1664-54-6Relevant articles and documents
PYRROLE DERIVATIVE
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Page 93, (2010/02/06)
A novel pyrrole derivative represented by the following formula (1) and a salt thereof: wherein R1 means substituted alkenyl, etc.; R2 means substituted benzoyl, etc.; and R3 to R5 each means hydrogen, alkyl, halogeno, etc. The derivative and salt have antidiabetic activity.
IL-8 receptor antagonists
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Page 9, (2008/06/13)
This invention relates to novel phenyl ureas useful in the treatment of disease states mediated by the chemokine, Interleukin-3 (IL-3)
Carbapenem antibiotic compounds
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, (2008/06/13)
The present invention provides a compound of the formula: STR1 or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: A is a group of the formula (IA) or (IB): STR2 R1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R2 is hydrogen or C1-4 alkyl; R3 and R4 are the same or different and are a variety of substituents X is alkanediyl containing 1-6 carbon atoms optionally interrupted by O, S(O)x (wherein x is zero, one or two), --CONR5 -- or --NR5 -- or wherein R5 is hydrogen or C1-4 alkyl; or X is alkenediyl containing 1-6 carbon atoms optionally interrupted by O, S(O)x or --NR5 --.
A new series of photoactivatable and iodinatable linear vasopressin antagonists
Carnazzi,Aumelas,Barberis,Guillon,Seyer
, p. 1841 - 1849 (2007/10/02)
A series of new linear photoactivatable and iodinatable antagonists of the neuropeptidic hormone vasopressin was designed and synthesized by a combination of PyBOP-mediated Boc/solid-phase peptide synthesis and solution synthesis approaches. These were based on modifications of a previously reported potent and selective antagonist of the vasopressor response (V(1a) receptor) to [arginine]vasopressin, phenylacetyl-D-Tyr(Me)-Phe-Gln-Asn-Arg- Pro-Arg-Tyr-NH2. (Azidophenyl)alkyl substitutions, of the general structure N3-C6H4(CH2)(n)CO (n = 0, 1, 2, or 3), were employed in position 1. The seven new analogues are 4-N3-C6H4CO-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg- Tyr-NH2 (3), 3-N3-C6H4CO-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 (12), 4-N3-C6H4CH2CO-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 (13), 3-N3- C6H4CH2CO-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 (14), 4-N3- C6H4(CH2)2CO-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 (15) 3-N3- C6H4(CH2)2CO-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 (16), 4-N3- C6H4(CH2)3CO-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 (17). All analogues were tested for their affinity of the rat hepatic V(1a) receptor. Analogues 3 and 12 have a low affinity (K(i) ? 20 nM) and analogues 13-17 show a high affinity (K(i) between 0.04 and 0.3 nM). The affinity values appear to be mainly a function of the alkyl chain length and to a lesser extent of the meta or para position of the azido group on the aromatic ring. Analogues 13-17 were iodinated on the Tyr-9 residue, giving compounds 18-22. All these five iodinated derivatives exhibited K(i) values of 0.2-1 nM for rat liver membranes. Their affinities for oxytocin and renal V2 vasopressin receptors were much lower. Moreover, all analogues completely antagonized the vasopressin-stimulated inositol phosphates production in WRK1 cells and were devoided of any agonistic potency. Preliminary covalent binding studies showed improved covalent yields as compared to any previously reported results. They are very promising candidates as potential high-affinity, highly selective, photosensitive ligands for the V(1a) receptor. They could serve as useful pharmacological tools for studies on the vasopressin binding site.
Gamma-Glutamyl-4-azoanilides
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, (2008/06/13)
The present invention provides gamma-glutamyl-4-azoanilides, processes for their preparation and their use as substrates for gamma-glutamyl transferase determination, of the formula STR1 wherein X is alkyl, --(CH2)m --COOH or --O--(CH2)n --COOH wherein m is 0-4 and n is 1-4; R is optionally substituted p-nitrophenyl; an optionally substituted thiophene residue; an optionally substituted thiazole residue; an optionally substituted benzothiazole residue; an optionally substituted benzoisothiazole residue; an N-alkylthiazole residue; or an optionally substituted 1,3,5-thiodiazole residue; as well as the alkali metal, alkaline earth metal and ammonium salts thereof.
