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公开(公告)号:US08912329B2
公开(公告)日:2014-12-16
申请号:US13380597
申请日:2010-06-25
申请人: Ronald Schoenmakers , Wilfried Weber , Marc Gitzinger , Martin Fussenegger , Marcel Tigges , Peter Schneider
发明人: Ronald Schoenmakers , Wilfried Weber , Marc Gitzinger , Martin Fussenegger , Marcel Tigges , Peter Schneider
IPC分类号: A61K31/4965 , C07D295/108 , C07D413/02 , C07D413/06 , A61K31/167 , A61K45/06 , A61K31/443 , A61K31/4015 , A61K31/17 , C07D265/30 , A61K31/4439 , A61K31/496 , C07D207/12 , C07D241/04 , A61K31/397 , C07D207/08 , C07D295/185 , A61K31/341 , C07D401/06 , C07D205/04 , A61K31/40 , A61K31/5377 , C07D213/74 , A61K31/44 , C07D213/38 , C07D413/04 , A61K31/7008 , A61K31/5375 , C07D307/32 , A61K31/495
CPC分类号: A61K31/4015 , A61K31/167 , A61K31/17 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/443 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/7008 , A61K45/06 , C07D205/04 , C07D207/08 , C07D207/12 , C07D213/38 , C07D213/74 , C07D241/04 , C07D265/30 , C07D295/185 , C07D307/32 , C07D401/06 , C07D413/02 , C07D413/04 , C07D413/06 , A61K2300/00
摘要: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C≡CH, C≡N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N═CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
摘要翻译: 本发明涉及包含式(1)化合物的药物组合物,其中R 1是任选取代的苯基,任选取代的吡啶基或任选取代的吲哚基; R2是(CH2)n,其中n是0,1,2,3或4; R3是(CH2)mR3A,其中m是0,1,2,3或4,R3A是甲基,异丙基,叔丁基,OCH3,OH,任选取代的苯氧基,C≡CH,C≡N,任选取代的苯基, 呋喃基或噻吩基; A是含有O,S,NH,N(CH 3)或CH 2的X 1的环; X2是O,S或NH; 和式(2)的化合物,其中R 4是任选取代的苯基,任选取代的吡啶基,任选取代的吲哚基,-NR 7 R 8; 或-NH-N = CH-R 9; 并且取代基R 5至R 9具有在说明书中指出的含义,特别是乙二胺。 药物组合物可用于例如治疗多重耐药性结核病。
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公开(公告)号:US20120101080A1
公开(公告)日:2012-04-26
申请号:US13380597
申请日:2010-06-25
申请人: Ronald Schoenmakers , Wilfried Weber , Marc Gitzinger , Martin Fussenegger , Marcel Tigges , Peter Schneider
发明人: Ronald Schoenmakers , Wilfried Weber , Marc Gitzinger , Martin Fussenegger , Marcel Tigges , Peter Schneider
IPC分类号: A61K31/397 , A61K31/5375 , A61K31/496 , A61K31/4965 , A61K31/443 , A61K31/4439 , A61K31/44 , A61K31/40 , C07D413/06 , C07D413/04 , C07D265/30 , C07D401/06 , C07D241/04 , C07D405/06 , C07D207/16 , C07D205/04 , A61P31/06 , A61K31/5377
CPC分类号: A61K31/4015 , A61K31/167 , A61K31/17 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/443 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/7008 , A61K45/06 , C07D205/04 , C07D207/08 , C07D207/12 , C07D213/38 , C07D213/74 , C07D241/04 , C07D265/30 , C07D295/185 , C07D307/32 , C07D401/06 , C07D413/02 , C07D413/04 , C07D413/06 , A61K2300/00
摘要: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C≡CH, C≡N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N═CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
摘要翻译: 本发明涉及包含式(1)化合物的药物组合物,其中R 1是任选取代的苯基,任选取代的吡啶基或任选取代的吲哚基; R2是(CH2)n,其中n是0,1,2,3或4; R3是(CH2)mR3A,其中m是0,1,2,3或4,R3A是甲基,异丙基,叔丁基,OCH3,OH,任选取代的苯氧基,C≡CH,C≡N,任选取代的苯基, 呋喃基或噻吩基; A是含有O,S,NH,N(CH 3)或CH 2的X 1的环; X2是O,S或NH; 和式(2)的化合物,其中R 4是任选取代的苯基,任选取代的吡啶基,任选取代的吲哚基,-NR 7 R 8; 或-NH-N = CH-R 9; 并且取代基R 5至R 9具有在说明书中指出的含义,特别是乙二胺。 药物组合物可用于例如治疗多重耐药性结核病。
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公开(公告)号:US20110053880A1
公开(公告)日:2011-03-03
申请号:US12808801
申请日:2008-11-25
IPC分类号: A61K31/7028 , A61K31/44 , A61K31/175 , G01N33/53 , A61P31/06
CPC分类号: A61K31/17 , A61K31/4409 , A61K45/06 , A61K2300/00
摘要: The invention relates to a pharmaceutical composition comprising a compound preventing EthR from binding to the ethA promoter, for example a compound of formula 1 wherein R1 is optionally substituted phenyl or optionally substituted pyridyl; R2 (CH2)n wherein n is 1, 2, 3 or 4; R3 is CH3(CH2)m wherein m is 0, 1, 2 or 3; X1 is O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; in particular 2-phenylethyl butyrate, and a thioamide or thiourea of formula 2 wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N═CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
摘要翻译: 本发明涉及包含防止EthR与ethA启动子结合的化合物的药物组合物,例如式1的化合物,其中R 1是任选取代的苯基或任选取代的吡啶基; R2(CH2)n,其中n为1,2,3或4; R3是CH3(CH2)m,其中m是0,1,2或3; X 1是O,S,NH,N(CH 3)或CH 2; X2是O,S或NH; 特别是丁酸2-苯基乙酯和式2的硫代酰胺或硫脲,其中R 4是任选取代的苯基,任选取代的吡啶基,任选取代的吲哚基,-NR 7 R 8; 或-NH-N = CH-R 9; 并且取代基R 5至R 9具有在说明书中指出的含义,特别是乙二胺。 药物组合物可用于例如治疗多重耐药性结核病。
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公开(公告)号:US09050295B2
公开(公告)日:2015-06-09
申请号:US12808801
申请日:2008-11-25
IPC分类号: A61K31/17 , A61K31/4409 , A61K45/06
CPC分类号: A61K31/17 , A61K31/4409 , A61K45/06 , A61K2300/00
摘要: The invention relates to a pharmaceutical composition comprising a compound preventing EthR from binding to the ethA promoter, for example a compound of formula 1 wherein R1 is optionally substituted phenyl or optionally substituted pyridyl; R2 (CH2)n wherein n is 1, 2, 3 or 4; R3 is CH3(CH2)m wherein m is 0, 1, 2 or 3; X1 is O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; in particular 2-phenylethyl butyrate, and a thioamide or thiourea of formula 2 wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N═CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
摘要翻译: 本发明涉及包含防止EthR与ethA启动子结合的化合物的药物组合物,例如式1的化合物,其中R 1是任选取代的苯基或任选取代的吡啶基; R2(CH2)n,其中n为1,2,3或4; R3是CH3(CH2)m,其中m是0,1,2或3; X 1是O,S,NH,N(CH 3)或CH 2; X2是O,S或NH; 特别是丁酸2-苯基乙酯和式2的硫代酰胺或硫脲,其中R 4是任选取代的苯基,任选取代的吡啶基,任选取代的吲哚基,-NR 7 R 8; 或-NH-N = CH-R 9; 并且取代基R 5至R 9具有在说明书中指出的含义,特别是乙二胺。 药物组合物可用于例如治疗多重耐药性结核病。
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公开(公告)号:US20110151006A1
公开(公告)日:2011-06-23
申请号:US12996492
申请日:2009-06-05
CPC分类号: A61K38/52 , A61K38/1866 , A61K47/549 , A61K47/552 , A61K47/58 , A61K47/60 , A61K47/62 , A61K47/6903
摘要: The present invention relates to a hydrogel comprising a polymer, a first polypeptide and a polypeptide binding partner, wherein the polypeptide binding partner is a second polypeptide, a nucleic acid or a small molecule, and wherein the interaction between the first polypeptide and the polypeptide binding partner stabilizes the hydrogel and is modulated by the addition of a modulating compound. A drug may be physically entrapped in the hydrogel, bound to the polymer forming the hydrogel structure, or bound to the first polypeptide or the polypeptide binding partner, and then be set free on addition of the modulating compound. Such a hydrogel comprising a drug may be injected into a patient, and drug release modulated by orally administering the modulating compound.
摘要翻译: 本发明涉及包含聚合物,第一多肽和多肽结合配偶体的水凝胶,其中多肽结合配偶体是第二多肽,核酸或小分子,并且其中第一多肽和多肽结合之间的相互作用 配偶体稳定水凝胶,并通过加入调节化合物进行调节。 药物可以被物理地包埋在水凝胶中,与形成水凝胶结构的聚合物结合,或者与第一多肽或多肽结合配偶体结合,然后在加入调节化合物时释放。 包含药物的这种水凝胶可以注射到患者体内,并通过口服施用调节化合物调节药物释放。
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公开(公告)号:US08653046B2
公开(公告)日:2014-02-18
申请号:US13263149
申请日:2010-04-01
申请人: Martin Fussenegger , Marc Gitzinger
发明人: Martin Fussenegger , Marc Gitzinger
CPC分类号: C12N15/8509 , A61K9/0014 , A61K47/10 , C12N2820/55 , C12N2830/002 , C12N2830/005
摘要: The invention relates to the use of a skin permeating compound such as phloretin for controlling transgene expression under control of the Pseudomonas putida DOT-T1E-derived bacterial repressor TtgR, to a vector comprising the genetic code for the repressor TtgR fused to a transactivation or a transrepressor domain, to a vector comprising a TtgR-specific operator sequence (OTtgR), a promoter and a polynucleotide coding for an endogenous or exogenous protein, and to a mammalian cell transiently or constitutively transfected with the mentioned vectors, and to mammals comprising such cells in nano- or microcontainers.
摘要翻译: 本发明涉及使用皮肤渗透化合物如根皮素用于控制恶臭假单胞菌DOT-T1E衍生的细菌阻遏物TtgR的控制下的转基因表达,所述载体包含与转录激活融合的阻遏物TtgR的遗传密码 包含TtgR特异性操纵子序列(OTtgR),启动子和编码内源或外源蛋白的多核苷酸的载体,以及用所述载体瞬时或组成型转染的哺乳动物细胞,以及包含这些细胞的哺乳动物 在纳米或微型容器中。
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公开(公告)号:US20120029074A1
公开(公告)日:2012-02-02
申请号:US13263149
申请日:2010-04-01
申请人: Martin Fussenegger , Marc Gitzinger
发明人: Martin Fussenegger , Marc Gitzinger
IPC分类号: A61K31/235 , A61P43/00 , C12N5/10 , A61K31/12 , C12N15/63
CPC分类号: C12N15/8509 , A61K9/0014 , A61K47/10 , C12N2820/55 , C12N2830/002 , C12N2830/005
摘要: The invention relates to the use of a skin permeating compound such as phloretin for controlling transgene expression under control of the Pseudomonas putida DOT-T1E-derived bacterial repressor TtgR, to a vector comprising the genetic code for the repressor TtgR fused to a transactivation or a transrepressor domain, to a vector comprising a TtgR-specific operator sequence (OTtgR), a promoter and a polynucleotide coding for an endogenous or exogenous protein, and to a mammalian cell transiently or constitutively transfected with the mentioned vectors, and to mammals comprising such cells in nano- or microcontainers.
摘要翻译: 本发明涉及使用皮肤渗透化合物如根皮素用于控制恶臭假单胞菌DOT-T1E衍生的细菌阻遏物TtgR的控制下的转基因表达,所述载体包含与转录激活融合的阻遏物TtgR的遗传密码 包含TtgR特异性操纵子序列(OTtgR),启动子和编码内源或外源蛋白的多核苷酸的载体,以及用所述载体瞬时或组成型转染的哺乳动物细胞,以及包含这些细胞的哺乳动物 在纳米或微型容器中。
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公开(公告)号:US20110177162A1
公开(公告)日:2011-07-21
申请号:US13003420
申请日:2009-07-10
CPC分类号: A61K35/52 , A61K9/5042 , A61K9/5068
摘要: The invention relates to microcapsules consisting of a polymer degradable by a polypeptide comprising a drug or other compound of interest and a genetically engineered cell expressing said polypeptide in response to a triggering compound, and to methods of directed release of the compound of interest. The preferred polymer is optionally modified cellulose sulfate/poly-diallyl-dimethyl-ammonium chloride. Such microcapsules are non-toxic, do not elicit an immunological response and have an extended half-life time in mammals. The expression system for cellulase is, for example, based on TET and doxycycline, or E.REX and erythromycin. In another example, expression of cellulase is triggered by luteinizing hormone, which can be used for artificial insemination with microcapsules carrying sperm.
摘要翻译: 本发明涉及由可由可包含药物或目的的其它化合物的多肽降解的聚合物和响应于引发化合物表达所述多肽的遗传工程改造的细胞组成的微胶囊以及目的化合物的定向释放方法。 优选的聚合物是任选改性的硫酸纤维素/聚二烯丙基二甲基氯化铵。 这样的微胶囊是无毒的,不引起免疫应答并且在哺乳动物中具有延长的半衰期。 纤维素酶的表达系统例如是基于TET和多西环素,或E.REX和红霉素。 在另一个实例中,纤维素酶的表达由黄体生成激素引发,其可用于携带精子的微胶囊的人工授精。
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公开(公告)号:US07273723B2
公开(公告)日:2007-09-25
申请号:US09949470
申请日:2001-09-07
申请人: Martin Fussenegger , Wilfried Weber
发明人: Martin Fussenegger , Wilfried Weber
CPC分类号: C12N15/635 , A01K2217/05 , C12N15/8238 , C12N2799/021
摘要: The invention relates to a novel system for gene regulation in eukaryotic cells, and methods of using the same for protein production, tissue engineering and gene therapy. In particular, the invention provides a new system for antibiotic-regulated gene expression in eukaryotic cells based on sequences from Enterobacteriaceae antibiotic resistance promoters, polypeptides that bind to the same in an antibiotic responsive manner, and nucleotides encoding such polypeptides. Further, the invention provides novel and sensitive methods of screening for candidate antibiotics.
摘要翻译: 本发明涉及一种用于真核细胞中基因调控的新系统,以及用于其中的蛋白质生产,组织工程和基因治疗的方法。 特别地,本发明基于肠杆菌科抗生素抗性启动子,以抗生素反应性方式与其结合的多肽和编码这些多肽的核苷酸的序列,提供了真核细胞中抗生素调节基因表达的新系统。 此外,本发明提供了筛选候选抗生素的新型和敏感的方法。
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公开(公告)号:US08506950B2
公开(公告)日:2013-08-13
申请号:US13605307
申请日:2012-09-06
CPC分类号: A61K35/52 , A61K9/5042 , A61K9/5068
摘要: The invention relates to microcapsules consisting of a polymer degradable by a polypeptide comprising a drug or other compound of interest and a genetically engineered cell expressing said polypeptide in response to a triggering compound, and to methods of directed release of the compound of interest. The preferred polymer is optionally modified cellulose sulfate/poly-diallyl-dimethyl-ammonium chloride. Such microcapsules are non-toxic, do not elicit an immunological response and have an extended half-life time in mammals. The expression system for cellulase is, for example, based on TET and doxycycline, or E.REX and erythromycin. In another example, expression of cellulase is triggered by luteinizing hormone, which can be used for artificial insemination with microcapsules carrying sperm.
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