- 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 206; 231
(2021/06/26)
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- One-pot aerobic oxidative sulfonamidation of aromatic thiols with ammonia by a dual-functional β-MnO2 nanocatalyst
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High-surface-area β-MnO2 (β-MnO2-HS) nanoparticles could act as effective heterogeneous catalysts for the one-pot oxidative sulfonamidation of various aromatic and heteroaromatic thiols to the corresponding sulfonamides using molecular oxygen (O2) and ammonia (NH3) as respective oxygen and nitrogen sources, without the need for any additives.
- Hayashi, Eri,Yamaguchi, Yui,Kita, Yusuke,Kamata, Keigo,Hara, Michikazu
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supporting information
p. 2095 - 2098
(2020/02/26)
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- Fe(III)/ l -Valine-Catalyzed One-Pot Synthesis of N -Sulfinyl- and N -Sulfonylimines via Oxidative Cascade Reaction of Alcohols with Sulfinamides or Sulfonamides
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An efficient Fe(III), l -valine, and 4-OH-TEMPO catalytic system was found for the oxidation of alcohols followed by condensation with sulfinamide or sulfonamide in one pot for the synthesis of N -sulfinyl- and N- sulfonylimines compounds under mild conditions. This transformation accommodates a variety of substrates, shows high functional-group tolerance, and affords the corresponding products in good to excellent yields.
- Zhang, Guofu,Xing, Yunzhe,Xu, Shengjun,Ding, Chengrong,Shan, Shang
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supporting information
p. 1232 - 1238
(2018/03/23)
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- Palladium-Catalyzed Carbonylative Cyclization of Amines via γ-C(sp3)-H Activation: Late-Stage Diversification of Amino Acids and Peptides
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The selective γ-C(sp3)-H carbonylation of N-(2-pyridyl)sulfonyl (N-SO2Py)-protected amines has been accomplished by using palladium catalysis and Mo(CO)6 as carbonyl source. The reaction provides a powerful approach for derivatization of amine-based moieties, including amino acids, into richly functionalized γ-lactams. Not only methyl groups, but also methylene C-H bonds of cyclopropanes and conformationally biased molecules can be activated to provide ring-fused γ-lactam derivatives. This carbonylation protocol is also amenable to the late-stage diversification of more-complex multifunctional molecules such as dipeptides and tripeptides, demonstrating the key role of the N-SO2Py as directing group and its capacity to override other inherent substrate coordinating elements. In addition to providing an attractive solution to the difficulties in handling hazardous CO gas, the use of Mo(CO)6 as an air-stable solid source of CO in substoichiometric amount (0.33 equiv) ensures PdII-catalytic activity by preventing its decomposition or deactivation under excess of CO via reduction of PdII to Pd0 or saturation of the metal coordination sphere. Indeed, significantly lower efficiency is observed when the reactions are carried out under CO atmosphere (1 atm), or in the presence of increased amounts of Mo(CO)6. A series of experimental and DFT mechanistic studies provide important insights about the reaction mechanism.
- Hernando, Elier,Villalva, Julia,Martínez, ángel Manu,Alonso, Inés,Rodríguez, Nuria,Gómez Arrayás, Ramón,Carretero, Juan C.
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p. 6868 - 6882
(2016/10/18)
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- SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME
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ABSTRACT The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.
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Page/Page column 122; 123
(2016/09/15)
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- Synthesis of Heteroaryl Sulfonamides from Organozinc Reagents and 2,4,6-Trichlorophenyl Chlorosulfate
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A method for the preparation of aryl and heteroaryl sulfonamides using 2,4,6-trichlorophenyl chlorosulfate (TCPC) is described. The reaction of 2-pyridylzinc reagents with TCPC resulted in 2,4,6-trichlorophenyl (TCP) pyridine-2-sulfonates, and the parent pyridine-2-sulfonate was shown to react with amines. Less electron-rich aryl- and heteroarylzinc reagents reacted with TCPC to afford sulfonyl chlorides that were converted in situ to sulfonamides.
- Colombe, James R.,Debergh, J. Robb,Buchwald, Stephen L.
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p. 3170 - 3173
(2015/06/30)
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- Crystal structures of pyridine sulfonamides and sulfonic acids
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Despite the widespread occurrence of pyridinesulfonic acid and pyridinesulfonamide functional groups in drugs and pharmaceuticals, and their use as ligands in metal-organic frameworks, a systematic structural study of their hydrogen bonding and molecular packing is lacking. We discuss crystal structures of 2-, 3-, and 4-pyridinesulfonic acids/amides in terms of N +-H???O- hydrogen bonds, N-H???O dimer/catemer synthons, and graph set notations. This model study provides a background for polymorph screening and solid form hunting of pharmacologically active sulfonamides.
- Akiri, Kalyanachakravarthi,Cherukuvada, Suryanarayan,Rana, Soumendra,Nangia, Ashwini
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p. 4567 - 4573
(2012/11/13)
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- Lewis base assisted Bronsted base catalysis: Bidentate phosphine oxides as activators and modulators of bronsted basic lanthanum-aryloxides
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(Chemical Equation Presented) Dynamic Duo: A Lewis basic bidentate phosphine oxide was effective for activating and modulating the properties of Bronsted basic lanthanum aryl oxides. The Lewis base 1/lanthanum aryl oxide system was suitable for anti-selective Mannich-type reactions of trichloromethyl ketones (see scheme), affording unique building blocks for azetidine-2-carboxylic acids as well as β-amino acids.
- Morimoto, Hiroyuki,Yoshino, Tatsuhiko,Yukawa, Takafumi,Lu, Gang,Matsunaga, Shigeki,Shibasaki, Masakatsu
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supporting information; experimental part
p. 9125 - 9129
(2009/02/08)
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- From haloquinolines and halopyridines to quinoline- and pyridinesulfonyl chlorides and sulfonamides
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The action of sodium methanethiolate (in boiling DMF) towards haloazines (i.e. chloro- or bromo-pyridines and quinolines) (1) (with halogen substituent in non-aza-activated position) causes sequentially halogen ipso-substitution to methylthioazines (2) and then S-demethylation to azinethiolates (3A), which were: i) subjected to S-methylation, ii) oxidized to diazinyl disulfides (4) and iii) oxidatively chlorinated to azinesulfonyl chlorides (5). α- and γ-pyridine- and quinolinesulfonyl chlorides (5a, 5c, 5d and 5f) were prepared by oxidative chlorination of respective disulfides (4) performed in conc. hydrochloric acid and characterized by 1H and 13C NMR spectra. All azinesulfonyl chlorides (5) were effectively converted to corresponding azinesulfonamides (6).
- Maslankiewicz, Andrzej,Marciniec, Krzysztof,Pawlowski, Maciej,Zajdel, Pawel
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p. 1975 - 1990
(2008/09/16)
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- SULPHONAMIDES
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Compounds of the formula STR1 wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.
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- PYRANONE COMPOUNDS USEFUL TO TREAT RETROVIRAL INFECTIONS
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The present invention relates to compounds of formulae (I) and (II) which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R 10 and R 20 taken together are formulae (III) and (IV). STR1
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- Pyridyl sulfonylurea herbicides
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N-Pyridinesulfonyl-N'-pyrimidinyl- and -triazinylureas of the formula I STR1 in which R1 is hydrogen, halogen, C1 -C4 alkyl, C1 -C4 alkoxy, C1 -C4 alkylthio, C1 C4 haloalkoxy or CF3 ; R2 is hydrogen or C1 -C4 alkyl; A is C1 -C6 alkyl or C3 -C6 cycloalkyl, each of which is monosubstituted to trisubstituted by halogen, or is C1 -C4 alkyl or C3 -C6 cycloalkyl, each of which is substituted by C1 -C4 alkoxy, C1 -C4 alkylthio, C1 -C4 alkylsulfonyl, C1 -C4 alkylsulfinyl, C2 -C4 alkenyl, C5 -C6 cycloalkenyl, amino, C1 -C4 alkylamino, C1 -C4 dialkylamino or C2 -C4 alkynyl, it being possible for the C2 -C4 alkenyl radical and the C5 -C6 cycloalkenyl radical to be additionally monosubstituted to trisubstituted by halogen; or A is a 4- to 6-membered saturated heterocycle which contains a hetero atom selected from the group comprising O, N and SO2 ; or A is C1 -C4 alkyl which is substituted by a 4- to 6-membered saturated heterocycle which contains a hetero atom selected from the group comprising O, N and SO2 ; X is C1 -C3 alkyl, C1 -C3 alkyl which is monosubstituted to trisubstituted by halogen, or is C1 -C3 alkoxy or C1 -C3 alkoxy which is monosubstituted to trisubstituted by halogen; Y is halogen, C1 -C3 alkyl, C1 -C3 alkyl which is monosubstituted to trisubstituted by halogen, or is C1 -C3 alkoxy, C1 -C3 alkoxy which is monosubstituted to trisubstituted by halogen, or is cyclopropyl, methylamino or dimethylamino; and E is nitrogen or the methine group, and the salts of these compounds with amines, alkali metal bases or alkaline earth metal bases or with quaternary ammonium bases have good selective herbicidal properties pre-emergence and post-emergence, and good growth-regulating properties.
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- Substituted peptide derivatives
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The invention provides a series of novel substituted peptide derivatives of the formulae Ia, Ib and Ic (set out hereinafter) and pharmaceutically acceptable salts thereof, in which the radicals A, R1, R2 and R4-R9 have the meanings defined in the following specification. The compounds of formulae Ia, Ib, and Ic are inhbitors of human leukocytic elastase. The invention also provides pharmaceutical compositions containing a compound of formula Ia, Ib or Ic, or a pharmaceutically acceptable salt thereof and processes and intermediates for the manufacture of compounds of formulae Ia, Ib, and Ic.
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