专利号:EP-1383732-B1 优先权日:2001-05-04 标题:Labelling reagents, method for synthesis of said reagents and methods for detecting biological molecules 发明人:BOURGET CECILE; LHOMME JEAN; LAAYOUN ALI; KOTERA MITSUHARU; TREVISIOL EMMANUELLE; MENOU LIONEL; BERNAL MENDEZ ELOY 权利人:BIO MERIEUX; UNIV GRENOBLE 1; CENTRE NAT RECH SCIENT 摘要:The invention concerns a temperature-stable labelling reagent of formula (I), wherein: R<1> represents H or an alkyl, aryl or substituted aryl group; R<2> represents a detectable marker or at least two detectable markers linked together by at least a multimeric structure; L is a linking arm comprising a linear catemer concatenation of at least two covalent bonds; and n is an integer equal to 0 or 1; R<3> and R<4> represent, independently of each other: H, NO2, Cl, Br, F, I, R<2>-(L)n-Y-X-, OR, SR, NR2, R, NHCOR, CONHR, COOR with R = alkyl or aryl, A is a linking arm comprising at least a double bond enabling the conjugation of the diazo function with the aromatic cycle; and u is a whole number between 0 and 2, preferably between 0 and 1; and -Y-X- represents -CONH-, -NHCO-, -CH2O-, -CH2S-. The invention also concerns a method for the synthesis of said markers and uses for labelling biological molecules, in particular nucleic acids, with a labelling reagent bearing the diazomethyl function. The invention is particularly applicable in the field of diagnosis.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-12110273-B2 优先权日:2022-07-26 标题:Method of preparing indolin-2-one compound and method of using indolin-2-one 发明人:LUO MEI 权利人:UNIV HEFEI TECHNOLOGY 摘要:A compound, having a structure represented by a formula (I), n n n n n n n n n n and prepared by one-pot synthesis of benzophenone hydrazone, 7-chloroisatin, and copper(II) acetate monohydrate, and refluxing in 100 mL of anhydrous methanol solvent for 48 hrs. A method for preparing the compound includes: collecting and placing 0.0235 g of benzophenone hydrazone, 0.6914 g of 7-chloroisatin, and 0.6720 g of copper(II) acetate monohydrate complex in a 100.0 mL flask; adding 50 mL of anhydrous methanol as a solvent; stirring a resulting mixture at room temperature for 48 hrs; performing column chromatography separation, and elution with petroleum ether/dichloromethane in a volume ratio of 1:1, and collecting final component points and naturally volatilizing the final component points to obtain 7(E)-chloro-3-diphenylmethylindolin-2-one crystals. The compound is used as a catalyst for reaction between benzophenone imine and trimethylsilonitrile, and has a catalytic effect with a conversion rate reaching 99%.
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-6465693-B2 优先权日:1998-02-26 标 题 :Metal-catalyzed arylations of hydrazines, hydrazones, and related substrates 发明人:BUCHWALD STEPHEN L; WAGAW SEBLE; GEIS O 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.
专利号:EP-1058678-B1 优先权日:1998-02-26 标 题:Metal-catalyzed arylations and vinylations of hydrazines, hydrazones, hydroxylamines and oximes 发明人:BUCHWALD STEPHEN L; WAGAW SEBLE; GEIS OLIVER 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.