Patent classifications
C07D213/79
Synthesis of Esters by Functionalisation of CO2
The invention relates to a method for (I) producing a carboxylic ester of formula (I). Said method comprises the steps of: a) bringing an organosilane/borane of formula Si or B into contact with CO.sub.2, in the presence of a catalyst and an electrophilic compound of formula (III), the groups R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y, and M′ being as defined in claim 1; and optionally b) recovering the compound of formula (I) produced.
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CONJUGATES OF AUXIN ANALOGS
Described herein are methods of enhancing formation and/or growth of an adventitious root in a plant and/or plant tissue, and/or for promoting grafting unification, enhancing fruit size and/or reducing flowering in a plant. The method comprises contacting at least a portion of the plant and/or plant tissue with a compound having Formula I:
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wherein X, Y and R.sub.1-R.sub.7 are as defined herein. Further described are compositions for enhancing formation and/or growth of an adventitious root in a plant and/or plant tissue, and/or for promoting grafting unification, enhancing fruit size and/or reducing flowering in a plant, comprising the abovementioned compound and a horticulturally acceptable carrier. Novel compounds having Formula I are also described herein.
4-SUBSTITUTED PYRIDINE-2,6-DICARBOXYLIC ACID DERIVATIVES AND METHOD OF PREPARING SAME
The present invention relates to novel 4-substituted pyridine-2,6-dicarboxylic acid derivatives, compounds of formula I, wherein R.sup.1 and R.sup.2 are defined herein. The compounds of formula I are useful for making pharmaceutical compositions to treat proliferative diseases. The present invention also relates to concise methods for preparing compounds of formula I that may be performed under mild reaction conditions.
4-SUBSTITUTED PYRIDINE-2,6-DICARBOXYLIC ACID DERIVATIVES AND METHOD OF PREPARING SAME
The present invention relates to novel 4-substituted pyridine-2,6-dicarboxylic acid derivatives, compounds of formula I, wherein R.sup.1 and R.sup.2 are defined herein. The compounds of formula I are useful for making pharmaceutical compositions to treat proliferative diseases. The present invention also relates to concise methods for preparing compounds of formula I that may be performed under mild reaction conditions.
Non-systemic TGR5 agonists
The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs. ##STR00001##
INHIBITORS OF HISTONE DEMETHYLASES
The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form
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INHIBITORS OF HISTONE DEMETHYLASES
The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form
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Pyridine compounds as sodium channel blockers
The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein A.sup.1, X, A.sup.2, R.sup.1a, R.sup.1b, R.sup.1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain. ##STR00001##
Pyridine compounds as sodium channel blockers
The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein A.sup.1, X, A.sup.2, R.sup.1a, R.sup.1b, R.sup.1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain. ##STR00001##
IDO inhibitors
There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention. ##STR00001##