Category: Thiomorpholine

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Discovery of a potent parenterally administered factor XIa inhibitor with hydroxyquinolin-2(1H)-one as the P2? moiety

Structure-activity relationship optimization of phenylalanine P1? and P2? regions with a phenylimidazole core resulted in a series of potent FXIa inhibitors. Introducing 4-hydroxyquinolin-2-one as the P2? group enhanced FXIa affinity and metabolic stability. Incorporation of an N-methyl piperazine amide group to replace the phenylalanine improved both FXIa potency and aqueous solubility. Combination of the optimization led to the discovery of FXIa inhibitor 13 with a FXIa Ki of 0.04 nM and an aPTT EC2x of 1.0 muM. Dose-dependent efficacy (EC50 of 0.53 muM) was achieved in the rabbit ECAT model with minimal bleeding time prolongation.

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 39093-93-1, molcular formula is C4H9NO2S, introducing its new discovery. , 39093-93-1

NOVEL COMPOUNDS

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity

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128453-98-5, Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 128453-98-5

NOVEL COMPOUNDS

This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted piperidines, according to Formula I. Specifically, the invention is directed to compounds according to Formula (I). Wherein R1 is optionally substituted aryl; X is CH2, S, or SO2, and n = 1 or 2.

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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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In an article, published in an article,authors is Battula, Kumara Swamy, once mentioned the application of 39093-93-1, Name is Thiomorpholine 1,1-dioxide,molecular formula is C4H9NO2S, is a conventional compound. this article was the specific content is as follows. 39093-93-1

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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39093-93-1, Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 39093-93-1

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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39093-93-1, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 39093-93-1, name is Thiomorpholine 1,1-dioxide, introducing its new discovery.

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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39093-93-1, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 39093-93-1, Name is Thiomorpholine 1,1-dioxide,introducing its new discovery.

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,
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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 39093-93-1, molcular formula is C4H9NO2S, introducing its new discovery. , 39093-93-1

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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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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