ES2572980T3 - Combinación de inhibidores de la proteasa del VHC con un tensioactivo - Google Patents

Combinación de inhibidores de la proteasa del VHC con un tensioactivo Download PDF

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Publication number
ES2572980T3
ES2572980T3 ES06760571.7T ES06760571T ES2572980T3 ES 2572980 T3 ES2572980 T3 ES 2572980T3 ES 06760571 T ES06760571 T ES 06760571T ES 2572980 T3 ES2572980 T3 ES 2572980T3
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surfactant
combination
protease inhibitors
hcv protease
hydrochloride salt
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Inventor
Bruce A. Malcolm
Prudence K. Bradley
Anastasia Pavlovsky
Wing-Kee Philip Cho
Zhihui Qiu
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/47—Quinolines; Isoquinolines
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    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Abstract

Una formulacion farmaceutica que comprende: (a) al menos un tensioactivo, en donde dicho al menos un tensioactivo es lauril sulfato de sodio, y (b) al menos un compuesto seleccionado entre el grupo que consiste en el compuesto de Formula Ia:**Fórmula** y sales o solvatos farmaceuticamente aceptables de la misma.

Description

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Método D
En otra variación más, la sal de clorhidrato 1.13 se convirtió en el carbamato de 4-nitrofenilo 1.15 mediante la reacción con cloroformiato de 4-nitrofenilo. El tratamiento posterior con una amina (o sal de clorhidrato de amina) de elección proporcionó el compuesto objetivo 1.14.
imagen15
10 Método E
En otra variación más, la sal de clorhidrato dipeptídica 1.04 se convirtió en el carbamato de 4-nitrofenilo como se ha descrito anteriormente. El tratamiento con una amina (o sal de clorhidrato de amina) de elección proporcionó el
15 derivado de urea 1.05. La hidrólisis y la elaboración adicional como se ha descrito en los Métodos A/B proporcionaron los compuestos objetivo 1.14.
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Claims (1)

  1. imagen1
ES06760571.7T 2005-06-02 2006-05-31 Combinación de inhibidores de la proteasa del VHC con un tensioactivo Active ES2572980T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US68694505P 2005-06-02 2005-06-02
US686945P 2005-06-02
PCT/US2006/021003 WO2006130628A2 (en) 2005-06-02 2006-05-31 Combination of hcv protease inhibitors with a surfactant

Publications (1)

Publication Number Publication Date
ES2572980T3 true ES2572980T3 (es) 2016-06-03

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ES06760571.7T Active ES2572980T3 (es) 2005-06-02 2006-05-31 Combinación de inhibidores de la proteasa del VHC con un tensioactivo

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Country Link
US (1) US7772178B2 (es)
EP (1) EP1919478B1 (es)
JP (2) JP5160415B2 (es)
KR (1) KR20080021634A (es)
CN (1) CN101212970B (es)
AR (1) AR055198A1 (es)
AU (1) AU2006252553B2 (es)
BR (1) BRPI0610737A2 (es)
CA (1) CA2611155A1 (es)
ES (1) ES2572980T3 (es)
MX (1) MX2007015270A (es)
NO (1) NO20076613L (es)
NZ (1) NZ563365A (es)
PE (1) PE20070011A1 (es)
TW (1) TWI428138B (es)
WO (1) WO2006130628A2 (es)
ZA (1) ZA200709987B (es)

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US7772178B2 (en) 2010-08-10
TWI428138B (zh) 2014-03-01
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AR055198A1 (es) 2007-08-08
PE20070011A1 (es) 2007-03-08
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JP5160415B2 (ja) 2013-03-13
AU2006252553A1 (en) 2006-12-07
CN101212970B (zh) 2010-07-21
CA2611155A1 (en) 2006-12-07
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NZ563365A (en) 2011-02-25
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US20070010431A1 (en) 2007-01-11
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MX2007015270A (es) 2008-02-21

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