- β-AMINO ACID DERIVATIVES
-
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.
- -
-
Page/Page column 50
(2010/11/24)
-
- SUBSTITUTED BENZYLIMIDAZOLES USEFUL FOR THE TREATMENT OF INFLAMMATORY DISEASES
-
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.
- -
-
Page/Page column 70-71
(2008/06/13)
-
- PIPERIDINE COMPOUND AND PROCESS FOR PREPARING THE SAME
-
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.
- -
-
Page/Page column 63; 134
(2010/10/20)
-
- Synthesis of 6-(3,5-dichlorobenzyl) derivatives as isosteric analogues of the HIV drug 6-(3,5-dimethylbenzyl)-1-(ethoxymethyl)-5-isopropyluracil (GCA-186)
-
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.
- Sorensen, Esben R.,El-Brollosy, Nasser R.,Jorgensen, Per T.,Pedersen, Erik B.,Nielsen, Claus
-
p. 299 - 304
(2007/10/03)
-
- Design, synthesis, and structure - Activity relationship studies of ATP analogues as DNA gyrase inhibitors
-
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.
- Luebbers, Thomas,Angehrn, Peter,Gmuender, Hans,Herzig, Silvia,Kulhanek, Josef
-
p. 821 - 826
(2007/10/03)
-
- Benzylated 1,2,3-triazoles as anticoccidiostats
-
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.
- 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)
-
- Insecticidal alkenes
-
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
-
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.
- -
-
-