CO6220933A2 - Formulaciones de dosis unitaria y metdods para el tratamiento de la trombosis con un inhibidor oral del facror xa - Google Patents

Formulaciones de dosis unitaria y metdods para el tratamiento de la trombosis con un inhibidor oral del facror xa

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Publication number
CO6220933A2
CO6220933A2 CO09070741A CO09070741A CO6220933A2 CO 6220933 A2 CO6220933 A2 CO 6220933A2 CO 09070741 A CO09070741 A CO 09070741A CO 09070741 A CO09070741 A CO 09070741A CO 6220933 A2 CO6220933 A2 CO 6220933A2
Authority
CO
Colombia
Prior art keywords
4alkylene
6alkynyl
6alkenyl
4alkyl
substituents
Prior art date
Application number
CO09070741A
Other languages
English (en)
Inventor
Uma Sinha
Stanley Hollenbach
Keith Abe
Original Assignee
Millennium Pharm Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39110529&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO6220933(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Publication of CO6220933A2 publication Critical patent/CO6220933A2/es

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Classifications

    • 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)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Investigating Or Analysing Biological Materials (AREA)

Abstract

1.- Un método para inhibir coagulación en un paciente humano en necesidad del mismo, que comprende administrar al paciente una cantidad inhibitoria de la coagulación de un compuesto inhibidor del factor X de la Fórmula I:en donde: A se selecciona a partir de: (a) C1-C6-alquilo; (b) C3- C8- Cicloalquilo; (c) -N(R1R2), N(R1,R2) - C(N=R3)-, N(R1,R2) - C(=NR3) - N(R4)-, R1-C(=NR3)-R1-C(=NR3)-N(R4) -; (d) fenilo, el cual es independientemente sustituido por 0- 2 sustituyentes R; (e) naftilo, el cual es independientemente sustituido por 0- 2 sustituyentes R; y un sistema anular monocíclico o heterocíclico bicíclico fusionado que tiene entre 5 y 10 átomos cíclicos, en donde 1- 4 átomos cíclicos del sistema anular son seleccionados a partir de N, O y S, y en donde el sistema anular se puede sustituir con 0- 2 Sustituyentes R; R se selecciona a partir del grupo H, halo, -CN, -CO2R1, -C(=O) - N(R1, R2) , -(CH2V-CO2R1, -(CH2)m-C(=O)- N(R1, R2), -NO2, -SOjNCR1, R2), - SO2R1, -(CH2)mNR1R2, -(CH2)m-C(=NR3)-R1, -(CH2)m-C(=NR3) - N(R1, R2), -(CH2) m-N(R4) - C(=NR3) - N(R1,R2), (CH2VNR1- anexado a un anillo heterocíclico de 3 a 6 miembros conteniendo entre 1 y 4 heteroátomos seleccionados a partir de N, O y S, - C1-4alquilo, -C2-6alquenilo, - C2-6alquinilo, - C3-8Cicloalquilo, -C0-4alquileno-C3-8Cicloalquilo, -CF3, -O, y un sistema heterocíclico de 5- 6 miembros conteniendo entre 1 y 4 heteroátomos seleccionados a partir de N, O y S, en donde entre 1 y 4 átomos de hidrógeno sobre el sistema heterocíclico se pueden independientemente reemplazar por un miembro seleccionado a partir del grupo que consta de halo, -C1-C4- alquilo, -C1-4alquil-CN, - C2- 6alquenilo, -C2-6alquinilo, -C3-8Cicloalquilo, -C0-4alquileno-C3- 8Cicloalquilo y - NO2;m es un entero de 0- 2; R1, R2, R3 y R4 son independientemente seleccionados a partir del grupo que consta de: H, -OR5, -N(-R5, -R6), -C1-4alquilo, - C2-6alquenilo, -C2-6alquinilo, -C3-8Cicloalquilo, -C0-4alquileno-C3-8Cicloalquilo, -C0-4alquilfenilo y -C0- 4alquilnaftilo, en donde entre 1 y 4 átomos de hidrógeno sobre los átomos cíclicos de las fracciones de fenilo y naftilo se pueden independientemente reemplazar ...
CO09070741A 2006-12-08 2009-07-08 Formulaciones de dosis unitaria y metdods para el tratamiento de la trombosis con un inhibidor oral del facror xa CO6220933A2 (es)

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
CO6220933A2 true CO6220933A2 (es) 2010-11-19

Family

ID=39110529

Family Applications (1)

Application Number Title Priority Date Filing Date
CO09070741A CO6220933A2 (es) 2006-12-08 2009-07-08 Formulaciones de dosis unitaria y metdods para el tratamiento de la trombosis con un inhibidor oral del facror xa

Country Status (19)

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)
HK (1) HK1134031A1 (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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RU2009126147A (ru) 2011-01-20
US20080153876A1 (en) 2008-06-26
AU2007333377A1 (en) 2008-06-19
RU2452484C2 (ru) 2012-06-10
CA2671502A1 (en) 2008-06-19
WO2008073670A3 (en) 2008-11-27
EP2101760B1 (en) 2013-02-27
US8404724B2 (en) 2013-03-26
IL199219A0 (en) 2010-03-28
PT2101760E (pt) 2013-05-07
CA2913963A1 (en) 2008-06-19
HK1134031A1 (en) 2010-04-16
WO2008073670A2 (en) 2008-06-19
AU2007333377B2 (en) 2014-01-16
MA31086B1 (fr) 2010-01-04
IL199219A (en) 2013-10-31
CR10914A (es) 2009-08-12
SG10201504425SA (en) 2015-07-30
NI200900145A (es) 2010-11-29
KR20090107499A (ko) 2009-10-13
CA2671502C (en) 2017-01-24
EP2101760A2 (en) 2009-09-23
ECSP099501A (es) 2010-01-29
NZ578180A (en) 2012-02-24
KR101472765B1 (ko) 2014-12-15
RU2012104816A (ru) 2013-08-20
ES2409090T3 (es) 2013-06-24

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