103260-44-2Relevant articles and documents
NEW MACROCYCLIC LRRK2 KINASE INHIBITORS
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Page/Page column 258-259, (2021/11/13)
Compounds of formula (I): wherein R, X1, X2, X3, Z1, Z2, Z3, A and Ra are as defined in the description. Medicaments.
Dihydropyrrolopyridine inhibitors of ROR-gamma
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Page/Page column 31; 32, (2016/11/21)
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORγ. Also provided are pharmaceutical compositions co
ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
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Paragraph 00484, (2016/04/20)
Described herein are compounds of Formula (S-I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA
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Paragraph 00105, (2016/05/24)
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions co
NDM INHIBITOR
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Paragraph 0114; 0116-0117, (2014/06/24)
An objective of the present invention is to provide a novel NDM (New Delhi metallo-β-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of β-lactam antibiotics that have been inactivated as a result of decomposition by NDM. According to the present invention, there is provided an NDM inhibitor contains a compound represented by general formula (I):
EP1 RECEPTOR LIGANDS
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Page/Page column 76, (2013/03/28)
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
AZAINDOLE GLUCOKINASE ACTIVATORS
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Page/Page column 54, (2011/06/26)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
Synthesis of bicyclic tertiary α-amino acids
Strachan, Jon-Paul,Whitaker, Regina C.,Miller, Craig H.,Bhatti, Balwinder S.
, p. 9909 - 9911 (2007/10/03)
Novel bicyclic α-amino acids, exo and endo-1-azabicyclo-[2.2.1] heptane-2-carboxylic acid, 1-azabicyclo[2.2.1]heptane-7-carboxylic acid, and 1-azabicyclo[3.2.2]nonane-2-carboxylic acid have been readily synthesized for the generation of neuronal nicotinic receptor ligands. Alkylation of glycine-derived Schiff bases or nitroacetates with cyclic ether electrophiles, followed by acid-induced ring opening and cyclization in NH4OH, allowed for the preparation of substantial quantities of the three tertiary bicyclic α-amino acids.
3-CYCLOALKYLCARBONYL INDOLES AS CANNABINOID RECEPTOR LIGANDS
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Page/Page column 115, (2008/06/13)
The present invention provides novel compounds of Formula (I), which are CB2 selective ligands useful for the treatment of pain.
New high affinity H3 receptor agonists without a basic side chain
Kitbunnadaj, Ruengwit,Hoffmann, Marcel,Fratantoni, Silvina A.,Bongers, Gerold,Bakker, Remko A.,Wieland, Kerstin,El Jilali, Ahmed,De Esch, Iwan J. P.,Menge, Wiro M. P. B.,Timmerman, Henk,Leurs, Rob
, p. 6309 - 6323 (2007/10/03)
In this study, we replaced the basic amine function of the known histamine H3 receptor agonists imbutamine or immepip with non-basic alcohol or hydrocarbon moieties. All compounds in this study show a moderate to high affinity for the cloned human H3 receptor and, unexpectedly, almost all of them act as potent agonists. Moreover, in the alcohol series, we consistently observed an increased selectivity for the human H3 receptor over the human H4 receptor, but none of the compounds in this series possess increased affinity and functional activity compared to their alkylamine congeners. In this new series of compounds VUF5657, 5-(1H-imidazol-4-yl)-pentan-1-ol, is the most potent histamine H3 receptor agonist (pKi = 8.0 and pEC50 = 8.1) with a 320-fold selectivity at the human H3 receptor over the human H 4 receptor.