Patents by Inventor Edward Borowski
Edward Borowski has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 9745335Abstract: The invention provides semisynthetic N-substituted derivatives of the antifungal antibiotic Amphotericin B and water soluble salts and complexes, pharmaceutical compositions and plant and building treatment products comprising the derivatives and their use as antifungal antibiotics.Type: GrantFiled: June 14, 2013Date of Patent: August 29, 2017Assignee: BLIRT S.A.Inventors: Edward Borowski, Natalia Salewska, Joanna Boros-Majewska, Maria Milewska, Malgorzata Wysocka, Slawomir Milewski, Izabela Chabowska, Michal Sabisz
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Patent number: 9447136Abstract: The invention provides semisynthetic derivatives of Nystatin A1, water soluble salts and complexes, pharmaceutical compositions and plant protection products comprising the derivatives and their use, as antifungal antibiotics (Formula 1a).Type: GrantFiled: March 7, 2013Date of Patent: September 20, 2016Assignee: BLIRT S.A.Inventors: Edward Borowski, Natalia Salewska, Joanna Boros-Majewska, Maria Milewska, Malgorzata Wysocka, Slawomir Milewski, Andrzej Skladanowski, Adam Treder, Ewa Sadowska, Izabela Chabowska
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Publication number: 20150291648Abstract: The invention provides semisynthetic N-substituted derivatives of the antifungal antibiotic Amphotericin B and water soluble salts and complexes, pharmaceutical compositions and plant and building treatment products comprising the derivatives and their use as antifungal antibiotics.Type: ApplicationFiled: June 14, 2013Publication date: October 15, 2015Inventors: Edward Borowski, Natalia Salewska, Joanna Borosmajewska, Maria Milewska, Malgorzata Wysocka, Slawomir Milewski, Izabela Chabowska, Michal Sabisz
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Patent number: 9096536Abstract: The invention relates to the new, asymmetrically substituted derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione and their use as cytostatics exhibiting activity against tumor cells, especially against cells with multidrug resistance (MDR). In particular, the invention concerns derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione represented by the general formula (I).Type: GrantFiled: April 13, 2012Date of Patent: August 4, 2015Assignee: BS-154 S.P. ZO.O.Inventors: Edward Borowski, Barbara Stefanska, Maria Dzieduszycka, Marcin Cybulski, Wieslaw Szelejewski, Janusz Obukowicz, Maria Bontemps-Gracz, Malgorzata Wysocka, Jan Mazerski, Pawel Punda, Joanna Wietrzyk
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Publication number: 20150045316Abstract: The invention provides semisynthetic derivatives of Nystatin A1, water soluble salts and complexes, pharmaceutical compositions and plant protection products comprising the derivatives and their use, as antifungal antibiotics (Formula 1a).Type: ApplicationFiled: March 7, 2013Publication date: February 12, 2015Applicant: BLIRT S.A.Inventors: Edward Borowski, Natalia Salewska, Joanna Borosmajewska, Maria Milewska, Malgorzata Wysocka, Slawomir Milewski, Andrzej Skladanowski, Adam Treder, Ewa Owska, Izabela Lacka
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Publication number: 20140031357Abstract: The invention relates to the new, asymmetrically substituted derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione and their use as cytostatics exhibiting activity against tumor cells, especially against cells with multidrug resistance (MDR). In particular, the invention concerns derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione represented by the general formula (I).Type: ApplicationFiled: April 13, 2012Publication date: January 30, 2014Applicant: BS-154 SP. Z O.O.Inventors: Edward Borowski, Barbara Stefanska, Maria Dzieduszycka, Marcin Cybulski, Wieslaw Szelejewski, Janusz Obukowicz, Maria Bontemps-Gracz, Malgorzata Wysocka, Jan Mazerski, Pawel Punda, Joanna Wietrzyk
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Publication number: 20040002465Abstract: A composition having a negatively charged molecule and a cationic polyene macrolide compound having two to four positive charges that reacts with the negatively charged molecule is described. This compound can be used to vector molecules and especially nucleic acids into cells.Type: ApplicationFiled: February 26, 2003Publication date: January 1, 2004Applicants: UNIVERSITE PIERRE ET MARIE CURIE, TECHNICAL UNIVERSITY OF GDANSKInventors: Jacques Bolard, Christine Garcia, Olivier Seksek, Edward Borowski, Jolanta Grzybowska
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Patent number: 5942495Abstract: The invention relates to an N-alkyl-N-glycosyl derivative of antifungal antibiotics of the polyene macrolide group of general formula 1(a), wherein M represents polyene macrolide antibiotics residues, R represents a variable part of sugar residue, R.sup.1 represents a C.sub.1-4 alkyl group and R.sup.2 represents hydrogen or a C.sub.1-4 alkyl group; their salts of general formula 2(a), wherein R, R.sup.1, R.sup.2 and M are as herein defined and A represents an anion of organic or inorganic acid. Compounds of formula 1(b) and 2(b) wherein the N-alkyl and alkyl ester groups are represented by methyl are of particular interest.The invention relates also to processes for preparation of the compounds, to compositions containing these compounds and to their use in therapy and the treatment of external and internal fungal infections in humans and animals.Type: GrantFiled: May 16, 1997Date of Patent: August 24, 1999Assignee: BTG International LimitedInventors: Edward Borowski, Jolanta Grzybowska, Pawel Sowinski, Jerzy Gumieniak, Andrzej Czerwinski
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Patent number: 5863937Abstract: New derivatives of N.sup.3 -D-trans-2,3-epoxysuccinamoyl-L-2,3-diaminopropanoic acid of formula (1) ##STR1## wherein R.sub.1 is hydrogen; or R.sub.1 is the residue of an amino acid selected from L-valine, L-norvaline, L-leucine, L-isoleucine, L-norleucine, L-methionine, L-lysine, L-2-aminobutanoic acid, L-aspartic acid and L-glutamic acid;or R.sub.1 is the residue of a dipeptide selected from L-norvalyl-L-norvaline, L-lysyl-L-norvaline, L-methionyl-L-norvaline, L-glutamyl-L-norvaline, L-norvalyl-L-methionine, L-methionyl-L-methionine, L-leucyl-L-norvaline, L-norleucyl-L-norvaline, L-valyl-L-norvaline, L-glutamyl-L-leucine, L-asparginyl-L-norvaline and L-leucyl-L-leucine;wherein R.sub.2 is hydroxyl;or R.sub.2 is the residue of an amino acid selected from L-alanine, L-methionine, L-valine, L-norvaline, L-leucine, L-isoleucine, L-norleucine and L-2-aminobutanoic acid; with the provisos that when R.sub.1 is hydrogen then R.sub.2 is an amino acid residue and that when R.sub.Type: GrantFiled: April 8, 1996Date of Patent: January 26, 1999Assignee: BTG International LimitedInventors: Ryszard Andruszkiewicz, Henryk Chmara, Teresa Zieniawa, Edward Borowski
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Patent number: 4923965Abstract: The subject of this present invention is tripeptides of N.sup.3 -4-methoxyfumaryl-L-2,3-diaminopropanoic acid of the general formula ##STR1## where R is a hydrogen atom when R.sub.1 is the dipeptide residue containing the residue of alanine, methonine, valine, leucine or norvaline, or R and R.sub.1 have the same meaning and are the residue of monoaminomonocarboxylic aminoacid, such as those of alanine, methionine, valine, leucine, or norvaline, or R is the dipeptide residue containing the residue of alanine, methionine, valine, leucine, norvaline, lysine, ornithine, sarcosine, 2,4-diaminobutanoic acid and 2,3-diaminopropanoic acid, and R.sub.1 is a hydroxide group, and the method of their obtaining. The method of obtaining involves converting N.sup.2 -tetrbutoxycarbonyl, N.sup.3 -4-methoxyfumaroyl-L-2,3-diaminopropanoic acid into an active ester which is used for acylating a dipeptide or N.sup.2 -tetr-butoxycarbonyl, N.sup.Type: GrantFiled: July 21, 1988Date of Patent: May 8, 1990Assignee: Politechnika GdanskaInventors: Ryszard Andruszkiewicz, Henryk Chmara, Slawomir Milewski, Edward Borowski, Maria Zaremba, Jerzy Borowski
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Patent number: 4824944Abstract: The present invention relates to new enamine derivatives of daunorubicin and adriamycin of the formula l: ##STR1## and formula 2: ##STR2## wherein R denotes a hydrogen atom or hydroxyl group. The inventive compounds are useful antineoplastic antibiotics utilized in the treatment of cancer, primarily leukemia. The present derivatives demonstrate a reduction in toxicity, in particular cardiotoxicity, over their parent compounds, while retaining chemotherapeutic properties.Type: GrantFiled: January 12, 1987Date of Patent: April 25, 1989Assignee: Politechnika GdanskaInventors: Barbara J. Stefanska, Leonard S. Falkowski, Edward Borowski
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Patent number: 4783527Abstract: The invention relates to amides of polyene macrolide antibiotics and their derivatives characterized by the general formula I, ##STR1## where R is the polyene macrolide, R.sub.1 is an alkyl or isoalkyl chain of from one to eighteen carbons, unsubstituted or substituted with a primary or secondary amine; where R.sub.2 is an hydrogen or R.sub.1 or R.sub.1 and R.sub.2 are joined through the nitrogen to form a heterocyclic ring.The method of preparation of these substances according to our invention depends upon the reaction of the polyene macrolide or its derivative in which the carboxylic group is activated; in the environment of an organic solvent or mixture of solvents and in the presence of a substance neutralizing the acid; with a compound containing an amino group; leaving upon completion of the reaction; and precipitation of the product from the reaction mixture, by addition of ethyl ether or a mixture of ethyl ether with hydrocarbons; isolation and purification of the product by means of known methods.Type: GrantFiled: June 23, 1981Date of Patent: November 8, 1988Assignee: Politechnika GdanskaInventors: Leonard S. Falkowski, Andrzej B. Jarzebski, Barbara J. Stefanska, Elzbieta Troka, Edward Borowski
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Patent number: 4439363Abstract: The acetylmethyl ester of hetacyllin and/or its salts of an organic or inorganic acid are described and methods for their synthesis wherein a tertiary amine and chloroacetone are introduced to hetacyllin in an organic solvent or chloroacetone is introduced to hetacyllin in the form of a salt with an alkali metal in an organic solvent, and then from the reaction mixture, the acetylmethyl ester of hetacyllin is isolated in free form and, if desired, a salt of the ester is obtained by reaction with an organic or inorganic acid in an organic solvent.As tertiary amines, trialkylamine, N-methylpiperidine, N-ethylpiperidine or N-methylmorpholine are used; as organic solvents in obtaining the ester, dimethylformamide, dimethylacetamide or dimethylsulfoxide are used. In obtaining salts of the ester the organic solvents used are aliphatic alcohols of a chain length C.sub.2 -C.sub.5 ; ketones, preferably acetone; ethers, such as diethyl, dipropyl, diisopropyl, dibutyl ethers, or their mixtures.Type: GrantFiled: February 25, 1982Date of Patent: March 27, 1984Assignees: Politechnika Gdanska, Instytut Przemyslu Farmaceutyoznego MajakowskiegoInventors: Wojciech A. Gruszecki, Irena M. Busko-Oszczopowicz, Maria Gdulewicz-Gruszecka, Jerzy J. Cieslak, Edward Borowski, Teresa Gumiezna
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Patent number: 4365058Abstract: A process for production of esters of antibiotics from the group of polyene macrolides and of N-substituted derivatives thereof, having the general Formula 1, wherein R denotes the radical of antibiotic or of its R-COOR, I N-substituted derivative, and R.sub.1 denotes an alkyl with the chain length of C.sub.1 through C.sub.5, or an aryl, consisting therein that an antibiotic from the group of polyene macrolides or its N-substituted derivative is dissolved or suspended in alcohol and/or neutral organic solvent, or in a mixture of organic solvents, in presence of dicyclohexylcarbodiimide and/or hydrocybenzotriazole, the whole is allowed to stand at room temperature, or at temperature elevated to 40.degree. C., and then the obtained product is isolated from the reaction medium after known methods.Type: GrantFiled: July 7, 1980Date of Patent: December 21, 1982Assignee: Politechnika GdanskaInventors: Leonard S. Falkowski, Barbara J. Stefanska, Elzbieta Troka, Jerzy J. Golik, Edward Borowski
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Patent number: 4351937Abstract: The invention relates to the method of preparation of N-glycosyl compounds of anthracyclin antibiotics of formula I ##STR1## where R.sub.1 is the hydrogen atom or hydroxylic group, whereas R.sub.2 is the residue of a mono- or oligosaccharide of a series of aldeses and ketoses or the derivatives reacted with the amine group of the antibiotic. The invention depends upon the reaction of the antibiotic, which is converted into the form of base, in an organic solvent by treatment with molar excess of the saccharide or its derivative at temperature from 20.degree. up to 60.degree. C., for several hours, in the presence of a catalyst, under continuous stirring. The product is precipitated from the reaction mixture upon the addition of a nonpolar solvent and subsequently is purified by known methods.Type: GrantFiled: July 25, 1980Date of Patent: September 28, 1982Assignee: Politechnika GdanskaInventors: Barbara J. Stefanska, Leonard S. Falkowski, Edward Borowski
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Patent number: 4294958Abstract: Inorganic salts of trimethylammonium derivatives of polyene macrolides, particularly the inorganic salts of methyl esters of these derivatives having the general formula: ##STR1## wherein R is the residue of a polyene macrolide and X is an anion of a salt selected from the group consisting of methylsulphate, sulphate, chloride, phosphate and acetate.The preparation of salts of formula (I) or formula (II) is also disclosed.Type: GrantFiled: July 25, 1979Date of Patent: October 13, 1981Assignee: Politechnika GdanskaInventors: Leonard Falkowski, Barbara Stefanska, Jan Zielinski, Elzbieta Troka, Jerzy Golik, Pawel Kolodziejczyk, Andrzej Jarzebski, Emilia Cybulska, Edward Borowski
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Patent number: 4195172Abstract: The new compounds, N-methylglucamine salts of N-glycosyl derivatives of polyene macrolides particularly N-methylglucamine salts of N-glycosyl derivatives of amphotericin B, polifungin and nystatin are described herein. These compounds exhibit high pharamacological activity in some topical and sistemic fungal infections. The product is prepared by reaction of an amino group containing polyene macrolide with an aldose or ketose mono- or oligosaccharide, in an organic solvent medium or in the mixture of solvents characterized in that the formed N-glycosyl derivatives is precipitated from the reaction medium by water or with an aqueous solution of inorganic salt, preferably ammonium sulphate, and after crystallization from a higher alkanol of C.sub.3-6 atoms, preferably n-butanol transformed into a salt, preferably an N-methylglucamine salt and then crystallized from higher alkanol, preferably n-butanol.Type: GrantFiled: May 10, 1978Date of Patent: March 25, 1980Assignees: Politechnika Gdanska, Instytut Przemyslu FarmaceutycznegoInventors: Leonard Falkowski, Zuzanna Kowszyk-Gindifer, Zofia Plociennik, Jan Zielinski, Halina Dahlig, Jerzy Golik, Ewa Jakobs, Pawel Kolodziejczyk, Elzbieta Bylec, Danuta Roslik-Kaminska, Wladyslawa Wagner, Jan Pawlak, Edward Borowski
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Patent number: 4093796Abstract: A new class of polyene macrolide antibiotics which exhibit valuable therapeutic properties are obtained by reaction of said antibiotics containing at least one amino group with mono- or oligosaccharides, and/or their derivatives in a suitable solvent.A series of such have been obtained and examined. They all exhibit a high biological activity and form salts which are soluble in water.Said sugar derivatives of antibiotics can be used as antifungal agents, also as substances to reduce the overgrowth of the prostrate gland and cholesterol level in the blood.Type: GrantFiled: August 10, 1972Date of Patent: June 6, 1978Assignee: Politechnika GdanskaInventors: Leonard Falkowski, Miroslaw Bobrowski, Helena Buluk, Elzbieta Bylec, Barbara Cybulska, Jerzy Golik, Pawel Kolodziejczyk, Jan Pawlak, Andrzej Rudowski, Jan Zielinski, Tadeusz Ziminski, Edward Borowski