专利号:US-2023183177-A1 优先权日:2020-04-24 标题:Enantioselective chemo-enzymatic synthesis of optically active amino amide compounds 发明人:GRILL BIRGIT; WINKLER MARGIT; SCHWAB HELMUT; STROHMEIER GERNOT; DONSBACH KAI; WALDVOGEL SIEGFRIED R; ARNDT SEBASTIAN; WEIS DOMINIK 权利人:PHARMAZELL GMBH 摘要:The present invention relates to a novel biocatalytic process for the stereoselective preparation of alpha amino amide compounds catalyzed by NHase enzymes. A further aspect of the invention relates to novel NHase enzymes as well as further improved NHase enzyme mutants, nucleic acid molecules encoding these enzymes, recombinant microorganisms suitable for preparing such enzymes and mutants. Another aspect of the invention relates to a chemo-biocatalytic process for the preparation of lactam compounds comprising the new catalytic process for the preparation of alpha amino amide compounds catalyzed by NHase enzymes, as well as the chemical oxidation of the alpha amino amide by applying certain chemical oxidation catalysts suitable for converting the alpha amino amide under retention of its stereochemical configuration to the respective lactam. The novel chemo-biocatalytic process is particularly suited for the synthesis of valuable pharmaceutical compounds, like in particular (S)-Levetiracetam.
专利号:US-4873342-A 优先权日:1985-04-16 标题:Dipeptide derivative and synthesis and use thereof 发明人:TANAKA TAKAHARU; SAITOH MASAYUKI; HIGUCHI NAOKI; HASHIMOTO MASAKI 权利人:SUNTORY LTD 摘要:A novel depeptide derivative which exhibits inhibitory activity against prolyl endopeptidase and is effective for preventing and curing amnesia is disclosed. A process for chemical synthesis of such a derivative, as well as its use, is also disclosed.
专利号:US-4772587-A 优先权日:1985-04-16 标题:Dipeptide derivative of fatty acid 发明人:TANAKA TAKAHARU; HIGUCHI NAOKI; SAITOH MASAYUKI; HASHIMOTO MASAKI 权利人:SUNTORY LTD 摘要:A novel compound that exhibits inhibitory activity against prolyl endopeptidase and a method for chemical synthesis of said compound, as well as its use as a prolyl endopeptidase inhibitor and an anti-amnesic agent that contains said compound as the active ingredient are provided.
专利号:US-12383520-B2 优先权日:2019-05-16 标 题 :Compound and composition for use in the treatment of premenstrual syndrome and/or premenstrual dysphoric disorder 发明人:DANHIER PHILIPPE; AZZAM PASCALE 权利人:SYNAPHARM IND SYNTHESIS 摘要:This invention pertains to a compound and a composition for use in the treatment of premenstrual syndrome and/or premenstrual dysphoric disorder.
专利号:US-10793521-B2 优先权日:2016-10-24 标 题:Crystalline form II of dextral oxiracetam, preparation method therefor and use thereof 发明人:YE LEI 权利人:CHONGQING RUNZE PHARMACEUTICAL; CHONGQING RUZER PHARMACEUTICAL COMPANY LTD 摘要:The present invention provides a crystalline form of dextral oxiracetam. The crystalline form has a diffraction peak when a diffraction angle, 2θ, is 17.76±0.2°, 20.16±0.2°, 21.20±0.2°, 24.17±0.2°, or 25.88±0.2°. The crystalline form of dextral oxiracetam can promote synthesis of phosphorylcholine and phosphoethanolamine, boosts cerebral metabolism, has a stimulating function on a specific central nervous pathway through a blood-brain barrier, and has special biological activity in the field of sedation and the antiepileptic field. The crystalline form of dextral oxiracetam of the present invention is a water-containing crystalline form, contains 0.5 water molecules, loses crystallization water at 73.5±2° C., and is melted and decomposed at 138.0±2° C. The crystalline form of dextral oxiracetam of the present invention can stably exist at room temperature and relative humidity of 0-95%, does not transform, is used for storage and formulation processing, and has low requirements for processing or storage humidity.
专利号:EP-2524910-A1 优先权日:2011-05-17 标题 :Process for the resolution of aminobutyramide 发明人:BOESTEN WILHELMUS HUBERTUS JOSEPH; BOONEN JOZEF JOHANNES CATHERINA JACOBUS; WOESTENBORGHS PIERRE LOUIS 权利人:DSM IP ASSETS BV 摘要:The present invention relates to a process for the resolution of Schiff bases of racemic ( R,S )-2-aminobutyramide to give optically pure ( S )-2-aminobutyramide, an intermediate in the synthesis of levetiracetam.
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