摘要:
The present disclosure provides preparation method for water-soluble magnolol derivatives and honokiol derivatives and intermediates thereof, and related monohydroxy protection intermediates. The nitrification intermediate has a structure shown in Formula I. Formula I is
R2 is a hydroxyl, and R3 is H; or, R2 is H, and R3 is a hydroxyl; and R1 and R4 are independently selected from C1˜C12 electron donor groups. The preparation method includes the following steps: performing monohydroxy protection on a compound A
with a hydroxy protection reagent in the presence of an acid binding agent to form a monohydroxy protection compound, herein R1, R2, R3 and R4 in the compound A have the same definition as above, and the hydroxy protection reagent is p-toluenesulfonyl chloride and 1-hydroxybenzotriazole; and performing a nitrification reaction and a deprotection reaction on the monohydroxy protection compound successively to obtain the nitrification intermediate.
摘要:
The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
摘要:
Compounds and their pharmaceutically acceptable salts for treatment of tauopathies, such as Alzheimer's disease, Pick's disease, progressive supranuclear palsy, corticobasal degeneration, familial frontotemporal dementia/Parkinsonism linked to chromosome 17, amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.
摘要:
The present invention relates to a compound of general formula (I): in which: X is OH, NH2, NHOH or RNH, where R may be a linear or branched, saturated or unsaturated, C1-C10 alkyl radical, Y is H, or an electron-withdrawing group, in particular selected from NO2, CF3 or a halogen, R1 and R2 are H or a linear or branched, saturated or unsaturated, C1-C10 alkyl radical, F is a reactive functional group that can be activated by click chemistry.
摘要:
The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.
摘要:
The invention relates to a method of preparing a high-purity nitrophenol and, more specifically, p-nitrophenol from a nitrohalobenzene. The inventive method comprises the following steps: (a) hydrolysis of a nitrohalobenzene compound by reacting said compound with a base; (b) acidification in order to produce the nitrophenol compound from the salt thereof by means of an acid treatment; (c) crystallisation of the nitrophenol compound obtained; and (d) separation of the product obtained. The invention is characterised in that it also comprises at least the following steps: (e) concentration of the reaction medium after hydrolysis (a) and before acidification (b); and (f) liquid/liquid decantation after acidification (b) and before crystallisation (c), which is intended to eliminate the water phase obtained after acidification (b).
摘要:
The invention provides compounds of formula I: ##STR1## wherein A, B, D, X, R.sup.1, and R.sup.3 have any of the values defined in the specification, as well as N-oxides thereof, S-oxides thereof, pharmaceutically acceptable salts thereof, and in vivo hydrolizable esters and amides thereof, that are useful to relieve pain. The invention also provides pharmaceutical compositions as well as synthetic and therapeutic methods relating to such compounds.
摘要:
The invention relates to a method for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer, characterized in that a substantially pure enantiomer of the general formula ##STR1## is prepared from a compound of the general formula ##STR2## wherein the variable are as defined as in claim 1. The method comprises the following successive reaction steps:(i) reaction with a substantially enantiomerically pure compound of the general formula ##STR3## wherein Z, R.sub.3 and R.sub.4 are defined as in claim 1; (ii) subjection of the compound formed to a deprotection/ring-closure reaction;(iii) optionally deprotection of the hydroxy group of the ring-closed product.The invention further relates to enantiomerically pure intermediates, the preparation of these intermediates and the preparation of a starting compound.
摘要:
Use of a compound of formula (I), wherein Ar is an aromatic ring system comprising one or more optionally substituted phenyl rings optionally linked to or fused with one or more other optionally substituted phenyl rings or one or more 5 or 6-membered, optionally substituted heterocyclic rings wherein the heteroatom is oxygen; and wherein the ring system comprises 1-4 phenyl rings and wherein Ar can be linked to another Ar via a group X wherein the Ar is independently selected; where X is optionally substituted C.sub.1-20 alkylene, C.sub.2-20 alkenylene or C.sub.2-20 alkynylene; R is hydrogen; C.sub.1-20 alkenyl, C.sub.2-20 alkynyl, C.sub.2-20 alkanoyl, C.sub.2-20 alkynoyl, each of which can be optionally substituted; R.sub.1 is independently selected and is hydrogen; optionally substituted C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl; --COOR'--NR'R', halogen, --OR', --COR', --CONR'R', .dbd.O, --SR', --SO.sub.3 R', --SO.sub.2 NR'R', --SOR', --SO.sub.2 R', --NO.sub.2, --CN, glycoside, silyl; where R' is independently hyrogen; alkyl, alkenyl or akynyl each optionally substituted; and where two groups R.sub.1 can be joined; wherein the optional substituents are one or more independently selected from C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl; --COOR"--NR"R", halogen, OR", --COR", --CONR"R", --SR", .dbd.O, --SO.sub.3 R", --SO.sub.2 NR"R", --SOR", --SO.sub.2 ", --NO.sub.2, --CN; wherein R" is independently hydrogen, alkyl, alkenyl, or alkynyl; n=1, 2 or 3; m=1, 2, 3 or 4; or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for inhibiting the action of Ca.sup.2+ -ATPase enzymes. Certain compounds of formula (I) and 8-lavandulyl flavone pharmaceutical formulations are new.
摘要:
This invention relates to a blend of different isomers of a compound represented by structure I ##STR1## wherein R is C.sub.9 -C.sub.20 alkyl; wherein Y is NO.sub.2 or SO.sub.3 R' or H; wherein R' is C.sub.1 -C.sub.20 alkyl; wherein X is NO.sub.2 or C.sub.1 -C.sub.20 alkyl; and wherein R" is H or C.sub.1 -C.sub.20 alkyl, m is 2 or 3, and n is 0, 1, 2, 3, with the provisos: (1) that Y may not be H and X may not be NO.sub.2 when n=0 and (2) that when R is C.sub.9 and n=0, X and Y may not both be NO.sub.2.