Abstract: A process for the preparation of novel 14.alpha., 17.alpha.-dihydroxy-17.beta.-substituted steroids by reacting 14.alpha.-hydroxy-17-oxo-steroids with metal organic compounds and the use of the said novel steroids in the production of 14.alpha., 17.alpha.-methylenedioxy-pregnane derivatives.
Type:
Grant
Filed:
February 16, 1990
Date of Patent:
March 3, 1992
Assignee:
Akzo N.V.
Inventors:
Peter M. Smid, Willem J. Van Zoest, Pieter G. Weber, Arthur F. Marx
Abstract: The invention relates to an implant of polymeric material which can release a contraceptive agent for a relatively long time when fitted subcutaneously or locally.
Abstract: Leukoregulin is identified, a biologically active lymphokine of molecular weight of about 120,000 to 140,000 with subunits of about 30,000 to 35,000, having the isoelectric focusing pH's of between 4.8 and 5.5 or between 7.5 and 8.3, which has the ability to regulate tumor cell physiology and growth without affecting the growth of normal cells. Methods for stimulating its production by mononuclear cells, method for its isolation and purification, and methods for its therapeutic uses are also disclosed.
Abstract: Disclosed are stabilized aqueous preparations containing an antidepressant in admixture with a stabilizing compound such as L-methionine, D-methionine, DL-methionine, or mixtures thereof. The stabilized preparations display better stability when exposed to light, relatively high temperatures, time, and peroxides resulting in longer shelf-lives. Antidepressants which are stabilized include mirtazapine, mianserin, septiline, and amitriptyline.
Type:
Grant
Filed:
December 3, 1990
Date of Patent:
January 21, 1992
Assignee:
Akzo N.V.
Inventors:
Petrus J. M. Van den Oetelaar, Maria M. F. Mentink
Abstract: The present invention concerns novel immunogens. These immunogens comprise novel compounds which consist of an antigen or antigenic determinant couple dot an amphiphilic adjuvant molecule and optionally also free amphiphilic adjuvant molecules. An advantageous features of these novel immunogens is the presence of both an excellent immunogen activity as well as a pronounced adjuvant activity in a single complex.
Abstract: The invention relates to sulphated K5 antigen and sulphated K5 antigen fragments containing at least 3 monosaccharide units and salts thereof, having interesting antiangiogenic and antitumor activities and a favorable ratio of the activities with respect to anticoagulant properties. In addition, the compounds can be used for the treatment of diseases caused by envelope viruses.
Type:
Grant
Filed:
March 8, 1989
Date of Patent:
December 10, 1991
Assignee:
Akzo N.V.
Inventors:
Constant A. A. van Boeckel, Gijsbert W. K. van Dedem, Neeltje A. Kraayeveld
Abstract: The present invention is concerned with a novel Mycoplasma vaccine which is avirulent for chickens and is not pathogenic for turkeys. In particular such vaccine contains the Mycoplasma strain Intervet 6/85 (deposit No. I-673 at CNCM, Pasteur Institute, Paris France).
Abstract: The invention relates to monoclonal antibodies against prosomal proteins of a prosome, said prosome having a sedimentation coefficient of approximately 19S, and to a method for detecting cancer using monoclonal antibodies specifically directed against said prosomal proteins. The invention also relates to diagnostic reagents for use in such a detection method.
Type:
Grant
Filed:
January 17, 1989
Date of Patent:
October 22, 1991
Assignee:
Pro-Soma
Inventors:
Klaus Scherrer, Maria-Fatima Grossi de Sa
Abstract: The present invention provides a pharmaceutical product for combating cancer with vincristine as active constituent, the neuropathic complications being prevented by a peptide. The product according to the invention contains:(a) vincristine or a salt thereof, and(b) a peptide having the general formula I:H--L--Met(X)--L--Glu--L--His--L--Phe--A--B--Yor a salt or an N-acyl derivative thereof in which Met(X) represents the amino acid radical Met, Met(O) or Met(O.sub.2),A represents the amino acid radical L-Lys, D-Lys, L-Arg or D-Arg,B represents the amino acid radical L-Trp or L-Phe,Y represents the hydroxyl group, an esterified hydroxyl group or an optionally substituted amino group.
Abstract: This invention relates to dopamine uptake-inhibiting compounds of the general formula I: ##STR1## wherein R.sup.1 and R.sup.2 independently are hydrogen, NO.sub.2, OH, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, unsubstituted amino or C.sub.1 -C.sub.4 alkyl substituted amino;X denotes O, S, CH.sub.2, NH or NALK;A represents C.sub.m H hd 2m or C.sub.k H.sub.2k O;l is 1 to 4;m is 0 to 2;n is 0 to 1;Q represents hydrogen, phenyl or an ALK group optionally substituted by phenyl, whereinALK is a C.sub.1 -C.sub.6 aliphatic hydrocarbon;and the acid addition salts thereof.
Abstract: A pharmaceutical composition which contains a pharmaceutically suitable carrier and the compound having the structure (7.alpha.,17.alpha.)-17-hydroxy-7-methyl-19-nor-17-pregn-5(10)-en-20-yn-3- one, characterized in that the said compound is crystalline pure and completely or virtually completely free from the other crystalline form.
Type:
Grant
Filed:
March 15, 1990
Date of Patent:
August 6, 1991
Assignee:
Akzo N.V.
Inventors:
Gerard A. J. M. T. Sas, Emile M. van Doornum
Abstract: The present invention is concerned with live combined vaccines for immunizing poultry comprising at least two different viruses, wherein at least one of the viruses is an infectious bronchitis virus showing the property of spontaneously hemagglutinating chicken erythrocytes.
Abstract: The invention relates to new oligosaccharides comprising the structure (D-ribose-D-ribitol-phosphate).sub.m, (D-ribitol-phosphate-D-ribose).sub.m or (phosphate-D-ribose-D-ribitol).sub.m, m being 2,3,4 . . . 19 or 20, to immunogens containing such oligosaccharide, to vaccines containing such immunogens and to methods for preparing such oligosaccharides, immunogens and vaccines. The vaccine is very suitable for treating infections caused by Haemophilus influenzae type b.
Type:
Grant
Filed:
December 29, 1987
Date of Patent:
July 23, 1991
Assignee:
De Staat Der Nederlanden
Inventors:
Eduard C. Beuvery, Adolf Evenberg, Jan T. Poolman, Jacobus H. van Boom, Peter Hoogerhout, Constant A. A. van Boeckel
Abstract: The use of an androstane derivative of the formula ##STR1## in which X.sup.- represents a pharmaceutically acceptable anion, or its pharmaceutically acceptable salts for the preparation of a medicament with prophylactic properties against malignant hyperthermia.
Abstract: The invention relates to .DELTA..sup.4 -androstene derivatives with aromatase-inhibiting activity having the formula: ##STR1## wherein R.sub.1 =O, (.alpha.R.sub.5,.beta.H) or N--O--R.sub.6 ;R.sub.2 =H, (1-12C)hydrocarbon radical, --SH, --S--(1-12C)-hydrocarbon radical or (1-12C)acyl;R.sub.3 =O or (.alpha.R.sub.7,.beta.R.sub.8);R.sub.4 =H or (1-12C)hydrocarbon radical;R.sub.5 =OH, O--(1-12C)hydrocarbon radical or O--(1-12C)acyl;R.sub.6 =H or (1-12C)hydrocarbon radical;R.sub.7 =H or (1-12C)hydrocarbon radical; andR.sub.8 =OH, O--(1-12C)acyl or O--(1-12C)hydrocarbon radical with the proviso that R.sub.1 is not O if R.sub.4 is H.
Type:
Grant
Filed:
March 22, 1989
Date of Patent:
July 9, 1991
Assignee:
Akzo N.V.
Inventors:
Helenius J. Kloosterboer, Hubert J. J. Loozen
Abstract: According to the present invention oil-free vaccines are provided which contain polyoxypropylenepolyoxyethylene polyols as well as an acrylic acid polymer as adjuvating constituents. These vaccines were found to show excellent immunizing properties.
Abstract: A method is provided for treating patients suffering from or susceptible to bronchoconstriction, particularly for patients suffering from an asthmatic attach which comprises the use of benzothiophene, benzofuran, dihydronaphthalene or indene derivatives represented by formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently H, (1-4C) alkyl, (1-4C) halogen substituted alkyl, OH, (1-4C) alkoxy, (1-4C) halogen substituted alkoxy, NO.sub.2, CN, halogen, an unsubstituted or (1-4C) alkyl substituted amino group, or wherein two adjacent groups R.sup.1, R.sup.2, R.sup.3 or R.sup.4 together form methylenedioxy;X is S, O or (CH.sub.2).sub.m in which m is 1 or 2;R.sup.5 is H or (1-4C) alkyl;R.sup.6 is H, NH.sub.2 or (1-4C) alkyl;R.sup.7 is H, (1-4C) alkyl or OR.sup.8 in whichR.sup.8 is H, (1-4C) alkyl or (1-8C) acyl;and its pharmaceutically acceptable salts for the preparation of a medicament with bronchodilator activity.
Type:
Grant
Filed:
July 5, 1989
Date of Patent:
June 25, 1991
Assignee:
Akzo N.V.
Inventors:
Robert T. Logan, James Redpath, George McGarry, Robert G. Roy
Abstract: The invention relates to tricyclic aromatase inhibitors, their preparation and their use in a pharmaceutical preparation.The compounds according to the invention possess the general formula I ##STR1## wherein R.sup.1 and R.sup.2 independently of one another denote H, halogen, alkyl, alkoxy, alkylthio, OH, CN, CF.sub.3, NO.sub.2, an amino group which is unsubstituted or substituted by alkyl, an NHacyl group, carbonamide or a free or esterified carboxylate group;R.sup.3 is H, alkyl, alkoxyalkyl or arylalkyl;R.sup.4 is H, OH, alkoxy or arylalkoxy;m is 1 or 2;n is 2, 3 or 4;the broken line represents an optional bond;Q denotes ##STR2## with the proviso that when R.sup.1 and R.sup.2 are H, halogen, alkyl, alkoxy or OH, m=1, n=3, the broken line does not represent a bond and Q is imidazolyl, R.sup.3 and R.sup.4 may not both be H;and also pharmaceutically acceptable salts.
Abstract: A pharmaceutical tablet that is readily divisible into sub-dosage units of two and three equal parts, said tablet comprising two surfaces on opposite sides of the tablet each having scoremarkings thereon, the scoremarkings on the one surface dividing the tablet into two equal parts and the scoremarkings on the second surface dividing the tablet into three equal parts, said tablet having an approximately triangular cross section in the plane of said scoremarked surfaces.