The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.

Described herein are compounds of the formulae (I), (Ia), (Ib), and (II) and pharmaceutically acceptable salts, isomers, mixture of isomers, crystalline forms, non-crystalline forms, hydrates, or solvates thereof, as well as methods of making and using compounds of the formulae (I), (Ia), (Ib), and (II) to, among other things, treat HIV/AIDS.

Described herein are compounds of the formulae (I), (Ia), (Ib), and (II) and pharmaceutically acceptable salts, isomers, mixture of isomers, crystalline forms, non-crystalline forms, hydrates, or solvates thereof, as well as methods of making and using compounds of the formulae (I), (Ia), (Ib), and (II) to, among other things, treat HIV/AIDS.

The aspects of the disclosed embodiments are directed to novel compounds, specifically, quaternary ammonium derivatives of tertiary amine containing opioid drug compounds such as hydrocodone, hydromorphone and oxycodone, formulations containing said. compounds or pharmaceutically acceptable salts thereof, which are capable of providing controlled release of the opioid drug upon administration to a patient in order to treat pain.

A compound having the general structure shown in Formula I: ##STR00001##
or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK.sub.1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.

The present invention provides a new forms of (R)-N-methylnaltrexone, and compositions thereof, useful as a peripheral mu opioid receptor antagonist.

This invention is directed to photoluminescent compounds based on rhodamine dyes with red-shifted absorption and emission maxima and uses thereof for photoluminescence based devices.

The subject of the present invention are water-soluble derivatives of camptothecin, their synthesis and use. These compounds exhibit preferable biological properties for use in anti-neoplasm therapy.

A process for preparation of (2S,5R)-7-oxo-6-sulphooxy-2-[((3R)-piperidine-3-carbonyl)-hydrazino carbonyl]-1,6-diaza-bicyclo[3.2.1]octane of Formula (I) is disclosed which is comprising reacting a compound of Formula (II) with a compound of Formula (III) to obtain a compound of Formula (IV). Crystalline compounds of Formula (I) are claimed. ##STR00001##

The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) ##STR00001##
wherein a, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.