Abstract: The instant invention provides novel benzo?b!thiophene compounds, intermediates, compositions, pharmaceutical formulations, and methods of use for the inhibition of bone loss or bone resorption and for treatment of cardiovascular-related pathological conditions.

Abstract: A method of inhibiting melanoma comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino, or a pharmaceutically acceptable salt of solvate thereof; alone or in combination with one or more melanoma-inhibiting agents.

Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.

Abstract: A method for antagonizing or blocking calcium channels in vascular tissue, comprising administering to an animal in need thereof a pharmaceutically-effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.4 alkyl, --CO--(C.sub.1 -C.sub.6 alkyl), or --CH.sub.2 Ar, --CO--Ar, wherein Ar is phenyl or substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically-acceptable salt thereof.

Abstract: The present invention provides for a novel ICE related protease and nucleic acids coding same. The present invention also provides a method to isolate an ICE related protease and related DNA compounds encoding this protease. The present invention further comprises a method using said protease to screen for inhibitors of apoptosis. Additionally, the invention further comprises a method of using said inhibitors of apoptosis in the treatment in human patients with the acquired disease states of brain ischemia, stroke, Alzheimer's disease, amyotrophic lateral sclerosis (ALS), head trauma, or other neurodegenerative disorders.

Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.

Abstract: The present invention provides glycopeptide antibiotic derivative compounds. These derivative compounds possess antibacterial activity against a wide variety of bacteria, including activity against vancomycin-resistant isolates. Methods of making and using these glycopeptide antibiotic derivative compounds are also provided.

Abstract: The present invention is directed to an improved process for preparing in high yield an obesity protein analog using a dipeptidylaminopeptidase isolated from the slime mold, Dictyostelium discoideum.

Abstract: The invention provides dihydrobenzo?b!indenothiophene compounds, intermediates, processes, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies, and estrogen-dependent cancer.

Abstract: The present invention relates to therapeutically active heterocyclic compounds and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.

Abstract: The invention provides isolated nucleic acid compounds encoding the murD stem peptide biosynthetic gene of Streptococcus pneumoniae. Also provided are vectors and transformed heterologous host cells for expressing the MurD enzyme product and a method for identifying compounds that inhibit stem peptide biosynthesis.

Abstract: The present invention provides novel compounds, which comprise an obesity protein analog complexed with a divalent metal cation, pharmaceutical formulations thereof, and methods of using such compounds for treating obesity, and disorders associated with obesity such as diabetes, cardiovascular disease and cancer.

Abstract: The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl; R.sub.2 and R.sub.3 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl), or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogenR.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ;R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen;n is 0-4; and pharmaceutically acceptable salts and solvates thereof.

Abstract: This invention provides certain substituted 2,3-dihydrobenzofurylsulfonamide derivatives and methods for using them in the treatment of susceptible neoplasms in mammals. Also provided are certain novel pharmaceutical formulations employing these benzenesulfonamide derivatives in combination with a carrier.

Abstract: The present invention provides a method for preventing the accumulation of aberrant expression vectors during fermentation processes which rely on the expression of an expression vector coded gene for production of a polypeptide product of interest. Antibiotics are added at approximately the time at which product expression begins.

Abstract: In an injection apparatus, a guide screw shaft of a body section (20) and a screw of an operation knob (34) of a movable section (30) allow the movable section (30) to move relative to the body section (20). An ampule (7) is radially inserted into a ampule holding portion (36) of the movable section (30) and temporarily held by means of an elastic blade (36a) and at the same time, a flange (75) of the ampule (70) is inserted into a flange insertion portion (38). When the operation knob (34) is rotated, the movable section (30) moves toward the body section (20) together with the ampule (70). A guide sleeve formed in the body section (20) is inserted into a syringe (77) of the ampule (70). An operation knob (50) is rotated to set the feeding amount of a piston rod, and the operation knob (50) is pressed to perform an injection. When a release button (40) is pressed, the piston rod is returned to an initial position.

Abstract: The invention provides isolated nucleic acid compounds encoding the glycosyltransferase protein GtfD of Amycolatopsis orientalis. Also provided are vectors carrying the gtfD gene, transformed heterologous host cells for expressing the GtfD protein, and methods for producing glycopeptide compounds using the cloned gtfD gene.

Abstract: The invention provides isolated nucleic acid compounds encoding the glycosyltransferase protein GtfC of Amycolatopsis orientalis. Also provided are vectors carrying the gtfC gene, transformed heterologous host cells for expressing the GtfC protein, and methods for producing glycopeptide compounds using the cloned gtfC gene.

Abstract: The invention provides tetrahydrobenzo?a!fluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia.

Abstract: The invention provides isolated nucleic acid compounds encoding the murE stem peptide biosynthetic gene of Streptococcus pneuinoniae. Also provided are vectors and transformed heterologous host cells for expressing the murE enzyme product and a method for identifying compounds that inhibit stem peptide biosynthesis.