- An Invastigation of Structure and Conformation of Thiophene-2-sulphonyl Radicals
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The e.s.r. spectra of a variety of photochemically generated thiophene-2-sulphonyl radicals are described.Their spin distribution is typical of ?-radicals; radicals without substituents at position 3 exhibit relatively rapid rotation about the C-S bond at all accessible temperatures while the 3-bromo-substituted ones demonstrate a marked conformational preference which has been interpreted in terms of a ?-type conjugated structure.These findings are substantiated also by the results of INDO calculations carried out for the unsubstituted thiophene-2-sulphonyl radical with different relative arrangements of the SO2 and heteroatomic moieties.
- Alberti, Angelo,Chatgilialoglu, Chryssostomos,Guerra, Maurizio
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Read Online
- Functionalization of α-C(sp3)?H Bonds in Amides Using Radical Translocating Arylating Groups
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α-C?H arylation of N-alkylamides using 2-iodoarylsulfonyl radical translocating arylating (RTA) groups is reported. The method allows the construction of α-quaternary carbon centers in amides. Various mono- and disubstituted RTA-groups are applied to the arylation of primary, secondary, and tertiary α-C(sp3)?H-bonds. These radical transformations proceed in good to excellent yields and the cascades comprise a 1,6-hydrogen atom transfer, followed by a 1,4-aryl migration with subsequent SO2 extrusion.
- Radhoff, Niklas,Studer, Armido
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supporting information
p. 3561 - 3565
(2021/01/04)
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- 2-AMINO-N-(AMINO-OXO-ARYL-LAMBDA6-SULFANYLIDENE)ACETAMIDE COMPOUNDS AND THEIR THERAPEUTIC USE
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The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ6- sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
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Page/Page column 218
(2021/06/26)
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- One-pot synthesis of triazolothiadiazepine 1,1-dioxide derivatives via copper-catalyzed tandem [3+2] cycloaddition/N-arylation
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A practical and efficient synthesis of triazolothiadiazepine-1,1-dioxide derivatives via copper-catalyzed [3+2]cycloaddition, followed by N-arylation is described. The method is also applicable to the synthesis of indoline- and thiophene-fused triazolothiadiazepine 1,1-dioxide derivatives.
- Barange, Deepak Kumar,Tu, Yu-Chen,Kavala, Veerababurao,Kuo, Chun-Wei,Yao, Ching-Fa
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scheme or table
p. 41 - 48
(2011/03/22)
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- NOVEL DUAL ACTION RECEPTORS ANTAGONISTS (DARA) AT THE AT1 AND ETA RECEPTORS
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The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.
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Page/Page column 47; 58; 68; 75-76; 105; 124; 287; 291
(2010/11/28)
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- NOVEL COMPOUNDS
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This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted amino -azepines, according to Formula (I). Specifically, the invention is directed to compounds according to Formula (I), wherein: R1 is optionally substituted C3-7cycloalkyl, optionally substituted C3-7cycloalkenyl, optionally substituted Het-C3-7alkyl, optionally substituted Het-C3-7-alkenyl, optionally substituted aryl, optionally substituted heterocycloalkyl, optionally substituted heteroaryl, or optionally substituted indenyl; R2 is H, optionally substituted C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; each R3 is independently H, optionally substituted C1-8alkyl, optionally substituted C2-8alkenyl, optionally substituted C2-8alkynyl, Het-C1-6 alkyl, optionally substituted C3-6cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl, or optionally substituted C1-C6 alkoxy; R4 is H, or optionally substituted C1-C4 alkyl; R5 is H, optionally substituted C1-8alkyl, optionally substituted C2-8alkenyl, optionally substituted C2-8alkynyl, optionally substituted C3-6cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is H or C1-6alkyl; and X is SO2, CO, CH2, or CONH, and pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof.
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Page/Page column 47
(2008/06/13)
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- ACYCLIC 1,3-DIAMINES AND USES THEREFOR
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This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted -acyclic diamines according to Formula (I): or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a combination thereof, wherein: the R groups are as defined herein. The present invention also relates to a pharmaceutical composition and a method of treatment using the compound of Formula (I).
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(2010/10/20)
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- N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
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Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
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Page column 100
(2010/01/30)
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- Sulfonamides for treatment of endothelin-mediated disorders
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Thienylsulfonamides and their pharmaceutically acceptable derivatives, pharmaceutical compositions, articles of manufacture, combinations, lyophilized powders and methods for the treatment of endothelin diseases using these formulations and sulfonamides a
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- Biphenylsulfonamides and derivatives thereof that modulate the activity of endothelin
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Biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, bicyclic or tricyclic carbon or heterocyclic ring biphenylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
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- Sulfonamides for treatment of endothelin-mediated disorders
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Thienyl-, furyl- and pyrrolyl-sulfonamides, pharmaceutically-acceptable salts of sulfonamides, formulations of salts and the sulfonamides, and methods for modulating or altering the activity of the endothelin family of peptides using the formulations and
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- Formulation of sulfonamides for treatment of endothelin-mediated disorders
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Formulations of pharmaceutically-acceptable salts of thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides using the formulations are provided. In particular, formulations of so
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- Isoxazoline and isoxazole fibrinogen receptor antagonists
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This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
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- THIENYL-, FURYL- AND PYRROLYL SULFONAMIDES AND DERIVATIVES THEREOF THAT MODULATE THE ACTIVITY OF ENDOTHELIN
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Thienyl-, furyl-and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl) furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
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- Thiophenesulfonamides as endothelin receptor antagonists
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The synthesis and in vitro binding affinities of a series of thiophenesulfonamides as ET(A) selective endothelin receptor antagonists is described. The most potent inhibitor displayed an IC50 of 43 nM and 3 μM to ET(A) and ET(B) receptors, respectively.
- Raju,Wu, Chengde,Kois, Adam,Verner, Erik,Okun, Ilya,Stavros, Fiona,Chan, Ming Fai
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p. 2651 - 2656
(2007/10/03)
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