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81. 发明申请

US20140275088A1 SMALL MOLECULE MALARIAL ALDOLASE-TRAP ENHANCERS AND GLIDEOSOME INHIBITORS 有权
标题翻译：小分子MALALAL ALDOLASE-TRAP增强剂和GLIDEOSOME抑制剂
公开(公告)号：US20140275088A1
公开(公告)日：2014-09-18
申请号：US14353438
申请日：2012-10-25
申请人： NEW YORK UNIVERSITY , JOHNS HOPKINS UNIVERSITY
发明人： Timothy J. Cardozo , Jürgen Bosch , Sondra Maureen Nemetski
IPC分类号： C07C249/16 , C07D215/14 , C07D333/24 , C07D207/337 , C07C235/78 , G06F19/12 , C07D239/47 , C07D487/04 , C07D239/46 , G06F19/16 , C12Q1/527 , C07C243/18 , C07D271/12
CPC分类号： C07C249/16 , C07C235/78 , C07C243/18 , C07D207/337 , C07D215/14 , C07D239/46 , C07D239/47 , C07D239/54 , C07D271/12 , C07D277/34 , C07D333/24 , C07D487/04 , C12Q1/527 , G01N2333/44 , G01N2333/445 , G01N2500/04 , G06F19/12 , G06F19/16
摘要： In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase. The method includes providing a first model comprising Aldolase or residues of the amino acid sequence corresponding to SEQ ID NO: 1 said residues being at amino acid positions selected from the group consisting of 10-13, 26, 27, 29, 30, 31, 32, 33, 37, 39, 40, 41, 43, 44, 47, 48, 51, 52, 60, 63, 66, 79, 84, 85, 92, 93, 103, 106-109, 112-117, 138, 142, 146, 148, 151, 153, 179, 182, 183, 185, 186, 194, 196, 197, 198, 199, 208, 226-228, 231-269, 270, 272, 277-283, 285-289, 294, 295, 297-299, 301-304, 306-310 312, 313, 316, 317, 319, 321, 323, 326, 330, 344, 345, and 347, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for modifying the activity of Aldolase. The present invention also discloses compounds and compositions which modify the activity of Aldolase, or a complex between Aldolase and TRAP. Methods of treating or preventing malaria, or an infection by apicomplexan organisms are also disclosed.
摘要翻译：一方面，本发明涉及鉴定可用于改变醛缩酶活性的化合物的方法。该方法包括提供包含Aldolase或对应于SEQ ID NO：1的氨基酸序列的残基的第一模型，所述残基位于选自下组的氨基酸位置：10-13,26,27,29,30,31， 32，33，37，39，40，41，43，44，47，48，51，52，60，63，66，79，84，85，92，93，103，106-109，112-117， 138,142,146,148,151,153,179,182,183,185,186,194,196,197,198,199,208,226-228,231-269,270,272,277-283， 285-289,294,295,297-299,301-304,306-310 312,313,316,317,319,321,232,326,330,344,345和347，提供一种或多种候选化合物评估候选化合物与第一模型之间的接触以确定一种或多种候选化合物中的哪一种具有结合和/或适合于第一模型的能力，以及鉴定化合物，其基于所述评估具有与第一模型结合和/或适合作为可能用于改变醛缩酶活性的化合物。本发明还公开了改变Aldolase活性的化合物和组合物，或Aldolase和TRAP之间的复合物。还公开了治疗或预防疟疾或由复合物有机体感染的方法。

82. 发明申请

US20140197024A1 MICROWAVE INDUCED SINGLE STEP GREEN SYNTHESIS OF SOME NOVEL 2-ARYL ALDEHYDES AND THEIR ANALOGUES 审中-公开
标题翻译：微波诱导的单步绿色合成一些新型二芳基醛及其类似物
公开(公告)号：US20140197024A1
公开(公告)日：2014-07-17
申请号：US14156862
申请日：2014-01-16
申请人： COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
发明人： Arun Kumar SINHA , Abhishek SHARMA , Rakesh KUMAR , Naina SHARMA
IPC分类号： C07C45/28 , C07D317/54 , C07C249/16
CPC分类号： C07C45/28 , C07C45/30 , C07C249/16 , C07C311/49 , C07D317/54 , C07C47/228 , C07C47/24 , C07C47/23 , C07C47/277
摘要： A microwave-induced process for the preparation of 2-aryl and 2,2-diaryl aldehydes and analogues wherein halohydrin formation and subsequent rearrangement to 2-aryl aldehydes from corresponding aryl alkanols occurs without formation of an intermediate epoxide or use of transition metal catalysts or lewis acids/bases.
摘要翻译：用于制备2-芳基和2,2-二芳基醛和类似物的微波诱导方法，其中卤代醇形成和随后的从相应的芳基链烷醇重新排列成2-芳基醛而不形成中间体环氧化物或使用过渡金属催化剂或路易斯酸/碱。

83. 发明授权

US08779200B2 Microwave induced single step green synthesis of some novel 2-aryl aldehydes and their analogues 失效
标题翻译：微波诱导单步绿色合成一些新型2-芳基醛及其类似物
公开(公告)号：US08779200B2
公开(公告)日：2014-07-15
申请号：US13203100
申请日：2010-02-25
申请人： Arun Kumar Sinha , Abhishek Sharma , Rakesh Kumar , Naina Sharma
发明人： Arun Kumar Sinha , Abhishek Sharma , Rakesh Kumar , Naina Sharma
IPC分类号： C07C241/00 , C07C47/00
CPC分类号： C07C45/28 , C07C45/30 , C07C249/16 , C07C311/49 , C07D317/54 , C07C47/228 , C07C47/24 , C07C47/23 , C07C47/277
摘要： The present invention provides a process for the preparation of some novel 2-aryl and 2,2-diaryl aldehydes and analogues which are privileged intermediates for commercially important nonsteroidal anti-inflammatory drugs including naproxen, flurbiprofen and potent anticancer drug candidates, including phenstatin through a unique single step synthetic methodology utilizing easily available substrates in the form of aryl alkenes as well as environmentally benign aqueous reaction conditions in the form of solvents such as mixtures of water and DMSO or Dioxane and reagents N-bromosuccinimide, N-iodosuccinimide, N-cholorosuccinimide and phase transfer catalyst such as cetyltrimethyl ammonium bromide, N-hexyl ammonium chloride for a reaction time varying from 1 min-30 min, depending upon microwave or conventional heating, without using expensive transition metal catalysts or lewis acids/bases with yield varying from 35-55%, depending upon the solvent and substrate used. The developed method provides a clean and convenient alternative to access a diverse range of medicinally important 2-aryl and 2,2-diaryl aldehyde based scaffolds in lieu of the conventional multistep protocols employing expensive and hazardous transition metal catalysts and lewis acids/bases.
摘要翻译：本发明提供了一种制备一些新的2-芳基和2,2-二芳基醛和类似物的方法，其是用于商业上重要的非甾族抗炎药物的特权中间体，包括萘普生，氟比洛芬和有效的抗癌药物候选物，包括通过使用易于获得的芳基烯烃底物的独特的单步合成方法以及溶剂形式的环境友好的水性反应条件，例如水和DMSO或二恶烷的混合物以及试剂N-溴琥珀酰亚胺，N-碘代琥珀酰亚胺，N-氯代氯代琥珀酰亚胺和相转移催化剂如十六烷基三甲基溴化铵，N-己基氯化铵，反应时间为1分钟-30分钟，取决于微波或常规加热，不使用昂贵的过渡金属催化剂或路易斯酸/碱，产率从35 -55％，这取决于所用的溶剂和底物。开发的方法提供了一种干净和方便的替代方案，以便获得各种各样的药物重要的2-芳基和2,2-二芳基醛基支架，代替常规的多步骤方案，其采用昂贵且危险的过渡金属催化剂和路易斯酸/碱。

84. 发明申请

US20120041234A1 MICROWAVE INDUCED SINGLE STEP GREEN SYNTHESIS OF SOME NOVEL 2-ARYL ALDEHYDES AND THEIR ANALOGUES 失效
标题翻译：微波诱导的单步绿色合成一些新型二芳基醛及其类似物
公开(公告)号：US20120041234A1
公开(公告)日：2012-02-16
申请号：US13203100
申请日：2010-02-25
申请人： Arun Kumar Sinha , Abhishek Sharma , Rakesh Kumar , Naina Sharma
发明人： Arun Kumar Sinha , Abhishek Sharma , Rakesh Kumar , Naina Sharma
IPC分类号： C07C251/80 , C07C45/00 , B01J19/12 , C07C47/27
CPC分类号： C07C45/28 , C07C45/30 , C07C249/16 , C07C311/49 , C07D317/54 , C07C47/228 , C07C47/24 , C07C47/23 , C07C47/277
摘要： The present invention provides a process for the preparation of some novel 2-aryl and 2,2-diaryl aldehydes and analogues which are privileged intermediates for commercially important nonsteroidal anti-inflammatory drugs including naproxen, flurbiprofen and potent anticancer drug candidates, including phenstatin through a unique single step synthetic methodology utilizing easily available substrates in the form of aryl alkenes as well as environmentally benign aqueous reaction conditions in the form of solvents such as mixtures of water and DMSO or Dioxane and reagents N-bromosuccinimide, N-iodosuccinimide, N-cholorosuccinimide and phase transfer catalyst such as cetyltrimethyl ammonium bromide, N-hexyl ammonium chloride for a reaction time varying from 1 min-30 min, depending upon microwave or conventional heating, without using expensive transition metal catalysts or lewis acids/bases with yield varying from 35-55%, depending upon the solvent and substrate used. The developed method provides a clean and convenient alternative to access a diverse range of medicinally important 2-aryl and 2,2-diaryl aldehyde based scaffolds in lieu of the conventional multistep protocols employing expensive and hazardous transition metal catalysts and lewis acids/bases.
摘要翻译：本发明提供了一种制备一些新的2-芳基和2,2-二芳基醛和类似物的方法，其是用于商业上重要的非甾族抗炎药物的特权中间体，包括萘普生，氟比洛芬和有效的抗癌药物候选物，包括通过使用易于获得的芳基烯烃底物的独特的单步合成方法以及溶剂形式的环境友好的水性反应条件，例如水和DMSO或二恶烷的混合物以及试剂N-溴琥珀酰亚胺，N-碘代琥珀酰亚胺，N-氯代氯代琥珀酰亚胺和相转移催化剂如十六烷基三甲基溴化铵，N-己基氯化铵，反应时间为1分钟-30分钟，取决于微波或常规加热，不使用昂贵的过渡金属催化剂或路易斯酸/碱，产率从35 -55％，这取决于所用的溶剂和底物。开发的方法提供了一种干净和方便的替代方案，以便获得各种各样的药物重要的2-芳基和2,2-二芳基醛基支架，代替常规的多步骤方案，其采用昂贵且危险的过渡金属催化剂和路易斯酸/碱。

85. 发明授权

US08044241B2 Ligands for estrogen related receptors and methods for synthesis of said ligands 有权
标题翻译：雌激素相关受体的配体和合成所述配体的方法
公开(公告)号：US08044241B2
公开(公告)日：2011-10-25
申请号：US12475323
申请日：2009-05-29
申请人： Barry Forman , Donna Yu
发明人： Barry Forman , Donna Yu
IPC分类号： C07C243/18
CPC分类号： C07D333/44 , C07C249/16 , C07D207/335 , C07D207/34 , C07D251/46 , C07D307/52 , C07D333/22 , C07C251/86
摘要： Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.
摘要翻译：描述了雌激素相关受体（ERR）调节化合物和合成所述化合物的方法。

86. 发明申请

US20090318693A1 LIGANDS FOR ESTROGEN RELATED RECEPTORS AND METHODS FOR SYNTHESIS OF SAID LIGANDS 有权
标题翻译：雌激素相关受体的配体和合成配体的方法
公开(公告)号：US20090318693A1
公开(公告)日：2009-12-24
申请号：US12475323
申请日：2009-05-29
申请人： Barry Forman , Donna Yu
发明人： Barry Forman , Donna Yu
IPC分类号： C07D251/30 , C07D333/22 , C07D307/02 , C07D207/30
CPC分类号： C07D333/44 , C07C249/16 , C07D207/335 , C07D207/34 , C07D251/46 , C07D307/52 , C07D333/22 , C07C251/86
摘要： Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.
摘要翻译：描述了雌激素相关受体（ERR）调节化合物和合成所述化合物的方法。

87. 发明申请

US20080033171A1 Ligands for Metals and Improved Metal-Catalyzed Processes Based Thereon 有权
标题翻译：金属配体和改进的金属催化工艺
公开(公告)号：US20080033171A1
公开(公告)日：2008-02-07
申请号：US11781651
申请日：2007-07-23
申请人： Stephen Buchwald , David Old , John Wolfe , Michael Palucki , Ken Kamikawa
发明人： Stephen Buchwald , David Old , John Wolfe , Michael Palucki , Ken Kamikawa
IPC分类号： C07D295/00 , C07D211/70 , C07F7/04 , C07F9/02
CPC分类号： C07C1/26 , C07C1/321 , C07C17/16 , C07C17/263 , C07C29/32 , C07C29/38 , C07C37/18 , C07C41/30 , C07C45/68 , C07C45/71 , C07C49/675 , C07C67/31 , C07C201/12 , C07C209/10 , C07C209/18 , C07C211/59 , C07C213/02 , C07C213/08 , C07C221/00 , C07C225/12 , C07C227/08 , C07C227/18 , C07C231/08 , C07C231/12 , C07C249/02 , C07C249/16 , C07C251/24 , C07C253/30 , C07C2531/24 , C07C2531/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/50 , C07D213/72 , C07D213/74 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/1892 , C07F9/4875 , C07F9/5022 , C07F9/5027 , C07F9/5728 , C07F9/653 , C07F9/6547 , C07F9/65719 , C07F15/0066 , C07C25/18 , C07C49/255 , C07C49/213 , C07C49/657 , C07C49/67 , C07C49/84 , C07C49/245 , C07C49/755 , C07C49/215 , C07C49/683 , C07C47/575 , C07C49/782 , C07C69/92 , C07C211/48 , C07C211/55 , C07C217/40 , C07C217/84 , C07C217/92 , C07C225/22 , C07C229/36 , C07C229/60 , C07C233/07 , C07C235/46 , C07C251/86 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07C15/14 , C07C35/21 , C07C33/24 , C07C205/04 , C07C205/06 , C07C43/205 , C07C43/225 , C07C39/15 , C07C35/08
摘要： One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
摘要翻译：本发明的一个方面涉及用于过渡金属的新配体。本发明的第二方面涉及包含这些配体的催化剂在过渡金属催化的碳 - 杂原子和碳 - 碳键形成反应中的用途。本发明方法提供了过渡金属催化反应的许多特征的改进，包括合适底物的范围，反应条件和效率。

88. 发明申请

US20080015387A1 Process for Producing Hydrazone Compound 失效
标题翻译：生产腙化合物的方法
公开(公告)号：US20080015387A1
公开(公告)日：2008-01-17
申请号：US11571399
申请日：2005-06-28
申请人： Kiyokazu Takaso , Katsumi Abe , Atsushi Takesue
发明人： Kiyokazu Takaso , Katsumi Abe , Atsushi Takesue
IPC分类号： C07C249/16
CPC分类号： C07C249/16 , C07C241/02 , C07C251/86 , C07C243/22
摘要： The present invention provides a process for producing a hydrazone compound represented by the general formula (5): which comprises a step of condensing a hydrazine compound represented by the general formula (3): with a carbonyl compound represented by the general formula (4): without taking the hydrazine compound out of a reactor According to the invention, the target hydrazone compound can be obtained in high quality and in a high yield without taking the hydrazine compound out of the reactor at all, the hydrazine compound being a reaction intermediate which is structurally unstable and has a fear of influencing safety of workers owing to its toxicity (mutagenicity).
摘要翻译：本发明提供由通式（5）表示的腙化合物的制造方法：其包括将通式（3）表示的肼化合物与通式（4）表示的羰基化合物缩合的工序，：不将肼化合物从反应器中取出根据本发明，可以以高品质和高产率获得目标腙化合物，而不将肼化合物从反应器中取出，肼化合物是反应中间体，其中在结构上是不稳定的，并且由于其毒性（致突变性）而害怕影响工人的安全。

89. 发明申请

US20060264673A1 Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds 有权
公开(公告)号：US20060264673A1
公开(公告)日：2006-11-23
申请号：US11431154
申请日：2006-05-09
申请人： Stephen Buchwald , Artis Klapars , Jon Antilla , Gabriel Job , Martina Wolter , Fuk Kwong , Gero Nordmann , Edward Hennessy
发明人： Stephen Buchwald , Artis Klapars , Jon Antilla , Gabriel Job , Martina Wolter , Fuk Kwong , Gero Nordmann , Edward Hennessy
IPC分类号： C07C209/10
CPC分类号： C07F9/4056 , C07B37/04 , C07B41/04 , C07B43/04 , C07C41/16 , C07C45/68 , C07C45/71 , C07C51/353 , C07C67/343 , C07C209/10 , C07C213/08 , C07C221/00 , C07C227/18 , C07C231/08 , C07C231/12 , C07C241/04 , C07C249/02 , C07C249/16 , C07C253/14 , C07C253/30 , C07C269/06 , C07C273/1854 , C07C277/08 , C07C281/02 , C07C303/38 , C07C319/20 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D205/08 , C07D207/16 , C07D207/267 , C07D207/27 , C07D207/323 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/48 , C07D209/86 , C07D211/26 , C07D211/76 , C07D213/30 , C07D213/64 , C07D213/74 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/56 , C07D235/06 , C07D237/32 , C07D239/42 , C07D245/06 , C07D249/08 , C07D249/18 , C07D263/22 , C07D295/023 , C07D295/033 , C07D295/073 , C07D307/79 , C07D333/36 , C07D333/66 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D471/04 , C07D473/00 , C07C49/84 , C07C59/68 , C07C69/76 , C07C69/65 , C07C69/612 , C07C69/734 , C07C69/616 , C07C69/732 , C07C311/21 , C07C323/41 , C07C211/48 , C07C211/52 , C07C211/55 , C07C211/54 , C07C215/68 , C07C217/84 , C07C215/16 , C07C225/22 , C07C217/08 , C07C229/56 , C07C229/60 , C07C211/58 , C07C243/38 , C07C251/86 , C07C43/205 , C07C43/2055 , C07C43/235 , C07C43/23 , C07C43/16 , C07C43/215 , C07C43/225 , C07C237/30 , C07C255/58 , C07C233/07
摘要： The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-oxygen bond between the oxygen atom of an alcohol and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. The present invention also relates to copper-catalyzed methods of forming a carbon-carbon bond between a reactant comprising a nucleophilic carbon atom, e.g., an enolate or malonate anion, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. Importantly, all the methods of the present invention are relatively inexpensive to practice due to the low cost of the copper comprised by the catalysts.

90. 发明授权

US07138548B2 Process for the preparation of aryl hydrazone and aryl hydrazine 失效
标题翻译：芳基腙和芳基肼的制备方法
公开(公告)号：US07138548B2
公开(公告)日：2006-11-21
申请号：US10493503
申请日：2002-10-02
申请人： Andrew John Blacker , David Dodman , David Anthony Jackson , Jan Michael Fielden , John Heathcote Atherton
发明人： Andrew John Blacker , David Dodman , David Anthony Jackson , Jan Michael Fielden , John Heathcote Atherton
IPC分类号： C07C249/16 , C07C241/02
CPC分类号： C07C249/16 , C07C251/86
摘要： A process for the preparation of a compound of formula (I): wherein Ar represents an optionally substituted aromatic carbocycle or heterocycle, and R1 and R2 independently represent hydrogen, C1-10 alkyl, C(O)C1-10 alkyl or optionally substituted aryl provided that R1 and R2 are not both hydrogen which process comprises reacting together a compound of formula (II): Ar—X (II) wherein Ar is as defined in relation to formula (I) and X represents a leaving group with a a compound of formula (III) wherein R1 and R2 are as defined in relation to formula (I) under aqueous conditions in the presence of a Pd (II) salt, a ligand and a Group I or Group II metal hydroxide base at a pH greater than 7. Compounds of formula (I) may be hydrolysed to the corresponding hydrazine.
摘要翻译：制备式（I）化合物的方法：其中Ar表示任选取代的芳族碳环或杂环，R 1和R 2独立地表示氢，C C（O）C 1-10烷基或任选取代的芳基，条件是R 1和R 2可以相同或不同，（II）的化合物反应：式中，式（II）所示的化合物与式（II）化合物反应：＆lt;线内公式描述=“In-Line Formula”end =“lead”→Ar-X 其中Ar如关于式（I）所定义，X表示具有式（III）化合物的离去基团，其中R

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