专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:US-2023212788-A1 优先权日:2020-03-26 标 题:New method for automated on-demand biomolecular array synthesis 发明人:ZHANG YIXIN; LIN WEILIN 权利人:UNIV DRESDEN TECH 摘要:The invention provides an amphiphilic coating for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, comprising a hydrophilic chemical structure and a lipophilic group, wherein said peptides and small molecular compounds differ from spot to spot from each other in the chemical structure, characterized in that said amphiphilic coating possesses low wettability to polar aprotic solvents used in the array synthesis; said amphiphilic coating possessing low wettability is designed that it can be converted to a coating possessing high wettability by hydrolysis of the lipophilic group; and said amphiphilic coating comprises an amino group for the reaction with an electrophilic reagent. The invention further provides a solid support comprising said amphiphilic coating and a method for method for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, wherein said planar surface of a solid support comprises said amphiphilic coating. Said method includes the enhancing of the wettability of a glass surface to organic solvents to realize automated on-demand biomolecular array synthesis comprising both, peptides and small molecular compounds. The amphiphilic surface can be switched to a hydrophilic surface, resulting in high density arrays suitable for protein- and cell-based screening.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
专利号:US-5093530-A 优先权日:1987-03-30 标 题:2,4-dimethoxy-4'-hydroxy-benzophenone 发明人:RINK HANS 权利人:CIBA GEIGY CORP 摘要:A synthetic resin based on a polystyrene that can be used as a support for solid phase peptide synthesis and that has been cross-linked with from 0 to 5 mol % of divinyl benzene, characterized in that it has been substituted at benzene rings of its skeletal structure by groups of the formula ##STR1## in which X represents --O-- or --NH-- and R represents C 1 -C 4 -alkyl, as a support renders possible the solid phase synthesis of peptides and peptide amides that are, if desired, protected at the N-terminal and/or at other functional groups. The resin is manufactured by reaction of a customary chloromethylated polystyrene resin with an alkali metal salt of the corresponding 4-hydroxybenzophenone and subsequent reduction of the carbonyl group and, optionally, amination.
专利号:US-2024279231-A1 优先权日:2021-05-20 标题:Map4k4 inhibitors and methods of synthesis and use thereof 发明人:AWASTHI VIBHUDUTTA; EEDA VENKATESWARARAO 权利人:UNIV OKLAHOMA 摘要:The compound DMX-5804, IUPAC name 5-(4-(2-methoxyethoxy)phenyl)-7-phenyl-3,4a,7,7a-tetrahydro-4H-pyrrolo[2,3-d]pyrimidin-4-one, is a potent and selective inhibitor of mitogen-activated protein kinase kinase kinase kinase-4 (MAP4K4). The present disclosure describes a scalable and practical synthesis process for making DMX-5804. The process (1) doesn't rely on transition metals, (2) has reduced duration of reactions, (3) is streamlined with significantly improved yields using low cost raw materials, (4) includes no microwave-assisted reactions, (5) does not require column purification, and (6) generally results in crystalized products having over a 95% purity in each step. The present disclosure also describes DMX-5804 analogs and derivatives for use in inhibiting MAP4K4, and scalable and practical processes for making such DMX-5804 analogs.
专利号:US-6204361-B1 优先权日:1996-01-18 标 题 :Method of peptide synthesis 发明人:CARPINO LOUIS A; IONESCU DUMITRU 权利人:RES CORP TECHNOLOGIES INC 摘要:The present invention relates to a process for forming an N-α-amino protected amino acid fluoride in situ by reacting an N-α-amino protected amino acid with an ionic fluoride salt in the presence of a peptide coupling agent. It is also directed to the use of the amino acid fluoride thus formed in peptide synthesis.
参考标题:Mitsunobu Approach To The Synthesis Of Optically Active α,α-Disubstituted Amino Acids 作者:Jonathan E. Green,David M. Bender,Stona Jackson,Martin J. O'Donnell,James R. Mccarthy |发布日期:2009.2.19 摘要:α-Azido Esters By Mitsunobu Reaction With Hn3. Optimization Of This Reaction Was Shown To Proceed At Room Temperature With High Chemical Yield Using 1,1-(Azodicarbonyl)Dipiperidine (Addp) And Trimethylphosphine (Pme3). Complete Inversion Of Configuration Was Observed At The α-Carbon. Several α,α-Disubstituted Amino Acids Were Synthesized In High Overall Chemical Yield And Optical Purity.
合成参考文献
参考文献:10.1002/chir.10116 摘要:Vandenabeele‐Trambouze O, Geffard M, Bodet D, Despois M, Dobrijevic M, Loustalot MG, Commeyras A. Antibodies directed against L and D isovaline using a chemical derivatizing reagent for the measurement of their enantiomeric ratio in extraterrestrial samples: First step–production and characterization of antibodies. Chirality. 2002 Jan;14(6):519–26. doi: 10.1002/chir.10116. 参考文献:10.1007/s10858-006-9045-6 摘要:Raap J, Hollander J, Ovchinnikova TV, Swischeva NV, Skladnev D, Kiihne S. Trans and surface membrane bound zervamicin IIB: 13C-MAOSS-NMR at high spinning speed. Journal of Biomolecular NMR. 2006 Aug 09;35(4):285–93. doi: 10.1007/s10858-006-9045-6.