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09/18/08 - USPTO Class 514 |  58 views | #20080227858 | Prev - Next | About this Page  514 rss/xml feed  monitor keywords

Inhibitors of matrix metalloproteinase

Title: Inhibitors of matrix metalloproteinase




Brief Patent Description - Full Patent Description - Patent Claims

The Patent Description & Claims data below is from USPTO Patent Application 20080227858, Inhibitors of matrix metalloproteinase.


1. A compound of formula (I): wherein: R1 represents optionally substituted C4-12 alkyl, optionally substituted C2-6alkylaryl, or optionally substituted 5- or 6-membered aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR4, OCR4R5, CR4R50, or Z, R1 and Q together form an optionally substituted fused tricyclic group; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents COR3 or N(OR8)COR9; R2 represents SO2R10 or SO2NR10R9; R3 represents OR6, NR6R7 or NR6OH; R4 and R5 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R6 and R7 each independently represents H, C1-6 alkyl, or C1-6 alkyl substituted with one or more heteroaryl groups, or R6 and R7 together with the nitrogen atom to which they are attached form a 5- or 6-membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; R8 and R9 each independently represents H or C1-6 alkyl; R10 and R11 each independently represents H or C1-6 alkyl; and and physiologically functional derivatives thereof, with the exception of N-(ethoxycarbonyl)-N-[4-(1H-tetrazol-1-yl)phenyl]glycine.

2. A compound of formula (Ia): wherein: R10 represents H or C1-6 alkyl; R12 represents H, halo, CF3, cyano, OCF3, nitro, OR3, SR3, COR13 or C1-6 alkyl; R13 represents C1-6 alkyl or C1-4alkylaryl; and physiologically functional derivatives thereof.

3. A method for treatment of a human or animal subject suffering from or susceptible to an autoimmune disorder or an inflammatory condition, which comprises administering to said human or animal subject an effective amount of a compound of claim 1.

4. A pharmaceutical composition, comprising a compound of claim 1 and a pharmaceutically acceptable carrier therefor, and optionally one or more other therapeutic agents.

5. A process for preparation of compounds of formula (I) according to claim 1, which comprises: (A) preparing a compound of formula (I), wherein Z represents a bond and R1 represents an optionally substituted C2-6alkylaryl or an optionally substituted 5- or 6-membered aryl or heteroaryl, by reacting a compound of formula (II): wherein R2, Q and X are as previously defined for formula (I) and L represents a leaving group, with a reagent suitable to introduce the group R1; or (B) preparing a compound of formula (I), wherein Z represents a bond and R1 represents an optionally substituted C4-12alkyl, by reacting a compound of formula (III): wherein R2, Q and X are as previously defined for formula (I), with a reagent suitable to introduce the group R1; or (C) preparing a compound of formula (I), wherein Z represents OS, SO, SO2, NR4 or OCR4R5, and R1 represents an optionally substituted C4-12alkyl, by reacting a compound of formula (IV): wherein X, R2 and Q are as previously defined for formula (I), and Y represents OH, SH, NR4H or HCR4R5, with a reagent suitable to introduce group R1, provided that when Y is SH it is followed by optional oxidation of sulphide to sulfoxide or sulfone; or (D) preparing a compound of formula (I), wherein Z represents OS, SO, SO2, or NR4, and R1 represents an optionally substituted C2-6alkylaryl or an optionally substituted 5- or 6-membered aryl or heteroaryl, by reacting a compound of formula (IV): wherein X, R2 and Q are as previously defined for formula (I), and Y represents OH, SH or NR4H, with a reagent suitable to couple to group R1, provided that when Y is SH it is followed by optional oxidation of the sulphide to sulfoxide or sulfone; or (E) preparing a compound of formula (I), wherein Z represents OCR4R5 and R1 represents an optionally substituted C2-6alkylaryl or an optionally substituted 5- or 6-membered aryl or heteroaryl, by reacting a compound of formula (V): wherein X, R2 and Q are as defined for formula (I) and L4 is a suitable leaving group, with a reagent suitable to introduce group R1—O; or (F) preparing a compound of formula (I), wherein Z represents CR4R50, by reacting a compound of formula (IV): wherein R2 and Q are as defined for formula (I), and Y represents OH, with a reagent suitable to introduce group R1CR4R5—; or (G) preparing a compound of formula (I), wherein Z represents CH2, by reacting a compound of formula (III): wherein R2, Q and X are as defined for formula (I), with a reagent suitable to introduce group R1CH2; (H) reacting a compound of formula (VI) or a protected derivative thereof, wherein R1, Z, Q and X are as defined for formula (I), with a reagent suitable to introduce group R2 as defined for formula (I): or (J) carrying out a process selected from processes (A) to (G) followed by interconversion of one or more functional groups.

Brief Patent Description - Full Patent Description - Patent Claims

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Drug, bio-affecting and body treating compositions

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