Abstract: Process for preparing the L-monovaline ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process relates to an improved process whereby ganciclovir is esterified with an L-valine derivative to provide a di-valine ganciclovir intermediate. Removal of one of the valine groups with a lower alkyl amine, benzylamine or benzyl methylamine provides the mono-valine ester compound of Formula I. These products are of value as antiviral agents with improved absorption.

Abstract: A method for treating osteoporosis via administration of a compound of the formula, 1.alpha.-fluoro-25-hydroxy-16-ene-23-yne-26,27-hexafluorocholecalciferol, in an amount therapeutically effective to restore bone density to an asymptomatic level, without inducing hypercalciuria, hypercalcemia, or nephrotoxicity is provided.

Abstract: Synthetic polypeptide analogs of parathyroid hormone PTH, parathyroid hormone related peptide PTHrp, and of the physiologically active truncated homologs and analogs of PTH and PTHrp, in which amino acid residues (22-31) form an amphipathic .alpha.-helix, these residues (22-31) selected from hydrophilic amino acids (Haa) and lipophilic amino acids (Laa) ordered in the sequence:Haa (Laa Laa Haa Haa).sub.2 Laaand their pharmaceutically acceptable salts are useful for the prophylaxis and treatment of ostoporosis in mammals. Processes for the production of the polypeptides via solid phase and recombinant methods are provided.

Abstract: Synthetic polypeptide analogs of parathyroid hormone PTH, parathyroid hormone related peptide PTHrp, and of the physiologically active truncated homologs and analogs of PTH and PTHrp, in which amino acid residues (22-31) form an amphipathic .alpha.-helix, said residues (22-31) selected from hydrophilic amino acids (Haa) and lipophilic amino acids (Laa) ordered in the sequence:Haa (Laa Laa Haa Haa).sub.2 Laaand their pharmaceutically acceptable salts are useful for the prophylaxis and treatment of osteoporosis in mammals. Processes for the production of the polypeptides via solid phase and recombinant methods are provided.

Abstract: High dose, dry granulations or powder blends and aqueous oral suspensions of mycophenolate mofetil or mycophenolic acid, contain: active compound (7.5-30%), suspending/viscosity agent, sweetener, flavor, buffer (to a pH of 5-7.5), and optionally contain flavor enhancer, wetting agent, antimicrobial agent and color.

Abstract: This invention relates to a compound of the Formula I: ##STR1## as a racemic mixture and its individual enantiomers, in particular the (R)-enantiomer, and their pharmaceutically acceptable salts. These compounds are useful as sodium channel blockers, and are particularly useful for the alleviation of neuropathic pain.

Abstract: The present invention relates to novel .alpha..sub.1 -adrenoceptor antagonists of Formula I: ##STR1## in which: p is 0 or 1;t is 0, 1 or 2;X is O, S or NR.sup.6 (in which R.sup.6 is hydro or (C.sub.1-6)alkyl);Y and Z are independently CH or N;R.sup.1 is hydro, hydroxy, halo, nitro, amino, cyano, (C.sub.1-4)alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C.sub.1-6)alkyl, (C.sub.3-6)cycloalkyl, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl (C.sub.1-4)alkyl, heteroaryl (C.sub.1-4)alkyl, (C.sub.1-6)alkyloxy, (C.sub.3-6)cycloalkyloxy, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl (C.sub.1-4)alkyloxy or heteroaryl (C.sub.1-4)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms and aryl or heteroaryl is optionally substituted with one to two substituents independently selected from halo and cyano);R.sup.2 is hydro, hydroxy, halo, cyano, (C.sub.1-6)alkyl or (C.sub.

Abstract: 10,11-Methanodibenzosuberane derivatives, i.e., the compounds of Formula I: ##STR1## wherein: A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.a --CH.sub.2 --, or --CH.sub.2 --CHR.sup.a --CHR.sup.b --CH.sub.2 --, where one of R.sup.a or R.sup.b is H, OH, or lower acyloxy, and the other is H;R.sup.1 is H, F, Cl or Br;R.sup.2 is H, F, Cl or Br; andR.sup.3 is heteroaryl or phenyl optionally substuted with F, Cl, Br, CF.sub.3, CN, NO.sub.2 or OCHF.sub.2 ;and the pharmaceutically acceptable salts thereof, are useful chemosensitizing agents, e.g., for cancer chemotherapy, particularly for treating multidrug resistance.

Abstract: 10,11-Methanodibenzosuberane derivatives, i.e., the compounds of Formula I: ##STR1## wherein: A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.a --CH.sub.2 --, or --CH.sub.2 --CHR.sup.a --CHR.sup.b --CH.sub.2 --, where one of R.sup.a or R.sup.b is H, OH, or lower acyloxy, and the other is H;R.sup.1 is H, F, Cl or Br;R.sup.2 is H, F, Cl or Br; andR.sup.3 is heteroaryl or phenyl optionally substituted with F, Cl, Br, CF.sub.3, CN, NO.sub.2 or OCHF.sub.2 ;and the pharmaceutically acceptable salts thereof, are useful chemosensitizing agents, e.g., for cancer chemotherapy, particularly for treating multidrug resistance.

Abstract: The disclosed hexenoic acid side-chain derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil, including immune, inflammatory, tumor, proliferative, viral or psoriatic disorders.

Abstract: Pyrrole pyridazine and pyridazinone compounds are described. These compounds are useful as anti-inflammatory agents in the treatment of inflammation and pain. The preparation of these compounds, their pharmaceutically acceptable salts, and pharmaceutical compositions containing these compounds, is also described.

Abstract: This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4, R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.

Abstract: (S)-ibuprofen may be separated from a mixture of (S)-ibuprofen and (R)-ibuprofen in high yield and enantiomeric purity in a single resolution step using an N-alkyl-D-glucamine as the resolving agent.

Abstract: Synthetic polypeptide analogs of parathyroid hormone PTH, parathyroid hormone related peptide PTHrp, and of the physiologically active truncated homologs and analogs of PTH and PTHrp, in which amino acid residues (22-31) form an amphipathic .alpha.-helix, said residues (22-31) selected from hydrophilic amino acids (Haa) and lipophilic amino acids (Laa) ordered in the sequence:Haa(Laa Laa Haa Haa).sub.2 Laaand their pharmaceutically acceptable salts are useful for the prophylaxis and treatment of ostoporosis in mammals. Processes for the production of the polypeptides via solid phase and recombinant methods are provided.

Abstract: This invention relates to processes for preparing 2-(1-azabicyclo[2.2.2]oct-3-yl)-2,3,3a,4,5,6-tetrahydro-1H-benz[de]isoquin olin-1-one, particularly 2-(1-azabicyclo[2.2.2]oct-3S-yl)-2, 3,3aS,4,5,6-tetrahydro-1H-benz[de]isoquinolin-1-one, and to intermediates useful in such processes.

Abstract: A process for the preparation of acyclovir includes contacting an at least partially silylated guanine or mixture of at least partially silylated guanines with 1,3-dioxolane in the presence of a selective alkylation catalyst selected from the group consisting of trifluoromethanesulfonic acid, trimethylsilyl trifluoromethanesulfonate, and bistrimethylsilyl sulfonate, and hydrolyzing the product thus formed.

Abstract: The invention relates to efficient and selective processes for the synthesis of the antiviral N-9 substituted guanine compounds acyclovir and ganciclovir.

Abstract: Mycophenolate mofetil and mycophenolic acid can be conveniently manufactured into high dose oral formulations by the hot melt filling of a supercooled mycophenolate mofetil or mycophenolic acid liquid into a pharmaceutical dosage form. High dose oral pharmaceutical formulations and manufacturing methods therefor are disclosed.

Abstract: This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.

Abstract: The crystalline anhydrous salt formed by complexing mycophenolate mofetil with an anion selected from the group chloride, sulfate, phosphate and acetate (in particular the hydrochloride salt), and pharmaceutical compositions, intravenous formulations and a kit thereof, and associated methods of treatment.