192329-80-9Relevant academic research and scientific papers
Aromatic sulfone hydroxamic acid metalloprotease inhibitor
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, (2008/06/13)
A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor. A contemplated compound corresponds in structure to formula B, below,
Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof
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, (2008/06/13)
The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt of solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.
Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their pharmaceutical uses
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, (2008/06/13)
The present invention relates to compounds of formula I:wherein Ar is an aryl group or a heteroaryl group; X is -NH-OH or -OH; R1 is H, -CH(R3)(R4), -C(O)R3, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group, wherein R3 is
Metalloproteinase inhibitors and intermediates useful for their preparation
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, (2008/06/13)
PCT No. PCT/US96/19328 Sec. 371 Date Jun. 29, 1998 Sec. 102(e) Date Jun. 29, 1998 PCT Filed Dec. 5, 1996 PCT Pub. No. WO97/20824 PCT Pub. Date Jun. 12, 1997The invention relates to compounds of formula (1) wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder is carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of formula (1) or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.
METALLOPROTEINASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR PHARMACEUTICAL USES
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, (2008/06/13)
Compounds of the formula I: STR1 wherein Y is O or S, Ar is an aryl group or a heteroaryl group, R is H, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, or--C(O)R. sub.1, wherein R 1 is hydrogen, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, or NR. sub.2 R 3, wherein R 2 and R 3 independently are hydrogen, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group, and X is--NH--OH or--OH. Pharmaceutically acceptable prodrugs, salts and solvates of these compounds. Methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt of solvate thereof. Pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates.
