专利号:US-12251674-B2 优先权日:2012-11-14 标 题:Substrates, systems, and methods for array synthesis and biomolecular analysis 发明人:RAJASEKARAN JOHN J; JAYARAMAN VASANTH; WANG TIANHAO; BEI KANG; KRISHNAMURTHY HARI KRISHNAN; VEDANTHAM PUNITHA 权利人:VIBRANT HOLDINGS LLC 摘要:Disclosed herein are formulations, substrates, and arrays. In certain embodiments, substrates and arrays comprise a porous layer for synthesis and attachment of polymers or biomolecules. Also disclosed herein are methods for manufacturing and using the formulations, substrates, and arrays, including porous arrays. Also disclosed herein are formulations and methods for one-step coupling, e.g., for synthesis of peptides in an N→C orientation. In some embodiments, disclosed herein are formulations and methods for high efficiency coupling of biomolecules to a substrate.
专利号:US-2004054161-A1 优先权日:2002-09-13 标题 :Stepwise solid-phase synthesis of peptide-oligonucleotide conjugates and supports therefor 发明人:ANTOPOLSKII MAXIM; AZHAYEVA ELENA; AZHAYEV ALEX 权利人:GLEN RES CORP 摘要:A support for peptide-oligonucleotide conjugate synthesis includes an article of manufacture according to the formula: n n n wherein: (a) substitutent A includes a polymeric base material and/or a silica base material; (b) one of substituents B and C includes an NHFmoc-containing group and/or a peptide-containing group; (c) one of substituents B and C includes an NHBoc-containing group, an O-DMTr-containing group, and/or an oligonucleotide-containing group; and (d) each X independently represents â•?O, S, and/or NH. Suitable supports include those according to the formula: n n n wherein substituents A, B, and C have the meanings described above. When used to synthesize a peptide-oligonucleotide conjugate, the resulting conjugate may have the formula: n n n wherein substituent B includes a peptide and substituent C includes an oligonucleotide.
专利号:US-6534627-B1 优先权日:1989-10-23 标题:Synthesis and use of amino acid fluorides as peptide coupling reagents 发明人:CARPINO LOUIS A; EL-FAHAM AYMAN AHMED 权利人:RES CORP TECHNOLOGIES INC 摘要:The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: n or the acid fluoride salts thereof wherein n BLK is an N-amino protecting group; n AA is an amino acid residue; and n X is absent or a protecting group. n The amino acid fluoride is useful as a coupling agent in peptide synthesis.
专利号:US-5985844-A 优先权日:1992-03-26 标题:Homoerythromycin A derivatives modified at the 4'-and 8A-positions 发明人:HECK JAMES V; LEANZA WILLIAM J; RATCLIFFE RONALD W; SALZMANN THOMAS N; SHANKARAN KOTHANDARAMAN; SZYMONIFKA MICHAEL J; WILKENING ROBERT R 权利人:MERCK & CO INC 摘要:Compounds of the formula: where R is hydrogen, hydroxyl, alkyl or acyl, R' and R'' together are oxo, hydroxyimino or alkoxyimino, and R' and R'' independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.
专利号:EP-0508699-B1 优先权日:1991-04-04 标 题 :9-Deoxo-8a-aza-8a-homoerythromycin a derivatives modified at the 4'- and 8a-positions 发明人:HECK JAMES V; LEANZA WILLIAM J; RATCLIFFE RONALD W; SALZMANN THOMAS N; WILKENING ROBERT R; SZYMONIFKA MICHAEL J; SHANKARAN KOTHANDARAMAN 权利人:MERCK & CO INC 摘要:Compounds of the formula: where R is hydrogen, hydroxyl, alkyl or acyl, R min and R sec together are oxo, hydroxyimino or alkoxyimino, and R min and R sec independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.
专利号:US-5717083-A 优先权日:1994-02-23 标题 :Phosphoramidate and phosphorothiomidate oligomeric compounds 发明人:COOK PHILLIP DAN; ACEVEDO OSCAR; HEBERT NORMAND 权利人:ISIS PHARMACEUTICALS INC 摘要:PCT No. PCT/US95/02267 Sec. 371 Date Aug. 19, 1996 Sec. 102(e) Date Aug. 19, 1996 PCT Filed Feb. 23, 1995 PCT Pub. No. WO95/23160 PCT Pub. Date Aug. 31, 1995Compounds are provided having structure (I), wherein the L groups are backbone segments, the Y and T groups are functional groups for interacting with target molecules of interest, the X groups are oxygen or sulfur and the E groups are H, conjugate groups or intermediate groups used during the synthesis of the compounds and wherein the compounds are prepared using H phosphonate type chemistry wherein the functional groups are added during an oxidation step or during a coupling step. (I)
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1007/s10989-010-9214-z 摘要:Narendra N, Vishwanatha TM, Sureshbabu VV. Peptidomimetics Through Click Chemistry: Synthesis of Novel β-Keto Triazole Acids from N-Protected Amino Acids. International Journal of Peptide Research and Therapeutics. 2010 May 16;16(4):283–90. doi: 10.1007/s10989-010-9214-z.