JP2010526103A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010526103A5 JP2010526103A5 JP2010506696A JP2010506696A JP2010526103A5 JP 2010526103 A5 JP2010526103 A5 JP 2010526103A5 JP 2010506696 A JP2010506696 A JP 2010506696A JP 2010506696 A JP2010506696 A JP 2010506696A JP 2010526103 A5 JP2010526103 A5 JP 2010526103A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- pharmaceutically acceptable
- acceptable salt
- inhibitor
- 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
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 46
- 239000003814 drug Substances 0.000 claims 37
- 229940124597 therapeutic agent Drugs 0.000 claims 35
- 150000003839 salts Chemical class 0.000 claims 24
- 229950011103 betrixaban Drugs 0.000 claims 14
- XHOLNRLADUSQLD-UHFFFAOYSA-N betrixaban Chemical group C=1C=C(Cl)C=NC=1NC(=O)C1=CC(OC)=CC=C1NC(=O)C1=CC=C(C(=N)N(C)C)C=C1 XHOLNRLADUSQLD-UHFFFAOYSA-N 0.000 claims 14
- 239000003146 anticoagulant agent Substances 0.000 claims 13
- 229940127219 anticoagulant drug Drugs 0.000 claims 13
- 229940127218 antiplatelet drug Drugs 0.000 claims 12
- WUPZRLYEGIXBNO-UHFFFAOYSA-N 1-(5-chlorothiophen-2-yl)sulfonyl-1-[4-[6-fluoro-7-(methylamino)-2,4-dioxo-1h-quinazolin-3-yl]phenyl]urea Chemical compound O=C1C=2C=C(F)C(NC)=CC=2NC(=O)N1C(C=C1)=CC=C1N(C(N)=O)S(=O)(=O)C1=CC=C(Cl)S1 WUPZRLYEGIXBNO-UHFFFAOYSA-N 0.000 claims 8
- 229940123583 Factor Xa inhibitor Drugs 0.000 claims 8
- -1 fencoumarol Chemical compound 0.000 claims 7
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 7
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 7
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound 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 claims 6
- 208000007536 Thrombosis Diseases 0.000 claims 6
- 238000011287 therapeutic dose Methods 0.000 claims 6
- 229960001500 bivalirudin Drugs 0.000 claims 5
- OIRCOABEOLEUMC-GEJPAHFPSA-N bivalirudin Chemical compound C([C@@H](C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)CNC(=O)CNC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 OIRCOABEOLEUMC-GEJPAHFPSA-N 0.000 claims 5
- 108010055460 bivalirudin Proteins 0.000 claims 5
- 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 claims 4
- 241000124008 Mammalia Species 0.000 claims 4
- 229960003886 apixaban Drugs 0.000 claims 4
- 229950004274 ifetroban Drugs 0.000 claims 4
- BBPRUNPUJIUXSE-DXKRWKNPSA-N ifetroban Chemical compound CCCCCNC(=O)C1=COC([C@H]2[C@H]([C@@H]3CC[C@H]2O3)CC=2C(=CC=CC=2)CCC(O)=O)=N1 BBPRUNPUJIUXSE-DXKRWKNPSA-N 0.000 claims 4
- 229960001148 rivaroxaban Drugs 0.000 claims 4
- 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 claims 4
- 229940122204 Cyclooxygenase inhibitor Drugs 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 239000002599 prostaglandin synthase inhibitor Substances 0.000 claims 3
- XSNMGLZVFNDDPW-ZWKOTPCHSA-N (2s)-1-[(2r)-2-[3-chloro-5-(difluoromethoxy)phenyl]-2-hydroxyacetyl]-n-[[4-(n'-methoxycarbamimidoyl)phenyl]methyl]azetidine-2-carboxamide Chemical compound C1=CC(C(/N)=N/OC)=CC=C1CNC(=O)[C@H]1N(C(=O)[C@H](O)C=2C=C(OC(F)F)C=C(Cl)C=2)CC1 XSNMGLZVFNDDPW-ZWKOTPCHSA-N 0.000 claims 2
- 125000005273 2-acetoxybenzoic acid group Chemical group 0.000 claims 2
- XEMDFESAXKSEGI-UHFFFAOYSA-N 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine Chemical compound O1C(C)(C)C(C)(C)OB1C1=CC=CN=C1 XEMDFESAXKSEGI-UHFFFAOYSA-N 0.000 claims 2
- BSYNRYMUTXBXSQ-FOQJRBATSA-N 59096-14-9 Chemical compound CC(=O)OC1=CC=CC=C1[14C](O)=O BSYNRYMUTXBXSQ-FOQJRBATSA-N 0.000 claims 2
- 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 claims 2
- 108010056764 Eptifibatide Proteins 0.000 claims 2
- 229940123849 Factor IXa inhibitor Drugs 0.000 claims 2
- 229940082863 Factor VIIa inhibitor Drugs 0.000 claims 2
- 229940105278 Factor XI inhibitor Drugs 0.000 claims 2
- 229940122036 Factor XIa inhibitor Drugs 0.000 claims 2
- QNVSXXGDAPORNA-UHFFFAOYSA-N Resveratrol Natural products OC1=CC=CC(C=CC=2C=C(O)C(O)=CC=2)=C1 QNVSXXGDAPORNA-UHFFFAOYSA-N 0.000 claims 2
- 229940100389 Sulfonylurea Drugs 0.000 claims 2
- 229940099508 TP receptor antagonist Drugs 0.000 claims 2
- 101000712605 Theromyzon tessulatum Theromin Proteins 0.000 claims 2
- 229940122388 Thrombin inhibitor Drugs 0.000 claims 2
- LUKBXSAWLPMMSZ-OWOJBTEDSA-N Trans-resveratrol Chemical compound C1=CC(O)=CC=C1\C=C\C1=CC(O)=CC(O)=C1 LUKBXSAWLPMMSZ-OWOJBTEDSA-N 0.000 claims 2
- 229960000446 abciximab Drugs 0.000 claims 2
- 229960001138 acetylsalicylic acid Drugs 0.000 claims 2
- KXNPVXPOPUZYGB-XYVMCAHJSA-N argatroban Chemical compound OC(=O)[C@H]1C[C@H](C)CCN1C(=O)[C@H](CCCN=C(N)N)NS(=O)(=O)C1=CC=CC2=C1NC[C@H](C)C2 KXNPVXPOPUZYGB-XYVMCAHJSA-N 0.000 claims 2
- 229960003856 argatroban Drugs 0.000 claims 2
- 229960004588 cilostazol Drugs 0.000 claims 2
- RRGUKTPIGVIEKM-UHFFFAOYSA-N cilostazol Chemical compound C=1C=C2NC(=O)CCC2=CC=1OCCCCC1=NN=NN1C1CCCCC1 RRGUKTPIGVIEKM-UHFFFAOYSA-N 0.000 claims 2
- 229960003850 dabigatran Drugs 0.000 claims 2
- YBSJFWOBGCMAKL-UHFFFAOYSA-N dabigatran Chemical compound N=1C2=CC(C(=O)N(CCC(O)=O)C=3N=CC=CC=3)=CC=C2N(C)C=1CNC1=CC=C(C(N)=N)C=C1 YBSJFWOBGCMAKL-UHFFFAOYSA-N 0.000 claims 2
- 229960004969 dalteparin Drugs 0.000 claims 2
- 229960003828 danaparoid Drugs 0.000 claims 2
- 229960002768 dipyridamole Drugs 0.000 claims 2
- IZEKFCXSFNUWAM-UHFFFAOYSA-N dipyridamole Chemical compound C=12N=C(N(CCO)CCO)N=C(N3CCCCC3)C2=NC(N(CCO)CCO)=NC=1N1CCCCC1 IZEKFCXSFNUWAM-UHFFFAOYSA-N 0.000 claims 2
- 229960000622 edoxaban Drugs 0.000 claims 2
- 229960000610 enoxaparin Drugs 0.000 claims 2
- 229960004468 eptifibatide Drugs 0.000 claims 2
- GLGOPUHVAZCPRB-LROMGURASA-N eptifibatide Chemical compound N1C(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H](CCCCNC(=N)N)NC(=O)CCSSC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]1CC1=CN=C2[C]1C=CC=C2 GLGOPUHVAZCPRB-LROMGURASA-N 0.000 claims 2
- 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 claims 2
- 229960001318 fondaparinux Drugs 0.000 claims 2
- 229920000669 heparin Polymers 0.000 claims 2
- 229960004408 lepirudin Drugs 0.000 claims 2
- OTQCKZUSUGYWBD-BRHMIFOHSA-N lepirudin Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(O)=O)C(C)C)[C@@H](C)O)[C@@H](C)O)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(C)C)[C@@H](C)O)C1=CC=C(O)C=C1 OTQCKZUSUGYWBD-BRHMIFOHSA-N 0.000 claims 2
- VYNKVNDKAOGAAQ-RUZDIDTESA-N n-[(1r)-2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-2-oxo-1-phenylethyl]-1h-indole-6-carboxamide Chemical compound C1CN(C)CCC1N1CCN(C(=O)[C@H](NC(=O)C=2C=C3NC=CC3=CC=2)C=2C=CC=CC=2)CC1 VYNKVNDKAOGAAQ-RUZDIDTESA-N 0.000 claims 2
- SHZKQBHERIJWAO-AATRIKPKSA-N ozagrel Chemical compound C1=CC(/C=C/C(=O)O)=CC=C1CN1C=NC=C1 SHZKQBHERIJWAO-AATRIKPKSA-N 0.000 claims 2
- 229950003837 ozagrel Drugs 0.000 claims 2
- 230000007170 pathology Effects 0.000 claims 2
- 239000000106 platelet aggregation inhibitor Substances 0.000 claims 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical group [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims 2
- 229940016667 resveratrol Drugs 0.000 claims 2
- 235000021283 resveratrol Nutrition 0.000 claims 2
- 159000000000 sodium salts Chemical class 0.000 claims 2
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 2
- 239000003868 thrombin inhibitor Substances 0.000 claims 2
- 229960003425 tirofiban Drugs 0.000 claims 2
- COKMIXFXJJXBQG-NRFANRHFSA-N tirofiban Chemical compound C1=CC(C[C@H](NS(=O)(=O)CCCC)C(O)=O)=CC=C1OCCCCC1CCNCC1 COKMIXFXJJXBQG-NRFANRHFSA-N 0.000 claims 2
- 229960005080 warfarin Drugs 0.000 claims 2
- PJVWKTKQMONHTI-UHFFFAOYSA-N warfarin Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 claims 2
- ZXIBCJHYVWYIKI-PZJWPPBQSA-N ximelagatran Chemical compound C1([C@@H](NCC(=O)OCC)C(=O)N2[C@@H](CC2)C(=O)NCC=2C=CC(=CC=2)C(\N)=N\O)CCCCC1 ZXIBCJHYVWYIKI-PZJWPPBQSA-N 0.000 claims 2
- 229960001522 ximelagatran Drugs 0.000 claims 2
- OFJRNBWSFXEHSA-UHFFFAOYSA-N 2-(3-amino-1,2-benzoxazol-5-yl)-n-[4-[2-[(dimethylamino)methyl]imidazol-1-yl]-2-fluorophenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide Chemical compound CN(C)CC1=NC=CN1C(C=C1F)=CC=C1NC(=O)C1=CC(C(F)(F)F)=NN1C1=CC=C(ON=C2N)C2=C1 OFJRNBWSFXEHSA-UHFFFAOYSA-N 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 208000005189 Embolism Diseases 0.000 claims 1
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 1
- 208000007718 Stable Angina Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010043561 Thrombocytopenic purpura Diseases 0.000 claims 1
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 206010047249 Venous thrombosis Diseases 0.000 claims 1
- 206010000891 acute myocardial infarction Diseases 0.000 claims 1
- 238000002399 angioplasty Methods 0.000 claims 1
- 238000013172 carotid endarterectomy Methods 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 210000004351 coronary vessel Anatomy 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 238000003780 insertion Methods 0.000 claims 1
- 230000037431 insertion Effects 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- MVPQUSQUURLQKF-MCPDASDXSA-E nonasodium;(2s,3s,4s,5r,6r)-6-[(2r,3r,4s,5r,6r)-6-[(2r,3s,4s,5r,6r)-2-carboxylato-4,5-dimethoxy-6-[(2r,3r,4s,5r,6s)-6-methoxy-4,5-disulfonatooxy-2-(sulfonatooxymethyl)oxan-3-yl]oxyoxan-3-yl]oxy-4,5-disulfonatooxy-2-(sulfonatooxymethyl)oxan-3-yl]oxy-4,5-di Chemical compound [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[O-]S(=O)(=O)O[C@@H]1[C@@H](OS([O-])(=O)=O)[C@@H](OC)O[C@H](COS([O-])(=O)=O)[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@@H]2[C@@H]([C@@H](OS([O-])(=O)=O)[C@H](O[C@H]3[C@@H]([C@@H](OC)[C@H](O[C@@H]4[C@@H]([C@@H](OC)[C@H](OC)[C@@H](COS([O-])(=O)=O)O4)OC)[C@H](O3)C([O-])=O)OC)[C@@H](COS([O-])(=O)=O)O2)OS([O-])(=O)=O)[C@H](C([O-])=O)O1 MVPQUSQUURLQKF-MCPDASDXSA-E 0.000 claims 1
- 201000011461 pre-eclampsia Diseases 0.000 claims 1
- 229950010535 razaxaban Drugs 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- CHGIUIJBKPEFOO-UHFFFAOYSA-N CNC(C(C=C1C(N2c(cc3)ccc3NC(NS(c([s]3)ccc3Cl)(=O)=O)=O)=O)F)C=C1NC2=O Chemical compound CNC(C(C=C1C(N2c(cc3)ccc3NC(NS(c([s]3)ccc3Cl)(=O)=O)=O)=O)F)C=C1NC2=O CHGIUIJBKPEFOO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91564907P | 2007-05-02 | 2007-05-02 | |
| US60/915,649 | 2007-05-02 | ||
| US91591107P | 2007-05-03 | 2007-05-03 | |
| US60/915,911 | 2007-05-03 | ||
| US94792107P | 2007-07-03 | 2007-07-03 | |
| US60/947,921 | 2007-07-03 | ||
| US97870007P | 2007-10-09 | 2007-10-09 | |
| US60/978,700 | 2007-10-09 | ||
| PCT/US2008/062561 WO2008137787A2 (en) | 2007-05-02 | 2008-05-02 | Combination therapy with a compound acting as a platelet adp receptor inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010526103A JP2010526103A (ja) | 2010-07-29 |
| JP2010526103A5 true JP2010526103A5 (https=) | 2011-09-01 |
| JP5439363B2 JP5439363B2 (ja) | 2014-03-12 |
Family
ID=39587017
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010506696A Expired - Fee Related JP5439363B2 (ja) | 2007-05-02 | 2008-05-02 | 血小板ａｄｐ受容体阻害剤として作用する化合物による併用療法 |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US20080279845A1 (https=) |
| EP (2) | EP2586439A1 (https=) |
| JP (1) | JP5439363B2 (https=) |
| KR (1) | KR101509829B1 (https=) |
| CN (1) | CN101686959B (https=) |
| AU (1) | AU2008247435A1 (https=) |
| BR (1) | BRPI0811000A2 (https=) |
| CA (1) | CA2684722A1 (https=) |
| CO (1) | CO6241105A2 (https=) |
| EA (1) | EA020045B1 (https=) |
| EC (1) | ECSP099775A (https=) |
| ES (1) | ES2467468T3 (https=) |
| GT (1) | GT200900283A (https=) |
| IL (1) | IL201826A (https=) |
| MA (1) | MA31396B1 (https=) |
| MX (1) | MX2009011755A (https=) |
| NZ (2) | NZ581324A (https=) |
| PT (1) | PT2146705E (https=) |
| TN (1) | TN2009000444A1 (https=) |
| WO (1) | WO2008137787A2 (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001064642A2 (en) * | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| US7696352B2 (en) * | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| KR101195801B1 (ko) | 2004-06-18 | 2012-11-05 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Ｘａ 인자 억제제 |
| EP1945632B1 (en) | 2005-11-08 | 2013-09-18 | Vertex Pharmaceuticals Incorporated | Heterocyclic modulators of atp-binding cassette transporters |
| US20090186810A1 (en) * | 2006-03-27 | 2009-07-23 | Portola Pharmaceuticals, Inc. | Potassium channel modulators and platelet procoagulant activity |
| NZ572418A (en) * | 2006-05-05 | 2011-08-26 | Millennium Pharm Inc | Factor xa inhibitors |
| CN101595092B (zh) | 2006-11-02 | 2012-02-01 | 米伦纽姆医药公司 | 合成因子xa抑制剂的医药盐的方法 |
| WO2008086226A2 (en) * | 2007-01-05 | 2008-07-17 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
| EA020531B1 (ru) * | 2007-04-13 | 2014-11-28 | Милленниум Фармасьютикалз, Инк. | КОМБИНИРОВАННАЯ ТЕРАПИЯ АНТИКОАГУЛИРУЮЩЕГО СРЕДСТВА С СОЕДИНЕНИЕМ, КОТОРОЕ ДЕЙСТВУЕТ КАК ИНГИБИТОР ФАКТОРА Ха |
| SI2225230T1 (sl) | 2007-12-07 | 2017-03-31 | Vertex Pharmaceuticals Incorporated | Trdne oblike 3-(6-(1-2,2-difluorobenzo(d)(1,3)dioxol-5-il)ciklopropan- karboksamido)-3-metilpiridin-2-il) benzojske kisline |
| AU2009313867A1 (en) * | 2008-11-14 | 2011-06-30 | Patheon Inc. | Solid composition for controlled release of ionizable active agents with poor aqueous solubility at low pH and methods of use thereof |
| CN102762550B (zh) | 2009-12-17 | 2015-04-01 | 米伦纽姆医药公司 | Xa因子抑制剂的盐和结晶形式 |
| US8742120B2 (en) | 2009-12-17 | 2014-06-03 | Millennium Pharmaceuticals, Inc. | Methods of preparing factor xa inhibitors and salts thereof |
| EP2633857B1 (en) * | 2009-12-23 | 2015-08-12 | ratiopharm GmbH | Solid pharmaceutical dosage form of ticagrelor and acetylsalicylic acid |
| JP2013518034A (ja) * | 2010-01-21 | 2013-05-20 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 薬物として使用するための特別な組成物 |
| SI2538925T1 (sl) * | 2010-02-25 | 2016-04-29 | Bristol-Myers Squibb Company | Apiksaban formulacije |
| HRP20211752T1 (hr) | 2010-04-07 | 2022-02-18 | Vertex Pharmaceuticals Incorporated | Farmaceutski pripravci 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline i njihova primjena |
| AR082804A1 (es) | 2010-09-01 | 2013-01-09 | Portola Pharm Inc | Formas cristalinas de un inhibidor del factor xa |
| RU2597423C2 (ru) * | 2011-03-29 | 2016-09-10 | Санофи | Бензойнокислая соль отамиксабана |
| US20150224091A1 (en) * | 2011-08-31 | 2015-08-13 | Portola Pharmaceuticals, Inc. | Prevention and treatment of thrombosis in medically ill patients |
| WO2013112804A1 (en) | 2012-01-25 | 2013-08-01 | Vertex Pharmaceuticals Incorporated | Formulations of 3-(6-(1-(2.2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| WO2014099695A1 (en) * | 2012-12-19 | 2014-06-26 | Merck Sharp & Dohme Corp. | Factor ixa inhibitors |
| WO2014120346A1 (en) * | 2012-12-19 | 2014-08-07 | Merck Sharp & Dohme Corp. | Factor ixa inhibitors |
| US9695198B2 (en) | 2012-12-19 | 2017-07-04 | Merck Sharp & Dohme Corp. | Factor IXa inhibitors |
| US9200268B2 (en) | 2012-12-27 | 2015-12-01 | Portola Pharmaceuticals, Inc. | Compounds and methods for purification of serine proteases |
| JP6963896B2 (ja) | 2013-11-12 | 2021-11-10 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Ｃｆｔｒ媒介性疾患の処置のための医薬組成物を調製する方法 |
| WO2015123091A1 (en) * | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| CN106831553A (zh) * | 2015-09-11 | 2017-06-13 | 天津科伦药物研究有限公司 | 贝曲西班或其类似物的制备方法 |
| CN105250286A (zh) * | 2015-11-13 | 2016-01-20 | 谭惠娟 | 一种抗血栓组合物 |
| EP3254674A1 (en) * | 2016-06-08 | 2017-12-13 | Sandoz Ag | Pharmaceutical compositions of betrixaban maleate |
| EP3541375B1 (en) | 2016-11-18 | 2023-08-23 | Merck Sharp & Dohme LLC | Factor xiia inhibitors |
| US11654036B2 (en) | 2020-05-26 | 2023-05-23 | Elixir Medical Corporation | Anticoagulant compounds and methods and devices for their use |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6440147B1 (en) * | 1998-09-03 | 2002-08-27 | Rubicor Medical, Inc. | Excisional biopsy devices and methods |
| US6509348B1 (en) * | 1998-11-03 | 2003-01-21 | Bristol-Myers Squibb Company | Combination of an ADP-receptor blocking antiplatelet drug and a thromboxane A2 receptor antagonist and a method for inhibiting thrombus formation employing such combination |
| CA2360305A1 (en) | 1999-02-09 | 2000-08-17 | Bristol-Myers Squibb Company | Lactam inhibitors of fxa and method |
| US6844367B1 (en) * | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| ES2316383T3 (es) * | 1999-09-17 | 2009-04-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del factor xa. |
| MY125533A (en) | 1999-12-06 | 2006-08-30 | Bristol Myers Squibb Co | Heterocyclic dihydropyrimidine compounds |
| US6906063B2 (en) | 2000-02-04 | 2005-06-14 | Portola Pharmaceuticals, Inc. | Platelet ADP receptor inhibitors |
| WO2001064642A2 (en) * | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| US20040192753A1 (en) | 2000-06-15 | 2004-09-30 | Samuel Chackalamannil | Methods of use of thrombin receptor antagonists |
| US7235567B2 (en) | 2000-06-15 | 2007-06-26 | Schering Corporation | Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist |
| US7312325B2 (en) | 2000-09-26 | 2007-12-25 | Duke University | RNA aptamers and methods for identifying the same |
| US7312235B2 (en) * | 2001-03-30 | 2007-12-25 | Millennium Pharmaceuticals, Inc. | Benzamide inhibitors of factor Xa |
| ZA200508481B (en) * | 2003-04-09 | 2007-04-25 | Japan Tobacco Inc | Heteroaromatic pentacyclic compound and medicinal use thereof |
| KR20060113699A (ko) | 2003-10-03 | 2006-11-02 | 포톨라 파마슈티컬스, 인코포레이티드 | 치환된 이소퀴놀리논 |
| US7022695B2 (en) * | 2003-10-09 | 2006-04-04 | Millennium Pharmaceuticals, Inc. | Thioether-substituted benzamides as inhibitors of Factor Xa |
| KR101195801B1 (ko) * | 2004-06-18 | 2012-11-05 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Ｘａ 인자 억제제 |
| US7696352B2 (en) * | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| WO2006045756A1 (en) * | 2004-10-25 | 2006-05-04 | Boehringer Ingelheim International Gmbh | Use of dipyridamole in combination with antithrombotics for treatment and prevention of thromboembolic diseases |
| EP1844002A1 (en) | 2005-02-02 | 2007-10-17 | Vitae Pharmaceuticals, Inc. | 1-acylamino-2-hydroxy-3-amino-w-arylalkanes as renin inhibitors |
| US7467697B2 (en) * | 2005-10-07 | 2008-12-23 | Ford Global Technologies, Llc | Electromagnetic coupling device for engine accessories |
| PT1951254E (pt) * | 2005-11-03 | 2012-04-12 | Portola Pharm Inc | [4-(6-halo-7-substituído-2,4-dioxo-1,4-di-hidro-2hquinazolin- 3-il)-fenil]-5-cloro-tiofen-2-il-sulfonilureias e formas e métodos relacionados com as mesmas |
| PE20070717A1 (es) | 2005-11-08 | 2007-08-17 | Millennium Pharm Inc | Sal de maleato y polimorfo de [2-({4-[(dimetilamino)iminometil]fenil}carbonilamino)-5-metoxifenil]-n-(5-cloro-(2-piridil))carboxamida |
| US20090186810A1 (en) * | 2006-03-27 | 2009-07-23 | Portola Pharmaceuticals, Inc. | Potassium channel modulators and platelet procoagulant activity |
| NZ572418A (en) | 2006-05-05 | 2011-08-26 | Millennium Pharm Inc | Factor xa inhibitors |
| KR101472765B1 (ko) * | 2006-12-08 | 2014-12-15 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 경구용 Ｘａ 인자 억제제를 포함하는 단위 용량 제형 및 경구용 Ｘａ 인자 억제제를 사용하는 혈전증의 치료 방법 |
| WO2008086226A2 (en) * | 2007-01-05 | 2008-07-17 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
| EA020531B1 (ru) * | 2007-04-13 | 2014-11-28 | Милленниум Фармасьютикалз, Инк. | КОМБИНИРОВАННАЯ ТЕРАПИЯ АНТИКОАГУЛИРУЮЩЕГО СРЕДСТВА С СОЕДИНЕНИЕМ, КОТОРОЕ ДЕЙСТВУЕТ КАК ИНГИБИТОР ФАКТОРА Ха |
-
2008
- 2008-05-02 KR KR1020097024870A patent/KR101509829B1/ko not_active Expired - Fee Related
- 2008-05-02 EP EP13151486.1A patent/EP2586439A1/en not_active Withdrawn
- 2008-05-02 EA EA200901442A patent/EA020045B1/ru not_active IP Right Cessation
- 2008-05-02 NZ NZ581324A patent/NZ581324A/en not_active IP Right Cessation
- 2008-05-02 MX MX2009011755A patent/MX2009011755A/es active IP Right Grant
- 2008-05-02 EP EP08747590.1A patent/EP2146705B1/en not_active Not-in-force
- 2008-05-02 PT PT87475901T patent/PT2146705E/pt unknown
- 2008-05-02 WO PCT/US2008/062561 patent/WO2008137787A2/en not_active Ceased
- 2008-05-02 JP JP2010506696A patent/JP5439363B2/ja not_active Expired - Fee Related
- 2008-05-02 CA CA002684722A patent/CA2684722A1/en not_active Abandoned
- 2008-05-02 BR BRPI0811000-0A2A patent/BRPI0811000A2/pt not_active Application Discontinuation
- 2008-05-02 AU AU2008247435A patent/AU2008247435A1/en not_active Abandoned
- 2008-05-02 ES ES08747590.1T patent/ES2467468T3/es active Active
- 2008-05-02 US US12/114,706 patent/US20080279845A1/en not_active Abandoned
- 2008-05-02 NZ NZ599556A patent/NZ599556A/xx not_active IP Right Cessation
- 2008-05-02 CN CN200880021658.3A patent/CN101686959B/zh not_active Expired - Fee Related
-
2009
- 2009-10-23 TN TNP2009000444A patent/TN2009000444A1/fr unknown
- 2009-10-29 IL IL201826A patent/IL201826A/en not_active IP Right Cessation
- 2009-10-30 GT GT200900283A patent/GT200900283A/es unknown
- 2009-11-20 CO CO09132196A patent/CO6241105A2/es not_active Application Discontinuation
- 2009-11-26 MA MA32375A patent/MA31396B1/fr unknown
- 2009-12-01 EC EC2009009775A patent/ECSP099775A/es unknown
-
2010
- 2010-10-20 US US12/908,837 patent/US8946219B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2010526103A5 (https=) | ||
| Nopp et al. | Factor XI inhibitors for prevention and treatment of venous thromboembolism: a review on the rationale and update on current evidence | |
| US8946219B2 (en) | Combination therapy with a compound acting as a platelet ADP receptor inhibitor | |
| Bates et al. | The status of new anticoagulants | |
| Harenberg et al. | Current and future prospects for anticoagulant therapy: inhibitors of factor Xa and factor IIa | |
| Ahrens et al. | Development and clinical applications of novel oral anticoagulants. Part II. Drugs under clinical investigation | |
| Rupprecht et al. | Clinical pharmacology of direct and indirect factor Xa inhibitors | |
| Goel et al. | Newer oral anticoagulant agents: a new era in medicine | |
| TWI377945B (en) | Prevention and treatment of thromboembolic disorders | |
| Harenberg | Development of new anticoagulants: present and future | |
| Ieko et al. | Development of new anticoagulants targeting coagulation factor XI and prospects for clinical use | |
| Broussalis et al. | Latest developments in anticoagulant drug discovery | |
| Hammwöhner et al. | Will warfarin soon be passe? New approaches to stroke prevention in atrial fibrillation | |
| Yong et al. | Factor Xa inhibitors in acute coronary syndromes and venous thromboembolism | |
| Harenberg | Indirect and direct anticoagulants predominantly inhibiting factor Xa | |
| Chaudhry | Factor Xa inhibitors, Era to replace traditional anticoagulants | |
| Muralidharan-Chari et al. | Ciraparantag. Heparin neutralizer, anticoagulant reversal agent | |
| Ahmad et al. | New oral anticoagulants: An update | |
| Escolar et al. | Betrixaban: a direct oral inhibitor of activated factor X for the prophylaxis of venous thromboembolism in patients hospitalized for acute medical illness | |
| Capranzano et al. | Clinical development of selective anticoagulants: a state of the art | |
| Faltas | A new anticoagulant for a new era: review of recent data on dabigatran etexilate | |
| Chapman | Thrombus formation and use of anticoagulants. | |
| Chapman | Current drug information: Thrombus formation and use of anticoagulants | |
| McRae | Drugs that affect blood coagulation, fibrinolysis, and hemostasis | |
| NZ733574B2 (en) | Dihydroindolizinone derivative |