Patent classifications
C07C327/06
COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEUROLOGICAL DISEASES
The compositions and compounds of Formula I which includes a salt of duloxetine or its polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of major depressive disorder, general anxiety disorder, urinary incontinence, painful peripheral neuropathy, diabetic neuropathy, fibromyalgia, and chronic musculoskeletal pain associated with osteoarthritis and chronic lower back pain.
Organocatalysts of oxidative protein folding
Catalysts of protein-disulfide isomerization of formula: ##STR00001##
where R.sub.1 is hydrogen or COR.sub.4, where R.sub.4 is an optionally substituted aliphatic group or an optionally substituted aryl group; R.sub.2 is hydrogen or COR.sub.5, where R.sub.5 is alkyl having 1-8 carbon atoms, an alkenyl having 3-8 carbon atoms or a phenyl, benzyl, phenethyl or naphthyl group; and R.sub.3 is hydrogen or alkyl group having 1-3 carbon atoms. Protein folding buffers comprising one or more of the above compounds. Method of catalyzing, in vivo or in vitro, the isomerization of disulfide linkages in a protein or peptide employing above catalysts. Method of forming, in vivo or in vitro, disulfide linkages in a protein or peptide employing above catalysts.
Organocatalysts of oxidative protein folding
Catalysts of protein-disulfide isomerization of formula: ##STR00001##
where R.sub.1 is hydrogen or COR.sub.4, where R.sub.4 is an optionally substituted aliphatic group or an optionally substituted aryl group; R.sub.2 is hydrogen or COR.sub.5, where R.sub.5 is alkyl having 1-8 carbon atoms, an alkenyl having 3-8 carbon atoms or a phenyl, benzyl, phenethyl or naphthyl group; and R.sub.3 is hydrogen or alkyl group having 1-3 carbon atoms. Protein folding buffers comprising one or more of the above compounds. Method of catalyzing, in vivo or in vitro, the isomerization of disulfide linkages in a protein or peptide employing above catalysts. Method of forming, in vivo or in vitro, disulfide linkages in a protein or peptide employing above catalysts.
Metal-Catalyzed Oxidative Coupling of Thiols
Disclosed are methods for preparing disulfide compounds through oxidative coupling of thiol compounds. Thiols are oxidized to the corresponding disulfide compound in high yield in presence of a base and a metal salt. The method uses low catalyst loadings and provides organic disulfide compounds with little to no byproducts.
SYNTHESIS OF THERAPEUTIC AND DIAGNOSTIC DRUGS CENTERED ON REGIOSELECTIVE AND STEREOSELECTIVE RING OPENING OF AZIRIDINIUM IONS
Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
DIAMINE CROSSLINKING AGENTS, CROSSLINKED ACIDIC POLYSACCHARIDES AND MEDICAL MATERIALS
The invention provides a diamine crosslinking agent for acidic polysaccharides consisting of a diamine compound having a primary amino group at both terminals and an ester or thioester bond in the molecule, wherein the number of atom in the linear chain between at least one of the amino groups and the carbonyl carbon in the ester or thioester is 1 to 5; in particular, a diamine crosslinking agent for acidic polysaccharides which is represented by the general formula (I) below:
##STR00001##
[the symbols in the formula are as described in the specification]; a crosslinked acidic polysaccharide obtained by forming crosslinks by amide bonding between the amino groups in the diamine crosslinking agent and carboxyl groups in an acidic polysaccharide; and a medical material including the crosslinked product.
DIAMINE CROSSLINKING AGENTS, CROSSLINKED ACIDIC POLYSACCHARIDES AND MEDICAL MATERIALS
The invention provides a diamine crosslinking agent for acidic polysaccharides consisting of a diamine compound having a primary amino group at both terminals and an ester or thioester bond in the molecule, wherein the number of atom in the linear chain between at least one of the amino groups and the carbonyl carbon in the ester or thioester is 1 to 5; in particular, a diamine crosslinking agent for acidic polysaccharides which is represented by the general formula (I) below:
##STR00001##
[the symbols in the formula are as described in the specification]; a crosslinked acidic polysaccharide obtained by forming crosslinks by amide bonding between the amino groups in the diamine crosslinking agent and carboxyl groups in an acidic polysaccharide; and a medical material including the crosslinked product.
Cytotoxic and anti-mitotic compounds, and methods of using the same
Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.
Cytotoxic and anti-mitotic compounds, and methods of using the same
Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.
ANTIOZONANT AND ASSOCIATED RUBBER COMPOSITION AND RUBBER ARTICLE
An antiozonant of formula (I):
##STR00001##
wherein X is selected from the group consisting of O, S, and N; and wherein R is selected from the group consisting of hydrogen, an alkyl moiety, a cycloalkyl moiety, an aryl moiety, an amine moiety, an amide moiety, an alcohol moiety, an aldehyde moiety, a ketone moiety, a carboxylic acid moiety, an ether moiety, an ester moiety, and a thiol moiety. A rubber composition contains the antiozonant, a diene elastomer; a reinforcing filler; a sulfur-based curing agent; and an accelerator for the curing agent.