5563-21-3Relevant academic research and scientific papers
DIHYDRONAPHTHALENE DERIVATIVE
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, (2017/10/25)
A compound shown by general formula (I) (in the formula, all of the symbols are as defined in the specification) has selective S1P5 receptor agonist activity due to having a linker from a phenyl group to a cyclic substituent in a dihydronaphthalene skelet
Solvent-free friedel-crafts cyclization with trichloroacetic anhydride
Andrews, Ben,Bullock, Kae,Condon, Shannon,Corona, John,Davis, Roman,Grimes, John,Hazelwood, Andrew,Tabet, Elie
experimental part, p. 2664 - 2673 (2009/12/04)
Friedel-Crafts cyclization products were obtained using 1.1 equivalents of environmentally benign trichloroacetic anhydride as sole reagent and solvent. The resulting ketones included benzothiepins, benzothiopyrans, benzoxepins, dibenzothiepins, dibenzoxepins, and tetralones.
Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: Influence of heteroaryl derivatization on potency and selectivity
Heim, Ralf,Lucas, Simon,Grombein, Cornelia M.,Ries, Christina,Schewe, Katarzyna E.,Negri, Matthias,Müller-Vieira, Ursula,Birk, Barbara,Hartmann, Rolf W.
scheme or table, p. 5064 - 5074 (2009/07/11)
Recently, we reported on the development of potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. A major drawback of these nonsteroidal compounds was a strong inhibition of the hepatic drug-metabolizing enzyme CYP1A2. In the present study, we examined the influence of substituents in the heterocycle of lead structures with a naphthalene molecular scaffold to overcome this unwanted side effect. With respect to CYP11B2 inhibition, some substituents induced a dramatic increase in inhibitory potency. The methoxyalkyl derivatives 22 and 26 are the most potent CYP11B2 inhibitors up to now (IC50 = 0.2 nM). Most compounds also clearly discriminated between CYP11B2 and CYP11B1, and the CYP1A2 potency significantly decreased in some cases (e.g., isoquinoline derivative 30 displayed only 6% CYP1A2 inhibition at 2 μM concentration). Furthermore, isoquinoline derivative 28 proved to be capable of passing the gastrointestinal tract and reached the general circulation after peroral administration to male Wistar rats.
CHEMICAL COMPOUNDS
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Page/Page column 41-42, (2010/02/15)
The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel naphthalene compounds that are particularly useful for selective estrogen receptor modulation.
1-AMINOMETHYL-1,2,3,4-TETRAHYDRONAPHTHALENES
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, (2008/06/13)
Compounds of the formula STR1 and pharmaceutically acceptable salt thereof, wherein R 2 is selected from hydroxy and lower alkoxy, R 5 is lower alkyl, and R 11 and R 12 are independently selected from hydrogen, halo, hydroxy, methoxy, and lower alkyl, are selective . alpha.. sub.2 adrenergic receptor antagonists useful in the treatment of glaucoma.
1-aminomethyl-1,2,3,4-tetrahydronaphthalenes
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, (2008/06/13)
The present invention provides compounds of the formula STR1 or a pharmaceutically acceptable salt thereof wherein R1 is selected from hydrogen, halo, lower alkyl, lower alkoxy, or thioalkoxy; and R2 is lower alkoxy; or R1 and R2 together form a methylenedioxy or ethylenedioxy ring; R3 and R4 are independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, (lower alkyl)amino, (lower alkylsulfonyl)amino, and halo; and R7 is selected from the group consisting of 2- or 3-thienyl, 2- or 3-furyl, and STR2 where R13 and R14 are independently selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower alkyl, lower alkoxy, lower alkylthio, methylenedioxy, or ethylenedioxy. The compounds of the present invention selectively inhibit α2 -adrenergic receptors as well as inhibit the uptake of biogenic amines and are thus useful in the treatment of certain cardiovascular and psychiatric disorders.
