Abstract: Peptidyl derivatives of diesters of .alpha.-aminoalkylphosphonic acids, particularly those with proline or related structures, their use in inhibiting serine proteases with chymotrypsin-like, trypsin-like, elastase-like, and dipeptidyl peptidase IV specificity and their roles as anti-inflammatory agents, anticoagulants, and anti-tumor agents.

Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## The new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) have a particularly pronounced activity against animal pests, in particular against insects and arachnids, and against weeds.

Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

Abstract: The present invention relates to novel water-soluble analogs of carbamazepine and compositions containing them. The novel compositions are particularly suited for intravenous administration. The analogs of carbamazepine are useful in the treatment of epilepsy and related disorders.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is H or an optionally substituted hydrocarbon or acyl group; ring A is an optionally further substituted benzene ring; n is an integer of 1 to 10; R.sup.2, R.sup.3 and R.sup.4 are H or an optionally substituted hydrocarbon group; R.sup.3 and R.sup.4 may form an optionally substituted heterocyclic group, taken together with the adjacent nitrogen atom; k is an integer of 0 to 3; and m is an integer of 1 to 8; provided that when k=0 and m=2, n is an integer of not less than 2 or a pharmaceutically acceptable salt thereof, exhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic/prophylactic medicaments of senile dementia.

Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.

Abstract: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is --OOO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

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: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to treat allergic diseases: ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

Abstract: Compounds of the formula I ##STR1## in which R can be hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.1 hydrogen, C.sub.1 -C.sub.6 -alkyl, aryl, aryl-C.sub.1 -C.sub.4 -alkyl, amino-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -dialkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.7 -alkenyl, R.sup.2 R.sup.1 or C.sub.2 -C.sub.7 -alkenyl, C.sub.1 -C.sub.6 -alkylmercapto, C.sub.1 -C.sub.6 -alkoxy, phenoxy-C.sub.1 -C.sub.4 -alkyl,amino, C.sub.1 -C.sub.4 -alkylamino, di-C.sub.1 -C.sub.4 -alkylamino, morpholino, thiomorpholino, pyrrolidino, piperidino, hexamethyleneimino, pyrasolino, imidazolino, n 0, 1 or 2 and R.sup.1 and R.sup.

Abstract: A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## and the carboxylic and phosphonic alkyl esters and salts thereof; wherein the substituents are defined herein.

Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

Abstract: The present invention relates to new phosphorylated diazacycloalkanes, to processes for their preparation, and to their use as pesticides, in particular as insecticides and nematicides. The new compounds have the general formula (I) ##STR1## in which R.sup.1 represents hydrogen, or represents alkyl, alkenyl or aryl, each of which is optionally substituted by halogen or alkoxy,A represents an alkanediyl radical which is optionally substituted by alkyl,R.sup.2 represents alkyl,R.sup.3 represents alkyl andR.sup.4 represents hydrogen, or represents alkyl, alkenyl or aryl, each of which is optionally substituted by halogen or alkoxy.

Abstract: The present invention relates to the N-phosphonomethyl-biaryl substituted amino acid derivatives of formula I ##STR1## wherein X represents a direct bond, C.sub.1-4 -alkylene or C.sub.2 -C.sub.4 -alkenylene; R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, .alpha.-(trichloromethyl, carboxyl, esterified carboxyl or amidated carboxyl)substituted-(lower alkyl or aryl-lower alkyl), acyloxymethyl optionally monosubstituted on methyl carbon by C.sub.1-20 -alkyl, by C.sub.5 -C.sub.7 -cycloalkyl, by aryl or by aryl-lower alkyl; R.sub.1 represents monocyclic carbocyclic or monocyclic heterocyclic aryl; COR.sub.3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; R.sub.2 and R.sub.

Abstract: Processes for the preparation of biotinylated polynucleotides and analogues thereof and protected intermediate products for use in such processes are described and claimed. The processes may be conveniently used in the automated synthesis of biotinylated polynucleotide on a DNA synthesizer. The polynucleotides so prepared may be used as labelled probes e.g. as diagnostic tools for clinical and research uses.

Abstract: Herbicides have the formula ##STR1## in which R is hydrogen, mono- or poly-halo, mono- or di-(C.sub.1 -C.sub.4 alkyl), C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, phenoxy or nitro;R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.3 is C.sub.1 -C.sub.6 alkyl;R.sub.2 is C.sub.2 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, optionally substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, one or more halogens, or two C.sub.1 -C.sub.4 alkoxy groups, or one C.sub.1 -C.sub.4 alkyl and one C.sub.1 -C.sub.4 alkoxy group, phenyl-(C.sub.1 -C.sub.2)alkyl or pyridyl; orR.sub.1 and R.sub.2, and/or R.sub.3 and R.sub.4 respectively, taken together with the nitrogen atom, form a 4-8 member ring, optionally including an oxygen heteroatom;and R.sub.4 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, optionally substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, one or more halogens, or two C.sub.1 -C.sub.

Abstract: A novel glycerol derivative which is effective to reduce blood pressure has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is lower acyl, benzoyl, aryl, mono-, di- or triarylalkyl, alkyl, cycloalkyl, or cycloalkylalkyl; Q is substituted or unsubstituted alkylene containing 1-4 carbon atoms, l is 0 or 1; Y is a nitrogen-containing heterocyclic group or a nitrogen-containing bridged heterocyclic group (--(Q).sub.l -- is attached to a carbon atom contained in a hetero-ring of the heterocyclic group) in which Y is the bridged heterocyclic group where l is 0; and each of R.sup.5, R.sup.6 and R.sup.7 is hydrogen, lower alkyl, aryl or aralkyl.

Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## wherein X is ##STR2## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: A compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, alkenyl or phenylalkyl; or R.sup.1 and R.sup.2 taken together are --Ch.sub.2 CH.sub.2 --, --CH.sub.2 C(R.sup.6)(R.sup.7)CH.sub.2 --or --CH.sub.2 C(R.sup.8)(R.sup.9)--C(R.sup.10)(R.sup.11)CH.sub.2 --, where R.sup.6, R.sup.8 and R.sup.10 are, independently, hydrogen, alkyl of 1 to 6 carbon atoms or hydroxyl and R.sup.7, R.sup.9 and R.sup.11 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; A is alkylene or alkenylene; X is CO.sub.2 R.sup.3 in which R.sup.3 is hydrogen or alkyl, P(O)(OR.sup.4)(OR.sup.5) in which R.sup.4 and R.sup.5 are, independently, hydrogen or alkyl, 3,5-dioxo-1,2,4-oxadiazolindin-2-yl or 5-tetrazolyl; or a pharmaceutically acceptable salt thereof are useful as neuroprotectants.

Abstract: The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.

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: Compounds of the formula (I): ##STR1## in which the nitrogen-containing hetero ring portion is a 1,4-dihydropyridine ring or a pyridine ring, R.sup.1 is only present when the nitrogen-containing hetero ring is a 1,4-dihydropyridine ring, and Z is either a CO.sub.2 R.sup.8 group or a group of the formula (II): ##STR2## in which R.sup.4 and R.sup.5 may be the same or different and together may form one divalent group, are effective agents for enhancing the antitumor effect or antitumor drugs.

Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).

Abstract: Novel compositions of phosphoroustriscaprolactams, including tris(caprolactyl)phosphite which may be produced in accordance with the methods disclosed, finding particular utility as catalysts for esterification and other condensation reactions.

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: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.

Abstract: Novel compounds are disclosed having the formula ##STR1## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. These compounds are useful, for example, as cardiovascular agents and especially as anti-ischemic agents.

Abstract: A glycerol derivative which is effective to reduce blood pressure and has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is a lower acyl group or benzoyl, each of R.sup.3 and R.sup.4 independently is hydrogen or a straight or branched chain alkyl group having 1-6 carbon atoms; each of R.sup.5, R.sup.6 and R.sup.7 independently is hydrogen, a straight or branched chain alkyl group having 1-6 carbon atoms, an aryl group or an aralkyl group; and each of m and n independently is 0 or a positive integer under the condition of m+n=2-8.

Abstract: Aminotriazines of the formula ##STR1## wherein E is nitrogen,Z is oxygen or sulfur,R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.4 -alkenyl or C.sub.1 -C.sub.4 -alkoxy,R.sup.4 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.2 -C.sub.4 -alkoxyalkoxy, cyclopropyl, -NH.sub.2, C.sub.1 -C.sub.4 -alkylamino, di-C.sub.1 -C.sub.4 -alkylamino, or a saturated 5- to 7-membered nitrogen heterocycle bound by way of the nitrogen atom and selected from pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine and hexamethyleneimine,R.sup.5 is cyano, --CZ--R.sup.

Abstract: .alpha.-adrenoceptor antagonists having the formula: ##STR1## which are useful to produce .alpha.-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of using these antagonists to produce .alpha.-adrenoceptor antagonism in mannals.

Abstract: Reagents useful in the preparation of 5'-biotinylated oligonucleotides are disclosed.

Abstract: Antihypertensive phosphate derivatives are described having the following formula: ##STR1## wherein n is an integer 1 or 2; m is an integer 1 or 2, and the sum of n and m must be 3; X is selected from the group consisting of C.sub.1 -C.sub.24 branched or straight chain alkoxy and substituted phenoxy wherein the substituents are selected from one or more of the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, phenyl and substituted phenyl; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino, Q is a bivalent radical selected from the group consisting of --(CH.sub.2).sub.p -- and --(CHR).sub.p --, where p is an integer from 2 to 12 and the moiety --(CHR).sub.

Abstract: Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from the group consisting of a phenyl radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted at any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen, and a naphthalene radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted at any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.

Abstract: The invention relates primarily to quaternized polycyclic compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.2 together with the quaternary nitrogen, forms a 5 to 14 membered heterocyclic ring, said ring containing from 1 to 2 hetero atoms selected from the group of nitrogen, sulfur and oxygen; R.sub.1 forms a double bond in the heterocyclic ring of the quaternized nitrogen or is alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, alkylamidoalkyl and X.sup.- is a chloride, bromide or iodide anion. The invention also relates to the preparation and use of said quaternized polycyclic compounds.

Abstract: A reaction medium of ethanol condensed with 1-20, most preferably 4-6 moles, of ethylene or propylene oxide per mole of ethanol greatly improves the practicality of the preparation of azacycloalkane-2,2-diphosphonic acids of the general formula I: ##STR1## where R means a hydrogen or a lower alkyl radical with from 1 to 3 carbon atoms, and n means an integer between 3 and 11, by phosphonylating the corresponding lactams with phosphonic acid and phosphorous trihalides in the presence of water.

Abstract: Aromatically substituted azacycloalkylalkanediphosphonic acids of the formula ##STR1## in which R represents an aromatically substituted azacycloaliphatyl radical that is bonded to the group alk by way of a nitrogen atom and that optionally contains an additional nitrogen atom, and alk represents a divalent aliphatic radical, and their salts, can be used for the treatment of illnesses that can be attributed to calcium metabolism disorders. They are manufactured, for example, by reacting a compound of the formulaR--alk--X.sub.3 (IV)in which X.sub.3 represents carboxy, carbamoyl or cyano, with phosphorus acid and phosphorus trichloride and in an intermediate of the formula ##STR2## obtained by starting from compounds of the formula IV in which X.sub.3 represents cyano or carbamoyl and by working up by hydrolysis, or in a salt thereof, replacing the amino group by hydroxy by treatment with nitrous acid.

Abstract: The disclosure relates to a class of 2-(pyridylalkylamino)-3-hydroxypyridines which are active as histamine H.sub.1 -antagonists.

Abstract: Process for the conversion of an organophosphonic acid of the formula ##STR1## in which n=3-5 and R=H or C.sub.1 -C.sub.3 alkyl, into an alkali metal or ammonium salt comprising reacting the moist filter cake which accumulates during the production of organophosphonic acids by known processes (water content 10 to 40% by weight) with anhydrous or concentrated aqueous alkali metal hydroxide or ammonia and exposing the paste formed, which has a water content of from 20 to 80% by weight, to intense shear forces in mixing, dispersing, or kneading units, water being removed from the paste under reduced pressure and with application of heat until the paste changes into a free-flowing powder.

Abstract: Compounds of formula (I): ##STR1## [wherein: m is 1-3; A and B are oxygen or sulfur; and one of R.sup.1 and R.sup.2 is C.sub.10 -C.sub.22 alkyl and the other is a group of formula (II). ##STR2## where: n is 2 or 3; and --NR.sup.3 R.sup.4 R.sup.5 is an amino group] and salts thereof are effective anti-cancer agents.

Abstract: New reaction products, useful as additives for functional fluids, are obtained by reacting, at elevated temperature,(A) a triazole having the formula IA or IB: ##STR1## wherein R.sub.7 is hydrogen or a C.sub.1 -C.sub.20 alkyl residue;R.sub.8 and R.sub.9 are the same or different and each is C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.20 alkenyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.7 -C.sub.13 aralkyl, C.sub.6 -C.sub.10 aryl or R.sub.8 and R.sub.9, together with the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic residue or R.sub.8 and R.sub.9 is each a residue of formula:R.sub.12 X[(alkylene)O].sub.n (alkylene)-- IIwherein X is O, S or N(R.sub.12), R.sub.12 is hydrogen or C.sub.1 -C.sub.20 alkyl, "alkylene" is a C.sub.1 -C.sub.12 alkylene residue and n is 0 or an integer from 1 to 6;R.sub.10 is hydrogen, C.sub.1 -C.sub.20 alkyl or C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.18 alkyl phenyl; and R.sub.11 is hydrogen, C.sub.1 -C.sub.20 alkyl or a residue --CH.sub.2 NR.sub.8 R.sub.

Abstract: N-Arylsulfonyl-N'-(4-mercaptomethyl-pyrimidinyl- and -triazinyl)-ureas of the formula: ##STR1## and the salts of these compounds with amines, alkali metal bases or alkaline-earth metal bases or with ammonium bases, have good pre- and post-emergence-selective, herbicidal and growth-regulating properties.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 denote alkyl, OH, CF.sub.3 or cyanoethyl, A preferably denotes --COOH, R.sub.3 denotes inter alia alkoxycarbonylalkoxy, fairly high-molecular (>C.sub.12) alkoxy, alkylcarbonylalkoxy or nitrobenzyloxy, are valuable herbicides and growth regulators.

Abstract: Benzodiazepines of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

Abstract: Compounds of the general formula ##STR1## are reacted with a strong base followed by a phosphorylating agent, such as dicyclicaminophosphinic halide or bis-di-lower alkylaminophosphinic halide to produce an imine of the formula ##STR2## wherein R is dicyclicaminophosphinyloxy or bis-di-lower alkylaminophosphinyloxy.R represents a leaving group which will undergo nucleophilic displacement with nitrogen, oxygen, sulfur and carbon containing nucleophiles, that is, nucleophiles which have, as a reactive site, a nitrogen, oxygen, sulfur or carbon atom, such that, when the cyclic imine undergoes nucleophilic displacement, there is formed C--N, C--O, C--S and C--C bonds between the carbon atom of the cyclic imine and the nucleophilic group.The end products may be utilized as intermediates in the production of pharmaceutically valuable compounds and, in some instances, are pharmaceutically valuable compounds per se.

Abstract: Compounds of the general formula ##STR1## wherein two of the residues R.sup.1, R.sup.2 and R.sup.3 represent C.sub.10-30 -alkyl residues with at least 8 C-atoms in a straight chain, at least one of these residues being substituted by at least 2 C.sub.1-3 -alkyl residues and the sum of the C-atoms in the two residues being greater than 20; and the third residue is a residue --P(O)(O.sup.-)OR.sup.4 in which R.sup.4 represents a lower-alkyl or C.sub.5-7 -cycloalkyl residue which is substituted by a quaternary ammonium group or a C.sub.5-7 -cycloalkyl residue which contains a di-(lower-alkyl)-substituted nitrogen atom,are useful for the manufacture of colloidal solution systems. The compounds of formula I can be prepared starting from glycerol derivatives as described in more detail in the specification.

Abstract: A catecholamine compound is converted to a new mono O-phosphate ester derivative thereof which exhibit improved absorption and effectiveness.

Abstract: Triazolobenzodiazepines of the formula: ##STR1## are disclosed which are antagonists of cholecystokinin (CCK).

Abstract: Phosphonous acid monoester-monoamides of the formula ##STR1## in which n is 1, R.sub.1 is phenyl, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen or alkyl, R.sub.5 is alkyl or cyclohexyl, R.sub.6 is 2,2,6,6-tetramethylpiperidin-4-yl or ##STR2## R.sub.3 may also be ##STR3## where X is methylene or isopropylidene and R.sub.6 is alkyl or cyclohexyl. Said compounds are suitable for protecting organic material from the harmful effect of heat, oxygen and light.

Abstract: Phosphinylalkanoyl imino acids useful in the treatment of hypertension are disclosed.