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1. 发明申请

US20190100490A1 MULTI-DIRECTIONAL POLYDENTATE LIGANDS FOR METAL-ORGANIC HYBRID STRUCTURES 审中-公开
公开(公告)号：US20190100490A1
公开(公告)日：2019-04-04
申请号：US16085525
申请日：2017-07-28
申请人： LG CHEM, LTD. , Seoul National University R&DB Foundation
发明人： Dongwhan LEE , Jung Hwan KIM , Won Jong KWON , Yong Jin BAE
IPC分类号： C07C249/02 , B01J31/22 , C07C249/16 , C07D213/86
CPC分类号： C07C249/02 , B01J31/2243 , B01J2531/004 , B01J2531/26 , B01J2531/38 , B01J2531/46 , B01J2531/48 , B01J2531/56 , B01J2531/64 , B01J2531/72 , B01J2531/82 , B01J2531/842 , B01J2531/845 , B01J2531/847 , C07C249/16 , C07C251/24 , C07C251/48 , C07C251/86 , C07D213/86 , C07D251/24 , C07D251/48 , C07D401/14
摘要： A compound represented by Chemical Formula 1 according to the present invention can coordinate with metal ions to form a bidirectional or multidirectional metal-organic hybrid structure. Thus, the present invention can synthesize various ligands using amine-aldehyde condensation, and synthesize metal-organic materials using the same.

2. 发明授权

US09873661B2 Small molecule malarial Aldolase-TRAP enhancers and glideosome inhibitors 有权
公开(公告)号：US09873661B2
公开(公告)日：2018-01-23
申请号：US14353438
申请日：2012-10-25
申请人： NEW YORK UNIVERSITY , THE JOHNS HOPKINS UNIVERSITY
发明人： Timothy J. Cardozo , Jürgen Bosch , Sondra Maureen Nemetski
IPC分类号： A61K31/535 , C07C249/16 , C12Q1/527 , C07D239/54 , C07D277/34 , C07C235/78 , C07C243/18 , C07D207/337 , C07D215/14 , C07D239/46 , C07D239/47 , C07D271/12 , C07D333/24 , C07D487/04 , G06F19/12 , G06F19/16
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.

3. 发明授权

US09751835B2 Processes and intermediates for preparing indole pharmaceuticals 有权
公开(公告)号：US09751835B2
公开(公告)日：2017-09-05
申请号：US14890514
申请日：2014-05-13
申请人： INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
发明人： James R. McCarthy
IPC分类号： C07D209/04 , C07D401/12 , C07D403/12 , C07D209/14 , B01J23/44 , C07C249/16 , C07D295/135
CPC分类号： C07D209/14 , B01J23/44 , C07C249/16 , C07D295/135 , C07D403/12
摘要： The invention described herein pertains to processes and intermediates for preparing indole containing pharmaceuticals, particularly to processes and intermediates for preparing selective estrogen receptor modulators, such as bazedoxifene.

4. 发明授权

US09580382B2 p62-ZZ chemical inhibitor 有权
标题翻译： p62-ZZ化学抑制剂
公开(公告)号：US09580382B2
公开(公告)日：2017-02-28
申请号：US14237494
申请日：2012-08-08
申请人： Xiang-Qun Xie , Garson David Roodman , Kyaw-Zeyar Myint , Noriyoshi Kurihara
发明人： Xiang-Qun Xie , Garson David Roodman , Kyaw-Zeyar Myint , Noriyoshi Kurihara
IPC分类号： C07D475/08 , C07C229/36 , C07D309/40 , C07C211/50 , C07C317/34 , C07C217/58 , C07C217/76 , C07C219/06 , C07D241/44 , C07C229/14 , C07D487/04 , C07C235/48 , C07C251/76 , A61K31/137 , A61K31/351 , A61K31/495 , A61K31/519 , A61K31/15 , A61K31/498 , A61K45/06 , C07C249/16 , C07D309/32 , C12N5/09 , A61K31/216
CPC分类号： C07C229/36 , A61K31/137 , A61K31/15 , A61K31/216 , A61K31/351 , A61K31/495 , A61K31/498 , A61K31/519 , A61K45/06 , C07C211/50 , C07C217/58 , C07C217/76 , C07C219/06 , C07C229/14 , C07C235/48 , C07C249/16 , C07C251/76 , C07C317/34 , C07D241/44 , C07D309/32 , C07D309/40 , C07D475/08 , C07D487/04 , C12N5/0693
摘要： A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.
摘要翻译：一种用于治疗受试者中p62介导的疾病（例如多发性骨髓瘤）的方法，所述方法包括向受试者施用治疗有效量的至少一种p62-ZZ抑制剂化合物。

5. 发明授权

US09201001B2 Visual detection of fluoride ions 有权
标题翻译：目视检测氟离子
公开(公告)号：US09201001B2
公开(公告)日：2015-12-01
申请号：US14459956
申请日：2014-08-14
申请人： INDIAN INSTITUTE OF TECHNOLOGY MADRAS
发明人： Prasad Edamana , Rajamalli Pachaiyappan
IPC分类号： C07C243/38 , G01N21/29 , C07C249/16 , G01N21/64 , C07C251/84
CPC分类号： G01N21/29 , C07C243/38 , C07C249/16 , C07C251/84 , G01N21/6447 , Y10T436/19
摘要： Dendrimer-hydrazides are coupled to polycyclic aromatic hydrocarbons for use in the visual detection of the presence of low levels of fluoride in a sample. The dendrimers can have a phenyl core, a first generation of aralkyl ethers, and an optional second generation of aralkyl ethers. The compounds form gels with solvents. In the presence of fluoride ion, the gels undergo color changes and/or gel to liquid phase change.
摘要翻译：树枝状酰肼与多环芳烃偶联，用于视觉检测样品中低含量氟化物的存在。树枝状聚合物可以具有苯基核心，第一代芳烷基醚和任选的第二代芳烷基醚。化合物与溶剂形成凝胶。在存在氟离子的情况下，凝胶会发生颜色变化和/或凝胶转变为液相变化。

6. 发明授权

US09067955B2 Copper-catalyzed formation of carbon-heteroatom and carbon—carbon bonds 有权
标题翻译：铜催化形成碳 - 杂原子和碳 - 碳键
公开(公告)号：US09067955B2
公开(公告)日：2015-06-30
申请号：US11431154
申请日：2006-05-09
申请人： Stephen L. Buchwald , Artis Klapars , Jon C. Antilla , Gabriel E. Job , Martina Uhlenbrock , Fuk Y. Kwong , Gero Nordmann , Edward J. Hennessy
发明人： Stephen L. Buchwald , Artis Klapars , Jon C. Antilla , Gabriel E. Job , Martina Uhlenbrock , Fuk Y. Kwong , Gero Nordmann , Edward J. Hennessy
IPC分类号： C07F5/02 , C07C47/00 , C07C201/00 , C07C205/00 , C07B41/00 , C07C27/10 , C07F9/40 , C07B37/04 , C07B41/04 , C07B43/04 , C07C41/16 , C07C45/68 , C07C45/71 , C07C51/353 , C07C67/343 , C07C209/10 , C07C213/08 , C07C221/00 , C07C227/18 , C07C231/12 , C07C241/04 , C07C249/02 , C07C249/16 , C07C253/14 , C07C253/30 , C07C269/06 , C07C273/18 , C07C277/08 , C07C281/02 , C07C303/38 , C07C319/20 , 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 , C07C231/08
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, such as the reaction of Z-X with C(L)(R)(R′)2 in the present of a catalyst and a base, thereby forming C(Z)(R)(R′)2; wherein X represents I, Cl, alkylsulfonate, or arylsulfonate; Z represents optionally substituted aryl, heteroaryl or alkenyl; L represents H or a negative charge; catalyst comprises a copper atom or ion, and a ligand, wherein the ligand is an optionally substituted aryl alcohol, alkyl amine, 1,2-diamine, 1,2-aminoalcohol, 1,2-diol, imidazolium carbene, pyridine, or 1,10-phenanthroline; the ligand is a chelating ligand; and the base represents a Bronsted base; R represents H, optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; R′ represents independently for each occurrence H, alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl, formyl, acyl, —CO2R″, —C(O)N(R)2, sulfonyl, —P(O)(OR″)2, —CN, or —NO2; R″ represents independently for each occurrence optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; and C(R′)2(R) taken together may represent nitrile.
摘要翻译：本发明涉及铜催化的碳 - 杂原子和碳 - 碳键形成方法，例如在催化剂和碱的存在下ZX与C（L）（R）（R'）2的反应，从而形成C（Z）（R）（R'）2; 其中X表示I，Cl，烷基磺酸酯或芳基磺酸酯; Z表示任选取代的芳基，杂芳基或烯基; L表示H或负电荷; 催化剂包括铜原子或离子以及配体，其中配体是任选取代的芳基醇，烷基胺，1,2-二胺，1,2-氨基醇，1,2-二醇，咪唑鎓卡宾，吡啶或1 ，10-菲咯啉; 配体是螯合配体; 基地代表布朗斯台基地; R表示H，任选取代的烷基，环烷基，芳烷基，芳基或杂芳基; R'独立地表示H，烷基，环烷基，芳烷基，芳基或杂芳基，甲酰基，酰基，-CO 2 R“，-C（O）N（R）2，磺酰基，-P（O） 2，-CN或-NO 2; 任选取代的烷基，环烷基，芳烷基，芳基或杂芳基; 和C（R'）2（R）在一起可以代表腈。

7. 发明授权

US07582799B2 Method for producing hydrazone derivatives 有权
标题翻译：腙衍生物的制备方法
公开(公告)号：US07582799B2
公开(公告)日：2009-09-01
申请号：US11911441
申请日：2006-04-27
申请人： Hiroshi Yoshino , Kentaro Kobayashi , Yuichi Shiro
发明人： Hiroshi Yoshino , Kentaro Kobayashi , Yuichi Shiro
IPC分类号： C07C315/02 , C07C45/41 , C07C45/54 , C07C241/00
CPC分类号： C07C315/02 , C07C45/518 , C07C249/16 , C07C47/19 , C07C317/18 , C07C251/76
摘要： The present invention provides an industrially advantageous process for producing hydrazone derivative represented by the formula (5), which is shown by the following reaction formula.
摘要翻译：本发明提供了一种工业上有利的制备由式（5）表示的腙衍生物的方法，其由下列反应式表示。

8. 发明授权

US07557248B2 Method of forming a carbon-heteroatom bond 失效
标题翻译：形成碳 - 杂原子键的方法
公开(公告)号：US07557248B2
公开(公告)日：2009-07-07
申请号：US10556849
申请日：2004-05-12
申请人： Christelle Mauger , Gérard Mignani
发明人： Christelle Mauger , Gérard Mignani
IPC分类号： C07C241/00
CPC分类号： C07C249/16 , C07C251/86
摘要： The present invention relates to a method of creating a carbon-heteroatom bond, and preferably a carbon-nitrogen bond, by reacting a leaving group-bearing unsaturated compound and a nucleophilic compound. In particular, the invention relates to the creation of a carbon-nitrogen bond, using a method involving the arylation of nitrogenous organic derivatives; the inventive method consists in creating a carbon-heteroatom bond by reacting a leaving group-bearing unsaturated compound and a nucleophilic compound introducing a heteroatom which can be substituted for the leaving group, thereby creating a carbon-heteroatom bond, in the presence of a palladium-based catalyst, optionally a ligand. The invention is characterized in that the reaction takes place in the presence of an effective quantity of a metal hydroxide or ammonium hydroxide which is associated with an alcohol-type solvent.
摘要翻译：本发明涉及通过使含离去基团的不饱和化合物与亲核性化合物反应而产生碳 - 杂原子键，优选碳 - 氮键的方法。特别地，本发明涉及使用涉及含氮有机衍生物的芳基化的方法产生碳 - 氮键; 本发明的方法包括通过使带有离去基团的不饱和化合物和引入可被取代离去基团的杂原子的亲核化合物反应产生碳 - 杂原子键，从而在钯的存在下产生碳 - 杂原子键的催化剂，任选的配体。本发明的特征在于反应在有效量的与醇型溶剂相关的金属氢氧化物或氢氧化铵的存在下进行。

9. 发明授权

US07223879B2 Ligands for metals and improved metal-catalyzed processes based thereon 有权
标题翻译：金属配体和基于其的改进的金属催化方法
公开(公告)号：US07223879B2
公开(公告)日：2007-05-29
申请号：US10731702
申请日：2003-12-09
申请人： Stephen L. Buchwald , Xiaohua Huang , Danilo Zim
发明人： Stephen L. Buchwald , Xiaohua Huang , Danilo Zim
IPC分类号： C07F15/04 , C07F17/02 , C07F9/02 , C07C291/02 , C07C207/02
CPC分类号： C07D213/74 , C07B37/04 , C07C1/26 , C07C17/263 , C07C29/32 , C07C37/11 , C07C41/30 , C07C45/68 , C07C45/71 , C07C67/31 , C07C67/343 , C07C201/12 , C07C209/10 , C07C209/18 , C07C211/59 , C07C213/02 , C07C213/08 , C07C221/00 , C07C225/12 , C07C227/08 , C07C227/18 , C07C231/12 , C07C249/02 , C07C249/16 , C07C251/24 , C07C253/30 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/50 , C07D213/72 , C07D295/023 , C07D295/033 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/135 , C07D295/155 , C07D307/33 , C07D317/22 , C07D317/26 , C07D317/66 , C07D333/08 , C07D333/66 , C07D401/04 , C07F7/1892 , C07F9/4875 , C07F9/5018 , C07F9/5022 , C07F9/5027 , C07F9/5728 , C07F9/653 , C07F9/6547 , C07F9/65719 , C07F15/0066 , C07C25/18 , C07C49/245 , C07C49/782 , C07C49/67 , C07C49/755 , C07C49/683 , C07C49/213 , C07C49/255 , C07C47/575 , C07C49/84 , C07C49/657 , C07C49/215 , C07C69/92 , C07C69/76 , C07C69/616 , C07C69/612 , C07C211/45 , C07C211/48 , C07C211/52 , C07C211/55 , C07C217/40 , C07C217/84 , C07C217/92 , C07C225/22 , C07C229/36 , C07C229/60 , C07C233/07 , C07C233/43 , C07C235/46 , C07C237/30 , C07C251/86 , C07C255/33 , C07C255/50 , C07C255/54 , C07C255/56 , C07C255/58 , C07C205/04 , C07C205/06 , C07C43/205 , C07C43/225 , C07C39/15 , C07C33/24
摘要： One aspect of the present invention relates to 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过渡金属配体。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。

10. 发明授权

US07115784B2 Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds 有权
公开(公告)号：US07115784B2
公开(公告)日：2006-10-03
申请号：US11028500
申请日：2005-01-04
申请人： Stephen L. Buchwald , Artis Klapars , Jon C. Antilla , Gabriel E. Job , Martina Wolter , Fuk Y. Kwong , Gero Nordmann , Edward J. Hennessy
发明人： Stephen L. Buchwald , Artis Klapars , Jon C. Antilla , Gabriel E. Job , Martina Wolter , Fuk Y. Kwong , Gero Nordmann , Edward J. Hennessy
IPC分类号： C07C41/00 , C07C43/02 , C07C43/20
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.

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