- EIF4E INHIBITORS AND USES THEREOF
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The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.
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Paragraph 00506; 00548
(2021/09/11)
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- One-pot approach to construct benzo[4,5]thieno[3,2-b]indoles, pyrido[3′,2’:4,5]thieno[3,2-b]indoles and pyrazino[2′,3’:4,5]thieno[3,2-b]indoles based on the Fischer indole synthesis
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During this study, series of benzo[4,5]thieno[3,2-b]indoles, pyrido[3′,2’:4,5]thieno[3,2-b]indoles and pyrazino[2′,3’:4,5]thieno[3,2-b]indoles were efficiently synthesized from benzo- and pyrido- or pyrazino-fused 3-aminothiophene-2-carboxylates, respectively, using one-pot two-step strategy based on the Fischer indolization reaction. The essence of this synthetic approach is acid-promoted reaction of the 3-aminothiophene intermediates, in situ generated from the corresponding ring-fused 3-aminothiophene-2-carboxylates, with arylhydrazines to give arylhydrazones of thiophen-3(2H)-ones, followed by their indolization to afford thieno[3,2-b]indole-cored molecules.
- Irgashev, Roman A.,Steparuk, Alexander S.,Rusinov, Gennady L.
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supporting information
(2020/11/06)
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- Cu-Catalyzed Denitrogenative Transannulation of 3-Aminoindazoles to Assemble 1-Aminoisoquinolines and 3-Aminobenzothiophenes
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We disclose a novel Cu-catalyzed denitrogenative transannulation of 3-aminoindazoles to afford diverse functionalized 3-aminobenzothiophenes and 1-aminoisoquinolines, in which denitrogenative transannulation of 3-aminoindazoles is reported for the first t
- Zhou, Yao,Wang, Ya,Lou, Yixian,Song, Qiuling
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p. 8869 - 8873
(2019/09/12)
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- Red phosphorescent compound and organic light-emitting device using same
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The invention relates to a red phosphorescent compound and an organic light-emitting tube device using the same, in particular to a soluble phosphorescent compound with excellent color purity, high brightness and high light-emitting efficiency, and an organic light emitting diode (OLED) device using the same. The structural formula of the phosphorescent compound is shown as (I) (please see the specifications for the formula); in the structural formula (I), Z is independently selected from the following structure (please see the specifications for the formula (I)), wherein Ar is independently selected from one of C6-C30 aryl and C2-C30 heteroaryl, the C6-C30 aryl is selected from one of phenyl, naphthyl, xenyl, terphenyl and phenanthryl, and the C2-C30 heteroaryl is selected from one of pyridyl, bipyridyl, quinolyl, isoquinolyl, phenanthroline and triazinyl. According to the phosphorescent compound, the chemical formula shown as the formula (I) is used as a light-emitting layer of the OLED device, and the phosphorescent compound has the excellent color purity, excellent brightness, and the prolonged durability effect.
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Page/Page column 27
(2019/05/08)
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- 3-ALKYL-4-AMIDO-BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS
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The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
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Paragraph 0614-0615
(2016/08/29)
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- 2-Amino-4-aryl thiazole: A promising scaffold identified as a potent 5-LOX inhibitor
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Human 5-lipoxygenase (5-LOX) is an important enzyme in the biosynthesis of leukotrienes and is a target for asthma and allergy treatment. Zileuton is the only drug currently marketed that targets this enzyme (IC50 ～ 1 μM). So, the development of novel lead compounds is highly desirable. A series of 2-aryl indole, thiazolopyrazole acid, oxadiazolobenzothiophene, 1,4-disubstituted-1,2,3-triazole, 2-amino-4-aryl thiazole and 4,4′-(1,4-phenylene)bis(1,3-thiazole) derivatives when tested against this enzyme resulted in the identification of a potent compound (1d), p-fluoro substituted 2-amino-4-aryl thiazole, with an IC50 of ～10 μM. Another lead compound identified is (4a), a thiazolopyrazole acid derivative (IC50 ～ 40 μM). All the compounds exhibit poor DPPH radical scavenging activity which suggests that their action occurs not due to the disruption of the redox cycle of iron present in the enzyme (unlike zileuton) but through competitive inhibition, since the Vmax remains constant but the Km increases with an increase in inhibitor concentration. Molecular docking of 1d and 4a to the active site of 5-LOX also supports the experimental data, and suggests that their possible mechanism of action is through competitive inhibition. The current study identifies a promising lead molecule which could be improved further to match the activity of the commercial drug.
- Sinha, Shweta,Sravanthi,Yuvaraj,Manju,Doble, Mukesh
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p. 19271 - 19279
(2016/03/01)
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- Microwave-assisted synthesis of 3-aminobenzo[b]thiophene scaffolds for the preparation of kinase inhibitors
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Microwave irradiation of 2-halobenzonitriles and methyl thioglycolate in the presence of triethylamine in DMSO at 130°C provides rapid access to 3-aminobenzo[b]thiophenes in 58-96% yield. This transformation has been applied in the synthesis of the thieno
- Bagley, Mark C.,Dwyer, Jessica E.,Molina, Maria D. Beltran,Rand, Alexander W.,Rand, Hayley L.,Tomkinson, Nicholas C. O.
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p. 6814 - 6824
(2015/06/25)
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- CONDENSED CYCLIC COMPOUND, AND ORGANIC LIGHT EMITTING DEVICE INCLUDING THE SAME
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Disclosed are a condensed ring compound and an organic light emitting device comprising the condensed ring compound. The organic light emitting device comprises: a first electrode; a second electrode facing the first electrode; and an organic layer interposed between the first electrode and the second electrode, wherein the organic layer comprises the condensed ring compound.COPYRIGHT KIPO 2015
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Paragraph 1168
(2016/10/08)
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- An Aryne-Based Route to Substituted Benzoisothiazoles
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The combination of arynes, generated using fluoride from the corresponding 2-(trimethylsilyl)aryl triflates, and 3-hydroxy-4-aminothiadiazoles leads to the selective formation of 3-amino-substituted benzo[d]isothiazoles. Variation of the substitution pattern of the aryne precursor, and of the thiadiazole, is possible, with the target heterocycles being obtained in good to excellent yields. In all cases, use of 3-hydroxy-4-aminothiadiazoles leads to incorporation of the amino-substituent in the product heterocycle.
- Chen, Yiding,Willis, Michael C.
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supporting information
p. 4786 - 4789
(2015/10/12)
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- METHOD FOR PROMOTING PLANT GROWTH
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The present invention provides a method for promoting plant growth, which comprises treating a plant with at least one compound selected from a group consisting of a compound represented by the following Formula (1): and an agriculturally acceptable salt thereof, provided that a method for promoting plant growth which comprises treating plants with a compound corresponding to any one of the following (1) to (5) and an agriculturally acceptable salt thereof is excluded: (1) 4-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (2) 5-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (3) 6-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (4) 7-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, and (5) Benzo[b]thiophene-2-carboxylic acid.
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Paragraph 0388
(2015/11/16)
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- Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b] thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents
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Two new series of inhibitors of tubulin polymerization based on the 2-(alkoxycarbonyl)-3-(3′,4′,5′-trimethoxyanilino)benzo[b] thiophene and thieno[2,3-b]pyridine molecular skeletons were synthesized and evaluated for antiproliferative activity on a panel
- Romagnoli, Romeo,Baraldi, Pier Giovanni,Kimatrai Salvador, Maria,Preti, Delia,Aghazadeh Tabrizi, Mojgan,Bassetto, Marcella,Brancale, Andrea,Hamel, Ernest,Castagliuolo, Ignazio,Bortolozzi, Roberta,Basso, Giuseppe,Viola, Giampietro
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supporting information
p. 2606 - 2618
(2013/05/09)
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- Design and synthesis of condensed thienocoumarins by Suzuki-Miyaura reaction/lactonization tandem protocol
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A concise and efficient approach to a series of chromen-4-ones with fused thiophene ring has been developed using the Suzuki-Miyaura reaction of bromothiophene-2- and 3-carboxylates with 2-methoxyboronic acids and subsequent cyclization of prepared alkyl (2-methoxy)aryl thiophene-2- and 3-carboxylates under the action of BBr3/KOtBu. Starting bromothiophenes are easily obtained from corresponding commercially available aminothiophenes by diazotization/bromination reaction.
- Iaroshenko, Viktor O.,Ali, Sajid,Mkrtchyan, Satenik,Gevorgyan, Ashot,Babar, Tariq Mahmood,Semeniuchenko, Volodymyr,Hassan, Zahid,Villinger, Alexander,Langer, Peter
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supporting information
p. 7135 - 7139
(2013/01/15)
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- Tricyclic aminopyrimidine histamine H4 receptor antagonists
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This report discloses the development of a series of tricyclic histamine H4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H4 receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model.
- Savall, Brad M.,Gomez, Laurent,Chavez, Frank,Curtis, Michael,Meduna, Steven P.,Kearney, Aaron,Dunford, Paul,Cowden, Jeffery,Thurmond, Robin L.,Grice, Cheryl,Edwards, James P.
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scheme or table
p. 6577 - 6581
(2011/12/04)
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- Synthesis of a series of novel thieno-and benzothieno[3,2-d]pyrimidin-4(3H) -ones
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A series of novel thieno- and benzothieno[3,2-d]pyrimidin-4(3H)-ones is synthesised via condensation of 3-amino(benzo)thiophene-2-carboxylates with various lactams. Georg Thieme Verlag Stuttgart New York.
- Abdillahi, Ismail,Kirsch, Gilbert
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scheme or table
p. 1314 - 1318
(2011/05/19)
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- BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES SUBSTITUTED WITH AMIDE, PROCESS FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
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The present invention relates to a novel benzofuran or benzothiophene derivative substituted with amide. The inventive benzofuran or benzothiophene derivative substituted with amide effectively inhibits ischemic cell death, and thus, can be advantageously
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Page/Page column 22
(2009/05/28)
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- Modular access to heterocycles: Methyl 3-aminobenzo[b]thiophene-2- carboxylate-thiourea linkage or pyrimidine-4-one-2-thione formation
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Modular conditions for the formation of thioureas or pyrimidine-4-one-2- thiones connected to the benzo[b]thiophene, benzene and indole structures were performed. A benzo[b]thiophene isothiocyanate derivative was used as a model to study the condensation with simple aromatic amines and amino-l-sorbose derivative. The construction of pyrimidine-4-one-2-thiones using basic conditions afforded efficiently new heterocyclic aromatics, which were further transformed using the alkylated sulfur as a leaving group in palladium-catalyzed cross-coupling reactions.
- Rousseau, Jolanta,Krisciuniene, Vilija,Rimkeviciute, Ilona,Rousseau, Cyril,Amankaviciene, Virgine,Sackus, Algirdas,Tatibouet, Arnaud,Rollin, Patrick
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body text
p. 339 - 348
(2010/04/26)
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- Benzofuro- and benzothienopyrimidine modulators of the histamine H4 receptor
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Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions media
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Page/Page column 21
(2008/06/13)
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- Structure-activity relationships in the binding of chemically derivatized CD4 to gp120 from human immunodeficiency virus
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The first step in HIV infection is the binding of the envelope glycoprotein gp120 to the host cell receptor CD4. An interfacial "Phe43 cavity" in gp120, adjacent to residue Phe43 of gp120-bound CD4, has been suggested as a potential target for therapeutic intervention. We designed a CD4 mutant (D1D2F43C) for site-specific coupling of compounds for screening against the cavity. Altogether, 81 cysteine-reactive compounds were designed, synthesized, and tested. Eight derivatives exceeded the affinity of native D1D2 for gp120. Structure-activity relationships (SAR) for derivatized CD4 binding to gp120 revealed significant plasticity of the Phe43 cavity and a narrow entrance. The primary contacts for compound recognition inside the cavity were found to be van der Waals interactions, whereas hydrophilic interactions were detected in the entrance. This first SAR on ligand binding to an interior cavity of gp120 may provide a starting point for structure-based assembly of small molecules targeting gp120-CD4 interaction.
- Xie, Hui,Ng, Danny,Savinov, Sergey N.,Dey, Barna,Kwong, Peter D.,Wyatt, Richard,Smith III, Amos B.,Hendrickson, Wayne A.
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p. 4898 - 4908
(2008/03/11)
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- CYCLIC N-HYDROXY IMIDES AS INHIBITORS OF FLAP ENDONUCLEASE AND USES THEREOF
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Acylic n-hydroxy imides and their use in pharmaceutical compositions and in the inhibition of flap endonuclease are disclosed.
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Page/Page column 39-40
(2010/10/19)
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- Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents
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Heterocyclic analogues of 1192U90, 2-amino-N-(4-(4-(1,2-benzisothiazol- 3-yl)-1-piperazinyl)-butyl)benzamide hydrochloride (1), were prepared and evaluated as potential antipsychotic agents. These analogues were evaluated in vitro for their binding to the dopamine D2, serotonin 5-HT2, and serotonin 5-HT(1a) receptors and in vivo for their ability to antagonize the apomorphine-induced climbing response in mice. Nine different types of heterocyclic carboxamides were studied in this investigation (i.e., pyridine- , thiophene-, benzothiophene-, quinoline-, 1,2,3,4-tetrahydroquinoline-, 2,3- dihydroindole-, indole-, benzimidazole-, and indazolecarbox-amides). Two derivatives exhibited potent in vivo activities comparable to 1: 3-amino-N- (4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2-pyridinecarboxamide (16) and 3-amino-N-(4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2- thiophenecarboxamide (29). Furthermore, these derivatives were found to be much less active in behavioral models predictive of extrapyramidal side effects than in the mouse climbing assay, which predicts antipsychotic activity. Carboxamides 16 and 29 were selected for further evaluation as potential backup compounds to 1.
- Norman, Mark H.,Navas III, Frank,Thompson, James B.,Rigdon, Greg C.
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p. 4692 - 4703
(2007/10/03)
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- Relaxation of smooth muscle in a mammal
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4-Amino-6-arylpyrimidines and salts thereof, a novel class of inhibitors of platelet aggregation and broncho-dilators in mammals, and 4-hydroxy-6-arylpyrimidines as useful intermediates.
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