195202-09-6Relevant articles and documents
PROTEIN-BINDING COMPOUNDS
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Paragraph 0521; 0543-0545, (2020/05/19)
The technology relates in part to compounds that bind to proteins. In certain examples, the compounds can bind to proteins that bind to rapamycin. In some examples, the compounds can bind to cellular proteins, and/or variant forms of cellular proteins, th
MULTIMERIC PIPERIDINE DERIVATIVES
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Page/Page column 137; 138, (2019/07/13)
The technology relates in part to compounds that bind to multimeric ligand binding regions, referred to herein as "multimeric compounds." In certain examples, the multimeric compounds provided herein bind to and multimerize polypeptides that bind to rimiducid, such as for example, chimeric polypeptides that comprise FKBP12 polypeptide variant regions. Multimeric compounds provided include those having a structure of Formula I. Where A, Z, Y, Z' and A' moieties are described herein.
Synthetic process of homodimer of FKBP ligand
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, (2019/05/28)
The invention discloses a synthesis process of homodimer of FKBP ligand and belongs to an improved synthesis process of AP1903, wherein the homodimer of FKBP ligand refers to AP1903. According to theoptimized route of the synthesis process chooses, (S)-piperidine-2-methyl formate is connected to the compound Cpd9' as selected, an acid Cpd6' obtained after ester hydrolysis is easier to be purified by post-treatment purification, and precipitation or extraction treatment can be chosen by the post-treatment purification. Although the total reaction steps of the synthetic route in the prior literature are the same as the optimized route of the invention, the synthetic route in the prior literature belongs to the vertical route, and the post-treatment of the fifth, sixth and eighth steps requires column chromatography, thereby leading to a higher research and development cost. The optimized AP1903 synthetic route belongs to the parallel route, and the post-treatment is simpler and more advantageous for separation and purification, so that the cost of research and development is relatively low and the economic benefit is obviously superior to that of the synthetic route in the prior art.
An Inexpensive and Scalable Synthesis of Shld
J?rgensen, Frederik Pr?stholm,Bols, Mikael
, p. 6050 - 6055 (2018/05/24)
A synthesis of the important FKBP ligand Shld is reported. The synthesis avoids stoichiometric use of expensive and chiral reagents, maintains enantioselectivity and provides a high overall yield (39%). The main features in the method are enantioselective alkylation for preparation of the phenyl acetic acid moiety (building block A), catalytic enantioselective reduction for obtaining the chiral diaryl-1-propanol (building block C), and direct acylation of S-pipecolic tartrate rather than use of expensive Fmoc-pipecolic acid. The assembly of the building blocks A-C is reversed in comparison to previous synthesis, which also eliminates the need for protective groups.
METHODS AND COMPOSITIONS FOR THE SYNTHESIS OF MULTIMERIZING AGENTS
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, (2012/08/08)
The invention features methods and compositions for the synthesis of multimerizing agents.
