Patent classifications
C07C255/54
NOVEL THYROMIMETICS
Compounds are provided having the structure of Formula (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1, and Y.sup.2 are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
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[5]Helicene derivatives as molecular reporters for diagnostic applications and methods of synthesis therefor
The present invention provides the methods of synthesis of [5]helicene compounds and the use of the said compounds conjugating with biomolecules to work as molecular reporter for diagnostic. The compounds in the present invention have the chemical structure illustrated in the formula (1): wherein G is a connecting group composes of 2 carbon atoms selected from the group consisting of ethane and ethylene; A is a separated or connected group selected from the group consisting of cyano and imide; D1 is selected from the group consisting of oxyalkanoic acid, oxyalkanal and oxyalkanesulfonate; and D2 has structure selected from the group consisting of hydroxyl, oxyalkanoic acid, oxyalkanal, alkyl oxyalkanoate, oxyalkanol and oxyalkanesulfonate. The compounds in the present invention compose of aromatic [5]helicene core comprising long it-conjugating system. The said compounds contain functional groups which able to link with biomolecules and they are soluble in water or other solvents that used in binding process with biomolecules. Moreover, owing to having proper chemical structure, the compounds in the present invention exhibit good fluorescent emission in wavelength of 425-675 nm. When the said compounds connected with biomolecules, the biomolecules give good fluorescence and can be detected under ultraviolet radiation. ##STR00001##
[5]Helicene derivatives as molecular reporters for diagnostic applications and methods of synthesis therefor
The present invention provides the methods of synthesis of [5]helicene compounds and the use of the said compounds conjugating with biomolecules to work as molecular reporter for diagnostic. The compounds in the present invention have the chemical structure illustrated in the formula (1): wherein G is a connecting group composes of 2 carbon atoms selected from the group consisting of ethane and ethylene; A is a separated or connected group selected from the group consisting of cyano and imide; D1 is selected from the group consisting of oxyalkanoic acid, oxyalkanal and oxyalkanesulfonate; and D2 has structure selected from the group consisting of hydroxyl, oxyalkanoic acid, oxyalkanal, alkyl oxyalkanoate, oxyalkanol and oxyalkanesulfonate. The compounds in the present invention compose of aromatic [5]helicene core comprising long it-conjugating system. The said compounds contain functional groups which able to link with biomolecules and they are soluble in water or other solvents that used in binding process with biomolecules. Moreover, owing to having proper chemical structure, the compounds in the present invention exhibit good fluorescent emission in wavelength of 425-675 nm. When the said compounds connected with biomolecules, the biomolecules give good fluorescence and can be detected under ultraviolet radiation. ##STR00001##
Resin composition, method for producing resin composition, resin composition molded body, and method for producing resin composition molded body
A resin composition including: a magnetic fluid that includes magnetic particles, a dispersant, and a dispersion medium; and a resin or precursor thereof that includes, in a molecule thereof, at least one partial structure selected from the group consisting of a diene skeleton, a silicone skeleton, a urethane skeleton, a 4- to 7-membered ring lactone skeleton, an alkyl group having from 6 to 30 carbon atoms and an alkylene group having from 6 to 30 carbon atoms, a production method thereof, a resin composition molded body obtained by using the resin composition, and a production method thereof.
Process for the preparation of highly pure Crisaborole
The present invention provides a novel and improved process for the preparation of Crisaborole of Formula (I) and its pharmaceutically acceptable salts. The present invention also provides novel intermediates and process for the preparation of intermediates used in the preparation of Crisaborole. The present invention also provides an improved process for the preparation of Crisaborole and pharmaceutically acceptable salts thereof, that is commercially and industrially scalable.
Process for the preparation of highly pure Crisaborole
The present invention provides a novel and improved process for the preparation of Crisaborole of Formula (I) and its pharmaceutically acceptable salts. The present invention also provides novel intermediates and process for the preparation of intermediates used in the preparation of Crisaborole. The present invention also provides an improved process for the preparation of Crisaborole and pharmaceutically acceptable salts thereof, that is commercially and industrially scalable.
Process for the preparation of highly pure Crisaborole
The present invention provides a novel and improved process for the preparation of Crisaborole of Formula (I) and its pharmaceutically acceptable salts. The present invention also provides novel intermediates and process for the preparation of intermediates used in the preparation of Crisaborole. The present invention also provides an improved process for the preparation of Crisaborole and pharmaceutically acceptable salts thereof, that is commercially and industrially scalable.
IMMUNOMODULATOR COMPOUNDS
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II):
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including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
HERBICIDAL COMPOUNDS
The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.
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PREPARATION METHOD FOR (4-ISOPROPOXY-2-METHYL)PHENYL ISOPROPYL KETONE
The invention relates to a preparation method of (4-isopropoxy-2-methyl)phenyl isopropyl ketone, particularly the preparation method includes: reacting m-cresol with thiocyanate in the presence of a catalyst to obtain a product A; reacting the product A with haloisopropane in the presence of a base and a catalyst to obtain a product B; reacting the product B with isopropyl magnesium halide and treating to obtain (4-isopropoxy-2-methyl)phenyl isopropyl ketone. The purity of (4-isopropoxy-2-methyl)phenyl isopropyl ketone prepared is more than 99%, and the total yield is more than 79%. The method according to the present invention avoids the use of toxic reagents and the generation of a large amount of acidic wastewater, reduces the reaction temperature, and improves the reaction yield. The process route is simple and efficient, and the cost is reduced. The purity of the resulting product is high, the production security is greatly improved, and the method is easy to industrialize.