Day: March 5, 2021

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Benzothiazole derivatives with activity as adenosine receptor ligands

The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.

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Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR

Anthranilamide-based benzamidine compound 4 and its N-substituted analogs were designed and examined as factor Xa inhibitors using substituted benzamidines as unconventional S4 binding element. A group of N,N-dialkylbenzamidines (11, 17 and 24) have been discovered as potent factor Xa inhibitors with strong anticoagulant activity and promising oral PK profiles.

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Application of 39093-93-1, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. Application of 39093-93-1, Name is Thiomorpholine 1,1-dioxide, molecular formula is C4H9NO2S. In a Article, authors is Nagarajan, K.£¬once mentioned of Application of 39093-93-1

Nitroimidazoles: Part VII – 1-(1-Alkyl-5-nitroimidazol-2-yl)-aza(diaza,oxaza)cycloalkanes

Reaction of 1-methyl-2-methylsulphonyl-5-nitroimidazole (2) with pyrrolidine, piperidine and morpholine affords the amines (3a-c)(=9a-c) respectively in low yields, the reaction failing with other bases tried.Analogues (9d-t) have been obtained more readily by nitrating imidazoles (8), which are synthesized from thioureas (5) of cyclic secondary amines through the S-methylisothioureas (6) and the guanidinoacetals (7).

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SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1

The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

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COMPOSITIONS AND METHODS FOR MODULATING THE WNT SIGNALING PATHWAY

The present invention relates to compositions and methods for modulating the Wnt signaling pathway, using compounds having Formula (1) and (3): wherein A, B, Y and Z all represent rings, and R 1 , R 2 , R 3 are as defined herein.

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3-(Carboxymethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives

The invention relates to 3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

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BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS

The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.

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FLUOROPHENYL BICYCLIC HETEROARYL COMPOUNDS

The present invention provides a compound of formula (I); a method for manufacturing the compounds of the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition

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INDAZOLE-CARBOXAMIDE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS

The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

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Synthetic Route of 39093-93-1, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, Synthetic Route of 39093-93-1, molcular formula is C4H9NO2S, introducing its new discovery.

Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists

Using structure-based drug design principles, we identified opportunities to reduce the lipophilicity of our tertiary sulfonamide RORc inverse agonists. The new analogs possessed improved RORc cellular potencies with >77-fold selectivity for RORc over other nuclear receptors in our cell assay suite. The reduction in lipophilicity also led to an increased plasma-protein unbound fraction and improvements in cellular permeability and aqueous solubility.

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Thiomorpholine – Wikipedia,
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