RU2012104816A - Стандартные лекарственные препараты и способы лечения тромбоза пероральным введением ингибитора фактора ха - Google Patents
Стандартные лекарственные препараты и способы лечения тромбоза пероральным введением ингибитора фактора ха Download PDFInfo
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- RU2012104816A RU2012104816A RU2012104816/15A RU2012104816A RU2012104816A RU 2012104816 A RU2012104816 A RU 2012104816A RU 2012104816/15 A RU2012104816/15 A RU 2012104816/15A RU 2012104816 A RU2012104816 A RU 2012104816A RU 2012104816 A RU2012104816 A RU 2012104816A
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- thrombin
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- test sample
- whole blood
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- 238000000034 method Methods 0.000 title claims abstract 17
- 208000007536 Thrombosis Diseases 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 108090000190 Thrombin Proteins 0.000 claims abstract 18
- 229960004072 thrombin Drugs 0.000 claims abstract 18
- 239000000523 sample Substances 0.000 claims abstract 16
- 239000013068 control sample Substances 0.000 claims abstract 12
- 239000008280 blood Substances 0.000 claims abstract 10
- 210000004369 blood Anatomy 0.000 claims abstract 10
- 239000000758 substrate Substances 0.000 claims abstract 10
- 108010000499 Thromboplastin Proteins 0.000 claims abstract 8
- 102000002262 Thromboplastin Human genes 0.000 claims abstract 8
- 230000015271 coagulation Effects 0.000 claims abstract 8
- 238000005345 coagulation Methods 0.000 claims abstract 8
- 238000001514 detection method Methods 0.000 claims abstract 8
- 230000000694 effects Effects 0.000 claims abstract 8
- 150000001875 compounds Chemical class 0.000 claims abstract 6
- 230000002785 anti-thrombosis Effects 0.000 claims abstract 4
- 238000003776 cleavage reaction Methods 0.000 claims abstract 4
- 238000000338 in vitro Methods 0.000 claims abstract 4
- 238000001727 in vivo Methods 0.000 claims abstract 4
- 230000007017 scission Effects 0.000 claims abstract 4
- 238000012544 monitoring process Methods 0.000 claims abstract 3
- SXTGIAYWYXVNLT-NRFANRHFSA-N benzyl n-[2-[[2-[[(2s)-5-(diaminomethylideneamino)-1-[(4-methyl-2-oxochromen-7-yl)amino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]carbamate Chemical group N([C@@H](CCCNC(N)=N)C(=O)NC1=CC=2OC(=O)C=C(C=2C=C1)C)C(=O)CNC(=O)CNC(=O)OCC1=CC=CC=C1 SXTGIAYWYXVNLT-NRFANRHFSA-N 0.000 claims abstract 2
- 108010079115 benzyloxycarbonyl-glycyl-glycyl-arginine-4-methylcoumaryl-7-amide Proteins 0.000 claims abstract 2
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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- 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
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- 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
-
- 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
-
- 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
- A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
-
- 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
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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- 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
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- Diabetes (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Abstract
1. Способ определения in vitro антитромботической активности соединения in vivo, включающийа) введение испытуемого соединения в образец in vitro цельной крови или плазмы, содержащей тканевый фактор (TF) и обнаружимо меченный тромбиновый субстрат для формирования испытуемого образца;(b) определение степени активности тромбина в испытуемом образце путем отслеживания расщепления обнаружения меченного для тромбинового субстрата в испытуемом образце как функцию времени;с) определение степени активности тромбина в контрольном образце путем мониторинга расщепления меченного для обнаружения тромбинового субстрата в контрольном образце как функцию времени, где контрольный образец содержит цельную кровь или плазму, содержащую тканевый фактор (TF) и меченный для обнаружения тромбиновый субстрат;d) сравнение степени активности тромбина в испытуемом образце и в контрольном образце, где степень активности тромбина в испытуемом образце является показателем того, что испытуемое соединение имеет in vivo антитромботическую активность.2. Способ по п.1, где испытуемый образец и контрольный образец содержат цельную кровь.3. Способ по п.2, где цельную кровь предохраняют от коагуляции.4. Способ по п.2, где цельную кровь не предохраняют от коагуляции.5. Способ по п.1, где испытуемый образец и контрольный образец содержат плазму.6. Способ по п.5, где плазму предохраняют от коагуляции.7. Способ по п.5, где плазму не предохраняют от коагуляции.8. Способ по п.1, где меченным для обнаружения тромбиновым субстратом является Z-Gly-Gly-Arg-AMC.
Claims (8)
1. Способ определения in vitro антитромботической активности соединения in vivo, включающий
а) введение испытуемого соединения в образец in vitro цельной крови или плазмы, содержащей тканевый фактор (TF) и обнаружимо меченный тромбиновый субстрат для формирования испытуемого образца;
(b) определение степени активности тромбина в испытуемом образце путем отслеживания расщепления обнаружения меченного для тромбинового субстрата в испытуемом образце как функцию времени;
с) определение степени активности тромбина в контрольном образце путем мониторинга расщепления меченного для обнаружения тромбинового субстрата в контрольном образце как функцию времени, где контрольный образец содержит цельную кровь или плазму, содержащую тканевый фактор (TF) и меченный для обнаружения тромбиновый субстрат;
d) сравнение степени активности тромбина в испытуемом образце и в контрольном образце, где степень активности тромбина в испытуемом образце является показателем того, что испытуемое соединение имеет in vivo антитромботическую активность.
2. Способ по п.1, где испытуемый образец и контрольный образец содержат цельную кровь.
3. Способ по п.2, где цельную кровь предохраняют от коагуляции.
4. Способ по п.2, где цельную кровь не предохраняют от коагуляции.
5. Способ по п.1, где испытуемый образец и контрольный образец содержат плазму.
6. Способ по п.5, где плазму предохраняют от коагуляции.
7. Способ по п.5, где плазму не предохраняют от коагуляции.
8. Способ по п.1, где меченным для обнаружения тромбиновым субстратом является Z-Gly-Gly-Arg-AMC.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87379206P | 2006-12-08 | 2006-12-08 | |
| US60/873,792 | 2006-12-08 | ||
| US94762907P | 2007-07-02 | 2007-07-02 | |
| US60/947,629 | 2007-07-02 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2009126147/15A Division RU2452484C2 (ru) | 2006-12-08 | 2007-11-15 | Стандартные лекарственные препараты и способы лечения тромбоза пероральным введением ингибитора фактора ха |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2012104816A true RU2012104816A (ru) | 2013-08-20 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2009126147/15A RU2452484C2 (ru) | 2006-12-08 | 2007-11-15 | Стандартные лекарственные препараты и способы лечения тромбоза пероральным введением ингибитора фактора ха |
| RU2012104816/15A RU2012104816A (ru) | 2006-12-08 | 2012-02-10 | Стандартные лекарственные препараты и способы лечения тромбоза пероральным введением ингибитора фактора ха |
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| RU2009126147/15A RU2452484C2 (ru) | 2006-12-08 | 2007-11-15 | Стандартные лекарственные препараты и способы лечения тромбоза пероральным введением ингибитора фактора ха |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8404724B2 (ru) |
| EP (1) | EP2101760B1 (ru) |
| KR (1) | KR101472765B1 (ru) |
| CN (1) | CN105193799A (ru) |
| AU (1) | AU2007333377B2 (ru) |
| CA (2) | CA2913963A1 (ru) |
| CO (1) | CO6220933A2 (ru) |
| CR (1) | CR10914A (ru) |
| EC (1) | ECSP099501A (ru) |
| ES (1) | ES2409090T3 (ru) |
| IL (1) | IL199219A (ru) |
| MA (1) | MA31086B1 (ru) |
| NI (1) | NI200900145A (ru) |
| NZ (1) | NZ578180A (ru) |
| PT (1) | PT2101760E (ru) |
| RU (2) | RU2452484C2 (ru) |
| SG (1) | SG10201504425SA (ru) |
| WO (1) | WO2008073670A2 (ru) |
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| JPH0813834B2 (ja) * | 1990-08-01 | 1996-02-14 | 日東紡績株式会社 | トリペプチド誘導体及びそれを有効成分とする蛋白分解酵素阻害剤 |
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| JP2002533454A (ja) * | 1998-12-23 | 2002-10-08 | イーライ・リリー・アンド・カンパニー | 芳香族アミド類 |
| US6844367B1 (en) * | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| DK1259485T3 (da) * | 2000-02-29 | 2006-04-10 | Millennium Pharm Inc | Benzamider og beslægtede inhibitorer for faktor Xa |
| GB0021497D0 (en) * | 2000-09-01 | 2000-10-18 | Novartis Res Foundation | Compounds and their use |
| US20040077690A1 (en) * | 2000-09-29 | 2004-04-22 | Bing-Yan Zhu | Quaternary amidino based inhibitors of factor xa |
| NZ592533A (en) * | 2005-11-08 | 2012-08-31 | Millennium Pharm Inc | METHOD FOR THE PREPARATION OF N-(5-CHLORO-2-PYRIDINYL)-2-[[4-[(DIMETHYLAMINO) IMINOMETHYL] BENZOYL] AMINO]-5-METHOXY-BENZAMIDE, A FACTOR Xa INHIBITOR |
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- 2007-11-15 KR KR1020097014306A patent/KR101472765B1/ko not_active Expired - Fee Related
- 2007-11-15 RU RU2009126147/15A patent/RU2452484C2/ru not_active IP Right Cessation
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- 2007-11-15 CA CA2671502A patent/CA2671502C/en not_active Expired - Fee Related
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- 2007-11-15 ES ES07864488T patent/ES2409090T3/es active Active
- 2007-11-15 EP EP07864488A patent/EP2101760B1/en not_active Revoked
- 2007-11-15 SG SG10201504425SA patent/SG10201504425SA/en unknown
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- 2009-07-08 CO CO09070741A patent/CO6220933A2/es not_active Application Discontinuation
- 2009-07-08 MA MA32076A patent/MA31086B1/fr unknown
- 2009-07-08 EC EC2009009501A patent/ECSP099501A/es unknown
- 2009-07-21 NI NI200900145A patent/NI200900145A/es unknown
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- 2012-02-10 RU RU2012104816/15A patent/RU2012104816A/ru not_active Application Discontinuation
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| ECSP099501A (es) | 2010-01-29 |
| HK1134031A1 (en) | 2010-04-16 |
| SG10201504425SA (en) | 2015-07-30 |
| IL199219A0 (en) | 2010-03-28 |
| EP2101760A2 (en) | 2009-09-23 |
| US8404724B2 (en) | 2013-03-26 |
| EP2101760B1 (en) | 2013-02-27 |
| CA2913963A1 (en) | 2008-06-19 |
| CO6220933A2 (es) | 2010-11-19 |
| MA31086B1 (fr) | 2010-01-04 |
| WO2008073670A3 (en) | 2008-11-27 |
| AU2007333377B2 (en) | 2014-01-16 |
| WO2008073670A2 (en) | 2008-06-19 |
| NI200900145A (es) | 2010-11-29 |
| RU2009126147A (ru) | 2011-01-20 |
| AU2007333377A1 (en) | 2008-06-19 |
| KR20090107499A (ko) | 2009-10-13 |
| KR101472765B1 (ko) | 2014-12-15 |
| CA2671502C (en) | 2017-01-24 |
| PT2101760E (pt) | 2013-05-07 |
| CR10914A (es) | 2009-08-12 |
| CN105193799A (zh) | 2015-12-30 |
| RU2452484C2 (ru) | 2012-06-10 |
| US20080153876A1 (en) | 2008-06-26 |
| IL199219A (en) | 2013-10-31 |
| NZ578180A (en) | 2012-02-24 |
| ES2409090T3 (es) | 2013-06-24 |
| CA2671502A1 (en) | 2008-06-19 |
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