- The structure modification of seven-membered aza-brigded neonicotinoids in order to investigate their impact on honey bees
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In order to explore the relationship between the structure and the toxicity to honey bees of seven-membered aza-bridged neonicotinoids, 16 novel seven-membered aza-bridged neonicotinoid analogues are synthesized by replacing the pyridine ring, and changing the substituents on the pyridine ring, the electron-withdrawing group NO2 and the imidazole ring of our previously developed aza-bridged neonicotinoid 1-[(6-chloropyridin-3-yl)methyl)]-10-(2,5-dimethylphenyl)-9-nitro-2,3,5,6,7,8-hexahydro-1H-5,8-epiminoimidazo azepine (C-29). The insecticidal bioactivities against cowpea aphid (Aphis craccivora) and the bee toxicities of these compounds are tested. Some of the title compounds present good insecticidal activities against cowpea aphid. The results also show that some of the title compounds exhibit lower bee toxicity than that of C-29 and imidacloprid. This suggests that changing the substituents on the neonicotinoids can influence the toxicity toward honey bees of these analogues.
- Cao, Xiaofeng,Chen, Xi,Chen, Yuce,Li, Zhong,Xu, Xiaoyong
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p. 835 - 844
(2021/05/29)
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- A New Synthesis of 2-Aminoindoles and 6-Aminopyrrolo[3,2- d ]pyrimidines from π-Deficient 1,2-Dihaloarenes and Geminal Enediamines
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An efficient approach for the synthesis of fused 2-aminopyrroles via geminal enediamines and π-deficient 1,2-dihaloarenes is presented. The two-step methodology includes aromatic nucleophilic substitution of the activated halogen of dihaloarene with enediamine C-nucleophilic center followed by Cu-catalyzed intramolecular N-arylation. This approach allows access to a variety of 2-amino-6-nitroindoles and 6-aminopyrrolo[3,2-d]pyrimidines (including N-mono- and N,N-disubstituted) in moderate and good yields under mild conditions.
- Mishina, Maria S.,Ivanov, Alexander Yu.,Lobanov, Pavel S.,Dar'In, Dmitrii V.
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p. 2851 - 2862
(2016/08/30)
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- Microwave-Assisted Bohlmann-Rahtz Synthesis of Highly Substituted 2-Aminonicotinates
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Microwave irradiation of 2-carbethoxyacetamidine and an ethynyl ketone under acidic or basic conditions in ethanol at 150 °C for 1.5 hours facilitated Bohlmann-Rahtz pyridine synthesis to give highly substituted ethyl 2-aminonicotinates with total regiocontrol and in reasonable to excellent yield, following purification by immobilization upon an acidic resin.
- Bagley, Mark C.,Alnomsy, Ayed,Temple, Scott J.
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supporting information
p. 1728 - 1732
(2016/07/06)
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- BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
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Paragraph 0412
(2015/06/25)
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- SUBSTITUTED HYDRAZIDE COMPOUNDS AND USE THEREOF
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The invention relates to substituted hydrazide compounds as shown by general formula I, including geometrical isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, and use of the same, wherein the substitutents Ar and R have the same meanings as given in the Description. The invention further relates to the use of compounds of general formula I in the preparation of medicament for the treatment and/or prevention of cancer and other proliferative diseases.
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Page/Page column 15
(2012/06/16)
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- SUBSTITUTED HYDRAZIDE COMPOUNDS AND APPLICATION THEREOF
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The invention relates to substituted hydrazide compounds as shown by general formula I, including geometrical isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, and use of the same, wherein the substitutents Ar and R having the same meanings as given in the Description. T The invention further relates to the use of compounds of general formula I in the preparation of medicament for the treatment and/or prevention of cancer and other proliferative diseases.
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Page/Page column 17
(2012/07/03)
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- Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines
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A series of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines have been synthesised, characterised and tested for their in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity. The compounds were prepared from ethyl cyanoacetate and α-bromoacetophenones via the 2-amino-3-ethoxycarbonyl-5- aryl-pyrroles and 4-chloro-6-arylpyrrolopyrimidines. Aromatic substitution with benzylic amines was performed by conventional thermal substitution, and palladium catalysed coupling. The two methods resulted in similar yields, but the palladium coupling had the benefit of lower chemical consumption and reduced reaction times. Eight of the new compounds had IC50 values in the range of 2.8-9.0 nM. Four of these have a fluorine atom positioned at sites otherwise potentially susceptible to oxidative metabolism. Structural variation of the 6-aryl group indicated that the inhibitory action was only moderately sensitive to modifications in this fragment. However, the potency depended strongly on the structure of the aromatic part of the 4-amino group, and any aromatic substitution except fluorine reduced the in vitro activity. The cellular EGFR internalization response of selected compounds was evaluated using HeLa cells. Three fluorinated derivatives had a pronounced effect in inhibiting EGFR internalization.
- Kaspersen, Svein Jacob,Sorum, Christopher,Willassen, Veronica,Fuglseth, Erik,Kjobli, Eli,Bjorkoy, Geir,Sundby, Eirik,Hoff, Brd Helge
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scheme or table
p. 6002 - 6014
(2012/01/02)
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- FUSED BICYCLIC PYRIMIDINES AS PTK INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to fused bicyclic pyrimidine containing zinc- binding moiety based derivatives that have unique properties as protein tyrosine kinase (PTK) inhibitors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 70
(2008/06/13)
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- MULTI-FUNCTIONAL SMALL MOLECULES AS ANTI-PROLIFERATIVE AGENTS
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The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.
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Page/Page column 254-255
(2008/06/13)
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- TRIAZOLOPYRIDINE DERIVATIVES AS HERBICIDES
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Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
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Page/Page column 53
(2008/06/13)
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- New carboxylic acid amides of the pyrrole series: Synthetic routes and biological aspects
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Complex II inhibitors play an important role in agrochemical fungicide research and have been known for more than 40 years. With the introduction of ortho-substituted heterocyclic amides, a breakthrough in activity level and spectrum within this class was achieved. In the meantime all major agrochemical companies have entered this field. In this paper, a special complex II subclass, the pyrrole carboxamides, will be introduced in more detail and the synthesis of selected compounds as well as a short biological SAR analysis of the pyrrole subclass will be discussed.
- Walter, Harald
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scheme or table
p. 351 - 362
(2009/01/31)
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- A facile construction of the 3,6-diamino-1,2,3,4-tetrahydropyridine-4-one scaffold: synthesis of N-3 to carbon replacement analog of TAN-1057A/B
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A facile construction of the 3,6-diamino-1,2,3,4-tetrahydropyridine-4-one class of compounds is described. Compound 2, a carbon analog at the N-3 position of TAN-1057A/B, was synthesized using this approach.
- Zhang, Lijun,Kim, Choung U.,Xu, Lianhong
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p. 3273 - 3275
(2008/02/02)
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- Novel compounds and compositions for treating diseases asociated with protease activity
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Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.
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- Novel 2-amino-1,4-dihydropyridine calcium antagonists. I. Synthesis and antihypertensive effects of 2-amino-1,4-dihydropyridine derivatives having nitroxyalkoxycarbonyl groups at 3- and/or 5-position
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Novel 2-amino-1,4-dihydropyridine derivatives, which contain nitroxy-alkoxycarbonyl groups at the 3- and/or 5-position, were synthesized and their pharmaceutical effect was evaluated in spontaneously hypertensive rats. The structure-activity relationships are discussed in terms of potency, onset-rapidity, and duration of antihypertensive activity. Remarkably prolonged duration of antihypertensive action was observed when a tertiary amino group was introduced on either side of an ester chain.
- Kobayashi,Inoue,Kita,Yoshiya,Nishino,Oizumi,Kimura
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p. 788 - 796
(2007/10/02)
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- HMG-COA REDUCTASE-INHIBITING SUBSTITUTED AMINO-PYRIDINES
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HMG-COA reductase-inhibiting compounds of the formula STR1 in which X represents a group of the formula--CH 2--CH 2--or--CH=CH--,R represents a group of the formula STR2 R 1 represents optionally substituted aryl, R 2 represe
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