- A two-fluoro the benzyl is wicked zole miticides (by machine translation)
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The invention provides a two-fluoro the benzyl is wicked zole compound, structure such as shown in formula I: In the formula: R1 Is selected from methyl or ethyl; R2 Is selected from methyl, ethyl or tertiary butyl; R3 Selected from H or Cl. The formula I compound to the insects, mites of killing effect, can be regarded as insecticide, acaricide for pests in agriculture, digestion control. (by machine translation)
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Paragraph 0017; 0018; 0019; 0021
(2019/02/25)
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- ARYL ANNULATED MACROCYCLIC INDOLE DERIVATIVES
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The present invention relates to aryl annulated macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
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Page/Page column 139
(2019/06/05)
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- Pyrazole amide compound, and preparation method and application thereof
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The invention discloses a pyrazole amide compound represented by the formula (I), and a preparation method and an application thereof, wherein R, R1, R2 and W have the definitions indicated in the specification. The compound represented by the formula (I) has bactericidal, insecticidal or acaricidal biological activities, and specially has quite high activity on pathogenic bacteria such as sphaerotheca fuliginea, botrytis cinerea, melampsora lini and the like.
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Paragraph 0111-0113
(2017/06/02)
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- 5-pyrazole amide compound, and preparation method and application thereof
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The invention discloses a 5-pyrazole amide compound as shown in a formula (I) which is described in the specification, and a preparation method and application thereof. In the formula (I), R, R1, R2, R3 and n are as defined in the specification. The 5-pyrazole amide compound as shown in the formula (I) has bactericidal, insecticidal or acaricidal bioactivity and especially has good activity to insects like aphids belonging to Homoptera and pathogens like Sphaerotheca fuliginea, Botrytis cinerea and rust pathogens.
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Paragraph 0104; 0105
(2017/08/28)
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- Highly regioselective organocatalyzed synthesis of pyrazoles from diazoacetates and carbonyl compounds
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A general, organocatalytic inverse-electron-demand [3+2] cycloaddition reaction between a range of carbonyl compounds and diazoacetates has been developed. This reaction is catalyzed by secondary amines as a "green promoter" to generate substituted pyrazoles with high levels of regioselectivity. It is noteworthy that this [3+2] cycloaddition reaction proceeds efficiently at room temperature with a simple and inexpensive catalyst. Considering the large variety and ready availability of the starting materials (e.g. ketones, β-ketoesters, β-diketones, and aldehydes), as well as the operational simplicity of this process, a convenient, practical, and highly modular pyrazole synthesis has been developed. We believe that this work will arouse more research interest in the organocatalytic synthesis of other biologically active heterocycles. Such studies are currently underway in our laboratory. Dipoles apart: In situ formed enamines react with diazoacetates under mild conditions to afford the corresponding polysubstituted pyrazoles in good-to-excellent yields through an inverse-electron-demand 1,3-dipolar cycloaddition process (see scheme). Copyright
- Wang, Lei,Huang, Jiayao,Gong, Xiaojie,Wang, Jian
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supporting information
p. 7555 - 7560
(2013/07/05)
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- Design, synthesis, and insecticidal activity of novel pyrazole derivatives containing α-hydroxymethyl-N-benzyl carboxamide, α-chloromethyl-N- benzyl carboxamide, and 4,5-dihydrooxazole moieties
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On the basis of commercial insecticides tebufenpyrad and tolfenpyrad, two series of novel pyrazole-5-carboxamides containing α-hydroxymethyl-N- benzyl or α-chloromethyl-N-benzyl and pyrazoles containing 4,5-dihydrooxazole moieties were designed and synthesized via the key intermediate 2-amino-1-(4-substituted) phenyl ethanol. The structures of target compounds were confirmed by 1H NMR and elemental analysis or high-resolution mass spectrum (HRMS), and their activities against cotton bollworm (Helicoverpa armigera), diamondback moth (Plutella xylostella), bean aphid (Aphis craccivora), mosquito (Culex pipiens pallens), and spider mite (Tetranychus cinnabarinus) were tested. The results of bioassays indicated that compounds containing α-chloromethyl-N-benzyl and compounds containing 4,5-dihydrooxazole showed high insecticidal activity against cotton bollworm. Especially, stomach activities of compounds Ij, Il, and IIe were 60% at 5 mg kg-1. Moreover, the target compounds exhibited high selectivity between cotton bollworm and diamondback moth, although both of them belong to the order Lepidoptera. Although the activities against diamondback moth were at a low level, some of the target compounds exhibited antifeedant activity. The compounds also had good activities against bean aphid, mosquito, and spider mite. The foliar contact activity of compounds Ic, Id, Ie, and IIf against bean aphid were 95, 95, 100, and 95%, respectively, at 200 mg kg-1. The miticidal and ovicidal activities of compound IIi against spider mite were both 95% at 200 mg kg-1. Furthermore, a trivial change at 4-position of pyrazole ring would lead to great changes in properties and activities, which can easily be deduced by comparing the activities of compounds in series I (4-chloro-pyrazole compounds) with corresponding compounds in series II (4-hydro-pyrazole compounds), especially from the miticidal and ovicidal activities of Ii and IIi against spider mite.
- Song, Hongjian,Liu, Yuxiu,Xiong, Lixia,Li, Yongqiang,Yang, Na,Wang, Qingmin
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experimental part
p. 1470 - 1479
(2012/05/04)
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- BENZPYRAZOL DERIVATIVES AS INHIBITORS OF PI3 KINASES
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The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
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Page/Page column 110-111
(2009/12/28)
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- 1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists
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A new series of 1,3-dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives has been identified as potent A2B adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A2B, A1, A2A, and A3 adenosine receptors. N-(4-chloro-phenyl)-2-[3-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-5-methyl-pyrazol-1-yl] (11c) showed a high affinity for the human A2B adenosine receptor Ki = 7 nM and good selectivity (A1, A2A, A3/A2B > 140). Synthesis and SAR of this novel class of compounds is presented herein.
- Tabrizi, Mojgan Aghazadeh,Baraldi, Pier Giovanni,Preti, Delia,Romagnoli, Romeo,Saponaro, Giulia,Baraldi, Stefania,Moorman, Allan R.,Zaid, Abdel Naser,Varani, Katia,Borea, Pier Andrea
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p. 2419 - 2430
(2008/09/21)
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- Agonist lead identification for the high affinity niacin receptor GPR109a
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A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of pyrazole acid derivatives. Further elaboration of these compounds provided a series of 5,5-fused pyrazoles to be used as lead compounds for further optimization.
- Gharbaoui, Tawfik,Skinner, Philip J.,Shin, Young-Jun,Averbuj, Claudia,Jung, Jae-Kyu,Johnson, Benjamin R.,Duong, Tracy,Decaire, Marc,Uy, Jane,Cherrier, Martin C.,Webb, Peter J.,Tamura, Susan Y.,Zou, Ning,Rodriguez, Nathalie,Boatman, P. Douglas,Sage, Carleton R.,Lindstrom, Andrew,Xu, Jerry,Schrader, Thomas O.,Smith, Brian M.,Chen, Ruoping,Richman, Jeremy G.,Connolly, Daniel T.,Colletti, Steven L.,Tata, James R.,Semple, Graeme
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p. 4914 - 4919
(2008/02/12)
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- Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a
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A series of 5-alkyl pyrazole-3-carboxylic acids were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niacin receptor, GPR109b. A further series of 4-fluoro-5-alkyl pyrazole-3-carboxylic acids were shown to display similar potency. One example from the series was shown to have improved properties in vivo compared to niacin.
- Skinner, Philip J.,Cherrier, Martin C.,Webb, Peter J.,Shin, Young-Jun,Gharbaoui, Tawfik,Lindstrom, Andrew,Hong, Vu,Tamura, Susan Y.,Dang, Huong T.,Pride, Cameron C.,Chen, Ruoping,Richman, Jeremy G.,Connolly, Daniel T.,Semple, Graeme
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p. 5620 - 5623
(2008/04/02)
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- Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction
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Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R1 is C1 to C3 alkyl substituted with C3 to C6 cycloalkyl, CONR5R6 or a N-linked heterocyclic group; (CH2)nHet or (CH2)nAr; R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy; R4 is SO2NR7R8; R5 and R6 are each independently selected from H and C1 to C4 alkyl optionally substituted with C1 to C4 alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R7 and R8, together with the nitrogen atom to which they are attached, form a 4-R10-piperazinyl group; R10 is H or C1 to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; H is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction.
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Page column 44
(2010/02/06)
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- Therapeutic agents
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The invention relates anhydrous para-toluenesulphonic acid salts of 3-ethyl-5-[5-(4-ethylpiperazin-1-ylsulphonyl)-2-(2-methoxyethoxy) pyridin-3-yl]-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo [4,3-d]pyrimidin-7-one having the formula (I): a process for
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Page column 9
(2010/11/30)
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- Novel process for the preparation of pyrazoles
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A “one-pot” process is described herein for the production of pyrazole compounds of general formula (II) comprising the steps of reacting a compound of general formula (III) with an acylating agent in the presence of a base and an optional activating agent followed by the addition of a hydrazine compound in situ.
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- Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction
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Compounds of the formulae (IA) and (IB): wherein R1is C1to C3alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted by one or more substitutents selected from C1to C4alkoxy; halo; CN; CF3; OCF3or C1to C4alkyl wherein said C1to C4alkyl group is optionally substituted by C1to C4haloalkyl or haloalkoxy either of which is substituted by one or more halo atoms; R2is C1to C6alkyl and R13is OR3or NR5R6, or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).
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- Process for the preparation of pyrazolo [4,3-d] pyrimidin-7-ones-3-pyridylsulphonyl compounds and intermediates thereof
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A process is provided for the preparation of compounds of formula (I) herein comprising reacting a compound of formula (II), (III) or (IV) in the presence of -OR and a hydroxide trapping agent or in the case of compounds of formula (IV) reacting in the presence of an auxiliary base and a hydroxide trapping agent (i.e. -OR is substituted by the auxiliary base), wherein X is a leaving group and R1 to R4 are as defined above.
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- Process for preparation of pyrazolo[4,3-d]pyrimidin-7-ones and intermediates thereof
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A process is provided for the preparation of a compound of formulae (IA) (sidenafil) and (IB) comprising reacting a compound of formula (IIA) and (IIB) respectively in the presence of—OR, wherein R in the case of formation of compound (IA) is CH2CH3and R in the case of formation of compound (IB) is CH2CH2CH3, where X is a leaving group:
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- Pyrazolodiazepines. 1,3 (and 2,3) dialkyl 4,6 dihydro 8 arylpyrazolo[4,3 e][1,4] diazepin 5 ones as antianxiety agents
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A series of 1, 3 (and 2, 3) dialkyl 4, 6 dihydro 8 arylpyrazolo [4, 3 e][1, 4] diazepin 5 ones was synthesized and evaluated for psychotropic activity. Intermediates are new dialkylnitropyrazolyl aryl ketones prepared from dialkylnitropyrazolecarboxylic acids. Many of these pyrazolodiazepines exhibit high CNS activity in animals. One compound, 1 ethyl 4, 6 dihydro 3 methyl 8 phenylpyrazolo [4, 3 e] [1, 4] diazepin 5 (1H) one is about as potent as diazepam as an antianxiety agent with less sedative properties and is being studied in the clinic.
- DeWald,Nordin,L'Italien,Parcell
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p. 1346 - 1354
(2007/10/04)
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