CAS: 860352-01-8; (S)-5-(3-Fluorophenyl)-N-(Piperidin-3-yl)-3-Ureidothiophene-2-Carboxamide

上下游产品

(S)-3-{[5'-(3''-Fluorophenyl)-3'-Ureidothiophene-2'-Carbonyl]Amino}Piperidine-1-Carboxylic Acid Tert-Butyl Ester 860354-61-6
(S)-3-(3-氨基-5-(3-氟苯基)噻吩-2-甲酰胺基)哌啶-1-甲酸叔丁酯 (S)-3-{[3'-Amino-5'-(3''-Fluorophenyl)Thiophene-2'-Carbonyl]Amino}Piperidine-1-Carboxylic Acid Tert-Butyl Ester 1192875-04-9

(S)-3-(2-Chloro-Acetylamino)-Piperidine-1-Carboxylic Acid Tert-Butyl Ester置于盐酸,Sodium Methylate,三乙胺体系中,用 四氢呋喃,2-甲基四氢呋喃,甲醇,水 作为反应溶剂,化学反应 10.83H,反应生成 (3R)-1-[4,4-双(3-甲基噻吩-2-基)丁-3-烯基]哌啶-3-甲酸盐酸盐
参考文献:改进的收敛性合成azd7762:多公斤级高度取代的噻吩的一锅构建.
标题:改进的收敛性合成azd7762:多公斤级高度取代的噻吩的一锅构建.
摘要:Azd7762的多公斤级合成已使用高度收敛的路线实现,该路线采用两个有效的伸缩序列反应生成关键中间体.氨基噻吩11由肉桂腈9以四步,一锅加成-消除-环化顺序形成,从而构建了具有所需api取代模式的三取代噻吩环.肉桂腈9是通过3-氟苯乙酮的精制而得到的.从手性哌啶5分离的5个阶段中,尿素官能团的反应生成以及随后的脱保护作用,以49%的收率提供azd7762与第一代方法相比,收率提高了5倍,从而减少了原料负担并消除了以前对金属介导的偶联和色谱法的要求.
DOI:10.1021/acs.Oprd.6B00364

专利信息

专利号:US-10772971-B2
优先权日:2017-06-22
标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
发明人：GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

专利号:US-2025034520-A1
优先权日:2022-04-08
标 题:Increasing developmental potential of human preimplantation embryos by reducing genetic instability, aneuploidies and chromosomal mosaicism
发明人：EGLI DIETRICH
权利人:UNIV COLUMBIA
摘要:Disclosed herein are agents, compositions and methods for increasing the developmental potential of human preimplantation embryos. n Disclosed herein are methods of reducing or decreasing replication abnormalities and/or aneuploidies in an embryo as well as increasing genome stability and/or developmental potential of an embryo by activating kinases and/or their signaling pathway in an oocyte including but not limited to ATR, WEE1, and CHK1. n Also disclosed herein are methods of reducing or decreasing replication abnormalities and/or aneuploidies in an embryo as well as increasing genome stability and/or developmental potential of an embryo using polynucleotides, polypeptides and/or agents which increase efficiency of the “fork reversion and repairâ€? pathway and/or decrease detrimental outcomes such as fork collapse, translesion synthesis and/or gap formation. n Lastly disclosed herein are methods of reducing or decreasing replication abnormalities and/or aneuploidies in an embryo as well as increasing genome stability and/or developmental potential of an embryo using one or more polynucleotides or polypeptides including but not limited to CHEK1, WEE1, ETAA1, ATRX, BLM, BRCA2, CHD4, DNA2 (DNA2L), EXO1, FANCC, FANCG, FBH1 (FBX018), HLTF (SMARCA3), MCM9, MSH6, POLD3, POLK, RAD51, RAD52, RAD54L, RB1, RECQL, REV3L, RIF1, RNF8, SETD1A, SHPRH, SMARCAL1, TDRD3, TOPBP1, TP53BP1, WRNIP1, XRCC2, WRN, BRCAI, ZRANB3, CDC6, CDT1, POLH, POLI, FANCD2, INO80, FANCB, ASH2L, FAM35A, XRCC3, BRIP1, and NF168.

专利号:US-9487539-B2
优先权日:2009-09-18
标 题 :Compounds and therapeutic use thereof for protein kinase inhibition
发明人：WU ZHANGGUI
权利人:WU ZHANGGUI
摘要:Novel compound having the following formula: n nwherein Y is N, O, or S. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.