- Synthesis, structural characterization, and theoretical studies of new pyrazole (E)-2-{[(5-(tert-butyl)-1H-pyrazol-3-yl)imino]methyl}phenol and (E)-2-{[(1-(4-bromophenyl)-3-(tert-butyl)-1H-pyrazol-5-yl]imino]methyl}phenol
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In this paper, theoretical and experimental studies of two new Schiff bases were performed. The (E)-2-{[(5-(tert-butyl)-1H-pyrazol-3-yl)imino]methyl}phenol (3) and (E)-2-{[(1-(4-bromophenyl)-3-(tert-butyl)-1H-pyrazol-5-yl]imino]methyl}phenol (5)compounds were characterized by spectroscopic techniques, (i.e. MS, NMR, FT–IR, UV–vis, and single-crystal X–ray diffraction). The molecular geometry of both compounds in the ground state, vibrational frequencies, and chemical shift were calculated by using the functional density theory method, with B3LYP as functional and 6-31G** as basis set, using the GAUSSIAN 09 program package. With the VEDA 4 program, the vibrational frequencies were allocated in terms of potential energy distribution (PED). In this paper, theoretical and experimental studies of two new Schiff bases were performed. The (E)-2-{[(5-(tert-butyl)-1H-pyrazol-3-yl)imino]methyl}phenol (3) and (E)-2-{[(1-(4-bromophenyl)-3-(tert-butyl)-1H-pyrazol-5-yl]imino]methyl}phenol (5) compounds were characterized by spectroscopic techniques, (i.e. MS, NMR, FT-IR, UV–vis, and single-crystal X-ray diffraction). The molecular geometry of both compounds in the ground state, vibrational frequencies, and chemical shift were calculated by using the functional density theory method, with B3LYP as functional and 6-31G** as basis set, using the GAUSSIAN 09 program package. With the VEDA 4 program, the vibrational frequencies were allocated in terms of potential energy distribution (PED). Molecular stabilities were determined in terms of softness and hardness, and the values were determined from the energies of HOMO and LUMO orbitals. Remarkably, good agreements between the calculated IR, NMR and UV–vis spectra in comparison to those experimental ones, were found.
- Cuenú, Fernando,Restrepo-Acevedo, Andrés,Isabel-Murillo, María,Eduard Torres, John,Moreno-Fuquen, Rodolfo,Abonia, Rodrigo,Kennedy, Alan R.,Tenorio, Juan Carlos,Lehmann, Christian W.
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- Enhanced pyrazolopyrimidinones cytotoxicity against glioblastoma cells activated by ROS-Generating cold atmospheric plasma
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Pyrazolopyrimidinones are fused nitrogen-containing heterocyclic systems, which act as a core scaffold in many pharmaceutically relevant compounds. Pyrazolopyrimidinones have been demonstrated to be efficient in treating several diseases, including cystic fibrosis, obesity, viral infection and cancer. In this study using glioblastoma U-251MG cell line, we tested the cytotoxic effects of 15 pyrazolopyrimidinones, synthesised via a two-step process, in combination with cold atmospheric plasma (CAP). CAP is an adjustable source of reactive oxygen and nitrogen species as well as other unique chemical and physical effects which has been successfully tested as an innovative cancer therapy in clinical trials. Significantly variable cytotoxicity was observed with IC50 values ranging from around 11 μM to negligible toxicity among tested compounds. Interestingly, two pyrazolopyrimidinones were identified that act in a prodrug fashion and display around 5–15 times enhanced reactive-species dependent cytotoxicity when combined with cold atmospheric plasma. Activation was evident for direct CAP treatment on U-251MG cells loaded with the pyrazolopyrimidinone and indirect CAP treatment of the pyrazolopyrimidinone in media before adding to cells. Our results demonstrated the potential of CAP combined with pyrazolopyrimidinones as a programmable cytotoxic therapy and provide screened scaffolds that can be used for further development of pyrazolopyrimidinone prodrug derivatives.
- Charleton, Clara,Conway, Gillian E.,Cullen, Patrick J.,Curtin, James F.,Devereux, Michael,Devine, Robert W.,Gunes, Sebnem,He, Zhonglei,Kelada, Mark,Kinsella, Gemma K.,Malone, Renee,Mondala, Julie Rose Mae,O'Shea, Denis,Stephens, John C.,Tian, Furong,Tiwari, Brijesh,Walsh, John M. D.,Wang, Wenxin
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supporting information
(2021/08/13)
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- Synthesis of pyrazolopyrimidinones using a “one-pot” approach under microwave irradiation
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A simple one-pot method for the microwave-assisted synthesis of substituted pyrazolo[1,5-a]pyrimidinones, a core scaffold in many bioactive and pharmaceutically relevant compounds, has been established. A variety of substituents was tolerated at the 2 and 5 positions, including functionalized aryls, heterocycles, and alkyl groups.
- Kelada, Mark,Walsh, John M. D.,Devine, Robert W.,McArdle, Patrick,Stephens, John C.
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supporting information
p. 122 - 1228
(2018/06/13)
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- Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists
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A series of 1-substituted 3-(t-butyl/trifluoromethyl)pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides were investigated for hTRPV1 antagonism. The structure activity relationship indicated that the 3-chlorophenyl group at the 1-position of pyrazole was the optimized hydrophobic group for antagonistic potency and the activity was stereospecific to the S-configuration, providing exceptionally potent antagonists 13S and 16S with Ki(CAP) = 0.1 nM. Particularly significant, 13S exhibited antagonism selective for capsaicin and NADA and not for low pH or elevated temperature. Both compounds also proved to be very potent antagonists for rTRPV1, blocking in vivo the hypothermic action of capsaicin, consistent with their in vitro mechanism. The docking study of compounds 13S and 16S in our hTRPV1 homology model indicated that the binding modes differed somewhat, with that of 13S more closely resembling that of GRT12360.
- Lee, Sunho,Kim, Changhoon,Ann, Jihyae,Thorat, Shivaji A.,Kim, Eunhye,Park, Jongmi,Choi, Sun,Blumberg, Peter M.,Frank-Foltyn, Robert,Bahrenberg, Gregor,Stockhausen, Hannelore,Christoph, Thomas,Lee, Jeewoo
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p. 4383 - 4388
(2017/09/12)
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- Novel pyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating DRAK relating diseases containing the same as an active ingredient
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The present invention relates to a novel pyrimidine derivative, a production method thereof, and a pharmaceutical composition for preventing or treating death-associated protein related apoptosis inducing protein kinase (DRAK)-associated diseases containing the same as an active ingredient. According to the present invention, the novel pyrimidine derivative, an optical isomer thereof, or a pharmaceutically acceptable salt thereof exhibits effective inhibitory activities on DRAK, and thus can be useful for treating diseases caused by DRAK such as cancer and tumor.COPYRIGHT KIPO 2017
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Paragraph 0116; 0160-0162
(2017/08/02)
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- FUSED CYCLOALKYL-PYRIMIDINE COMPOUNDS AND USES THEREOF
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Fused cycloalkyl-pyrimidine compounds that are kinase inhibitors, such as multi-kinase inhibitors, are provided. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused cycloalkyl-pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused cycloalkyl- pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer.
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Paragraph 0220
(2016/01/25)
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- Pyrazolotriazines as inhibitors of nucleases
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The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3 and R4 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
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Paragraph 0122; 0123; 0124; 0125; 0126; 0127; 0151-0157
(2016/01/12)
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- Discovery of mixed type thymidine phosphorylase inhibitors endowed with antiangiogenic properties: Synthesis, pharmacological evaluation and molecular docking study of 2-thioxo-pyrazolo[1,5-a][1,3,5]triazin-4-ones. Part II
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In our drug discovery program, a series of 2-thioxo-pyrazolo[1,5-a][1,3,5] triazin-4-ones were designed, synthesized and evaluated for their TP inhibitory potential. All the synthesized analogues conferred a varying degree of TP inhibitory activity, comparable or better than positive control, 7-deazaxanthine (7-DX, 2) (IC50 value = 42.63 μM). A systematic approach to the lead optimization identified compounds 3c and 4a as the most promising TP inhibitors, exhibiting mixed mode of enzyme inhibition. Moreover, selected compounds demonstrated the ability to attenuate the expression of the angiogenic markers (viz. MMP-9 and VEGF) in MDA-MB-231 cells at sublethal concentrations. In addition, molecular docking studies revealed the plausible binding orientation of these inhibitors towards TP, which was in accordance with the experimental results. Taken as a whole, these compounds would constitute a new direction for the design of novel TP inhibitors with promising antiangiogenic properties.
- Bera, Hriday,Ojha, Probir Kumar,Tan, Bee Jen,Sun, Lingyi,Dolzhenko, Anton V.,Chui, Wai-Keung,Chiu, Gigi Ngar Chee
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p. 294 - 303
(2014/04/17)
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- SUBSTITUTED HETEROAROMATIC PYRAZOLE-CONTAINING CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted heteroaromatic pyrazole-containing carboxamide and urea derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 104
(2013/03/26)
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- Substituted Heteroaromatic Pyrazole-Containing Carboxamide and Urea Compounds as Vanilloid Receptor Ligands
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Substituted heteroaromatic pyrazole-containing carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also to a method of using these compounds for treating and/or inhibiting pain and further diseases and/or disorders.
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Paragraph 0668
(2013/03/26)
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- SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH AN N-CYCLIC GROUP AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with an N-cyclic group as vanilloid receptor ligands formula (S) to pharmaceutical compositions containing these compounds of the general formula (S) and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 46
(2013/05/23)
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- SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH AN O-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives of formula (Q) as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 67
(2013/05/23)
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- SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH A CO-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with a CO-containing group as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 48
(2013/05/23)
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- SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH AN N-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives of formula (R) bearing a phenyl moiety substituted with an N-containing group as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 56
(2013/05/23)
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- SUBSTITUTED PYRAZOLYL-BASED CARBOXAMIDE AND UREA DERIVATIVES BEARING A PHENYL MOIETY SUBSTITUTED WITH AN SO2-CONTAINING GROUP AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with a S02-containing group as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Page/Page column 48
(2013/05/23)
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- Substituted Cyclic Carboxamide and Urea Derivatives as Ligands of the Vanilloid Receptor
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Substituted cyclic carboxamide and urea compounds, a process for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for the treatment and/or inhibition of pain and other conditions mediated by the vanilloid receptor 1.
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Page/Page column 29
(2012/03/10)
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- Substituted Heteroaromatic Carboxamide and Urea Compounds as Vanilloid Receptor Ligands
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Substituted heteroaromatic carboxamide and urea compounds corresponding to formula (i) processes for the preparation thereof, pharmaceutical compositions containing these compounds and also a method of using these compounds in pharmaceutical compositions for treating or inhibiting pain and other conditions mediated at least in part via the vanilloid receptor 1.
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Page/Page column 33
(2012/05/20)
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- SUBSTITUTED HETEROAROMATIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted heteroaromatic carboxamide and urea derivatives of formula (I), to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
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Page/Page column 73
(2012/05/31)
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- Substituted Bicyclic Carboxamide and Urea Compounds as Vanilloid Receptor Ligands
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Substituted bicyclic carboxamide and urea compounds corresponding to formula (I) processes for the preparation thereof, pharmaceutical compositions containing these compounds, and a method of using these compounds for the treatment and/or inhibition of pain and other conditions mediated at least in part via the vanilloid receptor 1.
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Page/Page column 29
(2012/05/20)
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- SUBSTITUTED BICYCLIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted bicyclic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
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Page/Page column 72
(2012/05/31)
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- Synthesis of novel 1,2,5-trisubstituted benzimidazoles as potential antitumor agents
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Novel methyl 1-(5-tert-butyl-1H-pyrazol-3-yl)-2-(aryl)-1H-benzo[d] imidazole-5-carboxylates 11 were synthesized by following a four-step strategy involving a nucleophilic aromatic displacement (SNAr) and a solvent free approach as key steps for the formation of the desired products. Structure of intermediates and products were confirmed by X-ray diffraction as well as the tautomeric rearrangement suffered by the pyrazole moiety during the curse of the final cyclization process. Several of the obtained compounds were screened by the US National Cancer Institute (NCI) for their ability to inhibit 60 different human tumor cell lines. Products 11b and 11n exhibited the highest activity against a range of cancer cell lines with remarkable values in panels of Non-Small Cell Lung Cancer, Melanoma and Leukemia, with GI50 range of 1.15-7.33 μM and 0.167-7.59 μM, respectively, and suitable LC 50 with values greater than 100 μM.
- Abonia, Rodrigo,Cortes, Edwar,Insuasty, Braulio,Quiroga, Jairo,Nogueras, Manuel,Cobo, Justo
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scheme or table
p. 4062 - 4070
(2011/11/12)
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- INHIBITORS OF AKT ACTIVITY
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The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
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Page/Page column 240
(2010/10/03)
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- SUBSTITUTED AROMATIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions (formula (I)).
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Page/Page column 95
(2010/11/18)
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- SUBSTITUTED PHENYLLUREAS AND PHENYLAMIDES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted phenylureas and phenylamides of formula (I), to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
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Page/Page column 78
(2010/11/18)
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- The design and synthesis of novel α-ketoamide-based p38 MAP kinase inhibitors
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We have identified a novel series of potent p38 MAP kinase inhibitors through structure-based design which due to their extended molecular architecture bind, in addition to the ATP site, to an allosteric pocket. In vitro ADME and in vivo PK studies show these compounds to have drug-like characteristics which could result in the development of an oral treatment for inflammatory conditions.
- Montalban, Antonio Garrido,Boman, Erik,Chang, Chau-Dung,Ceide, Susana Conde,Dahl, Russell,Dalesandro, David,Delaet, Nancy G.J.,Erb, Eric,Ernst, Justin T.,Gibbs, Andrew,Kahl, Jeffrey,Kessler, Linda,Lundstroem, Jan,Miller, Stephen,Nakanishi, Hiroshi,Roberts, Edward,Saiah, Eddine,Sullivan, Robert,Wang, Zhijun,Larson, Christopher J.
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p. 1772 - 1777
(2008/09/20)
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- Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases
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The design, synthesis and biological evaluation of a series of 4-aminopyrazolylpyrimidines as potent Trk kinase inhibitors is reported. High-throughput screening identified a promising hit in the 4- aminopyrazolylpyrimidine chemotype. Initial optimization of the series led to more potent Trk inhibitors. Further optimization using two strategies resulted in significant improvement of physical properties and led to the discovery of 10z (AZ-23), a potent, orally bioavailable Trk A/B inhibitor. The compound offers the potential to test the hypothesis that modulation of Trk activity will be of benefit in the treatment of cancer and other indications in vivo.
- Wang, Tao,Lamb, Michelle L.,Scott, David A.,Wang, Haixia,Block, Michael H.,Lyne, Paul D.,Lee, John W.,Davies, Audrey M.,Zhang, Hai-Jun,Zhu, Yanyi,Gu, Fei,Han, Yongxin,Wang, Bin,Mohr, Peter J.,Kaus, Robert J.,Josey, John A.,Hoffmann, Ethan,Thress, Ken,MacIntyre, Terry,Wang, Haiyun,Omer, Charles A.,Yu, Dingwei
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scheme or table
p. 4672 - 4684
(2009/07/25)
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- Microwave-assisted synthesis of N-pyrazole ureas and the p38α inhibitor BIRB 796 for study into accelerated cell ageing
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Microwave irradiation of substituted hydrazines and β-ketoesters gives 5-aminopyrazoles in excellent yield, which can be transformed to the corresponding N-carbonyl derivatives by treatment with an isocyanate or chloroformate. Derivatization of 4-nitronaphth-1-ol using predominantly microwave heating methods and reaction with an N-pyrazole carbamate provides a rapid route to the N-pyrazole urea BIRB 796 in high purity, as a potent and selective inhibitor of p38α mitogen-activated protein kinase for the study of accelerated ageing in Werner syndrome cells. The Royal Society of Chemistry 2006.
- Bagley, Mark C.,Davis, Terence,Dix, Matthew C.,Widdowson, Caroline S.,Kipling, David
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p. 4158 - 4164
(2008/09/19)
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- QUINAZOLINE DERIVATIVES
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The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
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Page/Page column 120
(2008/06/13)
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- Synthesis and chemistry of 3-tert-butyl-1,5-diaminopyrazole
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N-Amination of 3-amino-5-tert-butylpyrazole 11 with hydroxylamine-O-sulfonic acid gave the 1,5-diaminopyrazole 12 with good regiochemical control. The reactions of 12 with certain electrophiles (e.g. acetic anhydride, DMF acetal, aromatic aldehydes, methoxymethylene Meldrum's acid) took place at one (or both) of the amino groups and no cyclised products were obtained. Reaction of 12 with carbon disulfide followed by alkylation under basic conditions provided the pyrazolo[1,5-b]1,2,4-triazole 26 which is a useful photographic magenta coupler. Reactions of 12 with 1,2- and 1,3-dicarbonyl compounds (diketones and ketoesters) provided new pyrazolo[1,5-b]1,2,4-triazines 29, 30, 42 and 43 and the first derivatives of the pyrazolo[1,5-b]1,2,4-triazepine system 31 and 35-36. The X-ray crystal structure of the pyrazolotriazepine 33 is reported.
- Blake, Alexander J.,Clarke, David,Mares, Richard W.,McNab, Hamish
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p. 4268 - 4274
(2007/10/03)
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- Photographic coupler and silver halide color photographic material
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A 1H-pyrazolo[1,5-b][1,2,4]triazole magenta coupler having a t-alkyl group at the position-6 and an amido group-substituted phenyl group at the position-2 is disclosed. There is also disclosed a silver halide color photographic material containing the same.
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- Dipolar Cycloaddition Reactions of Diazoazoles with Electron-Rich and with Strained Unsaturated Compounds
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Regiospecific net 1,7-cycloaddition reactions of electron-rich or strained olefins and electron-donor acetylenes occur readily (-70 to -10 degC) with diazoazoles having nitrogen in the 2-positions of their azole rings.Diazoazoles such as 5-tert-butyl-3-diazo-3H-pyrazole (20), 3-diazo-5-phenyl-3H-pyrazole (24), 2-diazo-2H-imidazole (28), 4,5-dicyano-2-diazo-2H-imidazole (12), 4-diazo-4H-imidazole (63), 4-diazo-5-phenyl-4H-1,2,3-triazole (70), 5-cyano-4-diazo-4H-1,2,3-triazole (74), 3-diazo-3H-1,2,4-triazole (76), and 3-diazo-5-phenyl-3H-1,2,4-triazole (79) thus usually add effectively to unsaturated reactans such as enamines, 1-alkoxyalkenes, ketene acetals, aryl isocyanates, norbornene, and norbornadiene to give new 1,7-cycloadducts.These cyclization reactions may be followed by tautomerization processes leading to new stabilized fused heterocycles or by elimination to novel highly delocalized heteroaromatic derivatives. 4,5-Dicyano-2-diazo-2H-imidazole (12) undergoes various accelerated cycloadditions to unsaturates and adds to norbornene and norbornadiene by exclusive exo dipolar processes.Addition of activated acetylenes to representative α-diazoazoles also results in regiospecific 1,7-cyclization to give stabilized fused azolo heterocycles.
- Magee, W. L.,Rao, C. B.,Glinka, J.,Hui, H.,Amick, T. J.,et al.
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p. 5538 - 5548
(2007/10/02)
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- Herbicidal 5-t-butyl-3-pyrazalylcarbamates and ureas
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A novel pyrazole derivative represented by the formula [I]: STR1 wherein X and Y are defined in the specification, which has herbicidal activity, is disclosed. A process for preparing the pyrazole derivative of the formula [I] is also disclosed. A herbicide containing as an active ingredient the pyrazole derivative of the formula [I] is further disclosed as is a method for using the herbicide.
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- Herbicidal 5-t-butyl-3-(N-alkanoylamino)pyrazoles
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A novel pyrazole derivative represented by the formula [I]: STR1 wherein X and Y are defined in the specification, which has a herbicidal activity, is disclosed. A process for preparing the pyrazole derivative of the formula [I] is also disclosed. A herbicide containing as an active ingredient the pyrazole derivative of the formula [I] is further disclosed.
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