📜(2R,Rs)-2-(Tert-Butylsulfinamido)Pent-4-Enoic Acid置于盐酸体系中,用 水 作为反应溶剂,化学反应 4.0H,以69%的收率获得产物d-烯丙基甘氨酸 参考文献:Diastereoselective Amidoallylation Of Glyoxylic Acid With Chiral Tert-Butanesulfinamide And Allylboronic Acid Pinacol Esters: Efficient Synthesis Of Optically Active γ,δ-Unsaturated α-Amino Acids 标题:Diastereoselective Amidoallylation Of Glyoxylic Acid With Chiral Tert-Butanesulfinamide And Allylboronic Acid Pinacol Esters: Efficient Synthesis Of Optically Active γ,δ-Unsaturated α-Amino Acids 摘要:A Convenient Synthesis Of Delta,Gamma-Unsaturated Amino Acids Has Been Developed. After A Mixture Of (R)-Tert-Butanesulfinamide And Glyoxylic Acid With Molecular Sieves In Ch2Cl2 Was Stirred For 42 H At Room Temperature,Allylboronic Acid Pinacol Ester Was Added To The Mixture To Give (R)-2-((R)-Tert-Butanesulfinamido)Pent-4-Enoic Acid With High Diastereoselectivity. The Corresponding Reaction Of (Z)-Crotylboronic Acid Pinacol Ester Produced No Product; However,That Of (E)-Crotylboronic Acid Pinacol Ester Produced (2R,3S)-2-((R)-Tert-Butylsulfinamido)-3-Methylpent-4-Enoic Acid With Excellent Diastereoselectivity. (C) 2013 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Tetasy.2013.07.026
专利号:US-2012282180-A1 优先权日:2011-05-06 标题 :Compounds with Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof 发明人:KOLB HARTMUTH C; HAUFE GUENTER; BEHRENDS MALTE; KOPKA KLAUS; WAGNER STEFAN; HUGENBERG VERENA; BREYHOLZ HANS-JOERG; HERMANN SVEN; SCHAEFERS MICHAEL 权利人:KOLB HARTMUTH C; HAUFE GUENTER; BEHRENDS MALTE; KOPKA KLAUS; WAGNER STEFAN; HUGENBERG VERENA; BREYHOLZ HANS-JOERG; HERMANN SVEN; SCHAEFERS MICHAEL 摘要:The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.
专利号:US-12234299-B2 优先权日:2018-11-22 标 题 :Peptides for inducing bacteriocin synthesis and methods to identify and/or select and/or optimize the same 发明人:MIGNOLET JOHANN; HOLS PASCAL; LEDESMA GARCÃ?A LAURA 权利人:SYNGULON S A; UNIV CATHOLIQUE LOUVAIN 摘要:Described herein is a peptide or peptidomimetic with a length of at least 6 residues comprising, consisting essentially of, or consisting of the sequence motif Xaa1-Trp-Xaa2-Xaa3-Xaa4-Xaa5 (SEQ ID NO:1), wherein: Xaa1 represents an aromatic residue (Phe, Tyr, Trp, His), Cys or Ser; Xaa2, Xaa3 and Xaa4 represent any residue; and Xaa5 represents Gly, lie or Val.
专利号:EP-3070087-B1 优先权日:2011-08-05 标题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors
专利号:EP-3070087-A1 优先权日:2011-08-05 标 题 :Intermediates for the synthesis of cyclic p1 linkers as factor xia inhibitors
专利号:EP-2520573-A1 优先权日:2011-05-06 标 题:Compounds with matrix-metalloproteinase inhibitory activity 发明人:HAUFE GUENTER; BEHRENDS MALTE; KOPKA KLAUS; WAGNER STEFAN; HUGENBERG VERENA; BREYHOLZ HANS-JOERG; HERMANN SVEN; SCHAEFERS MICHAEL; KOLB HARTMUTH 权利人:UNIV MUENSTER WILHELMS; SIEMENS MEDICAL SOLUTIONS 摘要:The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.
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合成参考文献
摘要:Hall, M.; Faber, K.; Tasnádi, G., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 310. 摘要:Hall, M.; Faber, K.; Tasnádi, G., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 305. 参考文献:10.1007/bf01388171 摘要:Meffre P. Syntheses of optically active 2-amino-4-oxobutyric acid and N,O-protected derivatives. Amino Acids. 1999;16(3-4):251–72. doi: 10.1007/bf01388171.