Abstract: The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a lipophilic, pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 by weight (diglyceride:monoglyceride) wherein the diglyceride and monoglyceride are mono- or di- unsaturated fatty acid esters of glycerol having sixteen to twenty-two carbon chain length, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic compounds.

Abstract: This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

Abstract: The coat protein gene of cucumber mosaic virus strain WL (CMV-WL), the method of preparing it, its use to prepare transgenic plants and transgenic plants containing it are provided.

Abstract: Methods for isolating thymidine kinase-encoding DNA of a herpes virus are described. These methods utilize degenerate primers based on regions of relatively conserved amino acid sequence in herpes virus thymidine kinase proteins to initiate a polymerase chain reaction which yields large amounts of the thymidine kinase-encoding DNA. The methods are illustrated in the isolation of the thymidine kinase gene of feline herpes virus, which can be used to construct recombinant thymidine kinase-negative feline herpes viruses for purposes of constructing live vaccines and expression vectors. In addition, the regulatory elements of the feline herpes virus thymidine kinase gene are useful in the construction of recombinant DNA vectors.

Abstract: Provided are ribosome binding sites having an increased number of adenine (A) and thymidine (T) residues as compared to the naturally occurring ribosome binding sites from which they are derived or to which they are related, which allow high level expression of genes encoding heterologous polypeptides, particularly somatotropins, operatively linked thereto.

Abstract: Amine salts of alkane-1,n-dicarboxylic acid mono-(2-sulfatoethyl)amides of the Formula IHOC(O)--(CH.sub.2).sub.n --C(O)--N(R.sub.1)--CH.sub.2 CH.sub.2 SO.sub.3.sup.--+ HN(R.sub.2).sub.3 Iwherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.8 alkyl and phenyl, R.sub.2 is C.sub.1 -C.sub.8 alkyl or (R.sub.2).sub.3 when taken together with the nitrogen atom is pyridinyl; and n is an integer from 4 to 20, their preparation and use to prepare water-soluble esters of corticosteroids.

Abstract: Provided are novel .alpha.-aminoindole-3-acetic acid derivatives having the formula ##STR1## wherein R through R9 are as defined in the specification, and pharmacologically acceptable salts of compounds wherein R.sub.9 is not OM, which are useful as anti-diabetic, anti-obesity and anti-atherosclerotic agents.

Abstract: Process for alkylating protected spectinomycin enone derivatives in the gamma position in order to produce intermediates useful in the synthesis of 6'alkylspectinomycins. The intermediate have the formula ##STR1## which comprises reacting a compound having the formula ##STR2## with a strong base and an alkenyl halide, wherein R.sub.1 is selected from the group consisting of alkoxycarbonyl, halogenated alkoxycarbonyl, aralkoxycarbonyl, and arylsulfone; R.sub.2 is selected from the group consisting of hydrogen, trimethylsilyl (TMS), tetrahydropyran (THP), and triethylsilyl (TES); A is selected from the group consisting of oxygen and sulfur; M is selected from the group consisting of lithium and potassium; and n is an integer from 1 to 3.

Abstract: New pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of formula (I), ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4 and m are as defined in the specification, e.g., 4-(benzoylmethyl)-6-cyclohexyl-6,7-dihydro-2-phenyl-4H-pyrazolo[1,5-a]pyrr olo[3,4-d]pyrimidine-5,8-dione, have been found to be potentially useful to treat warm-blooded animal patients suffering from the symptoms of atherosclerosis and cholesterol buildup to relieve the same and for favorably altering the high density lipoprotein (HDL) to low density lipoprotein (LDL) ratio in blood samples of such patients.

Abstract: A method for the prevention of central nervous system toxicity of acivicin which comprises the concomitant administration of acivicin and an amino acid solution consisting essentially of large neutral amino acids.

Abstract: An controlled release implant antibiotic formulation comprising (a) a crystalline salt of the antibiotic; (b) an amorphous salt of the antibiotic; and (c) excipients; whereas the excipients comprise from 0% to 10% of the tablet by weight.

Abstract: A 7-phenylpyrimido[1,2-a][1,4]benzodiazepin-3(5H)-ones of the formula II: ##STR1## wherein R.sub.o is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, --COOR in which R is alkyl defined as above, ##STR2## in which n is a number of 1 to 4, R.sub.6 and R.sub.7 are hydrogen or alkyl defined as above or together ##STR3## is selected from the group consisting of pyrrolidino, piperidino, morpholino, and 4-methylpiperazino, and --CH.sub.2 OH; wherein R.sub.1 is selected from the group consisting of hydrogen, hydroxy, acetoxy, propionoxy, succinyloxy, and alkyl esters thereof; wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.

Abstract: 1-Substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula (III): ##STR1## wherein R is selected from the group consisting of hydroxy, esters thereof, and alkoxy, in which the alkyl group is of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoylamino, and dialkylamino in which the carbon chain moieties are of 1 to 3 carbon atoms, inclusive, are produced by condensing a 1,3-dihydro-5-phenyl-2H-1,4-benzodiazepine-2-thione of the formula (I): ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.

Abstract: A method for the prevention of pancreatitis utilizing cis- and trans-N-(3-aminocycloaliphatic)-2-arylacetamide derivative compounds of the formula ##STR1## e.g., N-[2-(n',N'-dimethylamino)cyclohexyl]-N-methyl-2-(4-bromophenyl)acetamide and trans-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]acetamide, 2-(3,4-dichlorophenyl) and their pharmaceutically acceptable salts.

Abstract: An estrogen sulfotransferase inhibitor composition comprises a compound of the formula ##STR1## wherein R.sub.1 is F, Br, NO.sub.2, or H; R.sub.2 is F, 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; R.sub.5 is H.sub.2, .alpha.-H and .beta.-OH or B-H and .alpha.-OH in admixture with a pharmaceutically acceptable carrier with the proviso that R.sub.1, R.sub.2 and R.sub.3 cannot all be hydrogen and one of R.sub.1 and R.sub.2 is F.

Abstract: The invention concerns a novel nogamycin having a heretofore unknown configuration and novel analogs which are active against various microorganisms. The invention also includes novel methods of making substituted and unsubstituted nogamycin having an essentially pure isomeric form of a preferred configuration.

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

Abstract: Process for preparing clindamycin and analogs thereof by reacting lincomycin or an analog thereof with a dimethylformamide and an excess of thionyl halide.

Abstract: Novel antibiotic U-56,407 producible in a fermentation under controlled conditions using a biologically pure culture of the microorganism Streptomyces hagronensis strain 360, NRRL 15064. This antibiotic is active against various Gram-positive bacteria, for example, Staphylococcus aureus, Streptococcus pyogenes and Streptococcus pneumoniae. Thus, antibiotic U-56,407 can be used in various environments to eradicate or control such bacteria.

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.