- THIOAMIDE-CONTAINING COMPOSITIONS AND METHODS OF USE THEREOF
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Provided herein are compositions and methods for preparing albumin-targeting moieties that feature a thioamide linkage. Methods to use the albumin targeting molecules to generate drugs with improved in vivo pharmacodynamics and biodistribution are described. Therapeutic compounds incorporating these thioamide linked albumin-targeting moieties are disclosed.
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Page/Page column 18-19
(2020/06/05)
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- FUNCTIONALLY MODIFIED POLYPEPTIDES AND RADIOBIOSYNTHESIS
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Provided herein are compositions and methods for generating polypeptides using non-natural amino acids (nnAAs) and genetic machinery, wherein the modified polypeptides, such as therapeutic polypeptides, bind to albumin, such as serum albumin. Methods of substituting a non-natural amino acid in a first polypeptide to obtain a modified polypeptide, the nnAA in some instances comprising an albumin targeting group, are disclosed, as are methods for making populations of such modified polypeptides. A therapeutic polypeptide, interleukin-1 receptor antagonist (IL-1RA) is exemplified using the disclosed methods.
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Paragraph 0172; 0173; 0174
(2018/03/25)
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- Synthesis of new ferrocene derivatives with rod-like structure
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The Suzuki-Miyaura cross-coupling of tris(4-ferrocenylphenyl)- and tris[4-(2-ferrocenylethynyl)phenyl]boroxines with functionalized iodoarenes gives new ferrocene derivatives of rod-like structure.
- Okulov, Vladimir N.,Popov, Damir A.,Panfilova, Anastasia V.,Dyadchenko, Marina A.,Lemenovskii, Dmitrii A.,Dyadchenko, Victor P.
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p. 111 - 113
(2015/04/14)
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- A Mild and General One-Pot Synthesis of Densely Functionalized Diaryliodonium Salts
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Diaryliodonium salts are powerful and widely used arylating agents in organic chemistry. Here we report a scalable synthesis of densely functionalized diaryliodonium salts from aryl iodides under mild conditions. This two-step, one-pot process has remarkable functional group tolerance, is compatible with commonly employed acid-labile protective group strategies, avoids heavy metal and transition metal reagents, and provides a direct route to stable precursors to PET imaging agents.
- Qin, Linlin,Hu, Bao,Neumann, Kiel D.,Linstad, Ethan J.,McCauley, Katelyenn,Veness, Jordan,Kempinger, Jayson J.,DiMagno, Stephen G.
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supporting information
p. 5919 - 5924
(2015/09/22)
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- Design and synthesis of conformationally constrained analogues of cis-cinnamic acid and evaluation of their plant growth inhibitory activity
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1-O-cis-Cinnamoyl-β-d-glucopyranose is known to be one of the most potent allelochemical candidates and was isolated from Spiraea thunbergii Sieb by Hiradate et al. (2004), who suggested that it derived its strong inhibitory activity from cis-cinnamic acid, which is crucial for phytotoxicity. In this study, key structural features and substituent effects of cis-cinnamic acid (cis-CA) on lettuce root growth inhibition was investigated. These structure-activity relationship studies indicated the importance of the spatial relationship of the aromatic ring and carboxylic acid moieties. In this context, conformationally constrained cis-CA analogues, in which the aromatic ring and cis-olefin were connected by a carbon bridge, were designed, synthesized, and evaluated as plant growth inhibitors. The results of the present study demonstrated that the inhibitory activities of the five-membered and six-membered bridged compounds were enhanced, up to 0.27 μM, and were ten times higher than cis-CA, while the potency of the other compounds was reduced.
- Nishikawa, Keisuke,Fukuda, Hiroshi,Abe, Masato,Nakanishi, Kazunari,Tazawa, Yuta,Yamaguchi, Chihiro,Hiradate, Syuntaro,Fujii, Yoshiharu,Okuda, Katsuhiro,Shindo, Mitsuru
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p. 223 - 234
(2014/01/06)
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- Carboxylation of alkylboranes by N-heterocyclic carbene copper catalysts: Synthesis of carboxylic acids from terminal alkenes and carbon dioxide
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Caught in the act: N-Heterocyclic carbene copper(I) complexes (1; IPr=1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene) serve as an excellent catalyst for the carboxylation of alkylboranes (2; R=alkyl) with CO2 to afford a variety of functionalized carboxylic acids (3) in high yields. A novel copper methoxide/alkylborane adduct (A) and its subsequent CO2 insertion product (B) have been isolated and shown to be true active catalyst species.
- Ohishi, Takeshi,Zhang, Liang,Nishiura, Masayoshi,Hou, Zhaomin
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p. 8114 - 8117
(2011/10/18)
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- 4-aryl piperidines
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This invention is directed to 4-aryl piperidines and related heterocyclic compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.
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Page/Page column 14
(2010/02/12)
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- Synthesis of meta- and paracyclophanes containing unsaturated amino acid residues
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[7.7], [8.8], [9.9] and [13.13] Paracyclophanes and [9.9] and [13.13] metacyclophanes containing two unsaturated amino acid residues have been synthesised. An X-ray crystallographic study of three of the paracyclophanes and molecular modelling of two para
- Gibson, Susan E.,Jones, Jerome O.,Kalindjian, S. Barret,Knight, Jamie D.,Mainolfi, Nello,Rudd, Matthew,Steed, Jonathan W.,Tozer, Matthew J.,Wright, Paul T.
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p. 6945 - 6958
(2007/10/03)
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