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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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Prior art keywords
surfactant
combination
protease inhibitors
hcv protease
hydrochloride salt
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Active
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ES06760571.7T
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English (en)
Inventor
Bruce A. Malcolm
Prudence K. Bradley
Anastasia Pavlovsky
Wing-Kee Philip Cho
Zhihui Qiu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Organon Pharma UK Ltd
Merck Sharp and Dohme LLC
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Merck Sharp and Dohme Ltd
Merck Sharp and Dohme LLC
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Publication of ES2572980T3 publication Critical patent/ES2572980T3/es
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • 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
    • A61K31/445—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
    • A—HUMAN NECESSITIES
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    • 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
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    • A61K38/05—Dipeptides
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    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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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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Application Number Title Priority Date Filing Date
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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ZA200709987B (en) 2008-11-26
BRPI0610737A2 (pt) 2010-07-20
AR055198A1 (es) 2007-08-08
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