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1. 发明授权

US5942495A Antibiotics 失效
标题翻译：抗生素
公开(公告)号：US5942495A
公开(公告)日：1999-08-24
申请号：US857281
申请日：1997-05-16
申请人： Edward Borowski , Jolanta Grzybowska , Pawel Sowinski , Jerzy Gumieniak , Andrzej Czerwinski
发明人： Edward Borowski , Jolanta Grzybowska , Pawel Sowinski , Jerzy Gumieniak , Andrzej Czerwinski
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08
摘要： 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. ##STR1##
摘要翻译：本发明涉及通式1（a）的多烯大环内酯类抗真菌抗生素的N-烷基-N-糖基衍生物，其中M表示多烯大环内酯抗生素残基，R表示糖残基的可变部分，R1表示C1 -4-烷基，R 2表示氢或C 1-4烷基; 其通式2（a）的盐，其中R，R 1，R 2和M如本文所定义，A代表有机或无机酸的阴离子。特别令人感兴趣的是其中N-烷基和烷基酯基由甲基表示的式1（b）和2（b）的化合物。本发明还涉及制备化合物的方法，含有这些化合物的组合物及其在治疗和治疗人和动物中的外部和内部真菌感染中的用途。

2. 发明授权

US4439363A Acetylmethyl ester of hetacyllin and/or salts of this ester 失效
标题翻译： hetacyllin的乙酰基甲酯和/或该酯的盐
公开(公告)号：US4439363A
公开(公告)日：1984-03-27
申请号：US352118
申请日：1982-02-25
申请人： Wojciech A. Gruszecki , Irena M. Busko-Oszczopowicz , Maria Gdulewicz-Gruszecka , Jerzy J. Cieslak , Edward Borowski , Teresa Gumiezna
发明人： Wojciech A. Gruszecki , Irena M. Busko-Oszczopowicz , Maria Gdulewicz-Gruszecka , Jerzy J. Cieslak , Edward Borowski , Teresa Gumiezna
IPC分类号： C07D499/08 , A61K31/415 , A61K31/43 , A61P31/04 , C07D20060101 , C07D499/46 , C07D499/64 , C07D499/68 , C07D499/80
CPC分类号： C07D499/80
摘要： 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.The obtained compounds show an antibacterial action like ampicillin but after administration per os they show a considerably higher level of the antibiotic than that after administration of free ampicillin or its esters.
摘要翻译：描述了hetacyllin的乙酰甲基酯和/或其有机或无机酸的盐，并将其合成方法，其中叔胺和氯丙酮在有机溶剂或氯丙酮中引入hetacyllin，以盐的形式引入到hetacyllin中，在有机溶剂中的碱金属，然后从反应混合物中分离出游离形式的海参酰基乙酰甲基酯，如果需要，通过在有机溶剂中与有机或无机酸反应获得酯的盐。作为叔胺，使用三烷基胺，N-甲基哌啶，N-乙基哌啶或N-甲基吗啉; 作为获得酯的有机溶剂，使用二甲基甲酰胺，二甲基乙酰胺或二甲基亚砜。在获得酯的盐时，使用的有机溶剂是链长C 2 -C 5的脂族醇; 酮，优选丙酮; 醚，如二乙基，二丙基，二异丙基，二丁基醚或它们的混合物。所得化合物显示出抗菌作用，如氨苄青霉素，但是在施用之后，它们显示比施用游离氨苄青霉素或其酯后显着高得多的抗生素水平。

3. 发明授权

US4093796A Antibiotic derivatives of polyene macrolide group and method of obtaining the same 失效
标题翻译：多烯大环内酯类抗生素衍生物及其获得方法
公开(公告)号：US4093796A
公开(公告)日：1978-06-06
申请号：US279737
申请日：1972-08-10
申请人： Leonard Falkowski , Miroslaw Bobrowski , Helena Buluk , Elzbieta Bylec , Barbara Cybulska , Jerzy Golik , Pawel Kolodziejczyk , Jan Pawlak , Andrzej Rudowski , Jan Zielinski , Tadeusz Ziminski , Edward Borowski
发明人： Leonard Falkowski , Miroslaw Bobrowski , Helena Buluk , Elzbieta Bylec , Barbara Cybulska , Jerzy Golik , Pawel Kolodziejczyk , Jan Pawlak , Andrzej Rudowski , Jan Zielinski , Tadeusz Ziminski , Edward Borowski
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07G11/00 , C07H17/08
CPC分类号： C07H17/08
摘要： 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.
摘要翻译：通过将含有至少一个氨基的所述抗生素与单糖或寡糖和/或其衍生物在合适的溶剂中反应，可获得出现有价值的治疗性质的新一类多烯大环内酯类抗生素。

4. 发明授权

US4783527A Amides of amphoteric polyene macrolide antibiotics 失效
标题翻译：酰胺两性多烯大环内酯类抗生素
公开(公告)号：US4783527A
公开(公告)日：1988-11-08
申请号：US276462
申请日：1981-06-23
申请人： Leonard S. Falkowski , Andrzej B. Jarzebski , Barbara J. Stefanska , Elzbieta Troka , Edward Borowski
发明人： Leonard S. Falkowski , Andrzej B. Jarzebski , Barbara J. Stefanska , Elzbieta Troka , Edward Borowski
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07C11/00 , C07C237/26 , C07H5/06 , C07H17/08 , C12P19/62
CPC分类号： C07H17/08 , C12P19/62
摘要： 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.
摘要翻译：本发明涉及多烯大环内酯抗生素及其衍生物的酰胺，其特征在于通式I，其中R是多烯大环内酯，R1是具有1至18个碳的烷基或异烷基链，未被取代或被一个或多个仲胺; 其中R 2是氢或R 1或R 1和R 2通过氮连接形成杂环。根据本发明的这些物质的制备方法取决于多烯大环内酯或其衍生物的羧基被活化的反应; 在有机溶剂或溶剂混合物的环境中和在中和酸的物质的存在下进行; 与含有氨基的化合物; 完成反应后离开; 并从反应混合物中沉淀产物，加入乙醚或乙醚与烃的混合物; 通过已知方法分离和纯化产物。

5. 发明授权

US4294958A Water-soluble salts of trimethylammonium derivatives of polyene macrolide antibiotics and the preparation thereof 失效
标题翻译：多烯大环内酯类抗生素的三甲基铵衍生物的水溶性盐及其制备方法
公开(公告)号：US4294958A
公开(公告)日：1981-10-13
申请号：US60427
申请日：1979-07-25
申请人： Leonard Falkowski , Barbara Stefanska , Jan Zielinski , Elzbieta Troka , Jerzy Golik , Pawel Kolodziejczyk , Andrzej Jarzebski , Emilia Cybulska , Edward Borowski
发明人： Leonard Falkowski , Barbara Stefanska , Jan Zielinski , Elzbieta Troka , Jerzy Golik , Pawel Kolodziejczyk , Andrzej Jarzebski , Emilia Cybulska , Edward Borowski
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： 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.
摘要翻译：多烯大环内酯的三甲基铵衍生物的无机盐，特别是具有以下通式的这些衍生物的甲基酯的无机盐：其中R是多烯大环内酯的残基，X是选自以下的盐的阴离子：硫酸盐，氯化物，磷酸盐和乙酸盐。还公开了式（I）或式（II）的盐的制备。

6. 发明申请

US20140031357A1 ASYMMETRICALLY SUBSTITUTED ANTHRAPYRIDAZONE DERIVATIVES AS CYTOSTATICS 有权
标题翻译：作为细胞周期的非对称取代的蒽环类衍生物
公开(公告)号：US20140031357A1
公开(公告)日：2014-01-30
申请号：US14111022
申请日：2012-04-13
申请人： Edward Borowski , Barbara Stefanska , Maria Dzieduszycka , Marcin Cybulski , Wieslaw Szelejewski , Janusz Obukowicz , Maria Bontemps-Gracz , Malgorzata Wysocka , Jan Mazerski , Pawel Punda , Joanna Wietrzyk
发明人： Edward Borowski , Barbara Stefanska , Maria Dzieduszycka , Marcin Cybulski , Wieslaw Szelejewski , Janusz Obukowicz , Maria Bontemps-Gracz , Malgorzata Wysocka , Jan Mazerski , Pawel Punda , Joanna Wietrzyk
IPC分类号： C07D237/26 , C07D487/06
CPC分类号： C07D237/26 , A61K31/502 , A61K31/5025 , C07D237/36 , C07D487/06
摘要： 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).
摘要翻译：本发明涉及2,7-二氢-3H-二苯并[de，h]噌啉-3,7-二酮的新的不对称取代的衍生物及其作为细胞抑制剂的用途，其表现出对肿瘤细胞的活性，特别是抗多药耐药性细胞 MDR）。特别地，本发明涉及由通式（I）表示的2,7-二氢-3H-二苯并[de，h]噌啉-3,7-二酮的衍生物。

7. 发明授权

US4365058A Method of preparation of esters of antibiotics selected from the group consisting of polyene macrolides and of N-substituted derivatives thereof 失效
标题翻译：制备选自多烯大环内酯类及其N-取代衍生物的抗生素酯的方法
公开(公告)号：US4365058A
公开(公告)日：1982-12-21
申请号：US166598
申请日：1980-07-07
申请人： Leonard S. Falkowski , Barbara J. Stefanska , Elzbieta Troka , Jerzy J. Golik , Edward Borowski
发明人： Leonard S. Falkowski , Barbara J. Stefanska , Elzbieta Troka , Jerzy J. Golik , Edward Borowski
IPC分类号： C07G11/00 , A61K31/7048 , C07H17/08
CPC分类号： C07H17/08
摘要： 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.
摘要翻译：具有通式1的多烯大环内酯类和N-取代的衍生物的抗生素酯的制备方法，其中R表示抗生素或其R-COOR，I N-取代的衍生物和R1的基团表示链长为C1至C5的烷基或其中包含多烯大环内酯类或其N-取代衍生物的抗生素溶解或悬浮在醇和/或中性有机溶剂中或在混合物中的芳基的有机溶剂中，在二环己基碳二亚胺和/或氢氰苯并三唑的存在下，将其全部在室温下放置，或在升至40℃的温度下放置，然后将所得产物从已知方法中分离出来。

8. 发明授权

US09096536B2 Asymmetrically substituted anthrapyridazone derivatives as cytostatics 有权
标题翻译：不对称取代的蒽代哒嗪衍生物作为细胞抑制剂
公开(公告)号：US09096536B2
公开(公告)日：2015-08-04
申请号：US14111022
申请日：2012-04-13
申请人： Edward Borowski , Barbara Stefanska , Maria Dzieduszycka , Marcin Cybulski , Wieslaw Szelejewski , Janusz Obukowicz , Maria Bontemps-Gracz , Malgorzata Wysocka , Jan Mazerski , Pawel Punda , Joanna Wietrzyk
发明人： Edward Borowski , Barbara Stefanska , Maria Dzieduszycka , Marcin Cybulski , Wieslaw Szelejewski , Janusz Obukowicz , Maria Bontemps-Gracz , Malgorzata Wysocka , Jan Mazerski , Pawel Punda , Joanna Wietrzyk
IPC分类号： C07D237/26 , C07D487/06 , A61K31/502 , A61K31/5025 , C07D237/36
CPC分类号： C07D237/26 , A61K31/502 , A61K31/5025 , C07D237/36 , C07D487/06
摘要： 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).
摘要翻译：本发明涉及2,7-二氢-3H-二苯并[de，h]噌啉-3,7-二酮的新的不对称取代的衍生物及其作为细胞抑制剂的用途，其表现出对肿瘤细胞的活性，特别是抗多药耐药性细胞 MDR）。特别地，本发明涉及由通式（I）表示的2,7-二氢-3H-二苯并[de，h]噌啉-3,7-二酮的衍生物。

9. 发明授权

US5863937A Pharmaceutical compositions 失效
标题翻译：药物组合物
公开(公告)号：US5863937A
公开(公告)日：1999-01-26
申请号：US624559
申请日：1996-04-08
申请人： Ryszard Andruszkiewicz , Henryk Chmara , Teresa Zieniawa , Edward Borowski
发明人： Ryszard Andruszkiewicz , Henryk Chmara , Teresa Zieniawa , Edward Borowski
IPC分类号： A61K38/00 , A01N25/02 , A01N25/10 , A01N37/18 , A61P31/04 , A61P31/10 , C07K1/06 , C07K5/06 , C07K5/062 , C07K5/068 , C07K5/072 , C07K5/083 , C07K5/09 , C07K5/093 , A61K31/335
CPC分类号： C07K5/0819 , C07K5/06034 , C07K5/0606 , C07K5/06086 , C07K5/0808 , C07K5/081 , C07K5/0815 , A61K38/00
摘要： 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.1 is an amino acid residue or a peptide residue then R.sub.2 is hydroxyl; the derivative optionally being in the form of a physiologically acceptable salt thereof; are of value as antimicrobial agents, particularly as antifungal agents, especially in relation to Candida albicans.
摘要翻译： PCT No.PCT / GB94 / 02162 Sec。 371日期：1996年4月8日 102（e）日期1996年4月8日PCT 1994年10月5日PCT PCT。出版物WO95 / 09867 日期1995年4月13日公式（1）的N 3 -D-反式-2,3-环氧琥珀酰基甲酰基-L-2,3-二氨基丙酸的新衍生物是选自L-缬氨酸，L-正缬氨酸，L L-亮氨酸，L-异亮氨酸，L-正亮氨酸，L-甲硫氨酸，L-赖氨酸，L-2-氨基丁酸，L-天冬氨酸和L-谷氨酸; 或R1是选自L-缬氨酰-L-正缬氨酸，L-赖氨酰-L-正缬氨酸，L-甲硫氨酰-L-正缬氨酸，L-谷氨酰-L-正缬氨酸，L-缬氨酰-L-甲硫氨酸的二肽的残基， L-赖氨酰-L-正缬氨酸，L-亮氨酰-L-正缬氨酸，L-正亮氨酰-L-正缬氨酸，L-缬氨酰-L-正缬氨酸，L-谷氨酰-L-亮氨酸，L-天冬氨酰-L-正缬氨酸和L- 亮氨酰-L-亮氨酸; 其中R2是羟基; 或R2是选自L-丙氨酸，L-甲硫氨酸，L-缬氨酸，L-正缬氨酸，L-亮氨酸，L-异亮氨酸，L-正亮氨酸和L-2-氨基丁酸的氨基酸的残基; 条件是当R1为氢时，则R2为氨基酸残基，当R1为氨基酸残基或肽残基时，则R2为羟基; 所述衍生物任选地为其生理上可接受的盐的形式; 作为抗微生物剂，特别是作为抗真菌剂，特别是与白色念珠菌有关。

10. 发明授权

US4923965A Tripeptides of N.sup.3 -4-methoxyfumaryl-L-2,3-diaminopropanoic acid 失效
标题翻译： N3-4-甲氧基芳香基-L-2,3-二氨基丙酸的三肽
公开(公告)号：US4923965A
公开(公告)日：1990-05-08
申请号：US222190
申请日：1988-07-21
申请人： Ryszard Andruszkiewicz , Henryk Chmara , Slawomir Milewski , Edward Borowski , Maria Zaremba , Jerzy Borowski
发明人： Ryszard Andruszkiewicz , Henryk Chmara , Slawomir Milewski , Edward Borowski , Maria Zaremba , Jerzy Borowski
IPC分类号： C07K20060101 , C07K5/02 , C07K5/083 , C07K5/09
CPC分类号： C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0815
摘要： 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.3 -4-methoxyfumaryl-L-2,3-diaminopropanoic acid into an active ester which is used for acylating the aminoacid whereafter the protection of the amino group is removed and the latter is acylated with an active ester of the N-protected aminoacid or N.sup.3 -4-methoxyfumaryl-L-2,3-diaminopropanoic acid is acylated with an active ester of the N-protected dipeptide and the protection of the amino group is removed from the obtained N-protected tripeptide in the medium of a non-polar organic solvent or its mixture with water, whereas the final product in the form of a salt is isolated by being crystallized or being converted into a free acid.

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