专利号:US-2014371316-A1 优先权日:2011-11-23 标 题:Derivatives of phenoxyisobutyric acid 发明人:LALEZARI IRAJ; FABRICANT JILL S 权利人:FABRICANT JILL S; LALEZARI IRAJ 摘要:The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
专利号:WO-0144184-A1 优先权日:1999-12-16 标题:Synthesis of indole-containing spla2 inhibitors 发明人:MARTINELLI MICHAEL JOHN; SAWYER JASON SCOTT 权利人:LILLY CO ELI; MARTINELLI MICHAEL JOHN; SAWYER JASON SCOTT 摘要:A method of making a compound include reacting a compound represented by formula (I), with a base, to form the compound of formula (II); and where R1 is H, R10 or -C(O)R10; R2 is R20 -OR20, -SR20, -NR20R20' or -C(O)R20;R3, R4, R5, R6 and R7 are each individually H, halogen, R, -OR, -SR, -NRR', -C(O)R, -C(O)OR, -S(O)R or -S(O)2R; provided that at least one of R4 and R5 is not H; each R, R10 and R20 is individually alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; each R' and R20' is individually H, alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; and W is a trisubstituted phosphorous. The method provides an alternative route to indole-3-glyoxylamide compounds.
专利号:US-6894173-B2 优先权日:1999-07-09 标 题 :Intermediates useful for synthesis of heteroaryl-substituted urea compounds, and processes of making same 发明人:ZHANG LIN-HUA; ZHU LEI 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar 1 , Ar 2 , L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
专利号:WO-0144185-A1 优先权日:1999-12-16 标题 :Carbon monoxide-based synthesis of spla2 inhibitors 发明人:SAWYER JASON SCOTT 权利人:LILLY CO ELI; SAWYER JASON SCOTT 摘要:A method of making a compound, comprises reacting a compound represented by formula (I), with CO and a catalyst, to form the compound of formula (II); where formula (I) is and, formula (II) is and where R2 is selected from the group consisting of R20 -OR20, -SR20, -NR20R20'and -C(O)R20; R3, R4, R5, R6 and R7 are each individually selected from the group consisting of H, halogen, R, -OR, -SR, -NRR', -C(O)R, -C(O)OR, -S(O)R and -S(O)2R; provided that at least one of R4 and R5 is not H; each R and R20 is individually selected from the group consisting of alkyl, alkenyl, alkynyl, aryl and heterocyclic radical; and each R' and R20' is individually selected from the group consisting of H, alkyl, alkenyl, alkynyl, aryl and heterocyclic radical. The method provides an alternative route to indole-3-glyoxylamide compounds.
专利号:US-2009036650-A1 优先权日:2005-03-25 标 题 :Compounds and methods for peptide synthesis 发明人:CUERVO JULIO HERMAN; YANACHKOVA MILKA; PETTER RUSSELL C; DURAND-REVILLE THOMAS F; JIMENEZ-GARCIA JOSE CARLOS 权利人:CUERVO JULIO HERMAN; YANACHKOVA MILKA; PETTER RUSSELL C; DURAND-REVILLE THOMAS F; JIMENEZ-GARCIA JOSE CARLOS 摘要:A backbone nitrogen modifying group can prevent aggregation of peptides during peptide synthesis. The modifying group can promote aqueous solubility of the peptides, and be compatible with solid phase peptide synthesis. Methods for making peptides are also described.
专利号:US-2003166931-A1 优先权日:1999-07-09 标 题 :Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents