Abstract: The invention is a new process for the preparation of .alpha.-ethynyl-benzohydrols and of ring-substituted derivatives thereof by reacting the starting benzophenone or a ring-substituted derivative thereof with acetylene in a solvent delivering no protons, in the presence of an alkali metal tertiary alcoholate, preferably potassium-tert.-butylate or potassium-tert.-amylate. Also new substituted derivatives of .alpha.-ethynyl-benzhydrol are prepared by the invention.
Abstract: New compounds of the formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straightchained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom form a substituted or unsubstituted heterocyclic group which can contain a further oxygen or nitrogen hetero atom,But when R.sub.1 is methyl, R.sub.2 is a group other than methyl, are prepared by reacting a compound of the formula (II), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2. (iii)the new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.
Abstract: The invention relates to the preparation of biologically active polypeptides containing the aspartyl group, particularly an aspartyl-glycine moiety, using the active-ester technique.According to the method of the invention, human adrenocorticotropic hormone and its fragments characteristic to the individual species, as well as the blocked derivatives of such compounds are prepared by the pentafluorophenol method, i.e., the carboxy group of the acylating component is activated by converting it into pentafluorophenyl ester in the coupling reaction carried out with blocked peptides containing the aspartyl group or an aspartylglycine moiety. The acylation is carried out preferably using equimolar quantities of the respective reactants. The free peptides obtained after removing the blocking groups can be converted into their acid addition salts or pharmaceutically acceptable complexes or condensates.Human adrenocorticotropic hormone and its derivatives are valuable substances of therapeutical activity.
Type:
Grant
Filed:
May 14, 1973
Date of Patent:
April 27, 1976
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt
Inventors:
Lajos Kisfaludy, Miklos Low, Istvan Schon, Tamas Szirtes, Maria Sz. Sarkozi, Sandor Bajusz, Andrae Turan, Rosa Beks, Attila Juhasz, Laszlo Graf, Kalman Medzihradszky, Laszlo Szporny
Abstract: New benzimidazole derivatives of the general formula (I) ##SPC1##and acid addition salts thereof, whereinR.sub.1 and R.sub.2 each represent hydrogen or methyl,R.sub.5 and R.sub.6 form together a valence bond and at the same time R.sub.3 and R.sub.4 form together a group of the general formula (II), ##EQU1## wherein n is equal to zero or one, or R.sub.4, R.sub.5 and R.sub.6 form together a group of the formula (III) ##EQU2## and at the same time R.sub.3 stands for benzyl group, were prepared by reacting a compound of the general formula (IV), ##SPC2##wherein R.sub.7 stands for hydrogen or benzyl group and R.sub.1, R.sub.2 and n each have the same meanings as defined above, or an acid addition salt thereof with epichlorohydrine optionally in the presence of a base.The new compounds of the general formula (I) and their acid addition salts inhibit the reproduction of viruses and can be used in therapy as antiviral agents.
Type:
Grant
Filed:
April 24, 1974
Date of Patent:
March 2, 1976
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt
Inventors:
Olga Hankovszky, Kalman Hideg, Sandor Pacsa
Abstract: A process for the continuous drying of chemical products by milling fluidization, in which a fluidized bed of particles of an inert carrier, e.g., quartz sand having a particle diameter of 0.5-1.0 mm., is maintained and the chemical product to be dried is introduced in a wet state, e.g., wet solid or paste or suspension, into the fluidized carrier bed. The chemical product dries on the surface of the inert carrier particles and dry particles of the chemical product leave the relatively large and heavy carrier particles and are carried off in the exit gas. The carrier particles, however, are too large and heavy to leave in the exit gas and so remain in the fluidized bed. If desired, the dried product particles can be further dried, for example by additional drying gas in a cyclone chamber, after which the dried particles are separated from the gas which can be vented and/or recycled.
Abstract: New tricyclic fused imidazole derivatives of the general formula (I), ##SPC1##whereinR.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##EQU1## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a =C-- group, orA stands for a group of the general formula (III), ##EQU2## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##SPC2##wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##EQU3## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(CH.sub.2).sub.m --X (VI)in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen.
Type:
Grant
Filed:
May 24, 1974
Date of Patent:
January 13, 1976
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Kalman Hideg, Olga Hankovszky, Eva Palosi, Gyorgy Hajos, Laszlo Szporny