摘要:
This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.
摘要:
This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.
摘要:
The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled cell growth and spread of abnormal cells occurs.
摘要:
The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
摘要:
The present invention is directed to novel dipeptides represented by the general Formula I: ##STR1## where R.sub.1 -R.sub.2 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
摘要:
A computer system and method provide a CAD tool by which application specific optical integrated circuits may be easily and quickly designed. The computer system has a graphical user interface which provides the designer with an empty canvas upon which the user may place selected icons of any one of a plurality of optical devices. The designer can select from any one of a number of interconnects to place an icon of the selected interconnect between two of the optical devices. The characteristics of each optical device or interconnect may be varied from default settings to a desired group of settings. To verify the operation of a designed circuit, the user simply clicks each icon along an optical path and the computer system provides a spectral analysis of optical power versus wavelength for the defied optical path. The user can also design optical chips by selecting and placing end ports into an optical circuit and can then clump or group the entire optical circuit into a single icon representing the chip. The computer system also provides the designer with the ability to group optical chips together to form wafers. The optical circuits, as well as the chips and wafers, may be designed in any one of several manufacturing standards.
摘要:
Process for the preparation of chlorite salts by the controlled reaction of chlorine dioxide with a reducing agent under reduced pressure to form chlorous acid. The chlorous acid is reacted with an aqueous solution of base to form the desired chlorite salt. The process is rapid, economical and is conducted in a generator which is significantly smaller than equipment currently used for production of chlorite salts.
摘要:
Process for the preparation of saturated aqueous solution of chlorite salts by the controlled reaction of chlorine dioxide with a reducing agent under reduced pressure to form chlorous acid. The chlorous acid is reacted with an aqueous solution of base to form an aqueous solution chlorite salt and the aqueous solution is recycled through the process. The process is rapid, economical and is conducted in a generator which is significantly smaller than equipment currently used for production of chlorite salts.
摘要:
A ballast circuit system provides for efficient starting and operation of high voltage discharge lamps using a common 120 volt AC power source. As a result of this improved ballast circuit system, the necessary high voltage is generated from a normal 120 volt AC in such a way that there is low power loss. The system efficiency allows for use of plastic fixtures and small size packaging of the discharge lamp.
摘要:
FIG. 1 is a top perspective view of a TV antenna showing my new design. FIG. 2 is a bottom perspective view thereof. FIG. 3 is a front view thereof FIG. 4 is a rear view thereof. FIG. 5 is a left side view thereof. FIG. 6 is a right side view thereof. FIG. 7 is a top view thereof; and, FIG. 8 is a bottom view thereof. The broken lines illustrate portions of the TV antenna that form no part of the claimed design.