Abstract: The present invention is concerned with a novel process for the preparation of a hydroxybenzothiophene that is an intermediate for synthesizing pharmaceutically active substances, e.g. 5- [4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-7-benzothiophenylmethyl]-2,4-thiazolidinedione and the corresponding sodium salt which are useful in the treatment of diabetes.

Abstract: In accordance with the first object of this invention soluble derivatives of sexithiophene in which terminal carbons are substituted with various polar groups such as phosphonic esters, phosphonic acids, phosphonates, carboxylic acids, carboxylates, amines, amides, carbamates, and alcohols, each separated from the terminal thiophene rings by one or more methylene groups, are synthesized. An TFT device in accordance with the second objective of this invention employs films of the above sexithiophene derivatives as the semiconducting component. These organic semiconductors are dissolved in common organic solvents and applied to the surface of a substrate using inexpensive, low-temperature solution-based processing such as spin-coating, dip-coating, drop-casting, or microcontact printing.

Abstract: A lipid compound comprising: 1

Abstract: Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-COA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to HMG-CoA reductase and the distance between ligands is at least 10 Å. The multibinding compounds of this invention are useful in the treatment and prevention of hypercholesterolemia, hyperlipidemia, atherosclerosis and the like.

Abstract: Olefin co- or homopolymers having a good molecular weight and short chain branching may be prepared in the presence of a tridentate complex of a Group 8, 9 or 10 metal.

Abstract: Novel phosphoramidate derivatives of hydroxy functional or amino functional compounds, including amino acids, peptides, peptidomimetics and nucleotide analogs, are described. The compounds enable enhanced intracellular delivery of drugs as their corresponding phosphate esters or amides. Described phosphoramidate compounds exhibit antiproliferative activity. Pharmaceutical formulations are provided for treatment of cancers.

Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The present invention relates to metabotropic glutamate receptor ligand derivatives and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders, pain, diabetic neuropathy, and prostate diseases, as well as pharmaceutical compositions comprising the same.

Abstract: Silane compounds represented by formula (1), a synthesis method thereof, luminescent device materials comprising such silane compounds, and luminescent devices containing such materials: wherein each of R1 and R2 groups represents an aryl group containing no alkenyl substituent, or a heteroaryl group containing no alkenyl substituent; each of R3, R4, R5 and R6 groups represents a hydrogen atom or a substituent group; each of R7 and R8 groups represents an aryl group or a heteroaryl group; and each of Ar1 and Ar2 groups represents an arylene group or a heteroarylene group; provided that the compound represented by the formula (1) takes neither polymeric nor oligomeric form and the case is excluded therefrom wherein all or three of R1 R2, Ar1 and Ar2 groups have heteroaryl structures.

Abstract: This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R2)W, —C(CH3)2CO2R3, 5-thiazolidine-2,4-dione, —CH(R4)CH2CO2R3, —COR3, or —PO3(R3)2; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, —CH2(1H-imidazol-4-yl), —CH2(3-1H-indolyl), —CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), —CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or —CH2(3-pyridyl); W is —CO2R3, —CONH2, —CONHOH, —CN, CONH(CH2)2CN, 5-tetrazole, or —PO3(R3)2; R3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.

Abstract: The present invention relates to a method for preparing a functional halosilanes by reacting A) a cyclic silyl ether having the formula  wherein each R is independently selected from a hydrocarbyl group or a halogen-substituted hydrocarbyl group having 1 to 20 carbon atoms, each R′ is independently selected from a group consisting of hydrogen and R and b is 3, 4 or 5; and (B) a halogen-functional compound having a formula selected from  wherein Q is a monovalent group having 2 to 20 carbon atoms selected from alkenyl groups, aralkenyl groups or a heterocyclic hydrocarbyl group having oxygen, nitrogen or sulfur hetero atoms in its ring, G is an m-valent organic group, m is at least 2, X is halogen, R″ is independently selected from hydrocarbyl groups or halogen-substituted hydrocarbyl groups having 1 to 20 carbon atoms, j is an integer having a value of 1 to 3 and k is an integer having a value of 1 to 3.

Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

Abstract: Combinatorial libraries are constructed to include aminodiol monomer subunits connected by phosphodiester, phosphorothioate, or phosphoramidate linking moieties. Combinatorial libraries of the invention feature a plurality of functional groups attached to backbone and phosphoramidate combinatorial sites.

Abstract: A process for the manufacture of bisphosphine oxide compounds and bisphosphonates as intermediates for the production of bisphosphine ligands, in which in a single step processa) a phosphine oxide compound is reacted in an organic solvent at -70.degree. C. to 20.degree. C. with 0.5-3 eq. of a lithium or magnesium amide compound,b) 0.5-3 eq. of oxidatively-acting metal salt or metal salt complex are added to the suspension obtained in stage a) in a temperature range of -70.degree. C. to 20.degree. C., with a racemate of a bisphosphine oxide compound being obtained;c) a racemate cleavage is carried out if desired; andd) the bisphosphonates obtained in stage b) or c) are converted into bisphosphine oxides.

Abstract: Diphosphines of a mixed heteroarylic-arylic type, wherein the phosphine group carrying backbone is constituted by the interconnection of a five-atom heteroaromatic ring and a carbocyclic aromatic ring, forming an atropoisomeric chiral system with a C.sub.1 symmetry. Said chiral diphosphines are advantageously used as ligands for the formation of chiral complexes with transition metals, in particular Ru, Rh, Pd, Ir, Ni. The so-obtained chiral complexes are used as chiral complexes are used as chiral catalysts for stereocontrolled reactions, in particular diastereo and enantioselective reduction reactions, hydroformylation reactions, hydrosilylation reactions, hydrocyanation reactions, double-bond isomerisation reactions, other reactions of carbon--carbon bond formation.

Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein A is hydrogen, halogen, or OH;B and D are each, independently, hydrogen, halogen, CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms, nitro, amino or OR;R is hydrogen, alkyl of 1-6 carbon atoms, --COR.sup.1, --CH.sub.2 CO.sub.2 R.sup.1, --CH(R.sup.1a)CO.sub.2 R.sup.1, or --SO.sub.2 R.sup.1 ;R.sup.1 and R.sup.1a are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms or aryl;E is S, SO, SO.sub.2, O;X is hydrogen, halogen, alkyl of 1-6 carbon atoms, CN, perfluoroalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy, arylalkoxy of 6-12 carbon atoms, nitro, amino, alkylsulfanyl of 1-6 carbon atoms, arylsulfanyl, pyridylsulfanyl, 2-N,N-dimethylaminoethylsulfanyl, or --OCH.sub.2 CO.sub.2 R.sup.1b ;R.sup.1b is hydrogen or alkyl of 1-6 carbon atoms;Y and Z are each, independently, hydrogen or OR.sup.2 ;R.sup.

Abstract: This invention provides compounds of Formula I having the structure: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, W, X, Y, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: Chiral diphosphines are constituted by an aromatic pentatomic biheterocyclic system, suitable to act as chiral ligands and complexes between the diphosphines and transition metals. They may be utilized as chiral catalysts in stereocontrolled reactions, such as diastereo- and enantioselective reduction reactions. Process is for the preparation of these chiral diphosphines; and process is for the preparation of these complexes and for their utilization as chiral catalysts in stereocontrolled reactions.

Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms;R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, --CH(R.sup.2)W, --C(CH.sub.3).sub.2 CO.sub.2 R.sup.3, 5-thiazolidine-2,4-dione, --CH(R.sup.4)CH.sub.2 CO.sub.2 R.sup.3, --COR.sup.3, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, --CH.sub.2 (1H-imidazol-4-yl), --CH.sub.2 (3-1H-indolyl), --CH.sub.2 CH.sub.2 (1,3-dioxo-1,3-dihydro-isoindol-2-yl), --CH.sub.2 CH.sub.2 (1-oxo-1,3-dihydro-isoindol-2-yl), or --CH.sub.2 (3-pyridyl);W is --CO.sub.2 R.sup.3, --CONH.sub.2, --CONHOH, --CN, CONH(CH.sub.2).sub.2 CN, 5-tetrazole, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl;R.sup.

Abstract: The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.

Abstract: The present invention relates to asymmetric syntheses and intermediates for preparing enantiomer-enriched hydroxyphosphinyl derivatives.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.

Abstract: The invention provides novel substituted dibenzothiophenes of Formulae (I), (II), (III) and (IV) which have antiangiogenic activity and further provides a method using substituted dibenzothiophenes of Formula (V) as antiangiogenic agents.

Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein: B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms;X is H, or halogen;R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, --CH(R.sup.2)W, --C(CH.sub.3).sub.2 CO.sub.2 R.sup.3, 5-thiazolidine-2,4-dione, --CH(R.sup.4)CH.sub.2 CO.sub.2 R.sup.3, --COR.sup.3, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, --CH.sub.2 (1H-imidazol-4-yl), --CH.sub.2 (3-1H-indolyl), --CH.sub.2 CH.sub.2 (1,3-dioxo-1,3-dihydro-isoindol-2-yl), --CH.sub.2 CH.sub.2 (1-oxo-1,3-dihydro-isoindol-2-yl), or --CH.sub.2 (3-pyridyl);W is --CO.sub.2 R.sup.3, --CONH.sub.2, --CONHOH, --CN, --CONH(CH.sub.2).sub.2 CN, 5-tetrazole, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl;R.sup.

Abstract: Fluorescent conjugates suitable for use in flow cytometry and other biological applications. The fluorescent conjugates comprise an antibody having a polymeric dye bound thereto. The polymeric dye is preferably enhanced by a hydrophobic and conformationally restrictive moiety either bound thereto or in close association therewith. The hydrophobic and conformationally restrictive moiety is preferably derived from a cyclodextrin. The polymeric dye comprises a polymeric entity having signal-generating groups, such as aminostyryl pyridinium dye residues attached thereto. The fluorescent conjugates exhibit exceptional stability characteristics and avoid many of the problems of energy transfer, bio-conjugability, and solubility.

Abstract: Benzyl-phosphonate compounds represented by the formula I: ##STR1## are disclosed as useful in treating bone wasting diseases and as an immunosuppresant.

Abstract: A phosphonic diester derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a cycloalkyl group; a phenyl group which may have 1 to 3 substituents selected from the group consisting of a lower alkoxy group, a lower alkyl group, a halogen atom, a halogen-substituted lower alkyl group, a lower alkanoyl group, a nitro group, a benzoyl group, a cyano group, an N-lower alkylcarbamoyl group, an N-phenyl-lower alkylcarbamoyl group, an N-(halogen-substituted phenyl)carbamoyl group and an N,N-di-lower alkylcarbamoyl group; a 1,3,4-thiadiazol-2-yl group having a halogen-substituted lower alkyl group as a substituent; a thiazolyl group; a pyridyl group which may be substituted by a halogen atom; a benzothiazol-2-yl group having 1 to 2 lower alkoxy groups on the phenyl ring; or a 4,5-dihydrothieno[3,2-e]benzothiazol-2-yl group; R.sup.2 represents a hydrogen atom or a phenyl lower alkyl group; R.sup.3 and R.sup.

Abstract: The present invention includes compositions and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include glutamate-derived hydroxyphosphinyl derivative compounds, acidic peptide analogs, phosphinic acid derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.

Abstract: A novel estrogen derivative represented by the formula: ##STR1## is useful for treating or preventing diseases caused by estrogen deficiency.

Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.

Abstract: Chiral diphosphines constituted by an aromatic pentatomic biheterocyclic system, suitable to act as chiral ligands, complexes between said diphosophines and transition metals, and their utilization as chiral catalysts in sterocontrolled reactions, such as diastereo- and enantioselective reduction reactions. Process for the preparation of said chiral diphosophines and process for the preparation of said complexes and for their utilization as chiral catalysts in sterocontrolled reactions.

Abstract: The invention is relates to a method of producing aryl-substituted, amino-acylated phosphonic-acid derivatives with the aid of metal complexes of chiral amphiphilic ligands in that according to the invention .alpha.-N-acyl-protected, .beta.-substituted alkene phosphone derivatives are asymmetrically hydrogenated in the presence of a chiral rhodium catalyst in a solvent or a suspension. The use of the micelle-forming catalyst makes possible the hydrogenation of unsaturated phosphonic-acid derivatives in water with a high reaction rate with the obtainment of very good enantiomeric excesses.

Abstract: The present invention relates to thio-substituted, nitrogen-containing heterocyclic phosphonate compounds, including bisphosphonates, phosphonoalkylphosphinates, phosphonocarboxylates, and phosphonosulfonates, and the pharmaceutically-acceptable salts and esters thereof useful for the treatment and prevention of osteoporosis and arthritis. These compounds have the general structure: ##STR1## (a) Z is a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N, at least one of which is N;(b) Q is covalent bond; O, S, N, or NR.sub.1 ;(c) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is substituted or unsubstituted C.sub.1 -C.sub.8 alkyl;(d) each R1 is independently selected from --SR.sup.6 ; --R.sup.8 SR.sup.6 ; nil; hydrogen; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl; unsubstituted or substituted aryl; hydroxy; --CO.sub.2 R.sup.3 ; --O.sub.2 CR.sup.3 ; --NR.sup.3.sub.2 ; --OR.sup.3 ; --C(O)N(R.sup.3).sub.2 ; --N(R.sup.

Abstract: A phosphorylamide derivative represented by the general formula (I): ##STR1## wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.

Abstract: The invention provides compounds which are useful as inhibitors of matrix metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are described in the claims, a stereoisomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable alkoxyamide, ester acyloxyamide, imide or derivative thereof.Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by matrix metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: The present invention includes compositions and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include glutamate-derived hydroxyphosphinyl derivative compounds, acidic peptide analogs, phosphinic acid derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia.

Abstract: Compounds of the formula ##STR1## wherein the variables are defined as in the specification, are capable of lowering introaocular pressure in the eye of a mammal.

Abstract: A novel chiral unsymmetric diphosphine compound of formula (I): ##STR1## wherein Ar.sup.1 and Ar.sup.2, which are different from each other, each represent a substituted or unsubstituted phenyl group, a substituted or unsubstituted naphthyl group, a pyridyl group, a quinolyl group, an isoquinolyl group, a furfuryl group, a benzofurfuryl group, a thienyl group, or a benzothienyl group, and a transition metal complex containing the diphosphine compound as a ligand. The complex catalyzes various asymmetric synthesis reactions, e.g., asymmetric hydrogenation or asymmetric hydrosilylation, exhibiting excellent performance in selectivity, conversion and catalytic activity, to provide a product of desired absolute configuration at high optical purity and in high yield.

Abstract: Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: ##STR1## wherein n is 0 or an integer; X is O or S, CH.sub.2, CH-halogen, CH--N.sub.3, or C.dbd.CH.sub.2 ;Q and U are independently selected from: O, S, and CH(R.sub.a) wherein R.sub.a is hydrogen, OH, halogen, N.sub.3, NH.sub.2, SH, carboxyl, C.sub.1-6 alkyl or R.sub.a is CH.sub.2 (R.sub.b) wherein R.sub.b is hydrogen, OH, SH, NH.sub.2, C.sub.1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond;Z is selected from: O, a C.sub.1-6 alkoxy, a C.sub.1-6 thioalkyl, a C.sub.1-6 aminoalkyl, (CH.sub.2).sub.m wherein m is 0 or an integer, and N(R.sub.c).sub.2 wherein both R.sub.c are independently hydrogen or a C.sub.1-6, alkyl; andR2 is a purine or pyrimidine base or an analogue or derivative thereof are disclosed. Members of this series of analogues possess anti-viral activity.

Abstract: The present invention provides novel compounds represented by the general formula I: ##STR1## wherein R.sub.1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl;R.sub.2 is hydrogen, a straight or branched lower alkyl, a cycloalkyl, or a cycloalkyl-lower alkyl;R.sub.3 and R.sub.3 ' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; orR.sub.3 and R.sub.3 ' together form a ring structure;R.sub.3 " is hydrogen, lower alkyl or an aryl; orR.sub.2 and R.sub.3 " together form a lower alkylene group --(CH.sub.2).sub.n -- wherein n is an integer of 1, 2 or 3; orR.sub.2 and R.sub.3 " together form a group represented by the formula: --(CH.sub.2).sub.p --Ar-- or --Ar--(CH.sub.2).sub.p --, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene;C(.dbd.X) is C(.dbd.

Abstract: The present invention relates to quaternary nitrogen-containing phosphate compounds, and the pharmaceutically-acceptable salts and esters thereof having the general structure: ##STR1## wherein: Z is a saturated, unsaturated, or aromatic, monocyclic or polycyclic carbocycle or monocyclic or polycyclic heterocycle containing one or more heteroatoms selected from O, S, or N;Y is N.sup.+ (R.sup.8).sub.2 or C(R.sup.1).sub.2 and when Y is C(R.sup.1).sub.2, at least one R.sup.2 must be N.sup.+ (R.sup.8).sub.3 ;R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are defined in claim 1, m and n are integers from 0 to 10; m+n is from 0 to 10;R is COOH; PO.sub.3 H.sub.2 ; SO.sub.3 H; or P(O)(OH)R.sub.4, wherein R.sub.4 is substituted or unsubstituted alkyl of 1-8 carbons atoms.The present invention further relates to pharmaceutical compostions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients.

Abstract: Ligands useful for transition metal catalyzed bond forming reactions are provided with a metal binding portion having at least one metal binding moiety ##STR1## wherein Ar and Ar' each is an aryl or a heteroaryl. These ligands may be prepared by providing an aromatic carboxylic acid having a diarylphosphino or diheteroarylphosphino substituent on the aromatic ring, and forming an ester or an amide derivative of the carboxylic acid by coupling with a chiral diol or a chiral diamine. The ligands facilitate, for example, flexible strategies for enantiocontrolled construction of five membered carbocyclic rings with varying substitution patterns and high enantioselectivity.

Abstract: Compounds of formula (I), in which X is oxygen or sulfur, R.sub.1, R.sub.2 and R.sub.3 independently of one another are a group (a), C.sub.2 -C.sub.8 alkenyl, phenyl which is unsubstituted or is substituted from one to four times with C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.6 alkylthio and/or halogen, or are naphthyl which is unsubstituted or is substituted from one to four times with C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.6 alkylthio and/or halogen, or are biphenyl which is unsubstituted or is substituted from one to four times with C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.6 -alkylthio and/or halogen, or R.sub.1, R.sub.2 and R.sub.3 independently of one another are an O-, S- or N-containing 5- or 6-membered heterocyclic ring, R.sub.1 is in addition a group of formula (II), or R.sub.1 and R.sub.2 are linked to form a ring containing 4 to 10 carbon atoms which is unsubstituted or substituted by 1 to 6 C.sub.1 -C.sub.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, are capable of lowering intraocular pressure in the eye of a mammal.

Abstract: An unsaturated phosphonic ester is produced by reaction of an acetylene compound with a secondary phosphite in the presence of a palladium complex catalyst.

Abstract: Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. This invention relates to a process of making the carboxy-peptidyl compounds of formula I.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.