- A new approach for the synthesis of novel naphthoquinone chalcone hybrid compounds
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A facile and efficient synthesis of novel naphthoquinone-based chalcone hybrids (7 and 24) via the microwave-assisted one-pot three-component reactions of 2-substituted-1,4-naphthoquinones, N,N-dimethylformamide dimethyl acetal (DMF-DMA), and acetophenone derivatives has been reported. Whereas the synthesis of hybrids 7 proceeded via a condensation, 1,4-addition, rotation, elimination, and [1,3]-H shift sequence of steps, the synthesis of hybrids 24 were formed through a three-step sequence including condensation, 1,4-addition, and elimination reactions.
- Nguyen, Ha-Thanh,Dang Thi, Tuyet Anh,Hoang Thi, Phuong,Le-Nhat-Thuy, Giang,Nguyen Thi, Quynh Giang,Nguyen Tuan, Anh,Le Thi, Tu Anh,Van Nguyen, Tuyen
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supporting information
(2021/08/27)
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- FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton’ s tyrosine kinase (Btk), and for treating disorders mediated thereby.
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Paragraph 0176; 0177
(2018/06/26)
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- FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
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Paragraph 0167; 0176; 0177
(2014/11/13)
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- Synthesis, preliminary structure-activity relationships, and in vitro biological evaluation of 6-aryl-3-amino-thieno[2,3-b]pyridine derivatives as potential anti-inflammatory agents
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In our previous study, a series of 6-aryl-3-amino-thieno[2,3-b]pyridine derivatives exhibited potent antiproliferative activities and an unique hepatocellular carcinoma (HCC)-specific anticancer activity was also observed. In further anti-inflammatory research, thienopyridine derivative 1a showed potent inhibition of nitric oxide (NO) production. So a series of thienopyridine analogues of 1a were synthesized and evaluated for anti-inflammatory activities. The structure-activity relationships (SARs) revealed that the most potent analogues 1f and 1o were identified as potent inhibitors of NO production with IC50 values of 3.30 and 3.24 μM, respectively. These results suggest that these 6-aryl-3-amino-thieno[2,3-b]pyridine derivatives might potentially constitute a novel class of anti-inflammatory agents, which require further studies.
- Liu, Huan,Li, Yi,Wang, Xiang-Ying,Wang, Bo,He, Hai-Yun,Liu, Ji-Yan,Xiang, Ming-Li,He, Jun,Wu, Xiao-Hua,Yang, Li
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supporting information
p. 2349 - 2352
(2013/05/09)
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- 3-Acyl-5-hydroxybenzofuran derivatives as potential anti-estrogen breast cancer agents: A combined experimental and theoretical investigation
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We first report the application of 3-acyl-5-hydroxybenzofurans as a scaffold to develop potential drugs for breast cancer. Seven novel derivative compounds were synthesized by using a microwave-assisted synthesis method. Those compounds exhibited different antiproliferation against human breast cancer MCF-7 cells, with the best activity of IC50 = 43.08 μM for compound 1. A Quantum Mechanics Polarized Ligand Docking (QPLD) study was carried out to investigate the binding interactions between these compounds and estrogen receptor alpha (ERα). The simulation results showed that the trend of receptor-ligand binding interactions was same as that of their antiproliferative activities. A detailed analysis indicated that compound 1 possesses the highest Van der Waals and hydrogen bond interactions compared to the other six compounds and better inhibitors are achievable by enhancing the hydrogen bond interactions. Based on these results, we addressed that 3-acyl-5-hydroxybenzofuran is an attractive scaffold for designing drugs against breast cancer.
- Li, Xiao-Yan,He, Bi-Feng,Luo, Hua-Jun,Huang, Nian-Yu,Deng, Wei-Qiao
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supporting information
p. 4617 - 4621
(2013/08/15)
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- IMMUNODETECTION AND QUANTIFICATION OF PYRAZOLOPYRIMIDINE SEDATIVES
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The invention relates to novel immunogens, antibodies, methods and kits for use in immunoassays to detect and quantify zaleplon, metabolites of zaleplon and indiplon. These are the first described immunoassays for these compounds and have greater sensitivity than alternative analytical techniques.
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Page/Page column 10
(2011/02/24)
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- NOVEL HETEROBICYCLIC COMPOUNDS
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This invention relates to novel pyrazolo-pyrimidine compounds and their use as analytical tools and in methods of treating neurological disorders, including sleep disorders such as insomnia.
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Page/Page column 42
(2010/11/29)
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- Synthesis of deuterium-labeled zaleplon-d5 as an internal standard
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Zaleplon is licensed for the short-term treatment of insomnia. Excessive usage causes side effects; hence, the drug is controlled. Identifying zaleplon in a drug abuser requires an isotope-labeled internal standard. This work presents a synthesis of stable isotope-labeled internal standard for zaleplon, zaleplon-d5, by a five-step synthetic sequence. Copyright
- Shaikh, Ajam C.,Chen, Chinpiao
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- 2-AMINOPHENYL-4-PHENYLPYRIMIDINES AS KINASE INHIBITORS
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The present invention relates to compounds of Formula: (I), or pharmaceutically acceptable salt thereof, wherein the variables are defined in the description. The compounds act as kinase inhibitors.
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Page/Page column 46
(2010/02/10)
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- Controlled-release sedative hypnotic compositions and method related thereto
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Controlled-release formulations providing a "pulsed" plasma profile of a sedative-hypnotic compounds having a particularly short half-life are provided. The formulation contains a sedative-hypnotic compound or precursor thereof that is metabolized to generate a sedative-hypnotic compound in vivo, wherein the compound has a mean plasma half life ranging from 0.1 to 2 hours; and at least one release retardant such that, following administration of the formulation to a patient, the patient has specific pulsed plasma profile for the sedative-hypnotic compound as disclosed herein. In a preferred embodiment, the sedative-hypnotic compound is NBI-34060.
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- CONTROLLED-RELEASE SEDATIVE-HYPNOTIC COMPOSITIONS AND METHODS RELATED THERETO
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Controlled-release formulations providing a "pulsed" plasma profile of a sedative-hypnotic compounds having a particularly short half-life are provided. The formulation contains a sedative-hypnotic compound or precursor thereof that is metabolized to generate a sedative-hypnotic compound in vivo, wherein the compound has a mean plasma half life ranging from 0.1 to 2 hours; and at least one release retardant such that, following administration of the formulation to a patient, the patient has specific pulsed plasma profile for the sedative-hypnotic compound as disclosed herein. In a preferred embodiment, the sedative-hypnotic compound is NBI-34060.
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- Polymorphs of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto
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Polymorphs of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide (Compound 1), and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Processes for making the same, as well as related compositions and methods are also disclosed, particularly with regard to treatment of insomnia. A polymorph Form I possessing exception physical and heat stability is provided. A polymorph Form II
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- N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1, 5-α]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto
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N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide, and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Compositions containing N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide, as well as pharmaceutically acceptable salts thereof, are also disclosed.
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- Controlled-release sedative-hypnotic compositions and methods related thereto
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Controlled-release formulations providing a “pulsed” plasma profile of a sedative-hypnotic compound having a particularly short half-life are provided. The formulation contains a sedative-hypnotic compound or precursor thereof that is metabolized to generate a sedative-hypnotic compound in vivo, wherein the compound has a mean plasma half life ranging from 0.1 to 2 hours; and at least one release retardant such that, following administration of the formulation to a patient, the patient has specified pulsed plasma profile for the sedative-hypnotic compound as disclosed herein. In a preferred embodiment, the sedative-hypnotic compound is NBI-34060.
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- Aryl and heteroaryl[[7-(3-disubstituted amino)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]methanones
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Novel aryl and heteroaryl[7-(3-substituted amino phenyl)-pyrazolo[1,5-a]pyrimidin-3-yl]methanones useful as anxiolytic, antiepileptic and sedative-hypnotic agents and as skeletal muscle relaxants, methods of using the novel compounds, compositions containing them and processes for this production.
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- Aryl and heteroaryl[7-(aryl and heteroaryl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones
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Aryl and heteroaryl[7-(aryl and heteroaryl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones which are new compounds active as anxiolytic, anticonvulsant, sedative-hypnotic and skeletal muscle relaxant agents in mammals and the novel process of making these compounds.
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