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1. 发明授权

US5244880A Stable aqueous solutions of prymicin and pharmaceutical and cosmetic compositions containing these solutions 失效
标题翻译：稳定的含有这些溶液的蛋白质水溶液和药物和化妆品组合物
公开(公告)号：US5244880A
公开(公告)日：1993-09-14
申请号：US835097
申请日：1992-02-11
申请人： Peter Szentmiklosi , Tamas Szuts , Gyorgy Hidasi , Istvan Juhasz
发明人： Peter Szentmiklosi , Tamas Szuts , Gyorgy Hidasi , Istvan Juhasz
IPC分类号： A61K47/22
CPC分类号： A61K31/70 , A61K47/22 , A61K8/602 , A61K9/0014 , A61Q17/005 , A61K2800/52 , Y10S514/844 , Y10S514/97
摘要： The invention relates to novel stable aqueous primycin solutions containing 0.5 to 1.75% by mass/volume of primycin sulfate or 2.5 to 9% by mass/volume of a complex of primycin N-methylpyrrolidone and 2 to 15% by mass/volume of pyroglutamic acid, preferably L-pyroglutamic acid or a soluble salt, preferably the sodium salt thereof as calculated for the volume of the solution to be prepared and 40 to 60% by volume of isopropanol as calculated for the volume of the solution to be prepared as well as water in an amount adding up to 100%. The stable, aqueous primycin solutions are topical antibiotics.
摘要翻译：本发明涉及含有0.5〜1.75质量％/体积的硫酸伯霉素或2.5〜9质量％体积的伯霉素N-甲基吡咯烷酮和2〜15质量％的焦谷氨酸复合物的新型稳定含水伯霉素溶液，优选L-焦谷氨酸或可溶性盐，优选其钠盐，根据制备溶液的体积计算，和40至60体积％的异丙醇，根据所制备的溶液的体积计算，以及水量达100％。稳定的含水伯霉素溶液是局部抗生素。

2. 发明授权

US4460771A Antiphlogistic and anticoagulant condensed pyrimidine derivatives 失效
标题翻译：消炎和抗凝血嘧啶衍生物
公开(公告)号：US4460771A
公开(公告)日：1984-07-17
申请号：US742464
申请日：1976-11-17
申请人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermes , Agnes Horvath , Sandor Virag , Lelle Vasvari nee Debreczy , Agoston David
发明人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermes , Agnes Horvath , Sandor Virag , Lelle Vasvari nee Debreczy , Agoston David
IPC分类号： A61K31/505 , A61K31/519 , A61P7/02 , A61P25/04 , A61P29/00 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： New optionally racemic or optically active pyrimido(1,2a) heterocyclic compounds of the formula ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is an alkyl group containing one to six carbon atoms,R.sup.1 is hydrogen, alkyl containing one to six carbon atoms,R.sup.2 is hydrogen, alkyl containing one to six carbon atoms, optionally substituted amino, optionally substituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sup.1 and R.sup.2 together form a --(CH.dbd.CH).sub.2 -- group attached to the two adjacent carbon atoms of the ring A and the broken line represents a chemical bond,R.sup.3 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl or optionally substituted hydroxy,R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl orR.sup.3 and R.sup.4 together with the nitrogen can form an optionally substituted five-, six- or seven-membered ring, which can contain a further heteroatom or heteroatoms,R.sup.5 is oxygen or an optionally substituted imino group are disclosed as well as a process for the preparation thereof.
摘要翻译：新的任选的外消旋或光学活性嘧啶（1,2a）杂环化合物，其中m为0,1或2，n为0,1或2，R为含有1至6个碳原子的烷基，R 1为是氢，含有1至6个碳原子的烷基，R 2是氢，含1至6个碳原子的烷基，任选取代的氨基，任选取代的羟基，羧基或衍生自羧酸的基团或R 1和R 2一起形成 - （CH = CH）连接到环A的两个相邻碳原子上的2-基团，虚线表示化学键，R 3是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基，任选取代的酰基或任选取代的羟基，R 4是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基，选择可以将氮取代的酰基或R3和R4与氮一起形成任选取代的五元，六元或七元环，其可以含有另外的杂原子或杂原子，R5是氧或任选取代的亚氨基，其制备方法。

3. 发明授权

US4219649A Pyrido[1,2-a]pyrimidine derivatives 失效
标题翻译：吡啶并[1,2-a]嘧啶衍生物
公开(公告)号：US4219649A
公开(公告)日：1980-08-26
申请号：US934801
申请日：1978-08-17
申请人： Josef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
发明人： Josef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
IPC分类号： A61K31/505 , A61K31/519 , A61P25/04 , A61P29/00 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04
摘要： Compounds of the formula: ##STR1## or pharmaceutically acceptable acid addition or quaternary ammonium salts thereofwhereinR.sup.2 is C.sub.1 to C.sub.6 alkyl:R.sup.3 is C.sub.1 to C.sub.6 alkyl;R.sup.4 is a single electron pair, hydrogen or lower alkyl; and the dotted lines indicate saturated or unsaturated bonds, are disclosed with analgesic properties.
摘要翻译：下式的化合物或其药学上可接受的酸加成盐或季铵盐，其中R 2为C 1至C 6烷基：R 3为C 1至C 6烷基; R4是单电子对，氢或低级烷基; 虚线表示饱和或不饱和键，具有镇痛特性。

4. 发明授权

US4199560A Solid oral pharmaceutical product with increased efficacy and predetermined steady state of solubility 失效
标题翻译：固体口服药物具有增加的疗效和预定的稳定状态的溶解度
公开(公告)号：US4199560A
公开(公告)日：1980-04-22
申请号：US952932
申请日：1978-10-19
申请人： Laszlo Gyarmati , Istvan Racz , Peter Szentmiklosi , Janos Plachy
发明人： Laszlo Gyarmati , Istvan Racz , Peter Szentmiklosi , Janos Plachy
IPC分类号： A61K9/16 , A61K9/20 , A61K9/22 , A61K9/48 , A61K9/26 , A61K9/54 , A61K33/06
CPC分类号： A61K9/1652 , A61K9/1617 , A61K9/2077 , A61K9/4841
摘要： The present invention relates to a solid oral pharmaceutical preparation with protracted release of the active ingredient consisting of discrete solid granules containing the active ingredient soluble in the stomach and auxiliary agents and of an equally solid external phase surrounding the said granules, whereby the granules forming the internal phase consist of granules prepared from a powder mixture which contains as active ingredient, or in addition to it a non-toxic metal compound, being capable of binding an acid, and being insoluble or but slightly soluble in neutral aqueous medium--particularly bismuth, aluminium or magnesium compound--and auxiliary materials prepared with an aqueous emulsion containing a hydrophobic component and hydrophylic emulsifiers, and the external phase contains a solid, dry, amphoteric gel forming substance in an amount of 1-50 percent w/w related to the total weight of the preparation in admixture with auxiliary agents.The preparation is produced by the wetting of the powder mixture containing the basic metal compound, auxiliary material and in given case additional active ingredient with the aqueous emulsion of the hydrophobic component prepared by applying the hydrophylic emulsifiers then by granulation and admixing the dried granules with the amphoteric gel forming substance, and pressing it into tablets, or filling into capsules.
摘要翻译：本发明涉及具有长时间释放的活性成分的固体口服药物制剂，其由分散的固体颗粒组成，所述固体颗粒含有可溶于胃的活性成分和辅助剂以及围绕所述颗粒的同样固体的外部相，其中颗粒形成内相包含由粉末混合物制成的颗粒，所述粉末混合物含有作为活性成分的粉末混合物，或除此之外，还含有无毒金属化合物，其能够结合酸，并且在中性水性介质（特别是铋）中不溶或略微溶解，铝或镁化合物以及用含有疏水组分和亲水乳化剂的水性乳液制备的辅助材料，并且外相含有与总量相关的1-50％w / w的固体，干燥，两性凝胶形成物质制剂的重量与助剂混合。该制备是通过润湿包含碱性金属化合物，辅助材料的粉末混合物，并且在给定情况下，通过施用亲水性乳化剂制备疏水组分的水性乳液，然后通过造粒和将干燥颗粒与两性凝胶形成物质，并将其压制成片剂或填充到胶囊中。

5. 发明授权

US3954986A Pharmaceutical composition having synergistic analgesic activity 失效
标题翻译：具有协同止痛活性的药物组合物
公开(公告)号：US3954986A
公开(公告)日：1976-05-04
申请号：US415749
申请日：1973-11-14
申请人： Jozsef Knoll , Zsuzsanna Furst , Zoltan Meszaros , Peter Szentmiklosi , Agoston David , Istvan Hermecz , Attila Mandi , Rezso Bognar , Sandor Makleit , Gyula Valovics , Laszlo Szlavik , Sandor Nagy
发明人： Jozsef Knoll , Zsuzsanna Furst , Zoltan Meszaros , Peter Szentmiklosi , Agoston David , Istvan Hermecz , Attila Mandi , Rezso Bognar , Sandor Makleit , Gyula Valovics , Laszlo Szlavik , Sandor Nagy
IPC分类号： A61K31/655 , A61K31/505 , A61K31/485
CPC分类号： A61K31/655
摘要： An analgesic substitute for morphine comprising the synergistic combination of azidomorphine or azidocodeine with a pyrimidazolium.
摘要翻译：吗啡的止痛剂替代物，其包含叠氮吗啡或叠氮基与佐剂的协同组合。

6. 发明授权

US4670440A Medicinal norfloxacin salts 失效
标题翻译：药用诺氟沙星盐
公开(公告)号：US4670440A
公开(公告)日：1987-06-02
申请号：US854395
申请日：1986-04-21
申请人： Tamas Szuts , Peter Szentmiklosi , Jozsef Lengyel , Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Geza Kerszturi , Gabor Kovacs , Gabor Horvath , Katalin Marmarosi nee Kellner
发明人： Tamas Szuts , Peter Szentmiklosi , Jozsef Lengyel , Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Geza Kerszturi , Gabor Kovacs , Gabor Horvath , Katalin Marmarosi nee Kellner
IPC分类号： A23K1/16 , A61K31/4709 , A61K31/495 , A61K31/496 , A61P31/04 , C07C67/00 , C07C213/00 , C07C215/40 , C07D215/56 , C07D401/10 , C07D401/04
CPC分类号： C07D215/56
摘要： N,N,N-trimethyl-2-hydroxyethyl-ammonium-[1-ethyl-6-fluoro-4-oxo-7-(1-piperazinyl)-1,4-dihydro-quinolizine-3-carboxylate] of the formula I ##STR1## as a norfloxacin antimicrobial salt capable of enteral administration.
摘要翻译： N，N，N-三甲基-2-羟乙基 - 铵 - [1-乙基-6-氟-4-氧代-7-（1-对异哌嗪基）-1,4-二氢 - 喹嗪-3-羧酸酯] 配方I 作为能够肠内给药的诺氟沙星抗微生物盐。

7. 发明授权

US4666912A Treating process 失效
标题翻译：治疗过程
公开(公告)号：US4666912A
公开(公告)日：1987-05-19
申请号：US715190
申请日：1985-03-22
申请人： Zoltan Meszaros , Jozse Knoll , Istvan Hurmecz , Peter Szentmiklosi , Agnes Horvath , Lelle Vasvari nee Debreczy , Gabor Kovacs , Klara Gyires , Sandor Virag
发明人： Zoltan Meszaros , Jozse Knoll , Istvan Hurmecz , Peter Szentmiklosi , Agnes Horvath , Lelle Vasvari nee Debreczy , Gabor Kovacs , Klara Gyires , Sandor Virag
IPC分类号： C07D471/04 , A61K31/505 , A61P1/04
CPC分类号： A61K31/505 , Y10S514/926 , Y10S514/927
摘要： The invention relates to a process for the restoration and prevention of gastrointestinal injuries, which comprises treating a patient with an effective dose of racemic or optically active 1,6-dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrimido[1,2-a]pyrimidine-3-carboxamide.
摘要翻译：本发明涉及一种恢复和预防胃肠道损伤的方法，其包括用有效剂量的外消旋或光学活性的1,6-二甲基-4-氧代-1,6,7,8,9,9a - 六氢-4H-嘧啶并[1,2-a]嘧啶-3-甲酰胺。

8. 发明授权

US4495189A Condensed pyrimidines 失效
标题翻译：浓缩嘧啶
公开(公告)号：US4495189A
公开(公告)日：1985-01-22
申请号：US364753
申请日：1982-04-02
申请人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermecz , Agnes Horvath , Sandor Virag , Lelle Vasvari , Agoston David
发明人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermecz , Agnes Horvath , Sandor Virag , Lelle Vasvari , Agoston David
IPC分类号： C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： New compounds of the following formula are disclosed:1,6-dimethyl-3-carbamoyl-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)-pyrimidine;1,6-dimethyl-3-(N-tertiary-butyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-(N-2-phenethyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-[N-(3,3-diphenyl-propyl)-carbamoyl]-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-(N-phenyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine; and1,6-dimethyl-3-(N-methyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine, as well as pharmaceutical compositions containing these compounds and a method of inhibiting thrombocyte aggregation in mammals employing a pharmaceutically effective amount of at least one of these compounds.
摘要翻译：公开了下式的新化合物：1,6-二甲基-3-氨基甲酰基-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a） - 吡啶亚胺; 1,6-二甲基-3-（N-叔丁基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶; 1,1-二甲基-3-（N-2-苯乙基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-哒嗪（1,2-a）嘧啶; 1,6-二甲基-3- [N-（3,3-二苯基 - 丙基） - 氨基甲酰基] -4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶 ; 1,6-二甲基-3-（N-苯基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶; 和1,6-二甲基-3-（N-甲基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶，以及含有这些的药物组合物化合物和使用药学上有效量的这些化合物中的至少一种来抑制哺乳动物血小板聚集的方法。

9. 发明授权

US4291036A Pyrido[1,2-A]pyrimidine derivatives and method of analgesic treatment 失效
标题翻译：吡啶并[1,2-A]嘧啶衍生物和镇痛治疗方法
公开(公告)号：US4291036A
公开(公告)日：1981-09-22
申请号：US130371
申请日：1980-03-14
申请人： Jozsef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
发明人： Jozsef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
IPC分类号： A61K31/505 , A61K31/519 , A61P25/04 , A61P29/00 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04
摘要： Compounds of the formula ##STR1## or pharmaceutically acceptable acid-addition or quaternart ammonium salts thereofwhereinR is hydroxy, carboxy, lower alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, carbamoyl, N-loweralkyl-carbamoyl, N,N-dilower-alkyl-carbamoyl, carboazido, carbohydrazido or cyano;R.sup.2 is C.sub.1 to C.sub.6 alkyl;R.sup.3 is C.sub.1 to C.sub.6 alkyl or benzyl; andR.sup.4 is a single electron pair, hydrogen or lower alkyl; and the dotted lines represent saturated or unsaturated bonds, are disclosed with analgesic properties.
摘要翻译：其中R是羟基，羧基，低级烷氧基羰基，苄氧基羰基，苯氧基羰基，氨基甲酰基，N-低级烷基 - 氨基甲酰基，N，N-二 - 低级烷基 - 氨基甲酰基，碳氮杂，碳酰肼基或氰基; R2是C1-C6烷基; R3是C1-C6烷基或苄基; R4是单电子对，氢或低级烷基; 并且虚线表示饱和或不饱和键，其具有镇痛特性。

10. 发明授权

US5064815A Primycin-containing colloidal basic gel 失效
标题翻译：含乳液的胶体基础凝胶
公开(公告)号：US5064815A
公开(公告)日：1991-11-12
申请号：US500236
申请日：1990-03-26
申请人： Peter Szentmiklosi , Tamas Szuts , Jozsef Nemes , Jozsef Lengyel , Jeno Marton , Peter Sarkozi , Erzsebet Babos nee Vajas , Eniko Schreiner nee Kovats
发明人： Peter Szentmiklosi , Tamas Szuts , Jozsef Nemes , Jozsef Lengyel , Jeno Marton , Peter Sarkozi , Erzsebet Babos nee Vajas , Eniko Schreiner nee Kovats
IPC分类号： A61K9/00 , A61K31/40 , A61K36/06 , A61K47/00 , A61K47/22
CPC分类号： A61K31/70 , A61K47/22 , A61K8/4913 , A61K8/602 , A61K9/0014 , A61Q17/005
摘要： This invention relates to a primycin-containing colloidal basic gel comprising 5-30% of primycin and 95-70% of N-methyl-pyrrolidone-2. The invention also relates to antibacterial compositions particularly for the treatment of acne vulgaris comprising as active ingredient 0.1-100% of a primycin-containing colloidal basic gel, if desired together with further antimicrobial active ingredients, in admixture with 99.9-0% of usual inert pharmaceutical filling, diluting and other formulating additives. The invention also relates to combination composition comprising as active ingredient 1-60% of a primycin-containing colloidal basic gel and 0.1-40% of further pharmaceutical active ingredient(s), e.g. one or more antibiotic(s), chemotherapeutical agent(s), fungistatic or fungicidal agent(s), steroidal or non-steroidal antiinflammatory agent (s), epithelogenic agent(s), local anaesthetic(s), and/or vitamin(s).
摘要翻译：本发明涉及含有5-30％的伯霉素和95-70％N-甲基 - 吡咯烷酮-2的含有伯霉素的胶体碱性凝胶。本发明还涉及特别用于治疗寻常痤疮的抗菌组合物，其包含作为活性成分的含有含伯霉素的胶体碱性凝胶（如果需要的话）与其它抗微生物活性成分一起，与99.9-0％通常的惰性混合物药物灌装，稀释等配方添加剂。本发明还涉及组合组合物，其包含作为活性成分的含有含伯霉素的胶体碱性凝胶和0.1-40％的其它药物活性成分，例如，一种或多种抗生素，化学治疗剂，抑菌剂或杀真菌剂，类固醇或非甾体抗炎剂，上皮代谢剂，局部麻醉剂和/或维生素（ s）。

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