Abstract: The invention relates to a new synthesis for the preparation of tetracyclic compounds of the general formula: ##STR1## as well as the pharmaceutically acceptable salts thereof, in which: n is the number 1 or 2,m is the number 1, if n=2 and the number 2, if n=1,R.sub.1 and R.sub.2 stand for hydrogen, hydroxy, halogen, lower alkyl (1-4 C), lower alkoxy (1-4 C) or trifluoromethyl andR.sub.3 represents hydrogen, alkyl (1-6 C), aralkyl (7-10 C) or an amino alkyl group (1-6 C), in which the nitrogen atom has been substituted by two alkyl groups (1-4 C), or the nitrogen atom forms part of a heterocyclic 5- or 6-membered ring,having valuable biological properties.

Abstract: An immunoassay based on the agglutination or the agglutination inhibition of a suspension of immunologically coated particles by the sample. Measurements are made with an apparatus having means for providing electromagnetic radiation at wavelengths equal to or less than the mean diameter of the particles and in a range of at least about 100 nm. The apparatus also includes means for measuring, at a predetermined angle, a portion of the radiation transmitted through a cuvette containing the reaction mixture.

Abstract: There are disclosed branched chain and cycloaliphatic esters of steroids having the formula: ##STR1## or the 5.alpha.H analog thereof, where R is H or CH.sub.3 ;R.sub.1 is H or CH.sub.3 ;R.sub.2 is H or CH.sub.3 ;R.sub.3 is H, OH, CH.sub.3 or Cl;R.sub.4 is H or C.sub.1 to C.sub.4 alkyl;R.sub.5 is H, C.sub.1 to C.sub.4 alkyl or CF.sub.3 ;R.sub.6 is H, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halogen or .beta.-OH providing that when R.sub.6 is .beta.-OH, the steroid also contains 9.alpha.-F and further providing that R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 represent at least 4 and at most 5 hydrogen atoms, except in the case of a .DELTA..sup.1,4 -steroid, in which case R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are all hydrogen;R.sub.7 is H or CH.sub.3 ; ##STR2## providing the R.sub.8 is --OH or ##STR3## when the steroid has an aromatic ring A and the 3-position is substituted by ##STR4## R.sub.9 is ##STR5## where n is 0, 1 or 2;R.sub.10 is C.sub.1 to C.sub.10 alkyl;R.

Abstract: Novel peptides of the formula ##STR1## are disclosed (together with pharmaceutical compositions comprising a pharmaceutically effective amount of same) wherein X.sub.1 and X.sub.2 represent an hydroxy or amino group and B represents:(1) hydroxy or(2) an amino-acid residue selected from the group consisting of L-Asp-OH, L-Asn-OH, L-Glu-OH, L-Gln-OH, L-Ser-OH, or HN-A-COOH, wherein A is an alkylidene group from 1 to 6 carbon atoms;or a functional derivative thereof.These peptides have psychopharmacological properties; they are suitable for the treatment of certain mental disorders in which stimulation of brain function is desired, such as for the treatment of senility or amnesia.

Abstract: New and useful phenylalkylcarbohydroxamic acids are disclosed of the formula ##STR1## wherein: (a) R is selected from the group consisting of alkoxy of one to six carbon atoms, alkenyloxy of two to six carbon atoms, alkyl of one to six carbon atoms, and benzyloxy;(b) R.sub.1 and R.sub.2 are each selected from the group consisting of hydrogen, alkoxy of one to six carbon atoms, alkenyloxy of two to six carbon atoms, alkyl from one to six carbon atoms, and benzyloxy;(c) R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen or alkyl of one to six carbon atoms;(d) R.sub.5 is hydrogen or R.sub.5 together with R.sub.3 or R.sub.4 represent methylene; and(e) n signifies the number 0 or 1,and non-toxic salts thereof, which novel compounds exert a pronounced inhibition of blood platelet aggregation and accelerate the disaggregation of platelet aggregates already formed.

Abstract: Novel cyclization substrates of the formula: ##STR1## wherein: (a) R.sub.1 is H or alkyl of one to four carbons;(b) R.sub.2 is H or alkyl of one to four carbons, with the proviso that R.sub.1 is H when R.sub.2 is alkyl; and with the proviso that P.sub.2 is H when R.sub.1 is alkyl;(c) R.sub.3 is a leaving group selected from the group consisting of OH, alkoxy of one to four carbons, alkoxyalkyoxy of from two to about four carbons, acyloxy of from about one to about seven carbons, and trialkylsilyloxy;(d) R.sub.4 is halogen, alkoxy of from one to four carbons, hydrocarbyl of from one to about four carbons, hydrocarbyl of from one to about four carbons substituted by one or more (1) halogens or (2) alkoxy moieties of from one to two carbons; and(e) R.sub.5 is H, alkyl of one to six carbons, hydroxy, or an esterified or estherified moiety of (1) less than eight carbons selected from the group consisting of alkoxy, trialkylsilyloxy, aralkyloxy, cyclo-alkoxy, and heterocyclo-oxy radicals; (2) .alpha.

Abstract: The invention relates to novel dibenzo[1,2;5,6]cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7]oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7]thiepino pyridine or pyrrole derivatives and dibenzo[b,f]pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,m is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.

Abstract: Novel cyclization substrates are disclosed of the formula ##STR1## wherein: (a) R.sub.1 is H or alkyl of one to four carbon atoms;(b) R.sub.2 is H or alkyl of one to four carbon atoms, with the proviso that R.sub.1 is H when R.sub.2 is alkyl, and with the proviso that R.sub.2 is H when R.sub.1 is alkyl;(c) R.sub.3 is a leaving group selected from the group consisting of hydroxy, alkoxy of one to four carbons, alkoxyalkoxy of two to four carbons, acyloxy of one to about seven carbons, and trialkylsilyloxy of less than fifteen carbons;(d) R.sub.4 is hydrocarbyl of one to four carbon atoms, a hydrocarbyl of one to two carbon atoms substituted by halogen or alkoxy of one to two carbons, or alkoxy of one to four carbon atoms; and(e) R.sub.5 and R.sub.5 ' each are H, OH, alkyl, trialkylsilyloxy, or an esterified or etherified hydroxy-group of about one to ten carbon atoms.

Abstract: New and useful phenylalkylcarbohydroxamic acids are disclosed of the formula ##STR1## wherein: (a) R is selected from the group consisting of alkoxy of one to six carbon atoms, alkenyloxy of two to six carbon atoms, alkyl of one to six carbon atoms, and benzyloxy;(b) R.sub.1 and R.sub.2 are each selected from the group consisting of hydrogen, alkoxy of one to six carbon atoms, alkenyloxy of two to six carbon atoms, alkyl from one to six carbon atoms, and benzyloxy;(c) R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen or alkyl of one to six carbon atoms;(d) R.sub.5 is hydrogen or R.sub.5 together with R.sub.3 or R.sub.4 represent methylene; and(e) n signifies the number 0 to 1,and non-toxic salts thereof, which novel compounds exert a pronounced inhibition of blood platelet aggregation and accelerate the disaggregation of platelet aggregates already formed.

Abstract: New and useful stable peroxidase compositions are disclosed which are particularly useful as reagents in enzyme immunoassay (EIA) tests. The novel peroxidase compositions contain polyvalent ions of groups 3 and 4 of the Periodic Table. These novel compositions are stable even in low concentrations, and are relatively invulnerable to freeze-drying. Preferably, the polyvalent ions selected are those of Al, Zn, Mg, Fe, and Cu.

Abstract: The invention relates to novel dibenzo[1,2;5,6]cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7]oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7]thiepino pyridine or pyrrole derivatives and dibenzo[b,f]pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, r.sub.2, r.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,M is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## OR THE GROUP --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.

Abstract: The invention relates to novel dibenzo[1,2;5,6] cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7] oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7] thiepino pyridine or pyrrole derivatives and dibenzo[b,f] pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, r.sub.2, r.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,M is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.

Abstract: The present invention relates to novel benzo(b) bicyclo[3.3.1]nones of the general formula I: ##STR1## and a salt or nitrogen oxide thereof, in which R.sub.1 and R.sub.2 stand for hydrogen, alkyl of 1-6 carbon atoms, alkenyl of 1-6 carbon atoms, an optionally substituted aralkyl group or an acyl group orR.sub.1 and R.sub.2 together with the nitrogen atom represent a heterocyclic 5- or 6-membered ringR.sub.3 is a free, etherified or esterified hydroxy,X and Y stand for hydrogen, hydroxy, halogen, alkyl or alkoxy of 1-6 C-atoms, nitro, CF.sub.3 or an acyloxy group, having valuable biological activities, particularly anorectic activity.

Abstract: The invention relates to novel dibenzo[1,2;5,6]cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7]oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7]thiepino pyridine or pyrrole derivatives and dibenzo[b,f]pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, r.sub.2, r.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,M is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.

Abstract: A new and remarkably stable synthesized conjugated estrogen composition comprising one or more selected alkali metal synthetic conjugated estrogen sulfate salts and an effective amount of one or more suitable antioxidants has been found for use in novel and stable therapeutic preparations of a pH of not less than about 7 which are adapted to relieve, inter alia, complaints occurring in the menopausal syndrome and other female complaints. Preferably, the steroids are selected from the sodium and potassium salts of the group consisting of estrone, equilin, 17.alpha.-dihydroequilin, and mixtures or conjugates thereof. Most preferably, the preparations are so formulated so that sodium estrone sulfate, sodium equilin sulphate, and 17.alpha.-dihydroequilin sodium sulphate as conjugated estrogens are present in a weight ratio of about 6:3:1, respectively and administered in tablets containing 0.625 mg, 1.25 mg, or 2.5 mg of total conjugated estrogens.

Abstract: A new diagnostic labeled spine tool is disclosed for use in immunoassay techniques, e.g., determination of a component of the antigen-antibody reaction. The new tool is a labeled-spine material product of the formula ##STR1## where R is an organic group labeled with a radioisotope, fluorescent group, lysis-initiating compound, enzyme, or other suitable marker material; T.sub.1 and T.sub.2 are any of --CH.sub.3, ##STR2## --CH.sub.2 OH, --Ch.sub.2 SH, and --NH.sub.2 ; X is selected from the group consisting of (CH.sub.2).sub.m, where m is an integer from 0 to about 10, phenylene, hydroxyl-substituted phenylene, halogen-substituted phenylene, alkyl substituted phenylene or aminated phenylene groups;A is 0, 1 or 2;B is 2-a, with the proviso that there be at least two R groups in the product; andN is a number from 1 to about 100,000The new tool provides higher specific activity for labeled substances thus facilitating determination of the desired compound.

Abstract: The invention relates to an oral pharmaceutical preparation with androgenic activity on the basis of one or more esters of testosterone and/or 5.alpha.-dihydrotestosterone, the ester group of which has been derived exclusively from aliphatic carboxylic acids having 9-16 carbon atoms, preferably 10-12 carbon atoms in combination with a non-steroidal lipoid. The preparation may additionally contain a progestational steroid, an oestrogen or a precursor of an A-aromatic steroid.

Abstract: A three-phase method of human female contraception wherein (1) starting on about the ninth to about the twelfth day of the female cycle (first cycle day being first menstruation day) an effective amount of at least one progestagenic substance is administered in daily or shorter intervals for about three to about six days followed at substantially similar intervals by (2) administration for about one to about three days starting from about the fourth to about the seventh day after the first phase of both an effective amount of the progestagenic substance(s), and a peptide possessing LHRF (Luteinizing Hormone Release Factor) activity, followed by (3) administration of an effective amount of the progestagenic substance(s) until the total time of the progestagenic substance administration with and without the LHRF compound is from about seven to about fifteen days.

Abstract: The invention discloses novel compounds of the general formula: ##STR1## and salts thereof, in which X stands for oxygen, sulphur, the group >NR.sub.7 or the group --CR.sub.8 R.sub.9 --;R.sub.1, r.sub.2, r.sub.3 and R.sub.4 represent hydrogen, hydroxy, halogen, alkyl (1-6 C), alkoxy (1-6 C), alkylthio (1-6 C) or trifluoromethyl;R.sub.5 and R.sub.6 represent hydrogen, alkyl (1-6 C), aralkyl (7-10 C) or together in combination with the nitrogen atom a heterocyclic five- or six-membered ring;R.sub.7 stands for hydrogen or alkyl (1-4 C);R.sub.8 and R.sub.9 stand for hydrogen or methyl,n is the number 0, 1 or 2 andThe dotted line means an optional C--C bond,With valuable central nervous system (CNS) activities, especially antidepressant activity.

Abstract: Biologically active novel peptide compounds are disclosed of the formulaA-L-B-D-Lys-L-Phe-Gly-(L or D)Lys-L-Pro-L-Val-Gly-L-Lys-L-Lys-Xor a pharmaceutically acceptable non-toxic functional derivative thereof; A is a N-terminal chain prolongation selected from the group consisting of (1) hydrogen and (2) N-acyl radicals derived from (a) alkyl carboxylic acids having from one to about six carbons, (b) aralkyl carboxylic acids having from seven to about ten carbons, (c) amino acids, (d) peptides, (e) the N-alkylcarbonyl or N-aralkylcarbonyl derivatives of the amino acids, and (f) the N-alkylcarbonyl or N-aralkylcarbonyl derivatives of the peptides; B is an amino-acid residue selected from the group consisting of Phe, Trp, Tyr, and --NH--CHR.sub.1 --CO--, wherein R.sub.1 is hydrogen or alkyl from one to about six carbons; and X is a member selected from the group consisting of hydroxy, esterified hydroxy radicals, unsubstituted amino radicals and substituted amino radicals.