Abstract: The present invention is directed to novel chemical compositions of matter and their methods of synthesis, and in particular novel analogs of Psilocin having enhanced physical and pharmacokinetic characteristics.

Abstract: The present invention is directed to novel chemical compositions of matter and their methods of synthesis, and in particular novel analogs of Psilocin having enhanced physical and pharmacokinetic characteristics.

Abstract: The present invention is directed to novel chemical compositions of matter and their methods of synthesis, and in particular novel analogs of Psilocin having enhanced physical and pharmacokinetic characteristics.

Abstract: The present invention is directed to novel chemical compositions of matter, and in particular a novel MDMA class of compounds MDMA analogs having 1,3-benzothiazoles substituted at the 5 and 6-position with a MDMA basic or modified side chain.

Abstract: The present invention is directed to novel chemical compositions of matter, and in particular novel MDMA class of compounds having substituted methylenedioxyphenethylamine and substituted amphetamine, having a metabolically labile thioether group.

Abstract: The present invention includes a novel class of MDMA carbamates that can be activated in vivo as prodrugs. The MDMA prodrugs of the invention are enzymatically cleaved in vivo and produce alcohols of low toxicity that are well tolerated and metabolized in humans.

Abstract: The present invention includes a novel class of psilocin carbamates and carbonate prodrug compounds having one or more aza substitution within the psilocin core. The psilocin prodrugs of the invention are enzymatically cleaved in vivo.

Abstract: The present invention is directed to novel chemical compositions of matter and their methods of synthesis, and in particular novel analogs of Psilocin having enhanced physical and pharmacokinetic characteristics.

Abstract: The present invention is directed to novel chemical compositions of matter, and in particular novel MDMA class of compounds having substituted methylenedioxyphenethylamine and substituted amphetamine, having a metabolically labile thioether group.

Abstract: The present invention is directed to novel chemical compositions of matter and their methods of synthesis, and in particular novel analogs of Psilocin having enhanced physical and pharmacokinetic characteristics.

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(?O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(?O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0–6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1? protease activity in a mammal utilizing the compounds and compositions.

Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: 1

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1&bgr; protease activity, the compounds having the formula (I).

Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, sybstituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1&bgr; protease activity in a mammal utilizing the compounds and compositions.

Abstract: Disclosed are compounds, compositions, and methods for inhibiting interleukin-1&bgr; protease activity, wherein the compounds are &agr;-substituted methyl ketones having formula (I) as set forth herein. These compounds are inhibitors of IL-1&bgr; converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.

Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate;R.sub.2 is COOR.sub.5, C(.dbd.O)NH(CHR.sub.5).sub.m --COOR.sub.5, NH(CHR.sub.5).sub.m CON(R.sub.5)R.sub.6, C(.dbd.O)N(R.sub.5)R.sub.6 or NH(CHR.sub.5).sub.m OH;R.sub.3 is H or alkyl;R.sub.4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl;R.sub.5 and R.sub.6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta. protease activity in a mammal utilizing the compounds and compositions.

Abstract: Disclosed are compounds, compositions and methods for inhi.beta.iting interleukin-1.beta. protease activity, the compounds .alpha.-substituted methyl ketones having the formula (I) set forth herein. These compounds are inhibitors of IL-1.beta. converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.

Abstract: Compounds which Inhibit interleukin-1.beta. protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1## wherein n is 0-2; each AA is Independently L-valine or L-alanine;R.sub.1 is selected from the group consisting of N-?4(N,N-dimethylaminomethyl)!benzoyl, N-benzoyloxycarbonyl, N-methyl-N-?4-(pyridyl)methyl!, N-?4-(pyddyl)methyl!carbonyl, N-3-(piperidinopropionyl), N-?4-(morpholinoethoxy)benzoyl, N-2-(quinuclidinyl)carbonyl, N-(3-pyridyl)methoxy carbonyl, N-(2-pyddyl)methoxy carbonyl, N-methyl-N-benzyl carbonyl, N-methyl-N-?2-(4-pyridyl)ethyl!carbonyl, and N-(N-phenylpiperazino) carbonyl; andR.sub.8, R.sub.9 and R.sub.10 are as defined below.