CAS: 10596-23-3; (Dichloromethylene)Diphosphonic Acid

上下游产品

tetraisopropyl dichloromethylenebisphosphonateuridine-5'-β,γ-dichloromethylene triphosphate ammonium adenosine 5'-(β,γ-dichloromethylene)triphosphate

(二氯亚甲基)二磷酸四异丙酯置于盐酸体系中,用 水 用作溶剂,化学反应 3.0H,反应生成氯屈瞵酸
参考文献:双膦酸盐生成的 Atp 类似物抑制细胞信号通路
标题:双膦酸盐生成的 Atp 类似物抑制细胞信号通路
摘要:双膦酸盐是一类主要用于治疗骨质疏松症,佩吉特病和癌症的药物.已经提出它们通过抑制一种或多种靶标起作用,包括蛋白质异戊二烯化,表皮生长因子受体或腺嘌呤核苷酸移位酶.后者的抑制是由于 Atp 类似物在细胞中的形成:Atp 的异戊烯酯 (Apppi) 或 Atp 的 Appxp 型类似物,例如 Amp-氯膦酸盐 (Appccl2P).我们针对一组 369 种激酶筛选了 Apppi 和 Appccl2P,发现 Appccl2P 能有效抑制某些酪氨酸激酶,这归因于酪氨酸和末端膦酸酯之间形成强氢键.然后我们合成了在细胞中转化为其他 Atp 类似物的双膦酸盐前体药物,发现了抑制细胞信号通路的低 Nm 激酶抑制剂.
Doi:10.1021/jacs.8B02363

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-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-6909010-B2
优先权日:2001-04-11
标题:Facile synthesis of symmetric esters of alkylenebisphosphonic acids
发明人：HERLINGER ALBERT W; STEPINSKI DOMINIQUE C
权利人:UNIV LOYOLA CHICAGO
摘要:A facile synthesis of symmetric esters of C 1 -C 10 alkylenebisphopsphonic acids is disclosed in which a C 1 -C 10 alkylenebis(phosphonic dichloride) is reacted with an alcohol in the presence of a catalytic amount of 1H-tetrazole and a base in an aprotic solvent to form a first reaction mixture. The first reaction mixture is maintained for a time period sufficient to form a C 1 -C 10 alkylenebis(chloro ester phosphonate) that is reacted under basic conditions with an excess of a hydroxylated compound to form a second reaction mixture that is itself maintained for a time period sufficient to form a C 1 -C 10 alkylenebis(ester phosphonate) partial ester, homoleptic tetraester or mixed tetraester. The material so formed can be recovered or used as is.

专利号:US-7202226-B2
优先权日:2000-10-23
标 题 :Augmentation of wound healing by elF-4E mRNA and EGF mRNA
发明人：MURRAY MARY THERESA; DULCHAVSKY SCOTT ALEXANDER
权利人:DETROIT R & D
摘要:There is provided a method of augmenting transient protein synthesis in a cell by delivering to the cell mRNA functionally related to protein production. Also provided is a method of augmenting transient protein synthesis in cells by increasing protein synthesis of growth factors from endogenous cellular mRNA and exogenous mRNA delivered to the cells. A treatment for transiently increasing protein production in cells, said treatment comprising mRNA functionally related to protein production is also provided. There is provided a method of augmenting wound healing by delivering mRNA functionally related to wound healing. Further provided is a therapeutic for transiently increasing protein synthesis in cells, said therapeutic comprising mRNA related to protein production.

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-9662347-B2
优先权日:2010-05-11
标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system
发明人：LEE BONG HEE; BYUN KYUNG HEE
权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND
摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.