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US 8,993,544 B2Granted
Carbamoylphosphonates as inhibitors and uses thereof
AssigneeYissum Research Development Company of the Hebrew University of Jerusalem
InventorsEli Breuer, Reuven Reich, Julia Frant, Amnon Hoffman, Veerendhar Ainelly
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel metalloproteinase inhibitors having an aryloxybenzenesulfonamide moiety and a carbamoylphosphonic acid moiety, to pharmaceutical compositions comprising them, and to their uses in the prevention and/or treatment of disease or disorder associated with MMP.
Claims32
A compound defined by formula (II):
- wherein
- L is a C1-C10-alkylene, being optionally substituted with A;
- X1 is at least one substituent selected from —H;
- halo;
- —C1-C6-alkyl;
- —C2-C6-alkenyl;
- —C2-C6-alkynyl;
- —C3-C6-cycloalkyl;
- —C6-C10-aryl;
- —CF3;
- —OH;
- —O—C1-C6-alkyl;
- —NO2;
- —NHC(O)R3;
- and —NR′R″, each of said R′ and R″ independently of each other is selected from —H and —C1-C6-alkyl;
- each of R1 and R2, independently of each other, is selected from —H, —C1-C6-alkyl, —CR4R5—O—(O)C—C1-C6-alkyl and a cation;
- R3 is selected from —C1-C6-alkyl;
- —C2-C6-alkenyl;
- —C2-C6-alkynyl;
- —C3-C6-carbocyclic rings;
- —O—C1-C6-alkyl;
- —CF3;
- and —C6-C10-aryl;
- each of R4 and R5, independently of each other, is selected from —H and C1-C6-alkylene;
- and
- A is selected from —H;
- halo;
- C1-C6-alkyl;
- —C2-C6-alkenyl;
- —C2-C6-alkynyl;
- —C3-C6-cycloalkyl;
- —CF3;
- —C6-C10-aryl;
- OH;
- —O—C1-C6-alkyl;
- —NO2;
- —N3, and —NR′R″, wherein each of said R′ and R″ independently of each other is selected from —H, —C1-C6-alkyl and —C(O)O-t-Bu.
34 more elements
The compound according to 1, being a compound of formula (III):
- wherein
- n is an integer from 2 to 10.
A compound defined by formula (VI):
- wherein
- X1 is at least one substituent selected from —H;
- halo;
- —C1-C6-alkyl;
- —C2-C6-alkenyl;
- —C2-C6-alkynyl;
- —C3-C6-cycloalkyl;
- —C6-C10-aryl;
- —CF3;
- —OH;
- —O—C1-C6-alkyl;
- —NO2;
- —NHC(O)R3;
- and —NR′R″, each of said R′ and R″ independently of each other is selected from —H and —C1-C6-alkyl;
- each of R1 and R2, independently of each other, is selected from —H, —C1-C6-alkyl, —CR4R5—O—(O)C—C1-C6-alkyl and a cation;
- Z is O or —NR6;
- R6 is selected from —H;
- —C2-C6-alkenyl;
- —C2-C6-alkynyl;
- —C3-C6-cycloalkyl;
- —CF3;
- and —C6-C10-aryl;
- and
- each of k and y, independently of each other is an integer between 1 and 9.
21 more elements
A compound selected from the following Compounds:
- wherein said compound is in a form selected from salt, internal salt, hydrate, polymorph, racemic, stereoisomeric and diastereomeric mixtures.
Dependencies are inferred from the claim text.