ECSP099501A - Formulaciones de dosis unitaria y métodos para el tratamiento de la trombosis con un inhibidor oral del factor xa - Google Patents
Formulaciones de dosis unitaria y métodos para el tratamiento de la trombosis con un inhibidor oral del factor xaInfo
- Publication number
- ECSP099501A ECSP099501A EC2009009501A ECSP099501A ECSP099501A EC SP099501 A ECSP099501 A EC SP099501A EC 2009009501 A EC2009009501 A EC 2009009501A EC SP099501 A ECSP099501 A EC SP099501A EC SP099501 A ECSP099501 A EC SP099501A
- Authority
- EC
- Ecuador
- Prior art keywords
- factor
- coagulation
- inhibitors
- patient
- inhibitor
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 4
- 108010074860 Factor Xa Proteins 0.000 title abstract 2
- 208000007536 Thrombosis Diseases 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 229940123583 Factor Xa inhibitor Drugs 0.000 abstract 4
- 230000015271 coagulation Effects 0.000 abstract 4
- 238000005345 coagulation Methods 0.000 abstract 4
- 230000002401 inhibitory effect Effects 0.000 abstract 3
- 239000003146 anticoagulant agent Substances 0.000 abstract 2
- 241000282412 Homo Species 0.000 abstract 1
- 230000002785 anti-thrombosis Effects 0.000 abstract 1
- 229940127219 anticoagulant drug Drugs 0.000 abstract 1
- 239000003130 blood coagulation factor inhibitor Substances 0.000 abstract 1
- 230000000052 comparative effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229940019332 direct factor xa inhibitors Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000005259 measurement Methods 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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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
-
- 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
-
- 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- 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
RESUMEN DEL INVENTOLa modelación comparativa de la medida de cambios en actividad de protominasa a niveles de eficacia antitrombótica ha llevado al descubrimiento de la actividad terapéutica en humanos de inhibidores de factor Xa. Este invento está dirigido a un método para inhibir coagulación en un paciente humano utilizando una cantidad inhibitoria cantidad inhibidora de la coagulación de un inhibidor de factor Xa. Específicamente, inhibidores directos oralmente disponibles de factor Xa son efectivos para inhibir coagulación en un paciente humano cuando se administran al paciente en una cantidad diaria agregada de entre 0.01 y 2.0 miligramos por kilogramo aproximadamente con base en el peso total del paciente ("mg/kg") . Se contempla que esta dosis será efectiva para cualquier compuesto el cual específicamente inhibe factor Xa y particularmente efectiva para inhibidores de factor Xa de las Fórmula I, II, III, IV o V descritas a continuación.El invento también está dirigido a un método de evaluar el estado de la coagulación del paciente. Se contempla que este método de evaluar el estado de la coagulación se puede utilizar para probar un número de clases diferentes de anticoagulantes además de inhibidores de factor Xa.Gráfico (Imagen en formato jpg)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87379206P | 2006-12-08 | 2006-12-08 | |
| US94762907P | 2007-07-02 | 2007-07-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP099501A true ECSP099501A (es) | 2010-01-29 |
Family
ID=39110529
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2009009501A ECSP099501A (es) | 2006-12-08 | 2009-07-08 | Formulaciones de dosis unitaria y métodos para el tratamiento de la trombosis con un inhibidor oral del factor xa |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8404724B2 (es) |
| EP (1) | EP2101760B1 (es) |
| KR (1) | KR101472765B1 (es) |
| CN (1) | CN105193799A (es) |
| AU (1) | AU2007333377B2 (es) |
| CA (2) | CA2671502C (es) |
| CO (1) | CO6220933A2 (es) |
| CR (1) | CR10914A (es) |
| EC (1) | ECSP099501A (es) |
| ES (1) | ES2409090T3 (es) |
| IL (1) | IL199219A (es) |
| MA (1) | MA31086B1 (es) |
| NI (1) | NI200900145A (es) |
| NZ (1) | NZ578180A (es) |
| PT (1) | PT2101760E (es) |
| RU (2) | RU2452484C2 (es) |
| SG (1) | SG10201504425SA (es) |
| WO (1) | WO2008073670A2 (es) |
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|---|---|---|---|---|
| WO2001064642A2 (en) * | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| KR101195801B1 (ko) | 2004-06-18 | 2012-11-05 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Xa 인자 억제제 |
| US7696352B2 (en) * | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| PT1737889E (pt) | 2004-10-19 | 2010-12-13 | Lonza Ag | Método para síntese de péptidos em fase sólida |
| EP1940786B1 (en) | 2005-09-16 | 2010-08-18 | Arrow Therapeutics Limited | Biphenyl derivatives and their use in treating hepatitis c |
| US20090186810A1 (en) * | 2006-03-27 | 2009-07-23 | Portola Pharmaceuticals, Inc. | Potassium channel modulators and platelet procoagulant activity |
| NZ572418A (en) * | 2006-05-05 | 2011-08-26 | Millennium Pharm Inc | Factor xa inhibitors |
| CN101595092B (zh) | 2006-11-02 | 2012-02-01 | 米伦纽姆医药公司 | 合成因子xa抑制剂的医药盐的方法 |
| WO2008086226A2 (en) * | 2007-01-05 | 2008-07-17 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
| EA020531B1 (ru) * | 2007-04-13 | 2014-11-28 | Милленниум Фармасьютикалз, Инк. | КОМБИНИРОВАННАЯ ТЕРАПИЯ АНТИКОАГУЛИРУЮЩЕГО СРЕДСТВА С СОЕДИНЕНИЕМ, КОТОРОЕ ДЕЙСТВУЕТ КАК ИНГИБИТОР ФАКТОРА Ха |
| KR101509829B1 (ko) * | 2007-05-02 | 2015-04-06 | 포톨라 파마슈티컬스, 인코포레이티드 | 혈소판 adp 수용체 억제제로 작용하는 화합물을 이용한 병용요법 |
| UA103319C2 (en) | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
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| FI3362065T3 (fi) | 2015-10-15 | 2024-06-19 | Servier Lab | Ivosidenibiä, sytarabiinia ja daunorubisiinia tai idarubisiinia käsittävä yhdistelmähoito akuutin myelooisen leukemian hoitamiseksi |
| AU2018300150A1 (en) | 2017-07-11 | 2020-01-30 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
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| US6844367B1 (en) * | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| WO2001064642A2 (en) * | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| GB0021497D0 (en) * | 2000-09-01 | 2000-10-18 | Novartis Res Foundation | Compounds and their use |
| EP1322637A2 (en) * | 2000-09-29 | 2003-07-02 | Millennium Pharmaceuticals, Inc. | Quaternary amidino based inhibitors of factor xa |
| PE20070717A1 (es) * | 2005-11-08 | 2007-08-17 | Millennium Pharm Inc | Sal de maleato y polimorfo de [2-({4-[(dimetilamino)iminometil]fenil}carbonilamino)-5-metoxifenil]-n-(5-cloro-(2-piridil))carboxamida |
-
2007
- 2007-11-15 KR KR1020097014306A patent/KR101472765B1/ko not_active Expired - Fee Related
- 2007-11-15 SG SG10201504425SA patent/SG10201504425SA/en unknown
- 2007-11-15 ES ES07864488T patent/ES2409090T3/es active Active
- 2007-11-15 WO PCT/US2007/084887 patent/WO2008073670A2/en not_active Ceased
- 2007-11-15 CA CA2671502A patent/CA2671502C/en not_active Expired - Fee Related
- 2007-11-15 CA CA2913963A patent/CA2913963A1/en not_active Abandoned
- 2007-11-15 AU AU2007333377A patent/AU2007333377B2/en not_active Ceased
- 2007-11-15 CN CN201510530619.8A patent/CN105193799A/zh active Pending
- 2007-11-15 PT PT78644887T patent/PT2101760E/pt unknown
- 2007-11-15 RU RU2009126147/15A patent/RU2452484C2/ru not_active IP Right Cessation
- 2007-11-15 EP EP07864488A patent/EP2101760B1/en not_active Revoked
- 2007-11-15 NZ NZ578180A patent/NZ578180A/en not_active IP Right Cessation
- 2007-12-07 US US11/999,957 patent/US8404724B2/en not_active Expired - Fee Related
-
2009
- 2009-06-07 IL IL199219A patent/IL199219A/en active IP Right Grant
- 2009-07-06 CR CR10914A patent/CR10914A/es unknown
- 2009-07-08 MA MA32076A patent/MA31086B1/fr unknown
- 2009-07-08 CO CO09070741A patent/CO6220933A2/es not_active Application Discontinuation
- 2009-07-08 EC EC2009009501A patent/ECSP099501A/es unknown
- 2009-07-21 NI NI200900145A patent/NI200900145A/es unknown
-
2012
- 2012-02-10 RU RU2012104816/15A patent/RU2012104816A/ru not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PT2101760E (pt) | 2013-05-07 |
| AU2007333377A1 (en) | 2008-06-19 |
| RU2452484C2 (ru) | 2012-06-10 |
| US20080153876A1 (en) | 2008-06-26 |
| MA31086B1 (fr) | 2010-01-04 |
| CN105193799A (zh) | 2015-12-30 |
| HK1134031A1 (en) | 2010-04-16 |
| KR101472765B1 (ko) | 2014-12-15 |
| KR20090107499A (ko) | 2009-10-13 |
| EP2101760A2 (en) | 2009-09-23 |
| CA2913963A1 (en) | 2008-06-19 |
| CA2671502A1 (en) | 2008-06-19 |
| RU2012104816A (ru) | 2013-08-20 |
| AU2007333377B2 (en) | 2014-01-16 |
| EP2101760B1 (en) | 2013-02-27 |
| ES2409090T3 (es) | 2013-06-24 |
| RU2009126147A (ru) | 2011-01-20 |
| SG10201504425SA (en) | 2015-07-30 |
| IL199219A0 (en) | 2010-03-28 |
| CR10914A (es) | 2009-08-12 |
| WO2008073670A3 (en) | 2008-11-27 |
| US8404724B2 (en) | 2013-03-26 |
| WO2008073670A2 (en) | 2008-06-19 |
| IL199219A (en) | 2013-10-31 |
| CO6220933A2 (es) | 2010-11-19 |
| NI200900145A (es) | 2010-11-29 |
| CA2671502C (en) | 2017-01-24 |
| NZ578180A (en) | 2012-02-24 |
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