Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: Drug and multidrug resistant modulators of the formula: ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or halo; A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.4 --CH.sub.2 --, or --CH.sub.2 --CHR.sup.5 --CHR.sup.6 --CH.sub.2 --, where R.sup.4 is --H, --OH, or acyloxy; one of R.sup.5 or R.sup.6 is --H, --OH, or acyloxy, and the other is --H; R.sup.3 is a polyaryl; and pharmaceutically acceptable salts and solvates thereof, are described and claimed. Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed. Also, methods of enhancing oral bioavailability of a drug and methods of enhancing bioavailability of a drug to the brain using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed.

Abstract: An improved method for the treatment of central nervous system disorders comprises treating patients with an enteric fluoxetine formulation.

Abstract: This invention provides a process for preparing a compound of formula III ##STR1## wherein R.sup.1 is bromo, iodo or COOR.sup.2 ;R.sup.2 is H, C.sub.1 -C.sub.4 alkyl, phenyl which may be substituted or benzyl; andA is a 5- or 6-membered aromatic residue which may contain up to three hetero atoms and which may optionally be substituted with one or two groups selected from the group consisting of halo, hydroxy, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy; or a salt thereof, which comprises(a) reacting a compound of formula I ##STR2## wherein R is C.sub.1 -C.sub.4 alkyl or phenyl which may be substituted; andR.sup.1, R.sup.2, and A are as defined above;or a salt thereof, with a sulfurization agent;(b) cyclizing the reaction product from step (a) with guanidine; and(c) optionally salifying the reaction product from step (b).

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: A superior enteric formulation of the antidepressant drug, fluoxetine, is in the form of enteric pellets of which the enteric layer comprises hydroxypropylmethylcellulose acetate succinate.

Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: Drug and multidrug resistant modulators of Formula (C): ##STR1## where Z is selected from the group consisting of --S--, --S(O).sub.w --, and --CH.sub.2 --, where w is 1 or 2; and pharmaceutically acceptable salts or solvates thereof are described and claimed.Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound of this invention are described and claimed. Also, methods of enhancing oral bioavailability of a drug and methods of enhancing bioavailability of a drug to the brain using a compound of this invention are described and claimed.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Processes for preparing 5-substituted pyrrolo[2,3-d]pyrimidines which are useful as intermediates for the preparation of pyrrolo[2,3-d]pyrimidine antineoplastic agents or as antineoplastic agents themselves are provided.

Abstract: A stereoselective glycosylation process for preparing beta-anomer enriched 2'-deoxy-2',2'-difluoropyrimidine nucleosides and 2'-deoxy-2'-fluoropyrimidine nucleosides which involves reacting an alpha-anomer enriched 2-deoxy-2,2-difluorocarbohydrate or 2-deoxy-2-fluorocarbohydrate with at least a molar equivalent of a pyrimidine nucleobase derivative in a low freezing inert solvent.

Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.

Abstract: A process for the preparation of 1-(2'-deoxy-2',2'-difluoro-D-ribo-pentofuranosyl)-cytosine (VI) from 2-deoxy-2,2-difluoro-.beta.-D-ribo-pentopyranose (I). The process uses a tritylation reaction (Step 3) for preparing 2-deoxy-2,2-difluoro-5-O-triphenylmethyl-ribo-pentofuranose (II) as a key intermediate. The 1-(2'-deoxy-2',2'-difluoro-D-ribo-pentofuranosyl)-cytosine (VI) is an antiviral and anti-cancer agent.

Abstract: This invention provides a method of reversing multidrug resistance in a multidrug resistance tumor comprising administering a multidrug resistance reversing amount of any of a series of phenoxy compounds as defined herein.

Abstract: Provided are methods for treating hyperglycemia and Alzheimer's disease utilizing certain rhodanine derivatives. Certain of the rhodanine derivatives utilized in the instant methods are novel and, accordingly, such compounds and pharmaceutical formulations thereof are also provided.

Abstract: This invention provides novel 1-alkylsulfonyl-2,2-difluoro-3-carbamoyl ribose intermediates and intermediate nucleosides derived therefrom. The compounds are particularly useful in the preparation of 2'-deoxy-2',2'-difluoro-beta-cytidine and other beta anomer nucleosides which are antiviral and anticancer agents.