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US 6,307,101 B1Granted
Inhibitors of metalloproteases, pharmaceutical compositions comprising same and methods of their use
OwnerDavid A. Campbell, Dinesh V. Patel +1inventors
InventorsDavid A. Campbell, Dinesh V. Patel, Xiao-Yi Xiao
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Abstract
Disclosed are novel inhibitors of metalloproteases, in particular matrix metalloproteases. The disclosed inhibitors are mercaptoketone and mercaptoalcohol compounds which are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, for example, arthropathy, dermatological conditions, bone resorption, inflammatory diseases, and tumor invasion and in the promotion of wound healing.
Claims4
A compound comprising the formula:
- wherein
- A is selected from the group consisting of C═O and CHOH;
- M is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, and heteroaryl;
- R1 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclic and heterocyclicalkyl;
- R2 is hydrogen, or R1 and R2 together with the nitrogen atom to which they are attached form a heterocyclic or heteroaryl ring;
- R3 is —(CH2)n—V wherein n is a whole number from 0 to 4 and V is selected from the group consisting of hydrogen, alkyl, substituted alkyl, —OR, —NR12R13, and —SR13, wherein R12 and R13 are each independently hydrogen, allyl, substituted alkyl, alkenyl, aryl, arylalkyl, —C(O)-alkyl, —C(O)-substituted alkyl, —C(O)-aryl, —C(O)-heteroaryl, heteroaryl heterocyclic, heterocyclicalkyl or heteroarylalkyl wherein, in the case of —NR12R13, the nitrogen atom is optionally incorporated into the heteroaryl or heterocyclic ring structure;
- and
- pharmaceutically acceptable salts thereof.
5 more elements
Dependencies are inferred from the claim text.