Day: March 4, 2021

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GPR40 AGONISTS IN ANTI-DIABETIC DRUG COMBINATIONS

Disclosed are compositions comprising (a) a GPR40 agonist and (b) an SGLT2 inhibitor, and methods for treating of disorders that are affected by the modulation of the GPR40 receptor and SGLT2 transporter. Such GPR40 compounds are represented by Formula (I) as follows: wherein ring W, R1, R2, R3, R5, R6, A, and Z, are defined herein.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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

FILGOTINIB: Tyrosine-protein kinase JAK1 inhibitor, treatment of rheumatoid arthritis, treatment of crohn’s disease

Rheumatoid arthritis (RA), a chronic autoimmune inflammatory disease, is associated with pain, progressive disability, systemic comorbidities and early death. Filgotinib (GLPG-0634), a new selective tyrosine-protein kinase (JAK1) inhibitor, is currently in phase II clinical trials for the treatment of RA and Crohn’s disease. In in vitro biochemical and cellular and human whole blood assays, filgotinib showed selective potency, inhibiting JAK1 in the nanomolar range. In models of RA and Crohn’s disease in vivo in rodents it showed antiinflammatory efficacy. In a proof-of-concept trial in 36 RA patients with insufficient response to methotrexate, at doses of 100 mg b.i.d. and 200 mg once daily 91.7% and 75% of patients reached ACR20 scores, respectively. The pooled values for ACR20, DAS28 and C-reactive protein (CRP) change versus placebo at week 4 reached statistical significance. Of note, typical side effects of non-selective JAK inhibitors, i.e., anemia and increases in LDL cholesterol, liver enzymes and creatinine, were not detected.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. SDS of cas: 39093-93-1, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 39093-93-1, name is Thiomorpholine 1,1-dioxide. In an article£¬Which mentioned a new discovery about 39093-93-1

PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS. (I)

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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A BRD4 inhibitors (by machine translation)

The invention of the formula I indicated by the BRD4 inhibitors, which belongs to the technical field of pharmaceutical compounds. The present invention provides the compounds of prostate cancer cell proliferation has very good inhibition action, the compounds of the invention can be used for the preparation of anti-tumor, autoimmune or inflammatory disease, virus infection, especially anti-prostate cancer drug. (by machine translation)

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4)

Inhibition of hepatitis B virus (HBV) capsid assembly is a novel strategy for the development of chronic hepatitis B (CHB) therapeutics. Herein we described our lead optimization studies including the synthesis, molecular docking studies and structure-activity relationship (SAR) studies of a series of novel heteroaryldihydropyrimidine (HAP) inhibitors of HBV capsid assembly inhibitors, and the discovery of a potent inhibitor of HBV capsid assembly of GLS4 (ethyl 4-[2-bromo-4-fluorophenyl]-6-[morpholino-methyl]-2-[2-thiazolyl]-1,4-dihydro-pyrimidine-5-carboxylate) which is now in clinical phase 2. GLS4 demonstrated potent inhibitory activities in HBV HepG2.2.15 cell assay with an EC50value of 1 nM, and it also exhibited high potency against various drug-resistant HBV viral strains with EC50values in the range of 10?20 nM, more potent than the typical HBV polymerase inhibitors such as lamivudine, telbivudine, and entecavir. Pharmacokinetic profiles of GLS4 were favorable and safety evaluation including acute toxicity and repeated toxicity study indicated that GLS4 was safe enough to support clinical experiments in human.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms

JAK2 kinase inhibitors are a promising new class of agents for the treatment of myeloproliferative neoplasms and have potential for the treatment of other diseases possessing a deregulated JAK2-STAT pathway. X-ray structure and ADME guided refinement of C-4 heterocycles to address metabolic liability present in dialkylthiazole 1 led to the discovery of a clinical candidate, BMS-911543 (11), with excellent kinome selectivity, in vivo PD activity, and safety profile.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Copper-Catalyzed Aerobic Oxidative Amidation of Benzyl Alcohols

A Cu-catalyzed synthesis of amides from alcohols and secondary amines using the oxygen in air as the terminal oxidant has been developed. The methodology is operationally simple requiring no high pressure equipment or handling of pure oxygen. The commercially available, nonprecious metal catalyst, Cu(phen)Cl2, in conjunction with di-tert-butyl hydrazine dicarboxylate and an inorganic base provides a variety of benzamides in moderate to excellent yields. The pKa of amine conjugate acid and electronics of alcohol were shown to impact the selection of base for optimal reactivity. A mechanism consistent with the observed reactivity trends, KIE, and Hammett study is proposed.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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. Recommanded Product: 39093-93-1

Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore

A series of tetrahydroisoquinolines acting as dual histamine H3/serotonin transporter ligands is described. A highly regio-selective synthesis of the tetrahydroisoquinoline core involving acid mediated ring-closure of an acetophenone intermediate followed by reduction with NaCNBH3 was developed. In vitro and in vivo data are discussed.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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FUSED RING PYRIDINE COMPOUND

[Problem] To provide a compound useful as a novel agent which is excellent in preventing and/or treating cannabinoid receptor type 2-related diseases, based on agonist action on a cannabinoid receptor type 2 [Means for Solution] The present inventors conducted thorough investigation regarding compounds having agonist action on a cannabinoid receptor type 2. They confirmed that the fused ring pyridine compound of the present invention has excellent agonist action on the cannabinoid receptor type 2, thereby completing the present invention. The fused ring pyridine compound of the present invention has agonist action on the cannabinoid receptor type 2, and can be used as an agent for preventing and/or treating cannabinoid receptor type 2-related diseases, for example, inflammatory diseases and pain.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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SOLID FORMS OF FILGOTINIB FREE BASE

The present invention relates to crystalline filgotinib free base, a method of its preparation and a pharmaceutical composition comprising the same.

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