Abstract: Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory terpenes and/or vanilloids covalently conjugated to one another so that the activity of the conjugate is greater than the sum of its parts. Also disclosed are methods of improving the potency of an anti-inflammatory terpene or vanilloid by linking it to another anti-inflammatory terpene or vanilloid via a carbamate linkage, where the potency of the conjugate is greater than the sum of its parts.

Abstract: Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory terpenes and/or vanilloids covalently conjugated to one another so that the activity of the conjugate is greater than the sum of its parts. Also disclosed are methods of improving the potency of an anti-inflammatory terpene or vanilloid by linking it to another anti-inflammatory terpene or vanilloid via a carbamate linkage, where the potency of the conjugate is greater than the sum of its parts.

Abstract: Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.

Abstract: A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X=C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.

Abstract: Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.

Abstract: A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X?C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.

Abstract: Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.

Abstract: Augmented or synergized anti-inflammatory constructs are disclosed including terpenes covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids, amino acids and polyamines; and anti-inflammatory molecules covalently conjugated with specific amino acids. For the latter, further conjugation with a choline bioisostere further augments the anti-inflammatory activity.

Abstract: Three unique subtypes of N-hydroxyamides and N-hydroxycarbamates containing both the vanilloid moiety (4-hydroxy-3-methoxybenzyl) and a lipophilic aliphatic moiety. Also disclosed are direct syntheses of these vanilloid fatty hydroxamates. The compounds possess inhibitory activity against the enzymes fatty acid amide hydrolase (FAAH) and matrix metallo-proteinase 9 (MMP-9). In addition, these substances bind to the calcium channel protein TRPV1 and inhibit vesicant-induced inflammation in skin and cornea. The compounds have utility in treating topical or systemic inflammatory processes in the skin and/or eye.

Abstract: Nitric oxide biosynthesis-inhibiting anti-inflammatory and anti-microbial compounds of Formula (3) and Formula (4) wherein R1 and R2 are independently selected from optionally substituted thienyl, optionally substituted furyl, optionally substituted —CH?CH-thienyl and optionally substituted —CH?CH-furyl, provided that R2 is substituted with as nitro group Treatment methods utilizing the compounds, and methods of synthesis of the compounds are also disclosed.

Abstract: Augmented or synergized anti-inflammatory constructs are disclosed including terpenes covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids, amino acids and polyamines; and anti-inflammatory molecules covalently conjugated with specific amino acids. For the latter, further conjugation with a choline bioisostere further augments the anti-inflammatory activity.

Abstract: A high throughput method and apparatus for rapidly screening a plurality of genotoxicants to determine the degree and type of genotoxicity are provided.

Abstract: A high throughput method and apparatus for rapidly screening a plurality of genotoxicants to determine the degree and type of genotoxicity are provided.

Abstract: This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain.

Abstract: Three unique subtypes of N-hydroxyamides and N-hydroxycarbamates containing both the vanilloid moiety (4-hydroxy-3-methoxybenzyl) and a lipophilic aliphatic moiety. Also disclosed are direct syntheses of these vanilloid fatty hydroxamates. The compounds possess inhibitory activity against the enzymes fatty acid amide hydrolase (FAAH) and matrix metallo-proteinase 9 (MMP-9). In addition, these substances bind to the calcium channel protein TRPV1 and inhibit vesicant-induced inflammation in skin and cornea. The compounds have utility in treating topical or systemic inflammatory processes in the skin and/or eye.

Abstract: This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain.

Abstract: Water-soluble dimethyl amino ethyl ether psoralens useful in the treatment of proliferative skin disorders, microbial infections and diseases, disorders of the blood and bone marrow of mammals and in microbiocidal compositions for sterilization of blood and blood products and surgical implants and inhibition of microbial growth in industrial applications are provided.

Abstract: Water-soluble dimethyl amino ethyl ether psoralens useful in the treatment of proliferative skin disorders, microbial infections and diseases, disorders of the blood and bone marrow of mammals and in microbiocidal compositions for sterilization of blood and blood products and surgical implants and inhibition of microbial growth in industrial applications are provided.

Abstract: This invention claims the process for producing two structural variants of functionalized 4-amino-3-mercapto-1,2,4-triazoles as inhibitors of nitric oxide synthase (NOS) and as inhibitors of malignant cell growth. This fundamental molecular construct operates as a heterocyclic mimic of the open-chain N-aminoarginines (or N-aminoguanidines) previously established as NOS inhibitors.

Abstract: This invention claims the utility of two structural variants of functionalized 4-amino-3-mercapto-1,2,4-triazoles as inhibitors of nitric oxide synthase (NOS) and as inhibitors of malignant cell growth. This fundamental molecular construct operates as a heterocyclic mimic of the open-chain N-aminoarginines (or N-aminoguanidines) previously established as NOS inhibitors. A convenient bioassay method, using PAM 212 keratinocytes for detection and quantification of relative NOS inhibition potential in a series of candidate drugs, is described as is a bioassay for growth inhibition.