Abstract: A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the like; R2 and R3 represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents —CH2—, —O—, or —NH—; A represents the following group (II): [in which R7 and R8 represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; R9 and R10 represents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.

Abstract: Novel compounds, N,N′-bis(phosphonomethyl)-N,N′-bis(hydroxycarbonylmethyl)urea and N,N,N′,N′-tetrakis(hydroxycarbonylmethyl)urea, suitable for use in preparing N-acyl aminocarboxylic acids that can be readily converted to N-(phosphonomethyl)glycine are provided. The compounds may be formed by the reaction of bis-(phosophonomethyl)urea or urea respectively with carbon monoxide and formaldehyde in the presence of a carboxymethylation catalyst precursor and solvent.

Abstract: The invention provides a compound of formula (I): 1

Abstract: Compounds able to chelate bi- and trivalent paramagnetic metal ions, their chelated complexes with these metal ions and physiologically compatible salts thereof and therein magnetic resonance imaging.

Abstract: A benzamidine derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an effect of inhibiting the blood coagulation based on their excellent effect of inhibiting activated blood-coagulation factor X. Thus, a blood-coagulation inhibitor or an agent for preventing or treating thrombosis or embolism, containing one of those compounds as the active ingredient, is provided.

Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.

Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: 1

Abstract: Novel compounds, N,N′-bis(phosphonomethyl)-N,N′-bis(hydroxycarbonylmethyl)urea and N,N,N′,N′-tetrakis(hydroxycarbonylmethyl)urea, suitable for use in preparing N-acyl aminocarboxylic acids that can be readily converted to N-(phosphonomethyl)glycine are provided. The compounds may be formed by the reaction of bis-(phosophonomethyl)urea or urea respectively with carbon monoxide and formaldehyde in the presence of a carboxymethylation catalyst precursor and solvent.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: New compounds of general formulae (III), (IV) and (V).

Abstract: The present invention relates to novel geranylgeranyl derivatives and the pharmaceutically acceptable salts thereof having antiproliferative activity in eukaryotic cells with respect to the inhibition of protein geranygeranylation. The invention also relates to the pharmaceutical compositions containing the novel derivatives and to the process of preparation thereof.

Abstract: This invention provides compounds of Formula I having the structure wherein: B, C, D, and R1 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: A pharmaceutical composition is provided comprising an effective amount of a phosphoenolpyruvate compound of the formula: wherein R1 and R2 are independently H, alky, alkenyl, alkoxy (except where applied to OR1), cycloalkyl, aryl, or aralkyl and Z1 and Z2 are independently OR1, or a pharmacologically acceptable salt thereof together with a pharmaceutically acceptable carrier.

Abstract: Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.

Abstract: The present invention provides compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase. The present invention also provides pharmaceutical compositions that contain a compound that inhibits the association of platelet-derived growth factor and phosphatidylinosital 3-kinase, and methods of treating cancer, restenosis, arthritis, dermatitis, atherosclerosis, vein graft intimal hyperplasia, neointimal hyperplasia of vascular smooth muscle and psoriasis using compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase.

Abstract: Phosphonic acid agents are synthesized and characterized which are potent inhibitors of angiogenesis, tumorigenesis and metalloproteinase activity. Their method of use for the inhibition of angiogenesis and metalloproteinase and the treatment of tumors is also shown.

Abstract: A class of novel naphthyl glyoxamide compounds of formula (I) is disclosed together with a process for making the novel naphthyl glyoxamide compounds and the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds are particularly useful for systemic control of pests.

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 salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.

Abstract: The present invention provides compounds that inhibit the binding of proteins containing an SH2 domain to cognate phosphorylated proteins. The invention also provides pharmaceutical compositions containing the compounds and methods of inhibiting the binding of proteins containing an SH2 domain to cognate phosphorylated proteins.

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: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

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: Compounds of the formula ##STR1## where m and n are integers 0 to 10 and m+n equals 0 to 10, (a) X is O or S(b) Z is a covalent bond; a monocyclic or polycyclic carbocycle ring moiety; or a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N;(c) Q is covalent bond; O; or S;(d) 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 C.sub.1 -C.sub.8 alkyl;(e) R.sup.1, R.sup.2 and R.sup.5 are as defined in the claims.are useful in the treatment of calcium and phosphate elated disorders, such as arthritis and the like.

Abstract: Compounds of formula (I), ##STR1## wherein R is a biphenyl group optionally substituted, by one or more substituents, the same or different selected among halogen atoms, hydroxy groups, alkoxy, alkyl thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C.sub.1 -C.sub.3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, momo- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylamino-carbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R.sub.1 is a hydrogen atom, a straight or branched C.sub.1 -C.sub.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and n have the meanings reported in the description are described.The compounds of formula I are endowed with a dual ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Compounds of the formula I, ##STR1## in which the symbols or substituents A, B, D, D*, E and E* have the meanings given in the specification, inhibit aspartyl proteases and are suitable for controlling viral diseases.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Aminomethanephosphonic acid and aminomethylphosphinic acids are interesting as biologically active compounds or as intermediates for the preparation of biologically active compounds. According to the invention, such compounds of the formula I ##STR1## in which R.sup.1 is OH, C.sub.1 -C.sub.4 -alkyl or phenyl, can be prepared in a technically simple manner by reacting compounds of the formula II ##STR2## in which R.sup.2 is H, C.sub.1 -C.sub.6 -alkyl, benzyl, phenyl, optionally substituted by C.sub.1 -C.sub.4 -alkyl, -alkoxy and/or halogen, and R.sup.1 is as defined above, with water, at 80.degree. to 300.degree. C.

Abstract: This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.

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: Compounds and methods are disclosed that are useful in inhibiting the TNF-.alpha. converting enzyme (TACE) responsible for cleavage of TNF-.alpha. precursor to provide biologically active TNF-.alpha.. The compounds employed in the invention are peptidyl derivatives having active groups capable of inhibiting TACE such as, hydroxamates, thiols, phosphoryls and carboxyls.

Abstract: The compounds disclosed inhibit the prenylation of several proteins. These compounds are potent inhibitors of famesyl-protein transferase and geranylgeranyl-protein transferase. Further contained in this invention are chemotherapeutic compositions containing these prenyl-transferase inhibitors and methods for their production.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, and inhibition of cholesterol biosynthesis, are effected by compounds of the formula ##STR1## their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:x is --ONR.sup.1 C(O)--, --N(OR.sup.1)C(O)--, --NR.sup.1 C(O)--, --C(O)NR.sup.1 --, --NR.sup.1 S(O.sub.2)--, --C(O)O--, --OC(O)--, --C(O)--, --O--, --NR.sup.1 -- or --(S).sub.q --;Y is --CO.sub.2 R.sup.2, --SO.sub.3 R.sup.2 or --P(O) (OR.sup.2) (R.sup.3);R is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkenylene or aryl;R.sup.3 is --(O).sub.t R.sup.4 ;R.sup.1, R.sup.2 and R.sup.4 are each independently hydrogen, alkyl, aryl or aralkyl;m and n are each independently 0 or an integer from 1 to 5;p and t are each independently 0 or 1; andq is an integer from 1 to 2.

Abstract: Novel .alpha.-aminophosphonates are provided along with processes and intermediates for their preparation. In preferred embodiments, scalemic .alpha.-aminophosphonates are prepared by the stereoselective addition of phosphite salts to chiral imines.

Abstract: Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R.sub.1 and R.sub.2 form a cycloalkyl ring of 3-8 members and R.sub.3 and R.sub.4 are as defined; or R.sub.3 and R.sub.4 form a cycloalkyl ring of 3-7 members and R.sub.1 and R.sub.2 are as defined; or R.sub.1 and R.sub.2 together, and R.sub.3 and R.sub.4 together, each form a cycloalkyl ring;R.sub.5 is --OR.sub.9 or --NHR.sub.9, wherein R.sub.9 is hydrogen or alkyl;n is 0 or 1;A.sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A.sub.1 and R.sub.5 together form a radical of an .alpha.-aminoacyl derivative; andR.sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or --A.sub.2 --R.sub.

Abstract: Phosphorus containing polypeptides as renin inhibitors, useful as antihypertensive agents.

Abstract: Acylaminomethanephosphinic acids, and a process for the preparation of acylaminomethanephosphonic acids and acylaminomethylphosphinic acidsAcylaminomethanephosphonic acid and acylaminomethylphosphinic acids of the formula I,R.sup.2 --CO--NH--CH.sub.2 --P(O)(OH)R.sup.1 (I)in which R.sup.1 is hydroxyl, C.sub.1 -C.sub.4 -alkyl or phenyl and R.sup.2 is H, C.sub.1 -C.sub.6 -alkyl, benzyl or phenyl, unsubstituted or substituted by one or more radicals from the group comprising C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy and halogen, are valuable intermediates for the preparation of biologically active compounds.They can be prepared by reacting a compound of the formula IIR.sup.2 --CO--NH--CH.sub.2 --OH (II)with compounds of the formula III,H--P(O)(OH)R.sup.1 (III)in the presence of an at least equimolar amount of acetic anhydride, based on the compound of the formula II.The compounds of the formula (I) where R.sup.1 is other than hydroxyl, are novel.

Abstract: N-acyl aminomethylene phosphonates are provided having a group defined by the following general formula: ##STR1## wherein R.sub.1 is hydrogen, an aliphatic radical having 1 to 25 carbon atoms, or an aromatic radical having 6 to 25 carbon atoms; R.sub.2 is hydrogen, an aliphatic radical having 1 to 25 carbon atoms, or an aromatic radical having 6 to 25 carbon atoms; and R.sub.3 is a group remaining after reaction of a hydroxyl group-containing or epoxy group-containing polymer with an acidic hydrogen of a ##STR2## group. Also provided are waterborne coating compositions containing metallic pigments which are normally reactive with water or moisture to release hydrogen gas, stabilized against gassing by incorporation of these N-acyl aminomethylene phosphonates into the waterborne coating compositions.

Abstract: The invention relates to a process for the enantioselective preparation of L-phosphinothricin (L-Ptc) and derivatives of the formula I ##STR1## in which R.sup.1 is H, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.4)-haloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl or (subst.) phenyl-(C.sub.1 -C.sub.4)-alkyl, R.sup.2 is hydrogen, formyl, [(C.sub.1 -C.sub.6)alkyl]carbonyl, [(C.sub.1 -C.sub.6)alkoxy]carbonyl, (subst.) benzyloxycarbonyl, (C.sub.1 -C.sub.6)-alkylsulfonyl or (subst.) (C.sub.6 -C.sub.10)-arylsulfonyl, and R.sup.3 is OH, NH.sub.2 or (C.sub.1 -C.sub.6)-alkoxy, or their salts with acids or bases.

Abstract: The present invention provides magnetic recording media comprising a magnetizable layer and optionally a backside coating provided on a nonmagnetizable substrate. At least one of the magnetizable layer and the optional backside coating comprises a polymeric binder, wherein the polymeric binder is obtained from reactants comprising a free radical generator and a radiation curable polymer. The radiation curable polymer comprises a plurality of radiation curable, .alpha.

Abstract: The present invention is directed to farnesyl pyrophosphate analogs which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention, and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: Certain benzylphosphonic acid compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).

Abstract: N-acylaminomethylphosphonic acid is prepared from an N-methylolamide compound and a phosphorus trihalide. The starting compounds are mixed and heated in an aprotic solvent in the presence of water in a 0.25 to 2.5 times molar amount relative to the phosphorus trihalide at 60.degree. to 160.degree. C., and the reaction mixture is contacted with water. The N-methylolamide compound is a compound selected from the group consisting of N-methylol-lower alkylamides and N-methylolarylamides. The phosphorus trihalide is preferably phosphorus trichloride. As the aprotic solvent is used one or more of hydrocarbons, halogenated hydrocarbons, ethers, polyethers, nitriles, and aromatic nitro compounds. The mixing may be carried out at a temperature of 60.degree. C. The water present at the initiation of the reaction is in a 1.0 to 1.8 times molar amount relative to the phosphorus trihalide.

Abstract: This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.

Abstract: The present invention is concerned with aniline derivatives of the general formula: ##STR1## wherein R.sub.1 is hydrogen or a lower alkyl or aryl, R.sub.2 is hydrogen or a lower alkyl which can be substituted by hydroxyl, amino carboxyl, lower alkoxycarbonyl, lower alkanoylamide lower alkyl or aryl or by a group of the structure ##STR2## is which R.sub.5 and R.sub.6 have the meanings given hereinafter, R.sub.3 is a hydrogen or halogen atom or a carboxyl group, R.sub.4 and R'.sub.4, which can be the same or different, are hydrogen or halogen, carboxyl or lower alkoxy or lower alkyl radicals which are preferably in the m-position, R.sub.5 is hydrogen or a lower alkyl and R.sub.