31995-08-1

Upstream product

• 107-25-5 methoxyethene 
• 107-19-7 propargyl alcohol 
• 109-86-4 2-methoxy-ethanol 
• 624-65-7 2-propynyl chloride 
• 6482-24-2 2-Bromoethyl methyl ether 
• 106-96-7 propargyl bromide 

Downstream Products

• 138166-51-5 [(Z)-3-(2-Methoxy-ethoxy)-propenylsulfanyl]-benzene 
• 138166-52-6 3<2-methoxymethyl>benzo-thiophene 
• 138166-50-4 C₁₈H₂₀O₂S₂ 
• 144252-25-5 3-methoxyethoxy-1-phenylthio-2-phenylprop-1-ene 
• 1189528-64-0 8-(4-iodophenyl)-1,7-dimethyl-3,5-bis(4-methoxystyryl)-4,4-bis(2,5-dioxaoct-7-ynyl)-4-bora-3a,4a-diaza-s-indacene 
• 1189528-65-1 8-(4-trifluoromethylphenyl)-1,7-dimethyl-3,5-bis(4-methoxystyryl)-4,4-bis(2,5-dioxaoct-7-ynyl)-4-bora-3a,4a-diaza-s-indacene 
• 1228437-61-3 C₄₃H₅₀BIN₂O₇ 
• 1228437-62-4 C₅₅H₆₄BIN₂O₁₀ 
• 1257341-79-9 C₄₅H₄₂BI₃N₂O₄ 
• 1257341-80-2 C₄₅H₄₂BBr₂IN₂O₄ 
• 1257341-76-6 C₅₆H₅₈BBr₂N₃O₅ 
• 1221262-42-5 10-(4-iodophenyl)-5,5-bis(3-(2-methoxyethoxy)prop-1-yn-1-yl)-1,3,7,9-tetramethyl-5H-dipyrrolo[1,2-c:2',1'-f][1,3,2]diazaborinin-4-ium-5-uide 
• 1258828-02-2 C₄₉H₅₄BIN₄O₄ 
• 1263506-68-8 [(C(C₄HN(CH₃)CHCHC₆H₄C₂CH₂N(CH₃)2)2C₆H₄I)B(C₂CH₂OC₂H₄OCH₃)2] 

Relevant academic research and scientific papers

NEUROACTIVE STEROIDS AND COMPOSITIONS AND METHODS THEREOF

The invention provides novel neuroactive steroids and pharmaceutical compositions thereof, as well as methods of their preparation and use, in therapy of various diseases and conditions, for example, various neurological or brain diseases.

DIMERIC IMMUNO-MODULATORY COMPOUNDS AGAINST CEREBLON-BASED MECHANISMS

Disclosed are small molecules against cereblon to enhance effector T cell function. Methods of making these molecules and methods of using them to treat various disease states are also disclosed.

Investigation of catalyst-transfer condensation polymerization for the synthesis of n-type π-conjugated polymer, poly(2-dioxaalkylpyridine-3,6-diyl)

Kumada-Tamao coupling polymerization of 6-bromo-3-chloromagnesio-2-(3-(2- methoxyethoxy)propyl)pyridine 1 with a Ni catalyst and Suzuki-Miyaura coupling polymerization of boronic ester monomer 2, which has the same substituted pyridine structure, with tBu3PPd(o-tolyl)Br were investigated for the synthesis of a well-defined n-type π-conjugated polymer. We first carried out a model reaction of 2,5-dibromopyridine with 0.5 equivalent of phenylmagnesium chloride in the presence of Ni(dppp)Cl2 and then observed exclusive formation of 2,5-diphenylpyridine, indicating that successive coupling reaction took place via intramolecular transfer of Ni(0) catalyst on the pyridine ring. Then, we examined the Kumada-Tamao polymerization of 1 and found that it proceeded homogeneously to afford soluble, regioregular head-to-tail poly(pyridine-2,5-diyl), poly(3-(2-(2-(methoxyethoxy)propyl) pyridine) (PMEPPy). However, the molecular weight distribution of the polymers obtained with several Ni and Pd catalysts was very broad, and the matrix-assisted laser desorption ionization time-of-flight mass spectra showed that the polymer had Br/Br and Br/H end groups, implying that the catalyst-transfer polymerization is accompanied with disproportionation. Suzuki-Miyaura polymerization of 2 with tBu3PPd(o-tolyl)Br also afforded PMEPPy with a broad molecular weight distribution, and the tolyl/tolyl-ended polymer was a major product, again indicating the occurrence of disproportionation. Copyright

SPHINGOSINE-1 -PHOSPHATE RECEPTOR AGONIST AND ANTAGONIST COMPOUNDS

The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.

Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors

A homologous series of polyethylene glycol (PEG) monomethyl ethers were conjugated with three ligand series for nicotinic acetylcholine receptors. Conjugates of acetylaminocholine, the cyclic analog 1-acetyl-4,4-dimethylpiperazinium, and pyridyl ether A-84543 were prepared. Each series was found to retain significant affinity at nicotinic receptors in rat cerebral cortex with tethers of up to six PEG units. Such compounds are hydrophilic ligands which may serve as models for fluorescent/affinity probes and multivalent ligands for nAChR.

Substituted 3-cyanoquinolines as protein tyrosine kinases inhibitors

This invention provides compounds of formula 1 wherein R1, G1, G2, R4, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof, which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.

1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel

The synthesis of a novel series of 1,4-dihydroindeno[1,2-c]pyrazoles with acetylene-type side chains is described. Optimization of those compounds as KDR kinase inhibitors identified 8, which displayed an oral activity in an estradiol-induced murine uterine edema model (ED50 = 3 mg/kg) superior to Sutent (ED50 = 9 mg/kg) and showed potent antitumor efficacy in an MX-1 human breast carcinoma xenograft tumor growth model (tumor growth inhibition = 90% at 25 mg/kg·day po). The compound was docked into a homology model of the homo-tetrameric pore domain of the hERG potassium channel to identify strategies to improve its cardiac safety profile. Systematic interruption of key binding interactions between 8 and Phe656, Tyr652, and Ser624 yielded 90, which only showed an IC50 of 11.6 μM in the hERG patch clamp assay. The selectivity profile for 8 and 90 revealed that both compounds are multitargeted receptor tyrosine kinase inhibitors with low nanomolar potencies against the members of the VEGFR and PDGFR kinase subfamilies.

SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS TYROSINE KINASE INHIBITORS

This invention provides compounds of formula (1) wherein X is C3-7 cycloalkyl, pyridinyl, pyrimidinyl or phenyl ring optionally substituted as described in claim 1, R1, R3 and R4 are chosen from the groups listed in claim 1. R2 is chosen from various unsaturated acyl groups listed in claim 1, with certain compounds being disclaimed. Use as tyrosine kinase inhibitors for the treatment of cancer and certain kidney diseases such as polycystic kidney disease.

SUBSTITUTED 3-CYANOQUINOLINES AS PROTEIN TYROSINE KINASES INHIBITORS

This invention provides compounds of formula (1) wherein R1, G1, G2, R4, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof, which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.

6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity

A series of new 6-substituted-4-(3-bromophenylamino)quinazoline derivatives that may function as irreversible inhibitors of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases have been prepared. These inhibitors have, at the C-6 position, butynamide, crotonamide, and methacrylamide Michael acceptors bearing water-solublilizing substituents. These compounds were prepared by acylation of 6-amino-4-(3-bromophenylamino)quinazoline with unsaturated acid chlorides or mixed anhydrides. We show that attaching a basic functional group onto the Michael acceptor results in greater reactivity, due to intramolecular catalysis of the Michael addition and/or an inductive effect of the protonated basic group. This, along with improved water solubility, results in compounds with enhanced biological properties. We present molecular modeling and experimental evidence that these inhibitors interact covalently with the target enzymes. One compound, 16a, was shown to have excellent oral activity in a human epidermoid carcinoma (A431) xenograft model in nude mice.