CAS: 118409-57-7; 2-(3,4-Dihydroxybenzylidene)Malononitrile

上下游产品

malononitrile 3,4-dihydroxybenzaldehyde 3,4-bis-methoxymethoxy-benzaldehyde piperidine AG 99

📜丙二腈,3,4-二羟基苯甲醛 以 水 用作溶剂,化学反应 0.25H,以78%的收率获得(3,4-二羟基苄基)丙二腈
参考文献:多羟基化的苯基丙烯酸衍生物作为新型抗肿瘤剂.
标题:多羟基化的苯基丙烯酸衍生物作为新型抗肿瘤剂.
摘要:初步证据表明,含有邻二羟基苯部分的抗肿瘤药对黑色素瘤细胞等具有高氧化潜能的恶性细胞表现出增强的抗肿瘤活性.基于此考虑,制备了具有不同氧化还原电势的11种羟苯丙烯酸衍生物作为黑素瘤特异性酶酪氨酸酶的潜在底物,其可能表现出一般的抗肿瘤活性并增强了对黑素瘤细胞的细胞毒性.这些化合物中的五个[α-氰基-β-(4-羟基苯基)-,α-氰基-β-(3,4-二羟基苯基)-和α-氰基-β-(3,4,5-三羟基苯基)丙烯酸发现酪氨酸酶(thppa)和3,4-二羟基-和3,4,5-三羟基苯并氰基乙酰胺]是酪氨酸酶的底物,Km值为0.08至4.13 Mm,Vmax值为0.18至3.02.这些数据表明,随着羟基数目的增加,氧化速率增加,并且氰酰胺比相应的氰酸的反应更快,其中二氰化物的反应性最低.相反,氰酰胺作为底物的效果不如氰酸.体外研究表明,除两种化合物外,所有化合物均对l1210(ic50范围为21-980 M
Doi:10.1002/jps.2600800503

专利信息

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-11406709-B2
优先权日:2014-09-15
标 题 :Therapeutic and research application of PDCL3
发明人：RAHIMI NADER
权利人:UNIV BOSTON
摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

专利号:US-7052692-B1
优先权日:1997-09-02
标题:Role of tyrosine phosphorylation of a cellular protein in adeno-associated virus 2-mediated transgene expression
发明人：SRIVASTAVA ARUN; QING KEYUN; WANG XU-SHAN; PONNAZHAGAN SELVARANGAN; BAJPAI ANIL
权利人:ADVANCED RES & TECH INST
摘要:The present invention identifies a protein, designated the D-sequence-binding protein (D-BP), is phosphorylated at tyrosine residues and blocks AAV-mediated transgene expression in infected cells by inhibiting the leading strand viral DNA synthesis. More particularly, the present invention demonstrates that D-BP is phosphorylated by EGF-R protein tyrosine kinase. Methods of increasing transcription and promoting replication of transgenes exploiting this information are disclosed herein.

专利号:US-2008096868-A1
优先权日:2004-11-12
标题:1,4 Substituted Pyrazolopyrimidines as Kinase Inhibitors
发明人：SCHMIEDEBERG NIKO; FURET PASCAL; IMBACH PATRICIA; HOLZER PHILIPP
权利人:SCHMIEDEBERG NIKO; FURET PASCAL; IMBACH PATRICIA; HOLZER PHILIPP
摘要:The invention relates to 1,4-substituted pyrazolopyrimidine compounds of the formula I, n npharmaceuticals comprising a 1,4-substituted pyrazolopyrimidine compound, the use of a 1,4-substituted pyrazolopyrimidine compound in the treatment or the use thereof in the manufacture of a pharmaceutical formulation for the treatment of a disease that depends on inadequate activity of a protein kinase, methods of treatment comprising administering a 1,4-substituted pyrazolopyrimidine compound, methods for the manufacture of a novel compound of that class, and novel intermediates and partial steps for their synthesis.

专利号:US-2008096883-A1
优先权日:2004-08-11
标题 :Trifluoromethyl substituted benzamides as kinase inhibitors
发明人：CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO
权利人:CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO
摘要:The invention relates to trifluoromethyl substituted benzamide compounds of the formula (I), pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.

专利号:US-2024408209-A1
优先权日:2023-06-07
标 题 :Peptide-Protected Gold Nanocluster and Use in Photodynamic Therapy
发明人：STAMPLECOSKIE KEVIN; AMINFAR PARIMAH; YOUSEFALIZADEH GOONAY; ZHENG GANG; CHEN JUAN
权利人:UNIV KINGSTON; UNIV HEALTH NETWORK
摘要:A gold nanocluster of the formula Au 16 (RGDC) 14 , wherein RGDC is arginine-glycine-aspartic acid-cysteine, and methods for synthesis, are described. The gold nanocluster effectively produces Type I ROS and functions as photosensitizer, and has utility in applications such as, but not limited to, biomedical applications and photocatalysis. The gold nanocluster may be useful in photodynamic therapy (PDT) in cells and tissues for treating diseases such as certain cancers.