Process for converting a carboxamide to a thiocarboxamide includes reacting (a) a substrate that comprises a heteroatom-containing moiety and a carboxamide moiety with (b) a dialkyl dithiophosphate and/or a salt thereof. The heteroatom-containing moiety includes a heteroatom selected from the group consisting of N, O, and S. Processes for preparing piperidine-4-thiocarboxamide are described.

Process for converting a carboxamide to a thiocarboxamide includes reacting (a) a substrate that comprises a heteroatom-containing moiety and a carboxamide moiety with (b) a dialkyl dithiophosphate and/or a salt thereof. The heteroatom-containing moiety includes a heteroatom selected from the group consisting of N, O, and S. Processes for preparing piperidine-4-thiocarboxamide are described.

Provided herein are compositions and methods for generating polypeptides using non-natural amino acids (nnAAs) and genetic machinery, wherein the modified polypeptides, such as therapeutic polypeptides, bind to albumin, such as serum albumin. Methods of substituting a non-natural amino acid in a first polypeptide to obtain a modified polypeptide, the nnAA in some instances comprising an albumin targeting group, are disclosed, as are methods for making populations of such modified polypeptides. A therapeutic polypeptide, interleukin-1 receptor antagonist (IL-1RA) is exemplified using the disclosed methods.

The present invention discloses an isolated substantially pure trans isomer of 3-(2-bromo-3,4-dihydroxy-phenyl)-N-(3,4,5-trihydroxy-benzyl)-thioacrylamide, methods for its preparation, pharmaceutical compositions comprising same, and use thereof in treating cancer.

The present invention discloses an isolated substantially pure trans isomer of 3-(2-bromo-3,4-dihydroxy-phenyl)-N-(3,4,5-trihydroxy-benzyl)-thioacrylamide, methods for its preparation, pharmaceutical compositions comprising same, and use thereof in treating cancer.

The invention discloses a novel intermediate for preparing tapentadol and analogs thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogs thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production. ##STR00001##

A compound of the formula (I) or a tautomeric isoform thereof wherein R1 is selected from the group consisting of halogen, nitro, lower alkyl sulfonyl, cyano, trifluromethyl lower alkyl, lower alkoxy, lower alkoxycarbonyl, carboxy, lower alkyl aminosulfonyl, perfluoro lower alkyl, lower alkylthio, hydroxy lower alkyl, alkoxy lower alkyl, lower alkylthio lower alkyl, lower alkylsulfinyl lower alkyl, lower alkylsulfonyl lower alkyl, lower alkylsulfonyl, lower alkanoyl, aroyl, aryl, aryloxy and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy, alkylthio, and alkylcarbonyl, and their non-toxic, pharmaceutically acceptable base addition salts or pro-drugs thereof. The compounds of the invention are useful in the treatment of nervous system diseases and disorders, which are responsive to modulation of the GABA.sub.A receptor complex.

A compound of the formula (I) or a tautomeric isoform thereof wherein R1 is selected from the group consisting of halogen, nitro, lower alkyl sulfonyl, cyano, trifluromethyl lower alkyl, lower alkoxy, lower alkoxycarbonyl, carboxy, lower alkyl aminosulfonyl, perfluoro lower alkyl, lower alkylthio, hydroxy lower alkyl, alkoxy lower alkyl, lower alkylthio lower alkyl, lower alkylsulfinyl lower alkyl, lower alkylsulfonyl lower alkyl, lower alkylsulfonyl, lower alkanoyl, aroyl, aryl, aryloxy and R2 is selected from the group consisting of hydrogen, alkyl, alkoxy, alkylthio, and alkylcarbonyl, and their non-toxic, pharmaceutically acceptable base addition salts or pro-drugs thereof. The compounds of the invention are useful in the treatment of nervous system diseases and disorders, which are responsive to modulation of the GABA.sub.A receptor complex.

Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) ##STR00001##
wherein
X, Y, Z, R, R.sub.1, R.sub.2, R.sub.3, R.sub.3 R.sub.4, R.sub.5, R.sub.6, R.sub.7 have the meanings defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives of formula (I) ##STR00001##
wherein
X, Y, Z, R, R.sub.1, R.sub.2, R.sub.3, R.sub.3 R.sub.4, R.sub.5, R.sub.6, R.sub.7 have the meanings defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.