专利号:US-9453044-B2 优先权日:2012-02-07 标题 :Method of synthesizing peptides, proteins and bioconjugates 发明人:LIU CHUAN FA; ZHAO JUNFENG 权利人:UNIV NANYANG TECH 摘要:The invention relates to the synthesis of peptides, proteins and related bioconjugates, and in particular, to such synthesis using a peptide ligation method whereby a C-terminal salicylaldehyde ester peptide is reacted with an aminoacyl-N-hydroxl peptide. The invention also relates to the synthesis of cyclic peptides, including serinyl- or threonyl-containing cyclic peptides. The invention further relates to a solid phase synthesis of C-terminal salicylaldehyde ester peptides.
专利号:US-5510528-A 优先权日:1993-04-08 标题:Preparation of halomethylbenzoly cyanides and novel halomethylbenzoyl cyanides 发明人:ISAK HEINZ; WETTLING THOMAS; KEIL MICHAEL; WOLF BERND; DOETZER REINHARD 权利人:BASF AG 摘要:A process for preparing halomethylbenzoyl cyanides I n n Ph-CO-CN I n n (Ph=phenyl radical substituted by chloromethyl or bromomethyl which, if desired, can additionally carry 1-4 further radicals) by reacting halomethylbenzoyl chlorides II n n Ph-CO-Cl II n n with an alkali metal cyanide or transition metal cyanide, if appropriate in an organic diluent, and novel halomethylbenzoyl cyanides I' ##STR1## (X=halogen, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, CF 3 , C 1 -C 5 -alkyl-(C 1 -C 5 -alkyl)hydroxyimino or C 1 -C 5 -alkyl-(C 2 -C 5 -alkenyl)hydroxyimino; m=0 to 4 and Y=chloromethyl or bromomethyl) are described. n The halomethylbenzoyl cyanides I are important intermediates for the synthesis of plant protection agents.
专利号:US-7732605-B2 优先权日:2005-03-29 标题 :Synthesis of diketopiperazines 发明人:HAYASHI YOSHIO 权利人:NEREUS PHARMACEUTICALS INC 摘要:Disclosed herein are methods for synthesizing diketopiperazines with enantiomeric excess by inducing cyclization of an α-keto acid with an acid catalyst.
专利号:US-7320993-B1 优先权日:1997-12-17 标题 :Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents 发明人:BIEDERMANN ELFI; HASMANN MAX; LOESER ROLAND; RATTEL BENNO; REITER FRIEDEMANN; SCHEIN BARBARA; SEIBEL KLAUS; VOGT KLAUS; WOSIKOWSKI KATJA; SCHEMAINDA ISABEL 权利人:ASTELLAS DEUTSCHLAND GMBH 摘要:The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
专利号:WO-2006079916-A1 优先权日:2005-01-26 标 题 :Thieno [2,3-d] pyrimidine compounds as inhibitors of adp-mediated platelets aggregation 发明人:ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; RAHMAN HAYAT; SCHWEITZER BARBARA ANN; TENBRINK RUTH ELIZABETH 权利人:PHARMACIA & UPJOHN CO LLC; ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; RAHMAN HAYAT; SCHWEITZER BARBARA ANN; TENBRINK RUTH ELIZABETH 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I): wherein A1, A2, A3, A4, A5, A6, A7, A8, X4, X6, R2, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2006235226-A1 优先权日:2005-03-29 标 题:Synthesis of diketopiperazines
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 123. 摘要:Arndtsen, B. A.; Tjutrins, J., Science of Synthesis: Multicomponent Reactions, (2013) 2, 512.