CAS: 1256580-46-7; 9-Ethyl-6,6-Dimethyl-8-(4-Morpholinopiperidin-1-yl)-11-Oxo-6,11-Dihydro-5H-Benzo[b]Carbazole-3-Carbonitrile

上下游产品

CAS号1256589-74-8 艾乐替尼盐酸盐

9-Ethynyl-6,6-Dimethyl-8-(4-Morpholin-4-Yl-Piperidin-1-yl)-11-Oxo-6,11-Dihydro-5H-Benzo[b]Carbazole-3-Carbonitrile置于palladium 10% On Activated Carbon,氢气体系中,用 四氢呋喃,甲醇 用作溶剂,化学反应 2.0H,以25%的收率获得艾乐替尼
参考文献:高选择性,口服活性和有效的间变性淋巴瘤激酶抑制剂(ch5424802)的设计与合成
标题:高选择性,口服活性和有效的间变性淋巴瘤激酶抑制剂(ch5424802)的设计与合成
摘要:间变性淋巴瘤激酶(alk)受体酪氨酸激酶被认为是人类癌症,尤其是非小细胞肺癌(nsclc)的有吸引力的治疗靶标.我们以前的研究表明,6,6-二甲基-11-氧代-6,11-二氢-5 H-苯并[ B ]咔唑支架的8,9侧链会严重影响激酶的选择性,细胞活性和代谢稳定性.在这项工作中,我们优化了侧链,并确定了具有高度选择性,口服活性且有效的alk抑制剂ch5424802(18A)作为临床候选药物.
Doi:10.1016/j.Bmc.2011.12.021

专利信息

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-9573932-B2
优先权日:2015-03-02
标题:Synthesis of intermediates in the preparation of ALK inhibitor
发明人：XU YONG
权利人:XU YONG
摘要:The present disclosure provides a method for preparing a compound of formula XVII, comprising: (1) contacting a compound of formula XIV with a compound of formula 3 to obtain a compound of formula 2; and (2) contacting the compound of formula 2 with a compound of formula 4 to obtain a compound of formula XVII. The method is low toxicity, cheap, easy to get, environmentally and friendly, and is economical and industrially applicable.

专利号:US-12398116-B2
优先权日:2020-09-10
标题:Total synthesis of alectinib
发明人：ZHOU LIHUA
权利人:SUZHOU FUDE ZHAOFENG BIOCHEMICAL TECH CO LTD
摘要:The present invention relates to a process for preparing alectinib or a pharmaceutically acceptable salt thereof. The present invention also relates to intermediate compounds which are useful in such process and to the preparation of such intermediate compounds.

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.