Abstract: A process for irreversible regio- and stereoselective enzyme catalyzed acylation of alcohols using enol esters as acylating reagents is disclosed. The present invention permits the selective modification of hydroxyl group(s) of chiral and meso alcohols, including sugars, organometallics, and glycosides. The enol freed upon transesterification rapidly tautomerizes to the corresponding volatile aldehyde or ketone thereby preventing the reverse reaction from occurring.

Abstract: Prostaglandins of the PGE type can be administered in a therapeutically effective amount to protect tissue from injury resulting from chemotherapeutic agents by administering the PGE-type prostaglandin prior to administration of the chemotherapeutic agent.

Abstract: Prostaglandins of the PGE type can be administered in a therapeutically effective amount to protect tissue from injury resulting from chemotherapeutic agents by administering the PGE-type prostaglandin prior to administration of the chemotherapeutic agent.

Abstract: The present invention relates to aldolase catalyzed stereo-selective synthesis of sugars and compositions of matter comprising arabinohexulose, xyloheptulose, threohexulose, and xylohexulose.

Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.

Abstract: A new and practical method for synthesizing heterocyclic polyhydroxylated alkaloids using enzymatic aldol condensation and catalytic intramolecular reductive amination is disclosed.

Abstract: The present invention relates to 2-deoxy-N-acetylneuraminic acid derivatives and methods for their preparation.

Abstract: This invention relates to compounds having the following formula ##STR1## or pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

Abstract: The present invention is directed to intermediates of the formula ##STR1## which are useful in a process for the preparation of aminoazanoradamanatanes.

Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositionswhich act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.

Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfonyl optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfonyl and nitro;n is 0, 1 or 2;m is 0 or 1;X is 0 or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.

Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated, conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof.

Abstract: The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.

Abstract: Novel urea compounds are provided which inhibit platelet aggregation as well as pharmaceutical compositions and methods of using said compounds.

Abstract: This invention relates to compounds having the following formula ##STR1## or pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

Abstract: This invention relates to methods of treating conditions responsive to 5-HT.sub.4 agonists and/or antagonists and 5-HT.sub.3 antagonists by administering compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfone and nitro;n is 0, 1 or 2;m is 0 or 1;X is O or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.

Abstract: The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

Abstract: An azatetracycle compound useful as 5HT.sub.3 antagonists of the general formula ##STR1## wherein D is a tetracycle of the structure ##STR2## wherein Ar is an aromatic moiety and B is either NH or O.