专利号:US-6815214-B2 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines 发明人:BOYCE JIM P; HOWBERT J JEFFRY; TABONE JOHN C 权利人:CELLTECH R & D INC 摘要:The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-α, TNF-β and also apoptosis.
专利号:US-9630923-B2 优先权日:2013-07-09 标题:Biocatalyzed synthesis of the optically pure (R) and (S) 3-methyl-1,2,3,4-tetrahydroquinoline and their use as chiral synthons for the preparation of the antithrombic (21R)- and (21S)-argatroban 发明人:GRISENTI PARIDE 权利人:EUTICALS SPA; EUTICALS SPA 摘要:The present invention relates to the biocatalyzed synthesis of enantiomerically pure (3R) and (3S)-methyl-1,2,3,4-tetrahydroquinoline. Said enantiomerically pure compounds are useful as chiral synthons in organic synthesis and, in particular, for the preparation of diastereomerically pure (21R) and (21S)-agratroban and its analogs. New compounds used as intermediates in the process of the invention are also disclosed.
专利号:WO-9611194-A1 优先权日:1994-10-06 标题:Pyridonecarboxylic acid derivative and intermediate for the synthesis of the same 发明人:OKADA HIDETSUGU; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 权利人:DAINIPPON PHARMACEUTICAL CO; OKADA HIDETSUGU; CHIBA KATSUMI; TOMINAGA YUKIO; MINAMI AKIRA 摘要:A pyridonecarboxylic acid derivative represented by general formula (I), an ester and a salt thereof, an antibacterial agent containing the same, and a bicyclic amine compound serving as a direct intermediate for the synthesis of the pyridonecarboxylic acid derivative, wherein R represents cycloalkyl, optionally substituted phenyl, etc.; G represents carbon, etc.; A represents C-Z (Z being hydrogen, halogeno, lower alkoxy, etc.) or nitrogen; X represents hydrogen, amino, etc.; Y represents hydrogen or halogeno; m is an integer of 1 to 3; and W represents -(CH2)nN(R1)R2 (R1 and R2 being the same or different and each representing hydrogen, lower alkyl, etc., and n being an integer of 0 or 1).
专利号:US-2013261317-A1 优先权日:2010-09-27 标题 :Methods for preparing synthetic bile acids and compositions comprising the same 发明人:MORIARTY ROBERT M; RAO PHOTON 权利人:MORIARTY ROBERT M; RAO PHOTON; KYTHERA BIOPHARMACEUTICALS INC 摘要:This invention relates generally to methods for preparing certain bile acids from non-mammalian sourced starting materials as well as to synthetic bile acids and compositions comprising such acids wherein the acids are characterized by a different C 14 population than naturally occurring bile acids as well as being free from any mammalian pathogens. This invention is also directed to the synthesis of intermediates useful in the synthesis of such bile acids. Accordingly, the C ring of the steroidal scaffold is oxidized to provide a synthetic route and intermediates to DCA. This invention also provides synthetic methods for preparing deoxycholic acid or a salt thereof starting from aromatic steroids such as estrogen, equilenin, and derivatives thereof. This invention is also directed to intermediates such as 12-oxo or delta-9,11-ene steroids as well as novel processes for their preparation. In preferred embodiments, bile acids are provided herein which have substituents on the B-ring and/or D-ring side chain and optionally on the hydroxy group of the A-ring.
专利号:US-2009215080-A1 优先权日:2005-10-13 标题:Methods for identification of inhibitors of enzyme activity 发明人:SINHA SUKANTO; CHILCOTE TAMIE JO 权利人:ACTIVESITE PHARMACEUTICALS 摘要:The invention discloses compositions and methods of synthesis to create novel ligands and drugs and identifying such compounds as inhibitors of enzyme targets for use in the treatment of clinical disorders, including cancer, infectious diseases, parasitic infestations, neurological disorders, reproductive disorders, inflammatory disorders, circulatory disorders, and metabolic disorders.
专利号:US-2005080086-A1 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines
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合成参考文献
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