JP2010526104A - トロンボキサン受容体アンタゴニストを用いて血栓症を治療及び予防する単位用量製剤及び方法 - Google Patents
トロンボキサン受容体アンタゴニストを用いて血栓症を治療及び予防する単位用量製剤及び方法 Download PDFInfo
- Publication number
- JP2010526104A JP2010526104A JP2010506700A JP2010506700A JP2010526104A JP 2010526104 A JP2010526104 A JP 2010526104A JP 2010506700 A JP2010506700 A JP 2010506700A JP 2010506700 A JP2010506700 A JP 2010506700A JP 2010526104 A JP2010526104 A JP 2010526104A
- Authority
- JP
- Japan
- Prior art keywords
- amount
- ifetroban
- platelet aggregation
- plasma concentration
- patient
- 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.)
- Pending
Links
- 238000000034 method Methods 0.000 title claims abstract description 136
- 208000007536 Thrombosis Diseases 0.000 title claims abstract description 62
- 239000000203 mixture Substances 0.000 title claims abstract description 56
- 238000009472 formulation Methods 0.000 title claims abstract description 37
- 102000003938 Thromboxane Receptors Human genes 0.000 title description 42
- 108090000300 Thromboxane Receptors Proteins 0.000 title description 42
- 229940044551 receptor antagonist Drugs 0.000 title description 11
- 239000002464 receptor antagonist Substances 0.000 title description 11
- 239000003146 anticoagulant agent Substances 0.000 claims abstract description 138
- 229960004676 antithrombotic agent Drugs 0.000 claims abstract description 128
- 208000024172 Cardiovascular disease Diseases 0.000 claims abstract description 15
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims description 134
- BBPRUNPUJIUXSE-DXKRWKNPSA-N ifetroban Chemical group 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 description 103
- 229950004274 ifetroban Drugs 0.000 claims description 102
- 239000008280 blood Substances 0.000 claims description 76
- 210000004369 blood Anatomy 0.000 claims description 72
- 230000036470 plasma concentration Effects 0.000 claims description 66
- 239000000556 agonist Substances 0.000 claims description 53
- 102000008186 Collagen Human genes 0.000 claims description 35
- 108010035532 Collagen Proteins 0.000 claims description 35
- 229920001436 collagen Polymers 0.000 claims description 35
- 230000002401 inhibitory effect Effects 0.000 claims description 21
- 241000124008 Mammalia Species 0.000 claims description 18
- 230000010412 perfusion Effects 0.000 claims description 17
- 230000002776 aggregation Effects 0.000 claims description 16
- 238000004220 aggregation Methods 0.000 claims description 16
- 230000001225 therapeutic effect Effects 0.000 claims description 12
- 229940122202 Thromboxane receptor antagonist Drugs 0.000 claims description 10
- 239000002396 thromboxane receptor blocking agent Substances 0.000 claims description 10
- 238000005259 measurement Methods 0.000 claims description 7
- 201000001320 Atherosclerosis Diseases 0.000 claims description 6
- 208000010378 Pulmonary Embolism Diseases 0.000 claims description 6
- 230000005540 biological transmission Effects 0.000 claims description 6
- 206010053567 Coagulopathies Diseases 0.000 claims description 5
- 206010067347 Thrombotic cerebral infarction Diseases 0.000 claims description 5
- 230000035602 clotting Effects 0.000 claims description 5
- 210000004351 coronary vessel Anatomy 0.000 claims description 5
- 208000002815 pulmonary hypertension Diseases 0.000 claims description 5
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 claims description 4
- 229930182837 (R)-adrenaline Natural products 0.000 claims description 4
- 206010002388 Angina unstable Diseases 0.000 claims description 4
- 208000007814 Unstable Angina Diseases 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 229960005139 epinephrine Drugs 0.000 claims description 4
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims description 4
- 208000010125 myocardial infarction Diseases 0.000 claims description 4
- 206010002383 Angina Pectoris Diseases 0.000 claims description 3
- 206010051055 Deep vein thrombosis Diseases 0.000 claims description 3
- 206010038563 Reocclusion Diseases 0.000 claims description 3
- 206010040070 Septic Shock Diseases 0.000 claims description 3
- 208000032109 Transient ischaemic attack Diseases 0.000 claims description 3
- 206010047249 Venous thrombosis Diseases 0.000 claims description 3
- 238000007887 coronary angioplasty Methods 0.000 claims description 3
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims description 3
- 208000037803 restenosis Diseases 0.000 claims description 3
- 230000036303 septic shock Effects 0.000 claims description 3
- 208000011580 syndromic disease Diseases 0.000 claims description 3
- 238000002560 therapeutic procedure Methods 0.000 claims description 3
- 230000002537 thrombolytic effect Effects 0.000 claims description 3
- 201000010875 transient cerebral ischemia Diseases 0.000 claims description 3
- 206010014498 Embolic stroke Diseases 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 229960001138 acetylsalicylic acid Drugs 0.000 description 62
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical group CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 61
- 238000003556 assay Methods 0.000 description 32
- 239000005557 antagonist Substances 0.000 description 31
- 150000003839 salts Chemical class 0.000 description 31
- -1 cyanoamino Chemical group 0.000 description 25
- 150000002148 esters Chemical class 0.000 description 25
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 22
- 102100037600 P2Y purinoceptor 1 Human genes 0.000 description 18
- 108010085249 Purinergic P2 Receptors Proteins 0.000 description 18
- 230000005764 inhibitory process Effects 0.000 description 17
- 239000004480 active ingredient Substances 0.000 description 16
- YZXBAPSDXZZRGB-DOFZRALJSA-N arachidonic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O YZXBAPSDXZZRGB-DOFZRALJSA-N 0.000 description 16
- 230000015572 biosynthetic process Effects 0.000 description 16
- 210000002966 serum Anatomy 0.000 description 16
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 15
- 150000001875 compounds Chemical class 0.000 description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 14
- 239000003814 drug Substances 0.000 description 14
- 230000002785 anti-thrombosis Effects 0.000 description 13
- XTWYTFMLZFPYCI-KQYNXXCUSA-N 5'-adenylphosphoric acid Chemical group C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O XTWYTFMLZFPYCI-KQYNXXCUSA-N 0.000 description 12
- 230000000694 effects Effects 0.000 description 12
- 201000010099 disease Diseases 0.000 description 11
- 238000001727 in vivo Methods 0.000 description 11
- 210000004623 platelet-rich plasma Anatomy 0.000 description 11
- 239000003795 chemical substances by application Substances 0.000 description 10
- 239000003112 inhibitor Substances 0.000 description 10
- 239000008194 pharmaceutical composition Substances 0.000 description 10
- 238000013268 sustained release Methods 0.000 description 10
- 239000005552 B01AC04 - Clopidogrel Substances 0.000 description 9
- GKTWGGQPFAXNFI-HNNXBMFYSA-N clopidogrel Chemical compound C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl GKTWGGQPFAXNFI-HNNXBMFYSA-N 0.000 description 9
- 238000013270 controlled release Methods 0.000 description 9
- 238000013167 light transmission aggregometry Methods 0.000 description 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 9
- 239000000243 solution Substances 0.000 description 9
- PHWBOXQYWZNQIN-UHFFFAOYSA-N ticlopidine Chemical compound ClC1=CC=CC=C1CN1CC(C=CS2)=C2CC1 PHWBOXQYWZNQIN-UHFFFAOYSA-N 0.000 description 9
- 229940114079 arachidonic acid Drugs 0.000 description 8
- 235000021342 arachidonic acid Nutrition 0.000 description 8
- 229960003009 clopidogrel Drugs 0.000 description 8
- 239000002552 dosage form Substances 0.000 description 8
- 229940079593 drug Drugs 0.000 description 8
- 238000000099 in vitro assay Methods 0.000 description 8
- 239000012730 sustained-release form Substances 0.000 description 8
- RZWIIPASKMUIAC-VQTJNVASSA-N thromboxane Chemical compound CCCCCCCC[C@H]1OCCC[C@@H]1CCCCCCC RZWIIPASKMUIAC-VQTJNVASSA-N 0.000 description 8
- 239000005528 B01AC05 - Ticlopidine Substances 0.000 description 7
- 229940123583 Factor Xa inhibitor Drugs 0.000 description 7
- 230000008901 benefit Effects 0.000 description 7
- 238000000338 in vitro Methods 0.000 description 7
- 210000002381 plasma Anatomy 0.000 description 7
- DTGLZDAWLRGWQN-UHFFFAOYSA-N prasugrel Chemical compound C1CC=2SC(OC(=O)C)=CC=2CN1C(C=1C(=CC=CC=1)F)C(=O)C1CC1 DTGLZDAWLRGWQN-UHFFFAOYSA-N 0.000 description 7
- 230000002829 reductive effect Effects 0.000 description 7
- 229960005001 ticlopidine Drugs 0.000 description 7
- 239000005465 B01AC22 - Prasugrel Substances 0.000 description 6
- 229940127218 antiplatelet drug Drugs 0.000 description 6
- 229960004197 prasugrel Drugs 0.000 description 6
- 102000005962 receptors Human genes 0.000 description 6
- 108020003175 receptors Proteins 0.000 description 6
- 230000004044 response Effects 0.000 description 6
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 description 5
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 5
- 241000282412 Homo Species 0.000 description 5
- 208000006673 asthma Diseases 0.000 description 5
- 239000011575 calcium Substances 0.000 description 5
- 229910052791 calcium Inorganic materials 0.000 description 5
- ACSIXWWBWUQEHA-UHFFFAOYSA-N clodronic acid Chemical compound OP(O)(=O)C(Cl)(Cl)P(O)(O)=O ACSIXWWBWUQEHA-UHFFFAOYSA-N 0.000 description 5
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 5
- 238000001990 intravenous administration Methods 0.000 description 5
- 150000004702 methyl esters Chemical class 0.000 description 5
- 230000010118 platelet activation Effects 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 229940127219 anticoagulant drug Drugs 0.000 description 4
- 239000002775 capsule Substances 0.000 description 4
- 238000011161 development Methods 0.000 description 4
- 239000003085 diluting agent Substances 0.000 description 4
- 230000002526 effect on cardiovascular system Effects 0.000 description 4
- 238000007918 intramuscular administration Methods 0.000 description 4
- 230000001404 mediated effect Effects 0.000 description 4
- 239000000106 platelet aggregation inhibitor Substances 0.000 description 4
- 239000003755 preservative agent Substances 0.000 description 4
- 108090000765 processed proteins & peptides Proteins 0.000 description 4
- 102000004196 processed proteins & peptides Human genes 0.000 description 4
- 239000000719 purinergic P2Y receptor antagonist Substances 0.000 description 4
- 229940124597 therapeutic agent Drugs 0.000 description 4
- DYWAPFDKPAHSED-UHFFFAOYSA-N 2-cycloheptyloxepane Chemical compound C1CCCCCC1C1OCCCCC1 DYWAPFDKPAHSED-UHFFFAOYSA-N 0.000 description 3
- XMIIGOLPHOKFCH-UHFFFAOYSA-N 3-phenylpropionic acid Chemical compound OC(=O)CCC1=CC=CC=C1 XMIIGOLPHOKFCH-UHFFFAOYSA-N 0.000 description 3
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 3
- 206010003178 Arterial thrombosis Diseases 0.000 description 3
- 108010029697 CD40 Ligand Proteins 0.000 description 3
- 102100032937 CD40 ligand Human genes 0.000 description 3
- 108010074860 Factor Xa Proteins 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 108090000190 Thrombin Proteins 0.000 description 3
- KVLRBRZHCOVMNX-IDTAVKCVSA-N [(2r,3s,4r,5r)-3,4-dihydroxy-5-[6-(2-methylsulfanylethylamino)-2-(3,3,3-trifluoropropylsulfanyl)purin-9-yl]oxolan-2-yl]methyl dihydrogen phosphate Chemical compound C1=NC=2C(NCCSC)=NC(SCCC(F)(F)F)=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@H]1O KVLRBRZHCOVMNX-IDTAVKCVSA-N 0.000 description 3
- 239000007864 aqueous solution Substances 0.000 description 3
- 230000023555 blood coagulation Effects 0.000 description 3
- 238000000586 desensitisation Methods 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 239000006185 dispersion Substances 0.000 description 3
- 239000008187 granular material Substances 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 239000013642 negative control Substances 0.000 description 3
- 230000037361 pathway Effects 0.000 description 3
- 229920001184 polypeptide Polymers 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 239000007916 tablet composition Substances 0.000 description 3
- XUTLOCQNGLJNSA-RGVLZGJSSA-N terbogrel Chemical compound CC(C)(C)\N=C(/NC#N)NC1=CC=CC(C(=C/CCCC(O)=O)\C=2C=NC=CC=2)=C1 XUTLOCQNGLJNSA-RGVLZGJSSA-N 0.000 description 3
- 229950006665 terbogrel Drugs 0.000 description 3
- 229960004072 thrombin Drugs 0.000 description 3
- 230000001732 thrombotic effect Effects 0.000 description 3
- DSNBHJFQCNUKMA-SCKDECHMSA-N thromboxane A2 Chemical compound OC(=O)CCC\C=C/C[C@@H]1[C@@H](/C=C/[C@@H](O)CCCCC)O[C@@H]2O[C@H]1C2 DSNBHJFQCNUKMA-SCKDECHMSA-N 0.000 description 3
- IULOBWFWYDMECP-UHFFFAOYSA-N 2-[4-[2-[(4-chlorophenyl)sulfonylamino]ethyl]phenyl]acetic acid Chemical compound C1=CC(CC(=O)O)=CC=C1CCNS(=O)(=O)C1=CC=C(Cl)C=C1 IULOBWFWYDMECP-UHFFFAOYSA-N 0.000 description 2
- YURNCBVQZBJDAJ-UHFFFAOYSA-N 2-heptenoic acid Chemical compound CCCCC=CC(O)=O YURNCBVQZBJDAJ-UHFFFAOYSA-N 0.000 description 2
- JLPYLHLUHJOPNL-UHFFFAOYSA-N 3-[1-[(4-chlorophenyl)methyl]-5-fluoro-3-methyl-2-indolyl]-2,2-dimethylpropanoic acid Chemical compound C12=CC=C(F)C=C2C(C)=C(CC(C)(C)C(O)=O)N1CC1=CC=C(Cl)C=C1 JLPYLHLUHJOPNL-UHFFFAOYSA-N 0.000 description 2
- FJKROLUGYXJWQN-UHFFFAOYSA-N 4-hydroxybenzoic acid Chemical compound OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 2
- KYWCWBXGRWWINE-UHFFFAOYSA-N 4-methoxy-N1,N3-bis(3-pyridinylmethyl)benzene-1,3-dicarboxamide Chemical compound COC1=CC=C(C(=O)NCC=2C=NC=CC=2)C=C1C(=O)NCC1=CC=CN=C1 KYWCWBXGRWWINE-UHFFFAOYSA-N 0.000 description 2
- 108010080422 CD39 antigen Proteins 0.000 description 2
- 108010048623 Collagen Receptors Proteins 0.000 description 2
- 102000001187 Collagen Type III Human genes 0.000 description 2
- 108010069502 Collagen Type III Proteins 0.000 description 2
- 206010010904 Convulsion Diseases 0.000 description 2
- 102100029722 Ectonucleoside triphosphate diphosphohydrolase 1 Human genes 0.000 description 2
- 108010012088 Fibrinogen Receptors Proteins 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- 101100501552 Homo sapiens ENTPD1 gene Proteins 0.000 description 2
- 101001012447 Homo sapiens Ectonucleoside triphosphate diphosphohydrolase 1 Proteins 0.000 description 2
- 206010021143 Hypoxia Diseases 0.000 description 2
- 239000002172 P2Y12 inhibitor Substances 0.000 description 2
- 102100038277 Prostaglandin G/H synthase 1 Human genes 0.000 description 2
- 108050003243 Prostaglandin G/H synthase 1 Proteins 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 108010000499 Thromboplastin Proteins 0.000 description 2
- 102000002262 Thromboplastin Human genes 0.000 description 2
- GAORIKFOSRGMEL-WOUKDFQISA-N [(2r,3s,4r,5r)-5-(6-amino-2-propylsulfanylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate Chemical compound C12=NC(SCCC)=NC(N)=C2N=CN1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@H]1O GAORIKFOSRGMEL-WOUKDFQISA-N 0.000 description 2
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 206010000891 acute myocardial infarction Diseases 0.000 description 2
- 230000004520 agglutination Effects 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 230000002744 anti-aggregatory effect Effects 0.000 description 2
- 239000003963 antioxidant agent Substances 0.000 description 2
- 230000006502 antiplatelets effects Effects 0.000 description 2
- 230000009286 beneficial effect Effects 0.000 description 2
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
- PAEBIVWUMLRPSK-IDTAVKCVSA-N cangrelor Chemical compound C1=NC=2C(NCCSC)=NC(SCCC(F)(F)F)=NC=2N1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)C(Cl)(Cl)P(O)(O)=O)[C@@H](O)[C@H]1O PAEBIVWUMLRPSK-IDTAVKCVSA-N 0.000 description 2
- 229960001080 cangrelor Drugs 0.000 description 2
- 150000001735 carboxylic acids Chemical class 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 230000007123 defense Effects 0.000 description 2
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 2
- 208000037765 diseases and disorders Diseases 0.000 description 2
- 239000003527 fibrinolytic agent Substances 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 description 2
- 230000007954 hypoxia Effects 0.000 description 2
- 230000006698 induction Effects 0.000 description 2
- 238000007912 intraperitoneal administration Methods 0.000 description 2
- 230000000670 limiting effect Effects 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 2
- 238000012544 monitoring process Methods 0.000 description 2
- 230000004660 morphological change Effects 0.000 description 2
- 238000002733 pharmacodynamic assay Methods 0.000 description 2
- LCPDWSOZIOUXRV-UHFFFAOYSA-N phenoxyacetic acid Chemical compound OC(=O)COC1=CC=CC=C1 LCPDWSOZIOUXRV-UHFFFAOYSA-N 0.000 description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 2
- WLJVXDMOQOGPHL-UHFFFAOYSA-N phenylacetic acid Chemical compound OC(=O)CC1=CC=CC=C1 WLJVXDMOQOGPHL-UHFFFAOYSA-N 0.000 description 2
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 description 2
- 239000002953 phosphate buffered saline Substances 0.000 description 2
- YIBNHAJFJUQSRA-YNNPMVKQSA-N prostaglandin H2 Chemical compound C1[C@@H]2OO[C@H]1[C@H](/C=C/[C@@H](O)CCCCC)[C@H]2C\C=C/CCCC(O)=O YIBNHAJFJUQSRA-YNNPMVKQSA-N 0.000 description 2
- 229940127293 prostanoid Drugs 0.000 description 2
- 150000003814 prostanoids Chemical class 0.000 description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- 150000003384 small molecules Chemical class 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- WOHSQDNIXPEQAE-QBKVZTCDSA-M sodium;3-[2-[[(1s,2r,3s,4r)-3-[4-(pentylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoate Chemical compound [Na+].CCCCCNC(=O)C1=COC([C@H]2[C@H]([C@@H]3CC[C@H]2O3)CC=2C(=CC=CC=2)CCC([O-])=O)=N1 WOHSQDNIXPEQAE-QBKVZTCDSA-M 0.000 description 2
- 238000010561 standard procedure Methods 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 230000002459 sustained effect Effects 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- DBDCNCCRPKTRSD-UHFFFAOYSA-N thieno[3,2-b]pyridine Chemical class C1=CC=C2SC=CC2=N1 DBDCNCCRPKTRSD-UHFFFAOYSA-N 0.000 description 2
- 229960000103 thrombolytic agent Drugs 0.000 description 2
- 231100000440 toxicity profile Toxicity 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- 108010047303 von Willebrand Factor Proteins 0.000 description 2
- 102100036537 von Willebrand factor Human genes 0.000 description 2
- NIONDZDPPYHYKY-SNAWJCMRSA-N (2E)-hexenoic acid Chemical compound CCC\C=C\C(O)=O NIONDZDPPYHYKY-SNAWJCMRSA-N 0.000 description 1
- GQGRDYWMOPRROR-XUSMOFMBSA-N (z)-7-[(1r,2r,3s,5s)-3-hydroxy-5-[(4-phenylphenyl)methoxy]-2-piperidin-1-ylcyclopentyl]hept-4-enoic acid Chemical compound O([C@H]1C[C@@H]([C@@H]([C@H]1CC\C=C/CCC(O)=O)N1CCCCC1)O)CC(C=C1)=CC=C1C1=CC=CC=C1 GQGRDYWMOPRROR-XUSMOFMBSA-N 0.000 description 1
- ZOESDBZUBAGGTA-UHFFFAOYSA-N 2-(2-acetyloxy-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)-2-cyclopropyl-2-(2-fluorophenyl)acetic acid Chemical compound C(C)(=O)OC1=CC=2CN(CCC=2S1)C(C1=C(C=CC=C1)F)(C1CC1)C(=O)O ZOESDBZUBAGGTA-UHFFFAOYSA-N 0.000 description 1
- VLMZAUCKMYJSGM-UHFFFAOYSA-N 2-[4-[3-(4-chlorophenyl)sulfonylpropyl]phenyl]acetic acid Chemical compound C1=CC(CC(=O)O)=CC=C1CCCS(=O)(=O)C1=CC=C(Cl)C=C1 VLMZAUCKMYJSGM-UHFFFAOYSA-N 0.000 description 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 description 1
- 229940090248 4-hydroxybenzoic acid Drugs 0.000 description 1
- UHZXPFSCJFEFPS-UHFFFAOYSA-N 7-(cyclohepten-1-yl)-2,3,4,5-tetrahydrooxepine Chemical class C1CCCCC=C1C1=CCCCCO1 UHZXPFSCJFEFPS-UHFFFAOYSA-N 0.000 description 1
- ZWAVGFSZMACJHA-PMNBYGLBSA-N 7-[2-Trifluoromethyl-4-(2-hydroxyphenyl)-1,3-dioxan-cis-5-yl]-hept-5z-enoic acid Chemical compound OC(=O)CCC\C=C/C[C@@H]1CO[C@H](C(F)(F)F)O[C@@H]1C1=CC=CC=C1O ZWAVGFSZMACJHA-PMNBYGLBSA-N 0.000 description 1
- 206010067484 Adverse reaction Diseases 0.000 description 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 1
- 102400000432 CD40 ligand, soluble form Human genes 0.000 description 1
- 101800000267 CD40 ligand, soluble form Proteins 0.000 description 1
- 101150071146 COX2 gene Proteins 0.000 description 1
- 101100114534 Caenorhabditis elegans ctc-2 gene Proteins 0.000 description 1
- 102000001327 Chemokine CCL5 Human genes 0.000 description 1
- 108010055166 Chemokine CCL5 Proteins 0.000 description 1
- 102000009268 Collagen Receptors Human genes 0.000 description 1
- 102000012422 Collagen Type I Human genes 0.000 description 1
- 108010022452 Collagen Type I Proteins 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- WQZGKKKJIJFFOK-QTVWNMPRSA-N D-mannopyranose Chemical compound OC[C@H]1OC(O)[C@@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-QTVWNMPRSA-N 0.000 description 1
- 229920002307 Dextran Polymers 0.000 description 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 1
- 208000005189 Embolism Diseases 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108010049003 Fibrinogen Proteins 0.000 description 1
- 102000008946 Fibrinogen Human genes 0.000 description 1
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 description 1
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 description 1
- 101150022345 GAS6 gene Proteins 0.000 description 1
- 108010024636 Glutathione Proteins 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- 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 description 1
- 101001098232 Homo sapiens P2Y purinoceptor 1 Proteins 0.000 description 1
- 101000582950 Homo sapiens Platelet factor 4 Proteins 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 102100025305 Integrin alpha-2 Human genes 0.000 description 1
- 102000004310 Ion Channels Human genes 0.000 description 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 241000238367 Mya arenaria Species 0.000 description 1
- 101150000187 PTGS2 gene Proteins 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 102100030304 Platelet factor 4 Human genes 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- LDXDSHIEDAPSSA-OAHLLOKOSA-N Ramatroban Chemical compound N([C@@H]1CCC=2N(C3=CC=CC=C3C=2C1)CCC(=O)O)S(=O)(=O)C1=CC=C(F)C=C1 LDXDSHIEDAPSSA-OAHLLOKOSA-N 0.000 description 1
- 108020004511 Recombinant DNA Proteins 0.000 description 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 1
- 108010023197 Streptokinase Proteins 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 102000002938 Thrombospondin Human genes 0.000 description 1
- 108060008245 Thrombospondin Proteins 0.000 description 1
- 229940123987 Thromboxane A2 receptor antagonist Drugs 0.000 description 1
- 108090000373 Tissue Plasminogen Activator Proteins 0.000 description 1
- 102000003978 Tissue Plasminogen Activator Human genes 0.000 description 1
- 102000006747 Transforming Growth Factor alpha Human genes 0.000 description 1
- 101800004564 Transforming growth factor alpha Proteins 0.000 description 1
- 108090000435 Urokinase-type plasminogen activator Proteins 0.000 description 1
- 102000003990 Urokinase-type plasminogen activator Human genes 0.000 description 1
- 206010047139 Vasoconstriction Diseases 0.000 description 1
- 239000003070 absorption delaying agent Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 230000008485 antagonism Effects 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000000702 anti-platelet effect Effects 0.000 description 1
- 239000003429 antifungal agent Substances 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 229940006138 antiglaucoma drug and miotics prostaglandin analogues Drugs 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 1
- 239000008135 aqueous vehicle Substances 0.000 description 1
- 230000003143 atherosclerotic effect Effects 0.000 description 1
- 239000005667 attractant Substances 0.000 description 1
- 230000003305 autocrine Effects 0.000 description 1
- 239000000022 bacteriostatic agent Substances 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 150000008331 benzenesulfonamides Chemical class 0.000 description 1
- 238000004166 bioassay Methods 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 229960000074 biopharmaceutical Drugs 0.000 description 1
- 208000015294 blood coagulation disease Diseases 0.000 description 1
- 239000007975 buffered saline Substances 0.000 description 1
- CWOWCGMKFUVBRQ-NBGZWUPPSA-L calcium;(z)-7-[(1r,2s,3s,4s)-3-(benzenesulfonamido)-2-bicyclo[2.2.1]heptanyl]hept-5-enoate Chemical compound [Ca+2].N([C@H]1[C@@]2([H])CC[C@](C2)([C@@H]1C\C=C/CCCC([O-])=O)[H])S(=O)(=O)C1=CC=CC=C1.N([C@H]1[C@@]2([H])CC[C@](C2)([C@@H]1C\C=C/CCCC([O-])=O)[H])S(=O)(=O)C1=CC=CC=C1 CWOWCGMKFUVBRQ-NBGZWUPPSA-L 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 230000031902 chemoattractant activity Effects 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- YURNCBVQZBJDAJ-WAYWQWQTSA-N cis-2-heptenoic acid Chemical compound CCCC\C=C/C(O)=O YURNCBVQZBJDAJ-WAYWQWQTSA-N 0.000 description 1
- 230000015271 coagulation Effects 0.000 description 1
- 238000005345 coagulation Methods 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 239000000084 colloidal system Substances 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- XUDOZULIAWNMIU-UHFFFAOYSA-N delta-hexenoic acid Chemical compound OC(=O)CCCC=C XUDOZULIAWNMIU-UHFFFAOYSA-N 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000000378 dietary effect Effects 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 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 description 1
- 229960002768 dipyridamole Drugs 0.000 description 1
- 239000002612 dispersion medium Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- PWTCIBWRMQFJBC-ZEMKZVSASA-N domitroban Chemical compound N([C@H]1[C@H]2CC[C@H](C2)[C@@H]1C\C=C/CCCC(=O)O)S(=O)(=O)C1=CC=CC=C1 PWTCIBWRMQFJBC-ZEMKZVSASA-N 0.000 description 1
- 229950010759 domitroban Drugs 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 230000003073 embolic effect Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 229940012952 fibrinogen Drugs 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 229960003180 glutathione Drugs 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 230000023597 hemostasis Effects 0.000 description 1
- 229920000669 heparin Polymers 0.000 description 1
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000003701 inert diluent Substances 0.000 description 1
- 230000036512 infertility Effects 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000028709 inflammatory response Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 150000007529 inorganic bases Chemical class 0.000 description 1
- 108010044426 integrins Proteins 0.000 description 1
- 102000006495 integrins Human genes 0.000 description 1
- 238000007917 intracranial administration Methods 0.000 description 1
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 description 1
- 239000007951 isotonicity adjuster Substances 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 229910052744 lithium Inorganic materials 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000003055 low molecular weight heparin Substances 0.000 description 1
- 229940127215 low-molecular weight heparin Drugs 0.000 description 1
- 159000000003 magnesium salts Chemical class 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 230000003278 mimic effect Effects 0.000 description 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 230000036963 noncompetitive effect Effects 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 108020004707 nucleic acids Proteins 0.000 description 1
- 102000039446 nucleic acids Human genes 0.000 description 1
- 150000007523 nucleic acids Chemical class 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 229940019331 other antithrombotic agent in atc Drugs 0.000 description 1
- 108010071584 oxidized low density lipoprotein Proteins 0.000 description 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N pentanoic acid group Chemical group C(CCCC)(=O)O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
- 125000004894 pentylamino group Chemical group C(CCCC)N* 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 1
- 229960003424 phenylacetic acid Drugs 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 229960001006 picotamide Drugs 0.000 description 1
- 229940020573 plavix Drugs 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 150000003141 primary amines Chemical class 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 230000004800 psychological effect Effects 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 230000001698 pyrogenic effect Effects 0.000 description 1
- 229950004496 ramatroban Drugs 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 239000013037 reversible inhibitor Substances 0.000 description 1
- GLLPUTYLZIKEGF-HAVVHWLPSA-N ridogrel Chemical compound C=1C=CC(C(F)(F)F)=CC=1C(=N/OCCCCC(=O)O)\C1=CC=CN=C1 GLLPUTYLZIKEGF-HAVVHWLPSA-N 0.000 description 1
- 229950006674 ridogrel Drugs 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 150000003335 secondary amines Chemical class 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 229960005202 streptokinase Drugs 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 150000003512 tertiary amines Chemical class 0.000 description 1
- 150000003536 tetrazoles Chemical class 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 230000002885 thrombogenetic effect Effects 0.000 description 1
- 239000003769 thromboxane A2 receptor blocking agent Substances 0.000 description 1
- 239000003768 thromboxane synthase inhibitor Substances 0.000 description 1
- OEKWJQXRCDYSHL-FNOIDJSQSA-N ticagrelor Chemical compound C1([C@@H]2C[C@H]2NC=2N=C(N=C3N([C@H]4[C@@H]([C@H](O)[C@@H](OCCO)C4)O)N=NC3=2)SCCC)=CC=C(F)C(F)=C1 OEKWJQXRCDYSHL-FNOIDJSQSA-N 0.000 description 1
- 229960002528 ticagrelor Drugs 0.000 description 1
- 229960000187 tissue plasminogen activator Drugs 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 229960005356 urokinase Drugs 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 231100000216 vascular lesion Toxicity 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
- 229940019333 vitamin k antagonists Drugs 0.000 description 1
- 229960001134 von willebrand factor Drugs 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/0004—Oxidoreductases (1.)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/60—Salicylic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Zoology (AREA)
- Hematology (AREA)
- Wood Science & Technology (AREA)
- Genetics & Genomics (AREA)
- Diabetes (AREA)
- Biotechnology (AREA)
- Vascular Medicine (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Microbiology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91578407P | 2007-05-03 | 2007-05-03 | |
| US91578507P | 2007-05-03 | 2007-05-03 | |
| US94731607P | 2007-06-29 | 2007-06-29 | |
| US94728907P | 2007-06-29 | 2007-06-29 | |
| PCT/US2008/062567 WO2008137793A1 (en) | 2007-05-03 | 2008-05-02 | Unit dose formulations and methods of treating and preventing thrombosis with thromboxane receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010526104A true JP2010526104A (ja) | 2010-07-29 |
| JP2010526104A5 JP2010526104A5 (enExample) | 2011-06-23 |
Family
ID=39943967
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010506700A Pending JP2010526104A (ja) | 2007-05-03 | 2008-05-02 | トロンボキサン受容体アンタゴニストを用いて血栓症を治療及び予防する単位用量製剤及び方法 |
| JP2010506698A Pending JP2010527331A (ja) | 2007-05-03 | 2008-05-02 | Ｔｐモジュレーターの、アスピリン感受性集団および他の集団における心血管障害の治療のための使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010506698A Pending JP2010527331A (ja) | 2007-05-03 | 2008-05-02 | Ｔｐモジュレーターの、アスピリン感受性集団および他の集団における心血管障害の治療のための使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20090012136A1 (enExample) |
| EP (2) | EP2146573A4 (enExample) |
| JP (2) | JP2010526104A (enExample) |
| KR (2) | KR20100032854A (enExample) |
| CN (2) | CN101686668A (enExample) |
| AU (2) | AU2008247441A1 (enExample) |
| CA (2) | CA2688319A1 (enExample) |
| IL (2) | IL201885A0 (enExample) |
| MX (2) | MX2009011745A (enExample) |
| WO (2) | WO2008137791A1 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017207510A (ja) * | 2012-08-06 | 2017-11-24 | Jnc株式会社 | 合成コラーゲンを用いる二重抗血小板薬／アスピリン応答および反応性試験 |
| JP2023519674A (ja) * | 2020-03-31 | 2023-05-12 | オグレットリー，マーティン | Ｃｏｖｉｄ－１９の治療のためのトロンボキサンａ２受容体拮抗薬の方法及び医薬組成物 |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2107907B1 (en) * | 2006-12-20 | 2012-02-01 | Cardoz AB | Combination of pemirolast and ramatroban for use in the treatment of inflammatory disorders |
| WO2008087371A1 (en) * | 2007-01-16 | 2008-07-24 | Cardoz Ab | New combination for use in the treatment of inflammatory disorders |
| AU2011279144A1 (en) * | 2010-07-14 | 2013-01-24 | Cumberland Emerging Technologies, Inc | Methods of treating hepatorenal syndrome and hepatic encephalopathy with thromboxane-A2 receptor antagonists |
| AU2012336036A1 (en) | 2011-11-07 | 2014-06-19 | Diakron Pharmaceuticals Inc. | An extended release formulation of a direct thrombin inhibitor |
| US12161632B2 (en) | 2014-05-16 | 2024-12-10 | Cumberland Pharmaceuticals Inc. | Compositions and methods of treating cardiac fibrosis with ifetroban |
| JP6273072B2 (ja) | 2014-05-16 | 2018-01-31 | カンバーランド ファーマシューティカルズ，インコーポレーテッド | イフェトロバンにより心臓線維症を治療する組成物及び方法 |
| ES2858551T3 (es) * | 2015-06-16 | 2021-09-30 | Atxa Therapeutics Ltd | Antagonistas del receptor de tromboxano |
| JP7033454B2 (ja) * | 2015-06-30 | 2022-03-10 | カンバーランド ファーマシューティカルズ，インコーポレーテッド | Ａｅｒｄ／喘息におけるトロンボキサン受容体拮抗薬 |
| WO2017197107A1 (en) | 2016-05-11 | 2017-11-16 | Cumberland Pharmaceuticals, Inc. | Compositions and methods of treating muscular dystrophy with thromboxane-a2 receptor antagonists |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005533830A (ja) * | 2002-07-09 | 2005-11-10 | ビー．エム．アール．エイ． コーポレイション ベスローテン フェンノートシャップ | トロンボキサンａ２受容体アンタゴニストおよびｃｏｘ−２阻害剤の薬剤の組み合わせ |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3895115A (en) * | 1974-03-01 | 1975-07-15 | Serono Ist Farm | Method of inhibiting platelet aggregation |
| US5071866A (en) * | 1989-07-31 | 1991-12-10 | Bristol-Myers Squibb Company | Arylpyrazole derivatives as anti-platelet agents |
| US5506248A (en) * | 1993-08-02 | 1996-04-09 | Bristol-Myers Squibb Company | Pharmaceutical compositions having good dissolution properties |
| US5605917A (en) * | 1994-12-22 | 1997-02-25 | Bristol-Myers Squibb Company | Method of treating dysmenorrhea employing an interphenylene 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analog |
| 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 |
| WO2006066008A2 (en) * | 2004-12-14 | 2006-06-22 | Portola Pharmaceuticals, Inc. | Device and methods for identifying and treating aspirin non-responsive patients |
| US7381536B2 (en) * | 2005-03-01 | 2008-06-03 | Gurbel Paul A | Assessment of cardiac health and thrombotic risk in a patient |
-
2008
- 2008-05-02 CA CA002688319A patent/CA2688319A1/en not_active Abandoned
- 2008-05-02 US US12/114,646 patent/US20090012136A1/en not_active Abandoned
- 2008-05-02 AU AU2008247441A patent/AU2008247441A1/en not_active Abandoned
- 2008-05-02 WO PCT/US2008/062565 patent/WO2008137791A1/en not_active Ceased
- 2008-05-02 JP JP2010506700A patent/JP2010526104A/ja active Pending
- 2008-05-02 AU AU2008247439A patent/AU2008247439A1/en not_active Abandoned
- 2008-05-02 WO PCT/US2008/062567 patent/WO2008137793A1/en not_active Ceased
- 2008-05-02 MX MX2009011745A patent/MX2009011745A/es not_active Application Discontinuation
- 2008-05-02 MX MX2009011744A patent/MX2009011744A/es not_active Application Discontinuation
- 2008-05-02 CN CN200880019332A patent/CN101686668A/zh active Pending
- 2008-05-02 EP EP08747595A patent/EP2146573A4/en not_active Withdrawn
- 2008-05-02 JP JP2010506698A patent/JP2010527331A/ja active Pending
- 2008-05-02 KR KR1020097025329A patent/KR20100032854A/ko not_active Withdrawn
- 2008-05-02 CN CN200880014605A patent/CN101711279A/zh active Pending
- 2008-05-02 KR KR1020097025330A patent/KR20100037029A/ko not_active Withdrawn
- 2008-05-02 EP EP08747593A patent/EP2144999A4/en active Pending
- 2008-05-02 CA CA002688317A patent/CA2688317A1/en not_active Abandoned
- 2008-05-02 US US12/114,642 patent/US20090012115A1/en not_active Abandoned
-
2009
- 2009-11-02 IL IL201885A patent/IL201885A0/en unknown
- 2009-11-02 IL IL201886A patent/IL201886A0/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005533830A (ja) * | 2002-07-09 | 2005-11-10 | ビー．エム．アール．エイ． コーポレイション ベスローテン フェンノートシャップ | トロンボキサンａ２受容体アンタゴニストおよびｃｏｘ−２阻害剤の薬剤の組み合わせ |
Non-Patent Citations (4)
| Title |
|---|
| JPN6013002250; Ｐｈａｒｍａｃｏｌｏｇｙ Ｖｏｌ．５０， Ｎｏ．２, 1995, ｐ．９２-１１０ * |
| JPN6013002252; ＣＬＩＮＩＣＡＬ ＰＨＡＲＭＡＣＯＬＯＧＹ ＆ ＴＨＥＲＡＰＥＵＴＩＣＳ Ｖｏｌ．５５， Ｎｏ．２, 1994, ｐ．２０２， ＰＩＩＩ-８２ * |
| JPN6013002254; Ｃａｒｄｉｏｖａｓｃｕｌａｒ Ｄｒｕｇ Ｒｅｖｉｅｗｓ Ｖｏｌ．１９， Ｎｏ．２, 2001, ｐ．９７-１１５ * |
| JPN6013002255; Ｐｒｏｓｔａｇｌａｎｄｉｎｓ Ｖｏｌ．４４， Ｎｏ．５, 1992, ｐ．３８９-３９７ * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017207510A (ja) * | 2012-08-06 | 2017-11-24 | Jnc株式会社 | 合成コラーゲンを用いる二重抗血小板薬／アスピリン応答および反応性試験 |
| JP2023519674A (ja) * | 2020-03-31 | 2023-05-12 | オグレットリー，マーティン | Ｃｏｖｉｄ－１９の治療のためのトロンボキサンａ２受容体拮抗薬の方法及び医薬組成物 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN101686668A (zh) | 2010-03-31 |
| EP2144999A1 (en) | 2010-01-20 |
| KR20100037029A (ko) | 2010-04-08 |
| US20090012115A1 (en) | 2009-01-08 |
| AU2008247441A1 (en) | 2008-11-13 |
| EP2146573A4 (en) | 2012-11-21 |
| IL201886A0 (en) | 2010-06-16 |
| KR20100032854A (ko) | 2010-03-26 |
| WO2008137793A1 (en) | 2008-11-13 |
| MX2009011744A (es) | 2010-02-12 |
| CA2688319A1 (en) | 2008-11-13 |
| EP2144999A4 (en) | 2010-06-16 |
| WO2008137791A1 (en) | 2008-11-13 |
| AU2008247439A1 (en) | 2008-11-13 |
| JP2010527331A (ja) | 2010-08-12 |
| MX2009011745A (es) | 2010-02-12 |
| CA2688317A1 (en) | 2008-11-13 |
| IL201885A0 (en) | 2011-08-01 |
| US20090012136A1 (en) | 2009-01-08 |
| EP2146573A1 (en) | 2010-01-27 |
| CN101711279A (zh) | 2010-05-19 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2010526104A (ja) | トロンボキサン受容体アンタゴニストを用いて血栓症を治療及び予防する単位用量製剤及び方法 | |
| JP5390184B2 (ja) | 貧血の改良された治療方法 | |
| Liverani et al. | The role of P2Y12 receptor and activated platelets during inflammation | |
| US20030109543A1 (en) | Novel combination of an ADP-receptor blocking antiplatelet drug and a thromboxane A2 receptor antagonist and a method for inhibiting thrombus formation employing such combination | |
| CA2413705A1 (en) | Use of meloxicam in combination with an antiplatelet agent for treatment of acute coronary syndrome and related conditions | |
| JP2011525194A (ja) | 線維性疾患または病態を治療するための組成物 | |
| JP2006524203A (ja) | トロンビンの過剰形成及び／又はトロンビンレセプターの発現上昇により生じる血栓塞栓性疾病及び疾患の治療及び予防のためのジピリダモール又はモピダモールの使用 | |
| US20190151291A1 (en) | Ifetroban treatment of portal hypertension | |
| KR20190021228A (ko) | 트롬복산-a2 수용체 길항제를 이용한 근위축증 치료 조성물 및 방법 | |
| US9132191B2 (en) | Compositions and methods of preventing or ameliorating abnormal thrombus formation and cardiovascular disease | |
| Bendel et al. | Dabigatran: an oral direct thrombin inhibitor for use in atrial fibrillation | |
| US20030220383A1 (en) | Use of inhibitors of the sodium-dependent chloride/bicarbonate exchanger for the treatment of thrombotic and inflammatory disorders | |
| US5523321A (en) | Prostacyclins, their analogs or prostaglandins and thromboxane antagonists for treatment of thrombotic and thromboembolic syndromes | |
| KR20050025604A (ko) | 동맥 경화증 치료를 위한 의약 조성물 | |
| Ezratty et al. | New approaches to antiplatelet therapy | |
| Kuliczkowski et al. | Aspirin failure course during exercise and its connection with soluble CD40L | |
| IES20030306A2 (en) | Inhibition of platelet aggregation | |
| IE861923L (en) | Prostacyclin derivatives and thromboxane antagonist¹compositions | |
| US20110034504A1 (en) | Agent for preventing and/or treating vascular diseases | |
| US6201015B1 (en) | Therapeutic method for thrombocytopathy treatment | |
| Jafri et al. | Reversal of Oral Anticoagulants in the Elderly | |
| KR20040053884A (ko) | 급성 관상동맥증후군 및 관련 상태의 치료를 위한항혈소판제와 병용하는 멜록시캄의 용도 | |
| CA3176619A1 (en) | Methods and pharmaceutical compositions of thromboxane a2 receptor antagonist for the treatment of covid-19 | |
| JP2005525338A (ja) | 血栓性および炎症性障害の治療のためのナトリウム依存性クロライド／バイカーボネート交換体の阻害剤の使用 | |
| Moss et al. | Inhibitory Kappa B Kinase Beta (IKKβ) Inhibition Attenuates Myocardial Injury and |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20110428 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20110428 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20130212 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20130730 |