92664-38-5

Upstream product

• 109-01-3 1-methyl-piperazine 
• 79-10-7 acrylic acid 
• 814-68-6 acryloyl chloride 

Relevant academic research and scientific papers

Method for catalytically synthesizing acrylamide compound by MOFs-derived zirconium-based ternary oxide solid acid

The invention provides a catalytic synthesis of acrylamide compounds with zirconium-based ternary oxide solid acid as a catalyst, and the low-temperature activity is good. In the synthesis process, the acid is small, the reaction conditions are mild and controllable, the byproducts are few, the reaction yield is effectively improved, the purity is high, the quality is good, and the method is suitable for large-scale production.

Functional monomer used for synthesizing polymer oil displacement agent and preparation method of functional monomer

The invention relates to a functional monomer used for synthesizing a polymer oil displacement agent and a preparation method of the functional monomer. The functional monomer is characterized by comprising the following structural general formula (please see the specifications for the formula), wherein R1 is -H or -CH3, and R2 is -CH3 or -CH2CH3 or -CH2CH2CH3 or -CH(CH3)2. The preparation methodof the functional monomer comprises the steps that (1) a certain amount of dichloromethane and acyl chloride are evenly mixed under stirring, the temperature of a mixed system is controlled to be 0-10DEG C, a certain amount of piperazine derivatives is added into the mixed system dropwise, the temperature of the system is increased to be 20-40 DEG C, and a reaction is continued for 1-6 h; and (2)after the reaction is completed, the pH value of reaction liquid is adjusted to be 8-14, then dichloromethane with the volume being 2-5 times that of the reaction liquid is added for extraction, organic phases are collected, drying and filtering are conducted, an organic solvent is removed at the temperature of 40-50 DEG C, a product is obtained, and the production rate is calculated. According to the method, through strict control and reasonable improvement of technological parameters, the production rate of the functional monomer can be increased, the purity of the functional monomer can beimproved, the polymerization success rate of the functional monomer serving as a polymerization monomer is increased, and the high production rate, purity and monomer polymerization rate can furtherbe maintained especially under the situation of mass production.

COVALENT TARGETING OF E3 LIGASES

Disclosed herein, inter alia, are compositions and methods for targeting E3 ligases. In an aspect is a targeted protein degrader including 1) a targeted protein binder and 2) an E3 Ubiquitin ligase binder, wherein the E3 Ubiquitin ligase is human RNF4 or human RNF114. In an aspect is provided a pharmaceutical composition including a compound as described herein, including embodiments, and a pharmaceutically acceptable excipient.

A Potent Isoprenylcysteine Carboxylmethyltransferase (ICMT) Inhibitor Improves Survival in Ras-Driven Acute Myeloid Leukemia

Blockade of Ras activity by inhibiting its post-translational methylation catalyzed by isoprenylcysteine carboxylmethyltransferase (ICMT) has been suggested as a promising antitumor strategy. However, the paucity of inhibitors has precluded the clinical validation of this approach. In this work we report a potent ICMT inhibitor, compound 3 [UCM-1336, IC50 = 2 μM], which is selective against the other enzymes involved in the post-translational modifications of Ras. Compound 3 significantly impairs the membrane association of the four Ras isoforms, leading to a decrease of Ras activity and to inhibition of Ras downstream signaling pathways. In addition, it induces cell death in a variety of Ras-mutated tumor cell lines and increases survival in an in vivo model of acute myeloid leukemia. Because ICMT inhibition impairs the activity of the four Ras isoforms regardless of its activating mutation, compound 3 surmounts many of the common limitations of available Ras inhibitors described so far. In addition, these results validate ICMT as a valuable target for the treatment of Ras-driven tumors.

Ink, ink cartridge, ink jet recording device, ink jet ink printed matter, compound, and composition

Ink contains at least one of a compound represented by the following chemical formula 1, a compound represented by chemical formula 2, a compound represented by chemical formula 3, or a compound represented by chemical formula 4.

TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS

Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N-H, N-(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.

INDAZOLYL, BENZIMIDAZOLYL, BENZOTRIAZOLYL SUBSTITUTED INDOLMONE DERIVATIVES AS KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER

The present invention is directed to a compound is represented by Structural Formula (A):or a pharmaceutically acceptable salt therof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.

Synthesis and preliminary evaluation of novel analogues of quindolines as potential stabilisers of telomeric G-quadruplex DNA

Telomeric DNA is a potential selective target for cancer therapy since the tumour-associated enzyme telomerase regulates telomere maintenance in most cancer cells. The 3′ single-stranded ends of telomeric DNA can be folded into quadruplex structures by appropriate small molecules. We describe the preparation of a new class of 2,7-disubstituted 10H-indolo[3,2-b]quinolines with enhanced selectivity for the stabilisation of quadruplex DNA compared to duplex DNA, and also the preparation of a key intermediate for the synthesis of trisubstituted quindolines.

ANTIPERSPIRANT COMPOSITIONS

An antiperspirant composition comprising a carrier substance and a water-soluble or water-dispersible thiolated polymer.