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: N-acylaminomethylphosphonic acids having the formula RCO--NH--CH.sub.2 --P(.dbd.O)(OH).sub.2, where R is a non-interfering organic radical, are prepared by (A) combining a solution of a carboxamide, RCO--NH.sub.2, paraformaldehyde and phosphorous acid in an anhydrous solvent with a carboxylic acid anhydride, e.g., acetic anhydride, or (B) combining a solution of the carboxamide and paraformaldehyde in an anhydrous solvent with a solution of the carboxylic acid anhydrid and phosphorous acid in an anhydrous solvent, followed by heating the resulting solution to complete the reaction. The N-acylaminomethylphosphonic acids can be hydrolyzed to aminomethylphosphonic acid.

Abstract: Novel phosphorus containing compounds are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.

Abstract: The present invention is novel substituted .alpha.-amino acids, pharmaceutical compositions, method of use, and preparations therefore having utility for treating disorders which benefit from blockade of aspartate and glutamate receptors.

Abstract: The invention discloses certain substituted .alpha.-aminoacids having the formula ##STR1## where m and n are 1 or 2, and R, R.sub.1, R.sub.2, R.sub.3 and Y have various significances, which compounds are useful in treating epilepsy, disorders associated with excess GH or LH secretion, anxiety, schizophrenia, depression, CNS degenerative disorders, cerebral hypoxic conditions and stress-related psychiatric disorders.

Abstract: Acylaminomethanephosphonic acids are useful intermediates for the preparation of the herbicide N-phosphonemethylglycine and its salts.According to the invention, acylaminomethanephosphonic acids of the formula (I)R.sup.1 --CO--NHCH.sub.2 P(.dbd.O) (OH).sub.2 (I)in which R.sup.1 is H, C.sub.1 -C.sub.6 -alkyl, benzyl or optionally substituted phenyl, can be prepared in a process which can be employed industrially, which comprises the reaction of the compound of the formula R.sup.1 --CO-NH--CH.sub.2 OH with P.sub.2 O.sub.3 and then hydrolysis with water.

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: Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical compounds are z-2-acylamino-3-monosubstituted propenoates.

Abstract: Dipeptide mimics which contain phosphorus and their pharmaceutical use and preparation are disclosed. The compounds have dehydropeptidase (DHP) enzyme inhibitor activity.

Abstract: New polyimides have been prepared from the reaction of aromatic dianhydrides with novel aromatic diamines containing carbonyl and ether connecting groups between the aromatic rings. Several of these polyimides were shown to be semi-crystalline as evidenced by wide angle x-ray diffraction and differential scanning calorimetry. Most of the polyimides form tough solvent resistant films with high tensile properties. Several of these materials can be thermally processed to form solvent and base resistant moldings.

Abstract: The invention relates to rhodium complexes of the formula[A--O--(CH.sub.2 CH.sub.2 O).sub.n --A].sup.2+ 2X.sup.- (Ia)and[A--O--(CH.sub.2 CH.sub.2 O).sub.m --CH.sub.3 ].sup.+ X.sup.-(Ib)in whichn=5-1,000,m=5-250,X.sup.- denotes a tetrafluoroborate, hexafluorophosphate or per-chlorate anion,A denotes a radical of the formula ##STR1## (en).sub.2 denotes two molecules of a monoolefin or one molecule of a diolefinAr denotes phenyl or phenyl which is substituted by one or two alkyl groups having 1 or 2 carbon atoms andR.sup.1 denotes an arylene or alkylene bridge,and their use for the preparation of L-phosphinothricin and its derivatives by enantioselective catalytic hydrogenation of 2,3-dehydrophosphinothricin (derivatives).

Abstract: The invention relates to compounds of formula: ##STR1## in which R.sup.4 is a group which can be hydrogenolyzed, R and R.sup.1 are alkyl groups, X.sup.- is an HSO.sub.4.sup.-, Cl.sup.- or R.sup.7 SO.sub.3.sup.- anion and to a process for the preparation of the compounds of formula (I) by the hydrolysis of the compounds of formula (II): ##STR2## in which R.sup.2 and R.sup.3 are alkyl groups linked to the oxygen via a secondary carbon, using sulphuric or hydrochloric acid. The invention also relates to the use of compounds of formula (I) for the preparation of herbicide by the hydrogenolysis of the compounds of formula (I).

Abstract: N-Acyl-aminomethylphosphonic acids represented by the formula ##STR1## wherein R is selected from the group consisting of methyl and aryl are prepared by:(a) bringing together under substantially anhydrous reaction conditions an amide represented by the formula ##STR2## wherein R is as defined above and paraformaldehyde; and thereafter, (b) adding phosphorous trihalide to the reaction mixture.

Abstract: Disclosed are some new aminoethylphosphinic acid derivatives useful as antibacterial agents.

Abstract: A method is disclosed for the sulfurization of a phosphorus containing compound, which comprises: solubilizing the phosphorous containing compound and then contacting the phosphorous containing compound, with a sulfur containing compound of the solution formula: ##STR1## wherein, B is selected from the group consisting of --CH.sub.2 --, --C(O)-- or --C(S)--;Q is a non-interfering moiety or radical; andm and n, same or different, are selected from the group consisting of zero or one.

Abstract: Sulfonamide derivatives of the formula I ##STR1## where R.sup.1 is a C.sub.1 -C.sub.4 -alkyl or phenyl group which may be substituted by halogen, trifluoromethyl or C.sub.1 -C.sub.4 -alkyl, R.sup.2 is hydrogen or C.sub.1 -C.sub.4 -alkyl, A is a group CHOR.sup.3 C.dbd.O, C.dbd.S or C.dbd.N--OR.sup.4, R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl phenyl, benzyl or C.sub.1 -C.sub.4 -acyl, R.sup.4 is hydrogen or methyl, B may be methylene or ethylene in the m or p position or, of A is not carbonyl, may be methyleneoxy, the oxygen atom being bonded to the aromatic, and E is a carboxyl, phosphonic acid or sulfo radical, their physiologically acceptable salts, esters with C.sub.1 -C.sub.4 -alcohols or amides or the tetrazol-5-yl radical, their preparation and their use as drugs.

Abstract: Preparation of a semi-crystalline catalyst for curing coating compositions wherein an isocyanate-sulfonate or -phosphonate is made by a Michael addition followed by chain extension with an isocyanate.

Abstract: Dipeptide mimics which contain phosphorus and their pharmaceutical use and preparation are disclosed. The compounds have dehydropeptidase (DHP) enzyme inhibitor activity.

Abstract: .alpha.-Aminoalkylphosphonic and .alpha.-aminoalkylphosphinic acids of the formula I ##STR1## where n=1 or 0,R.sub.1 =H, CH.sub.3 or CH.sub.2 --C.sub.6 H.sub.5R.sub.2 =H (for n=1) and also=alkyl or phenyl (for n=0)are prepared by Hofmann deradation from compounds of the formula II ##STR2## wherein n and R.sub.1 have the same meaning as in formula I,R.sub.3 =alkyl (for n=1), alkyl or phenyl (for n=0), andM.sup.p+ =p-valent cation,with subsequent working up in the known manner.Some of the compounds I are biologically active, and some are intermediates for the preparation of biologically active compounds.

Abstract: Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydrogen or hydroxy; R.sub.2 is hydrogen or alkyl; R.sub.3 is C.sub.3-6 alkyl; R.sub.4 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.4 is a group ##STR2## where R.sub.8 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl, and R.sub.9 is hydrogen or alkyl; and R.sub.5 is hydrogen or alkyl.

Abstract: The invention relates to a process for the racemization of D-2-N-phenacetylamino-4-methylphosphinobutyric acid ##STR1## which comprises carrying out the racemization in glacial acetic acid and in the presence of acetic anhydride. The invention makes it possible to convert economically a fairly inactive herbicide into the racemic mixture which contains the highly active L form. The latter can be separated off from the racemized mixture by known methods.

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: 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: Process for the preparation of aryloxy-benzoic acids containing a sulphonamide group by the direct reaction of a phenoxy-benzoic acid with a sulphonamide, in the presence of a halogenating agent such as P(O)Cl.sub.3.

Abstract: Preparation of compounds with herbicidal properties, of formula ##STR1## wherein R.sup.1 represents a hydrocarbon radical;R represents a hydrogen atm or a hydrocarbon radical; andR.sup.22 represents a hydrogen atom, an aryl radical, or a substituted aryl radical,said process being characterized in that hydrogenation of compounds of formula ##STR2## wherein R, R.sup.1 and R.sup.22 have the same meaning as in formula (IIa), R.sup.32 represents an aryl radical, or substituted aryl radical, and R.sup.4 represents a hydrogen atom or an R.sup.8 group which can be hydrogenolyzed, is carried out.

Abstract: The present invention provides a process for the preparation of the stereoisomers of 1-aminoalkylphosphonic acids and of 1-aminoalkylphosphinic acids by enzymatic resolution of their racemic N-acyl derivatives and subsequent deacylation, wherein the enzymatic resolution is carried out with penicillin G amidase.