- Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide against Klebsiella pneumoniae and in Vitro Toxicity Analysis
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Klebsiella pneumoniae causes a wide range of community and nosocomial infections. The high capacity of this pathogen to acquire resistance drugs makes it necessary to develop therapeutic alternatives, discovering new antibacterial molecules. Acetamides are molecules that have several biological activities. However, there are no reports on the activity of 2-chloro-N-(4-fluoro-3-nitrophenyl)acetamide. Based on this, this study aimed to investigate the in vitro antibacterial activity of this molecule on K. pneumoniae, evaluating whether the presence of the chloro atom improves this effect. Then, analyzing its antibacterial action more thoroughly, as well as its cytotoxic and pharmacokinetic profile, in order to contribute to future studies for the viability of a new antibacterial drug. It was shown that the substance has good potential against K. pneumoniae and the chloro atom is responsible for improving this activity, stabilizing the molecule in the target enzyme at the site. The substance possibly acts on penicillin-binding protein, promoting cell lysis. The analysis of cytotoxicity and mutagenicity shows favorable results for future in vivo toxicological tests to be carried out, with the aim of investigating the potential of this molecule. In addition, the substance showed an excellent pharmacokinetic profile, indicating good parameters for oral use.
- Andrade-Júnior, Francisco,Athayde-Filho, Petr?nio,Barbosa-Filho, José,Cordeiro, Laísa,Diniz-Neto, Hermes,Ferreira, Elba,Figueiredo, Pedro,Lima, Edeltrudes,Melo, Thamara,Oliveira, Rafael,Oliveira-Filho, Abrah?o,Sousa, Aleson,Souza, Helivaldo
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Read Online
- Heterocyclic compound and application thereof
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The present disclosure relates to a heterocyclic compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereoisomer, an atropisomer, an optical isomer, a raceme, a polymorphic substance, a solvate or an isotope labeled compound thereof, a pharmaceutical composition containing the heterocyclic compound, and a pharmaceutical use thereof. The heterocyclic compound disclosed by the invention is an immunomodulator, and particularly relates to an immunomodulator of a compound for activating STING.
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Paragraph 0131-0133
(2021/06/13)
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- Therapeutic Compounds
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Compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3 and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 13
(2011/04/25)
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- BENZIMIDAZOLECARBOXAMIDES AS INHIBITORS OF FAK
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This invention relates to benzimadolecarboxamides of formula (I) which are inhibitors of focal adhesion kinase, and as such are useful for treating proliferative diseases
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Page/Page column 49
(2010/11/17)
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- Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk)
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A series of novel potent benzimidazole based inhibitors of interleukin-2 T-cell kinase (Itk) were prepared. In this report, we discuss the structure-activity relationship (SAR), selectivity, and cell-based activity for the series. We also discuss the SAR associated with an X-ray structure of one of the small-molecule inhibitors bound to ITK.
- Moriarty, Kevin J.,Takahashi, Hidenori,Pullen, Steven S.,Khine, Hnin Hnin,Sallati, Rosemarie H.,Raymond, Ernest L.,Woska Jr., Joseph R.,Jeanfavre, Deborah D.,Roth, Gregory P.,Winters, Michael P.,Qiao, Lei,Ryan, Declan,DesJarlais, Renee,Robinson, Darius,Wilson, Matthew,Bobko, Mark,Cook, Brian N.,Lo, Ho Yin,Nemoto, Peter A.,Kashem, Mohammed A.,Wolak, John P.,White, André,Magolda, Ronald L.,Tomczuk, Bruce
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scheme or table
p. 5545 - 5549
(2009/06/18)
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- Benzimidazole Derivatives, Compositions Containing Them, Preparation Thereof and Uses Thereof
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Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 12
(2008/12/08)
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- Therapeutic Compounds
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Compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3 and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 13-14
(2008/06/13)
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- COMPOUNDS, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF III
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Compounds of Formula I, or pharmaceutically acceptable salts thereof: I (chemical formula to be inserted here - please see paper copy) wherein R1, R2, R3, R4, R5, R6 and G are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 34; 35
(2008/06/13)
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- Benzimidazole derivatives and their use as cannabinoid receptor ligands
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Compounds of Formula I, or pharmaceutically acceptable salts thereof: (I) wherein R1, R2, R3, R4, and R5 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 17
(2010/10/20)
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- BENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF I
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Compounds of Formula I, or pharmaceutically acceptable salts thereof: (chemical formula to be inserted here - please see paper copy) I wherein R1, R2, R3, R4, R5, and G are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 29-30
(2008/06/13)
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- COMPOUNDS, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF IIII
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Compounds of Formula I, or pharmaceutically acceptable salts thereof (I) wherein G, R1, R2, R3, R4, and R5 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 17-18
(2010/10/20)
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- BENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF
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Compounds of Formula I or pharmaceutically acceptable salts thereof wherein G, R1, R2, R3, R4 and R5 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 19
(2010/10/20)
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- Benzimidazole derivatives and their use as cannabinoid receptor ligands I
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Compounds of Formula I, or pharmaceutically acceptable salts thereof: (I) wherein R1, R2, R3, R4, and R5 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 19
(2010/10/20)
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- COMPOUNDS, COMPOSITIONS CONTAINING THEM, PREPARATIONS THEREOF AND USES THEREOF II
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Compounds of Formulae I, or pharmaceutically acceptable salts thereof: (I) wherein R1, R2, R3, R4 and G are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 28; 78
(2010/10/20)
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- ((11-OXO-10,11-DIHYDRODIBENZO [B, F] [1, 4] OXAZEPIN-1-YL)OXY) ACETIC ACID DERIVATIVES AND RELATED COMPOUNDS AS CARDIOVASCULAR PREPARATIONS USED TO TREAT ARTERIOLOSCLEROSIS
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The invention relates to dibenzoxazepines and to a method for the production thereof, use thereof in the treatment and/or prophylaxis of illnesses, in addition to the use thereof in the production of medicaments for treating and/or for the prophylaxis of diseases, in particular cardiovascular illnesses, e.g. arteriolosclerosis, and cancers: Said dibenzoxazepines are represented by formula (I), wherein R2 represents C1-C6-alkyl, alkyl can be substituted by 1 or 2 substituents, said substituents are selected independently from each other from the group consisting of halogen, hydroxy, oxo, C1-C6-alkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, aminocarbonyl and C1-C6-alkylaminocarbonyl, R3 represents O-CH2CO2H or -O-(CH2)2CO2H, R5 represents 5- 10-membered heteroaryl, -SO2-R6 or -NR7(C=O)R8, whereby heteroaryl can be substituted by 1, 2 or 3 substituents, said substituents being selected independently from each other from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, C1-C6 alkylamino, hydroxy, C1-C6-alkyl, C1-C6-aIkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, amino-carbonyl, C1-C6-alkylaminocarbonyl, C6-C10-aryl and C3-C8-aycloalkyl. The other substituents are defined in the claims.
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Page/Page column 26
(2010/02/13)
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- BENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM, PREPARATION THEROF AND USES THEREOF
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Compounds of Formulae (IA), (IB) or pharmaceutically acceptable salts thereof; wherein Het, X1, R1, R2, R3, R3a and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 67; 140
(2010/02/11)
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- Method of producing an amide
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The present invention discloses a new method for synthesizing an amide based on a fundamental mechanistic revision of the reaction of thio acids and organic azides. Moreover, the application of this method to the selective preparation of several classes of complex amides in nonpolar and polar solvents, including water, is provided.
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Page/Page column 1; 6
(2008/06/13)
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- BENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF
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Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 28
(2008/06/13)
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- BENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF
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Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, R4, n and Ar are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 77
(2010/02/11)
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- BENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF
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Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3 and Ar are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 82-83
(2010/02/11)
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- SULFIDE DYES
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Formula (I) wherein R1 and R2 each independently from each other are a residue of an organic dye; Y1 and Y2 each independently from each other are unsubstituted or substituted, straightchain or branched, interrupted or uninterrupted -C1-C10alkylene-; -C5-C10cycloalkylene-; C5-C10arylene; or-C5-C10arylene-(C1-C10alkylene)-; Z1 and Z2 independently from each other are Formula (II) are each independently from each other hydrogen; or unsubstituted or substituted, straight-chain or branched, monocyclic or polycyclic, interrupted or uninterrupted C1-C14alkyl; C2-C14alkenyl; C6-C10aryl; C6-C10aryl-C1-C10alkyl; or C5-C10alkyl(C5-C10aryl); r, q and n independently from each other are 0 or 1, if n is 0, Z3 is hydrogen; and if n is 1, Z3 is -S-; with the proviso that the method does not comprise treating the fiber with an enzyme of the type of a protein disulfidisomerase (EC 5.3.4.1). Further, the present invention relates to novel disulfid compounds, compositions thereof, especially comprising other dyes, and to processes for their preparation.
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Page/Page column 36
(2008/06/13)
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- 2,5-DIAMINO SUBSTITUTED AZO DYES
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Disclosed are azo dyes of formula (1) , wherein R1 is hydrogen; C1-C14alkyl; hydroxy- C1-C14alkyl; C2-C14alkenyl; a radical of formula (1a) -(CH2)n1-O-(CH2)n2-CH3; a radical of formula (1b) C10aryl; or C6-C10aryl-C1-C6alkyl; R3 is hydrogen; C1-C14alkyl; C2-C14alkenyl; C6-C10aryl; C6-C10aryl-C1-C6alkyl; or CO-R6; R4 is CO-R6; R5 is C1-C14alkyl; C2-C14alkenyl; C6-C10aryl; or C6-C10aryl-C1-C6alkyl; R6 is hydrogen; C1-C14alkyl; C2-C14alkenyl; or C6-C10aryl; R7, R8, R9 and R10, independently from each other are hydrogen; or C1-C5alkyl; m is 1; or 2; An- is an anion; If m = 1, R2 is hydrogen; C1-C14alkyl; C2-C14alkenyl; a radical of formula (1a); a radical of formula (1b) ; C6-C10aryl; or C6-C10aryl-C1-C6alkyl; If m = 2, R2 is the direct bond; or C1-C14alkylene, which is optionally substituted by one or more C1-C4alkyl, or which is optionally interrupted by C5-C10arylene, -O- or -NR9R10-; R9 and R10, independently from each other are hydrogen; or C1-C5alkyl; and n1, n2, n3 and n4, independently from each other are a number from 0 to 5. The compounds are useful for the dyeing of organic material, preferably human hair.
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Page/Page column 24
(2008/06/13)
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- BENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM, PREPARATION THEREOF AND USES THEREOF
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Compounds of formula (I) or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4 and Z are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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- Benzimidazole and pyridylimidazole derivatives
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This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
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- The reaction of thio acids with azides: A new mechanism and new synthetic applications
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A new amide synthesis strategy based on a fundamental mechanistic revision of the reaction of thio acids and organic azides is presented. The data demonstrate that amines are not formed as intermediates in this reaction. Alternative mechanisms proceeding through a thiatriazoline intermediate are suggested. The reaction has been applied to the preparation of simple and architecturally complex amides that are difficult to access using conventional methods. The reaction is chemoselective, effective for unprotected substrates, and compatible with aprotic and protic solvents, including water. Copyright
- Shangguan, Ning,Katukojvala, Sreenivas,Greenberg, Rachel,Williams, Lawrence J.
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p. 7754 - 7755
(2007/10/03)
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- o-NITROANILINE DERIVATIVES. PART 10. 5- AND 6-AMINO-1H-BENZIMIDAZOLE 3-OXIDES
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Cyclisation of N-(4- or 5-acylamino-2-nitrophenyl)glycine esters in basic media gives alkyl 5- or 6-acylaminobenzimidazole-2-carboxylate N-oxides, e.g. (11a) or (11b).Acid hydrolysis of the latter, followed by the reaction of ammonia, gives the title compounds (1b) and (1c), in acceptable yield.The corresponding reaction sequence with 4-acylamino-N-cyanomethyl-o-nitroanilines also gives (1b); where the acyl group is methylsulphonyl, however, the final product is 5-methanesulphonamidobenzimidazole N-oxide (9).Compound (1b) is also obtainable from ethyl 5-nitrobenzimidazole-2-carboxylate N-oxide by reduction followed by hydrolysis.Attempts to cyclise N-(o-nitrophenyl)glycine derivatives containing a free amino group at the 5-position are unsuccessful.This failure is attributed to mesomeric deactivation of the nitro group by the amino lone pair.
- McFarlane, Michael D.,Moody, David J.,Smith, David M.
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p. 691 - 696
(2007/10/02)
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- 4-Fluoro-3-nitro anilines
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Compounds of formula: SPC1 Wherein W is EQU1 or EQU2 in which: (a) R4 and R5 are 5 identical or different and represent hydrogen, monovalent aliphatic, substituted or unsubstituted aryl, aralkyl and cycloalkyl, providing that not more than 1 of R4 or R5 is hydrogen, and (b) R3 is a divalent aliphatic radical.
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