Patents Represented by Attorney Hugo E. Weisberger
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Patent number: 3978126Abstract: The invention relates to novel biologically active compounds of the formula I: ##SPC1##in which B is a N-hydroxy-amidino group of the general formula: ##EQU1## or ##EQU2## A represents a methylene-, ethylene- or propylene group, optionally substituted with lower alkyl groupsR stands for the number: 0, 1, 2, 3 or 4R.sub.1 is hydroxy, alkyl, alkylthio or alkoxy, halogen (F, Cl, Br or I), trifluoromethyl, nitro, amino or alkylenedioxy (1-4 C),C.sub.n H.sub.2n is an alkylene group with 0-4 carbon atomsR.sub.2 stands for hydrogen, alkyl, aryl or aralkyl,R.sub.3, r.sub.4, r.sub.5 represent hydrogen, alkyl, aralkyl or acyl, andR.sub.6 stands for hydrogen, alkyl, or phenyl or benzyl optionally substituted with methyl groupsAnd pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: July 15, 1974Date of Patent: August 31, 1976Assignee: Akzona IncorporatedInventor: Harm Jan Panneman
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Patent number: 3972932Abstract: The invention relates to compounds of the general formula: ##EQU1## in which one double bond is present between the carbon atom of the guanidine moiety and one of the adjacent nitrogen atoms andR.sub.0 stands for hydrogen, halogen, hydroxy, alkoxy or alkyl (1 to 6 C),R.sub.1, r.sub.2 for halogen, hydroxy, alkyl (1 to 4 C) or alkoxy (1 to 4 C),R.sub.3, r.sub.3 ', r.sub.3 " for hydrogen or alkyl (1 to 4 C) on the understanding that one of the substituents R.sub.3, R.sub.3 ' or R.sub.3 " is absent because of the presence of the double bond,R.sub.4 for hydrogen, alkyl (1-4 C), hydroxy, alkoxy (1-4 C) or amino optionally substituted with one or two alkyl (1 to 4 C) groups,R.sub.5, r.sub.6 for hydrogen, alkyl (1-6 C), acyl or R.sub.5 + R.sub.6 together represent an alkylidene, cyclic alklidene or aralkylidene group,As well as the acid addition salts thereof, provided that, if R.sub.4 stands for methyl and R.sub.0, R.sub.3, R.sub.3 ", R.sub.5 and R.sub.6 for hydrogen, R.sub.1 and R.sub.Type: GrantFiled: October 24, 1974Date of Patent: August 3, 1976Assignee: Akzona IncorporatedInventor: Harm Jan Panneman
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Patent number: 3972906Abstract: The present invention relates to novel 11-substituted steroids of the estrane series having the general formula ##SPC1##In whichR.sub.1 = a free, esterified or etherified hydroxyl group or halogen;R.sub.2 = an alkyl group with 1-4 C-atoms;R.sub.3 = 0 or (.alpha.Y)(.beta.Z), in which Y = H or a saturated or unsaturated alkyl group with 1-4 C-atoms and Z = a free, esterified or etherified hydroxyl group;R.sub.4 = h or a free or esterified hydroxyl group; and ring A including carbon atom 6 is ##SPC2##In whichR.sub.5 = h or a free, esterified or etherified hydroxyl group,R.sub.6 = h.sub.2, o or H(R.sub.7),R.sub.7 = a free, esterified or etherified hydroxyl group and a double bond is present starting from carbon atom 5, and to processes for their preparation.The compounds according to the present invention are of value for their contraceptive, estrogenic, progestational, ovulation-inhibiting, gonad-inhibiting and anabolic properties.Type: GrantFiled: April 15, 1975Date of Patent: August 3, 1976Assignee: Akzona IncorporatedInventors: Albertus Joannes van den Broek, Max Salomon DE Winter
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Patent number: 3966723Abstract: The invention discloses novel compounds of the general formula: ##SPC1##And salts thereof, in which the amino(alkyl) moiety is present at position 2 or 3 and in whichX 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 andn is the number 0, 1, 2 or 3,Having valuable central nervous system (CNS) activities, especially antidepressant activity.Type: GrantFiled: April 24, 1974Date of Patent: June 29, 1976Assignee: Akzona IncorporatedInventor: Willem Jacob van der Burg
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Patent number: 3965114Abstract: The invention relates to novel imidazolidine derivatives of the general formula: ##SPC1##In whichr and s = 0-5,R.sub.1 and R.sub.2 = hydroxy, halogen, alkyl or alkoxy with 1-6 carbon atoms, acyloxy with 1-8 carbon atoms or a trifluoromethyl group, R.sub.3 = hydrogen, and alkyl group with 1-6 carbon atoms, an aryl group or an aralkyl group (7-9 C)as well as pharmaceutically acceptable salts thereof, having valuable anticholinergic and anticonvulsive activities.Type: GrantFiled: September 4, 1974Date of Patent: June 22, 1976Assignee: Akzona IncorporatedInventor: Willem Jacob van der Burg
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Patent number: 3950425Abstract: The invention discloses novel compounds of the general formula: ##SPC1##And salts thereof,In whichX 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 stands 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) activites, especially antidepressant activity.The invention further discloses novel intermediates of the general formula: ##SPC2##As well as biologically active intermediates of the formula: ##SPC3##As well as salts and esters thereof.Type: GrantFiled: April 24, 1974Date of Patent: April 13, 1976Assignee: Akzona IncorporatedInventor: Willem Jacob van der Burg
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Patent number: 3947478Abstract: The invention relates to novel alkylated steroids of the pregnane series having the formula: ##SPC1##, whereinX = a member of the group consisting of H and halogen;Y = a member of the group consisting of H.sub.2, H(OH), H(OAcyl) and O;R.sub.1 = a member of the group consisting of H, CH.sub.3 and halogen;R.sub.2 = alkyl having 1-4 carbon atoms;R.sub.3 = a member of the group consisting of H (except when Y = H.sub.2), OAcyl, Oalkyl, and CH.sub.3 ;R.sub.4 = a member of the group consisting of H and alkyl having 1-4 carbon atoms and in which at least one of the substituents R.sub.3 and R.sub.4 is alkyl; andC.sub.1 -c.sub.2 and C.sub.6 -C.sub.7 are selected from a saturated and an unsaturated bond.The novel compounds possess strong anti-inflammatory properties and are useful in the treatment of inflammatory conditions especially those associated with the skin and allergic reactions.Type: GrantFiled: November 22, 1974Date of Patent: March 30, 1976Assignee: Akzona IncorporatedInventors: Gilbert Frederick Woods, James Cairns, George McGarry
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Patent number: 3944576Abstract: The invention relates to novel 7-substituted-steroids of the oestrane series of the general formula: ##SPC1##In whichRing A including carbon atom 6 is ##SPC2##R.sub.1 = an alkyl group with 1-4 C-atoms,R.sub.2 = oxygen or (.alpha.Y)(.beta.Z), in which Y = hydrogen or a saturated or unsaturated alkyl group with 1-4 C-atoms and Z = a free, esterified or etherified hydroxyl group,R.sub.3 = hydrogen or a free or esterified hydroxyl group,R.sub.4 = an alkylene- or alkylidene group with 1-3 C-atoms,R.sub.5 = hydrogen or a free, esterified or etherified hydroxyl group,R.sub.6 = H.sub.2, O, H(OH), H(Oalkyl) or H(Oacyl),X = H, an acyl group or an alkyl-, aralkyl-, cycloalkyl- or heterocyclic alkyl group, andA double bond is present starting from carbon atom 5, and to processes for their preparation.These novel steroids possess anabolic, androgenic, oestrogenic, progestative, ovulation-inhibiting and gonad-inhibiting properties.Type: GrantFiled: March 27, 1974Date of Patent: March 16, 1976Assignee: Akzona IncorporatedInventors: Albertus Joannes van den Broek, Jacob DE Visser
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Patent number: 3933675Abstract: Improved curing agents having long pot life for use with urethane elastomers are prepared by reacting orthochloroaniline, an ester of anthranilic acid, and formaldehyde in selected molar ratios in an acid medium.Type: GrantFiled: April 3, 1974Date of Patent: January 20, 1976Assignee: Anderson Development CompanyInventor: Joseph Theodore Willett