CAS: 955365-80-7; 2-Allyl-1-(6-(2-Hydroxypropan-2-yl)Pyridin-2-yl)-6-((4-(4-Methylpiperazin-1-yl)Phenyl)Amino)-1H-Pyrazolo[3,4-D]Pyrimidin-3(2H)-One

上下游产品

4-(4-Methyl-piperazino)-anilin 2-allyl-1-(6-(2-hydroxypropane-2-yl)pyridin-2-yl)-6-((4-(4-methylpiperazine)-1-yl)phenyl)amino-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one 2-(6-bromopyridin-2- yl)propan-2-ol methyl 6-Bromopicolinate

📜4-(4-甲基哌嗪)苯胺置于间氯过氧苯甲酸,N,N-二异丙基乙胺体系中,用 水,甲苯 作为反应溶剂,化学反应 0.33H,反应生成 2-烯丙基-1-(6-(2-羟基丙烷-2-基)吡啶-2-基)-6-(4-(4-甲基哌嗪-1-基)苯基氨基)-1H-吡唑并[3,4-D]嘧啶-3(2H)-酮
参考文献:Dihydropyrazolopyrimidinone Derivatives
标题:Dihydropyrazolopyrimidinone Derivatives
摘要:该发明涉及一般式(i)的化合物,其中ar1是可选择取代的芳基或杂环芳基;r1是可选择取代的较低烷基,较低烯烃基,较低炔烃基或环状较低烷基基团,或是具有取代基的芳基,芳基烷基或杂环芳基;r2是氢原子,较低烷基基团,较低烯烃基团或较低炔烃基团,或是具有取代基的芳基,芳基烷基或杂环芳基;r3是氢原子或较低烷基基团;r4是氢原子,卤素原子,羟基,较低烷基基团或-n(R1K)R1M基团;t和u是氮原子或亚甲基基团等.该发明的化合物具有出色的weel激酶抑制作用,因此在药物领域中特别适用于治疗各种癌症.

专利信息

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 repair†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:WO-2023091726-A1
优先权日:2021-11-18
标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12)
发明人：BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH
权利人:SYROS PHARMACEUTICALS INC
摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).

专利号:CN-113880844-A
优先权日:2021-09-29
标 题:A new method for chemical synthesis of Wee1 protein kinase inhibitor adavosertib

专利号:CN-113880844-B
优先权日:2021-09-29
标题 :Chemical Synthesis of Wee1 Protein Kinase Inhibitor Adavosertib

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.