📜4-[(3-乙炔基苯基)氨基]-7-甲氧基-喹唑啉-6-醇置于羟胺,Potassium Carbonate体系中,用 水,N,N-二甲基甲酰胺 用作溶剂,化学反应 24.5H,反应生成7-[[4-(3-乙炔基苯基氨基)-7-甲氧基喹唑啉-6-基]氧基]-N-羟基庚酰胺 参考文献:Formulation Of Quinazoline Based Egfr Inhibitors Containing A Zinc Binding Moiety 标题:Formulation Of Quinazoline Based Egfr Inhibitors Containing A Zinc Binding Moiety 摘要:本发明涉及一种包含环糊精和喹唑啉含锌结合基团衍生物的包含复合物的组合物.环糊精最好是β-环糊精或其衍生物.喹唑啉具有增强和意想不到的性质,作为表皮生长因子受体酪氨酸激酶(egfr-Tk)的抑制剂,以及它们在治疗egfr-Tk相关疾病和疾病如癌症中的用途.所述衍生物还可以作为hdac抑制剂.
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-2018371021-A1 优先权日:2017-05-11 标 题 :Peptidomimetic macrocycles and uses thereof 发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
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-2022396794-A1 优先权日:2019-06-04 标题:APTAMERS AGAINST TRANSFERRIN RECEPTOR (TfR) 发明人:HABIB NAGY; ROSSI JOHN; YOON SORAH; SWIDERSK PIOTR MAREK 权利人:APTERNA LTD; HOPE CITY 摘要:Methods of treating or preventing a disease or disorder are disclosed comprising administering to a subject in need thereof an effective amount of a nucleic acid compound comprising, or consisting of, a nucleic acid sequence capable of binding to a transferrin receptor (TfR) and an effective amount of an inhibitor of DNA synthesis. Also disclosed is a nucleic acid compound comprising, or consisting of, a nucleic acid sequence having at least 85% sequence identity to SEQ ID NO: 1, wherein said nucleic acid sequence is at least 30 nucleotides in length and at most 50 nucleotides in length, and wherein the nucleic acid sequence is capable of binding to a transferrin receptor (TfR).
1. Cai, Xiong; Zhai, Hai-Xiao; Wang, Jing; Forrester, Jeffrey; Qu, Hui; Yin, Ling; Lai, Cheng-Jung; Bao, Rudi; Qian, Changgeng. Discovery of 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer. Journal of Medicinal Chemistry (2010), 53(5), 2000-2009. CODEN: JMCMAR ISSN:0022-2623. CAN 152:326271 AN 2010:170333 2. Morphy, Richard. Selectively Nonselective Kinase Inhibition: Striking the Right Balance. Journal of Medicinal Chemistry (2010), 53(4), 1413-1437. CODEN: JMCMAR ISSN:0022-2623. CAN 152:183130 AN
合成参考文献
参考文献:10.1186/s12885-019-5861-4 摘要:Skaga E, Kulesskiy E, Fayzullin A, Sandberg CJ, Potdar S, Kyttälä A, Langmoen IA, Laakso A, Gaál-Paavola E, Perola M, Wennerberg K, Vik-Mo EO. Intertumoral heterogeneity in patient-specific drug sensitivities in treatment-naïve glioblastoma. BMC Cancer. 2019 Jun 25;19(1):628. 参考文献:10.1021/jm901453q 摘要:Cai X, Zhai HX, Wang J, Forrester J, Qu H, Yin L, Lai CJ, Bao R, Qian C. Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. J Med Chem. 2010 Mar 11;53(5):2000–9. doi: 10.1021/jm901453q.