Abstract: New indolocarbazoles of formula: ##STR1## or a pharmaceutically acceptable salt thereof, processes for their preparation, compositions containing, and methods for using the composition for the inhibition of protein kinases, such as protein kinase C, for the prevention and/or treatment of heart and blood vessel diseases such as thromboses, arterioscleroses, hypertension, or for inflammatory processes, allergies, cancers, viral diseases, and certain degenerative damages of the central nervous system are disclosed.

Abstract: A depolymerization and purification process, by which a poly(alkyl-.alpha.-cyanoacrylate) feed is depolymerized into high-purity cyanoacrylate monomers without the use of a high-boiling heat transfer medium such as tricresyl phosphate. The poly(alkyl-.alpha.-cyanoacrylate) feed, which contains one or more polymerization inhibitors such as hydroquinone and phosphorus pentoxide, is first introduced into a thin-film evaporator for a depolymerization reaction. The temperature of the film evaporator is maintained at about 200.degree..about.260.degree. C., and operated under a vacuum of 1.about.20 mm Hg. The produced gas stream from the depolymerization reactor is subject to a two-stage heat transfer process for condensation and purification. The first stage involves a very-high temperature condenser (about 150.degree. C.). The residue collected in the first stage condenser contains primarily dimers of .alpha.-cyanoacrylate.

Abstract: A process for the preparation of aminopropionitriles of the general formula I ##STR1## in which R denotes hydrogen or methyl, wherein ammonia is caused to react with an acrylonitrile of the general formula II ##STR2## In which the substituent has the aforementioned meanings, in a molar ratio of from 1:1 to 500:1 over a heterogenic catalyst at temperatures ranging from 40.degree. to 180.degree. C. and pressures ranging from 10 to 350 bar.

Abstract: Preparation of 5-cyanovalerates (I) by the carbonylation of a 1-cyanobutene with carbon monoxide and an alkanol (II) corresponding to the ester radical at an elevated temperature and under superatmospheric pressure in the presence of a cobalt catalyst as well as in the presence of an activating solvent, in which the activating solvent used is an effective amount of a carbonic diester, a carbamate, or a urea of the general formula IIIa, IIIb, or IIIcR--O--CO--O--R (IIIa)R.sub.2 N--CO--O--R (IIIb)R.sub.2 N--CO--NR.sub.2 (IIIc)or a mixture of these compounds (R's same or different, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl groups or together form 5-membered to 7-membered rings).The end products I serve as intermediates, chiefly for the preparation of .epsilon.-caprolactam.

Abstract: A compound selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of --CN, --NO.sub.2, halogen, --CF.sub.3, free carboxy, salified carboxy, and carboxy esterified with lower alkyl; -A-B- is selected from the group consisting of ##STR2## and X, R.sub.3, R.sub.4 and R.sub.5 are defined as in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-androgenic activity.

Abstract: A process for preparing an aqueous active substance solution which can be sterilized by filtration entails mixing anipamil hydrochloride with a phospholipid in the ratio of from 1:2 to 2:1 by weight, converting the resulting mixture into a gel by adding water at elevated temperature, and subsequently adding water to the gel at elevated temperature until the active substance is present in the required concentration.

Abstract: Selective isotopic-labeling of spin label compounds, used in electron spin resonance spectroscopy to detect, measure and monitor the presence of paramagnetic species, increases the sensitivity of the electron spin resonance technique in assays for paramagnetic species, such as the determination of oxygen tension in solution or in a biological sample, like a living organism. Spin label compounds, such as nitroxides, like 3-carbamoyl-2,2,5,5-tetramethyl-3-pyrroline-1-yloxyl (CTPO), are selectively, but not completely, isotopically-labeled, such as partially deuterated, to increase the sensitivity and reliability of assays employing electron spin resonance spectroscopic measurements.

Abstract: This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary salts of p-dialkylaminobenzamides having the formula ##STR1## wherein R' and R" are each selected from the group of C.sub.1 to C.sub.2 alkyl; n is an integer having a value of from 2 to 3; R is an alkyl radical having from 10 to 18 carbon atoms; R.sub.1 and R.sub.2 are each selected from the group of C.sub.1 to C.sub.2 alkyl, and X is an anion. These benzamide derivatives are active sunscreening agents which are usefully employed at a concentration of from about 0.5 to about 10 wt. % in a formulation requiring protection against the harmful effects of sunlight, such as skin burn, hair damage, color fading, etc.

Abstract: Disclosed is a method of combating Pneumocystis carinii Pneumonia in a subject in need of such treatment. The method comprises administering to the subject an effective Pneumocystis carinii-combating amount of a bis-benzimidazole compound such as bis[5-(2-imidazolyl)-2-benzimidazolyl]methane, 1,4-bis[5-2-imidazolyl)-2-benzimidazolyl]butane, or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations for carrying out the method and novel compounds are also disclosed, along with methods of combating Giardia lamblia.

Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a pyrrolidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having an N-phenyl-amino-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

Abstract: This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary ammonium salts of a para-dialkylamino benzamide having the formula ##STR1## wherein R' and R" are each selected from the group of C.sub.1 to C.sub.2 alkyl; n is an integer having a value of from 2 to 6; R is an alkyl radical having from 1 to 30 carbon atoms; R.sub.1 and R.sub.2 together with the attached cationic nitrogen atom forms a 5 to 6-membered heterocyclic ring containing a hetero oxygen atom in addition to the heteronitrogen atom and is selected from the group of ##STR2## and X is an anion. These benzamide heterocyclic derivatives are active sunscreening agents which are usefully employed at a concentration of from about 0.5 to about 10 wt. % in a formulation requiring protection against the harmful effects of sunlight, such as skin burn, hair damage, color fading, etc.

Abstract: Acetonitrile is purified by treatment with ozone. After ozone treatment is ended, acetonitrile is passed through packed columns of molecular sieve, activated alumina and charcoal or graphitized carbon; the process results in virtually pure acetonitrile obtained at an efficiency unachievable by prior art processes.

Abstract: Compounds of the formula I ##STR1## in which R.sub.1 and R.sub.2 independently of one another are C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl, or phenyl or benzyl which is unsubstituted or substituted by F, Cl, Br, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or di(C.sub.1 -C.sub.6 alkyl)amino.The compounds are suitable as .pi.-acceptors and electrical semiconductors, and they can be used for antistatic finishing of objects.

Abstract: L-alanyl-L-proline is stereoselectively prepared catalytically hydrogenating an N-(2-iminopropionyl)-L-proline in the presence of a metal hydrogenolysis catalyst and at a pH of less than about 4. Also disclosed are improved processes for production of N-pyruvyl-L-proline in which L-proline and a 2,2-disubstituted propionyl halide are allowed to react at a pH of at least 9 to produce an L-proline intermediate which is hydrolyzed at a pH range of from about 6.5 to about 8.5 to yield N-pyruvyl-L-proline.

Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 1,3-thiomorpholino-type group or a 1,4-thiomorpholino-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

Abstract: The invention relates to compounds of the formula ##STR1## in which A denotes an optionally substituted radical from the series comprising alkyl, acyl, cycloalkyl, aryl and heteroaryl; A.sub.1 represents CO, CS, C=NH, CN-alkyl, CN-O-alkyl, SO, optionally substituted CH.sub.2 or a bond; A.sub.2 represents NH, NCH.sub.3, O, CH.sub.2 or a bond; E represents CHOH, CO, SO or optionally N-substituted C=NH; A.sub.3 represents O, NH, NCH.sub.3 or a bond; R.sup.4 denotes an optionally substituted radical from the series comprising alkyl, cycloalkyl, aryl and heteroaryl; and R.sup.8 denotes hydrogen or optionally substituted alkyl, to a process for their preparation, and to their use as inhibitors of prolyl hydroxylase.

Abstract: Compounds characterized generally as morpholino/oxazinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is selected from morpholino, oxo-substituted-morpholino and 1,3-oxazinyl groups; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.tbd.C--Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.

Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is NR;R is hydrogen or lower alkyl;R.sup.1 and R.sup.2 are each, independently, hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.20 cycloalkyl, phenylloweralkyl, or substituted phenylloweralkyl substituted by halo, lower alkyl, lower alkoxy, halo lower alkyl, amino, monoloweralkylamino, diloweralkylamino or sulfonamido;A is O, S, NR, or a chemical bond;m is 0-15;n is 0-20;p is 0-15,where m+p.ltoreq.15;and the pharmacologically acceptable salts thereof, which by virtue of their ability to inhibit PLA.sub.2, are of use as antiinflammatory agents and there is also disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals, as well as in the modulation of PAF-mediated biological processes, such as embryonic implantation, thus making the compounds useful as antifertility agents.

Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a morpholino-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.