专利号:US-4101721-A 优先权日:1976-12-09 标题 :Solid phase synthesis of protected peptides 发明人:RICH DANIEL H; GURWARA SWEET K 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The invention is addressed to the preparation of 3-nitro-4-bromomethyl benzoic acid, as a new compound from which 3-nitro-4-bromomethyl benzoyl amide polystyrene resin can be prepared for solid synthesis of protected peptide acids and amides and separation thereof without cleavage of acid labile protecting groups or decomposition of aromatic acid groups and from which purified polypeptides can be formed.
专利号:US-4062746-A 优先权日:1975-05-07 标 题 :Solid phase synthesis of protected peptides 发明人:RICH DANIEL H; GURWARA SWEET K 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The invention is addressed to the preparation of 3-nitro-4-bromomethyl benzoic acid, as a new compound from which 3-nitro-4-bromomethyl benzoyl amide polystyrene resin can be prepared for solid synthesis of protected peptide acids and amides and separation thereof without cleavage of acid labile protecting groups or decomposition of aromatic acid groups and from which purified polypeptides can be formed.
专利号:US-5886104-A 优先权日:1993-06-18 标题 :Grafted cross-linked polyolefin substrates for peptide synthesis and assays 发明人:PEDERSEN WALTHER BATSBERG; ALMDAL KRISTOFFER; WINTHER LARS; BERG ROLF HENRIK 权利人:FORSKNIINGSCENTER RISO 摘要:A solid support for the solid-phase synthesis of peptides or proteins in high yield and in high purity, suited both to the synthesis of a single peptide or protein and to the parallel and substantially simultaneous synthesis of a plurality thereof, is based on a cross-linked polyolefin, especially polyethylene, substrate, the cross-linking having been obtained by irradiation with high energy electrons or γ radiation or treatment with organic peroxide such as benzoyl peroxide, to which substrate are grafted polymer chains such as polystyrene chains which are functionalized with a chemical functionality facilitating the formation of an anchoring linkage between the polymer moiety and another chemical species. The solid support is also suited for use in solid-phase biosystems, notably bioassays, such as immunoassays, DNA hybridization assays or PCR amplification. The grafted chains may bear substituents which are such that the polymer-grafted cross-linked polyolefin substrate is swellable by water or aqueous media, in other words, hydrophilic, which makes the solid support particularly well suited for assays of the ELISA type.
专利号:EP-0433345-B1 优先权日:1988-09-01 标题:Peptide synthesis method and solid support for use in the method 发明人:BERG ROLF H; ALMDAL KRISTOFFER; PEDERSEN WALTHER BATSBERG; HOLM ARNE; TAM JAMES P; MERRIFIELD ROBERT BRUCE 权利人:RISOE FORSKNINGSCENTER 摘要:A method for the solid-phase synthesis of peptides or proteins in high yield and high purity uses a solid support consisting of a functionalized polystyrene-grafted polymer substrate, the grafted polystyrene chains being substantially non-cross-linked and having a chain molecular weight, not including optional non-reactive substituents, of at least 200,000, preferably in the range of 600,000-1,200,000. Particularly suitable polymer substrates are substrates of a polyolefin such as polyethylene. The method is particularly well-suited to the compartmentalized synthesis of a multitude of peptides or proteins in a parallel and substantially simultaneous fashion. Preferred embodiments of a solid support for performing the synthesis are prepared from thin polyethylene sheet or film which has been grafted with polystyrene chains in a radical-initiated process in which the polyethylene sheet or film is immersed in a solution of optionally substituted styrene monomer in an alcohol such as methanol, the volume percentage of styrene in the solution preferably being about 30 % v/v, and subjected to gamma irradiation.
专利号:US-6867202-B1 优先权日:1997-06-25 标 题 :Treatment of insulin resistance 发明人:CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL 权利人:PFIZER 摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
参考标题:Design And Synthesis Of Novel Prodrugs Of 2′-Deoxy-2′-Methylidenecytidine Activated By Membrane Dipeptidase Overexpressed In Tumor Tissues 作者:Yasunori Kohchi,Kazuo Hattori,Nobuhiro Oikawa,Eisaku Mizuguchi,Yoshiaki Isshiki,Kohsuke Aso,Kiyoshi Yoshinari,Haruyoshi Shirai,Masanori Miwa,Yukiko Inagaki,Masako Ura,Kotaroh Ogawa,Hisafumi Okabe,Hideo Ishitsuka,Nobuo Shimma |发布日期:2007.4 摘要:Dna Microarray Analysis Comparing Human Tumor Tissues With Normal Tissues Including Hematopoietic Progenitor Cells Resulted In Identification Of Membrane Dipeptidase As A Prodrug Activation Enzyme. Novel Prodrugs Of 2'-Deoxy-2'-Methylidenecytidine (Dmdc) Including Compound 23 That Are Activated By Membrane Dipeptidase (Mdp) Preferentially In Tumor Tissue Were Designed And Synthesized To Generate The
合成参考文献
参考文献:10.1055/s-2008-1078209 摘要:Neuville L, Zhu J, Dufour J. Total Synthesis of Arylomycin A2, a Signal Peptidase I (SPase I) Inhibitor. Synlett. 2008 Aug 22;2008(15):2355–9. doi: 10.1055/s-2008-1078209.