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51. 发明申请

US20050228181A1 Process for making chiral 1,4-disubstituted piperazines 失效
标题翻译：制备手性1,4-二取代哌嗪的方法
公开(公告)号：US20050228181A1
公开(公告)日：2005-10-13
申请号：US11147055
申请日：2005-06-07
申请人： Joseph Zeldis , Gregg Feigelson , Ivo Jirkovsky
发明人： Joseph Zeldis , Gregg Feigelson , Ivo Jirkovsky
IPC分类号： C07D295/08 , C07B53/00 , C07C229/12 , C07D213/75 , C07D295/10 , C07D319/18 , C07D401/00 , C07D405/12 , C07D487/10 , A61K31/496 , C07C229/06 , C07D45/02
CPC分类号： C07D487/10 , C07B2200/07 , C07C229/12 , C07C309/06 , C07D319/18
摘要： A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.
摘要翻译：用于立体选择性制备新型手性氮芥衍生物的方法，其用于合成下式所示的光学活性1,4-二取代哌嗪：其中R，Ar和Q如本文所述定义，及其中间体化合物。 1,4-二取代的哌嗪作为可用于治疗中枢神经系统（CNS）障碍的5HT1A受体结合剂。

52. 发明申请

US20050209462A1 Synthesis of benzimidate from benzoic acid 有权
公开(公告)号：US20050209462A1
公开(公告)日：2005-09-22
申请号：US11008084
申请日：2004-12-09
申请人： Mukund Chorghade , Mukund Gurjar , Joseph Cherian
发明人： Mukund Chorghade , Mukund Gurjar , Joseph Cherian
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
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.

53. 发明授权

US06878828B2 Synthesis of 2-alkylcysteine via substituted thiazoline ester 有权
标题翻译：通过取代噻唑啉酯合成2-烷基半胱氨酸
公开(公告)号：US06878828B2
公开(公告)日：2005-04-12
申请号：US10439282
申请日：2003-05-15
申请人： Rayomand H. Gimi , Mukund S. Chorghade , Sunil V. Mhaskar
发明人： Rayomand H. Gimi , Mukund S. Chorghade , Sunil V. Mhaskar
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
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. In one embodiment, the present invention relates to a method of preparing a 2-alkylcysteine comprising condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, esterifying the 2-arylthiazoline-4-carboxylic acid using a substituted or unsubstituted alcohol group comprising one or more chiral carbons, and alkylating at the 4-position of the thiazoline ring to form a 2-aryl-4-alkyl-thiazoline-4-carboxylic acid ester. The chiral templates present in the thiazoline carboxylic acid ester can provide face selectivity, and consequently desired stereochemistry, during the delivery of an alkyl group to the 4-position of the thiazoline ring. 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 one embodiment, an aryl nitrile is condensed with cysteine or a 2-alkyl cysteine.
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。在一个实施方案中，本发明涉及制备2-烷基半胱氨酸的方法，其包括将半胱氨酸与芳基腈缩合以形成2-芳基噻唑啉-4-羧酸，使用取代或取代的2-芳基噻唑啉-4-羧酸酯化2-芳基噻唑啉-4-羧酸包含一个或多个手性碳的未取代的醇基，在噻唑啉环的4-位烷基化，形成2-芳基-4-烷基 - 噻唑啉-4-羧酸酯。存在于噻唑啉羧酸酯中的手性模板可以在将烷基递送至噻唑啉环的4-位期间提供面选择性，并因此提供所需的立体化学。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。在一个实施方案中，芳基腈与半胱氨酸或2-烷基半胱氨酸缩合。

54. 发明授权

US06861532B2 Synthesis of 2-alkylcysteine 有权
标题翻译： 2-烷基半胱氨酸的合成
公开(公告)号：US06861532B2
公开(公告)日：2005-03-01
申请号：US10438745
申请日：2003-05-15
申请人： Mukund S. Chorghade , Mukund K. Gurjar , Bhanu M. Chanda , Joseph Cherian
发明人： Mukund S. Chorghade , Mukund K. Gurjar , Bhanu M. Chanda , Joseph Cherian
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
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-alkylcysteine involves condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, followed by alkylating the 2-arylthiazoline-4-carboxylic acid at the 4-position. 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 or a 2-alkyl cysteine.
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-烷基半胱氨酸的方法包括将半胱氨酸与芳基腈缩合以形成2-芳基噻唑啉-4-羧酸，随后在4-位烷基化2-芳基噻唑啉-4-羧酸。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或2-烷基半胱氨酸缩合。

55. 发明申请

US20040110982A1 Process for preparing single enantiomers of 5,5,5,5',5',5'-hexafluoroleucine and protected analogs 失效
公开(公告)号：US20040110982A1
公开(公告)日：2004-06-10
申请号：US10663311
申请日：2003-09-16
发明人： James T. Anderson , Edward Neil Marsh , Peter Laurence Toogood
IPC分类号： C07C229/06
CPC分类号： C07C227/16 , C07C229/20
摘要： A process for synthesizing L and D-5,5,5,5null,5null,5null-hexafluoroleucine and protected analogs is disclosed. These compounds have utility in the preparation of fluorous peptides and proteins, which display interesting and unusual properties including strong self-association and an affinity for lipid bilayers.

56. 发明申请

US20020002298A1 Process for the production of esterquats 审中-公开
标题翻译：生产酯季铵盐的工艺
公开(公告)号：US20020002298A1
公开(公告)日：2002-01-03
申请号：US09854106
申请日：2001-05-11
发明人： Joaquim Bigorra Llosas , Rafael Pi Subirana , Nuria Bonastre Gilabert
IPC分类号： C07C229/06 , C11D001/38
CPC分类号： C07C213/06 , C07C213/08 , C07C219/06 , C07C219/08
摘要： The invention relates to a process for the production of esterquats in which triglycerides are transesterified with alkanolamines and the resulting fatty acid alkanolamine esters are subsequently quaternized with alkyl halides or dialkyl sulfates in the presence of solvents, characterized in that glycerol released during the transesterification is continuously removed from the reaction equilibrium.
摘要翻译：本发明涉及一种生产酯季铵盐的方法，其中甘油三酸酯与链烷醇胺进行酯交换，随后在溶剂存在下，将所得脂肪酸链烷醇胺酯与烷基卤化物或二烷基硫酸盐季铵化，其特征在于酯交换期间释放的甘油连续从反应平衡中除去。

57. 发明授权

US5708029A High blood pressure relief method and compositions 失效
标题翻译：高血压缓解方法和组合物
公开(公告)号：US5708029A
公开(公告)日：1998-01-13
申请号：US559758
申请日：1995-11-13
申请人： Arthur Vanmoor
发明人： Arthur Vanmoor
IPC分类号： A61K31/197 , A61K31/198 , A61K31/195 , C07C229/06
CPC分类号： A61K31/198 , A61K31/197
摘要： Disclosed is the method of determining the effectiveness of an agent for the relief of elevation of the blood pressure, comprising the steps of a) administering to a susceptible subject a quantity of a trigger substance reproducibly effective in producing within a period of six hours a perceptible increase in blood pressure lasting for at least twenty-four hours in the absence of treatment, b) administering to said subject having received said quantity of trigger substance a predetermined quantity of the agent whose effectiveness is to be determined, c) measuring the duration of said elevation of blood pressure upon administering said agent, and d) comparing the duration of said elevation with and without the administration of said agent. Also disclosed are effective quantities of certain nutrient substances which can reproducibly relieve elevated blood pressure produced in a susceptible subject by the administration of a trigger substance.
摘要翻译：公开了确定用于缓解血压升高的药剂的有效性的方法，包括以下步骤：a）向易感患者施用一定量的可触发性物质，其在六小时内可重现地产生有效的可察觉的在没有治疗的情况下，持续至少24小时的血压升高，b）对接受所述量的触发物质的所述受试者施用预定量的有效性的确定剂，c）测量持续时间所述药剂的给药时升高血压，和d）比较所述药物的施用时间和给药时间。还公开了通过施用触发物质可以可重复地缓解易感受试者产生的升高的血压的某些营养物质的有效量。

58. 发明授权

US5676926A Process for the production of DTPA-tetraesters of terminal carboxylic acids 失效
标题翻译：用于生产末端羧酸的DTPA-四酯的方法
公开(公告)号：US5676926A
公开(公告)日：1997-10-14
申请号：US634186
申请日：1996-04-18
申请人： Johannes Platzek , Ulrich Niedballa , Bernd Radeuchel
发明人： Johannes Platzek , Ulrich Niedballa , Bernd Radeuchel
IPC分类号： C07C227/08 , C07C229/16 , C07C229/36 , C07D213/55 , C07C229/06
CPC分类号： C07C229/16 , C07C227/08 , C07C229/36 , C07D213/55
摘要： The invention relates to a process for the production of diethylenetriaminepentacarboxylic acid tetraesters of general formula I ##STR1## in which R.sup.1 and Z have different meanings.
摘要翻译：本发明涉及一种制备通式Ⅰ的二亚乙基三胺四羧酸四酯的方法，其中R1和Z具有不同的含义。

59. 发明授权

US5639859A Carboxylate protective groups, a process for their preparation, their coupling to a functional group, and their use 失效
标题翻译：羧酸酯保护基团，其制备方法，与官能团的偶联及其用途
公开(公告)号：US5639859A
公开(公告)日：1997-06-17
申请号：US440836
申请日：1995-05-15
申请人： Horst Kunz , Gunther Braum , Peter Braun
发明人： Horst Kunz , Gunther Braum , Peter Braun
IPC分类号： C07K1/113 , C07C229/06 , C07C229/08 , C07C229/22 , C07C229/36 , C07C271/22 , C07K1/06 , C07K1/12 , C07K5/06 , C07K5/08 , C07K9/00 , C12P7/40
CPC分类号： C07K1/063 , C07C229/08 , C07C229/22 , C07C229/36 , C07C271/22 , C07K1/12 , Y02P20/55
摘要： Carboxylate protective groups, a process for their preparation, their coupling to a funcitonal group, and their useCarboxylates of polar, hydrophilic alcohols of the formula ##STR1## in which R is an unbranched or branched organic radical which contains, as polar members between aliphatic or araliphatic hydrocarbon bridges, ether oxygens, amine nitrogen groups or a mixture of ether and amine groups which can be incorporated into a cyclic structure, where the total length does not exceed 20 members and where, in the case of polyethylene glycol [(CH.sub.2 --CH.sub.2 --O).sub.n ], n indicates the number of the members and is defined as any integer, andR' is an aliphatic or araliphatic radical which has at least one functional group,are suitable as protective groups since they can be introduced selectively into functional groups of organic compounds and eliminated specifically by lipases.
摘要翻译：羧酸酯保护基团，它们的制备方法，它们与功能基团的偶联，以及它们的用途式为“IMAGE”的极性亲水醇的羧酸盐，其中R是无支链或支链的有机基团，其含有作为脂族或芳族烃桥，醚氧基，胺氮基团或可结合到环状结构中的醚和胺基团的混合物，其中总长度不超过20个成员，其中在聚乙二醇[（CH 2 - CH2-O）n]，n表示成员数，定义为任何整数，R'是具有至少一个官能团的脂族或芳脂族基，适合作为保护基，因为它们可以选择性地引入有机化合物的官能团，并由脂肪酶特异性消除。

60. 发明授权

US5536815A Cyclopropyl based O- and N- and S-protecting groups 失效
标题翻译：环丙基O-和N-和S-保护基
公开(公告)号：US5536815A
公开(公告)日：1996-07-16
申请号：US221226
申请日：1994-03-31
申请人： Louis A. Carpino , Hann-Guang Chao
发明人： Louis A. Carpino , Hann-Guang Chao
IPC分类号： C07C271/22 , C07C271/34 , C07K1/06 , C07C229/06 , C07C229/12 , C07C321/04
CPC分类号： C07K1/066 , C07C271/22 , C07C271/34 , C07K1/063 , C07K1/064 , C07K1/065 , C07K1/067 , C07K1/068 , C07C2101/02 , C07C2103/18 , Y02P20/55
摘要： The present invention is directed to the use of a cyclopropylmethyl derivative as a protecting group for compounds containing an amino group, carboxy group, amido group, mercapto group or hydroxy group and to the compounds formed having the cyclopropylmethyl moiety as the protecting group.
摘要翻译：本发明涉及环丙基甲基衍生物作为保护基用于含有氨基，羧基，酰氨基，巯基或羟基的化合物以及形成的具有环丙基甲基部分作为保护基的化合物的用途。

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