CAS: 136-70-9; 4-[2-[1-(1,3-Benzodioxol-5-yl)Propan-2-Ylamino]-1-Hydroxyethyl]Benzene-1,2-Diol

📜Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于乙醇,铂体系中,化学反应生成普罗托醇
参考文献:Bronchodilators,N-Substituted Derivatives Of 1-(3',4'-Dihydroxyphenyl)-2-Aminoethanol (Arterenol)
标题:Bronchodilators,N-Substituted Derivatives Of 1-(3',4'-Dihydroxyphenyl)-2-Aminoethanol (Arterenol)
摘要:
Doi:10.1021/ja01641A010

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-8853132-B2
优先权日:2008-11-27
标题 :Directed synthesis of oligophosphoramidate stereoisomers
发明人：HEINDL DIETER; KESSLER DIRK; ROESLER ANGELIKA; SEIDEL CHRISTOPH; THUER WILMA
权利人:ROCHE DIAGNOSTICS OPERATIONS
摘要:The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.

专利号:US-11766432-B2
优先权日:2018-07-27
标题 :Cleavable conjugates of catechol compounds and water-soluble polymers and methods of treatment using the same
发明人：BENTLEY MICHAEL; FANG ZHIHAO; WEIMER REBECCA; VIEGAS TACEY; MOREADITH RANDALL
权利人:SERINA THERAPEUTICS INC
摘要:Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.

专利号:US-7338932-B2
优先权日:2000-05-11
标题 :Methods of modulating functions of polypeptide GalNAc-transferases and of screening test substances to find agents herefor, pharmaceutical compositions comprising such agents and the use of such agents for preparing medicaments
发明人：CLAUSEN HENRIK; BENNETT ERIC PAUL; HASSAN HELLE; REIS CELSO ALBUQUERQUE
权利人:GLYCOZYM APS
摘要:Attachment of O-glycans to proteins is controlled by a large family of homologous polypeptide GalNAc-transferases. Polypeptide GalNAc-transferases contain a C-terminal sequence with similarity to lectins. This invention discloses that the putative lectin domains of GalNAc-transferase isoforms, GalNAc-T4, -T7, -T2, and -T3, are functional and recognize carbohydrates, glycopeptides, and peptides and discloses the lectin domains of GalNAc-T1-T16. These lectin domains have different binding specificities and modulate the functions of GalNAc-transferase isoforms differently. Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed. The present invention specifically discloses a novel selective inhibitor of polypeptide GalNAc-transferase lectin domains, which provides a major advancement in that this inhibitor and related inhibitors sharing common characteristics of activity bind lectin domains without serving as acceptor substrate for glycosyltransferases involved in synthesis of O-glycans. This inhibitor is represented by the β-anomeric configuration of GalNAc-benzyl, GalNAcβ-benzyl. Methods for inhibiting intracellular transport, cell surface expression, and secretion of mucins and O-glycosylated glycoproteins without affecting O-glycosylation processing are disclosed using the novel selective inhibitor identified.

专利号:EP-1558728-B1
优先权日:2002-11-08
标 题:Methods to identify agents modulating functions of polypeptide galnac-transferases, pharmaceutical compositions comprising such agents and the use of such agents for preparing medicaments
发明人：CLAUSEN HENRIK; BENNETT ERIC PAUL
权利人:GLYCOZYM APS
摘要:Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed. The present invention specifically discloses a novel selective inhibitor of polypeptide GalNAc-transferase lectin domains, which provides a major advancement in that this inhibitor and related inhibitors sharing common characteristics of activity bind lectin domains without serving as acceptor substrate for glycosyltransferases involved in synthesis of O-glycans. This inhibitor is represented by the O-anomeric configuration of GalNAc-benzyl, GalNAcbeta-benzyl. Methods for inhibiting intracellular transport, cell surface expression, and secretion of mucins and O-glycosylated glycoproteins without affecting O-glycosylation processing are disclosed using the novel selective inhibitor identified.

专利号:US-4668624-A
优先权日:1979-02-28
标 题:Protein translation method
发明人：ROBERTS BRYAN E
权利人:DU PONT
摘要:An improved method for in vitro synthesis of protein by in vivo processes in an extract from a living organism and containing endogenous ribosomes and endogenous transfer RNA, primarily from endogenous amino acids in said extract primarily by the use of a predetermined exogenous messenger ribonucleic acid (mRNA). An improved method of assaying such a synthesis by the use of a labelled amino acid, which is present during said synthesis and is incorporated into said protein. A kit for carrying out such synthesis and assay comprising a vial of substantially prokaryotic and eukaryotic cell-free extract from a living organism containing endogenous ribosomes, endogenous transfer RNA and endogenous amino acids, a vial containing translation cocktail for promoting the synthesis, and a vial containing control messenger RNA.