566159-08-8Relevant academic research and scientific papers
QUINAZOLINEDIONE DERIVATIVE
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, (2015/03/16)
The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
Synthesis, characterisation and in vitro cytotoxicity studies of a series of chiral platinum(II) complexes based on the 2-aminomethylpyrrolidine ligand: X-ray crystal structure of [PtCl2(R-dimepyrr)] (R-dimepyrr = N-dimethyl-2(R)-aminomethylpyrrolidine)
Diakos, Connie I.,Zhang, Mei,Beale, Philip J.,Fenton, Ronald R.,Hambley, Trevor W.
experimental part, p. 2807 - 2814 (2009/10/10)
A series of platinum(II) complexes were synthesised based on the enantiomerically pure amino acid proline. Novel synthetic pathways were developed, adapted from standard peptide chemistry, to produce the 2-aminomethylpyrrolidine (pyrr) ligand and its derivatives with differing arrangements of methyl substituents at the exocyclic amine sites. The crystal structure of [PtCl2(R-dimepyrr)] (R-dimepyrr = N,N-dimethyl-2(R)-aminomethylpyrrolidine) is reported and the five-membered ligand ring has been shown to be in an envelope conformation. Cytotoxicity studies were carried out on the ovarian cancer A2780 tumour cell line and its cisplatin-resistant variant, A2780cisR. Remarkably good activity was seen for several of the drugs when compared to cisplatin despite the addition of substantial steric bulk to the amine groups, and there was a lack of cross-resistance with cisplatin seen for some compounds.
New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists
Yea, Christopher M.,Allan, Christine E.,Ashworth, Doreen M.,Barnett, James,Baxter, Andy J.,Broadbridge, Janice D.,Franklin, Richard J.,Hampton, Sally L.,Hudson, Peter,Horton, John A.,Jenkins, Paul D.,Penson, Andy M.,Pitt, Gary R. W.,Rivière, Pierre,Robson, Peter A.,Rooker, David P.,Semple, Graeme,Sheppard, Andy,Haigh, Robert M.,Roe, Michael B.
body text, p. 8124 - 8134 (2009/11/30)
Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. The analogue of AVP, desmopressin, has proven an effective drug for diseases where a reduction of urine output is desired. However, its peptidic nature limits its bioavailability. We report herein the discovery of potent, nonpeptidic, benzylurea derived agonists of the vasopressin V2 receptor. We describe substitutions on the benzyl group to give improvements in potency and subsequent modifications to the urea end group to provide improvements in solubility and increased oral efficacy in a rat model of diuresis. The lead compound 20e (VA106483) is reported for the first time and has been selected for clinical development.
PYRIMIDYL SULPHONE AMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
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Page 56, (2008/06/13)
A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease, irritable bowel syndrome, osteoarthritis, osteoporosis, rheumatoid
