Patent classifications
C07C69/738
1,3-Di-oxo-indene derivative, pharmaceutically acceptable salt or optical isomer thereof, preparation method thereof, and pharmaceutical composition containing same as an antiviral, active ingredient
Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
PROCESS FOR PREPARING TAPINAROF
The present invention provides processes for the preparation of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and novel intermediates used therein. In some embodiments the 3, 5-Dihydroxy-4-isopropyl-trans-stilbene is prepared from (E)-2-chloro-2-isopropyl-5-styrylcyclohexane-1,3-dione. Also disclosed are crystal forms of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and pharmaceutical compositions comprising same.
PROCESS FOR PREPARING TAPINAROF
The present invention provides processes for the preparation of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and novel intermediates used therein. In some embodiments the 3, 5-Dihydroxy-4-isopropyl-trans-stilbene is prepared from (E)-2-chloro-2-isopropyl-5-styrylcyclohexane-1,3-dione. Also disclosed are crystal forms of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and pharmaceutical compositions comprising same.
Fluorinated organic compound production method
An object of the present invention is to provide a method for producing a fluorinated organic compound, whereby an iodosylbenzene derivative can be easily separated and recovered. The above object can be achieved by a method for producing a fluorinated organic compound, comprising step A of fluorinating an organic compound (1) by reaction with a fluorine source (3) in the presence of a hypervalent iodine aromatic ring compound (2a), or in the presence of an iodine aromatic ring compound (2b) and an oxidant (2bo); wherein the fluorine source (3) is a fluorine source (3a) represented by formula: MF.sub.n, wherein M is H, a metal of Group 1 of the periodic table, or a metal of Group 2 of the periodic table; and n is 1 or 2; and step B of separating the iodine aromatic ring compound from a reaction liquid after step A is started.
Fluorinated organic compound production method
An object of the present invention is to provide a method for producing a fluorinated organic compound, whereby an iodosylbenzene derivative can be easily separated and recovered. The above object can be achieved by a method for producing a fluorinated organic compound, comprising step A of fluorinating an organic compound (1) by reaction with a fluorine source (3) in the presence of a hypervalent iodine aromatic ring compound (2a), or in the presence of an iodine aromatic ring compound (2b) and an oxidant (2bo); wherein the fluorine source (3) is a fluorine source (3a) represented by formula: MF.sub.n, wherein M is H, a metal of Group 1 of the periodic table, or a metal of Group 2 of the periodic table; and n is 1 or 2; and step B of separating the iodine aromatic ring compound from a reaction liquid after step A is started.
AVOCADO-DERIVED LIPIDS FOR USE IN TREATING LEUKEMIA
A method of treating a leukemia comprising administering to a subject in need thereof a therapeutically effective amount of a composition comprising a compound of Formula (I) and/or (II) having the structure: OR2 R R1O n OR2 R R1O n I II wherein: 10 ---- represents a single or a double bond; R is OH when C----R is C—R, and R is O when C----R is C═R; n is 1, 3, 5 or 7; and R1 and R2 are independently hydrogen or acetyl, and/or isomers, stereoisomers or solvates thereof and/or mixtures thereof.
##STR00001##
IMPROVEMENTS IN OR RELATING TO ORGANIC COMPOUNDS
A fragrance precursor represented by the formula 1
##STR00001##
wherein
X and Y together represent a double bond to a carbon atom bearing R.sub.1 and R.sub.2, with R.sub.1═H, methyl, acetyl or C.sub.1—C.sub.3 alkoxycarbonyl (e.g. ethoxycarbonyl); and R2=phenyl optionally substituted with up to 3 (i.e. 0, 1, 2 or 3) groups selected from C.sub.1—C.sub.4 alkyl (e.g. methyl, ethyl, iso-propyl, tert-butyl), vinyl, hydroxy, C.sub.1—C.sub.3 alkoxy (e.g. ethoxy), and —O—CH.sub.2—O—, e.g. R.sub.2 is benzo[d][1,3]dioxol-5-yl, 4-methylphenyl, 4-methoxyphenyl, 4-vinylphenyl or 3-ethoxy-4-hydroxyphenyl or
R2=naphthyl, (naphthyl) methyl, 1,1,2,4,4,8-hexamethyl-1,2,3,4-tetrahydronaphthalen-7-yl, or 1,1,2,4,4,-penta methyl-1,2,3,4-tetrahydronaphthalen-7-yl or
R2=COR3, wherein R3 is H, C1-C10 alkoxy (e.g. ethoxy, 1-(3,3-dimethylcyclohexyl)ethoxy), C1-C4 alkyl (e.g. methyl, ethyl, propyl, iso-propyl, tert-butyl), e.g. R2 is formyl, acetyl, ethoxycarbonyl, 1-(3,3-dimethylcyclohexyl)ethoxycarbonyl; or wherein
X is OR4, with R4 being H or alkyl, and
Y is OR5, with R5 being alkyl,
useful as a perfume ingredient.
IMPROVEMENTS IN OR RELATING TO ORGANIC COMPOUNDS
A fragrance precursor represented by the formula 1
##STR00001##
wherein
X and Y together represent a double bond to a carbon atom bearing R.sub.1 and R.sub.2, with R.sub.1═H, methyl, acetyl or C.sub.1—C.sub.3 alkoxycarbonyl (e.g. ethoxycarbonyl); and R2=phenyl optionally substituted with up to 3 (i.e. 0, 1, 2 or 3) groups selected from C.sub.1—C.sub.4 alkyl (e.g. methyl, ethyl, iso-propyl, tert-butyl), vinyl, hydroxy, C.sub.1—C.sub.3 alkoxy (e.g. ethoxy), and —O—CH.sub.2—O—, e.g. R.sub.2 is benzo[d][1,3]dioxol-5-yl, 4-methylphenyl, 4-methoxyphenyl, 4-vinylphenyl or 3-ethoxy-4-hydroxyphenyl or
R2=naphthyl, (naphthyl) methyl, 1,1,2,4,4,8-hexamethyl-1,2,3,4-tetrahydronaphthalen-7-yl, or 1,1,2,4,4,-penta methyl-1,2,3,4-tetrahydronaphthalen-7-yl or
R2=COR3, wherein R3 is H, C1-C10 alkoxy (e.g. ethoxy, 1-(3,3-dimethylcyclohexyl)ethoxy), C1-C4 alkyl (e.g. methyl, ethyl, propyl, iso-propyl, tert-butyl), e.g. R2 is formyl, acetyl, ethoxycarbonyl, 1-(3,3-dimethylcyclohexyl)ethoxycarbonyl; or wherein
X is OR4, with R4 being H or alkyl, and
Y is OR5, with R5 being alkyl,
useful as a perfume ingredient.
Alpha keto acid compositions for treating hypo-albuminemia
Provided herein are nutritional, or therapeutic, compositions and methods of use in primarily treating kidney patients suffering from low serum albumin. The compositions are divided into four formulations, comprising: 1) the magnesium salt and/or the calcium salt of the alpha keto acids of: α-leucine, α-valine, α-isoleucine, α-phenylalanine, α-hydroxy methionine; and/or α-tryptophan, and/or α-tyrosine; 2) L-lysine monoacetate, L-threonine; and/or 3) histidine, tryptophan, and tyrosine, as amino acids or base acids. The specific formulation administered depends in part upon which stage 2-5 of renal disease the patient has. The invention further comprises methods of treatment of disorders associated with low serum albumin using the composition as an over-the-counter pill. The patient's serum albumin is tested on a periodic basis and the selected composition and dose are adjusted accordingly. And the invention comprises method of making α-leucine, α-valine, α-isoleucine, a-tyrosine and α-tryptophan in a multi-step process.
Cured film formation composition, orientation material, and retardation material
A cured-film formation composition that includes: (A) one or more compounds having a photo-aligning group and hydroxy group, etc.; (B) a polymer having at least one substituent from the group of a hydroxy group, carboxy group, amino group, and alkoxysilyl group, and the like; and (C) a cross-linking agent. Component (A) contains a compound having a group of Formula [1] below as the photo-aligning group: ##STR00001##
where A.sup.1 and A.sup.2 are independently a hydrogen atom or methyl group; and A.sup.3 is a hydroxy group. A cured-film is formed from the cured-film formation composition, and orientation material is formed by use of photo-alignment technique. A retardation material is obtained by applying a polymerizable liquid crystal on the orientation material and curing it.