Patent
Acetylenes disubstituted with a phenyl group and a heterobicyclic group having retinoid-like activity
Reads0
Chats0
TLDR
In this paper, the same authors describe the retinoid-like activity of compounds of the formula "STR1" where X is S, O or NR 1 where R 1 is hydrogen or lower alkyl; n is 0-5; R is H or lower a lower akyl and A is a pharmaceutically acceptable salt.Abstract:
Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR 1 where R 1 is hydrogen or lower alkyl; n is 0-5; R is H or lower alkyl and A is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH 2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR 2 or a ketal derivative thereof where R 2 is --(CH 2 ) m CH 3 where m is 0-4; or a pharmaceutically acceptable salt.read more
Citations
More filters
Patent
Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid-like activity
TL;DR: In this paper, the retinoid-like activity is exhibited by compounds of formula (I) where X is S, O, or NR' where R' is hydrogen or lower alkyl; R is H, -COOH or a pharmaceutically acceptable salt, ester or amide thereof, -CH2OH or an ether or ester derivative, or -CHO or an acetal derivative; m is 0-4; n is 0.
Patent
Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
Elliott S. Klein,Alan T. Johnson,Andrew M. Standeven,Richard L. Beard,Samuel J. Gillett,Tien T. Duong,Sunil Nagpal,Vidyasagar Vuligonda,Min Teng,Roshantha A. Chandraratna +9 more
TL;DR: Aryl-substituted and aryl and (3-oxo-1-propenly) substituted benzopyran, benzothiopyran and 1,2-dihydroquinoline derivatives have retinoid negative hormone and/or antagonist-like biological activities as discussed by the authors.
Patent
Substituted diaryl or diheteroaryl methans, ethers and amines having retinoid agonist, antagonist or inverse agonist type biological activity
TL;DR: In this article, the formula Y 3 (R 4 ) was used to define a class of compounds with either retinoid or inverse agonist type biological activity, where the symbols have the meaning defined in the specification.
Patent
Method of treatment with compounds having selective agonist-like activity on RXR retinoid receptors
TL;DR: A compound is defined to be a selective receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites as mentioned in this paper.
Patent
Treatment of mammals afflicted with tumors with compounds having RXR retinoid receptor agonist activity
TL;DR: The range of concentration of the active ingredient in the pharmaceutical compositions is approximately between 0.001 and 5 percent by weight, and such that the composition delivers approximately 0.1 mg to 100 mg of active ingredient per kg body weight of the patient, per day of treatment as discussed by the authors.
References
More filters
Patent
Diaryl acetylenes, their preparation and use
TL;DR: In this article, diarylacetylenes of the formula II were described, in which A and R 1 -R 6 have the meaning given in the description, and the new compounds some own for combating diseases.
Patent
Carboxylic acid derivatives useful for inhibiting the degradation of cartilage
TL;DR: In this paper, carboxylic acids of the formula NCOCH 3 and the pharmaceutically acceptable salts thereof, and certain esters and amides thereof, are useful for inhibiting the degradation of articular cartilage when administered to a mammalian subject afflicted with an arthritic disease.
Patent
Tetralin derivatives, their preparation and use
TL;DR: In this paper, the tetralin derivatives of the formula I have been described for controlling diseases, and the new compounds are suitable for controlling disease in the form of tetrahedra.