146726-08-1Relevant articles and documents
INDOLE DERIVATIVES USEFUL AS CCR2 ANTAGONISTS
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, (2012/10/07)
Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salt thereof wherein R7, A, X, B, and n are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds
6-(3-AZA-BICYCLO[3.1.0]HEX-3-YL)-2-PHENYL-PYRIMIDINES
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Page/Page column 47-48, (2010/11/03)
The present invention relates to 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
AZABICYCLIC MUSCARINIC RECEPTOR ANTAGONISTS
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Page/Page column 43-44, (2010/11/08)
The present invention generally relates to muscarinic receptor antagonists, which are useful for treating various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to processes for preparing compounds described herein, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.
Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones
Renslo, Adam R.,Jaishankar, Priyadarshini,Venkatachalam, Revathy,Hackbarth, Corinne,Lopez, Sara,Patel, Dinesh V.,Gordeev, Mikhail F.
, p. 5009 - 5024 (2007/10/03)
The oxazolidinones are a new class of synthetic antibacterials effective against a broad range of pathogenic Gram-positive bacteria, including multi-drug-resistant strains. Linezolid is the first drug from this class to reach the market and has become an
Synthesis of new fluoroquinolones and evaluation of their in vitro activity on Toxoplasma gondii and Plasmodium spp.
Anquetin,Rouquayrol,Mahmoudi,Santillana-Hayat,Gozalbes,Greiner,Farhati,Derouin,Guedj,Vierling
, p. 2773 - 2776 (2007/10/03)
The synthesis of four new computer-designed fluoroquinolones which have been predicted by QSAR analysis to be active against the protozoa Toxoplasma gondii is described. These compounds are inhibitory in vitro for T. gondii. One of these compounds has a remarkably high activity comparable to that of trovafloxacin. It combines the basic cyclopropyl-quinoline structure of gatifloxacin or moxifloxacin with the C-7 6-amino-3-azabicyclo[3.1.0]hexyl side chain of trovafloxacin. The four compounds are also inhibitory for blood stages of Plasmodium falciparum though at high concentration. These results confirm the potential of quinolones as anti-T. gondii and antimalarial drugs but also show that the QSAR models for T. gondii cannot be reliably extended for screening antimalarial activity.
Azabicyclo quinolone carboxylic acids
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, (2008/06/13)
Quinolone carboxylic acids 7-substituted by azabicyclo groups have antibacterial activity., Antibacterial wherein, R1 is hydrogen, a pharmaceutically acceptable cation, or alkyl;, Y, when taken independently, is ethyl, t-butyl, vinyl, cyclopropyl, 2-fluoroethyl, p-fluorophenyl, or o,p-difluorophenyl;, W is hydrogen, F, Cl, Br, alkyl, alkoxy, NH2, NHCH3;, A is CH, CF, CCl, COCH3, C-CH3, C-CN or N; or, A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five or six membered ring which may contain oxygen or a double bond, and which may have attached thereto R8 which is methyl or methylene; and, R2 is wherein R3, R4, R5, R6, R7, R9, R10 and R25 are each independently H, CH3, CH2NH2, CH2NHCH3 or CH2NHC2H5, and R5, R6, R7, and R9 may also independently be NH2, NHCH3 or NHC2H5.