专利号:US-8933227-B2 优先权日:2009-08-14 标题 :Selective synthesis of functionalized pyrimidines 发明人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN 权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.
专利号:US-2023295613-A1 优先权日:2020-02-14 标 题:Long chain carbon and cyclic amino acids substrates for genetic code reprogramming 发明人:JEWETT MICHAEL C; LEE JOONGOO; MOORE JEFFREY S; SCHWARZ KEVIN J 权利人:UNIV NORTHWESTERN; UNIV ILLINOIS 摘要:Abstract: Disclosed are methods, systems, components, and compositions for synthesis of sequence defined polymers. The methods, systems, components, and compositions may be utilized for incorporating novel substrates that include non-standard amino acid monomers and non-amino acid monomers into sequence defined polymers. As disclosed herein, the novel substrates may be utilized for acylation of tRNA via flexizyme catalyzed reactions. The tRNAs thus acylated with the novel substrates may be utilized in synthesis platforms for incorporating the novel substrates into a sequence defined polymer.
专利号:WO-2007091110-A1 优先权日:2006-02-09 标 题 :Enzymatic resolution process for the preparation of cycli-c beta-amino acid and ester enatiomers 发明人:FORRO ENIKO; FUELOEP FERENC 权利人:UNIV SZEGEDI; FORRO ENIKO; FUELOEP FERENC 摘要:The invention relates to a process for the preparation of cyclic β-amino acid and ester enantiomers of general formula (I) wherein R is hydrogen or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl and heteroaryl, wherein each ring may optionally be condensed; A is alkylene or alkenylene, and one or more carbon atoms of each groups may optionally be replaced with one or more heteroatoms; Rl and R2 are hydrogen or halogen, =(O)n, optionally halogenated alkyl, alkylidene, alkoxy, optionally protected hydroxy, optionally protected amino, mono- or dialkylamino and optionally substituted phenyl, or Rl and R2 taken together with one or any two atoms of the ring to which they are attached, form a saturated, unsaturated or aromatic fused homo- or heterocyclic ring; n is 0, 1 or 2; * denotes a chiral carbon atom; and the salts thereof, comprising the steps of hydrolysing a mixture of cyclic β-amino ester enantiomers with a stereoselective hydrolytic enzyme, and separating the obtained acid enantiomer and the unreacted ester enantiomer. The invention provides an enzymatic resolution procedure for the preparation of enantiomers of both the cis- and trans-cyclic β-amino acids and esters useful for the synthesis ' of biologically active agents.
专利号:US-2011190499-A1 优先权日:2009-08-14 标题 :Selective synthesis of functionalized pyrimidines
专利号:US-2024207458-A1 优先权日:2021-04-26 标 题:Targeted alpha particle therapy for somatostatin receptor 2 positive neuroendocrine tumors and metastases 发明人:MORSE DAVID; JI HAITAO; WADAS THADDEUS; PANDYA DARPAN 权利人:H LEE MOFFITT CANCER CT & RES 摘要:Disclosed are TATE derivatives having a linker between the TATE moiety and a macrocyclic radionuclide chelating moiety. Methods of synthesis and use are also disclosed. The compounds preferably exhibit a ratio of kidney: liver uptake by a subject within 24 hours of 5 or less, 3 or less, 1 or less, 0.5 or less, preferably from 2:1 to 1:2.
专利号:EP-2305808-B1 优先权日:2001-06-20 标 题:Templated molecules and methods for using such molecules 发明人:PEDERSEN HENRIK; GOULIAEV ALEX HAAHR; SAMS CHRISTIAN KLARNER; SLØK FRANK ABILGAARD; FRESKGÃ…RD PER-OLA; HOLTMANN ANETTE; OLSEN EVA KAMPMANN; HUSEMOEN GITTE NYSTRUP; FELDING JAKOB; FRANCH THOMAS; THISTED THOMAS; HYLDTOFT LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER 权利人:NUEVOLUTION AS 摘要:The present invention relates to a method for synthesising templated molecules. In one aspect of the invention, the templated molecules are linked to the template which templated the synthesis thereof. The intion allows the generation of libraries which can be screened for e.g . therapeutic activity.
参考文献:10.1038/s41557-023-01226-w 摘要:Watson ZL, Knudson IJ, Ward FR, Miller SJ, Cate JHD, Schepartz A, Abramyan AM. Atomistic simulations of the Escherichia coli ribosome provide selection criteria for translationally active substrates. Nat. Chem. 2023 Jun 12;15(7):913–21. doi: 10.1038/s41557-023-01226-w.