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3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS

The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

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Tetrahydrofuran – Wikipedia,
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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 22929-52-8, and how the biochemistry of the body works.COA of Formula: C4H6O2

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Novel spirooxaphosphirane complexes

Reaction of a transient Li/Cl phosphinidenoid pentacarbonyltungsten complex 3 (R = C5Me5) with 3-oxetanone, dihydro-3(2H)-furanone, and dihydro-4H-pyran-4-one led to the novel spirooxaphosphirane complexes 5, 7a,b, and 9a,b having an additional oxygen atom in the ring system, while delta-valerolactone furnished selectively the P,C-cage complex 10. All complexes have been characterized by heteronuclear NMR and mass spectrometry and by single-crystal X-ray analysis in the case of 7a and 9a.

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Tetrahydrofuran – Wikipedia,
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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, 22929-52-8, name is Dihydrofuran-3(2H)-one, introducing its new discovery. Product Details of 22929-52-8

BENZOTHIOPHENE SULFONAMIDES AND OTHER COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN

The present invention relates to benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

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Tetrahydrofuran – Wikipedia,
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Inhibiting growth hormone secretion with 5,5-substituted hydantoin derivatives

The compounds are free hydantoin derivatives of the formula: STR1 wherein X is a divalent radical consisting of from 2 to 5 linked units; one unit being –O–, and from one to 4 hydrocarbon units, independently, having the structure in which R is alkyl having from 1 to 6 carbon atoms and being free of branching on the alpha-carbon atoms; provided that no more than 2 units are of type b; or a pharmaceutically acceptable salt form thereof with a suitable cation; e.g. 7-oxa-1,3-diazaspiro[4.4]nonane-2,4-dione, and are useful as pharmaceuticals.

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CINNOLINE COMPOUNDS AND FOR THE TREATMENT OF HPK1-DEPENDENT DISORDERS SUCH AS CANCER

Cinnoline compounds of formula (I), variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the cinnoline compounds.

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Tetrahydrofuran – Wikipedia,
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SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C

This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.

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Tetrahydrofuran – Wikipedia,
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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, 22929-52-8, name is Dihydrofuran-3(2H)-one, introducing its new discovery. Product Details of 22929-52-8

SPIROCYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS

Disclosed are Spirocyclic Heterocycle Compounds of Formula (I) and pharmaceutically acceptable salts thereof, where A, B, X, Y, R1, R2 and R11 are as defined herein. Composition comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject are also disclosed.

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Tetrahydrofuran – Wikipedia,
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Synthesis of new (3-aminopyrrolidin-3-yl)phosphonic acid – A cucurbitine analogue – and (3-aminotetrahydrothiophen-3-yl)phosphonic acid via phosphite addition to heterocyclic hydrazones

Hydrazones were prepared by condensation of carbocyclic and heterocyclic ketones with benzoyl- and tosylhydrazines. These hydrazones underwent nucleophilic addition with phosphite to provide efficiently (3- hydrazinopyrrolidin-3-yl)-, (3-hydrazinotetrahydrothiophen-3-yl)-, (3-hydrazinotetrahydrofuran-3-yl)-, and (1-hydrazinocyclopentyl)phosphonates. Cleavage of the hydrazine N-N bonds followed by acidic hydrolysis of the phosphonate functions of the (3-aminoheterocyclopentyl)phosphonates gave the new (3-aminopyrrolidin-3-yl)- and (3-aminotetrahydrothiophen-3-yl)phosphonic acids. This synthesis was achieved in a four-step sequence from the appropriate ketones. Georg Thieme Verlag Stuttgart.

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Tetrahydrofuran – Wikipedia,
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Far-infrared spectra and two-dimensional potential energy surfaces for the out-of-plane ring vibrations of tetrahydrofuran-3-one in its S0 and S1(n,pi*) electronic states

The far-infrared spectra of tetrahydrofuran-3-one show ring-bending (100-120 cm-1), ring-twisting (227-237 cm-1), difference (115-137 cm-1), and overtone (200-225 cm-1) bands. Calculations for the two-dimensional potential energy surface governing the twisting and bending motions were carried out. The minima of the potential surface correspond to twisted conformations with twist angles of approximately ¡À35. The barrier to planarity is in the 1500 to 2000 cm-1 range. No saddle points corresponding to bent structures are present for the surface. A potential energy surface for the S1(n,pi*) excited state, based on previous fluorescence excitation data, was also calculated. The latter has an assumed barrier to planarity of 1400 cm-1 and a barrier to pseudorotation of 880 cm-1.

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Serotoninergic properties of new conformationally restricted benzamides

A new series of benzamides derived from metoclopramide have been synthesized, in which the vicinal carbon of the basic nitrogen atom of the ethyl chain is situated on the C3, C4, C5 and C6 rings. The diamino derivatives were prepared through Strecker’s reaction from the corresponding ketones except for the cyclopropyl derivatives where 1-ethoxy-1-trimethylsiloxy cyclopropane was used as the starting material. The benzamides were prepared using the mixed anhydride method. They were tested in binding assays for D2, 5-HT3 and 5-HT4 receptors. The results show a marked increase in the selectivity and potency of these derivatives for 5-HT3 receptors with regard to metoclopramide (compound 1d: 5-HT3 K(i) = 9.03 nM; 5-HT4 K(i) > 5000; D2 K(i) > 5000). The influences of steric hindrance and hydrophobic properties on the affinity of benzamide derivatives for 5-HT3 receptors were also emphasized by these data. The X-ray crystal structure of compound 1d was compared with that of the minimal energy conformer of BRL 24682, a reference 5-HT3 receptor antagonist benzamide, determined using the Random Search program. Superimposition of the two structures showed a suitable fit between the pharmacophore groups previously determined to be important for 5-HT3 receptor antagonists. On the other hand, the hydrophobic parts of the basic moieties had different spatial occupancies.

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