CAS: 267243-28-7; N-(4-((3-Chloro-4-Fluorophenyl)Amino)-7-(3-Morpholinopropoxy)Quinazolin-6-yl)Acrylamide

上下游产品

acrylic acid (3-CHLORO-4-FLUOROPHENYL)-[7-(3-MORPHOLIN-4-YL-PROPOXY)-6-AMINO-QUINAZOLINE-4-YL]-AMINE 3-morpholin-4-ylpropan-1-ol 3-chloro-4-fluorophenylamine

4-(3-羟丙基)吗啉置于sodium,铁粉,溶剂黄146,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺体系中,用 四氢呋喃,乙醇,N,N-二甲基乙酰胺 用作溶剂,化学反应 2.5H,反应生成卡奈替尼
参考文献:酪氨酸激酶抑制剂.17.表皮生长因子受体的不可逆抑制剂:具有附加增溶功能的4-(苯基氨基)喹唑啉-和4-(苯基氨基)吡啶并[3,2-D]嘧啶-6-丙烯酰胺.
标题:酪氨酸激酶抑制剂.17.表皮生长因子受体的不可逆抑制剂:具有附加增溶功能的4-(苯基氨基)喹唑啉-和4-(苯基氨基)吡啶并[3,2-D]嘧啶-6-丙烯酰胺.
摘要:通过使相应的6-胺与丙烯酸或丙烯酸酐反应,制备被可溶的7-烷基胺或7-烷氧基胺侧链取代的4-苯胺基喹唑啉-和4-苯胺基吡啶并[3,2-D]嘧啶-6-丙烯酰胺.在吡啶并[3,2-D]嘧啶系列中,中间体7-氨基-6-烷基胺是由7-溴-6-氟吡啶并[3,2-D]嘧啶在适当的条件下,通过钯与适当的锡烷偶联而制得的. 0)催化.这证明了引入阳离子增溶侧链的通用方法.评价化合物对分离的egfr酶的磷酸化的抑制,以及对a431细胞中egfr的egf刺激的egfr自身磷酸化的抑制以及mda-Mb 453细胞中调蛋白刺激的erbb2自身磷酸化的抑制.具有7-烷氧基胺增溶基团的喹唑啉类似物是分离的egfr酶的有效不可逆抑制剂,Ic(50P)值为2至4Nm,并有效抑制细胞中的egfr和erbb2自磷酸化.7-烷基氨基-和7-烷氧基氨基吡啶并[3,2-D]嘧啶也是不可逆的抑制剂,对分离的酶具有相同或更高的效力,但
Doi:10.1021/jm990482T

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

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-9365532-B1
优先权日:2011-02-14
标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines
发明人：ISAACMAN STEVEN
权利人:ISAACMAN STEVEN; NANOMETICS LLC
摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.

专利号:US-2019031650-A1
优先权日:2016-01-29
标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies
发明人：HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN
权利人:UNIV YALE
摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of 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.