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ThiolactonesRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Hetero Ring Is Six-membered And Includes At Least Nitrogen And Sulfur As Ring Members, Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., 1,3- And 1,4- Benzothiazines, Etc.), At Least Three Cyclos In The Polycyclo Ring SystemThiolactones description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070037798, Thiolactones. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] This application claims the benefit of U.S. Provisional Patent Application No. 60/450,648, filed Mar. 3, 2003, the entire contents of which are herein incorporated by reference. [0002] This invention provides new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, inhibiting angiogenesis, effecting a TGF-.beta. activity or a neuronal activity, and treating a glutamate abnormality, a compulsive disorder, neuropathy, pain, a prostate disease, cancer, Huntington's disease, diabetes, a retinal disorder or glaucoma. [0003] The NAALADase enzyme, also known as prostate specific membrane antigen ("PSMA") and human glutamate carboxypeptidase II ("GCP II"), catalyzes the hydrolysis of the neuropeptide N-acetyl-aspartyl-glutamate ("NAAG") to N-acetyl-aspartate ("NAA") and glutamate. Based upon amino acid sequence homology, NAALADase has been assigned to the M28 family of peptidases. [0004] Studies suggest that inhibitors of NAALADase may be useful in treating ischemia, spinal cord injury, demyelinating diseases, Parkinson's disease, Amyotrophic Lateral Sclerosis ("ALS"), Huntington's disease, alcohol dependence, nicotine dependence, cocaine dependence, opioid dependence, cancer, neuropathy, pain and schizophrenia, and in inhibiting angiogenesis. In view of their potential therapeutic applications, a need exists for new NAALADase inhibitors and prodrugs thereof. SUMMARY OF THE INVENTION [0005] This invention provides a compound of formula I, II or III or a pharmaceutically acceptable equivalent, an optical isomer or a mixture of isomers of the compound, wherein: [0006] X is C.sub.1-C.sub.4 alkylene, C.sub.2-C.sub.4 alkenylene, C.sub.2-C.sub.4 alkynylene, C.sub.3-C.sub.8 cycloalkylene, C.sub.5-C.sub.7 cycloalkenylene or Ar, wherein the alkylene, alkenylene, alkynylene, cycloalkylene or cycloalkenylene is unsubstituted or substituted with one or more substituent(s); [0007] L is a bond, --CR.sup.1R.sup.2--, --O--, --S--, --SO.sub.2-- or --NR.sup.1--; [0008] Y is --O--, --S--, --CR.sup.3R.sup.4-- or --NR.sup.3--; [0009] Z is --(CR.sup.5R.sup.6).sub.n--; [0010] n is 1, 2, 3 or 4; [0011] Ar is a bivalent aryl or heteroaryl radical that is unsubstituted or substituted with one or more substituent(s); [0012] R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen, C.sub.1-C.sub.4 alkyl or C.sub.2-C.sub.4 alkenyl, wherein the alkyl or alkenyl is unsubstituted or substituted with one or more substituent(s); [0013] R.sup.7 is hydrogen, phenyl, phenylethyl or benzyl wherein the phenyl, phenylethyl or benzyl is unsubstituted or substituted with one or more substituent(s); and [0014] R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are independently hydrogen, carboxy, hydroxy, halo, nitro, cyano, C.sub.1-C.sub.4 alkyl or C.sub.1-C.sub.4 alkoxy. [0015] This invention further provides a pharmaceutical composition and a diagnostic kit comprising the compound, and a method of using the compound for inhibiting NAALADase enzyme activity, detecting a disease where NAALADase levels are altered, inhibiting angiogenesis, effecting a TGF-.beta. activity or a neuronal activity, and treating a glutamate abnormality, a compulsive disorder, neuropathy, pain, a prostate disease, cancer, Huntington's disease, diabetes, a retinal disorder or glaucoma. BRIEF DESCRIPTION OF THE DRAWINGS [0016] FIG. 1 is a 27,000.times. magnified photograph of a retinal blood vessel from a control, non-diabetic rat. [0017] FIG. 2 is a 27,000.times. magnified photograph of a retinal blood vessel from a diabetic rat after six months of treatment with a vehicle. [0018] FIG. 3 is a 27,000.times. magnified photograph of a retinal blood vessel from a diabetic rat after six months of treatment with Compound B. [0019] FIG. 4 is a graph plotting the time courses of tail-flick responses of mice treated with a placebo, a NAALADase inhibitor, morphine, or a NAALADase inhibitor with morphine. [0020] FIG. 5 is a bar graph plotting the mean.+-.S.E.M. Area Under Curve (AUC) values. DETAILED DESCRIPTION Definitions Continue reading about Thiolactones... Full patent description for Thiolactones Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Thiolactones patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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