- 5-(THIOPHEN-2-YL)-1H-TETRAZOLE DERIVATIVES AS BCKDK INHIBITORS USEFUL FOR TREATING VARIOUS DISEASES
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Described herein are compounds of Formula (I), wherein R1, R2, and R3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors
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Page/Page column 77
(2021/01/23)
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- Synthesis of functionalized hydroxy-thiophene motifs as amido- and sulfonamido-phenol bioisosteres
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Novel highly substituted hydroxy thiophene motifs were designed and synthesized as viable amido phenol and sulfonamido phenol bioisosteres. Hydroxy group-directed regioselective bromination and palladium-catalyzed amination of thienyl bromide via Buckwald
- Chao, Jianhua,Taveras, Arthur G.,Aki, Cynthia J.
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scheme or table
p. 5005 - 5008
(2009/12/01)
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- DNA-BINDING POLYMERS
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Methods and compositions are provided for forming complexes between dsDNA and novel DNA-binding polymers comprising N-terminal thiophene-containing moieties which exhibit selectivity for T-A base pairs. By appropriate choice of target sequences and DNA-binding polymers, complexes comprising polymer-DNA are obtained with high association constants. The formation of complexes can be used for identification of specific dsDNA sequences, for inhibiting gene transcription, and as a therapeutic for inhibiting proliferation of undesired cells or modulation of expression of specific genes.
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Page/Page column 16
(2009/07/03)
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- DNA-binding polymers
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Methods and compositions are provided for forming complexes between dsDNA and novel DNA-binding polymers comprising N-terminal thiophene-containing moieties which exhibit selectivity for T-A base pairs. By appropriate choice of target sequences and DNA-binding polymers, complexes comprising polymer-DNA are obtained with high association constants. The formation of complexes can be used for identification of specific dsDNA sequences, for inhibiting gene transcription, and as a therapeutic for inhibiting proliferation of undesired cells or modulation of expression of specific genes.
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- 3,5-Disubstituted-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
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Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, R2, A, B and D are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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- Shape selective recognition of T·A base pairs by hairpin polyamides containing N-terminal 3-methoxy (and 3-Chloro) thiophene residues
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Hairpin polyamides selectively recognize predetermined DNA sequences with affinities comparable to naturally occurring proteins. Internal side-by-side pairs of unsymmetrical aromatic rings within the minor groove of DNA distinguish each of the four Watson-Crick base pairs. In contrast, N-terminal ring pairs exhibit less specificity, with the exception of Im/Py targeting G·C base pairs. In an effort to explore the sequence specificity of new ring pairs, a series of hairpin polyamides containing 3-substituted-thiophene-2-carboxamide residues at the N-terminus was synthesized. An N-terminal 3-methoxy (or 3-chloro) thiophene residue paired opposite Py displayed 6- (and 3-) fold selectivity for T·A relative to A·T base pair, while disfavoring G,C base pairs by >200-fold. Our data suggests shape selective recognition with projection of the 3-thiophene substituent (methoxy or chloro) to the floor of the minor groove.
- Foister, Shane,Marques, Michael A.,Doss, Raymond M.,Dervan, Peter B.
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p. 4333 - 4340
(2007/10/03)
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- Phosphorylamides, their preparation and use
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A phosphorylamide derivative represented by the general formula (I): STR1 wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.
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- Synthesis and preliminary pharmacological study of thiophene analogues of the antipyretic and analgesic agent ethenzamide
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A preliminary pharmacologcal study of a thiophene analogue 1b of the analgesic and antipyretic agent Ethenzamide and of a closely related compound 1a showed that a great similarity exists among Ethenzamide and the thiophenic compounds for analgesic, antipyretic, ulcerogenic, hypothermic, and sedative effects. However, the acute toxicity in mice for the thiophenic compounds is notably higher than that of Ethenzamide.
- Darias,Bravo,Abdallah,Sanchez Mateo,Exposito-Orta
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- Novel derivatives of 2-(2-thienyl)-imidazo[4,5-b]-pyridines and their pharmaceutically acceptable salts
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The invention relates to new therapeutically valuable derivatives of 2-(2-thienyl)-imidazo[4,5-b]pyridines of the general formula STR1 in which R is methyl or ethyl, R1 is hydrogen or methyl and R2 is methylthio, methylsulfinyl oder methoxy, and their pharmaceutically acceptable acid addition salts, which compounds possess pharmacological properties, especially a positively inotropic activity on the heart.
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- Novel 1-[3-(2-hydroxy-3-alkylaminopropoxy)-2-thienyl]-3-phenyl-1-propanones and their salts and a process for the preparation thereof
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The disclosure is directed to novel 1-[3-(2-hydroxy-3-alkylaminopropoxy)-2-thienyl]-3-phenyl-1-propanones and their salts. The compounds of the invention have the structural formula STR1 in which R and R1 are independently hydrogen or methyl an
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