公开(公告)号：EP1056770A1

公开(公告)日：2000-12-06

申请号：EP99909564.9

申请日：1999-02-24

申请人： Dovetail Technologies, Inc. ,  HAUSER CHEMICAL RESEARCH, INC.

发明人： TAUB, Floyd ,  MURRAY, Christopher, K. ,  DAUGHENBAUGH, Randall, J.

IPC分类号： C07K5/06 ,  C07K5/08

CPC分类号： C07K5/00 ,  A23L33/10 ,  A61K31/00 ,  A61K31/16 ,  A61K31/195 ,  A61K31/215 ,  A61K31/275 ,  A61K31/66 ,  A61K31/675 ,  A61K38/00 ,  A61K45/06 ,  C07C323/41 ,  Y02A50/411 ,  Y10S930/26 ,  A61K2300/00

摘要： The present invention is directed to novel disulfides and thiols that are of up to about eighteen amino acids. One example, is a compound of the formula (1): A-B-C-S-S-D-E-F, wherein: A and F are selected from the group consisting of hydrogen, an amino acid, a dipeptide, a tripeptide, a modified polypeptide up to three amino acids long, and a carbobenzoxy groups, B and E are selected from the group consisting of an amino acid, a dipeptide, a tripeptide, and a modified polypeptide comprising up to and including three amino acids, C and D are selected from the group consisting of a modified polypeptide and a polypeptide comprising up to and including three amino acids, and S is the sulfur atom in the modified polypeptide and the polypeptide in C and D.

公开(公告)号：EP1018877A1

公开(公告)日：2000-07-19

申请号：EP96936784.6

申请日：1996-10-17

申请人： Dovetail Technologies, Inc. ,  HAUSER CHEMICAL RESEARCH, INC.

发明人： TAUB, Floyd ,  PERUN, Thomas, J. ,  MURRAY, Christopher, K. ,  DAUGHENBAUGH, Randall, J. ,  LEDNICER, Daniel

IPC分类号： A01N37/34 ,  A61K45/00 ,  A61K45/05 ,  A61K47/00 ,  A61K39/00 ,  A61K39/38

CPC分类号： C07F9/091 ,  A61K39/39 ,  A61K2039/55511 ,  C07C309/15 ,  C07C323/41 ,  C07F9/3808 ,  Y02A50/407 ,  Y02A50/412 ,  Y10S514/885 ,  A61K2300/00 ,  A61K31/16

摘要： The present invention relates to peptide-like compounds, eg aminocarboxylic acid amide derivatives, and to methods of using same to stimulate cells of the immune system, bone marrow and other organs. The present compounds can be used to enhance vaccination, increase synthesis of and enhance function of blood cell components and enhance anti-neoplastic effects of various agents. The compounds of the invention can be used to produce a variety of further pharmacologic effects.

摘要翻译： 本发明涉及肽样化合物，例如， 氨基羧酸酰胺衍生物，以及使用它们刺激免疫系统，骨髓和其他器官的细胞的方法。 本发明化合物可用于增强疫苗接种，增加血细胞组分的合成和增强血细胞组分的功能并增强各种药剂的抗肿瘤作用。 本发明的化合物可用于产生多种其他药理学作用。

公开(公告)号：EP0815096A1

公开(公告)日：1998-01-07

申请号：EP96909628.0

申请日：1996-03-08

申请人： HAUSER CHEMICAL RESEARCH, INC.

发明人： ZHENG, Qun, Y. ,  MURRAY, Christopher, K. ,  DAUGHENBAUGH, Randall, J.

IPC分类号： A61K31 ,  A61P35 ,  C07D305 ,  C07D407

CPC分类号： C07D407/12 ,  C07D305/14

摘要： An antitumor compound of formula (5), in which R = Ac or H, and R1 = R2 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R3 = H; R1 = R2 = R3 = H; R1 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R2 = R3 = H; R1 = R3 = H, R2 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R1 = H, R2 = R3 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R1 = R2 = R3 = an alkyl group Me, Et, Pr, i-Pr, n-Bu or t-Bu. Me is an abbreviation for methyl, Et is ethyl, Pr is propyl, i-Pr is isopropyl, n-Bu is n-butyl, and t-Bu is tert-butyl. Also provided by the invention is a one-step method of preparing a compound of formula (5) whereby a taxane having a tiglate group attached to the side chain is contacted with an oxidizing reagent resulting in the formation of an epoxide having antitumor activity.