CAS: 129618-40-2; 11-Cyclopropyl-4-Methyl-5,11-Dihydro-6H-Dipyrido[3,2-B:2',3'-E][1,4]Diazepin-6-One

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2-氯烟酰氯置于吡啶,Sodium Hydride体系中,用 1,4-二氧六环,环己烷,Xylene 用作溶剂,化学反应 67.5H,反应生成萘维拉平
参考文献:Hiv-1逆转录酶的新型非核苷抑制剂.1.三环吡啶并苯并二氮杂二酮.
标题:Hiv-1逆转录酶的新型非核苷抑制剂.1.三环吡啶并苯并二氮杂二酮.
摘要:新型吡啶并[2,3-B] [1,4]苯并二氮杂酮(i),吡啶并[2,3-B] [1,5]苯并二氮杂酮(II)和二吡啶并[3,2-B:2',3发现在低至35 Nm的浓度下,'-E] [1,4]二氮杂酮(III)在体外抑制1型人类免疫缺陷病毒(hiv-1)逆转录酶.在所有三个系列中,在内酰胺氮上优选小的取代基(例如甲基,乙基,乙酰基),而在另一个(n-11)二氮杂庚酮氮上优选稍大的烷基部分(例如乙基,环丙基).通常,相对于在芳环上没有取代基的相应化合物,在a环上优选亲脂取代基,而在c环上的取代通常会降低效能.在内酰胺氮原子邻位的甲基取代可实现最大效力.然而,在这种情况下,优选未取代的内酰胺氮.A环上的其他取代基很容易被容忍.双吡啶二氮杂庚酮衍生物11-环丙基-5,11-二氢-4-甲基-6H-二吡啶并[3,2-B:2',3'-E] [1,4]二氮杂-6-1(96,奈韦拉平)是一种有效的(ic50
Doi:10.1021/jm00111A045

专利信息

专利号:WO-9624694-A1
优先权日:1995-02-10
标 题:Method and kit for fluorometric analysis of enzymes catalyzing synthesis of nucleic acids
发明人：CHAVAN SURENDRA J; PROCHASKA HANS J
权利人:SLOAN KETTERING INST CANCER
摘要:This invention provides a method for detecting in a sample an enzyme which catalyzes the synthesis of a double-stranded nucleic acid molecule from a nucleic acid template which comprises contacting the sample with a suitable fluorophore which selectively binds to double-stranded DNA. Also provided is a method for determining in a sample the activity of such an enzyme. This invention also provides a method for detecting an RNA-DNA heteroduplex in a sample which comprises contacting the sample with a suitable fluorophore which selectively binds to double-stranded DNA. This method for detecting an RNA-DNA heteroduplex may further comprise quantitatively determining detected RNA-DNA heteroduplex. This invention also provides a method for detecting in a sample en enzyme which catalyzes the synthesis of and RNA-DNA heteroduplex from a nucleic acid template, as well as a method of detecting the activity of such an enzyme in a sample. This invention further provides a method for detecting the viral load of HIV in a sample. Also provided is a method for diagnosing an HIV infection in a subject, and for monitoring the progression of an HIV infection in a subject. Also provided is a method for determining the viral load of HIV in a subject infected with HIV. This invention further provides a method for identifying whether a substance inhibits reverse transcriptase. Finally, this invention provides a kit for assaying an enzyme which catalyzes the synthesis of a double-stranded nucleic acid molecule from a nucleic acid template.

专利号:US-6818633-B2
优先权日:2001-06-29
标题:Antiviral compounds and methods for synthesis and therapy
发明人：BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN
权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING
摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).

专利号:US-2010261876-A1
优先权日:2007-09-25
标 题:Novel methods of synthesis for therapeutic antiviral peptides
发明人：BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E
权利人:BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E
摘要:Provided herein are methods for synthesis of peptides. In particular, provided herein are methods of synthesis for therapeutic antiviral peptides.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-2004077674-A1
优先权日:2002-03-01
标题:Mappicine analogs, intermediates in the synthesis of mappicine analogs and methods of synthesis of mappicine analogs
发明人：CURRAN DENNIS P; PARNIAK MICHAEL A; GABARDA ANA; ZHANG WEI; LUO ZHIYONG; CHEN CHRISTINE HIU-TUNG
摘要:A compound having the following structure: n n n wherein Z is —CHOR 1 R 2 or —C(O)R 2 ; R 1 is H, an alkyl group, an aryl group, —OC(O)OR a , wherein R a is an alkyl group, —C(O)R b wherein R b is an alkyl group, an aryl group, an alkoxy group, an amino group, an alkylamino group, a dialkylamino group, an aryl amino group, a diarylamino group, an arylalkyl amino group, a protecting group or a fluorous tag; R 2 is an alkyl group, an aryl group or an arylalkyl group; R 3 is H, an alkyl group, hydroxyalkyl group or an aryl group; R 4 —R 8 are independently the same or different and are hydrogen, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, an alkoxy group, an aryloxy group, an acyloxy group, a haloalkyl group, a perfluoroalkyl group, fluorine, chlorine, bromine, a haloalkyloxy group, a carbamoyloxy group, a hydroxy group, a nitro group, a cyano group, a cyanoalkyl group, an azido group, an azidoalkyl group, a formyl group, a hydrazino group, a hydrazinoalkyl group, a hydroxyalkyl group, an alkoxyalkyl group, —NR 1 R m , wherein R 1 and R m are independently hydrogen, an alkyl group, an aryl group, an arylalkyl group, or —C(O)R b , an aminoalkyl group, an alkylaminoalkyl group, a dialkylaminoalkyl group, an aryl aminoalkyl group, a diarylaminoalkyl group, an arylalkyl aminoalkyl group, —OC(O)OR a , wherein R a is an alkyl group, —C(O)R b , —SR c , S(O)R c or S(O 2 )R c wherein R c is hydrogen, —C(O)R b , an alkyl group, or an aryl group, (CH 2 ) n SiR d R e R f wherein n is an integer within the range of 0 through 10 and R d , R e and R f are independently a C 1-10 alkyl group, a C 2-10 alkenyl group, a C 2-10 alkynyl group, an aryl group, a haloalkyl group, a cyanoalkyl group, an azidoalkyl group, a hydrazinoalkyl group, a hydroxyalkyl group, an alkoxyalkyl group, an aminoalkyl group, an alkylaminoalkyl group, a dialkylaminoalkyl group, an aryl aminoalkyl group, a diarylaminoalkyl group, an arylalkyl aminoalkyl group. Alternatively R 4 and R 5 , R 5 and R 6 ; R 6 and R 7 ; or R 7 and R 8 can form together a chain of 3 or four groups selected from CH, CH 2 , O, S, N, NH, N-alkyl or N-aryl. Provided that, at least one of R 5 —R 7 is not H, a lower alkyl group, fluorine, a cyano group, a hydroxyl group, hydroxyalkyl group, an alkoxy group, an aminoalkyl group, an alkylaminoalkyl group, a dialkylaminoalkyl group, an amino group, an alkylamino group, a dialkylamino group, a carbamoyloxy group, a formyl group or —C(O)R x wherein R x is an alkyl group.

专利号:US-11845970-B2
优先权日:2016-01-15
标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins
发明人：WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN
权利人:UNIV MARYLAND
摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.