6566-40-1Relevant academic research and scientific papers
2-Amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
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Page/Page column 17, (2010/11/08)
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hy
Novel compounds
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Page 9-10, (2010/02/05)
Compounds of formula I, or a salt thereof or a hydrate thereof, as follows: wherein X and Y are selected independently from hydrogen and aryl, which aryl is unsubstituted or substituted one or more times by hydroxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aryl, heterocyclyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkoxy, C1-6alkyl, C1-6alkoxy or halo, which alkyl or alkoxy groups are unsubstituted or substituted one or more times by halo; m and n are independently 0 to 3, provided that m and n are not both 0; A represents a single bond or is —(CRpa Rpb)p— wherein p is 1-3 and Rpa and Rpb are selected independently from hydrogen, C1-6alkyl, C1-6alkoxy and halo, which alkyl or alkoxy groups are independently substituted one or more times by halo; B represents a C4-8 saturated or unsaturated ring, which ring is unsubstituted or substituted one or more times by C1-6alkyl, C1-6alkoxy, aryl, aryloxy, hydroxy, oxo, halo, amino, C1-6alkylamino, di(C1-6 alkyl)amino, and C1-6alkylamido, which C1-6alkyl or C1-6alkoxy groups are unsubstituted or substituted one or more times by halo, which aryl group is unsubstituted or substituted one or more times by aryl, heterocyclyl, aryloxy, arylC1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkyl, hydroxy, C1-6alkenoxy, C1-6alkoxy, halo, or C1-6alkyl, which C1-6alkyl may be substituted one or more times by halo, and which aryl group is linked to said ring by a single bond or is benzo-condensed therewith are ligands of the ORL-1 receptor.
Design, synthesis, and structure-activity relationships of novel tetracyclic compounds as peripheral benzodiazepine receptor ligands
Okubo, Taketoshi,Yoshikawa, Ryoko,Chaki, Shigeyuki,Okuyama, Shigeru,Nakazato, Atsuro
, p. 3569 - 3580 (2007/10/03)
The peripheral benzodiazepine receptor (PBR) is pharmacologically distinct from the central benzodiazepine receptor (CBR) and has been identified in a wide range of peripheral tissues as well as in the central nervous system. Although numerous studies have been performed of it, the physiological roles and functions of the PBR are still unclear. In the present study, in exploring new types of ligands for PBR, we found that a new series of compounds having a tetracyclic ring system, which were designed from FGIN-1-27, exhibited high affinities for PBR. We prepared and evaluated them for PBR affinities. The results of binding tests showed that 12e and 12f were the most potent PBR ligands among them (12e: IC50=0.44nM, 12f: IC50=0.37nM). In this paper, we present the design, synthesis, and structure-activity relationships (SARs) of novel tetracyclic compounds.
Preparation of (R)-(-)- and (S)-(+)-3-hydroxymethyl-1-tetralone tosylates, key intermediates in the synthesis of new CNS drugs, via resolution of precursors
Caro, Yolanda,Masaguer, Christian F.,Ravina, Enrique
, p. 381 - 387 (2007/10/03)
The preparation of (R)-(-)- and (S)-(+)-3-hydroxymethyl-1-tetralone tosylates, key intermediates in the synthesis of new CNS drugs in the aminobutyrophenone family, has been developed via classical resolutions or lipase-catalyzed kinetic resolution of one of their precursors.
Inhibitors of microsomal triglyceride transfer protein and method
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, (2008/06/13)
Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure STR1 wherein R1 to R7, Q, X and Y are as defined herein.
Nucleic acids encoding microsomal trigyceride transfer protein
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, (2008/06/13)
Nucleic acid sequences, particularly DNA sequences, coding for all or part of the high molecular weight subunit of microsomal triglyceride transfer protein, expression vectors containing the DNA sequences, host cells containing the expression vectors, and methods utilizing these materials. The invention also concerns polypeptide molecules comprising all or part of the high molecular weight subunit of microsomal triglyceride transfer protein, and methods for producing these polypeptide molecules. The invention additionally concerns novel methods for preventing, stabilizing or causing regression of atherosclerosis and therapeutic agents having such activity. The invention concerns further novel methods for lowering serum liquid levels and therapeutic agents having such activity.
STUDIES IN METAL-AMMONIA REDUCTION-5 REDUCTION AND REDUCTIVE METHYLATION OF SOME NAPHTHOIC ACIDS
Murthy, A. Radhakrishna,Sundar, N. Shyama,Rao, G. S. R. Subba
, p. 2831 - 2836 (2007/10/02)
Birch reduction and reductive methylation of some substituted naphthoic acids have been examined.The factors influencing the mechanism of reduction process have been discussed.Some of the reduced naphthoic acids are useful synthons for synthesis.
A new, potent, conformationally restricted analogue of amphetamine: 2-Amino-1,2-dihydronapthalene
Hathaway,Nichols,Nichols,Yim
, p. 535 - 538 (2007/10/02)
A new stimulant compound, 1,2-dihydro-2-naphthalenamine (2-amino-1,2-dihydronaphthalene, 2-ADN), was prepared as an analogue of amphetamine and of 2-aminotetralin. The optical isomers of 2-ADN were obtained by chemical resolution, and the absolute configuration was determined to be R-(+) and S-(-). Preliminary pharmacological evaluation revealed that racemic 2-ADN is approximately one-fourth as potent as (+)-amphetamine as a stimulant in mice. The S-(-) isomer of 2-ADN was found to be solely responsible for the stimulant effects of the racemate. Both reserpine and α-methyl-p-tyrosine antagonized the stimulation produced by 2-ADN.
Friedel-Crafts Acylation with 2-Methyl- or2-Benzylbutanedioic Anhydride
Hashimoto, Iwao
, p. 3219 - 3220 (2007/10/02)
The AlCl3-catalyzed acylation of benzene with 2-methylbutanedioic anhydride afforded mixture of 3-benzoyl-2-methylpropanoic acid and 3-benzoylbutanoic acid.The intramolecular acylation of 2-benzylbutanedioic anhydride in the presence of AlCl3 gave a mixtu
