Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclicring system bearing an exocyclic carbon-carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group. Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.

Abstract: The present invention relates to novel substituted acrylic acids, to methods for their preparation, compositions containing them, and their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention also relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings.

Abstract: Pyridylacetic acids of the formula I ##STR1## wherein X is NOCH.sub.3, CHOCH.sub.3 and CHCH.sub.3 ;Y is oxygen or NR.sup.a ;R is cyano, nitro, trifluoromethyl, halogen, alkyl and alkoxy;m is 0, 1 or 2;R.sup.1 is hydrogen or alkyl;R.sup.2, R.sup.3 and R.sup.4 are hydrogen, cyano, nitro, hydroxyl, amino, halogen, unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl and hetaryl, each of which is bonded directly or via --O--, --S-- or --N--,R.sup.4 is furthermore CR.sup.d .dbd.NOR.sup.e ;or a salt thereof, processes and intermediates for their preparation and their use for controlling harmful fungi or pests.

Abstract: The instant invention provides intermediates and processes for the preparation of compounds of formula IV ##STR1## wherein: n is 0, 1, or 2;R is hydrogen or C.sub.1 -C.sub.4 alkyl;X.sup.1 is hydrogen, cyano, 4-hydroxybenzoyl, 4-halobenzoyl, or 4-(C.sub.1 -C.sub.4 alkoxy)benzoyl;Y is NR.sup.4 R.sup.5, 4-hydroxyphenyl, or 4-(C.sub.1 -C.sub.4 alkoxy)phenyl;and R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.4 alkyl.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: Compounds of general Formula I ##STR1## wherein Z.sup.1 and Z.sup.2 in each case independently mean the residue--(CH.sub.2).sub.m --(C.sub.6 H.sub.4).sub.q --(O).sub.k --(CH.sub.2).sub.n --(C.sub.6 H.sub.4).sub.l --(O).sub.r --R,whereinm and n means the numbers 0-20,k, l, q and r means the numbers 0 and 1, andR means a hydrogen atom, an optionally OR.sup.1 -substituted C.sub.1 -C.sub.6 -alkyl residue, or a CH.sub.2 COOR.sup.1 group with R.sup.1 meaning it hydrogen atom, a C.sub.1 -C.sub.6 -alkyl residue, or a benzyl group,X means a hydrogen atom and/or a metal ion equivalent of an element of atomic number 21-29, 42, 44 or 57-83,with the provisos that at least two the substituents X stand for a metal ion equivalent; that one of the substituents Z.sup.1 and Z.sup.2 stands for a hydrogen and the other is not H; that--if n and l each mean the number 0--k and r do not simultaneously mean the number 1; that --(O).sub.r --R is not --OH; and that Z.sup.1 and Z.sup.2 are not --CH.sub.2 --C.sub.6 H.sub.4 --O--CH.sub.

Abstract: 5,5'-Pyrophosphates of non-naturally occurring nucleosides selected from 1-(1-thyminyl)-3-azido-2, 3-dideoxy-D-riboside, 1(5-fluoro-1-uracilyl)-2, 3-dideoxy-D-riboside, 1-(1-uracilyl)-3-azido-2, 3-dideoxy-D-riboside, 1-(9-guaninyl)-2, 3-dideoxy-D-riboside, 1-(9-hypoxanthinyl)-2, 3-dideoxy-D-riboside, 1-(1-cytosinyl)-2, 3-dideoxy-D-riboside, and 1-(9-adeninyl)-2, 3-dideoxy-D-riboside, are described as well as their manufacture and use as therapeutic agents against tumors and retroviral infections including HIV infections. The compounds may be administered as the active ingredients of pharmaceutical compositions or as prodrugs encapsulated within biological carriers, e.g. transformed erythrocytes, for targeting to specific cell populations responsible for the development of the noted pathological disorders.

Abstract: Sordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.

Abstract: A method is disclosed for improving the pharmacokinetics of a drug which is metabolized by cytochrome P450 monooxygenase.

Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: This invention relates in part to processes for producing one or more substituted or unsubstituted saturated alcohols which comprise reacting one or more substituted or unsubstituted alkadienes with carbon monoxide and hydrogen in the presence of a metal-ligand complex catalyst and a promoter and optionally free ligand to produce said one or more substituted or unsubstituted saturated alcohols. The substituted and unsubstituted saturated alcohols produced by the processes of this invention can undergo further reaction(s) to afford desired derivatives thereof. This invention also relates in part to reaction mixtures containing one or more substituted or unsubstituted saturated alcohols as principal product(s) of reaction.

Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification, have retinoid-like biological activity.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R.sup.2 is H or an optionally substituted hydrocarbon group; R.sup.3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR.sup.4, NR.sup.4, O or S in which R.sup.4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

Abstract: The invention relates to phenanthridine derivatives of the general formula I and II ##STR1## and also its salts, in which R.sub.1 means a hydrogen atom, an aromatic, carbocyclic or hetercyclic or heterocyclic residue and in which R.sub.2 and R.sub.3, which can be the same or different, mean a hydrogen atom, an alkyloxy residue, an alkylenoxy residue, a halogen atom or a nitro group.

Abstract: Synthetic methods for lactone-containing compounds such as the discodermolides are provided, as are compounds which mimic the chemical and/or biological activity thereof, and methods and intermediates useful in their preparation.

Abstract: The present invention addresses compounds which inhibit Mur D. The compounds are represented by structural formula 1: ##STR1## wherein: X represents OH, OC.sub.1-6 alkyl, O-aryl, O-Har, uridinyl, 5-iodouridinyl or O--Y.sup.+, wherein Y.sup.+ represents a charge balancing group; R.sup.1 and R.sup.2 independently represent H or C.sub.1-6 alkyl, or R.sup.1 and R.sup.2 taken together represent C.sub.1-6 alkylene unsubstituted or substituted with from 1-2 aryl or Har groups; W represents H, aryl, C.sub.1-6 alkyl or a charge balancing group; each M independently represents a member selected from the group consisting of: H, a charge balancing group and a protecting group.Salts and hydrates thereof are included.Also included are pharmaceutical compositions and methods of treatment.

Abstract: Compounds of formula (I), a method for obtaining them and pharmaceutical compositions containing them are described. The compounds are useful as human NK.sub.3 receptor antagonists.

Abstract: A process for the production of a solid dispersion of at least one therapeutic agent in a hydrophilic carrier having enhanced solubility in an aqueous media comprising dissolving at least one therapeutic agent in a volatile organic solvent containing a very hydrophilic polymer and evaporating the solvent to dryness; to form a co-precipitate of therapeutic agent and hydrophilic polymer. This invention relates to the resulting products and to their therapeutic method of use.

Abstract: Cyclobutane-1,2-dicarboxylic esters of the formula: ##STR1## in which R.sup.1 is a C.sub.1-8 -alkyl group, an optionally substituted mono- or bicyclic cycloaliphatic group having 3 to 10 ring carbon atoms, an optionally substituted aryl or arylalkyl group or an optionally substituted saturated heterocyclic group and R.sup.2 is either C.sub.1-4 -alkyl or both radicals R.sup.2 together form a group of the formula --(CH.sub.2).sub.n --(n is 2 to 4), are prepared from the corresponding maleic or fumaric esters and ketene acetals in the presence of a Lewis acid and a sterically hindered base. The reaction is stereoselective when optically active maleic or fumaric esters are employed. The cyclobutane-1,2-dicarboxylic esters (I), in particular those having trans configuration, are intermediates in the synthesis of pharmaceutically active compounds.

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.