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JAK kinase inhibitors and uses thereof (by machine translation)

The invention discloses a having the following general formula (I) compound. The invention also disclosed comprising this compound JAK kinase inhibitor and the compounds in the preparation of the treatment in the JAK related diseases of the application. JAK kinase inhibitors of the present invention, can inhibit the signal transduction of the involved in various JAK1, JAK2, JAK3 and TYK2 kinase biological activity, can effectively clinical treatment of various inflammatory diseases and JAK-mediated signal transduction by the driving of various diseases, very broad application prospects. . (by machine translation)

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Theoretical and experimental studies of cycloconjugation involving second-row elements

In a method proposed to investigate conjugative interactions between second-row elements (S, P) amd a pi-electron system, barriers to amide rotation have been measured using NMR line-shape methods, for N-acetyl-4-X(hetero)-1,4-dihydropyridines (X = SO2,7; P(O)OCH3,13; C(CH3)2, 6 (reference)) as well as the dihydro (8a) and tetrahydro (9) derivatives, respectively, of 7. It is suggested that such interactions would stabilize the transition states for amide rotation by cycloconjugation but not the planar equilibrium states, compressing the barriers relative to reference 6. In fact, amide barriers in 7,13, and N-acetylpyrrole are substantially (>6 kcal) less than in 6, 8ab, and 9, all ca. 17 kcal, in all of which saturated centers interrupt possible cycloconjugation. These conclusions are supported by the results of ab initio calculations at the Hartree-Fock level with the 3-21G(*) basis set.

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Thiomorpholine | C4H9NS – PubChem

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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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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 39093-93-1 is helpful to your research. Safety of Thiomorpholine 1,1-dioxide

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TETRACYCLIC COMPOUND

A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).

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POSITIVE ALLOSTERIC MODULATORS OF MGLUR2

The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia

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Benzoxazolamines and Benzothiazolamines: Potent, Enantioselective Inhibitors of Leukotriene Biosynthesis with a Novel Mechanism of Action

A series of benzoxazolamine and benzothiazolamine analogs that inhibit leukotriene (LT) biosynthesis are described.The initial lead, (S)-N-(benzothiazol-2-yl)phenylalanine ethyl ester (5a), was discovered in a screening program for inhibition of Ca-ionophore-A23187-induced LTB4 release in human polymorphonuclear leukocytes (IC50 0.23 muM).Through structural modification, it was determined that hydrophobic substituents in the 5-position and replacement of the phenyl ring of phenylalanine with a cyclohexyl group greatly enhance potency.Several ester bioisosteres that retain potency and enantiomeric selectivity are described.Lead optimization culminated in (S)-N-<2-cyclohexyl-1-(2-pyridinyl)ethyl>-5-methyl-2-benzoxazolamine (43b), IC50 0.001 muM.The compounds described are not inhibitors of 5-lipoxygenase but, rather, act at the level of arachidonic acid release.

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Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.C4H9NO2S, introducing its new discovery. , Application In Synthesis of Thiomorpholine 1,1-dioxide

Structure-based design of orally bioavailable 1 h -Pyrrolo[3,2- C ]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1)

The protein kinase MPS1 is a crucial component of the spindle assembly checkpoint signal and is aberrantly overexpressed in many human cancers. MPS1 is one of the top 25 genes overexpressed in tumors with chromosomal instability and aneuploidy. PTEN-deficient breast tumor cells are particularly dependent upon MPS1 for their survival, making it a target of significant interest in oncology. We report the discovery and optimization of potent and selective MPS1 inhibitors based on the 1H-pyrrolo[3,2-c]pyridine scaffold, guided by structure-based design and cellular characterization of MPS1 inhibition, leading to 65 (CCT251455). This potent and selective chemical tool stabilizes an inactive conformation of MPS1 with the activation loop ordered in a manner incompatible with ATP and substrate-peptide binding; it displays a favorable oral pharmacokinetic profile, shows dose-dependent inhibition of MPS1 in an HCT116 human tumor xenograft model, and is an attractive tool compound to elucidate further the therapeutic potential of MPS1 inhibition.

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METHODS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS

The present invention discloses compounds according to Formula (I): or a pharmaceutically acceptable salt thereof, or a solvate or the salt of a solvate thereof, pharmaceutical compositions comprising the same, and methods of treatment using the same, for use in the prophylaxis and/or treatment of cardiovascular disorders and/or dyslipidemia, by administering the compound according to Formula (I).

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Parallel synthesis and structure-activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors

Parallel synthesis and iterative optimization led to the discovery of a series of potent and specific factor Xa inhibitors demonstrating excellent in vitro activity with promising pharmacokinetics.

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CYCLOHEXYLPYRAZOLE-LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1

The present invention discloses novel compounds of Formula (I): having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compound

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem