- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
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This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said che
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- Novel piperazine based compounds as potential inhibitors for SARS-CoV-2 Protease Enzyme: Synthesis and molecular docking study
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Structurally diverse piperazine-based compounds hybrid with thiadiazole, isatin or with sulfur/nitrogen, functionalities were synthesized. The structures of the new compounds were established based on their spectral data and elemental analysis. The physicochemical, bioactivity scores and pharmacokinetic behavior of all the prepared ligands were evaluated using in silico computational tools. The new piperazine ligands have been screened for their inhibition activity against SARS-CoV-2 protease enzyme using molecular docking analysis. The docking studies showed that all the ligands have been docked with negative dock energy onto the target protease protein. Moreover, Molecular interaction studies revealed that SARS-CoV-2 protease enzyme had strong hydrogen bonding interactions with piperazine ligands. The present in silico study thus, provided some guidance to facilitate drug design targeting the SARS-CoV-2 main protease.
- El-atawy, Mohamed,El-sadany, Samer K.,Hamed, Ezzat A.,Mosa, Tawfik M.,Omar, Alaa Z.
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- Dihalopropenyl ether compounds,d and preparation and application thereof
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The invention discloses dihalopropenyl ether compounds, preparation and application thereof. The compound is shown in a formula (I), wherein Q, R, R1, R2, R3, R4, R5, n, and v in the formula are defined in the description. The compounds shown in the formula (I) have insecticidal and/or bactericidal biological activity, and has very high activity particularly on pests such as mythimna separata and plutella xylostella.
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Paragraph 0081; 0083
(2017/11/16)
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- Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors
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The structure-activity relationship studies of a novel series of carboxylic acid derivatives of pyridine-carboxamides as DGAT-1 inhibitors is described. The optimization of the initial lead compound 6 based on in vitro and in vivo activity led to the disc
- Ting, Pauline C.,Lee, Joe F.,Zorn, Nicolas,Kim, Hyunjin M.,Aslanian, Robert G.,Lin, Mingxiang,Smith, Michelle,Walker, Scott S.,Cook, John,Van Heek, Margaret,Lachowicz, Jean
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p. 985 - 988
(2013/03/13)
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- SUBSTITUTED AMIDE DERIVATIVES AS DGAT-1 INHIBITORS
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Described herein are compounds of formula I. The compounds of formula I act as DGAT-1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
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- Synthesis and solid state study of pyridine- and pyrimidine-based fragment libraries
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A library of pyridines and pyrimidines has been synthesised in excellent yields employing microwave and flow chemistry methodologies. Work-up bottlenecks have been facilitated substantially by the use of supported reagents and many of the final compounds have been studied in the solid state by single crystal X-ray diffraction.
- Spencer, John,Patel, Hiren,Callear, Samantha K.,Coles, Simon J.,Deadman, John J.
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p. 5905 - 5909
(2011/11/14)
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- INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
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The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).
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- INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
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The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (DGAT) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below:
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- Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability
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To improve antifungal activities, water solubility and bioavailability, a series of novel analogues of itraconazole-containing pyridine rings were designed and synthesized. Their antifungal activities were evaluated in vitro against six clinically important fungi by measuring the minimal inhibitory concentrations (MICs). Most of the compounds showed more potent antifungal activities than that of itraconazole. In particular, the analogues 30d, 30c, 31c, and 36d exhibited much higher solubility and bioavailability than that of itraconazole. The bioavailability of 36d (42.2%) was five times higher than that of itraconazole (8%) and was negative for genetic toxicology in the Ames test.
- Liu, Yu,Liu, Zining,Cao, Xufeng,Liu, Xin,He, Huili,Yang, Yushe
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scheme or table
p. 4779 - 4783
(2011/09/20)
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- INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
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The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.
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Page/Page column 182
(2010/07/10)
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- Synthesis and antibacterial activities of eperezolid analogs with glycinyl substitutions
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A series of eperezolid analogs with glycinyl substitutions were prepared and their antibacterial activities were studied against a panel of susceptible and resistant Gram-positive bacteria. The compounds with N-arylacyl or N-heteroarylacyl glycinyl struct
- Wang, Xiao-Jun,Wu, Ning,Du, Guang-Jian,Zhao, Shuang-Qi,Yan, Ming,Gu, Lian-Quan
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scheme or table
p. 377 - 385
(2009/10/23)
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- NOVEL HETEROCYCLES
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Described are novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs th
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Page/Page column 77-78
(2009/09/05)
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- STEAROYL COA DESATURASE INHIBITORS
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The present invention relates to novel Stearoyl CoA desaturase (SCD) inhibitors and uses thereof for treating diseases, conditions and/or disorders modulated by a Stearoyl CoA desaturase enzyme. The SCD inihibitors have the formula (I) or a pharmaceutical
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Page/Page column 27
(2010/11/30)
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- Novel heterocycles
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The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prod
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Page/Page column 43
(2010/11/27)
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- NOVEL HETEROCYCLES
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The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prod
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Page/Page column 71-72
(2010/11/28)
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- COMPOUNDS
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The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
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Page/Page column 43-44
(2010/11/23)
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- PIPERAZINE DERIVATIVES AS GLYT1 INHIBITORS
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The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
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Page/Page column 53-54
(2010/11/23)
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- Syntheses and antibacterial activity of a series of 3-(pyridine-3-yl)-2- oxazolidinone
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The syntheses of substituted piperazinyl pyridyl oxazolidinones 8-16 are described. Their in vitro activities against Gram-positive organisms such as Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus and enterococcus were evaluated by minim
- Cui, Yingjie,Dang, Yaxian,Yang, Yushe,Zhang, Shuhua,Ji, Ruyun
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p. 209 - 214
(2007/10/03)
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- Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2- yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist
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High throughput screening using the recombinant human TRPV1 receptor was used to identify a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands. Exploration of the structure-activity relationships by parallel synthesis identified t
- Swanson, Devin M.,Dubin, Adrienne E.,Shah, Chandra,Nasser, Nadia,Chang, Leon,Dax, Scott L.,Jetter, Michele,Breitenbucher, J. Guy,Liu, Changlu,Mazur, Curt,Lord, Brian,Gonzales, Lisa,Hoey, Kenway,Rizzolio, Michele,Bogenstaetter, Michael,Codd, Ellen E.,Lee, Doo H.,Zhang, Sui-Po,Chaplan, Sandra R.,Carruthers, Nicholas I.
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p. 1857 - 1872
(2007/10/03)
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- Bioisosteric bensamide derivatives and their use as apob-100 secretion inhibitors
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The present invention relates to A compound of formula (I) wherein A, U, V, X, Z, R1, Y, R2 and R3 are defined in the description or a physiologically acceptable salt, solvate or derivative thereof, to compositions and pro
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Page/Page column 10
(2010/02/05)
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- PHENYLPYRIDINE CARBONYL PIPERAZINE DERIVATIVE
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The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (whereinR1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like,R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like,R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, andn: 0 or 1).
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- Identification of metabolites of azaperone in horse urine
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Two metabolites of the tranquilizer azaperone were extracted from alkalinized horse urine after treatment with β-glucuronidase/sulfatase from limpets (Patella vulgata). The metabolites were identified by a combination of independent chemical synthesis and GC/MS and 1H NMR analysis. The metabolites were identified as 1-(fluorophenyl)-4-[4-(5-hydroxy-2-pyridinyl)- 1-piperazinyl]-1-butanol, designated as 5'-hydroxyazaperol, and 1- (fluorophenyl)-4-[4-(5-hydroxy-2-pyridinyl)-1-piperazinyl]-1-butanone, designated as 5'-hydroxyazaperone. A TLC screening test was developed for detecting both metabolites in basic extracts of horse urine treated with β- glucuronidase/sulfatase. The screening test was used to detect azaperone metabolites in extracts of horse urine collected for 24 h alter intravenous administration of azaperone. The administration of azaperone to horses was confirmed by GC/MS identification of 5'-hydroxyazaperone and 5'- hydroxyazaperol from basic extracts of horse urine treated with β- glucuronidase/sulfatase. The extracted metabolites were treated with bis(trimethylsilyl)acetamide to produce trimethylsilyl (TMS) ether derivatives, and mass spectra and retention times were compared to those of the synthesized metabolites treated in the same manner.
- Sams, Richard A.,Gerken, Diane F.,Detra, Randall L.,Stanley, Scott D.,Wood, William E.,Tobin, Thomas,Yang, Jyan-Ming,Tai, Hsin-Hsinng,Jegananthan, Alwarsamy,Watt, David S.
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- Pharmaceutically active amines
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The aromatic amines (I), alkyl amines (II), bicyclic amines (III). STR1 cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).
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