JP2014534270A5 - - Google Patents
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- 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
- 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
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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
- 210000004369 blood Anatomy 0.000 claims description 2
- 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
- 230000008485 antagonism Effects 0.000 description 4
- 125000000524 functional group Chemical group 0.000 description 4
- 229920000669 heparin Polymers 0.000 description 4
- 239000003055 low molecular weight heparin Substances 0.000 description 4
- 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
- 230000000694 effects Effects 0.000 description 3
- 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
- 206010047249 Venous thrombosis Diseases 0.000 description 2
- 208000034158 bleeding Diseases 0.000 description 2
- 230000000740 bleeding effect Effects 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 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
- 108010074860 Factor Xa Proteins 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 208000010378 Pulmonary Embolism Diseases 0.000 description 1
- 229930003448 Vitamin K Natural products 0.000 description 1
- 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
- 230000006793 arrhythmia Effects 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 229960003616 bemiparin Drugs 0.000 description 1
- 238000001574 biopsy Methods 0.000 description 1
- 238000007675 cardiac surgery Methods 0.000 description 1
- 229940107792 certoparin Drugs 0.000 description 1
- 229960004969 dalteparin Drugs 0.000 description 1
- 238000002405 diagnostic procedure Methods 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229960000622 edoxaban Drugs 0.000 description 1
- 229960000610 enoxaparin Drugs 0.000 description 1
- 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
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161564559P | 2011-11-29 | 2011-11-29 | |
| US61/564,559 | 2011-11-29 | ||
| US201261614292P | 2012-03-22 | 2012-03-22 | |
| US61/614,292 | 2012-03-22 | ||
| US201261641698P | 2012-05-02 | 2012-05-02 | |
| US61/641,698 | 2012-05-02 | ||
| US201261666291P | 2012-06-29 | 2012-06-29 | |
| US61/666,291 | 2012-06-29 | ||
| PCT/US2012/066938 WO2013082210A1 (en) | 2011-11-29 | 2012-11-29 | Anticoagulant reversal agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014534270A JP2014534270A (ja) | 2014-12-18 |
| JP2014534270A5 true JP2014534270A5 (https=) | 2016-01-28 |
| JP6134731B2 JP6134731B2 (ja) | 2017-05-24 |
Family
ID=47430065
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014544857A Active JP6134731B2 (ja) | 2011-11-29 | 2012-11-29 | 抗凝固剤拮抗剤 |
Country Status (34)
| Country | Link |
|---|---|
| US (5) | US9522892B2 (https=) |
| EP (1) | EP2785700B1 (https=) |
| JP (1) | JP6134731B2 (https=) |
| KR (1) | KR101892330B1 (https=) |
| CN (1) | CN104080772B (https=) |
| AP (1) | AP2014007662A0 (https=) |
| AR (1) | AR089020A1 (https=) |
| AU (1) | AU2012345975B2 (https=) |
| BR (1) | BR112014012892B1 (https=) |
| CA (1) | CA2856540C (https=) |
| CL (1) | CL2014001399A1 (https=) |
| CO (1) | CO6990738A2 (https=) |
| CR (1) | CR20140310A (https=) |
| CY (1) | CY1117414T1 (https=) |
| DK (1) | DK2785700T3 (https=) |
| EA (1) | EA027603B1 (https=) |
| EC (1) | ECSP14006696A (https=) |
| ES (1) | ES2569674T3 (https=) |
| HR (1) | HRP20160513T1 (https=) |
| HU (1) | HUE027452T2 (https=) |
| IL (1) | IL232788B (https=) |
| ME (1) | ME02424B (https=) |
| MX (1) | MX349514B (https=) |
| PE (1) | PE20141295A1 (https=) |
| PH (1) | PH12014501176A1 (https=) |
| PL (1) | PL2785700T3 (https=) |
| PT (1) | PT2785700E (https=) |
| RS (1) | RS54738B1 (https=) |
| SG (1) | SG11201402713WA (https=) |
| SI (1) | SI2785700T1 (https=) |
| SM (1) | SMT201600161B (https=) |
| UA (1) | UA116336C2 (https=) |
| WO (1) | WO2013082210A1 (https=) |
| ZA (1) | ZA201404793B (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9999690B2 (en) | 2013-11-08 | 2018-06-19 | Perosphere Pharmaceuticals Inc. | Labeled compounds and methods of imaging, diagnosing cartilage disorders and diseases, and monitoring cartilage health using labeled and unlabeled compounds |
| KR102483020B1 (ko) | 2016-03-28 | 2023-01-04 | 인사이트 코포레이션 | Tam 저해제로서의 피롤로트리아진 화합물 |
| MA50655B1 (fr) | 2017-09-27 | 2021-11-30 | Incyte Corp | Sels de dérivés de pyrrolotriazine utiles en tant qu'inhibiteurs de tam |
| WO2019094959A1 (en) * | 2017-11-13 | 2019-05-16 | Fernandez Joss | Reconstitution of post mortem circulation, specialized methods and procedures |
| AR117600A1 (es) | 2018-06-29 | 2021-08-18 | Incyte Corp | Formulaciones de un inhibidor de axl / mer |
| US11716989B2 (en) | 2019-04-16 | 2023-08-08 | Maximum Fidelity Surgical Simulations, LLC | Cadaver preservation systems and methods |
| US11915610B2 (en) | 2019-05-15 | 2024-02-27 | Maximum Fidelity Surgical Simulations, LLC | Cadaverous heart model |
| CN112010930B (zh) * | 2019-05-28 | 2022-08-02 | 首都医科大学 | Rgd修饰的五环哌嗪二酮及其制备和应用 |
| WO2021178779A1 (en) | 2020-03-06 | 2021-09-10 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| CN118684672A (zh) | 2023-03-24 | 2024-09-24 | 陕西麦科奥特科技有限公司 | 一种抗凝逆转剂及其制备方法和应用 |
| CN117624137A (zh) * | 2023-12-04 | 2024-03-01 | 中国药科大学 | 三嗪骨架小分子肝素逆转剂及其制备方法与用途 |
| US20250389737A1 (en) * | 2024-06-20 | 2025-12-25 | Instrumentation Laboratory Company | FACTOR Xa REAGENT |
| EP4667582A1 (en) * | 2024-06-20 | 2025-12-24 | Instrumentation Laboratory Company | Factor xa reagent |
| CN121622691A (zh) * | 2024-08-30 | 2026-03-10 | 陕西麦科奥特医药科技股份有限公司 | 使用抗凝逆转剂治疗抗凝剂导致的出血的方法 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3678157A (en) * | 1968-10-23 | 1972-07-18 | Oreal | Hair treatment compositions containing polycondensable compounds |
| IL115420A0 (en) * | 1994-09-26 | 1995-12-31 | Zeneca Ltd | Aminoheterocyclic derivatives |
| US6069232A (en) * | 1995-10-02 | 2000-05-30 | Hoechst Marion Roussel, Inc. | Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors |
| US6080852A (en) | 1996-06-27 | 2000-06-27 | The Perkin-Elmer Corporation | 4,7-dichlororhodamine dyes |
| WO1998016547A1 (en) | 1996-10-11 | 1998-04-23 | Cor Therapeutics, Inc. | SELECTIVE FACTOR Xa INHIBITORS |
| JP2001519806A (ja) * | 1997-04-07 | 2001-10-23 | アクシス ファーマシューティカルズ，インコーポレイティド | セリンプロテアーゼ活性、特にトリプターゼ活性に関連する疾病を処理するための化合物及び組成物 |
| FR2781221B1 (fr) * | 1998-07-17 | 2000-10-13 | Lafon Labor | Piperazinones substituees en alpha |
| CA2348740A1 (en) * | 1998-12-23 | 2000-07-06 | Ruth R. Wexler | Thrombin or factor xa inhibitors |
| NZ514877A (en) | 1999-05-19 | 2004-10-29 | Pharmacia Corp | Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents |
| EP1377554A1 (en) * | 1999-06-16 | 2004-01-07 | University Of Iowa Research Foundation | Antagonism of immunostimulatory cpg-oligonucleotides by 4-aminoquinolines and other weak bases |
| CA2405684A1 (en) | 2000-04-17 | 2001-10-25 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade |
| AU2001275857A1 (en) * | 2000-06-29 | 2002-01-14 | Bristol-Myers Squibb Pharma Company | Thrombin or factor xa inhibitors |
| EP1438292A1 (en) | 2001-10-03 | 2004-07-21 | Pharmacia Corporation | 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade |
| US20060148734A1 (en) * | 2002-03-27 | 2006-07-06 | Patrick Camilleri | Diaminoacid-aminoacid-polyamine based gemini surfactant compounds |
| JPWO2003099324A1 (ja) * | 2002-05-23 | 2005-09-22 | 中外製薬株式会社 | 組織因子阻害剤中和剤及び活性型血液凝固第ｖｉｉ因子製剤中和剤 |
| GB0214122D0 (en) | 2002-06-19 | 2002-07-31 | Eastman Kodak Co | High contrast photographic element containing a polyhydrazide nucleating agent |
| SE0400014D0 (sv) * | 2004-01-08 | 2004-01-08 | Astrazeneca Ab | Heterocyclic derivatives |
| US20060045865A1 (en) | 2004-08-27 | 2006-03-02 | Spherics, Inc. | Controlled regional oral delivery |
| WO2008105441A1 (ja) * | 2007-02-27 | 2008-09-04 | Ajinomoto Co., Inc. | リン吸収抑制活性を有するポリアミノ酸化合物及びリン吸収抑制剤 |
| EP2915564B1 (en) * | 2007-09-28 | 2020-11-04 | Portola Pharmaceuticals, Inc. | Antidotes for factor XA inhibitors and methods of using the same |
| GB2476643B (en) | 2009-12-23 | 2012-11-14 | Haomamedica Ltd | 1,4-Dihydro-1,4-dioxonaphtalene derivatives as anticoagulants |
| AR079944A1 (es) | 2010-01-20 | 2012-02-29 | Boehringer Ingelheim Int | Anticuerpo neutralizante de la actividad de un anticoagulante |
| PE20140964A1 (es) | 2011-03-30 | 2014-08-17 | Boehringer Ingelheim Int | Antidotos anticoagulantes |
-
2012
- 2012-11-29 US US13/688,442 patent/US9522892B2/en active Active
- 2012-11-29 SG SG11201402713WA patent/SG11201402713WA/en unknown
- 2012-11-29 CN CN201280060950.2A patent/CN104080772B/zh active Active
- 2012-11-29 EP EP12806229.6A patent/EP2785700B1/en active Active
- 2012-11-29 HR HRP20160513TT patent/HRP20160513T1/hr unknown
- 2012-11-29 JP JP2014544857A patent/JP6134731B2/ja active Active
- 2012-11-29 HU HUE12806229A patent/HUE027452T2/en unknown
- 2012-11-29 DK DK12806229.6T patent/DK2785700T3/en active
- 2012-11-29 ES ES12806229.6T patent/ES2569674T3/es active Active
- 2012-11-29 MX MX2014006349A patent/MX349514B/es active IP Right Grant
- 2012-11-29 CA CA2856540A patent/CA2856540C/en active Active
- 2012-11-29 EA EA201490823A patent/EA027603B1/ru unknown
- 2012-11-29 UA UAA201404997A patent/UA116336C2/uk unknown
- 2012-11-29 AP AP2014007662A patent/AP2014007662A0/xx unknown
- 2012-11-29 KR KR1020147016304A patent/KR101892330B1/ko active Active
- 2012-11-29 PE PE2014000763A patent/PE20141295A1/es active IP Right Grant
- 2012-11-29 PT PT128062296T patent/PT2785700E/pt unknown
- 2012-11-29 RS RS20160318A patent/RS54738B1/sr unknown
- 2012-11-29 SI SI201230558A patent/SI2785700T1/sl unknown
- 2012-11-29 PL PL12806229.6T patent/PL2785700T3/pl unknown
- 2012-11-29 AR ARP120104474A patent/AR089020A1/es active IP Right Grant
- 2012-11-29 WO PCT/US2012/066938 patent/WO2013082210A1/en not_active Ceased
- 2012-11-29 ME MEP-2016-95A patent/ME02424B/me unknown
- 2012-11-29 BR BR112014012892-8A patent/BR112014012892B1/pt active IP Right Grant
- 2012-11-29 AU AU2012345975A patent/AU2012345975B2/en active Active
-
2014
- 2014-05-26 PH PH12014501176A patent/PH12014501176A1/en unknown
- 2014-05-26 IL IL232788A patent/IL232788B/en active IP Right Grant
- 2014-05-27 CL CL2014001399A patent/CL2014001399A1/es unknown
- 2014-06-26 EC ECIEPI20146696A patent/ECSP14006696A/es unknown
- 2014-06-26 CR CR20140310A patent/CR20140310A/es unknown
- 2014-06-26 CO CO14137450A patent/CO6990738A2/es unknown
- 2014-06-27 ZA ZA2014/04793A patent/ZA201404793B/en unknown
-
2016
- 2016-04-25 CY CY20161100338T patent/CY1117414T1/el unknown
- 2016-06-08 SM SM201600161T patent/SMT201600161B/it unknown
- 2016-11-10 US US15/348,348 patent/US9877961B2/en active Active
-
2017
- 2017-10-06 US US15/726,497 patent/US20180207152A1/en not_active Abandoned
-
2020
- 2020-12-10 US US17/117,559 patent/US20210169874A1/en not_active Abandoned
-
2023
- 2023-12-15 US US18/541,391 patent/US20240366592A1/en active Pending
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