CAS: 89987-06-4; [(4-Chlorophenyl)Sulfanyl-Phosphonomethyl]Phosphonic Acid

📜4,4'-二氯二苯二硫醚置于三甲基溴硅烷,Sodium Hydride体系中,用 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 13.0H,反应生成 (4-氯苯硫基)甲叉二膦酸
参考文献:双膦酸盐反应生成的 Atp 类似物抑制细胞信号通路
标题:双膦酸盐反应生成的 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:EP-1566177-A1
优先权日:2004-02-23
标 题:The use of bisphosphonates for treating skin by stimulating of collagen synthesis
发明人：KIM JIN; YOOK JONG IN; KIM NAM HEE; RYU JU KYOUNG
权利人:TIGEN BIOTECH CO LTD
摘要:The present invention relates to a novel use of bisphosphonate, and morenparticularly to a composition for increasing collagen synthesis comprisingnbisphosphonate as an active ingredient, as well as the use thereof. The inventivencomposition comprising the bisphosphonate promotes collagen synthesis, and thus, whennit is applied to the skin, it reduces wrinkles of the skin and makes the skin elastic. Fornthis reason, the inventive composition will be useful as cosmetics for the prevention ornimprovement of skin aging or a wound-healing agent. Furthermore, the inventivencomposition can remarkably increase the collagen synthesis of fibroblasts in vitro , andnthus, can be effectively used in the production of products containing collagen.

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-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:EP-1404682-B1
优先权日:2001-06-29
标题:Method of inhibiting ptp 1b and/or t-cell ptp and/or other ptpases with an asp residue at position 48
发明人：HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL
权利人:NOVO NORDISK AS
摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al., Proc. Natl. Acad. Sci. USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1. This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.

专利号:US-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

专利号:US-2003064979-A1
优先权日:2001-06-29
标题 :Method of inhibiting PTP 1B and /or T-cell PTP and/or other PTPases with an Asp residue at position 48
发明人：HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL
摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al, Proc Natl Acad Sci USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1 n n n This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.