Matriptase inhibitors and uses thereof against orthomyxoviridae infections
AssigneeSocpra Sciences Sante Et Humaines S.E.C.
InventorsMartin Richter, Richard Leduc, Eloic Colombo, Eric Marsault
Life of this patent
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Abstract
The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flu infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and preventing orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.
Claims14
1-24. (canceled)
A method of preventing or treating an orthomyxovirus infection in a subject, said method comprising administering to said subject a therapeutically effective amount of a matriptase inhibitor, or a composition comprising said inhibitor, to said subject.
28-29. (canceled)
(canceled)
A method of inhibiting matriptase activity in a cell, comprising contacting the cell with an effective amount of a compound formula (1):
- or a pharmaceutically acceptable salt, hydrate, solvate, or stereoisomer thereof, wherein
- R12 is H, NH2 or NHR7;
- wherein R7 is an alkyl, aryl, (C═O)-alkyl, (C═O)-aryl, SO2-alkyl, SO2-aryl, C(═NH)—NH2, C(═NH)—NHalkyl, C(═NH)—NHaryl,
- or one or more amino acids residues;
- R13 is H, NH2 or NHR7;
- wherein R7 is an alkyl, aryl, (C═O)-alkyl, (C═O)-aryl, SO2-alkyl or SO2-aryl, C(═NH)—NH2, C(═NH)—NHalkyl, C(═NH)—NHaryl or one or more amino acids residues;
- R1 is H, NH2 or NHR7;
- wherein R7 is an alkyl, aryl, (C═O)-alkyl, (C═O)-aryl, SO2-alkyl or SO2-aryl, C(═NH)—NH2, C(═NH)—NHalkyl, C(═NH)—NHaryl or one or more amino acids residues;
- R2 and R5 are independently —CH2—R8 or
- wherein R8 is (CH2)n-NH(C═NH)NH—R14 or (CH2)n-NH—R14, wherein,
- n is 1 to 4;
- m is 0 to 3;
- R10 is —C(═NH)—NH2, NH2 or NH alkyl;
- and
- R14 is H, alkyl, NH2, NO2 or COalkyl;
- R3 and R4 are independently an alkyl, an aryl, a substituted alkyl, a substituted aryl, an heteroaryl, a substituted heteroaryl, a side chain of an amino acid or a substituted side chain of an amino acid;
- R6 is
- CF3, CO2H, CONH2, CONH-alkyl, CONH-aryl or CO-(amino acid residue)p, wherein p is 1 to 3;
- wherein W, X, Y and Z are independently N or CH;
- V and U are independently O, NH, NCH3 or S;
- and
- R11 is H, CO2H, CONH-alkyl, CONH-aryl, aryl, heteroaryl, halide or CO-(amino acid residue)q, wherein q is 1 or 2;
- or
- (ii) a composition comprising
- (a) a compound of formula (1)′
- (b) further therapeutic agent for treating or preventing an orthomyxovirus infection and/or associated symptoms;
- (c) a pharmaceutically acceptable excipient;
- or
- (d) a combination of (a) and (b);
- whereby said matriptase activity is inhibited.
38-76. (canceled)
Dependencies are inferred from the claim text.