Abstract: Compound having the formula ##STR1## wherein R can be selected from the group consisting of benzhydryl and lower alkyls having from about 5 to about 8 carbon atoms; R.sub.1 can be selected from the group of alkenyl, methyl thiomethyl, aryl, aralkyl, substituted aralkyl, cycloalkyl and lower alkyls, having from about 1 to about 6 carbon atoms; R.sub.2 can be selected from the group consisting of alkenyl, aryl, aralkyl, methyl thiomethyl, cycloalkyl and lower alkyls, having from about 5 to about 10 carbon atoms and X can be selected from the group consisting of organic acids, inorganic acids or is non-existant, thus forming a free base, the organic and inorganic acids are preferably those selected from the group consisting of HI, HBr, HCl, H.sub.2 SO.sub.4, (COOH).sub.2, Chrysanthemumic acid, HCO.sub.2 CH.sub.3, ##STR2## These compounds are active insecticides, miticides and lepidoptericides which can be applied to insects, mites or lepidoptera at any stage of development.

Abstract: The application relates to a process for partial dehydration of cyclohexanone oxime by treatment with an aqueous solution of an inorganic salt, the crude cyclohexanone oxime being extracted at above its melting point countercurrently in an extraction column with a concentrated solution of ammonium or/and hydroxylammonium salt. The salt solution may be used again after concentration. This may be effected by simple evaporation.

Abstract: Novel aromatic guanidine compounds having the formula: ##STR1## wherein: R.sub.1 is hydroxyl, methyl or hydroxymethyl and R.sub.2 is hydrogen or methyl, are found to have biological activity. The guanidine compounds and their salts are shown to be activate as vasoconstrictor agents and create useful pharmaceutical preparations when deployed with a pharmaceutically acceptable carrier for administration to a host, e.g., man, requiring vasoconstrictive therapy.

Abstract: Compositions having the formula ##STR1## in which hal is chlorine, bromine or iodine, R.sup.1 is (1) alkyl, (2) substituted alkyl, (3) alkenyl, (4) aryl, (5) nuclear substituted aryl in which the substituents are halogen, cyano, nitro, lower alkyl, or lower alkoxy, (6) styryl, (7) nuclear substituted styryl, in which the substituents are halogen, cyano, nitro, lower alkyl or lower alkoxy, (8) benzyl, (9) nuclear substituted benzyl in which said substituents are halogen, cyano, nitro, lower alkyl or lower alkoxy, (10) phenethyl, (11) nuclear substituted phenethyl in which the substituents are halogen, cyano, nitro, lower alkyl, or lower alkoxy, (12) cycloalkyl having 3 through 6 carbon atoms, (13) substituted cycloalkyl, and (14) furyl; R.sup.2 is H, Cl, or lower alkyl; and n is a whole number from 3 to 8, inclusive, and the use of these compositions as fungicides.

Abstract: The present invention relates to certain new and useful steroids which demonstrate anti-androgenic properties. These steroids are 5,10-secosteroids that have been found to be potent irreversible inhibitors of the enzyme .DELTA..sup.5 -3-ketosteroid isomerase which is involved in androgen biosynthesis. In addition, certain of the steroids of the invention compete reversibly with 5-.alpha.-dihydrotestosterone for binding to the prostatic cytoplasmic receptor protein while others inhibit the enzyme prostatic testosterone 5-.alpha.-reductase. The anti-androgenic properties of the present compounds indicate such utility as the control of abnormal growth of the human prostate, e.g. in the therapy of human prostatic cancer.

Abstract: A process is described for isomerizing the cis,cis- and cis,trans-isomers of di-(p-aminocyclohexyl)methane to the corresponding trans,trans-isomer. The starting isomer, or mixture of isomers, is converted to the corresponding bis-benzaldimine by reaction with benzaldehyde (or benzaldehyde containing 1 to 3 inert substituents), the bis-benzaldimine is isomerized in the presence of a basic catalyst (potassium t-butoxide, potassium hydroxide preferred) to give predominantly the trans,trans-isomer of the bis-benzaldimine, and the latter is subjected to acid hydrolysis to yield the trans,trans-isomer of the free diamine. The process can be applied to the individual cis,cis- and cis,trans-isomers of the diamine as well as to admixtures of these isomers with the trans,trans-isomer, such as the mixtures of these stereo-isomers obtained by catalytic hydrogenation of di-(p-aminophenyl)methane.

Abstract: Antibacterial compounds of the formula ##STR1## (where COB is carboxy or protected carboxy;Hal is halogen;R is amino or protected amino;R' is mercapto-protecting group; andX is nucleophilic group)Are prepared from penicillin 1-oxides having X on its 2-methyl group, and found to be used as starting materials for preparing cephalosporins.

Abstract: D-homosteroids of the formula ##STR1## WHEREIN R.sup.3.alpha. is hydrogen, R.sup.3.beta. is hydroxy, lower alkanoyloxy or aroyloxy and R.sup.3.alpha. and R.sup.3.beta. taken together are oxo; R.sup.17a.alpha. is hydrogen, lower alkyl, ethynyl, vinyl, allyl, methallyl, propadienyl, 1-propynyl, butadiynyl or chloroethynyl; R.sup.17a.beta. is hydrogen, alkanoyl, aroyl, lower alkyl, cycloalkyl-lower-alkyl, benzyl, furfuryl or tetrahydropyranyl; R.sup.18 is hydrogen or methyl and the dotted line in the C-ring denotes an additional carbon to carbon bond in the 11,12-position andProcesses for the preparation thereof are disclosed.The D-homosteroids of the present invention are useful as ovulation inhibitors and androgenic/anabolic agents.

Abstract: Disclosed are antibacterial penicillins of the formula ##STR1## wherein Y" is a residue of a strong nucleophile and processes for preparing same.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or hydroxy, R.sup.2 is a group of the formula: --CO-CH(NH.sub.2)-CH.sub.2 COR.sup.3 or --COCH.sub.2 -CH(NH.sub.2)-COR.sup.3, and R.sup.3 is selected from the group consisting of hydroxy, lower alkylamino, di-lower alkylamino, lower alkoxy and hydroxy-lower alkylamino, or R.sup.3 is amino when R.sup.2 is hydroxy. Several methods of preparing the compound [I] are also disclosed. The compound [I] and a pharmaceutically acceptable salt thereof are useful as antimicrobial agents.

Abstract: This invention relates to a novel .alpha.-amino.alpha.-(p-acyloxyphenyl)acetamidopenicillanic acid which is useful as an antibacterial agent, and also to a novel process for the production of 6-D-(-).alpha.-amino-.alpha.-(p-hydroxyphenylacetamido)penicillanic acid (also known as amoxycillin).BACKGROUND OF THE INVENTION1. Field of the InventionThe chemical compound of the present invention is an antibacterial agent of the class commonly called penicillins.2. Description of the Prior ArtU.S. Pat. No. 2,985,648 relates to .alpha.-aminobenzylpenicillins and discloses a general formula for such penicillins which includes, inter alia, lower alkanoyloxy substituents on the benzene ring. This document does not give any more specific details of compounds so substituted, and no specific examples are given of their preparation. The document indicates that the .alpha.-aminobenzylpenicillins exist in various optical forms and specific examples are given of the preparation of both D- and L- forms.U.S. Pat. No.

Abstract: Dichlorocyclopropylphenyl bisbiguanides are prepared by cyanoguanidine-amine condensations. Antimicrobial compositions thereof and their method of use are disclosed.

Abstract: A process for preparing 7-oxo cephalosporins and 6-oxo penicillins by reaction of a 7-amino cephalosporin or 6-amino penicillin with a carbonyl-containing oxidizing agent is disclosed.

Abstract: Novel azomethines are obtained when reacting a tertiary amine with an aromatic aldehyde or ketone having in orthoposition an activated methoxy group. These azomethines are capable of ring closure to yield a benzofurane and said tertiary amine. The benzofuranes are optical brighteners, tranquilizers or intermediates for optical brighteners, fluorescent dyestuffs, scintillators, sensibilizers for electrophotographic coatings.

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: Guanidine derivatives of the formula: ##STR1## in which R.sup.1 is a cyclohexyl, adamantyl, bicycloheptanyl, bicycloheptenyl, tricycloheptanyl or tetracyclononanyl radical and R.sup.2 is a phenyl or pyridyl radical optionally substituted by 1 or 2 halogen atoms, or alkyl, cyanoalkyl, alkoxycarbonyl or amino radicals, and the pharmaceutically-acceptable acid-addition salts thereof, active against rhinoviruses, are disclosed, along with processes for their manufacture, compositions containing them, a method of combatting rhinoviral infections and a method of selectively killing rhinoviruses in a mixed virus population.

Abstract: An improved process of preparing a 6-alkoxy-substituted penicillin or penicillin sulfoxide is disclosed. This process comprises adding a halogenating agent to penicillin or penicillin sulfoxide while cooling, and then adding an alkali metal alcoholate to the hydrogenation product in the presence of an alcohol corresponding to the alcoholate.

Abstract: N-Phenyl amidines which have diuretic, antithrombogenic, smooth muscle relaxant, anti-inflammatory and antiarrhythmic properties have been discovered. They are prepared by reacting a substituted aniline with a carboxamide selected from the group consisting of amides and lactams in the presence of phosphorus oxychloride. Typical examples of substituted N-phenyl amidines thus obtained are 5-methyl-2-(N-phenylbenzylamino)-1-pyrroline, 2-(N-phenylbenzylamino)-1-pyrroline, 3-[(N-1-pyrrolin-2-yl-p-anisidino)methyl]indole and 4,5,6,7,8,9-hexahydro-2-(N-phenylphenethylamino)-3H-azonine. Indole substituted N-phenyl amidines can be rearranged to provide iminopyrrolinidinylindoles which are useful as diuretic, antithrombogenic and smooth muscle relaxant agents. In the case of 3-[(N-1-pyrrolin-2-yl-p-anisidino)methyl]indole, the rearranged product is 3-[[2-(p-methoxyphenylimino)-1-pyrrolindinyl]methyl]indole.

Abstract: Novel d-.alpha.-isobutylsulfobenzylpenicillin hemi-solvate crystals of the formula: ##STR1## (wherein A is a solvent selected from the class consisting of alcohols, ketones, ethers and esters) have excellent antibacterial activities and improved stability in terms of shelf-life.

Abstract: A class of 6-methoxy-.alpha.-carboxy penicillins have antibacterial activity against a wide range of Gram-negative organisms.