Patents Represented by Attorney Robert H. Falk
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Patent number: 4271178Abstract: 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.Type: GrantFiled: June 26, 1978Date of Patent: June 2, 1981Assignee: Akzona IncorporatedInventor: Willem J. van der Burg
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Patent number: 4271179Abstract: 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.Type: GrantFiled: June 26, 1978Date of Patent: June 2, 1981Assignee: Akzona IncorporatedInventor: Willem J. van der Burg
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Patent number: 4271177Abstract: 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.Type: GrantFiled: June 26, 1978Date of Patent: June 2, 1981Assignee: Akzona IncorporatedInventor: Willem J. van der Burg
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Patent number: 4264626Abstract: The present invention relates to novel biologically active tricyclic compounds of the general formula: ##STR1## and salts thereof, in whichR.sub.1 and R.sub.2 stand for hydrogen, alkyl or alkenyl, an optionally substituted aralkyl group or an acyl group orR.sub.1 +R.sub.2 together with the nitrogen atom represent a heterocyclic 5- or 6-membered ring, andX and Y stand for hydrogen, hydroxy, halogen, alkyl or alkoxy of 1-6 carbon atoms, nitro, trifluoromethyl or an acyloxy group,which compounds have valuable biological activities, particularly anorectic activity.Type: GrantFiled: March 6, 1979Date of Patent: April 28, 1981Assignee: Akzona IncorporatedInventors: Colin L. Hewett, David S. Savage
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Patent number: 4256718Abstract: There is disclosed a sodium zirconium carbonate compound and the method of its preparation. The sodium zirconium carbonate compound is formed from a metastable aqueous solution comprising zirconium, sodium, sulfate, and carbonate ions.Type: GrantFiled: January 24, 1979Date of Patent: March 17, 1981Assignee: Organon Teknika CorporationInventors: Mary J. McArthur, Laurence B. Marantz, Abb L. Scarbrough
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Patent number: 4254223Abstract: An apparatus for use in the colorimetric determination of liquids is disclosed wherein the apparatus is a reaction vessel having a massive V-shaped bottom of transparent material with a refractive index of n.gtoreq.1.4. The bottom has a cone- or prism-shape with an apical angle from about 80.degree. to about 100.degree. or the shape of a polyhedral pyramid whose opposing surfaces intersect at an angle between about 80.degree. and about 100.degree.. The apparatus permits speeded-up colorimetric determinations.Type: GrantFiled: April 16, 1979Date of Patent: March 3, 1981Assignee: Akzona IncorporatedInventors: Antonius H. W. M. Schuurs, Johannes H. W. Leuvering
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Patent number: 4254031Abstract: 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.Type: GrantFiled: August 8, 1979Date of Patent: March 3, 1981Assignee: Akzona IncorporatedInventor: Jacques Olivie
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Patent number: 4250394Abstract: A novel method and a novel apparatus therefor are described for detecting and measuring a predetermined immunochemical substance, for example, an antigen, an antibody, a hapten, or certain low molecular weight substance. The detection and measurement of an immunochemical substance using the method and apparatus of the invention involves providing for the agglutination of a suspension of particles in a sample, or color intensity of solutions by which, using the apparatus of the invention to determine certain electromagnetic radiation properties of the sample, the presence and amount of the immunochemical substance can be determined.Type: GrantFiled: July 19, 1979Date of Patent: February 10, 1981Assignee: Akzona IncorporatedInventor: John J. O'Connor
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Patent number: 4248597Abstract: A novel depletion indicator (time watch) for removable substances containing acid or basic groups is disclosed, together with a novel method of use therefor. The removable substance of a predetermined concentration comes into contact with a suitable pH color indicator that can change color at a predetermined pH range within a much larger measurable pH range, which color change occurs as the concentration of the removable substance diminishes by passing through a permeable film containing both the removable substance and the pH color indicator.The color change occurs at a predetermined time, e.g., the same time that the active ingredient has diminished to the point it is determined to be inactive.Type: GrantFiled: December 12, 1978Date of Patent: February 3, 1981Assignee: Akzona IncorporatedInventor: Gerald W. McNeely
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Patent number: 4240751Abstract: A novel combination and a method are disclosed for detecting and measuring a predetermined substance capable of being specifically bound. The combination comprises a novel adapter which eliminates contact of a light conducting and receiving probe with the sample.Type: GrantFiled: November 9, 1978Date of Patent: December 23, 1980Assignee: Akzona IncorporatedInventors: Carl B. Linnecke, Daniel Wong
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Patent number: 4240926Abstract: A novel composition is disclosed which is useful as a sterilization indicator that can distinguish clearly between the types of sterilization employed, e.g., that indicates whether sterilization was accomplished by steam or dry heat. The novel composition comprises (1) thiobarbituric acid and (2) at least one suitable reacting moiety being capable of reacting with said acid under temperature and humidity conditions of steam and dry heat sterilization to form a colored product. Suitable reacting moieties disclosed are (a) parabanic acid and (b) dimethyl oxalate and urea.Type: GrantFiled: February 26, 1979Date of Patent: December 23, 1980Assignee: Akzona IncorporatedInventor: Gerald W. McNeely
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Patent number: 4237126Abstract: New and pharmacologically useful pharmaceutically acceptable acid addition salts are disclosed for the 16.beta.-mono-quaternary ammonium derivatives of either the 2.beta., 16.beta.-bis-piperdino-3-.alpha., 17.beta.-dihydroxy-5.alpha.-androstane 3.alpha., 17.beta.-di-lower aliphatic esters of the 2.beta., 16.beta.-bis-piperidino-3.alpha.-hydroxy-5.alpha.-androstane-3.alpha.-lowe r aliphatic esters, which salts are surprisingly relatively stable in aqueous solutions, so that they provide stable aqueous injection preparations.Type: GrantFiled: August 20, 1979Date of Patent: December 2, 1980Assignee: Akzona IncorporatedInventors: Ian C. Carlyle, Thomas Sleigh, David S. Savage
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Patent number: 4232552Abstract: Novel and stable compositions of matter are disclosed which change color sharply upon a transition from a liquid state to a solid state or from a solid state to a liquid state, which change of state is at substantially a predetermined temperature corresponding to a temperature to be measured.The constituents of the novel compositions of matter comprise:1. a solvent (I) consisting of a single substance or a mixture of substances and adapted to change from a solid state at substantially a predetermined temperature to a liquid state and2. an indicator system (II) consisting of one or more substances different from (I), characterized in that(a) (II) is soluble in (I) when the latter is in the liquid phase, and(b) (II) changes color visible to the naked eye when (I) passes from the solid to the liquid phase or from the liquid to the solid phase.Thermometers containing said stable compositions of matter are also disclosed.Type: GrantFiled: September 28, 1978Date of Patent: November 11, 1980Assignee: Akzona IncorporatedInventors: Craig R. Hof, Roy A. Ulin
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Patent number: 4232042Abstract: The invention relates to novel compounds of general formula I: ##STR1## and salts, esters and amides thereof, in which R.sub.1 and R.sub.2 represent hydrogen, alkyl or alkenyl (1-4 C),R.sub.3 represents hydrogen, halogen, hydroxy, alkyl (1-4 C) or alkoxy (1-4 C),n has the value 0, 1 or 2 andALK is a saturated or unsaturated hydrocarbon radical with 3-12 carbon atoms, in which a straight carbon chain in between the benzene rings is present, containing 3-8 carbon atoms, andthe dotted line indicates an optional extra bond between the first and second carbon counted from the phenyl ring, in case of an extra bond the group R.sub.2 and one hydrogen attached to said second carbon being absent, having valuable hypocholesterolaemic and hypotriglyceriolaemic properties.Type: GrantFiled: October 4, 1976Date of Patent: November 4, 1980Assignee: Akzona IncorporatedInventors: Alexander C. Campbell, Colin L. Hewett, Filippus J. Zeelen
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Patent number: 4228240Abstract: 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 at low concentrations of peroxidase, and are relatively invulnerable to freeze-drying. Preferably, the polyvalent ions selected are those of Al, Zn, Mg, Fe, and Cu.Type: GrantFiled: January 25, 1979Date of Patent: October 14, 1980Assignee: Akzona IncorporatedInventors: Edward C. Dawson, Jan D. H. Homan, Bauke K. Van Weemen
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Patent number: 4224321Abstract: Novel and biologically active tetracyclic compounds are disclosed of the formula: ##STR1## or a pharmaceutically acceptable non-toxic salt thereof, wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, halogen, or trifluoromethyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; and X is oxygen or methylene. Pharmaceutical compositions containing these compounds are disclosed to take advantage of CNS-inhibiting properties thereof, especially sedative and tranquillizing properties.Type: GrantFiled: September 23, 1977Date of Patent: September 23, 1980Assignee: Akzona IncorporatedInventor: Willem J. van der Burg
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Patent number: 4223030Abstract: New and useful steroids of the pregnane series and compositions therefor are disclosed of the formula: ##STR1## wherein R.sub.1 is selected from the group consisting of H, F, OH, and OR.sub.2, and R.sub.2 is carbacyl of one to eighteen carbon atoms, which steroids exhibit useful pharmacological utility, to wit, progestational and/or ovulation-inhibiting activity.Type: GrantFiled: September 15, 1978Date of Patent: September 16, 1980Assignee: Akzona IncorporatedInventor: Max S. de Winter
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Patent number: 4222940Abstract: There are disclosed substrates of the formula: ##STR1## wherein: (a) R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;(b) R.sub.2 is H or C.sub.1 -C.sub.4 alkyl 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 including hydroxy, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkoxalkoxy, C.sub.1 -C.sub.7 acyloxy, and trialkylsilyloxy of less than fifteen carbons; and(d) R.sub.5(1) and R.sub.5(2) are each H, C.sub.1 -C.sub.8 alkyl, or an optionally esterified or etherified hydroxy group including hydroxy, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkoxyalkoxy, C.sub.1 -C.sub.15 trialkylsilyloxy, C.sub.4 -C.sub.8 cycloalkoxy, C.sub.1 -C.sub.7 carboxyacyloxy, or unsubstituted heterocyclic ether of five to seven members, with the proviso that at least one of R.sub.5(1) and R.sub.5(2) is hydrogen.Type: GrantFiled: October 23, 1978Date of Patent: September 16, 1980Assignee: Akzona IncorporatedInventors: Filippus J. Zeelen, Arnoldus I. A. Broess
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Patent number: 4221713Abstract: Cyclisation 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 suitable 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 carbon atoms, and trialkylsilyloxy of less than fifteen carbons;(d) R.sub.4 is methyl; and(e) R.sub.5(1) and R.sub.Type: GrantFiled: October 23, 1978Date of Patent: September 9, 1980Assignee: Akzona IncorporatedInventors: Filippus J. Zeelen, Marinus B. Groen
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Patent number: 4220599Abstract: 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.Type: GrantFiled: November 2, 1978Date of Patent: September 2, 1980Assignee: Akzona IncorporatedInventor: Johannes van der Vies