Patent classifications
C07D249/16
BICYCLIC SULFONES AND SULFOXIDES AND METHODS OF USE THEREOF
The invention provides novel compounds having the general formula I:
##STR00001##
wherein R.sup.1, R.sup.B1, R.sup.B2, n, p, q, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
BICYCLIC SULFONES AND SULFOXIDES AND METHODS OF USE THEREOF
The invention provides novel compounds having the general formula I:
##STR00001##
wherein R.sup.1, R.sup.B1, R.sup.B2, n, p, q, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
METHOD FOR PREPARING HIGH-PURITY SULFONAMIDE COMPOUND, AND INTERMEDIATE OF SULFONAMIDE COMPOUND
The present invention discloses a method for preparing a high-purity sulfonamide compound and an intermediate of the sulfonamide compound. The method comprises the following steps: a, taking a crude product of a sulfonamide compound (I) as an initial raw material, and enabling the raw material to react with a compound of a formula (II) in presence of alkali and a catalyst so as to synthesize an intermediate of a formula (III); and b, enabling the compound represented by the formula (III) to react with alkali or acid, thereby obtaining the high-purity sulfonamide compound (I).
METHOD FOR PREPARING HIGH-PURITY SULFONAMIDE COMPOUND, AND INTERMEDIATE OF SULFONAMIDE COMPOUND
The present invention discloses a method for preparing a high-purity sulfonamide compound and an intermediate of the sulfonamide compound. The method comprises the following steps: a, taking a crude product of a sulfonamide compound (I) as an initial raw material, and enabling the raw material to react with a compound of a formula (II) in presence of alkali and a catalyst so as to synthesize an intermediate of a formula (III); and b, enabling the compound represented by the formula (III) to react with alkali or acid, thereby obtaining the high-purity sulfonamide compound (I).
Cyclooctynes for click chemistry
Provided herein are dibenzocyclooctyne compounds useful as reagents in 1,3-dipolar cycloaddition reactions, and methods for their preparation.
Cyclooctynes for click chemistry
Provided herein are dibenzocyclooctyne compounds useful as reagents in 1,3-dipolar cycloaddition reactions, and methods for their preparation.
Filtration process for purifying liquid azole heteroaromatic compound-containing mixtures
A process for removing impurities from a liquid azole heteroaromatic compound-containing (e.g., triazole-containing) mixture by: (a) providing a liquid azole heteroaromatic compound-containing mixture having impurities; and (b) passing the azole heteroaromatic compound-containing mixture through at least one filtration membrane which is a nanofiltration membrane and/or ultrafiltration membrane having a molecular pore size in the range of from about 200 daltons to about 1 kilodaltons to provide a permeate that is an at least partially purified azole heteroaromatic compound-containing mixture and a retentate with at least some impurities.
PROCESS FOR THE CYCLOADDITION OF A (HETERO)ARYL 1,3-DIPOLE COMPOUND WITH A (HETERO)CYCLOALKYNE
A process is provided, comprising reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein the (hetero)aryl 1,3-dipole compound comprises a 1,3-dipole functional group bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein: (i) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound comprises a substituent (ii) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound is an electron-poor (hetero)aryl group
and wherein the (hetero)cycloalkyne is a (hetero)cyclooctyne or a (hetero)cyclononyne according to Formula (1). The invention also relates to the products obtainable by the process according to the invention.
PROCESS FOR THE CYCLOADDITION OF A (HETERO)ARYL 1,3-DIPOLE COMPOUND WITH A (HETERO)CYCLOALKYNE
A process is provided, comprising reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein the (hetero)aryl 1,3-dipole compound comprises a 1,3-dipole functional group bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein: (i) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound comprises a substituent (ii) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound is an electron-poor (hetero)aryl group
and wherein the (hetero)cycloalkyne is a (hetero)cyclooctyne or a (hetero)cyclononyne according to Formula (1). The invention also relates to the products obtainable by the process according to the invention.
THIOETHER TRIAZOLOPYRIDINE AND TRIAZOLOPYRIMIDINE INHIBITORS OF MYELOPEROXIDASE
The present invention provides compounds of Formula (I): wherein A, X and Y are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
##STR00001##