- Radiolabelled MMP selective compounds
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The invention is directed to radiolabelled MMP selective compounds, a processes for the preparation thereof, and uses thereof. The derivatives of the invention have formula (I) wherein Y represents O, CH2, (CH2)2, S, NH, o
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(2009/12/05)
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- Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof
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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.
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- 3-(arylsulfonylamino)-tetrahydrofuran-3-carboxylic acid hydroxamides
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A compound of the formula wherein R1, R2and Q is as defined above, are useful in the treatment of a arthritis (including osteoarthritis and rheumatoid arthritis), cancer (such as solid tumor cancer including colon cancer, breast canc
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- Processes for preparing 3-Arylsulfur hydroxamic acids
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This invention provides processes for the preparation of a compound of Formula I: Y—C(═O—C(R1)(R2)—CH2—S(O)nR3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R1is hydrogen or lower alkyl; R2is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1and R2together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R3is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.
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- Arylsulfonylamino hydroxamic acid derivatives
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A compound of the formula wherein R1, R2and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal dise
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- 3-(arylsulfonylamino)-tetrahydropyran-3-carboxylic acid hydroxamides
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A compound of the formula wherein R1, R2, R3, R4and Q are as defined above, are useful in the treatment of arthritis (including osteoarthritis and rheumatoid arthritis), cancer and other diseases. In addition, t
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- Metalloproteinase inhibitors and intermediates useful for their preparation
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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.
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- (4-arylsulfonylamino)-tetrahydropyran-4-carboxylic acid hydroxamides
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PCT No. PCT/IB99/00505 Sec. 371 Date Sep. 1, 1999 Sec. 102(e) Date Sep. 1, 1999 PCT Filed Mar. 24, 1999 PCT Pub. No. WO99/52889 PCT Pub. Date Oct. 21, 1999A compound of the formula wherein Q is as defined above, are useful in the treatment of a condition
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