92613-96-2Relevant academic research and scientific papers
SUBSTITUTED ADIPIC ACID AMIDES AND USES THEREOF
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Page/Page column 87-88, (2012/10/07)
The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH2, or CH; Z is CH or N; R7 and R9 are hydrogen or (C1-C6)alkyl; R2 is (C1 C6)alkoxy, OH, CN, (C1-C6)alkyl, halogen, or CF3; r and s are 0, 1, or 2; and R1 and R3 are as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor.
PEPTIDYL DERIVATIVES AS METALLOPROTEINASE INHIBITORS
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, (2008/06/13)
Peptidyl derivatives are disclosed that are orally active metalloproteinase inhibitors. The peptidyl derivatives have a selective gelatinase action, have a long duration of action, and are useful in the prophylaxis or treatment of diseases or disorders in which stromelysis, collagenase or gelatinase have a role, for example, in the treatment of cancer to control the development of tumor metastases.
Studies Related to Thietan-2-ones. Part 1. Conversion of D-Penicillamine into DL-2-Methylpenicillamine using Thietan-2-one-based Chemistry
Al-Zaidi, Shakir M.R.,Crilley, Martine M. L.,Stoodley, Richard J.
, p. 2259 - 2266 (2007/10/02)
A series of N-substituted derivatives of (3R)-3-amino-4,4-dimethylthietan-2-one has been prepared from D-penicillamine (3).Attempts to effect the methylathion at position 3 of the N-acetyl (7a), N,N-diacetyl (12), N-benzyloxycarbonyl (7b), or N-(p-nitrobenzylidene) derivative (15a) were unrewarding.Although the N-benzylidene and N-furfurylidene derivatives (15b) and (15c) were successfully methylated at position 3 by using iodomethane and potassium t-butoxide in tetrahydrofuran (THF), best results were achieved by treating the N-(2-hydroxy-1-naphthylmethylene) derivative (15d) with iodomethane and sodium hydride in N,N-dimethylformamide.Cleavage of the imine linkage of the methylated derivatives of the thietanones (15c) and (15d), i.e. compounds (19b) and (19c), was effected by using, respectively, toluene-p-sulphonic acid in THF and dilute hydrochloric acid in acetone.The derived salts of (3RS)-3-amino-3,4,4-trimethylthietan-2-one, i.e. (21a) and (21b), underwent hydrolysis in boiling water to give the corresponding salts of DL-2-methylpenicillamine, i.e. (22a) and (22b).
