.000 description 1
• 206010003119 arrhythmia Diseases 0.000 description 1
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• 125000003118 aryl group Chemical group 0.000 description 1
• 229960003616 bemiparin Drugs 0.000 description 1
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• 238000007675 cardiac surgery Methods 0.000 description 1
• 229940107792 certoparin Drugs 0.000 description 1
• 229960004969 dalteparin Drugs 0.000 description 1
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• 231100000673 dose–response relationship Toxicity 0.000 description 1
• 229960000622 edoxaban Drugs 0.000 description 1
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• 238000002692 epidural anesthesia Methods 0.000 description 1
• 150000002148 esters Chemical class 0.000 description 1
• 229960001318 fondaparinux Drugs 0.000 description 1
• KANJSNBRCNMZMV-ABRZTLGGSA-N fondaparinux Chemical compound O[C@@H]1[C@@H](NS(O)(=O)=O)[C@@H](OC)O[C@H](COS(O)(=O)=O)[C@H]1O[C@H]1[C@H](OS(O)(=O)=O)[C@@H](O)[C@H](O[C@@H]2[C@@H]([C@@H](OS(O)(=O)=O)[C@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O[C@@H]4[C@@H]([C@@H](O)[C@H](O)[C@@H](COS(O)(=O)=O)O4)NS(O)(=O)=O)[C@H](O3)C(O)=O)O)[C@@H](COS(O)(=O)=O)O2)NS(O)(=O)=O)[C@H](C(O)=O)O1 KANJSNBRCNMZMV-ABRZTLGGSA-N 0.000 description 1
• 125000000623 heterocyclic group Chemical group 0.000 description 1
• 239000003112 inhibitor Substances 0.000 description 1
• 150000002576 ketones Chemical class 0.000 description 1
• -1 leviparin Chemical compound 0.000 description 1
• 229960000899 nadroparin Drugs 0.000 description 1
• 229960004762 parnaparin Drugs 0.000 description 1
• 230000001575 pathological effect Effects 0.000 description 1
• SHUZOJHMOBOZST-UHFFFAOYSA-N phylloquinone Natural products CC(C)CCCCC(C)CCC(C)CCCC(=CCC1=C(C)C(=O)c2ccccc2C1=O)C SHUZOJHMOBOZST-UHFFFAOYSA-N 0.000 description 1
• BXRNXXXXHLBUKK-UHFFFAOYSA-N piperazine-2,5-dione Chemical compound O=C1CNC(=O)CN1 BXRNXXXXHLBUKK-UHFFFAOYSA-N 0.000 description 1
• 238000002693 spinal anesthesia Methods 0.000 description 1
• 230000009861 stroke prevention Effects 0.000 description 1
• 238000011477 surgical intervention Methods 0.000 description 1
• 238000002560 therapeutic procedure Methods 0.000 description 1
• 229960005062 tinzaparin Drugs 0.000 description 1
• 235000019168 vitamin K Nutrition 0.000 description 1
• 239000011712 vitamin K Substances 0.000 description 1
• 150000003721 vitamin K derivatives Chemical class 0.000 description 1
• 229940046010 vitamin k Drugs 0.000 description 1