73244-50-5Relevant academic research and scientific papers
Styryl xanthine derivatives and uses thereof (by machine translation)
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Paragraph 0174; 0180; 0181; 0182, (2019/08/02)
The invention discloses styryl xanthine derivatives and application, and particularly, relates to a novel styryl xanthine derivative and a pharmaceutical composition containing the same, and can be used as selective adenosine A. 2A Are antagoni
Homoserine lactone derivatives, preparation method thereof and pharmaceutical composition for prevention or treatment of the periodontal diseases containing the same as an active ingredient
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Paragraph 0276-0279, (2017/04/14)
The present invention relates to homoserine lactone derivatives, optical isomers of the same, or pharmaceutically acceptable salts of the same. The homoserine lactone derivatives in the present invention have excellent properties as a quorum sensing antagonist which hinders communications among bacteria. According to the present invention, the homoserine lactone derivatives can hinder gene expressions of bacteria while effectively blocking formation of biofilm which is known to raise resistance against antibiotics, and suppress propagation of bacteria, thereby being useful as a pharmaceutical composition for preventing or treating periodontal diseases.
HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS
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Page/Page column 158; 163, (2011/05/06)
The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
Synthesis and pharmacological evaluation of 1-Alkyl-N-[(1R)-1-(4- fluorophenyl)-2-methylpropyl]piperidine-4-carboxamide derivatives as novel antihypertensive agents
Watanuki, Susumu,Matsuura, Keisuke,Tomura, Yuichi,Okada, Minoru,Okazaki, Toshio,Ohta, Mitsuaki,Tsukamoto, Shin-Ichi
experimental part, p. 1376 - 1385 (2012/01/05)
We synthesized and evaluated inhibitory activity against T-type Ca 2+ channels for a series of 1-alkyl-N- [(1R)-1-(4-fluorophenyl)-2- methylpropyl]piperidine-4-carboxamide derivatives. Structure-activity relationship studies have revealed that the isopropyl substituent at the benzylic position plays an important role in exerting potent inhibitory activity, and the absolute configuration of the benzylic position was found to be opposite that of mibefradil, which was first launched as a new class of T-type Ca2+ channel blocker. Oral administration of N- [(1R)-1-(4-fluorophenyl)-2-methylpropyl]-1-[2-(3-methoxyphenyl)ethyl] piperidine-4-carboxamide (17f) lowered blood pressure in spontaneously hypertensive rats without inducing reflex tachycardia, an adverse effect often caused by traditional L-type Ca2+ channel blockers.
ALKOXY COMPOUNDS FOR DISEASE TREATMENT
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Page/Page column 218, (2009/05/29)
The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
Rapid microwave-assisted synthesis of phenyl ethers under mildly basic and nonaqueous conditions
Sarju, Julien,Danks, Timothy N.,Wagner, Gabriele
, p. 7675 - 7677 (2007/10/03)
Microwave-assisted alkylation of phenols can be achieved within short reaction times under mild conditions using K2CO3 as a base, in methanol as a solvent. The method is suitable for base sensitive compounds or partially water-solubl
Substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and a medicament comprising them
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, (2008/06/13)
The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-f
A Comparison of the Inhibitory Action of 5-(Substituted-benzyl)-2,4-diaminopyrimidines on Dihydrofolate Reductase from Chicken Liver with That from Bovine Liver
Li, Ren-li,Hansch, Corwin,Kaufman, Bernard T.
, p. 435 - 440 (2007/10/02)
Forty-four 5-(substituted-benzyl)-2,4-diaminopyrimidines have been tested as inhibitors of chicken and bovine liver dihydrofolate reductase.The chicken enzyme is, on the average, about 10 times less easily inhibited than bovine enzyme.Substituents which show the greatest selectivity are 4-NHCOCH3, 3-OC4H9, 3-I, 3-CF3-4-OCH3, and 3,4,5-(OCH3)3.The inhibition constants have been used to formulate quantitative structure-activity relationships for comparative purposes.
