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CAS号92-92-2 4-苯基苯甲酸 | CAS号201230-82-2 carbon monoxide | CAS号92-93-3 4-硝基联苯 | CAS号32315-10-9 三光气 | CAS号92-67-1 4-氨基联苯 | CAS号75-44-5 光气 | CAS号2113-61-3 4-Aminobiphenyl... | CAS号13262-48-1 Urea,N-[1,1'-bi... | CAS号3185-71-5 Urea,N-[1,1'-bi... | CAS号4445-40-3 2-amino-5-pheny...4-苯基苯甲酸置于叠氮磷酸二苯酯,三乙胺体系中,用 甲苯 作为反应溶剂,化学反应 0.67H,反应生成 4-联苯异氰酸盐
参考文献:金黄色葡萄球菌 Rnpa 抑制剂:计算指导设计,合成和初步生物学评价
标题:金黄色葡萄球菌 Rnpa 抑制剂:计算指导设计,合成和初步生物学评价
摘要:抗生素耐药性正在全球蔓延,已成为现代医学中最重要的问题之一.在这种情况下,细菌 Rna 降解和加工机制是细菌活力的基本过程,可用于抗菌治疗.在金黄色葡萄球菌中,Rnpa 被假设为这些机制的主要参与者之一.金黄色葡萄球菌rnpa 能够调节 Mrna 降解并与核酶 (Rnpb),促进 Ptrna 成熟.相应的小分子筛选活动最近确定了几类 Rnpa 抑制剂,它们的结构活性关系 (Sar) 仅被部分探索.因此,在目前的工作中,使用金黄色葡萄球菌的计算建模rnpa 我们确定了已知 Rnpa 抑制剂的假定关键相互作用,并且我们使用这些信息来设计,合成和生物学评估新的潜在 Rnpa 抑制剂.目前的结果可能有助于全面了解属于 Rnpa2000 样氨基硫脲和 Jc 样哌啶甲酰胺分子类别的 Rnpa 抑制剂.我们评估了不同关键部分的重要性,例如 Jc2 的二氯苯基和哌啶,以及 Rnpa2000 的半硫代卡
DOI:10.3390/antibiotics10040438
专利信息
专利号:US-2007282078-A1
优先权日:2006-06-01
标题:Synthesis of aryl N-acylurea from aryl isocyanates or aryl carbodiimides for use as intermediate in novel sequential self-repetitive reaction (SSRR) to form amides, amide-imides and their polymers
发明人:DAI SHENGHONG A; LIN JIANG-JEN; WEI KUAN-LIANG; WU CHIH-HENG; HUANG WEI-HSIANG
权利人:DAI SHENGHONG A; LIN JIANG-JEN; WEI KUAN-LIANG; WU CHIH-HENG; HUANG WEI-HSIANG
摘要:Disclosed is a process for synthesizing an aryl N-acylurea in both high selectivity and high yield, comprising reacting an aryl carbodiimide with a carboxylic acid under mild conditions. Thermolysis of N-acylureas at above about 120° C. gives amides and isocyanates, and the latter will undergo the repetitive reaction sequences in the presence of a carbodiimide catalyst. Based on this unique model, a sequential self-repetitive reaction (SSRR) is also developed in a versatile manner for converting aryl carbodiimides into amides, polyamides, polyamide-imides and polyamide-imide elastomers.
专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
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:WO-9700244-A1
优先权日:1995-06-19
标题 :Process for parallel synthesis of a non-peptide library
发明人:FRITZ JAMES E; KALDOR STEPHEN W
权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W
摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
专利号:US-2005192265-A1
优先权日:2003-03-20
标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J
摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6906056-B2
优先权日:1998-06-22
标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J
权利人:LILLY CO ELI
摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.