Abstract: The invention is based on the discovery of a new class of heterocyclic compounds having, for example, antibacterial properties. The D-Ala-D-Ala ligase enzyme is a critical pathway enzyme in the bacterial cell-wall synthesis. The compounds can bind to and inhibit the enzyme D-Ala-D-Ala ligase. The new compounds' activity combined with their ability to cross bacterial cell membranes makes them suitable for use as antibacterial drugs or other antibacterial applications.

Abstract: The invention relates to D-Ala-D-Ala ligase inhibitors having the formula: wherein R1 is NH2; R2 is NH2; R3 is selected from hydrogen, alkyl, amino, hydroxy, alkoxy, and alkylamino; and R4 and R4? are each independently hydrogen or a substituted or unsubstituted, linear, branched, or cyclic, alkyl, alkenyl, alkynyl, aryl, acyl, aralkyl, or alkaryl group wherein one or more carbon or hydrogen atoms may be substituted by a substituent selected from amino, alkylamino, hydroxyl, alkoxyl, thio, halogen, nitro, and carbonyl; wherein NR4R4? incorporates a substituted or unsubstituted naphthyl group, wherein the substituents are selected from alkoxy, halogen, alkyl, and alkylene, and wherein said naphthyl group in NR4R4? is bonded to N through a substituted or unsubstituted alkylene moiety. These compounds have antibacterial properties based on their ability to bind and inhibit D-Ala-D-Ala ligase, a critical pathway enzyme in bacterial cell-wall synthesis, and are suitable for various antibacterial uses.

Abstract: The invention is based on the discovery that certain small molecules can bind to the ATP binding site of D-Ala-D-Ala ligase, even in the absence of the enzyme's substrate, and can cause a conformational change in the enzyme structure similar to that which occurs upon binding of ATP and substrate to the enzyme. Without wishing to be bound by any theory, it is believed that such a conformational change is required for either activation or inhibition of the enzyme. The information obtained from this discovery has enabled identification of key interactions in the active site of the enzyme, as well as the design and opimization of inhibitors.

Abstract: The present invention relates to 14 or 15 membered macrolides substituted at the 4? position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body

Abstract: The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-?) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain.

Abstract: Disclosed are methods for modifying or regulating at least one of glucose or lipid metabolism disorders which comprises administering to a human or vertebrate subject a D1 dopamine agonist in conjunction with a dopamine D2 agonist where the conjoined administration is effective to improve at least one of the following lipid and glucose metabolic indices: body weight, body fat, plasma insulin, plasma glucose and plasma lipid, and plasma lipoprotein. In preferred embodiments, the administration of the D1 dopamine agonist and the D2 dopamine agonist is conducted at a predetermined time.

Abstract: 9a-N-[N?-(phenylsulfonyl)carbamoyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A and of 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythronolide A and their pharmaceutically acceptable addition salts with inorganic or organic acids are provided, along with a process for their preparation, pharmaceutical compositons, and use in treating bacterial infections.

Abstract: The present invention relates to an amorphous torasemide modification, to a process for preparation thereof, to its use as a raw material for the preparation of pharmaceutically acceptable salts of torasemide, to pharmaceutical forms containing the amorphous torasemide modification as well as to its use as a diuretic.

Abstract: Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A having the Formula I: 1