- HEPATITIS B CORE PROTEIN MODULATORS
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The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound of formula:
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- HEPATITIS B CORE PROTEIN MODULATORS
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The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
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- CONJUGATES AND SMALL MOLECULES WHICH INTERACT WITH THE CD16A RECEPTOR
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The invention is related to medicine, in particular, to oncology and immunology. The novel compounds of the general formula 1 or 2, exhibiting affinity for CD16a receptor have been proposed. There were also proposed novel modified proteins active towards
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- 11-OXO-10,11-DIHYDRODIBENZO[B,F][1,4]THIAZEPINE S-OXIDE DERIVATIVES AND THEIR USE AS DOPAMINE D2 RECEPTOR ANTAGONISTS
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The disclosure includes compounds and pharmaceutically acceptable salts of Formula (I). Certain compounds and salts of Formula (I) are selective inhibitors of the Dopamine D2 receptor. The variables R1-R4, n, and L are defined herein. The disclosure also provides methods of synthesizing compounds of Formula (I) and pharmaceutical compositions containing compounds of Formula (I). Additionally the disclosure provides methods or treating patients suffering from central nervous system disorders, including Tourette's syndrome, bipolar disorder, hyperprolactinemia, tardive dyskinesia, Huntington's chorea, psychosis, depression, or schizophrenia.
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- HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS
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ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
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- Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists
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The D2 dopamine receptor (D2 DAR) is one of the most validated drug targets for neuropsychiatric and endocrine disorders. However, clinically approved drugs targeting D2 DAR display poor selectivity between the D2 and other receptors, especially the D3 DA
- Xiao, Jingbo,Free, R. Benjamin,Barnaeva, Elena,Conroy, Jennie L.,Doyle, Trevor,Miller, Brittney,Bryant-Genevier, Marthe,Taylor, Mercedes K.,Hu, Xin,Dulcey, Andrés E.,Southall, Noel,Ferrer, Marc,Titus, Steve,Zheng, Wei,Sibley, David R.,Marugan, Juan J.
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p. 3450 - 3463
(2014/05/20)
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- Evaluation of NTF1836 as an inhibitor of the mycothiol biosynthetic enzyme MshC in growing and non-replicating Mycobacterium tuberculosis
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The mycothiol biosynthesis enzyme MshC catalyzes the ligation of cysteine with the pseudodisaccharide GlcN-Ins and has been identified as an essential enzyme in Mycobacterium tuberculosis. We now report on the development of NTF1836 as a micromolar inhibi
- Newton, Gerald L.,Buchmeier, Nancy,La Clair, James J.,Fahey, Robert C.
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p. 3956 - 3964
(2011/08/06)
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- MUSCARINIC AGONISTS
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Compounds of the general formula (I) and methods are provided for the treatment of disease conditions in which the modification of cholinergic, especially muscarinic receptor activity, has a beneficial effect. In the method, an effective amount of a compo
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Page/Page column 26-27
(2010/06/17)
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- Synthesis and evaluation of dibenzothiazepines: A novel class of selective cannabinoid-1 receptor inverse agonists
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A novel class of CB1 inverse agonists was discovered. To efficiently establish structure-activity relationships (SARs), new synthetic methodologies amenable for parallel synthesis were developed. The compounds were evaluated in a mammalian cell-based func
- Pettersson, Hanna,Bülow, Anne,Ek, Fredrik,Jensen, Jacob,Ottesen, Lars K.,Fejzic, Alma,Ma, Jian-Nong,Tredici, Andria L. Del,Currier, Erika A.,Gardell, Luis R.,Tabatabaei, Ali,Craig, Darren,McFarland, Krista,Ott, Thomas R.,Piu, Fabrice,Burstein, Ethan S.,Olsson, Roger
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supporting information; experimental part
p. 1975 - 1982
(2009/12/31)
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- USE OF CANNABINOID MODULATING COMPOUNDS IN COMBINATION WITH OTHER THERAPEUTIC COMPOUNDS FOR ADJUNCTIVE THERAPY
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The present invention relates to pharmaceutical compositions that contain a compound that modulate the activity of a cannabinoid receptor in conjunction with another therapeutic compound and uses of compounds that modulate the activity of a cannabinoid re
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Page/Page column 85
(2008/12/04)
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- CB-1 MODULATING COMPOUNDS AND THEIR USE
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Disclosed herein is a compound of Formula (I). Also disclosed herein is a method of modulating the activity of a cannabinoid receptor using a compound of Formula (I). Furthermore, disclosed herein is a method of treating a disease or condition that would
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Page/Page column 55
(2008/06/13)
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- IRON CATALYZED CROSS-COUPLING REACTIONS OF IMIDOYL DERIVATIVES
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Disclosed is a process for preparing a compound of formula A - N=C(D)(B), from a compound of formula A-N=C(E)(B) and a compound of formula D-M using an iron catalyst, where the process has is represented by Equation (I).
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Page/Page column 37; 54; 55
(2010/11/27)
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- Iron-catalyzed cross-coupling of imidoyl chlorides with Grignard reagents
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A general, high yielding rapid iron-catalyzed cross-coupling reaction between Grignard reagents and imidoyl chlorides is described. These reactions are typically completed within 5 min, resulting in high yields of 71-96% using 5% iron catalyst in a THF-NM
- Ottesen, Lars K.,Ek, Fredrik,Olsson, Roger
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p. 1771 - 1773
(2007/10/03)
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