Abstract: The invention relates to a method of preventing or treating cartilage damage by administering a GABA analog such as, for example, a compound of Formula and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or straight or branched lower alkyl, and n is an integer of from 4 to 6.

Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, R2, R3, and R4 are as defined in the specification. The invention also provides related pharmaceutical compositions, methods of use, and combinations.

Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.

Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.

Abstract: Selective MMP-13 inhibitors are pyrimidine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R2 is hydrogen, halo, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.

Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, Y2, Y3, Y4, U5, U6, U8, and R2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition.

Abstract: GABA analogs such as gabapentin and pregabalin are useful to prevent and treat inflammatory diseases.

Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.

Abstract: Oxidation of organic compounds is catalyzed by addition of a catalytic amount of a metalloporphyrin in a non-reactive aprotic solvent.

Abstract: The present invention provides compounds and methods of synthesizing furanose and aminofuranose compounds of Formula I which are useful fro treating rheumatoid arthritis, immunomodulatory diseases and disorders, inflammation, and diseases and disorders characterized by exhibiting tissue proliferation.

Abstract: A compound selected from those of formula (I): wherein: X1, X2, and X3, represent N or —CR3 in which R3 is as described in the description, G1 represents a group selected from those of formulae (i/a) and (i/b): in which R4, R5, and R6 are as defined in the description, G2 represents a group selected from carbon-carbon triple bond, —CH═C═CH—, C═O, C═S, S(O)n1 in which n1 represents an integer from 0 to 2 inclusive, or a group of formula (i/c): in which Y1 represents O, S, —NH or —N alkyl, and Y2 represents O, S, —NH or —N alkyl, n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, Z1 represents —CR9R10, wherein R9 and R10 are as defined in the description, A represents a ring system, R1 represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d): in which p, Z2, B, q and G3 are as de

Abstract: Inhibitors of MMP enzymes are cyclic sulfonamides of Formula I or a pharmaceutically acceptable salt thereof, and cyclic sulfonamides of Formula III or a pharmaceutically acceptable salt thereof, wherein R1 and R2 include hydrogen, alkyl, and substituted alkyl; R3 and R4 include hydrogen, halo, and alkyl; X is OH or NHOH: Z is (CH2)n: and Y is S, SO or SO2. The compounds of Formulas I and III are useful for the treatment of diseases mediated by an MMP enzyme, including cancer, osteoarthritis, rheumatoid arthritis, heart failure, and inflammation.

Abstract: The invention described herein relates to a process for the preparation of (7-(3-carboxyphenyl)-4-chloroisoquinolin-1-yl)guanidine (I), intermediates thereto and new forms and formulations thereof, including the zwitterion monohydrate of (I), suitable for pharmaceutical use.

Abstract: The invention relates to a method of treating non inflammatory cartilage damage by administering a GABA analog of Formula: and pharmaceutically acceptable salts thereof.

Abstract: The present invention is directed to novel combinations of anti-epileptic compounds that demonstrate pain alleviating properties, with compounds selected from the group consisting of analgesics, N-methyl-D aspartate (NMDA) receptor antagonists and non-steroidal anti-inflammatory drugs (NSAIDS) and pharmaceutical compositions comprising same.

Abstract: Matrix metalloproteinase inhibitors are tricyclic substituted cyclic sulfonamides of the formula or a pharmaceutically acceptable salt thereof wherein R1 and R2 include hydrogen, alkyl, and substituted alkyl; R3 and R4 include hydrogen, halo, and alkyl; X is OH or NHOH, V is O, S, SO2, NR5, or CH2, R5 is a hydrogen or alkyl, and Z is (CH2)n, wherein n is an integer from 0 to 2.

Abstract: Matrix metalloproteinase inhibitors are tricyclic sulfonamides of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1 and R2 include hydrogen, alkyl, and substituted alkyl; R3 is OH or NHOH; X is O or S(O)n; n is 0, 1, or 2; p is 0, 1, 2, or 3; — is absent or a bond; and the sulfur atom bearing (O)q is bonded to the benzo ring at position a or position b.

Abstract: Metabolites of the products of formula (I) in which A and R are as defined in the description, which are phosphodiesterase 4 inhibitors.

Abstract: GABA analogs such as gabapentin and pregabalin are useful to prevent and treat inflammatory diseases.