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公开(公告)号:US20160022645A1
公开(公告)日:2016-01-28
申请号:US14875462
申请日:2015-10-05
IPC分类号: A61K31/426
CPC分类号: A61K31/426 , C07D277/12
摘要: A relatively non-toxic desazadesferrithiocin analog having the formula: wherein: R1, R2, R4 and R5 may be the same or different and may be H, straight or branched chain alkyl having up to 14 carbon atoms, e.g., methyl, ethyl, propyl and butyl, or arylalkyl wherein the aryl portion is hydrocarbyl and the alkyl portion is straight or branched chain, the arylalkyl group having up to 14 carbon atoms, R2 optionally being alkoxy having up to 14 carbon atoms; R3 is [(CH2)n—O]x—[(CH2)n—O]y-alkyl; n is, independently, an integer from 1 to 8; x is an integer from 1 to 8; y is an integer from 0 to 8, and R3O may occupy any position on the phenyl ring except the 4-position, or a salt, hydrate or solvate thereof; and methods and compositions for treating the effects of trivalent metal, i.e., iron, overload.
摘要翻译: 一种具有下式的相对无毒的脱氮基硫代赖氨酸类似物:其中:R 1,R 2,R 4和R 5可以相同或不同,并且可以是H,具有至多14个碳原子的直链或支链烷基,例如甲基,乙基,丙基 和芳基烷基,其中芳基部分为烃基,烷基部分为直链或支链,芳基烷基具有至多14个碳原子,R2任选为具有至多14个碳原子的烷氧基; R3是[(CH2)n-O] x - [(CH2)n-O] y-烷基; n独立地为1至8的整数; x是1至8的整数; y为0〜8的整数,R3O可以占有除4-位之外的苯环上的任何位置,或其盐,水合物或溶剂合物; 以及用于处理三价金属(即铁)过载的作用的方法和组合物。
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公开(公告)号:US09096553B2
公开(公告)日:2015-08-04
申请号:US14264959
申请日:2014-04-29
IPC分类号: C07D277/12 , C07D277/10
CPC分类号: C07D277/12 , A61K31/426 , C07B2200/07 , C07D277/10
摘要: Compounds represented by structural formulas described herein, such as Structural Formula (I): or a pharmaceutically acceptable salt thereof are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.
摘要翻译: 由结构式(I)表示的结构式表示的化合物或其药学上可接受的盐可用于治疗诸如金属过载,氧化应激和肿瘤和肿瘤前病症的病症。
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公开(公告)号:US08722899B2
公开(公告)日:2014-05-13
申请号:US13631025
申请日:2012-09-28
IPC分类号: A61K31/426 , C07D277/10
CPC分类号: C07D277/12 , A61K31/426 , C07B2200/07 , C07D277/10
摘要: Compounds represented by structural formulas described herein, such as Structural Formula (I): or a pharmaceutically acceptable salt thereof are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.
摘要翻译: 由结构式(I)表示的结构式表示的化合物或其药学上可接受的盐可用于治疗诸如金属过载,氧化应激和肿瘤和肿瘤前病症的病症。
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公开(公告)号:US08680126B2
公开(公告)日:2014-03-25
申请号:US13820480
申请日:2011-08-29
申请人: Joan Gil Santano , Rodolfo Lavilla Grifols , Fernando Albericio Palomera , Alba Pérez Perarnau , Sara Preciado Gallego , Diana Ma González Gironès , Daniel Iglesias Serret , Rosario Ramón Albalate
发明人: Joan Gil Santano , Rodolfo Lavilla Grifols , Fernando Albericio Palomera , Alba Pérez Perarnau , Sara Preciado Gallego , Diana Ma González Gironès , Daniel Iglesias Serret , Rosario Ramón Albalate
IPC分类号: A61K31/425 , C07D417/00
CPC分类号: C07D277/30 , C07D277/12 , C07D277/22 , C07D277/24 , C07D277/32 , C07D277/56 , C07D417/04
摘要: Compounds of formula (I) or their pharmaceutically acceptable salts, or their stereoisomers or mixtures of stereoisomers, where: R1 is selected from the group consisting of: phenyl, and phenyl mono-, di-, or tri-substituted by a radical independently selected from the group consisting of F, Cl, Br, I, (C1-C6)-alkyl, COO—(C1-C6)-alkyl, and (C1-C6)-alkoxy; and R2 is a radical selected from the same group as R1, further including a phenyl substituted in 4-position by a radical independently selected from the group consisting of —O(CH2)CONH(CH2)3CH3 and OCH2COOC(CH3)3, a biphenyl-4-yl, thiazol-2-yl, and a thiazol-2-yl mono- or di-substituted by a radical selected from F and phenyl; inhibit cell proliferation of tumor cells independently of p53 protein and may also induce apoptosis in several tumor cells independently of p53 protein, being useful for the treatment of several types of cancer.
摘要翻译: 式(I)化合物或其药学上可接受的盐或其立体异构体或立体异构体的混合物,其中:R 1选自:苯基和被独立选择的基团单,二或三取代的苯基 (C 1 -C 6) - 烷基,COO-(C 1 -C 6) - 烷基和(C 1 -C 6) - 烷氧基; 并且R 2是选自与R 1相同的基团,还包括被独立地选自-O(CH 2)CONH(CH 2)3 CH 3和OCH 2 COOC(CH 3)3的基团在4-位取代的苯基, 联苯-4-基,噻唑-2-基和被选自F和苯基的基团单取代或二取代的噻唑-2-基; 与p53蛋白无关地抑制肿瘤细胞的细胞增殖,并且可以独立于p53蛋白诱导几种肿瘤细胞的凋亡,可用于治疗几种类型的癌症。
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25.
公开(公告)号:US20140018400A1
公开(公告)日:2014-01-16
申请号:US13878189
申请日:2011-10-14
申请人: Eric W. Schmidt , Zhenjian Lin , Rowena R. Antemano , Alan Light , Baldomero M. Olivera , Gisela P. Concepcion
发明人: Eric W. Schmidt , Zhenjian Lin , Rowena R. Antemano , Alan Light , Baldomero M. Olivera , Gisela P. Concepcion
IPC分类号: C07D277/10 , A61K31/426 , C07D277/12 , A61K45/06
CPC分类号: C07D277/10 , A61K31/421 , A61K31/426 , A61K31/427 , A61K45/06 , C07D277/12 , A61K2300/00
摘要: In one aspect, the invention relates to compounds having a general structure: and methods of using same to modulate calcium release. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译: 一方面,本发明涉及具有一般结构的化合物及其用于调节钙释放的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具,而不意在限制本发明。
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公开(公告)号:US20130012719A1
公开(公告)日:2013-01-10
申请号:US13543403
申请日:2012-07-06
IPC分类号: C07D277/10 , C07D487/00 , C07D263/14
CPC分类号: C07D263/34 , C07D263/16 , C07D277/12 , C07D277/56 , C07D417/04
摘要: Azolines are oxidized in the presence of a copper-containing catalyst to azoles in the presence of molecular oxygen. A synthetic scheme converting azolines azoles is also provided.
摘要翻译: 在分子氧存在下,偶氮染料在含铜催化剂存在下被氧化成唑。 还提供了转化偶氮唑类的合成方案。
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公开(公告)号:US08324397B2
公开(公告)日:2012-12-04
申请号:US12450194
申请日:2008-03-14
IPC分类号: A61K31/426 , C07D277/12
CPC分类号: A61K31/426 , C07D277/12
摘要: A relatively non-toxic desazadesferrithiocin analog having the formula (I): wherein: R1, R2, R4 and R5 may be the same or different and may be H, straight or branched chain alkyl having up to 14 carbon atoms, e.g., methyl, ethyl, propyl and butyl, or arylalkyl wherein the aryl portion is hydrocarbyl and the alkyl portion is straight or branched chain, the arylalkyl group having up to 14 carbon atoms, R2 optionally being alkoxy having up to 14 carbon atoms; R3 is [(CH2)n—O]x—[(CH2)n—O]y-alkyl; n is, independently, an integer from 1 to 8; x is an integer from 1 to 8; y is an integer from O to 8, and R3O may occupy any position on the phenyl ring except the 4-position, or a salt, hydrate or solvate thereof; and methods and compositions for treating the effects of trivalent metal, i.e., iron, overload.
摘要翻译: 具有式(I)的相对无毒的脱氮代铁硫代类似物:其中:R 1,R 2,R 4和R 5可以相同或不同,可以是H,具有至多14个碳原子的直链或支链烷基,例如甲基, 乙基,丙基和丁基,或芳基烷基,其中芳基部分为烃基,烷基部分为直链或支链,芳基烷基具有至多14个碳原子,R2任选为具有至多14个碳原子的烷氧基; R3是[(CH2)n-O] x - [(CH2)n-O] y-烷基; n独立地为1至8的整数; x是1至8的整数; y为0至8的整数,R3O可占据除4-位之外的苯环上的任何位置,或其盐,水合物或溶剂合物; 以及用于处理三价金属(即铁)过载的作用的方法和组合物。
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公开(公告)号:US07576234B2
公开(公告)日:2009-08-18
申请号:US11305305
申请日:2005-12-16
IPC分类号: C07C321/00
CPC分类号: C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
摘要翻译: 非天然氨基酸例如2-烷基化氨基酸允许合成更多种类的肽和非肽类药物活性剂。 制备2-烷基氨基酸的方法包括向2-甲基亚烷基丙-1,3-二酸二烷基酯的双键加成亲核试剂,并将酯部分转化成氨基部分。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法,所述铁螯合剂全部含有噻唑啉环。 在该方法中,芳基腈或亚氨酸酯与半胱氨酸,2-烷基半胱氨酸或半胱氨酸酯缩合。
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公开(公告)号:US20080214630A1
公开(公告)日:2008-09-04
申请号:US11973001
申请日:2007-10-04
申请人: Raymond J. Bergeron
发明人: Raymond J. Bergeron
IPC分类号: A61K31/426 , A61P7/00 , C07D277/10
CPC分类号: C07D277/12 , A61K31/426 , C07B2200/07 , C07D277/10
摘要: Compounds represented by structural formulas described herein, such as Structural Formula (I): or a pharmaceutically acceptable salt thereof are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.
摘要翻译: 由结构式(I)表示的结构式表示的化合物或其药学上可接受的盐可用于治疗诸如金属过载,氧化应激和肿瘤和肿瘤前病症的病症。
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30.
公开(公告)号:US07294718B2
公开(公告)日:2007-11-13
申请号:US11008084
申请日:2004-12-09
IPC分类号: C07D277/02
CPC分类号: C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要: Benzimidates can be reacted with a large number of nucleophiles, leading to a wide variety of products. The present invention discloses a facile synthesis for ethyl 2,4-dihydroxybenzimidate, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid or 2,4-dibenzyloxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.
摘要翻译: 苯甲酰胺可与大量的亲核试剂反应,导致产品种类繁多。 本发明公开了2,4-二羟基苯甲酸或2,4-二苄氧基苯甲酸的2,4-二羟基苯甲亚胺乙酯及其醚和二醚的简便合成。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法,所述铁螯合剂全部含有噻唑啉环。 在该方法中,2,4-二羟基苄腈与(S)-2-甲基半胱氨酸缩合。
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