Abstract: An implantable endoluminal device which is fabricated from materials which present a blood or body fluid and tissue contact surface which has controlled heterogeneities in material constitution. An endoluminal stent which is made of a material having controlled heterogeneities in the stent material along the blood flow surface of the stent and the method of fabricating the stent using vacuum deposition methods.

Abstract: Compounds having the formula are .alpha..sub.1 adrenoreceptor antagonists. Processes for making these compounds, synthetic intermediates employed in these processes and a method for inhibiting .alpha..sub.1 adrenoreceptors and treating benign prostatic hyperplasia (also called benign prostatic hypertrophy or BPH) and other urological diseases such as BOO (bladder outlet obstruction), neurogenic bladder and gynecological syndromes such as dysmenorrhea are disclosed.

Abstract: The present invention provides a process of designing compounds which bind to a specific target molecule. The process includes the steps of a) identifying a first ligand to the target molecule using two-dimensional .sup.15 N/.sup.1 H NMR correlation spectroscopy; b) identifying a second ligand to the target molecule using two-dimensional .sup.15 N/.sup.1 H NMR correlation spectroscopy; c) forming a ternary complex by binding the first and second ligands to the target molecule; d) determining the three dimensional structure of the ternary complex and thus the spatial orientation of the first and second ligands on the target molecule; and e) linking the first and second ligands to form the drug, wherein the spatial orientation of step (d) is maintained.

Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; A is selected from (a) optionally substituted alkylene, (b) optionally substituted cycloalkylene, (c) optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, (d) optionally substituted alkenylene and (e) ##STR2## X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from --OR.sup.4, --NR.sup.6 R.sup.7, and a pharmaceutically acceptable metabolically cleavable group, (c) --OR.sup.2, (d) tetrazolyl, (e) --CH(OR.sup.2)--CH.sub.2 OR.sup.8, (f) --CH(OR.sup.2)--CH.sub.2 --CH.sub.2 OR.sup.8, (g) --CH(OR.sup.2)--CH(OR.sup.8)--CH.sub.2 OR.sup.9, and (h).dbd.N--OR.sup.2 ; and R.sup.

Abstract: The present invention provides a process for identifying compounds which bind to a specific target molecule. The process includes the steps of a) generating a first two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of a .sup.15 N-labeled target molecule; b) exposing the labeled target molecule to one or a mixture of chemical compounds; c) generating a second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of the labeled target molecule that has been exposed to one or a mixture of compounds in step (b); and d) comparing said first and second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectra to determine differences between said first and said second spectra, the differences identifying the presence of one or more compounds that are ligands which have bound to the target molecule.

Abstract: Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d)--NR.sup.6 SO.sub.2 R.sup.

Abstract: Compounds having the formula: ##STR1## wherein W.sup.1 and W.sup.2 are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted naphthyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is selected from thienyl, furyl, phenyl, naphthyl, benzo?b!thienyl, alkyl, hydroxyl, and hydrogen; Y an alkylene of one to six carbon atoms; and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.4, (c) --NR.sup.5 R.sup.6, (d)--NR.sup.4 SO.sub.2 R.sup.7 (e)--NH--Tetrazolyl, and (f) glycinyl; inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.

Abstract: The present invention provides a compound of the formula: ##STR1## Such compounds are useful for inhibiting prostaglandin synthesis. Pharmaceutical compositions and methods for inhibiting prostaglandin synthesis are also disclosed.

Abstract: The present invention provides a class of substituted indole and indene iminoxy derivatives of the formula ##STR1## which inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.

Abstract: Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.

Abstract: 7a-Substituted hexahydro-1H-pyrrolizine compounds having the formula ##STR1## wherein A is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to selectively control synaptic transmission in mammals.

Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from the group consisting of optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are one or more groups independently selected from hydrogen, alkyl, halolalkyl, alkoxy, and halogen; Z is selected from the group consisting of N--OH, N--O--A--COM, CH--COM, and CH--CH.dbd.N--0--A--COM wherein A is selected from the group consisting of alkylene, alkenylene, cycloalkylene, and optionally substituted alkylphenyl wherein the alkyl portion is of one to six carbon atoms, and M is selected from the group consisting of a pharmaceutically acceptable, metabolically clearable group, --OR.sup.3, and --NR.sup.4 R.sup.

Abstract: The present invention provides a process for the preparation of a compound of formula ##STR1## wherein R is a straight or branched alkyl group of from one to twelve carbon atoms; M represents hydrogen or a pharmaceutically acceptable cation; and A is selected from optionally substituted carbocyclic phenyl.

Abstract: The present invention provides a process for identifying compounds which bind to a specific target molecule. The process includes the steps of a) generating a first two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of a .sup.15 N-labeled target molecule; b) exposing the labeled target molecule to one or a mixture of chemical compounds; c) generating a second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectrum of the labeled target molecule that has been exposed to one or a mixture of compounds in step (b); and d) comparing said first and second two-dimensional .sup.15 N/.sup.1 H NMR correlation spectra to determine differences between said first and said second spectra, the differences identifying the presence of one or more compounds that are ligands which have bound to the target molecule.