Abstract: Novel antibacterially-active esters of antibiotic nodusmicin. Activity is demonstrated against Staphylococcus aureus, Streptococcus pyogenes, and Sarcina lutea. Thus, these esters can be used in various known environments, using well-known procedures, to eradicate or control susceptible microbes.

Abstract: A process for treating hypertension comprising the systemic administering to a hypertensive subject or a novel compound of the formula: ##STR1## wherein X is alkyl of from 1 to 3 carbon atoms, inclusive, or alkenyl of from 3 to 5 carbon atoms, inclusive.R.sub.1 is --NH.sub.2.R.sub.2 is chloro, bromo, or iodo.R.sub.3 is hydrogen or fluorine.R.sub.4 is hydrogen or fluorine, andR.sub.5 is hydrogen, fluorine, or CH.sub.3 ; or salt thereof, in association with a pharmaceutical carrier.The amount administered is from 0.1 mg to 400 mg/kg of body weight, dosage unit form and dosage amounts disclosed.

Abstract: This invention is a novel chemical particularly concerned with N-dealkylation of secondary amines as found in amino-cylitols of which spectinomycin is an example. Separation and further alkylation also comprise the present invention process.

Abstract: Novel cyclized .omega.-carboxyethyl mono or dithiocarbanilic acids are disclosed as immunoregulatory agents, useful in the treatment of organ transplant reject phenomenon and autoimmune diseases particularly where a delayed hypersensitivity component has been established, such as multiple sclerosis.Additionally described is the use of certain cyclized .omega.-carboxyalkyl mono- or dithiocarbamic acids and certain cyclized .omega.-carboxyalkyl mono- or dithiocarbamic acids.

Abstract: The present invention relates to novel methods of use for known pharmacological anti-allergenic agents including disodiumchromoglycate (DSCG) and related compounds thereof, including generally bis chromones, benzopyrans, oxamic acids and salts or esters of each, preferably lodoxamide, its THAM salt and ethyl ester. All are subsequently included in the term biologues. The methods are for the treatment of pathological cardiovascular ischemic states in animals, particularly humans. Additionally, novel compositions including the biologues of the present invention in combination with known vasodilators and feed stuffs are also disclosed.

Abstract: Novel processes for making arylpropionic acids are described. One process comprises carboxylating particular Grignard compounds which are the products of a catalyzed reaction between corresponding arylmagnesium bromides and ethylene. Furthermore, the reaction making the particular Grignard compounds is itself novel. Also, an improved method is disclosed for making coupled aryl compounds useful as intermediates for making compounds having a pharmaceutical use. For example, particular biaryls may be used to make some of the Grignard compounds herein from which the arylpropionic acids are made. Finally, an improved bromination is disclosed giving high yields of 4-bromo-2-fluoroaniline, which is thereafter coupled with benzene, then used to make the arylmagnesium bromide reacted with ethylene to obtain the particular Grignard compound and subsequent desired arylpropionic acid, i.e. 2-(2-fluoro-4-biphenylyl)propionic acid.

Abstract: This invention pertains to novel processes for preparing phosphorus derivatives of aminothiomethylcarbamates known to be useful as pesticides. The processes use products prepared by a novel method which reacts disulfides of various amides of phosphoric acids with chlorine or bromine. Such sulfenyl halide products are advantageous and obtained in unexpected yields. Therefore, the method is also unobvious. When the novel sulfenyl bromides of this invention are intermediates unexpected yields of pesticides are obtained.

Abstract: This invention pertains to novel processes for preparing phosphorus derivatives of aminothiomethylcarbamates using as intermediates corresponding phosphorus derivatives of aminothiocarbamic halides. The carbamates are useful as pesticides against insects, mites, and nematodes. Two processes for preparing the corresponding intermediates are described. One preparation generally reacts an appropriate N-chlorothiophosphoramide with N-methylcarbamoyl halide. The other preparation generally reacts an N-chlorothiomethylcarbamoyl halide with an appropriate phosphoramide. The intermediate will react with various alcohols to produce the desired carbamates in the process of the invention.

Abstract: Anomers and asteric mixtures of novel analogs of spectinomycin. Additionally provides novel intermediates and process for preparing spectinomycin and analogs thereof.

Abstract: This invention pertains to novel processes for preparing phosphorus derivatives of aminothiomethylcarbamates using as intermediates corresponding phosphorus derivatives of aminothiocarbamic halides. The carbamates are useful as pesticides against insects, mites, and nematodes. Two processes for preparing the corresponding intermediates are described. One preparation generally reacts an appropriate N-chlorothiophosphoramide with N-methylcarbamoyl halide. The other preparation generally reacts an N-chlorothiomethylcarbamoyl halide with an appropriate phosphoramide. The intermediate will react with various alcohols to produce the desired carbamates in the process of the invention.

Abstract: This invention is a novel chemical process particularly concerned with N-dealkylation of secondary amines as found in amino-cylitols of which spectinomycin is an example. Separation and further alkylation also comprise the present invention process.

Abstract: The invention concerns the novel compounds dialkyl 2-(3-fluoro-4-nitrophenyl)-2-methylmalonate IIIa and dialkyl 2-(3-fluoro-4-aminophenyl)-2-methylmalonate IVa useful as intermediates in an improved process for making 2-(2-fluoro-4-biphenylyl)propionic acid, known as flurbiprofen, having the formula ##STR1## and ester thereof. It has anti-inflammatory activity which is about 240 times that of aspirin and analgesic activity which is about 180 times that of aspirin in standard laboratory tests. However, despite this high activity, the toxicity (LD.sub.50) is only 1.2 to 2.4 times greater than that of aspirin in standard laboratory tests.Also within the invention is a novel method of making the above intermediates and analogs thereof useful to prepare corresponding biaryl compounds which have pharmaceutical uses.

Abstract: A method of treating depression in humans which comprises administering orally to humans an antidepressant effective amount of a compound having the formula I.sub.1 wherein Y is alkyl of from 1 to 3 carbons, inclusive; A is ethylene or --CH.sub.2 CH(CH.sub.2 Cl)--, T and T.sub.1 are the same or different and are SR.sub.3, OR or NR.sub.1 R.sub.2 ; R is hydrogen, alkyl of from 1 through 6 carbons, aryl, aralkyl or I(a) with the proviso that when one of T or T.sub.1 is NR.sub.1 R.sub.2 then the other cannot be SR.sub.3 or OR.

Abstract: Anomers and asteric mixtures of novel analogs of spectinomycin. Additionally provides novel intermediates and process for preparing spectinomycin analogs.

Abstract: This invention pertains to novel processes for preparing phosphorus derivatives of aminothiomethylcarbamates using as intermediates corresponding phosphorus derivatives of aminothiocarbamic halides. The carbamates are useful as pesticides against insects, mites, and nematodes. Two processes for preparing the corresponding intermediates are described. One preparation generally reacts an appropriate N-chlorothiophosphoramide with N-methylcarbamoyl halide. The other preparation generally reacts an N-chlorothiomethylcarbamoyl halide with an appropriate phosphoramide. The intermediate will react with various alcohols to produce the desired carbamates in the process of the invention.

Abstract: Isochromans, isothiochromans, 2-benzoxepins and 2-benzothiepins are described. The compounds possess hypotensive and antipsychotic properties; methods and compositions using them are described.

Abstract: Novel cyclized .omega.-carboxyethyl mono- or dithiocarbanilic acids are disclosed as immunoregulatory agents, useful in the treatment of organ transplant reject phenomenon and autoimmune diseases particularly where a delayed hypersensitivity component has been established, such as multiple sclerosis.Additionally described is the use of certain cyclized .omega.-carboxyalkyl mono- or dithiocarbamic acids and certain cyclized .omega.-carboxyalkyl mono- or dithiocarbamic acids.

Abstract: This invention relates to processes for base catalyzed acylations using enol esters, for example, isopropenyl acetate. Particularly, the processes are useful for acylating acid sensitive alcohols including hydroxy steroids.

Abstract: An estrogen sulfotransferase inhibitor composition comprises a compound of the formula ##STR1## wherein R.sub.1 is Br, NO.sub.2, or H; R.sub.2 is Br, NO.sub.2, NH.sub.2, or H; R is H or alkyl of 1-4 carbon atoms; R.sub.3 is O or H.sub.2 ; and R.sub.4 is H.sub.2, O, or .alpha.-H, .beta.-OH, in admixture with a pharmaceutically acceptable carrier. The specificity of the invention is believed targeted to the substituent at R.sub.2 or C.sub.4 and secondarily the OR group at C.sub.3.

Abstract: This invention pertains to novel phosphorus derivatives of aminothiocarbamic halides and processes for their preparation. The carbamic halides are readily prepared by two general procedures. In one procedure an appropriate N-(chlorothio)phosphorus amide reactant is readily prepared by reacting the corresponding phosphorus amide with sulfur dichloride which reactant will react with N-methylcarbamoyl halide so as to produce the corresponding object compounds of this invention. In a different procedure the same compounds that are the object of this invention are prepared by reacting an appropriate corresponding phosphorus amide with an N-chlorothiomethylcarbamoyl halide reactant which reactant is readily prepared by reacting N-methylcarbamoyl halide with sulfur chloride. The novel compounds of this invention are intermediates for the preparation of pesticides.