专利号:US-8158817-B2 优先权日:2003-12-24 标 题 :Synthesis of acylureas and composition comprising acylureas 发明人:BERNARD JEAN-MARIE; REVELANT DENIS; AMOUYAL CEDRIC 权利人:BERNARD JEAN-MARIE; REVELANT DENIS; AMOUYAL CEDRIC; PERSTORP FRANCE 摘要:The invention relates to a process for the synthesis of a polyisocyanate composition comprising acylureas. According to the invention, a starting composition comprising a compound having at least two isocyanate functional groups is subjected to a reaction with at least two acid functional groups, with at least one of the acid functional groups having a pKa value of less than or equal to 3, and at least one of the acid functional groups having a pKa value of more than 3 and less than or equal to 6, at a temperature at least equal to 50 ° C., wherein the acid functional group having a pKa value of less than or equal to 3 and the acid functional group having a pKa value of more than 3 and less than or equal to 6 are present on two different acids or on the same acid.
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-10407468-B2 优先权日:2016-03-23 标 题 :Methods for synthesizing α4β7 peptide antagonists 发明人:BHANDARI ASHOK; MANTHATI SURESH KUMAR; MEHROTRA MUKUND M; ANANDAN SAMPATH-KUMAR; PATEL DINESH V 权利人:PROTAGONIST THERAPEUTICS INC 摘要:The present invention provides methods of making α4β7 peptide monomer and dimer antagonists. Methods of the present invention include solid phase and solution phase methods, as well as synthesis via condensation of smaller peptide fragments. Methods of the present invention further include methods directed to the synthesis of peptides comprising one or more penicillamine residues.
专利号:WO-9729091-A1 优先权日:1996-02-09 标题:Balanol analogues 发明人:NIELSEN JOHN; LYNGSOE LARS OLE 权利人:AUDA PHARMACEUTICALS APS; NIELSEN JOHN; LYNGSOE LARS OLE 摘要:The present invention relates to a solid phase methodology for the preparation of a combinatorial library of structural analogues of the natural product balanol (ophiocordin, azepinostatin), which is a protein kinase C (PKC) and protein kinase A (PKA) inhibitor. The method comprises solid-phase synthesis of the analog variants of balanol whereby a high molecular diversity is introduced. The synthetic scheme is based on a retrosynthetic analysis of the native structure which revealed three main building blocks suitable as templates for modification. The dicarboxy-functional moiety can be immobilised to the polymer support either as the monoallyl ester or as the internal anhydride. The libraries produced by the method are especially suited for high throughput screening of potential drug candidates for the treatment of mammals, especially humans.
专利号:US-2007106048-A1 优先权日:2003-12-24 标题 :Synthesis of acylureas and composition comprising acylureas
专利号:US-2010216966-A1 优先权日:2003-12-24 标题 :Synthesis of acylureas and composition comprising acylureas
参考文献:10.1007/s002530100617 摘要:Gross RA, Kalra B, Kumar A. Polyester and polycarbonate synthesis by in vitro enzyme catalysis. Applied Microbiology and Biotechnology. 2001 Jun 01;55(6):655–60. doi: 10.1007/s002530100617. 参考文献:10.2116/analsci.22.715 摘要:Tamaya K, Moriguchi S, Naito K, Takei S. Interpretation of solute retention of some monovalent inorganic anions in anion-exchange chromatography using a dicarboxylic Acid as an eluent. Anal Sci. 2006 May;22(5):715–9. doi: 10.2116/analsci.22.715.