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Direct Amination of alpha-Hydroxy Amides

A TiCl4-mediated reaction for the direct amination of alpha-hydroxy amides has been developed. This simple, general, additive/base/ligand-free reaction is mediated by economical TiCl4. The reaction runs under mild conditions. This highly efficient C?N bond formation protocol is valid for diverse amines, including primary, secondary and heterocyclic amines, and even a primary amide and indole.

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Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model

Cortisol and the glucocorticoid receptor signaling pathway have been implicated in the development of diabetes and obesity. The reduction of cortisone to cortisol is catalyzed by 11beta-hydroxysteroid dehydrogenase type I (11beta-HSD1). 2,4-Disubsituted benzenesulfonamides were identified as potent inhibitors of both the human and mouse enzymes. The lead compounds displayed good pharmacokinetics and ex vivo inhibition of the target in mice. Cocrystal structures of compounds 1 and 20 bound to human 11alpha-HSD1 were obtained. Compound 20 was found to achieve high concentrations in target tissues, resulting in 95% inhibition in the ex vivo assay when dosed with a food mix (0.5 mg of drug per g of food) after 4 days. Compound 20 was efficacious in a mouse diet-induced obesity model and significantly reduced fed glucose and fasted insulin levels. Our findings suggest that 11beta-HSD1 inhibition may be a valid target for the treatment of diabetes.

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PHARMACEUTICAL COMPOSITION COMPRISING A BENZODIAZEPINE DERIVATIVE AND A INHIBITOR OF THE RSV FUSION PROTEIN

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.

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Extended knowledge of 128453-98-5

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! Read on for other articles about 891785-30-1!, 128453-98-5

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Ernouf, Guillaume and a compound is mentioned, 128453-98-5, 4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, introducing its new discovery. 128453-98-5

Photochemical Strain-Release-Driven Cyclobutylation of C(sp3)-Centered Radicals

A new photoredox-catalyzed decarboxylative radical addition approach to functionalized cyclobutanes is described. The reaction involves an unprecedented formal Giese-type addition of C(sp3)-centered radicals to highly strained bicyclo[1.1.0]butanes. The mild photoredox conditions, which make use of a readily available and bench stable phenyl sulfonyl bicyclo[1.1.0]butane, proved to be amenable to a diverse range of alpha-amino and alpha-oxy carboxylic acids, providing a concise route to 1,3-disubstituted cyclobutanes. Furthermore, kinetic studies and DFT calculations unveiled mechanistic details on bicyclo[1.1.0]butane reactivity relative to the corresponding olefin system.

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Thiomorpholine – Wikipedia,
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CRYSTALLINE FILGOTINIB SULFONIC ACID ADDITION SALTS

The present invention relates to filgotinib sulfonic acid addition salts, their polymorphs, a method of preparing the same as well as a pharmaceutical composition comprising the same.

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Thiomorpholine – Wikipedia,
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alpha-Bromodiazoacetamides – a new class of diazo compounds for catalyst-free, ambient temperature intramolecular C-H insertion reactions

In this work, we introduce a new class of halodiazocarbonyl compounds, alpha-halodiazoacetamides, which through a metal-free, ambient-temperature thermolysis perform intramolecular C-H insertions to produce alpha-halo-beta-lactams. When carried out with alpha-bromodiazoacetamides bearing cyclic side chains, the thermolysis reaction affords bicyclic alpha-halo-beta-lactams, in some cases in excellent yields, depending on the ring size and substitution pattern of the cyclic amide side chains.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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SPIROHEPTANE SALICYLAMIDES AND RELATED COMPOUNDS AS INHIBITORS OF ROCK

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

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PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING OR PREVENTING A RESPIRATORY SYNCYTIAL VIRUS INFECTION

Pyrimidine derivatives of formula (I) wherein: Z is a direct bond or -(CH2)n- wherein n is 1 or 2; one of X and Y is N, CH or CF, and the other of X and Y is CH; one of R1 and R2 is selected from -NHR, -NR2, -OR, -SR, -S(O)R, -S(O)2R and a group of the following formula (A) and the other of R1 and R2 is selected from -NHR’, -OH, -OR’ and a group of the above formula (A); R is unsubstituted C1-C6 alkyl; R’ is a group selected from C1-C6 alkyl, 5- to 12-membered aryl and C3-C6 cycloalkyl, which group is unsubstituted or substituted; W is -(CH2)m-, -CH2-O-CH2-, -CH2-S-CH2- or -CH2-S(O)2-CH2-; p is 1, q is an integer of 1 – 6 and V is N; or p is 1, q is 0 and V is CH; or p is 0, q is 0 and V is N; r is 0 or 1; and R3 is -(CH2)s-NH2 or -(CH2)s-OH wherein s is 0 or an integer of 1 to 4; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

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Thiomorpholine – Wikipedia,
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Synthesis and Biological Evaluation of Novel Thiomorpholine 1,1-Dioxide Derived 1,2,3-Triazole Hybrids as Potential Anticancer Agents

In this report, we describe the synthesis and biological evaluation of a new series of (4-((1-(aryl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)(1,1-dioxidothiomorpholino)methanone derivatives (6 a-6 n). All the new derivatives were well analyzed by 1H NMR, 13C NMR, FTIR, mass spectral and elemental data. The synthesized compounds were screened for in vitro anticancer activity against three cancer cell lines (MCF-7, HeLa, and HEK293) and compared with standard drug cisplatin. Three (6 b, 6 g and 6 i) out of fourteen derivatives exhibited potent anticancer activity against MCF-7, HeLa, and HEK293. Two (6 b and 6 g) potent hybrids were screened for in vivo studies against EAC bearing mice and found to possess potential anticancer activity.

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ACYCLIC CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS

The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem