Category: 39093-93-1

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Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials

In this paper we describe the optimization of a phenotypic hit against Plasmodium falciparum, based on a trisubstituted pyrimidine scaffold. This led to compounds with good pharmacokinetics and oral activity in a P. berghei mouse model of malaria. The most promising compound (13) showed a reduction in parasitemia of 96% when dosed at 30 mg/kg orally once a day for 4 days in the P. berghei mouse model of malaria. It also demonstrated a rapid rate of clearance of the erythrocytic stage of P. falciparum in the SCID mouse model with an ED90 of 11.7 mg/kg when dosed orally. Unfortunately, the compound is a potent inhibitor of cytochrome P450 enzymes, probably due to a 4-pyridyl substituent. Nevertheless, this is a lead molecule with a potentially useful antimalarial profile, which could either be further optimized or be used for target hunting.

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BENZOXAZINE ARYL SULFONAMIDE DERIVATIVES AS KV1.3 MODULATORS

Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, n, p, E, X, R1, R2, R3, R4R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with potassium channel modulation

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. name: Thiomorpholine 1,1-dioxide, 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

PYRROLOPYRIMIDIN DERIVATIVE FOR USE AS PI3K INHIBITOR, AND USE THEREOF

A preventive or therapeutic agent of a proliferative disease such as cancer, having superior PI3K inhibitory effects, superior cell proliferation inhibitory action as well as superior stability in a body and water solubility, is provided. A compound represented by formula (I): [wherein, Q represents a linking group represented by -X-Y-; X represents a single bond -CO-, -CONH-, -CON(C1-4 alkyl)-, -CS-, -CSNH-, -CSN(C1-4 alkyl)-, or -SO2-; Y represents a single bond, arylene or heteroarylene; provided that X and Y are not simultaneously single bonds; and R1 represents -C0-6 alkylene-(A)m-C1-6 alkyl, or C0-6 alkylene-(A)m-C0-6 alkylene-(heterocycle)] or a pharmaceutically acceptable salt thereof.

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Electric Literature of 39093-93-1, Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 39093-93-1In a document type isPatent ,introducing its new discovery.

HETEROCYCLIC COMPOUND

The present invention provide a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of autoimmune diseases and/or inflammatory diseases, graft versus host disease, cancers, central nervous diseases including neurodegenerative diseases, Charcot-Marie-Tooth disease and the like, and a pharmaceutical composition comprising the compound. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

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39093-93-1, Name is Thiomorpholine 1,1-dioxide, belongs to Thiomorpholine compound, is a common compound. category: ThiomorpholineIn an article, once mentioned the new application about 39093-93-1.

PHARMACEUTICAL COMPOSITION COMPRISING A BENZODIAZEPINE DERIVATIVE AND A INHIBITOR OF THE RSV FUSION PROTEIN

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.

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INDOLE AND INDAZOLE DERIVATIVES HAVING A CELL-, TISSUE- AND ORGAN-PRESERVING EFFECT

The present invention relates to a composition for preserving cells, tissues and organs, comprising as an active ingredient indole and indazole compounds of formula (1), or a pharmaceutically acceptable salt or isomer thereof, which are effective for preventing injury of organs, isolated cell systems or tissues caused by cold storage, transplant operation or post-transplantation reperfusion; a preservation method; and a preparation method of the composition.

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PYRAZOLE COMPOUNDS HAVING CANNABINOID RECEPTOR (CB1) ANTAGONIZING ACTIVITY

The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula:-N(R7)-, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula:-N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula:-N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.

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

CATHEPSIN CYSTEINE PROTEASE INHIBITORS

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

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IMIDAZOPYRROLOPYRIDINE AS INHIBITORS OF THE JAK FAMILY OF KINASES

2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.

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Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors of human lactate dehydrogenase A. Utilizing structure-based design and physical property optimization, multiple inhibitors were discovered with <10 muM lactate IC50 in a MiaPaca2 cell line. Optimization of the series led to 29, a potent cell active molecule (MiaPaca2 IC50 = 0.67 muM) that also possessed good exposure when dosed orally to mice. But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! Read on for other articles about !, HPLC of Formula: C4H9NO2S

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