Top Picks: new discover of 3-(Bromomethyl)tetrahydrofuran

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The bromodomain containing proteins TRIM24 (tripartite motif containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are involved in the epigenetic regulation of gene expression and have been implicated in human cancer. Overexpression of TRIM24 correlates with poor patient prognosis, and BRPF1 is a scaffolding protein required for the assembly of histone acetyltransferase complexes, where the gene of MOZ (monocytic leukemia zinc finger protein) was first identified as a recurrent fusion partner in leukemia patients (8p11 chromosomal rearrangements). Here, we present the structure guided development of a series of N,N-dimethylbenzimidazolone bromodomain inhibitors through the iterative use of X-ray cocrystal structures. A unique binding mode enabled the design of a potent and selective inhibitor 8i (IACS-9571) with low nanomolar affinities for TRIM24 and BRPF1 (ITC Kd = 31 nM and ITC Kd = 14 nM, respectively). With its excellent cellular potency (EC50 = 50 nM) and favorable pharmacokinetic properties (F = 29%), 8i is a high-quality chemical probe for the evaluation of TRIM24 and/or BRPF1 bromodomain function in vitro and in vivo.

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Tetrahydrofuran – Wikipedia,
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The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications.

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Systematic SAR optimization of the GPR119 agonist lead 1, derived from an internal HTS campaign, led to compound 29. Compound 29 displays significantly improved in vitro activity and oral exposure, leading to GLP1 elevation in acutely dosed mice and reduced glucose excursion in an OGTT study in rats at doses ?10 mg/kg.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Computed Properties of C5H9BrO, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 165253-29-2, name is 3-(Bromomethyl)tetrahydrofuran. In an article,Which mentioned a new discovery about 165253-29-2

Compounds of the formula: wherein R1, Y, W, A and R2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.

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Tetrahydrofuran – Wikipedia,
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The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants

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This invention relates to substituted bicyclic dihydropyrimidinones of formula (1) and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Disclosed are compounds having the formula: (I) wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, R17, Rx, and Ry are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Chemistry is traditionally divided into organic and inorganic chemistry. category: Tetrahydrofurans, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 165253-29-2

NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACID DERIVATIVES AND THEIR USE AS GPR40 RECEPTOR AGONISTS

The present invention relates to compounds of general formula I, (I), wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

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Tetrahydrofuran – Wikipedia,
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N-ACRYLIMINO HETEROCYCLIC COMPOUNDS

The present invention relates to N-acrylimino compound of formula (I): wherein X is O or S, in particular O; Het is a 5-or 6-membered carbon-bound or nitrogen-bound heterocyclic ring, W1-W2-W3-W4 represents a carbon chain group connected to N and C=N, and thus forming a saturated, unsaturated, or partially unsaturated 5 or 6 membered nitrogen containing heterocycle, wherein W1, W2, W3 and W4 each individually represent CRvRw, R1, R 2 may be hydrogen, halogen, etc. R3 is selected from the group consisting of hydrogen, halogen, CN, C1-C6-alkyl, etc. R4 is selected from the group consisting of hydrogen, halogen, CN, C1-C10-alkyl, etc. R5 is selected from the group consisting of hydrogen CN, C1-C10-alkyl, C2-C10-alkenyl C3-C8-cycloalkyl, S(O)nNR9aR9b, O-NR9aR9b, NR9aR9b, NR9a NR9aR9b, NR9aC(=O)R7a, NR9aC(=S)R7a, NR9aC(=O)NR9aR9b, NR9aC(=S)NR9aR9b, C(=O)OR8, C(=O)NR9aR9b, C(=S)NR9aR9b, C(=O)R7a, C(=S)R7a, a moitey Q-phenyl, where the phenyl ring is optionally substituted with 1, 2, 3, 4 or 5 identical or different substituents R10, and a moiety Q-HetNo. where HetNo. represents a 3- to 10- membered saturated, partly saturated or unsaturated aromatic heterocyclic ring. The invention also relates to the use of the N-acrylimino heterocyclic compounds, their stereoisomers, their tautomers and their salts,for combating invertebrate pests. Furthermore the invention relates also to methods of combating invertebrate pests, which comprises applying such compounds.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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165253-29-2, Name is 3-(Bromomethyl)tetrahydrofuran, belongs to Tetrahydrofurans compound, is a common compound. SDS of cas: 165253-29-2In an article, once mentioned the new application about 165253-29-2.

Evaluation of novel TGR5 agonist in combination with Sitagliptin for possible treatment of type 2 diabetes

TGR5 is a member of G protein-coupled receptor (GPCR) superfamily, a promising molecular target for metabolic diseases. Activation of TGR5 promotes secretion of glucagon-like peptide-1 (GLP-1), which activates insulin secretion. A series of 2-thio-imidazole derivatives have been identified as novel, potent and orally efficacious TGR5 agonists. Compound 4d, a novel TGR5 agonist, in combination with Sitagliptin, a DPP-4 inhibitor, has demonstrated an adequate GLP-1 secretion and glucose lowering effect in animal models, suggesting a potential clinical option in treatment of type-2 diabetes.

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Tetrahydrofuran – Wikipedia,
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