Abstract: The present invention relates to compounds of formula I and to compounds of formula II wherein the substituents have various meanings. These compounds are useful as beta lactamase inhibitors.

Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides novel 1,4-benzodiazepine-2,5-dione compounds, and methods of using novel 1,4-benzodiazepine-2,5-dione compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.

Abstract: An object of the present invention is to provide a carbapenem synthetic intermediate which is advantageous in an industrial process. There are provided a process for producing Compound (I), or a pharmaceutically acceptable salt, or a solvate, or a crystal thereof, comprising reacting Compound (III) and Compound (IV) in the presence of the secondary amine, and a benzyl alcoholated crystal of Compound (I). There are further provided a method of deprotecting Compound (I) with a Pd catalyst, and a crystal of Compound (IV).

Abstract: A compound of the structure ##STR1## or a 31- and/or 42-ester or ether thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Abstract: The present invention provides a compound of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, optionally substituted; acylamino, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkoxy, C.sub.1-6 alkanoyloxy, C.sub.1-6 alkylamino, di-(C.sub.1-6 alkyl)amino, C.sub.1-6 alkoxycarbonyl, aminocarbonyl, C.sub.1-6 alkylaminocarbonyl or di-(C.sub.1-6 alkyl)aminocarbonyl;R.sup.2 is hydrogen or C.sub.1-6 alkoxy; orR.sup.1 and R.sup.2 together form optionally substituted C.sub.1-6 alkylene;R.sup.3 and R.sup.5 are independently hydrogen or C.sub.1-6 alkyl; andone of R.sup.4 and R.sup.6 is hydrogen or C.sub.1-4 alkyl and the other is selected from a number of groups or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.Processes of their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.

Abstract: Disclosed is a process for preparing a .beta.-lactam compound represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy-substituted lower alkyl group or an amino group each of which may be protected; R.sup.2 represents hydrogen atom or an ester residue; X represents a methylene group which may be substituted by a lower alkyl group, sulfur atom or a group represented by the formula: --A--CH.sub.2 -- where A represents sulfur atom, oxygen atom or methylene group; and W represents an active ester residue of hydroxyl group,or a salt thereof, which comprises the steps of treating a 1-aza-3-thia-bicycloalkane compound represented by the formula: ##STR2## wherein R.sup.1, R.sup.2 and X have the same meanings as defined above, or a salt thereof with a base in the presence of a desulfurizing agent and then reacting the resulting compound with an active esterifying agent of hydroxyl group.

Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.