- 7-OXO -6-(SULFOOXY)- 1,6-DIAZABICYCLO [3.2.1] OCTANE CONTAINING COMPOUNDS AND THEIR USE IN TREATMENT OF BACTERIAL INFECTIONS
-
Compounds of Formula (I) or a stereoisomer or a pharmaceutically acceptable salt thereof, their preparation, and use in treating a bacterial infection are disclosed.
- -
-
Page/Page column 26
(2017/06/19)
-
- Synthesis of N- and C-azolyl-substituted pyrazolo[1,5-a]pyrimidines by recyclization of pyrimidinium salts
-
We studied the reaction of 2-(ethoxycarbonyl)methyl-1,4,6-trimethylpyrimidinium iodide with hydrazides of N-azolyl- and C-pyrazolyl-substituted carboxylic acids, which were synthesized by reacting the respective esters with hydrazine hydrate. This reaction was shown to result in recyclization and formation of ethyl 2-(pyrazolylalkyl)- and 2-(azolylalkyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidine- 3-carboxylates. Besides pyrazolopyrimidines, the separation of reaction mixture provided in some cases also another recyclization product, 2-hydroxy-5,7-dimethylpyrazolo[1,5-a]pyrimidine.
- Danagulyan, Gevorg G.,Tumanyan, Araksya K.,Attaryan, Oganes S.,Tamazyan, Rafael A.,Danagulyan, Anna G.,Ayvazyan, Armen G.
-
p. 483 - 490
(2015/10/19)
-
- PROTEIN KINASE INHIBITORS
-
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
- -
-
Paragraph 0158
(2015/02/18)
-
- PROTEIN KINASE INHIBITORS
-
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
- -
-
Page/Page column 39
(2013/04/25)
-
- Combinatorial synthesis of 3,5-Dimethylene substituted 1,2,4-Triazoles
-
Combinatorial cyclizations of imidates and hydrazides with methylene linked R groups, generated from the corresponding nitriles and carboxylic acids, respectively, provided a large library of 3,5-dimethylene substituted 1,2,4- trizoles. 2011 Bentham Science Publishers Ltd.
- Woodard, Scott S.,Jerome, Kevin D.
-
experimental part
p. 132 - 137
(2012/04/18)
-
- Substituted aryl or heteroarylpiperidine derivatives as melanocortin-4 receptor modulators
-
The present invention relates to substituted aryl or heteroarylpiperidine derivatives of structure (I) as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
- -
-
Page/Page column 47
(2009/03/07)
-
- Antidiabetic agents
-
The present invention provides compounds of Formula (I): wherein A, X, Q, Y, B, D, Z, and E have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antidiabetic agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.
- -
-
-
- Synthesis of 5-arylidene-2-aryl-3-(1, 2, 4-triazoloacetamidyl)-1, 3-thiadiazol-4-ones as antibacterial, antifungal, analgesic and diuretic agents
-
1, 2, 4-Triazole on reaction with ethyl chloroacetate affords 1, 2, 4-triazoloacetate 1 which on treatment with hydrazine hydrate yields (acetohydrazido)-1, 2, 4-triazole 2. Condensation of 2 with various substituted aromatic aldehydes affords arylideneacetohydrazido-1, 2, 4-triazoles 3 which on cycloaddition with mercaptoacetic acid gives 2-(substituted aryl)-3-(1, 2, 4-triazolylacetamidyl)-4-oxo-thiazolidines 4. Treatment of the 4-thiazolidinones with various substituted aromatic aldehydes affords 5-arylidene-2-aryl-3-(1, 2, 4-trizolylacetamidyl)-1, 3-thiazolidin-4-ones 5. Their structures have been elucidated on the basis of their elemental analysis and spectral data. All the products have been screened for their antibacterial, antifungal, analgesic and diuretic activities.
- Srivastava,Srivastava, Soumya,Srivastava
-
p. 1937 - 1945
(2007/10/03)
-
- Synthesis of new 1, 2, 4-triazolo-thiadiazoles and its 2-oxoazetidines as antimicrobial, anticonvulsant and antiinflammatory agents
-
Several 2-arylidenylamino-5-(N1-1, 2, 4-triazolomethyl) -1, 3, 4-thiadiazoles 4 and 1-[5′-(N1-1, 2, 4-triazolomethyl) -1′, 3′, 4′-thiadiazol-2′-yl]-4-(substituted phenyl)-3-chloro-2-oxo-azetidines 5 have been synthesised and evaluated for their antibacterial, antifungal, anticonvulsant and antiinflammatory activities. Structures of the synthesised compounds have been elucidated on the basis of their elemental analyses and spectral data.
- Srivastava,Srivastava, Soumya,Srivastava
-
p. 2357 - 2363
(2007/10/03)
-
- An investigation into the alkylation of 1,2,4-triazole
-
The alkylation of 1,2,4-triazole with 4-nitrobenzyl halides and a variety of bases afforded the 1- and 4-alkylated isomers with a consistent regioselectivity of 90:10. Previously reported regiospecific alkylations of 1,2,4-triazole were re-examined and the quoted isomer ratios were shown to depend on the isolation procedure. The use of DBU as base in the alkylation of 1,2,4-triazole allows for a convenient and high yielding synthesis of 1- substituted-1,2,4-triazoles. (C) 2000 Elsevier Science Ltd.
- Bulger, Paul G.,Cottrell, Ian F.,Cowden, Cameron J.,Davies, Antony J.,Dolling, Ulf-H.
-
p. 1297 - 1301
(2007/10/03)
-
- SYNTHESIS AND CHARACTERIZATION OF TAUTOMERIC TRIAZOLIUM YLIDES
-
In this paper, for the first time, it is announced the synthesis and characterization of tautomeric equilibrium in the class of cycloimmonium ylides.The synthesis of tautomeric triazolium ylides 10, 11 and 12 have been realized by the "salt method" in their 1,2,4-triazolium salt 7, 8 and 9 respectively, in the presence of a base (K2CO3 or TEA).Theoretically by the MINDO/3 procedure method and experimentally by the synthesis of disubstituted triazolium ylides 14, 15 and 16 it has been verified that the tautomeric phenacylide forms 10b, 11a and 12a are more reactive than their carbethoxymethylide from 10a, 11b and 12 b, respectively, in reaction with picryl chloride.All structures obtained in this paper have been established using elemental analysis, mass-, ir-, 1H-NMR- and 13C-NMR-spectra.
- Surpateanu, Gheorghe,Lablache-Combier, Alain,Grandclaudon, Pierre,Coutere, Alain,Mouchel, B.
-
p. 671 - 681
(2007/10/02)
-
- An improved method for the N-alkylation of benzotriazole and 1,2,4-triazole
-
The N-alkylation of benzotriazole and 1,2,4-triazole with alkyl halides proceeds efficiently in the presence of sodium hydroxide in N,N-dimethylformamide.
- Katritzky, Alan R.,Kuzmierkiewiecz, Wojciech,Greenhill, John V.
-
p. 369 - 373
(2007/10/02)
-
- STUDY AND CHARACTERIZATION OF TAUTOMERIC TRIAZOLIUM YLIDS
-
The presence of two tautomeric forms in equilibrium for some triazolium ylids has been revealed by nmr spectroscopy and confirmed by trapping with picryl chloride.
- Couture, Axel,Lablache-Combier, Alain,Grandclaudon, Pierre,Surpateanu, Gheorghe
-
p. 2111 - 2114
(2007/10/02)
-
- BIOMIMETIC, CHEMICAL, AND SPECTROSCOPIC EVALUATIONS FOR THE RADIOSENSITIZING POTENTIAL OF N1- AND N2-SUBSTITUTED DERIVATIVES OF 3-NITRO-1,2,4-TRIAZOLE TOWARD HYPOXIC CELLS IN THE RADIOTHERAPY: REMARKABLY DIFFERENT SUBSTITUTION EFFECT
-
N1- and N2-derivatives of 3-nitro-1,2,4-triazole (3-NTR) were subjected to the non-biological evaluation methods involving biomimetic, chemical, and spectroscopic procedures for the radiosensitizing potential.Consequently, the N1-derivatives of 3-NTR were suggested to be more promising radiosensitizers to hypoxic cells in vivo than the N2-derivatives.
- Nagao, Yoshimitsu,Sano, Shigeki,Oxhiai, Masahito,Fujita, Eichi
-
p. 3211 - 3232
(2007/10/02)
-