37686-68-3Relevant academic research and scientific papers
QUINAZOLINE DERIVATIVES AS ANTITUMOR AGENTS
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Page/Page column 203-204, (2020/04/25)
The present application relates to novel quinazoline compounds as inhibitors of type I receptor tyrosine kinases, the pharmaceutical compositions comprising one or more of the compounds and salts thereof as an active ingredient, and the use of the compounds and salts thereof in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals and especially in humans.
C5-ANILINOQUINAZOLINE COMPOUNDS AND THEIR USE IN TREATING CANCER
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Paragraph 0241; 0294, (2018/11/21)
The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their prepar
COMPLEMENT PATHWAY MODULATORS AND USES THEREOF
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Page/Page column 83, (2014/01/09)
The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Catechol derivatives
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, (2008/06/13)
Catechol derivatives of the formula STR1 wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure. Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
Syntheses and Adrenergic Activities of Ring-Fluorinated Epinephrines
Adejare, Adeboye,Gusovsky, Fabian,Padgett, William,Creveling, Cyrus R.,Daly, John W.,Kirk, Kenneth L.
, p. 1972 - 1977 (2007/10/02)
The study of chemical and biological effects of fluorine substitution on the aromatic ring of catecholamines has now been extended to epinephrine (Epi). 2- and 6-fluoroepinephrines (2-FEpi and 6-FEpi) have been synthesized.Fluorine substitution on the 2- or 6-carbon of the aromatic ring alters the selectivity of epinephrine toward α- and β-adrenergic receptors, similar in manner to the change in selectivity seen with norepinephrine (NE).Thus, 2-FEpi is a relatively selective β-adrenergic ligand, while 6-FEpi is a relatively selective α-adrenergic ligand.Fluorine substitution of Epi also can markedly increase potency at either α- or β-adrenergic receptors.
CONVENIENT, ONE-STEP SYNTHESES OF 2-FLUOROVERATROLE AND 2-FLUOROVERATRALDEHYDE
Peet, Norton P.,McCarthy, James R.,Sunder, Shyam,McCowan, Jefferson
, p. 1551 - 1556 (2007/10/02)
Metalated veratraldehyde and veratrole were quenched with perchloryl fluoride to provide one-step syntheses of 2-fluoroveratraldehyde and 2-fluoroveratrole, respectively.Previous syntheses of this precursors to 2-fluorodopamine and 5-fluoronorepinephrine are multi-step processess which involve introduction of fluorine at an early stage.Perchloryl fluoride is a potentially hazardous reagant, and should be used only on an appropriate (millimolar) scale with precautions.
Syntheses of Fluorinated 2-Benzylimidazolines
Adejare, Adeboye,Miller, Duane D.
, p. 171 - 193 (2007/10/02)
Perturbation of the electronic properties of the phenyl ring of 2-benzylimidazoline without appreciable steric modification can be achieved by fluorine substitution on the phenyl ring.The effects of such perturbation on biological activity can be evaluated.Syntheses of several fluorinated synthetic intermediates and 2-benzylimidazolines are described.Fluorine coupling of ortho benzylic protons and ortho methoxy protons were found to be 0-1.3 Hz.
