Abstract: The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a compound selected from a dihydroxy open acid statin and a pharmaceutically acceptable salt or ester thereof in a delayed-release pharmaceutical dosage form to a patient in need of such treatment wherein substantial release of the compound from the dosage form is delayed until after passage of the dosage form through the stomach.

Abstract: The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a crystalline hydrated form of the calcium salt of dihydroxy open acid simvastatin to a patient in need of such treatment. Methods for making the calcium salt of dihydroxy open acid simvastatin are also provided.

Abstract: The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a compound selected from a dihydroxy open acid statin and a pharmaceutically acceptable salt or ester thereof in a delayed-release pharmaceutical dosage form to a patient in need of such treatment wherein substantial release of the compound from the dosage form is delayed until after passage of the dosage form through the stomach.

Abstract: This invention encompasses a novel process for synthesizing compounds represented by formula A: These compounds are intermediates useful in the preparation of certain agents that are selective COX-2 inhibitors.

Abstract: A rearrangement process for the preparation of a 6,5,5-tricyclic, a 6,6,5-tricyclic and 6,5,5,7-tetracyclic ring system is disclosed.

Abstract: An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.

Abstract: A method of preparing intermediates for carbapenem antibiotics characterized by treating a N-deprotected acetoxy conpound of the formula: ##STR1## in the presence of a Lewis acid or a silylating agent to yeild an intermediate; and cyclizing the intermediate in the presence of rhodium (II) acetate to form a bicyclic ketoester.

Abstract: A process for enhancing the purity of 2R-?1-hydroxy-1-trifluoromethyl-3-cyclopropylpropyn-2-yl!-4-chloroaniline comprising the formation of an acid addition salt which is capable of rejecting the racemate in the selected organic solvent.

Abstract: An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl- 1,4-dihydro-2H-3, 1-benzoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.

Abstract: An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.

Abstract: A process for the manufacture of oxytocin receptor antagonists of the following formula (I) ##STR1## and their crystalline salts is disclosed.

Abstract: An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.

Abstract: The present invention is directed to a compound represented by the structural formula: ##STR1## wherein Z-- represents a negatively charged counterion.

Abstract: A chiral resolution process is described for the purification of a substituted chiral quinazoline, by salt formation with a resolving agent, followed by crystallization.

Abstract: The present invention is directed to a process of making 2-aryl carbapenems of formula 1 from a compound of formula A.

Abstract: An asymmetric synthesis of (S)-(-)-6-chloro-4-cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1H)-qu inazolinone comprises the chiral addition of 2-pyridylacetylide to N.sup.1 -protected 6-chloro-4-cyclopropyl-2-quinazolinone followed by removal of the protecting group.

Abstract: Described is a process for converting an alcohol to an azide with S.sub.N 2 inversion using a phosphoryl azide, e.g. diphenylphosphoryl azide (DPPA). Good yields of azide in high enantiomeric excess can be achieved specifically for benzylic alcohols and alpha-hydroxy alkyl esters. The process is carried at preferably room temperature in an inert dry aprotic solvent, e.g. toluene, and in the presence of a proton acceptor, e.g. 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) to afford high yields of high enantiomeric purities.

Abstract: 5,6-Dihydro-4-(R-amino)-4H-thieno[2,3-b]-thiopyran-2-sulfonamide-7,7-dioxid e is a potent carbonic anhydrase inhibitor useful in the treatment of ocular hypertension and glaucoma. The S-(+)-enantiomer of that compound, the more active enantiomer, is prepared by a process involving an intermediate step of an enantioselective reduction of a carbonyl group employing an oxazaborolidine chiral catalyst.

Abstract: A process is disclosed for obtaining manipulated proportions of the (+) and (-) enantiomers of [(6,7-dichloro-2,3-dihydro-2-methyl-1-oxo-2-phenyl-1H-inden-5-yl)oxy]aceti c acid by asymmetric chiral phase transfer catalysis.

Abstract: Disclosed is a process for preparing the R and S enantiomers of a compound of the formula; ##STR1## which comprises; (1) reacting an enzyme with a prochiral diester of the formula ##STR2## where M.sup.1 and M.sup.2 are the same, to produce a chiral monoester of the compound of formula II;(2) treating the chiral monoester product of step (1) with an amine and a trialkyl aluminum compound to produce the R enantiomer of the compound of formula I; or reacting the chiral monoester product of step (1) with an acid activating agent, an amine, and a base to produce the S enantiomer of the compound of formula I.