Patent classifications
C07C69/28
Ophthalmic composition containing compounds found in Harderian gland secretions
The present invention is directed to pharmaceutical compositions comprising compounds found in Harderian gland secretions, a method of treating dry eye in a human comprising ophthalmically administering an effective amount of a compound, e.g. a lipid compound, found in Harderian gland secretions, pharmaceutical compositions comprising said lipid compounds, as identified by characteristic chemical data and mass spectra of said lipid compounds, said lipid compound in essentially pure form, and an ophthalmic vehicle comprising a therapeutic agent and a compound present in the secretions of the Harderian gland, e.g. a lipid compound, found in the secretions of the Harderian gland, e.g. a rabbit Harderian gland.
Cannabinoid Emulsifier
Provided herein is a compound which is particularly suitable for use as a cannabinoid, as an emulsifier for a cannabinoid, in a formulation comprising the compound and in a method of treatment using the compound. The compound is defined by the General Formula:
##STR00001##
wherein:
R.sup.1-R.sup.10 are independently selected from H or an alkyl of 1-10 carbons; alkenyl of up to 10 carbons; or groups on adjacent carbons may be taken together to form an alkene;
R.sup.11 and R.sup.12 are independently H or —(CH.sub.2CHR.sup.16O).sub.x—R.sup.17 with the proviso that at least one of R.sup.11 or R.sup.12 represents —(CH.sub.2CHR.sup.16O).sub.xR.sup.17—; R.sup.11 and R.sup.10 may be taken together to represent —C(R.sup.19).sup.2—;
R.sup.13-R.sup.15 independently represent H or an alkyl of 1-8 carbons;
each R.sup.16 independently represents H or an alkyl of 1-3 carbons;
each R.sup.17 independently represents H, an alkyl or substituted alkyl of 1-22 carbons, aryl or substituted aryl or the ester of an acid;
each R.sup.19 independently represents H or an alkyl of 1-5 carbons; and
each x is independently an integer of 1-100.
FATTY ACID DERIVATIVE, PRODUCTION PROCESS THEREFOR, HAIR COMPOSITION AND HAIR-TREATMENT METHOD
A hair composition, a method of hair treatment, a process for producing fatty acid derivatives, and the use of these hair compositions, the hair composition comprising fatty hydroxy esters and fatty hydroxy amides in hair care compositions to improve hair shine and strength.
Hydroquinone compounds, preparation methods therefor, and use in anti-tumor or immunomodulation therapy
Disclosed are hydroquinone compounds, preparation methods therefor, and uses thereof in anti-tumor or immunomodulation. The structural formula of the hydroquinone compounds are shown by formula I, ##STR00001##
wherein X is C═O or CH.sub.2; Y is NH, O or absent; R is: a substituted or unsubstituted alkyl group having at least one carbon atom, a substituted or unsubstituted cycloalkyl group having at least three carbon atoms, a substituted or unsubstituted alkenyl group or alkynyl group having at least two carbon atoms; and a substituted or unsubstituted aryl group or heteroaryl group containing at least four carbon atoms. The compounds provided slowly release 2-tert-butyl-4-methoxyphenol in vivo and maintain stable plasma concentration of 2-tert-butyl-4-methoxyphenol (T1/2=12-24 h). The compounds provided by the present invention protect the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, avoids environmental oxidation and increase the environmental stability of drugs containing the compounds.
Hydroquinone compounds, preparation methods therefor, and use in anti-tumor or immunomodulation therapy
Disclosed are hydroquinone compounds, preparation methods therefor, and uses thereof in anti-tumor or immunomodulation. The structural formula of the hydroquinone compounds are shown by formula I, ##STR00001##
wherein X is C═O or CH.sub.2; Y is NH, O or absent; R is: a substituted or unsubstituted alkyl group having at least one carbon atom, a substituted or unsubstituted cycloalkyl group having at least three carbon atoms, a substituted or unsubstituted alkenyl group or alkynyl group having at least two carbon atoms; and a substituted or unsubstituted aryl group or heteroaryl group containing at least four carbon atoms. The compounds provided slowly release 2-tert-butyl-4-methoxyphenol in vivo and maintain stable plasma concentration of 2-tert-butyl-4-methoxyphenol (T1/2=12-24 h). The compounds provided by the present invention protect the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, avoids environmental oxidation and increase the environmental stability of drugs containing the compounds.
DIESTER OF BISPHENOL FLUORENE COMPOUNDS AND THERMOCHROMIC PIGMENT COMPOSITIONS COMPRISING THE SAME
There is a compound represented by the following formula (I):
##STR00001##
in which R1 and R2, identical or different, represent a C.sub.2-C.sub.30 alkyl group, a C.sub.2-C.sub.30 alkenyl group, a C.sub.2-C.sub.30 alkynyl group, or a C.sub.2-C.sub.30 alkoxy group, the alkyl, alkenyl, alkynyl, or alkoxy groups being optionally substituted with at least one hydroxy, halogen, amino, C.sub.1-C.sub.8 alkyl, or C.sub.1-C.sub.8 alkoxy group, as a temperature change regulating agent in a thermochromic ink composition. There also are thermochromic pigment microcapsules having a compound of formula (I) according to the disclosure, to ink compositions having such thermochromic pigment microcapsules, and to writing instruments comprising such ink compositions.
DIESTER OF BISPHENOL FLUORENE COMPOUNDS AND THERMOCHROMIC PIGMENT COMPOSITIONS COMPRISING THE SAME
There is a compound represented by the following formula (I):
##STR00001##
in which R1 and R2, identical or different, represent a C.sub.2-C.sub.30 alkyl group, a C.sub.2-C.sub.30 alkenyl group, a C.sub.2-C.sub.30 alkynyl group, or a C.sub.2-C.sub.30 alkoxy group, the alkyl, alkenyl, alkynyl, or alkoxy groups being optionally substituted with at least one hydroxy, halogen, amino, C.sub.1-C.sub.8 alkyl, or C.sub.1-C.sub.8 alkoxy group, as a temperature change regulating agent in a thermochromic ink composition. There also are thermochromic pigment microcapsules having a compound of formula (I) according to the disclosure, to ink compositions having such thermochromic pigment microcapsules, and to writing instruments comprising such ink compositions.
TREPROSTINIL DERIVATIVES AND COMPOSITIONS AND USES THEREOF
The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
TREPROSTINIL DERIVATIVES AND COMPOSITIONS AND USES THEREOF
The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
Kinetic resolution reaction of a (1RS,2SR)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound, a process for preparing optically active trans-α-necrodyl isobutyrate, and a process for preparing optically active γ-necrodyl isobutyrate
The present invention relates to a process for preparing a (1S,2R)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (S,R)-(2), wherein R.sup.1 represents a monovalent hydrocarbon group having 1 to 6 carbon atoms, and a bold wedged bond represents the absolute configuration, and a (1R,2S)-(2-acetoxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (R,S)-(3), wherein R.sup.1 is as defined above, a hashed wedged bond represents the absolute configuration, and Ac represents an acetyl group, the process comprising: subjecting a (1RS,2SR)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (RS,SR)-(2), wherein R.sup.1 is as defined above, and a hashed unwedged bond represents a relative configuration, to a kinetic resolution reaction with a lipase in the presence of vinyl acetate to obtain the (1S,2R)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound ((S,R)-(2)) and the (1R,2S)-(2-acetoxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound ((R,S)-(3)). ##STR00001##