- The involvement of the mitochondrial amidoxime reducing component (MARC) in the reductive metabolism of hydroxamic acidsS
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The mitochondrial amidoxime reducing component is a recently discovered molybdenum enzyme in mammals which, in concert with the electron transport proteins cytochrome b5 and NADH cytochrome b5 reductase, catalyzes the reduction of N-oxygenated structures.
- Ginsel, Carsten,Plitzko, Birte,Froriep, Danilo,Stolfa, Diana A.,Jung, Manfred,Kubitza, Christian,Scheidig, Axel J.,Havemeyer, Antje,Clement, Bernd
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supporting information
p. 1396 - 1402
(2018/09/13)
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- CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.
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Paragraph 00443; 00444
(2018/07/29)
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- 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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Page/Page column 11
(2009/12/05)
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- SUBSTITUTED TETRAHYDROISOCHINOLINES AS MMP INHIBITORS, RELATED PRODUCTION METHOD AND USE AS MEDICINE
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The invention concerns compounds of formula (I), wherein: at least one substituent R1, R2 or R3 represents an X-Q-Y group which enhances solubility, as well as the use of said compounds as medicines for preventing and/or treating diseases in which matrix metalloproteinases exhibit an increased activity.
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Page/Page column 37
(2008/06/13)
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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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- Sulfonylamino derivatives which inhibit matrix-degrading metalloproteinases
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Compounds of formula (I) wherein W is —OH or —NHOH; X is an optionally substituted heterocycle, NR1SO2R2, heterocyclylalkythio, CONR2R3or NR1COR2; Y, Z, R1-R3and n are as defined in the application. Compounds (I) are inhibitors of matrix-degrading metalloproteinases and are use for the treatment of related conditions.
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- Process for alkylating hindered sulfonamides
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The present invention relates to a process for alkylating hindered sulfonamides by Michael addition to propiolates, and to novel intermediates prepared in said process. The products of these reactions can be converted into pharmaceutical compounds useful
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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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- Sulfonylamino acid and sulfonylamino hydroxamic acid derivatives
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Compounds of formula wherein W is —OH or —NHOH; X is a heterocycle with the proviso that when X is a nitrogen containing heterocycle, the heterocycle is attached to the (CH2)mmoiety by a ring nitrogen, —CONR2R3,
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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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