Abstract: The present invention provides processes for the preparation of sugammadex: (I) In one aspect, there is provided a process for the preparation of sugammadex from 8-per-deoxy-8-bromo-?-cyclodextrin and 3-mercaptopropionic acid. In another aspect, there is provided an alternative process for the preparation of sugammadex from 8-per-deoxy-8-bromo-?-cyclodextrin and disodium 3 -mercaptopropionate. In another aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-?-cyclod extrin, which may be used in the production of sugammadex. In one such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-y-cyclodextrin from ?-cyclodextrin and a brominating agent. In another such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-?-cyclodextrin comprising, inter alia, reacting ?-cyclodextrin with an electrophilic brominating agent, a deoxygenating agent, and an acid in the presence of an organic solvent.

Abstract: The instant invention is related to a novel solid form of ceftolozane sulfate (the DMAc solvate of ceftolozane sulfate (Form 3)), compositions comprising ceftolozane sulfate DMAc solvate (Form 3), synthesis of Form 3 and an improved crystallization process using Form 3 to prepare ceftolozane sulfate Form 2. Novel compositions also include ceftolozane sulfate solid Form 3 and/or other crystalline and amorphous solid forms of ceftolozane.

Abstract: The instant invention is related to a novel solid form of ceftolozane sulfate (the DMAc solvate of ceftolozane sulfate (Form 3)), compositions comprising ceftolozane sulfate DMAc solvate (Form 3), synthesis of Form 3 and an improved crystallization process using Form 3 to prepare ceftolozane sulfate Form 2. Novel compositions also include ceftolozane sulfate solid Form 3 and/or other crystalline and amorphous solid forms of ceftolozane.

Abstract: The present invention provides processes for the preparation of sugammadex: (I) In one aspect, there is provided a process for the preparation of sugammadex from 8-per-deoxy-8-bromo-?-cyclodextrin and 3-mercaptopropionic acid. In another aspect, there is provided an alternative process for the preparation of sugammadex from 8-per-deoxy-8-bromo-?-cyclodextrin and disodium 3-mercaptopropionate. In another aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-?-cyclodextrin, which may be used in the production of sugammadex. In one such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-?-cyclodextrin from ?-cyclodextrin and a brominating agent. In another such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-?-cyclodextrin comprising, inter alia, reacting ?-cyclodextrin with an electrophilic brominating agent, a deoxygenating agent, and an acid in the presence of an organic solvent.

Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase, HIV replication and the treatment of human immunodeficiency virus infection in humans.

Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.

Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.

Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase, HIV replication and the treatment of human immunodeficiency virus infection in humans.

Abstract: This invention relates to deuterated compounds which are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: This invention relates to deuterated compounds which are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: The present invention is directed to processes for the preparation of 4-(3-methanesulfonyl-phenyl)-1-N-propylpiperidine (I) or a pharmaceutically acceptable salt thereof, which comprises: oxidizing a sulfide of the formula (II): with a catalytic oxidizing agent and an oxidant; to give a compound of the formula (III): followed by catalytic reduction of the compound of formula (III).

Abstract: Azo dyestuffs of the formulae: ##STR1## which are useful for reactively dyeing such cellulosic materials as cotton or cotton/polyester blends.

Abstract: Lithium salts of fiber reactive dyestuffs are stabilized in aqueous solution with N,N dialkylamine benzene sulfonic acid salt/acid buffers.

Abstract: Azo dyestuffs of the formula: ##STR1## wherein A is a phenylene or naphthalene nucleus containing at least one phosphoric or phosphonic acid group; R.sub.1 and R.sub.2 are hydrogen or --SO.sub.3 H; and R.sub.3 -R.sub.6 are hydrogen, --SO.sub.3 H, or NR.sub.7 Q wherein R.sub.7 is hydrogen or lower alkyl and Q is hydrogen or an acyl group of 2 to 8 carbon atoms, at least two of R.sub.1 -R.sub.6 being --SO.sub.3 H and at least one being --NHQ, provided that when the dyestuff is monoazo, then Q is an acyl group of 3 to 8 carbons and when the dyestuff is disazo, Q is hydrogen or an acyl group of 2 to 8 carbon atoms. The dyestuff may be used to reactively dye cellulosic materials, e.g., cotton or cotton/polyester blends. The dyestuffs are particularly useful in dyeing mixed fabrics of cellulose and synthetics together with disperse dyes from a single bath.

Abstract: Azo pyridone dyestuffs containing at least one reactive phosphoric or phosphonic acid group. The dyestuffs are characterized by the formula:A -- N .dbd. N -- Rwherein A is an aromatic radical containing at least one phosphoric or phosphonic acid group and R is a monovalent radical derived from a pyridone coupling component by removing a hydrogen atom attached to a ring carbon atom of the pyridone ring. The aromatic radical A is preferably a phenyl or naphthyl group. In addition to its phosphonic or phosphoric acid group or groups, radical A may be substituted with one or more halogen, alkyl, alkoxy, nitro, sulfonic acid or carboxylic acid groups. Cellulosic textiles, e.g., cotton or cotton/polyester blends, may be reactively dyed with these dyestuffs in an acid, neutral or alkaline bath using dicyandiamide or the equivalent. The phosphoric or phosphonic acid groups and the cellulosic material react to fix the dye through an ester linkage.