CAS: 193275-84-2; (R)-4-(2-(4-(3,10-Dibromo-8-Chloro-6,11-Dihydro-5H-Benzo[5,6]Cyclohepta[1,2-B]Pyridin-11-yl)Piperidin-1-yl)-2-Oxoethyl)Piperidine-1-Carboxamide

上下游产品

trimethylsilyl is°Cyanate cycloheptapyridin-11(R)-yl)-1-piperidine(+)-4-(8-chloro-3,10-dibromo-6,11-dihydro-5H-benzo-5,6cyclohepta1,2-bpyridin-11(R)-yl)-1-(4-piperidinyl)acetylpiperidine urea 2-(1-(tert-butoxycarbonyl)piperidin-4-yl)acetic acid

📜1-叔丁氧羰基-4-哌啶乙酸置于盐酸,Sodium Hydroxide,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺体系中,用 N-甲基吡咯烷酮,乙醇,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 34.0H,反应生成洛那法尼
参考文献:一种新的对映选择性烷基化及其在抗癌剂合成中的应用.
标题:一种新的对映选择性烷基化及其在抗癌剂合成中的应用.
摘要:报道了具有仲亲电试剂的双苄基底物的新型对映选择性烷基化.合成了一种简单的基于去氧麻黄碱的手性配体,该烷基化产物的收率为95%,Ee为95%.揭示了对对映选择性的独特水效应.使用许多双苄基底物和第二亲电试剂可获得非常好至优异的ee值.该新反应已被应用于有希望的抗癌剂的合成.
Doi:10.1021/jo034380T

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:WO-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
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 disgnostic and therapeutic uses.

专利号:US-2025235415-A1
优先权日:2022-02-23
标 题:Modulation of human breast milk composition
发明人：ROSS MICHAEL G; DESAI MINA
权利人:LUNDQUIST INST FOR BIOMEDICAL INNOVATION AT HARBOR UCLA MEDICAL CENTER
摘要:Compositions and methods for improving a child, such as an infant's health, are provided. The methods entail improving the quality of breast milk in a female human individual that provides breast milk, or expects to provide breast milk, to the child, by administering to the individual an agent that increases the individual's sensitivity to insulin, and/or an agent that reduces the substrate uptake, synthesis or secretion of long chain fatty acids, reduces the substrate uptake, synthesis or secretion of short chain fatty acids, increases the amino acid uptake, protein synthesis or protein secretion of proteins, or reduces the uptake or synthesis of lactose.

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:WO-2010034314-A1
优先权日:2008-09-24
标题:Retroviral delivery of synthectic gene cassettes
发明人：PEDERSEN FINN SKOU; BAHRAMI SHERWIN
权利人:UNIV AARHUS; PEDERSEN FINN SKOU; BAHRAMI SHERWIN
摘要:The present invention relates to a multifunctional molecule which is capable of initiating first and/or second strand DNA synthesis of a retroviral RNA genome or derivatives thereof. The multifunctional molecule comprises a first part complementary to a part of the retroviral RNA genome or derivatives thereof. A second part of the multifunctional molecule comprises genetic elements and/or labels. The genetic elements may be gene cassettes for the expression of proteins, peptides or polypeptides or for example functional RNA elements such as shRNA, siRNA, miRNA and the like. The multifunctional molecule represents a novel tool for insertion of genes into host cell genomes. The present invention therefore relates to the field of gene delivery and methods employed therefore.