- Ambident polyfluoroalkyl-substituted pyrazoles in the methylation reactions
-
The reactivity of polyfluoroalkyl-containing pyrazoles has been estimated using the quantum chemical calculations. A good regioselectivity in the methylation of polyfluoroalkylpyrazoles was reached while varying the reaction conditions. Under basic condit
- Ivanova, Anna E.,Burgart, Yanina V.,Saloutin, Viktor I.,Slepukhin, Pavel A.,Borisevich, Sophia S.,Khursan, Sergey L.
-
-
- SUBSTITUTED PYRIDINE AND PYRAZINE BMI-1 INHIBITORS
-
Amine substituted pyridine and pyrazine compounds and forms thereof that inhibit the function and reduce the level of B -cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
- -
-
Page/Page column 361
(2015/06/08)
-
- THERAPEUTIC COMPOUNDS
-
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which m, n, W, X, Y, Z, R, R1, R2, R3 and R4 are as defined in the specification, for use in therapy.
- -
-
Paragraph 0547; 0548; 0549; 0550; 0551; 0552
(2014/01/07)
-
- SULFONYL PIPERIDINE DERIVATIVES AND THEIR USE FOR TREATING PROKINETICIN MEDIATED DISEASES
-
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof : (I) in which m, n, W, X, Y, Z, R1, R2, R3 and R4 are as defined in the specification, for use in the treatm
- -
-
Page/Page column 46-47
(2014/01/07)
-
- SOLUBLE GUANYLATE CYCLASE ACTIVATORS
-
The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
- -
-
Page/Page column 46-47
(2011/10/13)
-
- Improved regioselectivity in pyrazole formation through the use of fluorinated alcohols as solvents: Synthesis and biological activity of fluorinated tebufenpyrad analogs
-
(Chemical Equation Presented) The preparation of N-methylpyrazoles is usually accomplished through reaction of a suitable 1,3-diketone with methylhydrazine in ethanol as the solvent. This strategy, however, leads to the formation of regioisomeric mixtures of N-methylpyrazoles, which sometimes are difficult to separate. We have determined that the use of fluorinated alcohols such as 2,2,2-trifluoroethanol (TFE) and 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP) as solvents dramatically increases the regioselectivity in the pyrazole formation, and we have used this modification in a straightforward synthesis of fluorinated analogs of Tebufenpyrad with acaricide activity.
- Fustero, Santos,Roman, Raquel,Sanz-Cervera, Juan F.,Simon-Fuentes, Antonio,Cunat, Ana C.,Villanova, Salvador,Murguia, Marcelo
-
p. 3523 - 3529
(2008/09/20)
-
- NOVEL HERBICIDES
-
Compounds of formula I: wherein R1, R2, R3, R4, m, R5, R6, n and Y are as defined in claim 1; or N-oxides, salts and optical isomers thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to herbicidal compositions comprising them and to methods of using them to control plants or to inhibit plant growth.
- -
-
Page/Page column 89
(2008/06/13)
-
- Pyrazolylarylalkines
-
The present invention relates to pyrazolylarylalkines and to their use, to a process for preparing pyrazolylarylalkines and also to intermediates.
- -
-
-
- Pyrazolylalkines
-
The present invention relates to pyrazolyalkines and to their use, to a process for preparing them and also to intermediates.
- -
-
-
- Synthesis of Some Trifluoromethyl Substituted 1-Methylpyrazoles
-
The major products from the reaction of β-alkoxyvinyl trifluoromethyl ketones 1a-c with methylhydrazine (2) in absolute ethanol are the 3-(trifluoromethyl)-substituted-1-methylpyrazoles 3a-3c with lesser amounts of the 5-(trifluoromethyl)-substituted prod
- Pavlik, James W.,Ayudhya, Theppawut Israsena Na,Tantayanon, Supawan
-
p. 1087 - 1089
(2007/10/03)
-
- Phosphosulfonate herbicides
-
This invention pertains to phosphosulfonates, having the general formula STR1 wherein Y is phenyl, naphthyl, benzyl, a (C5 -C8)cycloalkyl, a 5-membered heteroaromatic ring, a 6-membered heteraromatic ring, a fused 5,6-membered heteroaromatic ring, or a fused 6,6-membered heteroaromatic ring; and X is oxygen or sulfur; and R1 and R2 are each independently selected from substituted or unsubstituted alkyl, alkoxy, alkylthio, alkenyloxy, alkynyloxy, haloalkoxy, cyanoalkoxy, alkoxyalkoxy, cycloalkyloxy, cycloalkylalkoxy, alkylideneiminooxy, chloro, amino, phenyl or phenoxy; or R1 and R2 are both alkoxy, taken together with the phosphorus atom to form a 6-membered oxygen-containing ring; compositions containing these compounds and their use as herbicides.
- -
-
-
- Pyrazoles, fungicidal compositions and use
-
The invention compounds of formula I STR1 wherein R is H, C1-4 alkyl; optionally substituted aryl or CF3 ; Y is C1-4 alkyl or optionally substituted aryl; A is nitrogen or CH; and Z is optionally substituted hydrocarbyl or
- -
-
-
- INVESTIGATIO OF THE MECHANISMS OF FORMATION OF HETEROCYCLES BY NMR SPECTROSCOPY. INTERMEDIATES IN THE PRODUCTION OF PYRAZOLES FROM 1,3-DIKETONES AND HYDRAZINES
-
The structure of the intermediates formed in the reaction of 1,3-diketones RCOCH2COCH3 (R = Me, Et, t-Bu, Ph, CF3) with hydrazines NH2NHR' (R'= H, Me) in methanol and chloroform was determined by NMR spectroscopy in the normal and flow techniques.When R' = H, the reaction takes place through the formation of dihydroxypyrazolidine and 5-hydroxy-2-pyrazolines; for R'= Me, in addition, intermediate products with ketohydroxyazine and ketoenehydrazone structures were detected.A scheme with their participation is proposed for the formation of the isomeric pyrazoles.A pre-equilibrium between the 1,3-diketone, its hydrazinium salt in the Z,Z configuration, and the anion in the E,Z configuration was detected.The reaction rate of the ketone form of the 1,3-diketone is significantly higher than the reaction rate of the enol.
- Selivanov, S. I.,Bogatkin, R. A.,Ershov, B. A.
-
p. 788 - 795
(2007/10/02)
-