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Neurotherapeutic cephalosporin sulfoxide and sulfone-containing compositions

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Title: Neurotherapeutic cephalosporin sulfoxide and sulfone-containing compositions.
Abstract: The treatment of neurological disorders using cefazolin compositions and pharmaceutical compositions including oral dosage forms that include cefazolin compositions are described. ...

Browse recent Venable LLP patents - Washington, DC, US
Inventors: Gary A. Koppel, Michael O. Chaney
USPTO Applicaton #: #20110046103 - Class: 514206 (USPTO) - 02/24/11 - Class 514 
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 >1-thia-4-aza-bicyclo (3.2.0) Heptane Ring Containing (including Dehydrogenated) (e.g., Penicillins, Etc.) >3-position Substituent Contains Sulfur >7-position Substituent Contains Hetero Ring

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The Patent Description & Claims data below is from USPTO Patent Application 20110046103, Neurotherapeutic cephalosporin sulfoxide and sulfone-containing compositions.

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This invention relates to compounds and methods for neuropsychiatric intervention. More particularly, this invention is directed to pharmaceutical formulations and methods for treatment of a variety of neurological disease states using cephalosporin sulfoxides, cephalosporin sulfones, their pharmaceutically acceptable salts, and their active esters, illustratively in oral dosage form.




The pharmaceutical industry has directed extensive research and development efforts toward discovery and commercialization of drugs for treatment of neurological disorders. Such disorders typically derive from chemical imbalances in the brain. Overproduction or underproduction of pertinent neurochemical species and/or receptor dysfunction has been identified with many disease states recognized by neurologists, psychiatrists, psychologists and other medical practitioners skilled in the diagnosis and treatment of mental disease. Most of the discovery efforts for new neurologically active drugs have been based on the study of agonist/antagonist drug interactions with one or more of the numerous receptors in the brain and/or their respective receptor ligands.

The present invention provides for the use of oral dosage forms of cefazolin compounds and derivatives thereof as psychotherapeutics in the treatment of various neurological disorders.


FIGS. 1a-b show results using Δ3-cefazolin-1-sulfoxide (FIG. 1a) and Δ2-cefazolin-1-sulfoxide (FIG. 1b) in a dose-response study in the seed finding model of anxiety.

FIGS. 2a-b show results using Δ2-cefazolin-1-sulfoxide in an elevated plus-maze study. FIG. 2a shows latency to enter the closed arm, while FIG. 2b shows time in the open arm.

FIGS. 3a-d show results of testing for serenic activity in a resident/intruder model system using Δ2-cefazolin-1-sulfoxide. FIG. 3a shows latency to bite, FIG. 3b shows contact time, FIG. 3c shows number of bites, and FIG. 3d shows number of flank marks.

FIGS. 4a-b show motor activity subsequent to the resident/intruder test summarized in FIGS. 3a-d, with FIG. 4a showing open field activity and FIG. 4b showing sexual motivation.

FIG. 5 shows the number of errors demonstrating learning and memory in a radial arm maze system.

FIGS. 6a-c show levels of dopamine metabolites DOPAC (FIG. 6a) and HVA (FIG. 6b) and serotonin metabolite (FIG. 6c), all pg/15 μl, subsequent to treatment with Δ3-cefazolin-1-sulfoxide, as assessed by electrochemical detection.



The present invention and the various embodiments described and claimed herein derive, in part, from the discovery that certain carboxypeptidase E inhibitors exhibit potent neurotherapeutic activity when administered to provide effective threshold enzyme inhibitory concentrations of the same in the brain. Such inhibitors exhibit clinically significant neuroactivity evidenced in part by behavioral modification and enhanced cognition. Based on currently available test data and molecular modeling studies, it is now suggested that neurogenic carboxypeptidase E can be targeted/inhibited to provide basis for a multiplicity of neurotherapeutic effects. Carboxypeptidase E binding site models have identified certain cephalosporin sulfoxides and sulfones, illustratively Δ2- and Δ3-cefazolin sulfoxides as potential inhibitors of carboxypeptidase E. While cefazolin itself has some serenic activity, both Δ2- and Δ3-cefazolin sulfoxides have demonstrated both serenic and anxiolytic activity. Moreover, while cefazolin is known to have some antibiotic activity when administered parenterally, the cephalosporin sulfoxides and sulfones of the present invention have demonstrated both serenic and anxiolyic activity in hamsters, even when administered orally. Thus, one embodiment of this invention is the use of Δ2- and Δ3-cefazolin sulfoxides and sulfones and derivatives thereof (see Formula II below) as psychotherapeutics in the treatment of aggression, obsessive-compulsive disorder, anxiety, cognitive disorders, and the like. In one particular embodiment, the Δ2- and Δ3-cefazolin sulfoxides and derivatives thereof are provided in oral dosage forms.

Exemplary of behavioral and cognitive disorders susceptible to treatment in accordance with this invention include aggressive disorder, obsessive-compulsive disorder, anxiety, depression, schizophrenia, ADHD, and diseases evidenced by memory/learning impairment. Preliminary animal data indicate that the methods and compositions of this invention may be used in the treatment of neurotherapeutic disorders as anti-aggressive agents to control impulsivity and violence, illustratively in autism, Tourette\'s syndrome, mental retardation, psychosis, mania, senile dementia, and in the treatment of individuals with personality disorders and history of inappropriate aggression. Clinical applications extend as well, for example, to the treatment of children with ADHD and conduct disorder, as an anxiolytic, as a cognition enhancer for the geriatric population to improve learning and memory and to ameliorate disorientation. In accordance with this invention the cephalosporin sulfoxides and sulfones, illustratively oral dosage forms of Δ2- and Δ3-cefazolin sulfoxides and derivatives thereof, can be used in a multiplicity of psychotherapeutic applications.

The neurothoerapeutic cephalosporin compounds for use in preparing the oral dosage forms of this invention are generally compounds of the formulae

wherein n is 1 or 2;

R is hydrogen, an active ester forming group, or a pharmaceutically acceptable cation;

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