专利号:US-6417380-B1 优先权日:1987-12-31 标 题 :Synthesis of 1,2-dioxetanes and intermediates therefor 发明人:BRONSTEIN IRENA Y; EDWARDS BROOKS 摘要:Compounds having the formula: n wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C 1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (e.g., n m-phenylene), produced by reacting a compound having the formula: n with an R-ylating agent (e.g., R 2 SO 4 ) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: n are produced by reacting a compound having the formula: n with n wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula n are produced by reacting a compound of the formula n with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups. The aforementioned compounds and procedures are useful in the synthesis of enzyme-cleavable 1,2-dioxetane ring systems that can serve as members of a binding pair employed, for example, in chemiluminescent immunoassays, DNA probe assays, and direct assays for an enzyme.
专利号:US-5777133-A 优先权日:1987-12-31 标 题:Synthesis of 1, 2-dioxetanes and intermediates therefor 发明人:BRONSTEIN IRENA Y; EDWARDS BROOKS 权利人:TROPIX INC 摘要:Compounds having the formula: ##STR1## wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C 1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (eg., m-phenylene), produced by reacting a compound having the formula: ##STR2## with an R-ylating agent (e.g., R 2 SO 4 ) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: ##STR3## are produced by reacting a compound having the formula: ##STR4## wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula ##STR5## are produced by reacting a compound of the formula ##STR6## with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups. The aforementioned compounds and procedures are useful in the synthesis of enzyme-cleavable 1,2-dioxetane ring systems that can serve as members of a binding pair employed, for example, in chemiluminescent immunoassays, DNA probe assays, and direct assays for an enzyme.
专利号:US-4956477-A 优先权日:1987-12-31 标 题:Synthesis of 1,2-dioxetanes 发明人:BRONSTEIN IRENA Y; EDWARDS BROOKS 权利人:TROPIX INC 摘要:Compounds having the formula: ##STR1## wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C 1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (e.g., m-phenylene), produced by reacting a compound having the formula: ##STR2## with an R-ylating agent (e.g., R 2 SO 4 ) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: ##STR3## are produced by reacting a compound having the formula: ##STR4## wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula ##STR5## are produced by reacting a compound of the formula ##STR6## with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups. The aforementioned compounds and procedures are useful in the synthesis of enzyme-cleavable 1,2-dioxetane ring systems that can serve as members of a binding pair employed, for example, in chemiluminescent immunoassays, DNA probe assays, and direct assays for an enzyme.
专利号:WO-2009080631-A2 优先权日:2007-12-21 标 题 :Chemo-enzymatic synthesis of a c-terminal aryl amide of an amino acid or peptide 发明人:QUAEDFLIEG PETER JAN LEONARD MARIO; NUIJENS TIMO; CUSAN CLAUDIA 权利人:DSM IP ASSETS BV; QUAEDFLIEG PETER JAN LEONARD MARIO; NUIJENS TIMO; CUSAN CLAUDIA 摘要:The present invention relates to a method for preparing an aryl amide, comprising reacting an aryl amine with a compound selected from N-protected amino acids and optionally N-protected peptides in the presence of a hydrolytic enzyme. The invention further relates to the use of a compound obtained in a method according to the invention in the manufacture of a diagnostic. In addition the invention relates to the use of a compound obtained in a method according to the invention as a substrate for a proteolytic enzyme.
专利号:US-7897762-B2 优先权日:2006-09-14 标 题:Kinase inhibitors useful for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:DECIPHERA PHARMACEUTICALS LLC 摘要:The present invention relates to novel kinase inhibitors and modulator compounds 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-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.
[参考文献]: Alberto Diez-Torrubia, Et Al. Application Of The Dipeptidyl Peptidase Iv (Dppiv/cd26) Based Prodrug Approach To Different Amine-Containing Drugs. J Med Chem. 2010 Jan 28;53(2):559-72. [参考文献]: Arianna Loregian, Et Al. The 6-Aminoquinolone Wc5 Inhibits Human Cytomegalovirus Replication At An Early Stage By Interfering With The Transactivating Activity Of Viral Immediate-Early 2 Protein. Antimicrob Agents Chemother. 2010 May;54(5):1930-40. [参考文献]: Makoto Yasuda, Et Al. Simultaneous Determination Of Nicotine And Cotinine In Serum Using High-Performance Liquid Chromatography With Fluorometric Detection And Postcolumn Uv-Photoirradiation System. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Sep 1:934:41-5. [参考文献]: Marco Pieroni, Et Al. From 6-Aminoquinolone Antibacterials To 6-Amino-7-Thiopyranopyridinylquinolone Ethyl Esters As Inhibitors Of Staphylococcus Aureus Multidrug Efflux Pumps. J Med Chem. 2010 Jun 10;53(11):4466-80. [参考文献]: Nivedita Natarajan, Et Al. A Quantitative Metabolomics Peek Into Planarian Regeneration. Analyst. 2015 May 21;140(10):3445-64.
合成参考文献
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 73. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 453. 摘要:Huang, Y.; Dömling, A., Science of Synthesis: Multicomponent Reactions, (2013) 1, 261. 摘要:Merino, P., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 324. 摘要:J. J. Elliott and S. F. Mason. J. Chem. Soc. 1959, 2352.