Patent classifications
C07D233/84
PROCESS FOR SYNTHESIZING ERGOTHIONEINE AND RELATED COMPOUNDS
The invention provides a process for synthesising a compound of formula V
##STR00001##
wherein: n is 0, 1 or 2; and R is H or
##STR00002##
or a physiologically acceptable salt, tautomer, stereoisomer or mixture of stereoisomers thereof. The process utilizes a N-benzyl protected histidine rather than the unprotected form of histidine. The process of the invention comprises the steps of: (a) deprotecting a N-benzyl protected histidine of formula 11 to form N-benzyl histidine of formula 12; (b) converting compound 12 to (S)-3-(1-benzyl-1H-imidazol-4-yl)-2-(dimethylamino)propanoic acid of formula 13; (c) converting compound 13 to (2S)-N,N,N-2-trimethylethanaminium-3-(1-benzyl-1H-imidazol-4-yl)propanoic acid of formula 14; (d) brominating the imidazole ring of the compound of formula 14 to form 5-bromohercynine lactone (reactive intermediate); and (e) converting the 5-bromohercynine lactone of step (d) to (6-amino-6-carboxyethyl)ergothioneine sulfide of formula 15. The process optionally further includes one of steps (f) to (h): (f) converting the compound of formula 15 to a sulfoxide; (g) converting the compound of formula 15 to a sulfone; or (h) converting the compound of formula 15 to ergothioneine (ESH).
Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase
The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase
The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
Dithiolene metal complex colorless IR absorbers
The invention relates to the use of compounds of formulae (I) and/or (II) as colorless IR absorbers wherein M is Ni, Pd, Pt, Au, Ir, Fe, Zn, W, Cu, Mo, In, Mn, Co, Mg, V, Cr or Ti, X.sub.1, X.sub.2 and X.sub.3 are each independently of the others sulfur or oxygen, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently of the others hydrogen, NR.sub.7R.sub.8, unsubstituted or substituted C.sub.1-C.sub.18alkyl, C.sub.1-C.sub.18 alkyl wherein the alkylene chain is interrupted with oxygen, unsubstituted or substituted C.sub.1-C.sub.18alkenyl, unsubstituted or substituted aryl, unsubstituted or substituted arylalkyl or unsubstituted or substituted heteroarylalkyl, R.sub.7 and R.sub.8, each independently of the other, being unsubstituted or substituted C.sub.1-C.sub.18alkyl, unsubstituted or substituted aryl, unsubstituted or substituted arylalkyl or unsubstituted or substituted heteroarylalkyl, a further IR absorber optionally being added to the compounds of formulae (I) and (II). The invention relates also to novel dithiolene compounds of formulae (I) and (II) wherein X.sub.1 is oxygen and X.sub.2 and X.sub.3 are oxygen or sulfur. The invention relates furthermore to novel dithiolene compounds of formulae (I) and (II) wherein R.sub.1 to R.sub.6 are NR.sub.7R.sub.8. ##STR00001##
Dithiolene metal complex colorless IR absorbers
The invention relates to the use of compounds of formulae (I) and/or (II) as colorless IR absorbers wherein M is Ni, Pd, Pt, Au, Ir, Fe, Zn, W, Cu, Mo, In, Mn, Co, Mg, V, Cr or Ti, X.sub.1, X.sub.2 and X.sub.3 are each independently of the others sulfur or oxygen, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently of the others hydrogen, NR.sub.7R.sub.8, unsubstituted or substituted C.sub.1-C.sub.18alkyl, C.sub.1-C.sub.18 alkyl wherein the alkylene chain is interrupted with oxygen, unsubstituted or substituted C.sub.1-C.sub.18alkenyl, unsubstituted or substituted aryl, unsubstituted or substituted arylalkyl or unsubstituted or substituted heteroarylalkyl, R.sub.7 and R.sub.8, each independently of the other, being unsubstituted or substituted C.sub.1-C.sub.18alkyl, unsubstituted or substituted aryl, unsubstituted or substituted arylalkyl or unsubstituted or substituted heteroarylalkyl, a further IR absorber optionally being added to the compounds of formulae (I) and (II). The invention relates also to novel dithiolene compounds of formulae (I) and (II) wherein X.sub.1 is oxygen and X.sub.2 and X.sub.3 are oxygen or sulfur. The invention relates furthermore to novel dithiolene compounds of formulae (I) and (II) wherein R.sub.1 to R.sub.6 are NR.sub.7R.sub.8. ##STR00001##
Fluorinated benzenesulfonamides as inhibitors of carbonic anhydrase
Novel fluorinated benzenesulfonamides compounds of general formula (I) ##STR00001##
can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression.
Fluorinated benzenesulfonamides as inhibitors of carbonic anhydrase
Novel fluorinated benzenesulfonamides compounds of general formula (I) ##STR00001##
can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression.
Cytochrome P450 inhibitors and their method of use
Embodiments of the present invention relate to novel cytochrome P450 inhibitors and pharmaceutical compositions thereof having a disease-modifying action in the treatment of diseases associated with the production of cortisol that include metabolic syndrome, obesity, headache, depression, hypertension, diabetes mellitus, Cushing's Syndrome, pseudo-Cushing syndrome, cognitive impairment, dementia, heart failure, renal failure, psoriasis, glaucoma, cardiovascular disease, cancer, stroke or incidentalomas.
Cytochrome P450 inhibitors and their method of use
Embodiments of the present invention relate to novel cytochrome P450 inhibitors and pharmaceutical compositions thereof having a disease-modifying action in the treatment of diseases associated with the production of cortisol that include metabolic syndrome, obesity, headache, depression, hypertension, diabetes mellitus, Cushing's Syndrome, pseudo-Cushing syndrome, cognitive impairment, dementia, heart failure, renal failure, psoriasis, glaucoma, cardiovascular disease, cancer, stroke or incidentalomas.
EGFR dimer disruptors and use of the same
Provided herein are compounds that modulate EGFR and methods of using the same, for example to treat cancer.