Abstract: The present invention provides an aqueous tumor-targeting liposome nanoparticle composition comprising an aqueous dispersion of liposome nanoparticles. The nanoparticles preferably encapsulate an anti-cancer chemotherapeutic agent, which can be added to a pre-formed liposome composition or can be incorporated in the liposomes during the formation of the liposomes. The liposome nanoparticles comprise a legumain-targeting lipid admixed with one or more other micelle or vesicle-forming lipid materials in the form of nanoparticulate liposomes dispersed in an aqueous carrier. A preferred tumor-targeting liposome nanoparticle composition comprises (a) a legumain-targeting lipid component, (b) a zwitterionic lipid component; (c) an amino-substituted lipid component; (d) a neutral lipid component; and (e) polyethylene glycol-conjugated lipid component. The legumain-targeting lipid component comprising a hydrophobic lipid portion covalenetly attached to a legumain-binding moiety.

Abstract: Conjugates of drugs suitable for use in the treatment of inflammatory bowel disease and phospholipids, and their use in the treatment of inflammatory bowel disease, are disclosed. The disclosed conjugates serve as targeted prodrugs which are suitable for oral administration, and which are capable of releasing the drug selectively at the diseased tissue upon activation by PLA2.

Abstract: The present invention provides phosphonate compounds and methods of preparing the phosphonate compounds so as to allow, for example, increased capability to modify nanoparticles for targeted drug delivery applications.

Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is O or S; Z1 and Z2 are each independently CR9 or N; and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract: The present invention provides compositions and methods for protecting cells and tissues from damage associated with therapeutic treatments of cancers and other diseases and conditions where reactive oxygen species are produced. The present invention also provides compositions useful as research reagents.

Abstract: Novel florfenicol compounds having the chemical structure: or a pharmaceutically-acceptable salt thereof or a solvate thereof, or prodrug thereof, wherein R1 is CHCl2, CHClF, CHF2, CHBrCl, CH3, CH2N3, CH2CN, CH(R2)NH2 or CHX1X2; where R2 is H, CH3 or CH2OH, and X1 and X2 are independently selected halogens; and R3 is CH2Cl, CH2F, CHF2, CHCl2 or CH2OH are disclosed. The compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.

Abstract: The present invention relates to compounds of formula wherein the residues have various meanings and their use as pharmaceuticals.

Abstract: The invention relates to compounds having general formula I in which X represents an optically detectable moiety, n is an integer with 1?n?20, R1 is an unbranched or branched alkyl group having 1 to 20 carbon atoms, and R2 is hydrogen or —CH2—O—R3 group, wherein R3 has the same meaning as R1. These compounds are useful as inhibitors of lipolytic enzymes and can be used as tools for analysis as well as discrimination of lipolytic enzymes in biological samples.

Abstract: A phospholipid derivative represented by the following formula (I) wherein R1CO and R2CO independently represent an acyl group; R3 represents hydrogen atom, or a hydrocarbon group; symbol “a” represents an integer of 0 to 4; symbol “b” represents 0 or 1, provided that when a is 0, b is 0; X represents hydrogen atom, an alkali metal atom, an ammonium, or an organic ammonium; A1O and A3O represent an oxyalkylene group containing oxyethylene group, wherein the ratio of the oxyethylene group to the oxyalkylene group in A1O and A3O is 0.5 or larger in terms of a weight ratio; A2O represents an oxyalkylene group; symbols “m” and “q” represent an average molar number of added oxyalkylene groups; and symbol “n” represent an average molar number of added oxyalkylene groups; provided that m, n and q satisfy the following conditions: 5?m?600, 1?n?45, 0?q?200, 10?m+n+q?600, 0.04?n/(m+n+q), and q/(m+n+q)?0.

Abstract: Novel florfenicol compounds having the chemical structure: or a pharmaceutically-acceptable salt thereof or a solvate thereof, or prodrug thereof, wherein R1 is CHCl2, CHClF, CHF2, CHBrCl, CH3, CH2N3, CH2CN, CH(R2)NH2 or CH X1X2; where R2 is H, CH3 or CH2OH, and X1 and X2 are independently selected halogens; and R3 is CH2Cl, CH2F, CHF2, CHCl2 or CH2OH are disclosed. The compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.

Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpes virus, is disclosed. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative.

Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpes virus, is disclosed. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative.

Abstract: Compounds of Formula I ##STR1## are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or .alpha.-hydroxyamide group and Z is an acyl or .alpha.-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.

Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated esters and salts of inorganic or organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.

Abstract: A method of treating hepatitis virus infection is disclosed. The method comprising administering to a human subject in need of such treatment an effective hepatitis virus-combatting amount of an alkyl lipid or alkyl lipid derivative.

Abstract: A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: A method of treating hepatitis virus infection is disclosed. The method comprising administering to a human subject in need of such treatment an effective hepatitis virus-combatting amount of an alkyl lipid or alkyl lipid derivative.

Abstract: An improved process for producing ethylenically unsaturated phosphate ester compounds, especially 2-(methacryloyloxyethyl)-2' (trimethylammoniomethyl) phosphate, (HEMA-PC) comprises a two step reaction in the first of which a phospholane reagent is reacted with a hydroxyl containing ethylenically unsaturated starting material, and in the second of which the intermediate formed in the first step is ring opened by reaction with trimethylamine to produce a zwitterionic product. In the process the two steps of the reaction are carried out in the same solvent with substantially no removal or addition of solvent after the first step. The solvent is preferably acetonitrile. The use of pure reagents avoids the production of undesirable by-products. The product is suitable for polymerising, for instance to provide cross-linked hydrogel copolymers used in ophthalmic applications.

Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.

Abstract: The present invention is directed to novel phosphorous-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

Abstract: Phosphoric diesters having formula (1): ##STR1## wherein R.sup.1 is an acyl group having at least one phenyl group; R.sup.2 is a C.sub.2-12 linear or branched alkylene group which may optionally be inserted with an oxygen atom between carbon atoms thereof; L is a C.sub.2-40 linear or branched alkyl group which may optionally be inserted with an oxygen atom between carbon atoms thereof or the group R.sup.1 -O-R.sup.2 ; M is a hydrogen atom, an alkali metal ion, a metal ion of di- or higher valence, an ammonium group, an alkanolammonium group having 2 to 14 carbon atoms, C.sub.1-14 alkylammonium group; and n is the valence of M are useful UV absorbing compounds. The phosphoric diesters remain on the skin for long periods of time and exhibit lasting UV shielding effects. The compounds and the cosmetic compositions containing the compounds are very safe to the skin.

Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##

Abstract: Compounds of the general formula: ##STR1## are useful as surfactants in the preparation of fluorocarbon emulsions, which can be used as oxygen-carrying blood substitutes, and for many other therapeutic and diagnostic applications. They are further useful in liposomal formulations which are themselves therapeutic agents or provide a vehicle for such agents.

Abstract: An efficient, technically straightforward and inexpensive process for generating conjugates of phospholipids with biologically important molecules is described.

Abstract: Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.

Abstract: The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.

Abstract: New phosphonic acid derivatives are described which display antibacterial activity.

Abstract: A monophosphorylated L-dopa ester of formula ##STR1## (wherein the asterisk, R, R.sub.1, R.sub.2 and R.sub.3 have the meanings shown in the description),salts thereof with pharmaceutically acceptable acids or bases, a process for the preparation thereof and a pharmaceutical composition containing said compound or a salt thereof are described.The compound of formula I and the salts thereof are useful in the treatment of Parkinson's disease, renal failure, heart failure and hypertension.

Abstract: New phosphonic acid derivatives are described which display antibacterial activity.

Abstract: The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.

Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.

Abstract: A process for producing a phosphinylamino acid derivative of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, R.sup.2 is a hydrogen atom, a lower alkyl group, a halo-lower alkyl group or a substituted or unsubstituted phenyl group, and R.sup.3 is a substituted or unsubstituted alkyl group or a substituted or unsubstituted phenyl group, which comprises reacting a compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, and/or a compound of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are as defined above, with a compound of the formula:R.sup.3 CONH.sub.2 (IV)wherein R.sup.3 is as defined above, carbon monoxide and hydrogen in the presence of a catalyst containing a metal of group VIII of the Periodic Table.

Abstract: Acidic liquids, such as galvanic electrolyte solutions for metal electroplating, contain a surfactant and a foam inhibiting agent which is a perfluoroalkyl-containing ester of phosphoric acid.

Abstract: Herbicidal compounds of formula: ##STR1## in which R.sup.1 denotes an optionally halogenated alkyl radical containing from 1 to 4 carbon atoms,R denotes the hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms,R.sup.2 denotes the hydrogen atom or R.sup.21,R.sup.21 and R.sup.3 denotes optionally substituted aryl radicals,R.sup.4 denotes a hydrogen atom or a hydrogenolysable group R.sup.8,and the agriculturally acceptable salts of these compounds.

Abstract: Described are phosphatidyl compounds of the formula I ##STR1## in which R.sup.1 represents C.sub.3-14 -alkanoyl, benzoyl, the acyl radical of an .alpha.-aminocarboxylic acid that is other than glycine, L-alanine and derivatives thereof having a substituted amino group, and of which the .alpha.-amino group may be substituted by lower alkanoyl, lower alkoxycarbonyl or by benzyloxycarbonyl, or the acyl radical of a .beta.-aminocarboxylic acid or an .alpha.- or .beta.-hydroxycarboxylic acid,T represents a group NH that is unsubstituted or is substituted by lower alkyl, or oxygen,Y represents dimethylene that is unsubstituted or is substituted by free, etherified or amidated carboxy,W represents hydrogen, andZ represents a 1,2-dihydroxyethyl, 2-hydroxyethyl or hydroxymethyl group, in which at least one of the hydroxy groups is esterified by an aliphatic C.sub.8-30 -carboxylic acid or is etherified by an aliphaticC.sub.

Abstract: Process for the preparation of L-homoalanin-4-yl(methyl)-phosphinic acid (esters) of the formula I ##STR1## (R, R.sub.1 =H, alkyl) or salts thereof by reacting an R-3-isopropyl-2,5-dialkoxy-3,6-dihydropyrazine of the formula II with a .beta.-halogenoethyl(methyl)phosphinic acid ester of the formula IV ##STR2## (R', R.sub.1 '=alkyl) to give compounds of the formula V ##STR3## and then subjecting the latter to hydrolytic cleavage.

Abstract: A phenoxyalkanoylaminomethylphosphonic acid represented by the following formula (I) ##STR1## wherein X and Y are identical or different and each represents a hydrogen atom, a halogen atom, CF.sub.3 or an alkyl group having not more than 5 carbon atoms, Z represents CH or N, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and each represents a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms. The compound is useful, as a herbicide, for eradicating weeds, especially narrow-leaved weeds.

Abstract: Preparation of intermediates for herbicides of formula ##STR1## by the reaction of organic phosphites with benzoxazines of formulaBzx--CH.sub.2 --CO--Y (II)in whichBzx denotes the radical of formula: ##STR2## X is a usual substituent of phenols n is an integer from 0 to 4R.sup.1 and R.sup.2 are H or such that OR.sup.1 and OR.sup.2 are hydrolyzableY is --OM or --NR.sup.3 R.sup.4M is H or is such that COOM is a salt or an esterR.sup.3 and R.sup.4 are H or a hydrocarbon radical, and one of them can be R.sup.5 --SO.sub.2 --, andR.sup.5 is a hydrocarbon radical, substiuted if appropriate. Products obtained by the process and their use as herbicides.

Abstract: Herbidical compounds of the formula: ##STR1## in which R.sup.1 denotes an optionally substituted hydrocarbon radical, R denotes the hydrogen atom or has one of the meanings given for R.sup.1 ; R.sup.2 and R.sup.3 denote the hydrogen atom or are such that OR.sup.2 and OR.sup.3 are hydrolyzable groups; R.sup.4 denotes a hydrogen atom or a hydrogenolyzable group, and the agriculturally acceptable salts of these compounds.

Abstract: This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.

Abstract: Novel compounds having the formula ##STR1## wherein R is lower alkyl having 1 to 6 carbon atoms, have shown utility as insecticides and miticides.

Abstract: Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: Compounds having the formula ##STR1## in which R is hydrogen, cyano or --COOR.sub.2 ; R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and Z is ##STR2## in which A is halogen, B is halogen or hydrogen and Y is nitrogen or --CH--, are herbicides.

Abstract: The invention is related to 1-O-alkyl-3-amino-propan-1.

Abstract: When applied as safeners, the haloacylaminoalkylphosphinates, haloacylaminoalkylphosphinates and haloacylaminoalkylphosphine oxides of the formula I below are able to protect cultivated plants from the phytotoxic effects of herbicides. Suitable crops are preferably sorghum, cereals, rice, maize and soya beans and the herbicides employed are chloroacetanilides and thiocarbamates.The haloacylaminoalkylphosphonates, haloacylaminoalkylphosphinates and haloacylaminoalkylphosphine oxides have the formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyloxy, C.sub.2 -C.sub.4 alkynyloxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.8 alkoxyalkoxy or C.sub.1 -C.sub.4 cyanoalkoxy,R.sub.2 is hydrogen or a substituent as defined for R.sub.1,R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or one of R.sub.3 and R.sub.4 is also a radical ##STR2## or both taken together with the carbon atom to which they are attached are also a C.sub.3 -C.sub.