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公开(公告)号：US20080026056A1
公开(公告)日：2008-01-31
申请号：US11631030
申请日：2005-05-25
CPC分类号： A61K9/5084 , A61K9/5047 , A61K31/43
摘要： The invention relates to oral antibiotic drugs. The object of the invention is to limit or even stop the increase in antibiotic resistance without sacrificing the requirements of (a) increased efficacy of oral antibiotics, particularly for pediatric applications, (b) tolerance, (c) broad spectra of activity, and (d) good patient compliance. This object is achieved by the invention, which proposes the use of modified-release microcapsules, comprising a core that contains at least one active principle AP1 formed of at least one antibiotic, and a coating for said core that governs the modified release of said active principle, for the manufacture of a drinkable or orally dispersible antibiotic pharmaceutical formulation that makes it possible to limit the increase in the antibiotic resistance of the target germs, this formulation being: capable of administration in one or two, preferably two, intakes per day, and definable as follows, relative to an immediate-release oral formulation (IRF*) comprising at least one active principle API, and for the same dose D of API as IRF*: Tmic>T*micof IRF*
摘要翻译： 本发明涉及口服抗生素药物。 本发明的目的是限制或甚至阻止抗生素耐药性的增加，而不会牺牲（a）口服抗生素的功效增加，特别是儿科应用的要求，（b）耐受性，（c）活性的广谱谱和（ d）良好的患者依从性。 该目的是通过本发明来实现的，本发明提出使用包含至少一种由至少一种抗生素形成的至少一种活性成分AP1的芯的改性释放微胶囊和用于所述核心的涂层，所述涂层控制所述活性物质的修饰释放 原理，用于制造可以限制目标细菌的抗生素抗性增加的可饮用或口服分散的抗生素药物制剂，该制剂是：能够每天摄入一次或两次，优选两次， 并且可定义如下，相对于包含至少一种活性成分API的立即释放口服制剂（IRF *），和与IRF *相同的API剂量D：<？in-line-formula description =“In-line IRF *的公式“end =”lead“？> T > T * 在线公式描述=”在线公式“end =” 尾巴“？>
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公开(公告)号：US20070173464A1
公开(公告)日：2007-07-26
申请号：US11707034
申请日：2007-02-16
IPC分类号： A61K31/7056 , A61K9/22
CPC分类号： A61K9/5026 , A61K9/2077 , A61K9/48 , A61K9/5042 , A61K31/7056
摘要： The invention relates to oral pharmaceutical compositions for the prevention and/or the treatment of viral diseases. This invention also addresses methods of prevention and/or treatment of these viral diseases, using these oral compositions. One of the main problems considered in the present invention is to enhance the efficiency of anti-viral treatments, especially against Hepatitis C virus by means of ribavirin, for example in combination with interferon. The oral ribavirin antiviral composition according to the invention increases the bio-absorption time of ribavirin, and thus improves the treatment of patients. Said composition comprises at least one modified release form of ribavirin, the bio-absorption time BAT of which is greater than the bio-absorption time BAT* of a reference* immediate release form of ribavirin administered at the same dose; BAT being preferably comprised between 2 and 15 h and more preferably between 4 and 12 h. Said composition is a reservoir type form or a matrix type form. Said composition is a gastric retentive system or a multiparticulate form.
摘要翻译： 本发明涉及用于预防和/或治疗病毒性疾病的口服药物组合物。 本发明还涉及使用这些口服组合物预防和/或治疗这些病毒性疾病的方法。 本发明中考虑的主要问题之一是提高抗病毒治疗的效率，特别是通过利巴韦林（例如与干扰素组合）来抗丙型肝炎病毒。 根据本发明的口服利巴韦林抗病毒组合物增加了利巴韦林的生物吸收时间，从而改善了患者的治疗。 所述组合物包含至少一种改进释放形式的利巴韦林，其生物吸收时间BAT大于以相同剂量施用的参考*立即释放形式的利巴韦林的生物吸收时间BAT *; BAT优选包含2至15小时，更优选4至12小时。 所述组合物是储层型或矩阵型。 所述组合物是胃保持系统或多颗粒形式。
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公开(公告)号：US4629815A
公开(公告)日：1986-12-16
申请号：US276481
申请日：1981-06-23
申请人： Gerard Soula
发明人： Gerard Soula
IPC分类号： C07C17/00 , C07C17/358 , C07C21/24
CPC分类号： C07C17/00 , C07C17/358
摘要： Polychlorobenzenes are isomerized/rearranged, by reacting (i) at least one tetrachlorobenzene, or at least one tetrachlorobenzene in admixture with at least one trichlorobenzene, pentachlorobenzene and/or hexachlorobenzene, or (ii) pentachlorobenzene, or pentachlorobenzene in admixture with at least one trichlorobenzene and/or hexachlorobenzene, or (iii) hexachlorobenzene, or hexachlorobenzene in admixture with at least one trichlorobenzene and/or dichlorobenzene, with at least one alkali metal amide, or at least one alkali metal alcoholate, or admixture thereof, said reaction being conducted in the presence of an agent which complexes the cation of the amide, alcoholate, or admixture thereof.
摘要翻译： 通过使（i）至少一种四氯苯或至少一种四氯苯与至少一种三氯苯，五氯苯和/或六氯苯混合，或（ii）五氯苯或五氯苯与至少一种三氯苯的混合物进行异构化/重排， 和/或六氯苯，或（iii）六氯苯或六氯苯与至少一种三氯苯和/或二氯苯混合，与至少一种碱金属酰胺或至少一种碱金属醇盐或其混合物，或其混合物进行 存在使酰胺，醇化物或其混合物的阳离子络合的试剂。
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公开(公告)号：US4605543A
公开(公告)日：1986-08-12
申请号：US655730
申请日：1984-09-28
申请人： Jean-Luc Lepage , Gerard Soula
发明人： Jean-Luc Lepage , Gerard Soula
CPC分类号： C07F7/125 , C01B33/043
摘要： Silane, well adopted as a source of semiconductor/photovoltaic grade silicon, is facilely prepared from methyldichlorosilane and trichlorosilane and/or tetrachlorosilane by, (A) in a first step catalytically redistributing methyldichlorosilane with trichlorosilane or tetrachlorosilane, or admixture thereof, to form methyltrichlorosilane and dichlorosilane, and separating dichlorosilane from the resulting reaction medium, and (B) in a second step, catalytically disproportionating the dichlorosilane thus separated to form silane and trichlorosilane, and thence recovering silane thus formed and optionally recycling trichlorosilane to said step (A).
摘要翻译： 作为半导体/光电级硅源的硅烷，通过（A）在甲基二氯硅烷与三氯硅烷或四氯硅烷或其混合物催化重新分配的第一步中容易地由甲基二氯硅烷和三氯硅烷和/或四氯硅烷制备，形成甲基三氯硅烷和 二氯硅烷和从所得反应介质中分离二氯硅烷，和（B）在第二步中，催化歧化由此分离的二氯硅烷以形成硅烷和三氯硅烷，然后回收由此形成的硅烷，并任选地将三氯硅烷再循环到所述步骤（A）。
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公开(公告)号：US4578495A
公开(公告)日：1986-03-25
申请号：US739109
申请日：1985-05-30
申请人： Gerard Soula , Christian Simonnet
发明人： Gerard Soula , Christian Simonnet
CPC分类号： C07F7/125
摘要： The organosilanes/organopolysilanes, e.g., methylchlorosilanes useful in the production of silicones, are facilely prepared by contacting, in an inert atmosphere, (1) at least one disilane having the general formula:(R).sub.3 Si--Si--R).sub.3 (I)wherein the radicals R, which may be identical or different, are each C.sub.1 -C.sub.6 alkyl, hydrogen, 3,3,3-trifluoropropyl, trimethylsiloxy, fluorine, chlorine, bromine or iodine, with (2) a catalytically effective amount of a catalyst system comprising (a) at least one ionic inorganic salt having the formula:M.sup.+ A.sup.-wherein M.sup.+ is lithium, sodium, potassium, rubidium or cesium, and A.sup.- is fluoride, chloride, bromide or iodide, and (b) at least one compound which complexes the cation M.sup.+ of said salt (a), e.g., a sequestering agent having the formula:N--CHR.sub.1 --CHR.sub.2 O--CHR.sub.3 CHR.sub.4 O).sub.n R.sub.5 ].sub.3 (II).
摘要翻译： 有机硅烷/有机多硅烷，例如可用于生产硅氧烷的甲基氯硅烷，通过在惰性气氛中使（1）至少一种具有以下通式的乙硅烷：（R）3 Si-Si-R）3（ I），其中可以相同或不同的基团R各自为C 1 -C 6烷基，氢，3,3,3-三氟丙基，三甲基甲硅烷氧基，氟，氯，溴或碘，其中（2）催化有效量的 催化剂体系，其包含（a）至少一种具有下式的离子性无机盐：M + A-，其中M +是锂，钠，钾，铷或铯，A-是氟化物，氯化物，溴化物或碘化物，和（b） 至少一种与所述盐（a）的阳离子M +复合的化合物，例如具有下式的隔离剂：N-CHR 1 -CHR 2 O-CHR 3 CHR 4 O）n R 5] 3（II）。
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公开(公告)号：US4548917A
公开(公告)日：1985-10-22
申请号：US583208
申请日：1984-02-24
申请人： Jean-Luc Lepage , Gerard Soula
发明人： Jean-Luc Lepage , Gerard Soula
IPC分类号： B01J29/00 , C01B33/107 , C07F7/12 , C07F7/18 , C07F7/08
CPC分类号： C07F7/1884 , C01B33/10773 , C07F7/125
摘要： Silane, SiH.sub.4, and diochlorosilane, particularly suitable for the preparation of silicon are readily obtained by disproportionating trichlorosilane to dichlorosilane and, ultimately silane by reacting:(a) a silane containing at least one Si-H bond, of the general formula R.sub.n H.sub.m SiX.sub.4-(n+m) wherein R represents an alkyl or aryl group, x represents a halogen or an alkoxy group, n is an integer equal to 0, 1, 2 or 3 and m is an integer equal to 1, 2 or 3, and(b) a catalyst system comprising an ionic inorganic salt of the formula M.sup.+ A.sup.- and a compound capable of at least partially dissociating the salt by complexing its cation M.sup.+.
摘要翻译： 特别适用于制备硅的硅烷，SiH 4和二氯氯硅烷通过将三氯硅烷歧化成二氯硅烷，最终通过使（a）含有至少一个Si-H键的硅烷与通式RnHmSiX4-（ n + m）其中R表示烷基或芳基，x表示卤素或烷氧基，n为等于0,1,2或3的整数，m为等于1,2或3的整数，和（ b）催化剂体系，其包含式M + A的离子型无机盐和能够通过使其阳离子M +络合而至少部分地解离盐的化合物。
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公开(公告)号：US4479022A
公开(公告)日：1984-10-23
申请号：US365994
申请日：1982-04-06
申请人： Gerard Soula
发明人： Gerard Soula
CPC分类号： C07C17/358
摘要： Bromohalogenobenzenes are isomerized to useful, e.g., pharmaceutical or phytosanitary intermediates, by contacting the same with an alkaline base and a catalyst compound which forms a complex with the cation of said alkaline base.
摘要翻译： 通过使溴卤代苯与碱性碱和与所述碱性碱的阳离子形成络合物的催化剂化合物与溴化卤代苯异构化成有用的，例如药物或植物检疫中间体。
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公开(公告)号：US4417048A
公开(公告)日：1983-11-22
申请号：US351867
申请日：1982-02-24
申请人： Gerard Soula , Maurice Balme
发明人： Gerard Soula , Maurice Balme
IPC分类号： C07B31/00 , C07B43/04 , C07C67/00 , C07C209/00 , C07C209/08 , C07C209/10 , C07C209/16 , C07C209/18 , C07C211/52 , C07D207/323 , C07D207/333 , C07D209/48 , C07D235/00 , C07D235/04 , C07D235/06 , C07D279/22 , C07D279/28
CPC分类号： C07D209/48 , C07D235/06 , C07D279/28
摘要： Organonitrogen compounds bearing a labile hydrogen atom directly bonded to a reactive nitrogen function, e.g., nitrogen heterocycles or substituted anilines, are N-alkylated with an N-alkylating agent in the presence of inorganic base and at least one sequestering agent having the structural formula:N--CHR.sub.1 --CHR.sub.2 --O--(CHR.sub.3 --CHR.sub.4 --O).sub.n --R.sub.5 ].sub.3 (I)wherein n is a number ranging from 0 to 10, R.sub.1, R.sub.2, R.sub.3, R.sub.4, which may be identical or different, each represents a hydrogen atom or an alkyl radical having 1 to 4 carbon atoms, and R.sub.5 represents an alkyl or cycloalkyl radical having 1 to 12 carbon atoms, a phenyl radical, or a radical of the formula --C.sub.m H.sub.2m --.phi., or C.sub.m H.sub.2m+1 --.phi.--, m ranging from 1 to about 12 and .phi. being phenyl.
摘要翻译： 在无机碱和至少一种具有以下结构式的螯合剂的存在下，将与氮反应性氮官能团直接键合的不稳定氢原子（例如氮杂环或取代的苯胺）的有机氮化合物与N-烷基化剂N-烷基化， N-CHR1-CHR2-O-（CHR3-CHR4-O）n-R5] 3（I）其中n是0至10的数，R1，R2，R3，R4各自可相同或不同 表示氢原子或具有1至4个碳原子的烷基，R 5表示具有1至12个碳原子的烷基或环烷基，苯基或式-C m H 2 m-phi的基团或C m H 2n + phi - ，m范围从1到约12，phi是苯基。
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公开(公告)号：US4322336A
公开(公告)日：1982-03-30
申请号：US218265
申请日：1980-12-19
IPC分类号： C08K5/00 , C08K5/16 , C08K5/34 , C08K5/3412 , C08K5/3415 , C08L7/00 , C08L21/00 , C08L23/00 , C08L33/00 , C08L33/02 , C08L101/00
CPC分类号： C08K5/3415
摘要： In a filled/plasticized polymeric composition, e.g., a natural or synthetic rubber, the compatibility between reinforcing filler and plasticizer, particularly an oil, is markedly enhanced by incorporating therein a minor amount of an alkenyl succinimide.
摘要翻译： 在填充/增塑的聚合物组合物中，例如天然或合成橡胶中，通过在其中加入少量烯基琥珀酰亚胺，增强填料和增塑剂，特别是油之间的相容性明显增强。
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公开(公告)号：US4314086A
公开(公告)日：1982-02-02
申请号：US161516
申请日：1980-06-20
申请人： Gerard Soula , Daniel Michelet
发明人： Gerard Soula , Daniel Michelet
IPC分类号： C07C69/708 , C07C41/00 , C07C41/01 , C07C41/16 , C07C43/20 , C07C43/215 , C07C43/23 , C07C67/00 , C07D301/28 , C09K3/00
CPC分类号： C07C41/16 , C07C41/26 , C07C67/31 , C07D303/22
摘要： Aliphatic/aromatic ethers are prepared by reacting an aliphatic halide with either an alkali or alkaline earth metal, or ammonium phenolate or naphtholate, in an inert organic solvent, and in the presence of at least one tertiary amine sequestering agent having the formula:N--CHR.sub.1 CHR.sub.2 --O--CHR.sub.3 --CHR.sub.4 --O--.sub.n R.sub.5 ].sub.3
摘要翻译： 通过使脂族卤化物与碱金属或碱土金属或酚铵或萘酚酸酯在惰性有机溶剂中反应，并在至少一种具有下式的叔胺螯合剂存在下制备脂族/芳族醚：N- CHR1CHR2-O-CHR3-CHR4-O-nR5]
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