专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:WO-2009049476-A1 优先权日:2007-09-20 标题 :Process for the manufacture of (+)-biotin 发明人:CHEN FEN-ER; DAI HUI-FANG; HUANG JIAN; XIONG FEI; JING SHU-PING 权利人:DSM IP ASSETS BV; UNIV FUDAN; CHEN FEN-ER; DAI HUI-FANG; HUANG JIAN; XIONG FEI; JING SHU-PING 摘要:Disclosed are processes for preparing synthetic biotin intermediates and a process for preparing biotin using said intermediates. In particular, disclosed is a process for the stereoselective total synthesis of the natural product (+)-biotin 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.
专利号:US-2008051323-A1 优先权日:2004-08-21 标 题 :Chloroquine drug compositions and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-2007060499-A1 优先权日:2005-09-15 标 题 :Chloroquine combination drugs and methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
专利号:US-2007166281-A1 优先权日:2004-08-21 标题 :Chloroquine coupled antibodies and other proteins with methods for their synthesis 发明人:KOSAK KENNETH M 权利人:KOSAK KENNETH M 摘要:This invention discloses compositions of chloroquine-coupled active agents such as therapeutic antibodies or insulin, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the drug is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a drug directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing the drug for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and antibody or insulin to their site of action.