Patent classifications
C07D311/00
Inhibitors of viral replication, their process of preparation and their therapeutical uses
The present invention relates to aromatic carbocycle or heterocycle compounds comprising an acid function and being of formula (5), ##STR00001##
wherein W, Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, R.sup.1, R.sup.3, R.sup.4, R.sup.7, R.sup.9, R.sup.11, a, c, e, and g are as described in the description; and the use of such compounds in the treatment or the prevention of viral disorders, including HIV.
Methods for oxidation of alpha tocotrienol in the presence of non-alpha tocotrienols
A method of producing alpha-tocotrienol quinone or a stereoisomer thereof, the method comprising selective opening of alpha-tocotrienol chroman to alpha-tocotrienol quinone in the presence of non-alpha tocotrienol chromans by oxidizing alpha-to-cotrienol with a metal salt oxidizing agent, wherein the stoichiometric ratio of metal salt oxidizing agent/alpha-tocotrienol is at least 4:1 and wherein said metal oxidizing agent is added in sequential additions, in order to reduce oxidation of any amounts of non-alpha tocotrienol chromans that might have been present in the starting alpha-tocotrienol chroman material. This process uses conditions favoring oxidation rates of the alpha tocotrienol chroman vs. the non-alpha tocotrienol chromans.
Fluorescent turn-on chemosensors for detection of aluminum ion and azide
Two rhodamine reversible fluorescent sensor derivatives, L.sub.1 and L.sub.2, bearing 2-methoxy-1-naphthaldehyde and 5-bromo-3-methoxy salicylaldehyde units were synthesized using microwave-assisted organic synthesis and used for selective and sensitive reversible sequential fluorescence detection of aluminum ion (Al.sup.3+) and azide (N.sup.3) in aqueous acetonitrile solution via the fluorescence spectral changes. Stoichiometry and binding mechanisms for both sensors are well characterized and established by the respective spectroscopic techniques. L.sup.1 and L.sup.2 sensors are useful for the analysis of Al.sup.3+ and N.sup.3 in environmental samples and biological studies.
ULOTARONT HYDROCHLORIDE MANUFACTURING PROCESS
This disclosure provides improved methods of manufacturing ulotaront HCl, for reducing impurities in ulotaront HCl, and for processing ulotaront HCl into finished dosage forms.
COMPOUNDS FOR SELECTIVE BINDING TO ESTROGEN RECEPTORS ALPHA/BETA RELATIVE TO GPER/GPR30 AND METHODS OF TREATING DISEASE STATES AND CONDITIONS MEDIATED THROUGH THESE RECEPTORS
The current invention is in the field of molecular biology/pharmacology and provides novel 3-oxabicyclo[3.3.1]nonene compounds and derivatives that modulate the effects of the classical estrogen receptors alpha and beta (ERalpha and ERbeta) with little to no biological or physiological effects on the G protein-coupled estrogen receptor GPER (also known as GPR30). These compounds may function as agonists and/or antagonists of one or more of the disclosed classical estrogen receptors. Diseases that are mediated through one or more of these receptors are described. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.
Cyclohexane lipidoids for nucleic acid transfection and use thereof
A lipidoid of general formula I, where X is selected from C(O)NH,C(O)O, C(S)O, C(O)S, C(S)S, C(O)NHNH, CH.sub.2, O, OC(O), S, SC(O), NH, NHNH, NHC(O), NHNHC(O), CC, CHCH, a five-membered heterocycle containing at least 2 nitrogen atoms, CH.sub.2C(O)NH, CH.sub.2C(S)O, CH.sub.2C(S)S, CH.sub.2C(O)NHNH, NCH, CHN, NHNCH, and CHNNH; Y is alkylene C.sub.2-C.sub.10 chain; R.sup.1 is selected from alkyl C.sub.1-C.sub.46, alkenyl C.sub.2-C.sub.46, alkynyl C.sub.2-C.sub.46; Z is selected from H, OH, CH.sub.3, CH.sub.2OH, NH.sub.2, C(O)NH.sub.2, CONH(CH.sub.2).sub.2OH, CON[(CH.sub.2).sub.2OH].sub.2, CONHCH(CH.sub.2OH).sub.2, CONHCH.sub.2CH(OH)CH.sub.2OH, CONH(CH.sub.2).sub.2C(O)NH.sub.2, CON[CH.sub.2C(O)NH.sub.2].sub.2, CONH(CH.sub.2).sub.2NHC(O)NH.sub.2, CONH(CH.sub.2).sub.3N+(CH.sub.3).sub.2(CH.sub.2).sub.2SO.sub.3, CONH(CH.sub.2).sub.3N+(CH.sub.3).sub.2(CH.sub.2).sub.2COO, COO(CHCOO(CH.sub.2).sub.2OP(O)(O)O(CH.sub.2).sub.2N+(CH.sub.3).sub.3, N+(CH.sub.3).sub.2(CH.sub.2).sub.3SO.sub.3, N+(CH.sub.3).sub.2(CH.sub.2).sub.2COO. Transfection reagents, transfection particles containing this lipidoid are also described.
Cyclohexane lipidoids for nucleic acid transfection and use thereof
A lipidoid of general formula I, where X is selected from C(O)NH,C(O)O, C(S)O, C(O)S, C(S)S, C(O)NHNH, CH.sub.2, O, OC(O), S, SC(O), NH, NHNH, NHC(O), NHNHC(O), CC, CHCH, a five-membered heterocycle containing at least 2 nitrogen atoms, CH.sub.2C(O)NH, CH.sub.2C(S)O, CH.sub.2C(S)S, CH.sub.2C(O)NHNH, NCH, CHN, NHNCH, and CHNNH; Y is alkylene C.sub.2-C.sub.10 chain; R.sup.1 is selected from alkyl C.sub.1-C.sub.46, alkenyl C.sub.2-C.sub.46, alkynyl C.sub.2-C.sub.46; Z is selected from H, OH, CH.sub.3, CH.sub.2OH, NH.sub.2, C(O)NH.sub.2, CONH(CH.sub.2).sub.2OH, CON[(CH.sub.2).sub.2OH].sub.2, CONHCH(CH.sub.2OH).sub.2, CONHCH.sub.2CH(OH)CH.sub.2OH, CONH(CH.sub.2).sub.2C(O)NH.sub.2, CON[CH.sub.2C(O)NH.sub.2].sub.2, CONH(CH.sub.2).sub.2NHC(O)NH.sub.2, CONH(CH.sub.2).sub.3N+(CH.sub.3).sub.2(CH.sub.2).sub.2SO.sub.3, CONH(CH.sub.2).sub.3N+(CH.sub.3).sub.2(CH.sub.2).sub.2COO, COO(CHCOO(CH.sub.2).sub.2OP(O)(O)O(CH.sub.2).sub.2N+(CH.sub.3).sub.3, N+(CH.sub.3).sub.2(CH.sub.2).sub.3SO.sub.3, N+(CH.sub.3).sub.2(CH.sub.2).sub.2COO. Transfection reagents, transfection particles containing this lipidoid are also described.