5906-30-9Relevant academic research and scientific papers
DUAL ACTION CARBONIC ANHYDRASE INHIBITORS
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Page/Page column 77, (2015/03/13)
The present invention is directed to novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety substituted with a heterocycle or phosphinate and having sulfonamide, sulfamate or sulfamide groups. The present invention is also related to the use of these novel carbonic anhydrase IX inhibitors in cancer treatment, especially radiotherapy and chemotherapy and the use in treatment of infections.
Kinetic and mechanistic studies on sulfamate esters: Models of enzyme inhibitors
McCaw, Cheryl J. A.,Spillane, William J.
, p. 512 - 517 (2007/10/03)
Many compounds containing a sulfamate moiety, such as NH2SO 2O - are now known to be medicinally important. However, very little is known about their mechanisms of reaction even under non-biological conditions. In this work the vario
Insertion of an aspartic acid moiety into cyclic pseudopeptides: Synthesis and biological characterization of potent antagonists for the human tachykinin NK-2 receptor
Fedi, Valentina,Altamura, Maria,Balacco, Giuseppe,Canfarini, Franca,Criscuoli, Marco,Giannotti, Danilo,Giolitti, Alessandro,Giuliani, Sandro,Guidi, Antonio,Harmat, Nicholas J. S.,Nannicini, Rossano,Pasqui, Franco,Patacchini, Riccardo,Perrotta, Enzo,Tramontana, Manuela,Triolo, Antonio,Maggi, Carlo Alberto
, p. 6935 - 6947 (2007/10/03)
A new series of monocyclic pseudopeptide tachykinin NK-2 receptor antagonists has been derived from the lead compound MEN11558. A synthesis for these molecules sharing the same intermediate was designed and performed. The replacement of the succinic moiety with an aspartic acid and the functionalization of its amino group with a wide variety of substituents led to very potent and selective NK-2 antagonists. Best results were obtained through the insertion in position 12 of an amino group with R configuration, linked by a short spacer to a saturated nitrogen heterocycle (morpholine, piperidine, or piperazine). The study led to compounds 54 and 57, endowed with high in vivo potency at very low doses and long duration of action in animal models of bronchoconstriction. In particular 54 and 57 completely inhibited NK-2 agonist induced bronchoconstriction in guinea pig after intratracheal administration at subnanomolar doses (ED50 = 0.27 nmol/kg and 0.15 nmol/kg, respectively).
(Azetidin-1-ylalkyl) lactams as tachykinin antagonists
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, (2008/06/13)
The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C3 -C7 cycloalkyl, aryl or C1 -C6 alkyl, said C1 -C6 alkyl, said C1 -C6 alkyl being optionally substituted by fluoro, COOH, --COO(C1 -C4 alkyl), C3 -C7 cycloalkyl, adamantyl, aryl or het1, and said C3 -C7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C3 -C7 cycloalkyl, C1 -C4 alkoxy, hydroxy, fluoro, fluoro (C1 -C4) alkyl and fluoro (C1 -C4) Alkoxy; R1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C1 -C4 alkoxy, halo and trifluormethyl; R2 is --CO2 H, --CONR3 R4, --CONR5 (C3 -C7 cycloalkyl), --NR5 (C2 -C5 alkanoyl), --NR3 R4, --NR5 CONR5 R6, (C3 -C7 cycloalkyl-C1 -C4 alkyl)R5 N--, --NR5 COCF3, --NR5 SO2 CF3, --NR5 (SO2 C1 -C4 alkyl), --NR5 SO2 NR5 R6, --NR5 (SO2 aryl), --N(aryl) (SO2 C1 -C4 alkyl), --OR5, --O(C3 -C7 cycloalkyl), --SO2 NR5 R6, het3 or a group of formulas: (a), (b), (c), (d), (e), (f), (g) or (h); X is C1 -C4 alkylene; X1 is a direct link or C1 -C6 alkylene; X2 is a direct link, CO, SO2, or NR5 CO; and m is 0, 1 or 2; together with intermediates used in the preparation of compositions containing and the use as tachykinin angatonists of such derivatives. STR1
C-Piperazino-pyridine sulfonamides
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, (2008/06/13)
This invention relates to compounds of the formula: SPC1 Wherein R1 in the 3- or 5-position is preferably a substituted sulfonamido or a carboxamido group whereas R2 in the 2-, 4- or 6-position is preferably an alkyl- or hydroxyalkyl-piperazinyl group. Said compounds may be used as anti-inflammatory and cardiovascular agents.
