Abstract: This invention comprises certain analogs PGE or 11-deoxy-PGE compounds in which the carbonyl at C-9 is replaced by methylene. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.

Abstract: A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-acylaminocephalosporin, or 6-acylaminopenicillin, then the latter compounds are treated with an organolithium compound, followed with t-butyl-hypochlorite. Finally, a defined reagent is added yielding a side chain on the carbon adjacent to the amino-nitrogen. Novel intermediate compounds are also described. The end compounds prepared are active against both gram-positive and gram-negative bacteria.

Abstract: Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponing N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

Abstract: Methyldichlorophosphane is made by reacting methane with phosphorus trichloride in contact with carbon tetrachloride at temperatures higher than 500.degree. C. To this end, the starting reactant mixture is admixed with 2 to 7 mol % of reaction-initiating carbon tetrachloride, based on phosphorus trichloride; the carbon tetrachloride is reacted to an extent of 50 to 80% by varying the reaction temperature within the range 550.degree. to 650.degree. C for constant residence times of 0.1 to 0.9 second; and resulting reaction mixture containing a residual analytically detectable 20 to 50% proportion of the carbon tetrachloride used is condensed out.

Abstract: Azines are prepared by reacting aqueous ammonia and a carbonyl compound with chloramine in a series of two or more reactors arranged in a cascade system.

Abstract: This invention comprises certain analogs of the prostaglandins in which the C-1 carboxyl is replaced by a primary alcohol. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.

Abstract: Novel monospiroalkyl analogues or derivatives of prostaglandin A, E and F are useful modifiers of smooth muscle activity. The compounds have valuable pharmacalogical properties as platelet antiaggregating agents and gastric antisecretory agents. The compounds are also valuable pharmacological agents for increasing femoral blood flow and decreasing blood pressure and heart rate.

Abstract: The invention provides the benzhydrylsulphinyl derivatives of the formula:(C.sub.6 H.sub.5).sub.2 CH--SO--(CH.sub.2).sub.n --R Iwhere n is 1, 2 or 3 and R is C(.dbd.O)NHOH, C(.dbd.NH)NH.sub.2, C(.dbd.NH)NHOH, 2--.DELTA..sup.2 -imidazolinyl or NR.sub.1 R.sub.2 (where R.sub.1 is H or C.sub.1 --C.sub.3 -alkyl and R.sub.2 is H, C.sub.1 --C.sub.3 -alkyl, or CH.sub.2 CH.sub.2 OH, and R.sub.1 and R.sub.2 considered together can form, with the nitrogen atom to which they are bonded, a N-heterocyclic group of 5 to 7 ring members, which can be substituted and can contain a second hetero-atom such as O and N), and their addition salts. These products are useful in therapy for treating disturbances of the central nervous system.

Abstract: This invention comprises certain analogs of the prostaglandins in which the C-1 carboxyl is replaced by a primary alcohol. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.

Abstract: Novel ?N,N-di(higher alkyl)aminomethyl!benzamidine and substituted compounds such as ?N,N-di(higher alkyl)aminomethyl!-N-(2-propyl)-benzamidine and ?N,N-di(higher alkyl)aminomethyl!-N-(p-hydroxyphenyl)-benzamidine and their non-toxic acid addition salts are useful for combating viral infections in vertebrate animals.

Abstract: This invention comprises certain analogs of the prostraglandins in which the C-1 carboxyl is replaced by a primary alcohol. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.

Abstract: An in-situ process for preparing organic sulfone compounds by oxidizing the corresponding sulfide compound with a mixture of hydrogen peroxide, a carboxylic acid in the presence of a catalytic amount of a mineral acid or an organic sulfonic acid.

Abstract: 2,5-Dioxo-1,2-oxa-phospholanes of the formula (I) ##STR1## wherein R.sup.1 is an organic radical and R.sup.2 and R.sup.3 each also represents an organic radical or hydrogen, are prepared by reacting 2-haloformylethyl-phosphinic acid halides of the formula (II) ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are defined as in formula (I) and X means Cl or Br, preferably Cl, with an approximatey equimolar quantity of acrylic acid. The compounds (II) may also be produced in the reaction batch and in situ by reacting about equimolar quantities of a dihalophosphine of the formula (III) ##STR3## with an .alpha.,.beta.-unsaturated acid (IV)R.sup.4 -- OH (IV)In the formulae (III) and (IV) R.sup.1, R.sup.2, R.sup.3 and X are defined as indicated above.In the reaction there is formed, in addition to the compounds (I), practically exclusively .beta.-halopropionic acid and no free hydrogen halide.

Abstract: Styrylamidines are prepared by treating styrylsulfonylamidines with base. The styrylamidines are effective in the prevention of aggregation of blood platelets and as analgesics. Compounds of the invention are also useful as anticonvulsants, diuretics and antihypertensive agents. The styrylsulfonylamidines of the invention which serve as precursors to the styrylamidines also have analgesic properties. Illustrative of the styrylamidines of the present invention are 4-amino-N-(4-aminostyryl)benzamidine and N-(3,4-dichlorostyryl)acetamidine. An example of a styrylsulfonylamidine is N-(styrylsulfonyl)acetamidine.

Abstract: Novel N-haloalkanesulfenylcarbamoyloxime compounds have been found to have exceptional miticidal and insecticidal activity.

Abstract: In the halogenation under reflux conditions of an aldehyde of the formula ##STR1## with Cl.sub.2, Br.sub.2 or I.sub.2, the aldehyde and halogen are continuously fed into a reactor at a molar ratio of halogen to aldehyde between about 0.8:1 and about 1.1:1 and water is continuously fed into the reactor at a rate of between about 1 and about 20% by weight of aldehyde. The product .alpha.-haloaldehyde is thioalkylated and then oximated to form a 2-hydrocarbylthioaldoxime of the formula ##STR2## with improved yield and quality because of the improved yield and quality of .alpha.-haloaldehyde. An exemplary process includes the chlorination of isobutyraldehyde (IBA) to form .alpha.-chloroisobutyraldehyde (CIBA), the thiomethylation of CIBA to form 2-methyl-2 methylthio-propionaldehyde (MTIBA) and the oximation of MTIBA to form 2-methylthio-propionaldehyde oxime (aldicarb oxime or ADO).

Abstract: Certain alkanoyl chloride phenylhydrazones have been found to be active against insects and mites, and also active as herbicides. The phenylhydrazone ring can be substituted. Suitable substituent groups are halogen atoms, the nitro group, the trifluoromethyl group, and alkyl groups of from 1 to 6 carbon atoms, inclusive. The compounds are prepared by reacting an alkanoic acid phenylhy-drazide with phosphorus pentachloride to obtain an alkanoyl chloride (dichlorophosphinyl)phenylhydrazone intermediate that is reacted with phenol to produce the desired alkanoyl chloride phenylhydrazone. Certain compounds can be prepared by direct chlorination of an alkanaldehyde phenylhydrazone. Some of the compounds are novel. Methods of use and compositions are described.

Abstract: A process is described for the production of azines by contacting in the liquid phase ammonia, hydrogen peroxide and a carbonyl compound, either an aldehyde or a ketone. The reaction takes place in the presence of an amide (I) of a monocarboxylic or dicarboxylic acid, wherein at least one of the ionization constants is below 5 .times. 10.sup.-5, and further in the presence of an inorganic or organic catalyst (II), having the atomic structure H--X--Y.dbd.Z, H representing hydrogen, X and Z representing oxygen or nitrogen and Y representing carbon, nitrogen, phosphorus, arsenic, antimony, sulphur, selenium or tellurium. It is possible for X, Y or Z to carry other substituents, providing valency rules are obeyed. The process is carried out in the presence of the ammonium salt (III) of the carboxylic acid corresponding to the amide (I), at the rate of at least 0.1 mole of the ammonium salt (III) per mole of hydrogen peroxide employed.

Abstract: Weeds in rice are controlled by applying amidines of the formula ##STR1## wherein R is a (C.sub.4 -C.sub.12)alkyl group, and N IS 1 TO 3.The amidines and herbicidal compositions containing them are useful for the control of weeds in both direct-seeded and transplanted rice.

Abstract: This invention comprises certain analogs of the prostaglandins in which the C-1 carboxyl is replaced by a primary alcohol. Also provided in this invention, are novel chemical processes useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.