7778-01-0Relevant articles and documents
β-AMINO ACID DERIVATIVES
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Page/Page column 50, (2010/11/24)
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R8 and R9 are as defined herein, as well as to compositions containing such a compound and the uses of such a compound. Compounds of formula (I) are especially useful in the treatment of pain.
SUBSTITUTED BENZYLIMIDAZOLES USEFUL FOR THE TREATMENT OF INFLAMMATORY DISEASES
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Page/Page column 70-71, (2008/06/13)
The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory conditions.
PIPERIDINE COMPOUND AND PROCESS FOR PREPARING THE SAME
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Page/Page column 63; 134, (2010/10/20)
The present invention is to provide a piperidine compound represented by the formula [I]: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted benzene ring, R1 is hydrogen atom or a substituent for amino group, R2 is hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom, Z is oxygen atom or -N(R3)-, R3 is hydrogen atom or an optionally substituted alkyl group, R4a and R4b may be the same or different, and each is hydrogen atom or an optionally substituted alkyl group, or a pharmaceutically acceptable salt thereof, which has an excellent tachykinin receptor antagonistic action.
Synthesis of 6-(3,5-dichlorobenzyl) derivatives as isosteric analogues of the HIV drug 6-(3,5-dimethylbenzyl)-1-(ethoxymethyl)-5-isopropyluracil (GCA-186)
Sorensen, Esben R.,El-Brollosy, Nasser R.,Jorgensen, Per T.,Pedersen, Erik B.,Nielsen, Claus
, p. 299 - 304 (2007/10/03)
The HIV-1 inhibitors described in this paper is closely related to 6-(3,5-dimethylbenzyl)-1-(ethoxymethyl)-5-isopropyluracil (GCA-186) an anti-HIV-1 drug that is highly active against both wild type and mutated HIV-1 strains. The two methyl groups on the 6-benzyl moiety have been shown to improve the binding stability of the drug to the NNRTI-binding site in reverse transcriptase of drug mediated mutant HIV-1 viruses. The methyl groups are replaced with isosteric chloro-atoms to avoid metabolism due to the two methyl groups. However, the isosteric chloro derivatives show tenfold less activity against HIV-1 than their corresponding methyl derivatives. The synthesis and the antiviral activities of the corresponding 1-(allyloxy- and indanyloxy)methyl-6- (3,5-dichlorobenzyl)-5-ethyluracil derivatives are also reported.
Design, synthesis, and structure - Activity relationship studies of ATP analogues as DNA gyrase inhibitors
Luebbers, Thomas,Angehrn, Peter,Gmuender, Hans,Herzig, Silvia,Kulhanek, Josef
, p. 821 - 826 (2007/10/03)
We report herein the design and synthesis of ATP-analogues, namely 4-amino-pyrazolo[3,4-d]pyrimidines and 4-amino-pyrazolo[1,5-a][1,3,5]triazines, with DNA gyrase inhibitory activity. Among these series, some compounds exhibited promising antibacterial activity. (C) 2000 Elsevier Science Ltd. All rights reserved.
Benzylated 1,2,3-triazoles as anticoccidiostats
Bochis,Chabala,Harris,Peterson,Barash,Beattie,Brown,Graham,Waksmunski,Tischler,Joshua,Smith,Colwell,Wyvratt Jr.,Fisher,Tamas,Nicolich,Schleim,Wilks
, p. 2843 - 2852 (2007/10/02)
Substituted 5-amino-4-carbamoyl-1,2,3-triazoles 3a-w were prepared by two synthetic schemes and evaluated in vivo for anticoccidial activity. Both schemes proceeded by brominating appropriately substituted toluenes 4a-s,v to 5a-s,v. In Scheme I, the brominated benzyl analogues 5 were converted to the corresponding benzyl azides 6, which were treated with cyanoacetamide to yield 1-substituted-5-amino-4-carbamoyl-1,2,3-triazoles 3. In Scheme II, the benzyl halides 5 were employed to alkylate the sodium salt of 5-amino-4-carbamoyl-1,2,3-triazole (7). Preliminary screening data against Eimeria acervulina and E. tenella in chickens suggested structural requirements for maximizing activity. Further evaluation against a relatively resistant series of eight Eimeria field isolates revealed L-651,582 (3a) to be a highly effective coccidiostat. However, unacceptable tissue residues precluded further development. Mechanistic studies on this series of 5-amino-4-carbamoyl-1,2,3-triazoles and, in particular, on L-651,582 (3a) revealed that its mode of action does not involve inhibition of IMP dehydrogenase, but probably interferes with host cell calcium entry. In addition, L-651,582 has been found to have antiproliferative activity in several disease models and was recently reported to possess antimetastatic activity in a model of ovarian cancer progression.
Insecticidal alkenes
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, (2008/06/13)
Compounds of formula R3 --CH=CH--CR1 R2 --CH2 OCH2 R4 wherein R1 and R2 are H, alkyl or together form a cycloalkyl group with the adjacent carbon, R3 is a substituted phenyl group, R4 is an optionally substituted phenoxy phenyl group, and compositions containing them useful as insecticides, and compounds of formula HOCH2 --CR1 R2 --CH2 OCH2 R4 and OCH--CR1 R2 CH2 OCH2 R4, useful as intermediates therefor.
Insecticidal alkenes
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, (2008/06/13)
Compounds of formula R3 --CH=CH--CR1 R2 --CH2 OCH2 R4 wherein R1 and R2 are H, alkyl or together form a cycloalkyl group with the adjacent carbon, R3 is a substituted phenyl group, R4 is an optionally subsituted phenoxy phenyl group, and compositions containing them useful as insecticides, and compounds of formula HOCH2 --CR1 R2 --CH2 OCH2 R4 and OCH--CR1 R2 CH2 OCH2 R4, useful as intermediates therefor.