EA015122B1 - Фармацевтическая композиция и ее применение для лечения тромбоза - Google Patents
Фармацевтическая композиция и ее применение для лечения тромбоза Download PDFInfo
- Publication number
- EA015122B1 EA015122B1 EA200701841A EA200701841A EA015122B1 EA 015122 B1 EA015122 B1 EA 015122B1 EA 200701841 A EA200701841 A EA 200701841A EA 200701841 A EA200701841 A EA 200701841A EA 015122 B1 EA015122 B1 EA 015122B1
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- EA
- Eurasian Patent Office
- Prior art keywords
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- pharmaceutical composition
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- compound
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 37
- 208000007536 Thrombosis Diseases 0.000 title claims abstract description 8
- 150000001875 compounds Chemical class 0.000 claims abstract description 50
- 239000000106 platelet aggregation inhibitor Substances 0.000 claims abstract description 14
- 229940123900 Direct thrombin inhibitor Drugs 0.000 claims abstract description 10
- 239000003868 thrombin inhibitor Substances 0.000 claims abstract description 10
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 7
- 239000003937 drug carrier Substances 0.000 claims abstract description 5
- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 claims description 19
- 238000002360 preparation method Methods 0.000 claims description 19
- 150000003839 salts Chemical class 0.000 claims description 19
- 239000005552 B01AC04 - Clopidogrel Substances 0.000 claims description 18
- GKTWGGQPFAXNFI-HNNXBMFYSA-N clopidogrel Chemical compound C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl GKTWGGQPFAXNFI-HNNXBMFYSA-N 0.000 claims description 18
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 16
- 229960003009 clopidogrel Drugs 0.000 claims description 16
- 229960001138 acetylsalicylic acid Drugs 0.000 claims description 15
- 239000002253 acid Substances 0.000 claims description 14
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 13
- 229940127218 antiplatelet drug Drugs 0.000 claims description 13
- 238000013146 percutaneous coronary intervention Methods 0.000 claims description 10
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 8
- 239000005528 B01AC05 - Ticlopidine Substances 0.000 claims description 8
- 229960005001 ticlopidine Drugs 0.000 claims description 8
- PHWBOXQYWZNQIN-UHFFFAOYSA-N ticlopidine Chemical compound ClC1=CC=CC=C1CN1CC(C=CS2)=C2CC1 PHWBOXQYWZNQIN-UHFFFAOYSA-N 0.000 claims description 8
- 206010051055 Deep vein thrombosis Diseases 0.000 claims description 6
- 206010047249 Venous thrombosis Diseases 0.000 claims description 6
- 150000004677 hydrates Chemical class 0.000 claims description 6
- 208000010125 myocardial infarction Diseases 0.000 claims description 6
- 101000783577 Dendroaspis angusticeps Thrombostatin Proteins 0.000 claims description 5
- 101000783578 Dendroaspis jamesoni kaimosae Dendroaspin Proteins 0.000 claims description 5
- 230000001732 thrombotic effect Effects 0.000 claims description 5
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims description 4
- 230000002265 prevention Effects 0.000 claims description 4
- 239000012453 solvate Substances 0.000 claims description 4
- 230000002537 thrombolytic effect Effects 0.000 claims description 4
- 206010003658 Atrial Fibrillation Diseases 0.000 claims description 2
- 206010019280 Heart failures Diseases 0.000 claims description 2
- 206010049694 Left Ventricular Dysfunction Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000010378 Pulmonary Embolism Diseases 0.000 claims description 2
- 101000907549 Takifugu obscurus Flavor peptide Proteins 0.000 claims description 2
- 206010000891 acute myocardial infarction Diseases 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims description 2
- 239000000945 filler Substances 0.000 claims description 2
- 230000000399 orthopedic effect Effects 0.000 claims description 2
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims 2
- 238000007920 subcutaneous administration Methods 0.000 claims 2
- 125000005273 2-acetoxybenzoic acid group Chemical group 0.000 claims 1
- SEGHHPAKTYKSLB-UHFFFAOYSA-N ethyl 3-[[2-[[4-[(hexoxycarbonylhydrazinylidene)methyl]anilino]methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoate Chemical compound C1=CC(C=NNC(=O)OCCCCCC)=CC=C1NCC1=NC2=CC(C(=O)N(CCC(=O)OCC)C=3N=CC=CC=3)=CC=C2N1C SEGHHPAKTYKSLB-UHFFFAOYSA-N 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-M methanesulfonate group Chemical group CS(=O)(=O)[O-] AFVFQIVMOAPDHO-UHFFFAOYSA-M 0.000 claims 1
- 230000008520 organization Effects 0.000 claims 1
- 230000009861 stroke prevention Effects 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 description 24
- 239000002775 capsule Substances 0.000 description 12
- 239000003826 tablet Substances 0.000 description 10
- 108090000190 Thrombin Proteins 0.000 description 9
- 239000003112 inhibitor Substances 0.000 description 9
- 229960004072 thrombin Drugs 0.000 description 9
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 8
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
- YLEIFZAVNWDOBM-ZTNXSLBXSA-N ac1l9hc7 Chemical compound C([C@H]12)C[C@@H](C([C@@H](O)CC3)(C)C)[C@@]43C[C@@]14CC[C@@]1(C)[C@@]2(C)C[C@@H]2O[C@]3(O)[C@H](O)C(C)(C)O[C@@H]3[C@@H](C)[C@H]12 YLEIFZAVNWDOBM-ZTNXSLBXSA-N 0.000 description 6
- 238000010411 cooking Methods 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 239000003814 drug Substances 0.000 description 5
- -1 hydrosulfate Chemical compound 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 229920002261 Corn starch Polymers 0.000 description 4
- 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 4
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 4
- 229930195725 Mannitol Natural products 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- 239000008120 corn starch Substances 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 239000012458 free base Substances 0.000 description 4
- 239000008101 lactose Substances 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 4
- 239000000594 mannitol Substances 0.000 description 4
- 235000010355 mannitol Nutrition 0.000 description 4
- 229940098779 methanesulfonic acid Drugs 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 239000000829 suppository Substances 0.000 description 4
- 239000008215 water for injection Substances 0.000 description 4
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 3
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 3
- 150000007513 acids Chemical class 0.000 description 3
- 239000004480 active ingredient Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 229940125904 compound 1 Drugs 0.000 description 3
- 229940125782 compound 2 Drugs 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 244000215068 Acacia senegal Species 0.000 description 2
- 229920000084 Gum arabic Polymers 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 2
- 208000006011 Stroke Diseases 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 208000001435 Thromboembolism Diseases 0.000 description 2
- 239000000205 acacia gum Substances 0.000 description 2
- 235000010489 acacia gum Nutrition 0.000 description 2
- 239000003708 ampul Substances 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 239000002585 base Substances 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 238000007906 compression Methods 0.000 description 2
- 230000006835 compression Effects 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 239000011976 maleic acid Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 231100000252 nontoxic Toxicity 0.000 description 2
- 230000003000 nontoxic effect Effects 0.000 description 2
- 238000004806 packaging method and process Methods 0.000 description 2
- 239000008188 pellet Substances 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 239000006188 syrup Substances 0.000 description 2
- 235000020357 syrup Nutrition 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- DMJDEZUEYXVYNO-DHZHZOJOSA-N (e)-3-(4-phenylphenyl)prop-2-enoic acid Chemical compound C1=CC(/C=C/C(=O)O)=CC=C1C1=CC=CC=C1 DMJDEZUEYXVYNO-DHZHZOJOSA-N 0.000 description 1
- SJJCQDRGABAVBB-UHFFFAOYSA-N 1-hydroxy-2-naphthoic acid Chemical compound C1=CC=CC2=C(O)C(C(=O)O)=CC=C21 SJJCQDRGABAVBB-UHFFFAOYSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 239000001828 Gelatine Substances 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 210000004351 coronary vessel Anatomy 0.000 description 1
- 229960003850 dabigatran Drugs 0.000 description 1
- 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 description 1
- HUPFGZXOMWLGNK-UHFFFAOYSA-N diflunisal Chemical compound C1=C(O)C(C(=O)O)=CC(C=2C(=CC(F)=CC=2)F)=C1 HUPFGZXOMWLGNK-UHFFFAOYSA-N 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000002955 isolation Methods 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 229960002137 melagatran Drugs 0.000 description 1
- DKWNMCUOEDMMIN-PKOBYXMFSA-N melagatran Chemical compound C1=CC(C(=N)N)=CC=C1CNC(=O)[C@H]1N(C(=O)[C@H](NCC(O)=O)C2CCCCC2)CC1 DKWNMCUOEDMMIN-PKOBYXMFSA-N 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 229940020573 plavix Drugs 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000001587 sorbitan monostearate Substances 0.000 description 1
- 235000011076 sorbitan monostearate Nutrition 0.000 description 1
- 229940035048 sorbitan monostearate Drugs 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229960001522 ximelagatran Drugs 0.000 description 1
- 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 description 1
- 229950000339 xinafoate Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/55—Protease inhibitors
- A61K38/57—Protease inhibitors from animals; from humans
- A61K38/58—Protease inhibitors from animals; from humans from leeches, e.g. hirudin, eglin
-
- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05006711 | 2005-03-29 | ||
| PCT/EP2006/061046 WO2006103206A2 (en) | 2005-03-29 | 2006-03-27 | Combinations comprising at least one direct thrombin inhibitor for the treatment of thrombosis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200701841A1 EA200701841A1 (ru) | 2008-02-28 |
| EA015122B1 true EA015122B1 (ru) | 2011-06-30 |
Family
ID=36423564
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200701841A EA015122B1 (ru) | 2005-03-29 | 2006-03-27 | Фармацевтическая композиция и ее применение для лечения тромбоза |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US20060222640A1 (OSRAM) |
| EP (1) | EP1885354A2 (OSRAM) |
| JP (1) | JP2008534552A (OSRAM) |
| KR (1) | KR20070116936A (OSRAM) |
| CN (1) | CN101151030A (OSRAM) |
| AR (1) | AR056291A1 (OSRAM) |
| AU (1) | AU2006228600A1 (OSRAM) |
| BR (1) | BRPI0608656A2 (OSRAM) |
| CA (1) | CA2602563A1 (OSRAM) |
| CL (1) | CL2010000395A1 (OSRAM) |
| EA (1) | EA015122B1 (OSRAM) |
| IL (1) | IL186267A0 (OSRAM) |
| MX (1) | MX2007010664A (OSRAM) |
| NO (1) | NO20074149L (OSRAM) |
| NZ (1) | NZ562775A (OSRAM) |
| TW (1) | TW200722089A (OSRAM) |
| UA (1) | UA92603C2 (OSRAM) |
| WO (1) | WO2006103206A2 (OSRAM) |
| ZA (1) | ZA200706698B (OSRAM) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8906894B1 (en) | 2000-07-27 | 2014-12-09 | Thomas N. Thomas | Methods for preventing and treating thrombotic disorders |
| US20030181488A1 (en) | 2002-03-07 | 2003-09-25 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Administration form for the oral application of 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester and the salts thereof |
| DE10339862A1 (de) * | 2003-08-29 | 2005-03-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 3-[(2-{[4-(Hexyloxycarbonylamino-imino-methyl)- phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionsäure-ethylester-Methansulfonat und dessen Verwendung als Arzneimittel |
| IL159273A0 (en) * | 2003-12-09 | 2004-06-01 | Transpharma Medical Ltd | Transdermal delivery system for sustained release of polypeptides |
| CA2610757A1 (en) * | 2005-06-10 | 2006-12-14 | Transpharma Medical, Ltd. | Patch for transdermal drug delivery |
| EP2043632A2 (en) * | 2006-07-17 | 2009-04-08 | Boehringer Ingelheim International GmbH | New indications for direct thrombin inhibitors |
| US20100087488A1 (en) * | 2006-10-10 | 2010-04-08 | Boehringer Ingelheim International Gmgh | Physiologically Acceptable Salts of 3-[(2--1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester |
| DE102006051625A1 (de) | 2006-11-02 | 2008-05-08 | Bayer Materialscience Ag | Kombinationstherapie substituierter Oxazolidinone |
| WO2009057112A2 (en) * | 2007-10-29 | 2009-05-07 | Transpharma Medical, Ltd. | Vertical patch drying |
| WO2010013231A2 (en) * | 2008-07-29 | 2010-02-04 | Yeda Research And Development Co. Ltd. | Modulation of coagulation factors and effectors of same for control of transplant organ size |
| EP2323605A4 (en) * | 2008-09-10 | 2014-02-05 | Syneron Medical Ltd | TRANSDERMAL RELEASE OF OLIGOSACCHARIDES |
| TW201031651A (en) * | 2008-11-11 | 2010-09-01 | Boehringer Ingelheim Int | Method for treating or preventing thrombosis using dabigatran etexilate or a salt thereof with improved efficacy over conventional warfarin therapy |
| AR074313A1 (es) | 2008-11-11 | 2011-01-05 | Boehringer Ingelheim Int | Metodo para tratar o prevenir la trombosis utilizando etexilato de dabigatran o una sal del mismo. uso. kit |
| CA2738885A1 (en) * | 2008-11-11 | 2010-05-20 | Boehringer Ingelheim International Gmbh | Method for treating or preventing thrombosis using dabigatran etexilate or a salt thereof with improved efficacy over conventional warfarin therapy |
| EP2384196B1 (en) * | 2008-12-30 | 2017-09-13 | Johansson, Pär | Methods of identifying critically ill patients at increased risk of development of organ failure and compounds for the treatment hereof |
| PL2667878T3 (pl) * | 2011-01-25 | 2016-10-31 | Kompozycje i sposoby transplantacji komórek | |
| CN102250099B (zh) * | 2011-05-16 | 2013-10-16 | 中国药科大学 | 一类非肽类抗凝血酶抑制剂、其制法以及医药用途 |
| EP2806879B1 (en) | 2012-01-25 | 2019-03-06 | Université Catholique de Louvain | Compositions and methods for cell transplantation |
| WO2014001220A1 (en) | 2012-06-25 | 2014-01-03 | Boehringer Ingelheim International Gmbh | Method for prevention of stroke |
| EP2722034B1 (en) * | 2012-10-19 | 2020-09-16 | Sanovel Ilac Sanayi ve Ticaret A.S. | Oral pharmaceutical formulations comprising dabigatran |
| EP2722033A1 (en) * | 2012-10-19 | 2014-04-23 | Sanovel Ilac Sanayi ve Ticaret A.S. | Pharmaceutical Compositions of Dabigatran Free Base |
| JP6474394B2 (ja) | 2013-07-05 | 2019-02-27 | ユニベルシテ カトリック ドゥ ルーベン | ヒト成体肝臓幹細胞由来の馴化培地および肝臓障害の治療におけるその使用 |
| DE102014108210A1 (de) | 2014-06-11 | 2015-12-17 | Dietrich Gulba | Rodentizid |
| CN105250286A (zh) * | 2015-11-13 | 2016-01-20 | 谭惠娟 | 一种抗血栓组合物 |
| CN108236612A (zh) * | 2016-12-27 | 2018-07-03 | 李志忠 | 用于冠脉介入手术中抗凝的组合产品及其用途 |
| WO2020180489A1 (en) * | 2019-03-06 | 2020-09-10 | University Of Rochester | Anticoagulant compositions and uses thereof |
| US11654036B2 (en) | 2020-05-26 | 2023-05-23 | Elixir Medical Corporation | Anticoagulant compounds and methods and devices for their use |
| CN115192691B (zh) * | 2022-08-31 | 2025-03-04 | 晓恩医药包装材料(安庆)有限公司 | 一种阿加曲班注射液及预灌封注射器 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5510330A (en) * | 1994-03-25 | 1996-04-23 | Boehringer Mannheim Gmbh | Combinations of thrombolytically active proteins and non-heparin anticoagulants, and uses thereof. |
| EP0732102A2 (en) * | 1995-03-15 | 1996-09-18 | BEHRINGWERKE Aktiengesellschaft | Composite for the treatment of acute myocardial infarction containing hirudin and acetylsalicyclic acid |
| WO1998037075A1 (de) * | 1997-02-18 | 1998-08-27 | Boehringer Ingelheim Pharma Kg | Disubstituierte bicyclische heterocyclen, ihre herstellung und ihre verwendung als arzneimittel |
| US20030153506A1 (en) * | 2000-06-10 | 2003-08-14 | Ruth Bylund | Combination product comprising melagatran and factor VIIa inhibitor |
| EP1437137A1 (en) * | 2001-09-14 | 2004-07-14 | Mitsubishi Pharma Corporation | Drugs comprising combination of antithrombotic agent with pyrazolone derivative |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6087380A (en) * | 1949-11-24 | 2000-07-11 | Boehringer Ingelheim Pharma Kg | Disubstituted bicyclic heterocycles, the preparations and the use thereof as pharmaceutical compositions |
| FR2744918B1 (fr) * | 1996-02-19 | 1998-05-07 | Sanofi Sa | Nouvelles associations de principes actifs contenant un derive de thieno(3,2-c)pyridine et un antithrombotique |
| US6414008B1 (en) * | 1997-04-29 | 2002-07-02 | Boehringer Ingelheim Pharma Kg | Disubstituted bicyclic heterocycles, the preparation thereof, and their use as pharmaceutical compositions |
| DE19834751A1 (de) * | 1998-08-01 | 2000-02-03 | Boehringer Ingelheim Pharma | Disubstituierte bicyclische Heterocyclen, ihre Herstellung und ihre Verwendung als Arzneimittel |
| GB9930540D0 (en) * | 1999-12-23 | 2000-02-16 | Rhone Poulenc Rorer Pharma | Chemical compounds |
| DK1485094T4 (da) * | 2002-03-07 | 2020-06-22 | Boehringer Ingelheim Int | Doseringsform til oral indgivelse af 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1h-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionsyre-ethylester eller dets salte |
| DE10235639A1 (de) * | 2002-08-02 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Prodrugs von 1-Methyl-2-(4-amidinophenylaminomethyl)-benzimidazol-5-yl-carbonsäure-(N-2-pyridyl-N-2-hydroxycarbonylethyl)-amid, ihre Herstellung und ihre Verwendung als Arzneimittel |
| BRPI0409796A (pt) * | 2003-04-24 | 2006-05-30 | Boehringer Ingelheim Int | uso de dipiridamol ou mopidamol para tratamento e prevenção de doenças tromboembolìticas e distúrbios provocados pela formação excessiva de trombina e/ou pela expressão elevada de receptores de trombina |
-
2006
- 2006-03-26 US US11/277,503 patent/US20060222640A1/en not_active Abandoned
- 2006-03-27 MX MX2007010664A patent/MX2007010664A/es not_active Application Discontinuation
- 2006-03-27 CA CA002602563A patent/CA2602563A1/en not_active Abandoned
- 2006-03-27 UA UAA200711762A patent/UA92603C2/ru unknown
- 2006-03-27 KR KR1020077024953A patent/KR20070116936A/ko not_active Ceased
- 2006-03-27 CN CNA2006800108359A patent/CN101151030A/zh active Pending
- 2006-03-27 JP JP2008503489A patent/JP2008534552A/ja active Pending
- 2006-03-27 EP EP06725316A patent/EP1885354A2/en not_active Withdrawn
- 2006-03-27 BR BRPI0608656-0A patent/BRPI0608656A2/pt not_active IP Right Cessation
- 2006-03-27 NZ NZ562775A patent/NZ562775A/en unknown
- 2006-03-27 WO PCT/EP2006/061046 patent/WO2006103206A2/en not_active Ceased
- 2006-03-27 EA EA200701841A patent/EA015122B1/ru not_active IP Right Cessation
- 2006-03-27 AU AU2006228600A patent/AU2006228600A1/en not_active Abandoned
- 2006-03-28 TW TW095110732A patent/TW200722089A/zh unknown
- 2006-03-29 AR ARP060101205A patent/AR056291A1/es unknown
-
2007
- 2007-08-10 NO NO20074149A patent/NO20074149L/no not_active Application Discontinuation
- 2007-08-13 ZA ZA200706698A patent/ZA200706698B/xx unknown
- 2007-09-25 IL IL186267A patent/IL186267A0/en unknown
-
2010
- 2010-03-19 US US12/727,933 patent/US20100184729A1/en not_active Abandoned
- 2010-04-21 CL CL2010000395A patent/CL2010000395A1/es unknown
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5510330A (en) * | 1994-03-25 | 1996-04-23 | Boehringer Mannheim Gmbh | Combinations of thrombolytically active proteins and non-heparin anticoagulants, and uses thereof. |
| EP0732102A2 (en) * | 1995-03-15 | 1996-09-18 | BEHRINGWERKE Aktiengesellschaft | Composite for the treatment of acute myocardial infarction containing hirudin and acetylsalicyclic acid |
| WO1998037075A1 (de) * | 1997-02-18 | 1998-08-27 | Boehringer Ingelheim Pharma Kg | Disubstituierte bicyclische heterocyclen, ihre herstellung und ihre verwendung als arzneimittel |
| US20030153506A1 (en) * | 2000-06-10 | 2003-08-14 | Ruth Bylund | Combination product comprising melagatran and factor VIIa inhibitor |
| EP1437137A1 (en) * | 2001-09-14 | 2004-07-14 | Mitsubishi Pharma Corporation | Drugs comprising combination of antithrombotic agent with pyrazolone derivative |
Non-Patent Citations (4)
| Title |
|---|
| BYLOCK ANDERS ET AL.: "Comparison of the antithrombotic effects of ximelagatran plus acetylsalicylic acid (ASA) and clopidogrel plus ASA in a human, ex vivo arterial thrombosis model", CIRCULATION, vol. 108, no. 17 Supplement, 28 October 2003 (2003-10-28), pages IV-160, XP009067185, & AMERICAN HEART ASSOCIATION SCIENTIFIC SESSIONS 2003; ORLANDO, FL, USA; NOVEMBER 09-12, 2003, ISSN: 0009-7322, the whole document * |
| FOR THE ESTEEM INVESTIGATORS WALLENTIN L ET AL.: "Oral ximelagatran for secondary prophylaxis after myocardial infarction: the ESTEEM randomised controlled trial", LANCET THE, LANCET LIMITED. LONDON, GB, vol. 362, no. 9386, 6 September 2003 (2003-09-06), pages 789-797, XP004779172, ISSN: 0140-6736, page 794, column 1, last paragraph, page 795, column 2, last paragraph * |
| HONG TINGTING ET AL.: "Effect of melagatran combined with aspirin or clopidogrel on primary carotid artery thrombosis", FASEB JOURNAL, vol. 19, no. 5, suppl. S, part 2, March 2005 (2005-03), page A1083, XP009067187 & EXPERIMENTAL BIOLOGY 2005 MEETING/35TH INTERNATIONAL CONGRESS OF PHYSIOLOGICAL SCIENCES; SAN DIEGO, CA, USA; MARCH 31-APRIL 06, 2005, ISSN: 0892-6638, the whole document * |
| MORISHITA KAORU ET AL.: "Synergistic antithrombotic effects of argatroban and ticlopidine in the rat venous thrombosis model", THROMBOSIS RESEARCH, vol. 92, no. 6, 15 December 1998 (1998-12-15), pages 261-266, XP002383204, ISSN: 0049-3848, page 264; tab. 1, page 265, last paragraph * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2006103206A3 (en) | 2007-01-11 |
| CN101151030A (zh) | 2008-03-26 |
| US20100184729A1 (en) | 2010-07-22 |
| NO20074149L (no) | 2007-12-11 |
| AR056291A1 (es) | 2007-10-03 |
| US20060222640A1 (en) | 2006-10-05 |
| BRPI0608656A2 (pt) | 2010-01-19 |
| CA2602563A1 (en) | 2006-10-05 |
| IL186267A0 (en) | 2008-01-20 |
| TW200722089A (en) | 2007-06-16 |
| JP2008534552A (ja) | 2008-08-28 |
| NZ562775A (en) | 2011-03-31 |
| MX2007010664A (es) | 2007-12-12 |
| AU2006228600A1 (en) | 2006-10-05 |
| WO2006103206A2 (en) | 2006-10-05 |
| EA200701841A1 (ru) | 2008-02-28 |
| EP1885354A2 (en) | 2008-02-13 |
| KR20070116936A (ko) | 2007-12-11 |
| UA92603C2 (ru) | 2010-11-25 |
| CL2010000395A1 (es) | 2010-08-20 |
| ZA200706698B (en) | 2008-12-31 |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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