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公开(公告)号：US07002036B2
公开(公告)日：2006-02-21
申请号：US10438770
申请日：2003-05-15
IPC分类号： C07C34/00
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.
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公开(公告)号：US06903220B2
公开(公告)日：2005-06-07
申请号：US10439313
申请日：2003-05-15
IPC分类号： C07D233/64 , A61K31/426 , A61P7/02 , A61P11/06 , A61P29/00 , A61P31/12 , C07B53/00 , C07B55/00 , C07B61/00 , C07C217/46 , C07C227/18 , C07C229/06 , C07C229/42 , C07C249/02 , C07C253/00 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07C323/00 , C07C323/25 , C07C323/35 , C07C323/52 , C07C323/56 , C07C323/58 , C07D213/55 , C07D233/16 , C07D237/02 , C07D277/04 , C07D277/08 , C07D277/12 , C07D277/14 , C07D277/18 , C07D277/56 , C07D303/24 , 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 reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). 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使半胱氨酸（或其盐或其酯）和芳基羧酸反应形成噻唑啉环，立体特异性烷基化噻唑啉环，并水解噻唑啉环以获得2-烷基半胱氨酸 （或相关化合物）。 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：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：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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公开(公告)号：US07179937B2
公开(公告)日：2007-02-20
申请号：US10309754
申请日：2002-12-04
申请人： Mukund K. Gurjar , Radhika D. Wakharkar , Gautam R. Desiraju , Ashwini Nangia , Jhillu Singh Yadav , Anand C. Burman , Rama Mukherjee , Hanumant Bapu Rao Borate , Srivari Chandrasekhar , Manu Jaggi , Anuo T. Singh , Kamal Kapoor , Sanjay Sarkhel , K. V. V. M. Sairam
发明人： Mukund K. Gurjar , Radhika D. Wakharkar , Gautam R. Desiraju , Ashwini Nangia , Jhillu Singh Yadav , Anand C. Burman , Rama Mukherjee , Hanumant Bapu Rao Borate , Srivari Chandrasekhar , Manu Jaggi , Anuo T. Singh , Kamal Kapoor , Sanjay Sarkhel , K. V. V. M. Sairam
IPC分类号： C07C61/06 , C07C249/00
CPC分类号： C07C49/753 , C07C49/747 , C07C69/013 , C07C205/45 , C07C251/44 , C07C251/66 , C07C2601/10 , C07F7/1804
摘要： The invention relates to the use of derivatives of cyclopentenone for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of derivatives of cyclopentenone for the inhibition and/or prevention of cancer of the colon, pancreas, larynx, ovary, duodenum, kidney, oral cavity, prostate, lung, endothelial cells and leukemias.
摘要翻译： 本发明涉及环戊烯酮衍生物用于抑制或预防癌细胞生长或增殖的用途，以及含有这些化合物的治疗组合物的用途。 本发明更具体地涉及环戊烯酮衍生物用于抑制和/或预防结肠，胰腺，喉，卵巢，十二指肠，肾，口腔，前列腺，肺，内皮细胞和白血病的癌症。
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公开(公告)号：US06846932B1
公开(公告)日：2005-01-25
申请号：US10718267
申请日：2003-11-20
IPC分类号： C07D211/86
CPC分类号： C07D211/90
摘要： A process for the preparation of pharmaceutically acceptable salts of chiral Amlodipine namely S(−) Amlodipine and R(+) Amlodipine from without isolation of a free base from with optical purity rank between 96-99% is described in the present invention. The process comprises resolving RS amlodipine base using of L(+) or D(−) tartaric acid to obtain salt of corresponding to the acid used in ee rang from 96-99%.
摘要翻译： 在本发明中描述了制备手性氨氯地平的药学上可接受的盐即S（ - ）氨氯地平和R（+）氨氯地平的方法，该方法不分离游离碱与光学纯度等级在96-99％之间。 该方法包括使用L（+）或D（ - ）酒石酸分解RS氨氯地平碱，以获得与96-99％的所用酸相当的盐。
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公开(公告)号：US08686165B2
公开(公告)日：2014-04-01
申请号：US12917823
申请日：2010-11-02
IPC分类号： C07D305/14 , C07D305/06
CPC分类号： C07D305/14
摘要： The present disclosure relates to processes for the preparation of taxane derivatives with improved purity and enhanced stability. The taxane derivatives prepared according to the processes described herein are useful for the preparation of pharmaceutical compositions.
摘要翻译： 本公开涉及制备具有改善的纯度和增强的稳定性的紫杉烷衍生物的方法。 根据本文所述方法制备的紫杉烷衍生物可用于制备药物组合物。
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8.发明申请公开(公告)号：US20110046416A1
公开(公告)日：2011-02-24
申请号：US12858779
申请日：2010-08-18
申请人： Mukund K. Gurjar , Narendra K. Tripathy , Kiran A. Bapat , Vemavarapu P.K.V. Rao , Satyjeet B. Biswas , Samit S. Mehta
发明人： Mukund K. Gurjar , Narendra K. Tripathy , Kiran A. Bapat , Vemavarapu P.K.V. Rao , Satyjeet B. Biswas , Samit S. Mehta
IPC分类号： C07C209/84
CPC分类号： C07C209/08 , C07C211/27
摘要： The present invention provides a simple method for preparation of benzphetamine and its acid addition salt comprising reaction of methamphetamine hydrochloride of formula (III) with benzyl chloride and treating the isolated benzphetamine of formula (II) with an acid dissolved in an organic solvent to provide benzphetamine acid addition salt, more specifically, benzphetamine hydrochloride of formula (I).
摘要翻译： 本发明提供了制备苯并苯并及其酸加成盐的简单方法，其包括式（III）的甲基苯丙胺盐酸盐与苄基氯的反应，并用溶解在有机溶剂中的酸处理式（II）的分离苯并特丁胺，得到苯并苯 酸加成盐，更具体地，式（I）的苯并苯丙胺盐酸盐。
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公开(公告)号：US06875883B2
公开(公告)日：2005-04-05
申请号：US10439286
申请日：2003-05-15
IPC分类号： C07D233/64 , A61K31/426 , A61P7/02 , A61P11/06 , A61P29/00 , A61P31/12 , C07B53/00 , C07B55/00 , C07B61/00 , C07C217/46 , C07C227/18 , C07C229/06 , C07C229/42 , C07C249/02 , C07C253/00 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07C323/00 , C07C323/25 , C07C323/35 , C07C323/52 , C07C323/56 , C07C323/58 , C07D213/55 , C07D233/16 , C07D237/02 , C07D277/04 , C07D277/08 , C07D277/12 , C07D277/14 , C07D277/18 , C07D277/56 , C07D303/24 , C07C253/12
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： There is a significant demand for organic nitriles, based on their versatility in reactions. Compounds prepared from nitriles have properties including superoxide inhibition, ferrielectric liquid crystal dopant, antipicornaviral agents, anti-inflammatory agents, anti-asthma agents, and fibringoen antagonists. The present invention discloses a facile synthesis for 2,4-dihydroxybenzonitrile, and ethers and diethers thereof, from 2,4-dihydroxybenzaldehyde or 2,4-dimethoxybenzaldehyde. 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： 根据反应的多样性，对有机腈有很大的需求。 由腈制备的化合物具有包括超氧化物抑制，电介质液晶掺杂剂，止痒病毒药，抗炎剂，抗哮喘药和纤维蛋白拮抗剂的性质。 本发明公开了从2,4-二羟基苯甲醛或2,4-二甲氧基苯甲醛中轻松合成2,4-二羟基苄腈及其醚和二醚。 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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公开(公告)号：US06875882B2
公开(公告)日：2005-04-05
申请号：US10439341
申请日：2003-05-15
IPC分类号： C07D233/64 , A61K31/426 , A61P7/02 , A61P11/06 , A61P29/00 , A61P31/12 , C07B53/00 , C07B55/00 , C07B61/00 , C07C217/46 , C07C227/18 , C07C229/06 , C07C229/42 , C07C249/02 , C07C253/00 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07C323/00 , C07C323/25 , C07C323/35 , C07C323/52 , C07C323/56 , C07C323/58 , C07D213/55 , C07D233/16 , C07D237/02 , C07D277/04 , C07D277/08 , C07D277/12 , C07D277/14 , C07D277/18 , C07D277/56 , C07D303/24 , C07C255/50
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： There is a significant demand for organic nitriles, based on their versatility in reactions. Compounds prepared from nitriles have properties including superoxide inhibition, ferrielectric liquid crystal dopant, antipicornaviral agents, anti-inflammatory agents, anti-asthma agents, and fibringoen antagonists. The present invention discloses a facile synthesis for 2,4-dihydroxybenzonitrile, and ethers and diethers thereof, from 2,4-dihydroxybenzoic 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： 根据反应的多样性，对有机腈有很大的需求。 由腈制备的化合物具有包括超氧化物抑制，电介质液晶掺杂剂，止痒病毒药，抗炎剂，抗哮喘药和纤维蛋白拮抗剂的性质。 本发明公开了2,4-二羟基苯甲酸的2,4-二羟基苯甲腈及其醚和二醚的容易合成。 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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